기니어 페퍼

Aframomum melegueta Seed Extract with Standardized Content of 6-Paradol Reduces Visceral Fat and Enhances Energy Expenditure in Overweight Adults - A Randomized Double-Blind, Placebo-Controlled Clinical Study.

1. Drug Des Devel Ther. 2022 Oct 28;16:3777-3791. doi: 10.2147/DDDT.S367350. eCollection 2022. Aframomum melegueta Seed Extract with Standardized Content of 6-Paradol Reduces Visceral Fat and Enhances Energy Expenditure in Overweight Adults - A Randomized Double-Blind, Placebo-Controlled Clinica

Grains of paradise (Aframomum melegueta) extract activates brown adipose tissue and increases whole-body energy expenditure in men.

1. Br J Nutr. 2013 Aug;110(4):733-8. doi: 10.1017/S0007114512005715. Epub 2013 Jan 11. Grains of paradise (Aframomum melegueta) extract activates brown adipose tissue and increases whole-body energy expenditure in men. Sugita J(1), Yoneshiro T, Hatano T, Aita S, Ikemoto T, Uchiwa H, Iwanaga T, Kameya T, Kawai Y, Saito M. Author information: (1)Department of Nutrition, School of Nursing and Nutrition, Tenshi Collage, Kita-13, Higashi-3, Higashi-ku, Sapporo 065-0013, Japan. Brown adipose tissue (BAT) is responsible for cold- and diet-induced thermogenesis, and thereby contributes to the control of whole-body energy expenditure (EE) and body fat content. BAT activity can be assessed by fluoro-2-deoxyglucose (FDG)-positron emission tomography (PET) in human subjects. Grains of paradise (GP, Aframomum melegueta), a species of the ginger family, contain pungent, aromatic ketones such as 6-paradol, 6-gingerol and 6-shogaol. An alcohol extract of GP seeds and 6-paradol are known to activate BAT thermogenesis in small rodents. The present study aimed to examine the effects of the GP extract on whole-body EE and to analyse its relation to BAT activity in men. A total of nineteen healthy male volunteers aged 20-32 years underwent FDG-PET after 2 h of exposure to cold at 19°C with light clothing. A total of twelve subjects showed marked FDG uptake into the adipose tissue of the supraclavicular and paraspinal regions (BAT positive). The remaining seven showed no detectable uptake (BAT negative). Within 4 weeks after the FDG-PET examination, whole-body EE was measured at 27°C before and after oral ingestion of GP extract (40 mg) in a single-blind, randomised, placebo-controlled, crossover design. The resting EE of the BAT-positive group did not differ from that of the BAT-negative group. After GP extract ingestion, the EE of the BAT-positive group increased within 2 h to a significantly greater (P<0·01) level than that of the BAT-negative group. Placebo ingestion produced no significant change in EE. These results suggest that oral ingestion of GP extract increases whole-body EE through the activation of BAT in human subjects. DOI: 10.1017/S0007114512005715 PMID: 23308394 [Indexed for MEDLINE]

Daily ingestion of grains of paradise (Aframomum melegueta) extract increases whole-body energy expenditure and decreases visceral fat in humans.

2. J Nutr Sci Vitaminol (Tokyo). 2014;60(1):22-7. doi: 10.3177/jnsv.60.22. Daily ingestion of grains of paradise (Aframomum melegueta) extract increases whole-body energy expenditure and decreases visceral fat in humans. Sugita J(1), Yoneshiro T, Sugishima Y, Ikemoto T, Uchiwa H, Suzuki I, Saito M. Author information: (1)Department of Nutrition, School of Nursing and Nutrition, Tenshi Collage. We reported previously that a single ingestion of an alcohol extract of grains of paradise (GP, Aframomum melegueta), a species of the ginger family, increases energy expenditure (EE) through the activation of brown adipose tissue, a site of sympathetically mediated metabolic theromogenesis. The present study aimed to examine a daily ingestion of GP extract on whole-body EE and body fat in humans. Whole-body EE and body fat content were measured before and after daily oral ingestion of GP extract (30 mg/d) for 4 wk in 19 non-obese female volunteers aged 20-22 y in a single-blind, randomized, placebo-controlled, crossover design. Four-week daily ingestion of GP and a placebo decreased and increased slightly the visceral fat area at the umbilicus level, respectively. The GP-induced change was significantly different from that induced by the placebo (p<0.05), and negatively correlated with the initial visceral fat area (r=-0.64, p<0.01). Neither GP nor placebo ingestion affected subcutaneous or total fat. The daily ingestion of GP, but not the placebo, increased whole-body EE (p<0.05). These results suggest that GP extract may be an effective and safe tool for reducing body fat, mainly by preventing visceral fat accumulation. DOI: 10.3177/jnsv.60.22 PMID: 24759256 [Indexed for MEDLINE]

Comparative chloroplast genome analysis and phylogenomics of Nigerian Aframomum (Zingiberaceae): insights into chloroplast genome evolution and species divergence.

1. BMC Plant Biol. 2025 Dec 20;26(1):138. doi: 10.1186/s12870-025-07966-w. Comparative chloroplast genome analysis and phylogenomics of Nigerian Aframomum (Zingiberaceae): insights into chloroplast genome evolution and species divergence. Yaradua SS(1)(2). Author information: (1)State Key Laboratory for Vegetation Structure, Functions and Construction, Ministry of Education Key Laboratory for Transboundary Ecosecurity of Southwest China, and Yunnan Key Laboratory of Plant Reproductive Adaptation and Evolutionary Ecology, Institute of Biodiversity, School of Ecology and Environmental Science, Yunnan University, Kunming, 650500, China. dryaradua@gmail.com. (2)Department of Biological Sciences, Umaru Musa Yaradua University, Katsina, Nigeria. dryaradua@gmail.com. BACKGROUND: Aframomum is a genus of ecologically and economically important plants in the Zingiberaceae family, yet its genomic evolution remains poorly understood. Previous chloroplast genome studies in the family have focused mainly on Asian genera such as Alpinia and Amomum, leaving the African lineage unexplored. METHODS: This study presents a comparative analysis of the complete chloroplast genomes of five Aframomum species, including A. alboviolaceum, A. angustifolium, A. daniellii, A. melegueta, and A. sceptrum. High-throughput Illumina sequencing was used to assemble the chloroplast genomes, which were annotated and analyzed for structural features, sequence divergence, codon usage, simple sequence repeats (SSRs), long repeats, and selection pressure on protein-coding genes. Phylogenetic relationships and divergence times were inferred using Bayesian methods implemented in MrBayes and BEAST2, respectively. RESULTS: All five chloroplast genomes exhibited a conserved quadripartite structure with genome sizes ranging from 161,101 bp to 166,130 bp, but displayed lineage-specific variation at inverted repeat/single-copy boundaries, particularly the expanded ycf1 and rps19 gene junctions in A. alboviolaceum. Comparative analyses revealed high sequence conservation, with notable divergence hotspots in non-coding regions, including ycf1-rps15, atpH-atpI, and trnT-trnL. Codon usage patterns indicated strong AT-bias, and selection analyses revealed that most genes are under purifying selection, whereas ycf1, rpoC2, and rpl16 show signals of positive selection, suggesting adaptive evolution in photosynthetic and translational functions. SSR analysis revealed predominantly A/T-rich mononucleotide repeats, with slight interspecific variation. Phylogenomic analysis strongly supported the monophyly of Aframomum and its close relationship to Amomum. Divergence time estimation indicates that Aframomum began diversifying around 26 Mya, with major radiation during the Miocene, contemporaneous with the African climatic shift that likely drove speciation. CONCLUSIONS: This study provides valuable insights into the chloroplast genome evolution and phylogeny of Aframomum, highlighting regions of high variability that are potential targets for molecular marker development. The results also reinforce the utility of chloroplast genome data in resolving evolutionary relationships and estimating divergence times within Zingiberaceae. © 2025. The Author(s). DOI: 10.1186/s12870-025-07966-w PMCID: PMC12837450 PMID: 41420201 [Indexed for MEDLINE] Conflict of interest statement: Declarations. Ethics approval and consent to participate: Not applicable. The plant materials were collected from a public land and no special permission is required for the collection of plants from a public land. Consent for publication: Not applicable. Competing interests: The authors declare no competing interests.

Dietary melegueta seed powder modulates growth, hepatic function, and biomarkers to counteract aflatoxin B₁ toxicity in broilers.

2. Mycotoxin Res. 2025 Dec 6;42(1):10. doi: 10.1007/s12550-025-00617-x. Dietary melegueta seed powder modulates growth, hepatic function, and biomarkers to counteract aflatoxin B₁ toxicity in broilers. Oloruntola OD(1), Ogunji I(2), Falowo AB(2), Adelegan GF(2), Olarotimi OJ(2), Oloruntola DA(3), Agbede JO(4). Author information: (1)Department of Animal Science, Adekunle Ajasin University, Akungba Akoko, Nigeria. olugbenga.oloruntola@aaua.edu.ng. (2)Department of Animal Science, Adekunle Ajasin University, Akungba Akoko, Nigeria. (3)Department of Medical Laboratory Science, University of Medical Sciences, Ondo, Nigeria. (4)Department of Animal Production and Health, The Federal University of Technology, Akure, Nigeria. Aframomum melegueta seed powder (AMSP) is a phytogenic supplement with notable antioxidant and anti-inflammatory properties. This study assessed its potential to protect broiler chickens against aflatoxin B₁ (AFB₁)-induced toxicity. AMSP was screened for phytochemicals and antioxidant activity. A total of 320 Cobb 500 chicks were assigned to four diets using a completely randomized design: CTRL (control), ATB1 (0.4 mg/kg AFB₁), A1AF (AFB₁ + 0.5 g/kg AMSP), and A2AF (AFB₁ + 1.0 g/kg AMSP) for six weeks. Exposure to AFB₁ by the birds in ATB1 markedly (P < 0.05) impaired growth performance, as evidenced by reduced final body weight (2,315.82 g vs. 2,743.23 g in CTRL), lower protein intake (813.45 g vs. 837.24 g), and increased feed conversion ratio (1.70 vs. 1.47). AMSP supplementation, particularly at 1.0 g/kg in A2AF, restored growth performance to control levels, while supplementation at 0.5 g/kg in A1AF achieved partial recovery. Compared with the CTRL group, AFB₁ exposure in the ATB1 birds reduced (P < 0.05) packed cell volume (29.37% vs. 35.05%) and haemoglobin concentration (9.79 g/dL vs. 11.68 g/dL), elevated (P < 0.05) ALT (24.04 vs. 16.77 IU/L), AST (70.62 vs. 57.59 IU/L), creatinine (74.85 vs. 52.43 µmol/L), TNF-α, IL-6, and corticosterone, and suppressed (P < 0.05) IL-10. These disruptions were largely normalised by AMSP, especially at 1.0 g/kg, restoring ALT, AST, creatinine, IL-10, and corticosterone to CTRL values. Histopathological analysis further confirmed that periportal inflammation and hepatic architectural damage induced by AFB₁ in ATB1 were attenuated in A1AF and absent in A2AF. In conclusion, AMSP supplementation at 1.0 g/kg effectively mitigated AFB₁-induced growth, biochemical, and hepatic impairments in broilers. These findings highlight AMSP as a promising natural feed additive for improving poultry health and ensuring feed safety, warranting further investigation into its application under commercial production conditions. © 2025. The Author(s) under exclusive licence to Society for Mycotoxin (Research Gesellschaft für Mykotoxinforschung e.V.) and Springer-Verlag GmbH Germany, part of Springer Nature. DOI: 10.1007/s12550-025-00617-x PMID: 41351642 [Indexed for MEDLINE] Conflict of interest statement: Declarations. Competing interests: The authors declare no competing interests. Conflict of interest: None. Ethical approval: The animal care and use protocol for this study was approved by the Animal Care and Use Committee, Department of Animal Science, Adekunle Ajasin University, Akungba Akoko, Nigeria (Approval No.: AAUA-ANS-AEC-2024-034).

In silico nephroprotective evaluation of microbial biotransformed metabolites from Aframomum melegueta.

3. AMB Express. 2025 Oct 22;15(1):154. doi: 10.1186/s13568-025-01962-x. In silico nephroprotective evaluation of microbial biotransformed metabolites from Aframomum melegueta. Abdou RM(1), El-Dine RS(2), Samir R(3), El-Tanbouly ND(2), El-Sayed AM(2). Author information: (1)Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, Egypt. rabab.abdo@pharma.cu.edu.eg. (2)Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, Egypt. (3)Department of Microbiology and Immunology, Faculty of Pharmacy, Cairo University, Cairo, Egypt. Microbial biotransformation of three bioactive phenolic constituents from Aframomum melegueta K. schum, namely 6-gingerol, 6-paradol and 6-shogaol, was performed by Bacillus subtilis 168, Pseudomonas aeruginosa PO1A and Candida albicans ATCC10231. Structures of the isolated compounds were determined using LC/MS analyses. To assess and compare their potential nephroprotective effects, the parent compounds and their biotransformation metabolites were subjected to molecular docking studies targeting AMP-activated protein kinase (AMPK) for the first time. During microbial biotransformation, a series of reactions, primarily hydroxylation and reduction, were observed, resulting in the identification of five distinct metabolites. LC/MS analysis of the fermentation medium revealed that Bacillus subtilis 168 converted 6-gingerol into 6-gingerdiol (M1) and hydroxylated 6-gingerol (M2), while 6-shogaol was transformed into 6-paradol (M3) and hydroxylated 6-shogaol (M4). Additionally, 6-paradol underwent further reduction to form (M5). Docking results showed that all compounds demonstrated binding affinity to AMPK, indicating potential nephroprotective activity. Notably, M1 exhibited the highest binding affinity, suggesting its strong therapeutic promise as a nephroprotective agent of natural origin. M5 ranked second in binding affinity, followed by M4. These results highlight the effectiveness of microbial transformation in generating bioactive derivatives with potentially enhanced biological activity compared to their natural precursors. SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1186/s13568-025-01962-x. DOI: 10.1186/s13568-025-01962-x PMCID: PMC12546235 PMID: 41123816 Conflict of interest statement: Declarations. Ethics approval and consent to participate: Not applicable. Consent for publication: Not applicable. Competing interests: The authors declare no competing interests.

Neuroprotective effects of dietary inclusions of alligator pepper (Aframomum melegueta) and bastard melegueta (Aframomum danielli) seeds on scopolamine-induced amnesia in rats.

4. J Complement Integr Med. 2025 Jul 3;22(3):427-437. doi: 10.1515/jcim-2024-0450. eCollection 2025 Sep 1. Neuroprotective effects of dietary inclusions of alligator pepper (Aframomum melegueta) and bastard melegueta (Aframomum danielli) seeds on scopolamine-induced amnesia in rats. Agunloye OM(1), Olawuyi EA(1), Oboh G(1). Author information: (1)Department of Biochemistry, Federal University of Technology, Akure, Nigeria. OBJECTIVES: Neurodegeneration continues to drive conditions of progressive cognitive decline from amnesia to severe dementia in different age groups. Despite, the availability of standard drugs, the need for multi-targeted interventions with no side-effects remains to be explored. Hence, this study evaluates the neuroprotective effects of Aframomum melegueta and Aframomum danielli seeds dietary inclusion on neurocognitive decline in scopolamine-administered male rats. METHODS: Seven groups of experimental rats were studied for 14 days: normal rats (group 1), untreated scopolamine-administered rats (group 2), scopolamine-administered rats treated with donepezil (group 3), scopolamine-administered rats treated with dietary inclusions of 4 and 8 % A. melegueta (groups 4 and 5 respectively), and 4 and 8 % A. danielli (groups 6 and 7 respectively). Rats were trained with Morris water maze, pre-treated with the diets, and administered (I. P) scopolamine (3 mg/kg body weight from days 12-14). Memory functionality was evaluated using the maze test and hippocampal and cortical brain regions were analyzed biochemically. RESULTS: Scopolamine administration impaired working memory, evidenced by increased escape latency and activities of neurodegenerative biomarkers in untreated rats. A. melegueta and A. danielli dietary inclusions significantly reduced escape latency, improved working memory, and restored key biomarkers, including acetylcholinesterase, butyrylcholinesterase, monoamine oxidase, and reactive oxygen species. Treated rats also exhibited elevated total thiol levels, and improved anti-inflammatory markers (IL-10). CONCLUSIONS: Both A. melegueta and A. danielli seeds showed improved neuroprotective effect in the brain of scopolamine-induced amnesia rats highlighting significant intervention against cognition. However, A. melegueta showed greater neuroprotective efficacy. © 2025 Walter de Gruyter GmbH, Berlin/Boston. DOI: 10.1515/jcim-2024-0450 PMID: 40601544 [Indexed for MEDLINE]

Potential of Aframomum melegueta and Xylopia aethiopica Against Taenia spp.: Plant-Based Remedies as Novel Anthelmintics.

5. Pharmaceuticals (Basel). 2025 May 19;18(5):749. doi: 10.3390/ph18050749. Potential of Aframomum melegueta and Xylopia aethiopica Against Taenia spp.: Plant-Based Remedies as Novel Anthelmintics. Douti FV(1), Katawa G(1), Arndts K(2)(3), Bara FD(1), Awesso ER(1), Karou SD(1), Hoerauf A(2)(3)(4), Ritter M(2)(3). Author information: (1)Unité de Recherche en Immunologie et Immuno-Modulation (UR2IM), Laboratoire de Microbiologie et de Contrôle de Qualité des Denrées Alimentaires, École Supérieure des Techniques Biologiques et Alimentaires (ESTBA), Université de Lomé, Lomé 01 BP 1515, Togo. (2)Institute for Medical Microbiology, Immunology and Parasitology (IMMIP), University Hospital Bonn (UKB), 53127 Bonn, Germany. (3)German-West African Centre for Global Health and Pandemic Prevention (G-WAC), Partner Site Bonn, 53127 Bonn, Germany. (4)German Centre for Infection Research (DZIF), Partner Site Bonn-Cologne, 53127 Bonn, Germany. Background/Objectives: Taeniasis, a zoonotic infection, is a common foodborne disease. Niclosamide and praziquantel have proven to be effective in treating it, but the use of the same drugs can lead to resistance, so alternative drugs need to be explored. This study investigated the anthelmintic potential of derived fractions from hydroethanolic extracts (HEs) of Aframomum melegueta (AM) and Xylopia aethiopica (XA), two medicinal plants known for their diverse bioactive properties. Methods: AM-HE fractions (dichloromethane fraction (DCMF), ether fraction (EF), aqueous fraction (AF)) and XA-HE fractions (chloroform fraction (CF), ether fraction (EF), and aqueous fraction (AF)) were used, and in vitro anthelmintic activity was assessed against Taenia spp. by using an adult motility assay for the worm's paralysis time determination. The parasiticidal and parasitostatic activity was also tested on Taenia spp. adult worms. Cell viability was further evaluated using propidium iodide (PI) staining, with albendazole (20 mg/mL) as the reference drug. Results: The three fractions of each plant exhibited significant, dose-dependent anthelmintic activity, with AM-HE and XA-CF showing the greatest effects at 20 mg/mL. AM-EF demonstrated significant activity at 0.4% and 0.8%. Irreversibility tests revealed that most of the treated worms remained paralysis, except those exposed to the AF of both plants. PI staining confirmed the dose-dependent mortality of Taenia cells treated with HE, DCMF, and AF of AM. Conclusions: These results underscore the potential of AM and XA extracts and fractions as alternative treatments for helminth infections. Further, in vivo studies are warranted to confirm their safety and therapeutic efficacy. DOI: 10.3390/ph18050749 PMCID: PMC12115246 PMID: 40430566 Conflict of interest statement: The authors declare that this research was conducted in the absence of any commercial or financial relationships that could be construed as potential conflicts of interest.

Aframomum melegueta Seed Extract's Effects on Anxiety, Stress, Mood, and Sleep: A Randomized, Double-Blind, Pilot Clinical Trial.

6. Pharmaceuticals (Basel). 2025 Feb 19;18(2):278. doi: 10.3390/ph18020278. Aframomum melegueta Seed Extract's Effects on Anxiety, Stress, Mood, and Sleep: A Randomized, Double-Blind, Pilot Clinical Trial. Pérez-Machín R(1), Vega-Morales T(1), Elvira-Aranda C(2)(3), Lledó-Rico L(2), Gomis-Gomis MJ(2)(3), López-Ríos L(1). Author information: (1)Nektium Pharma S.L., C/Las Mimosas 8, Polígono Industrial Arinaga, 35118 Las Palmas, Spain. (2)Kinetic Performance S.L., Scientific Park of Alicante, 03690 Alicante, Spain. (3)Research Group on Physical Activity Sciences and Sport, Education School, University of Alicante, 03690 Alicante, Spain. Background and aims:Aframomum melegueta (A. melegueta) from the ginger family is appreciated for its pungent seeds widely used in African ethno-medicine. Among the several biological activities associated with the seed's preparations, some preclinical studies suggest a set of neuroactive properties that have not been tested in humans to date. We performed a clinical trial to investigate the effects of A. melegueta seed extracts on anxiety, stress, mood, and sleep in healthy subjects with moderate anxiety levels. In vitro pharmacological assays targeting the endocannabinoid, serotoninergic, and GABAergic systems were conducted to elucidate the underlying mechanism of action. Methods:A. melegueta standardized to 10% total vanilloids (primarily 6-gingerol, 6-shogaol, and 6-paradol) was obtained after hydroalcoholic extraction and the spray-drying microencapsulation process. Subjects consumed 50, 100, or 150 mg of the extract daily for two days. A set of validated psychometric test questionnaires was collected before and 48 h after the first intake. A. melegueta extract interaction with canonical endocannabinoid receptors (hCB1R and hCB2R), the serotonin receptor (5HT1AR) and gamma-aminobutyric acid receptor (GABAA1R) was evaluated by the radioligand binding assay. Additionally, receptor functional assays and enzyme inhibition assays were conducted to test the extract's functional activity on the non-canonical endocannabinoid receptor (TRPV1) and the cannabinoid fatty-acid amide hydrolase enzyme (FAAH), respectively. Results: In vitro pharmacological tests showed that the A. melegueta extract activated TRPV1, modulated both hCB2R and 5HT1AR and inhibited FAAH, which is the enzyme primarily responsible for hydrolyzing endogenous anandamide. After a 48 h intake period, the extract significantly reduced anxiety and tension related to stress, improved overall mood, and enhanced sleep quality in the participants at doses ranging from 50 to 150 mg, with no reported side effects. Conclusions: This study supports the potential of the A. melegueta extract for anxiety reduction, mood improvement, stress mitigation, and sleep enhancement. The in vitro tests suggest that the extract's primary mechanism of action may involve the inhibition of FAAH, which is a key target in anxiety management. DOI: 10.3390/ph18020278 PMCID: PMC11859572 PMID: 40006090 Conflict of interest statement: R.P.-M., L.L.-R. (Laura López-Ríos) and T.V.-M. are employees of the private company Nektium Pharma, which researches, develops, and commercializes botanical ingredients for the nutraceutical market. The A. melegueta hydro-alcoholic extract tested in this study is commercialized by Nektium Pharma under the trademark Vanizem®. C.E.-A., L.L.-R. (Loreto Lledó-Rico) and M.J.G.-G. are employees of Kinetic Performance SL, a spinoff company from Alicante University that provides research and development services, and which was financed by Nektium Pharma to conduct the human clinical trial included in the present publication. C.E.-A., L.L.-R. (Loreto Lledó-Rico) and M.J.G.-G. declare that they have no competing interests.

Inclusion of antimicrobial and antioxidant spices into milk candy towards enhancement of nutrient contents and bio-functional activities.

7. Heliyon. 2025 Jan 27;11(3):e42249. doi: 10.1016/j.heliyon.2025.e42249. eCollection 2025 Feb 15. Inclusion of antimicrobial and antioxidant spices into milk candy towards enhancement of nutrient contents and bio-functional activities. Faturoti AO(1), Ogidi CO(1). Author information: (1)Department of Food Science and Technology, Olusegun Agagu University of Science and Technology, PMB 353 Okitipupa, Nigeria. Herbs and spices are known for their health benefits and thus, commonly used in foods to enhance taste, flavour and shelf life. This study produced milk candy with medicinal spices, assessed their proximate composition, prebiotic, and antioxidant activities using standard methods. Phenol contents of extracts from Aframomum melegueta (25.40 mg/100g) and Ocimum gratissimum (24.80 mg/100g) were not significantly different (p ≥ 0.05). Extracts from Ocimum gratissimum (5.50 mg/100g), Piper guineense (5.50 mg/100g), Cinnamomum burmannii (5.10 mg/100g), and Trigonella foenum-graecum (5.20 mg/100g) have similar (p ≥ 0.05) terpenoid content. Zones of inhibition displayed by the spices against indicator microorganisms ranged from 5.20 mm to 10.30 mm with MIC values of 50-200 μg/mL. Extracts from Ocimum gratissimum, Aframomum melegueta, and Xylopia aethiopica scavenged 1, 1-diphenyl-2-picrylhydrazyl (DPPH) with similar (p ≥ 0.05) values of 90.6 %, 91.5 %, and 92.5 %, respectively. The crude fibre of milk candy with spices increased from 6.90 to 8.10 % when compared (p ≥ 0.05) to milk candy without spices (3.90 %). Milk candies with Xylopia aethiopica and Zingiber officinale have the same scavenging activity of 65.80 % against DPPH. Milk candy fortified with Cuminum cyminum supported the growth of probiotics; Lactobacillus fermentum with the highest values of 8.30 × 105 cfu/mL and 6.90 × 105 cfu/mL for Lactobacillus acidophilus. Addition of spices to milk candy gain wide acceptance by consumers due to savory. Medicinal herbs and spices can be successfully incorporated into milk products to enhance their bio-functional potentials, and to alleviate the intolerance of individual that are allergic to dairy products. © 2025 Published by Elsevier Ltd. DOI: 10.1016/j.heliyon.2025.e42249 PMCID: PMC11830343 PMID: 39959487 Conflict of interest statement: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Investigation of Aframomum melegueta compounds as ERK5 inhibitor related to breast cancer via molecular docking and dynamic simulation.

8. In Silico Pharmacol. 2025 Jan 25;13(1):18. doi: 10.1007/s40203-025-00304-w. eCollection 2025. Investigation of Aframomum melegueta compounds as ERK5 inhibitor related to breast cancer via molecular docking and dynamic simulation. Ottu PO(1), Babalola OO(1), Oluwamodupe C(1)(2), Oluwatobiloba AF(1), Kehinde IO(1), Akinola OA(1)(3), Ibrahim SO(4), Elekofehinti OO(1)(3). Author information: (1)Teady Bioscience Research Laboratory, Ilara Mokin, Ondo State Nigeria. (2)Phytomedicine, Molecular Biology and Bioinformatics lab, Department of Chemical Science (Biochemistry program), Olusegun Agagu University of Science and Technology, Okitipupa, Ondo State Nigeria. (3)Bioinformatics and Molecular Biology Lab, Department of Biochemistry, Federal University of Technology Akure, Akure, Ondo State Nigeria. (4)Department of Industrial Chemistry, University of Ilorin, Ilorin, Kwara State Nigeria. Breast cancer remains a global health challenge, with rising cases predicted in the coming decades. The complexity of breast cancer treatment arises from its complex nature, often involving multiple therapeutic strategies. One promising approach is targeting the ERK5 pathway, a key regulator in cancer cell proliferation and survival. In this study, we explored the anticancer potential of bioactive compounds from Aframomum melegueta, a plant traditionally used in West African medicine. The 3D structure of ERK5 (PDB ID: 4B99) was prepared and optimized using the Schrödinger Protein Preparation Wizard. Six phytochemicals from Aframomum melegueta were screened for their binding affinities to ERK5 using GlideXP docking. Dihydrogingerenone A,1-(3,4-dihydroxy-5-methoxyphenyl)-7-(3,4-dihydroxyphenyl) heptane-3,5-diyldiacetate and Dihydrogingerenone C emerged as the lead compound, demonstrating a high docking score of -  9.659 kcal/mol, -  9.383 kcal/mol, and - 8.264 kcal/mol compared to standard anticancer drugs like Docetaxel (- 4.175 kcal/mol) and Temozolomide (- 5.443 kcal/mol). Post-docking analyses using MM-GBSA free energy calculations confirmed the compound's high binding stability, with van der Waals interactions and hydrogen bonding at critical residues such as Met140 playing a significant role. Pharmacokinetic profiling using ADME analysis showed that our compounds exhibited favorable drug-likeness properties, adhering to Lipinski's Rule of Five without violations. QSAR modeling and molecular dynamics (MD) simulations further validated its pharmacological potential. These findings suggest that Aframomum melegueta contains bioactive compounds with strong potential as ERK5 inhibitors, offering a novel approach to breast cancer treatment. GRAPHICAL ABSTRACT: The molecular docking study of Dihydrogingerenone A, 1-(3, 4-dihydroxy-5-methoxyphenyl)-7-(3, 4-dihydroxyphenyl) heptane-3, 5-diyldiacetate, and Dihydrogingerenone C from Aframomum melegueta as effective breast cancer treatment. © The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature 2025. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law. DOI: 10.1007/s40203-025-00304-w PMCID: PMC11762040 PMID: 39872469 Conflict of interest statement: Conflict of interestsThe authors declare no competing interests.

Machine Learning-Driven Discovery of Structurally Related Natural Products as Activators of the Cardiac Calcium Pump SERCA2a.

9. ChemMedChem. 2025 May 5;20(9):e202400913. doi: 10.1002/cmdc.202400913. Epub 2025 Feb 6. Machine Learning-Driven Discovery of Structurally Related Natural Products as Activators of the Cardiac Calcium Pump SERCA2a. Cruz-Cortés C(1), Fernández-de Gortari E(2)(3), Aguayo-Ortiz R(4), Šeflová J(5), Ard A(6)(7), Clasby M(6)(7), Anumonwo J(1), Michel Espinoza-Fonseca L(1). Author information: (1)Center for Arrhythmia Research, Department of Internal Medicine, Division of Cardiovascular Medicine, University of Michigan, Ann Arbor, MI-48109, USA. (2)International Iberian Nanotechnology Laboratory, Braga, 4715-330, Portugal. (3)Euskal Oxcitas Biotek SL, Calle Lutxana 11 - DCHA, 48008, Bilbao, Spain. (4)Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, Mexico City, 04510, Mexico. (5)Department of Cell and Molecular Physiology, Loyola University Chicago, Maywood, IL-60153, USA. (6)College of Pharmacy, University of Michigan, Ann Arbor, MI-48109, USA. (7)Vahlteich Medicinal Chemistry Core, University of Michigan, Ann Arbor, MI-48109, USA. A key molecular dysfunction in heart failure is the reduced activity of the cardiac sarcoplasmic reticulum Ca2+-ATPase (SERCA2a) in cardiac muscle cells. Reactivating SERCA2a improves cardiac function in heart failure models, making it a validated target and an attractive therapeutic approach for heart failure therapy. However, finding small-molecule SERCA2a activators is challenging. In this study, we used a machine learning-based virtual screening to identify SERCA2a activators among 57,423 natural products. The machine learning model identified ten structurally related natural products from Zingiber officinale, Aframomum melegueta, Alpinia officinarum, Alpinia oxyphylla, and Capsicum (chili peppers) as SERCA2a activators. Initial ATPase assays showed seven of these activate SERCA at low micromolar concentrations. Notably, two natural products, Yakuchinone A and Alpinoid D displayed robust concentration-dependent responses in primary ATPase activity assays, efficient lipid bilayer binding and permeation in atomistic simulations, and enhanced intracellular Ca2+ transport in adult mouse cardiac cells. While these natural products exert off-target effects on Ca2+ signaling, these compounds offer promising avenues for the design and optimization of lead compounds. In conclusion, this study increases the array of calcium pump effectors and provides new scaffolds for the development of novel SERCA2a activators as new therapies for heart failure. © 2025 The Authors. ChemMedChem published by Wiley-VCH GmbH. DOI: 10.1002/cmdc.202400913 PMCID: PMC12058239 PMID: 39853697 [Indexed for MEDLINE] Conflict of interest statement: The authors declare no competing financial interests.

Deciphering phosphodiesterase-5 inhibitors from Aframemum melegueta: computational models against erectile dysfunction.

10. In Silico Pharmacol. 2024 Nov 9;12(2):101. doi: 10.1007/s40203-024-00284-3. eCollection 2024. Deciphering phosphodiesterase-5 inhibitors from Aframemum melegueta: computational models against erectile dysfunction. Omoboyowa DA(1). Author information: (1)Phyto-medicine and Computational Biology Lab, Department of Biochemistry, Adekunle Ajasin University, Akungba-Akoko, Ondo State Nigeria. Insufficient and inability to maintain erection in male for satisfactory sexual performance remains global challenge among couples. The identification of phosphodiesterase-5 (PDE-5) antagonist in the pathogenesis of erectile dysfunction has improved the search for therapeutic agents for the management of this sexual dysfunction. Here in, bioactive compounds from Aframomum melegueta were virtually screened against PDE-5 using Schrodinger suite 2017-1 as computational tool. The lead compound was further validated in comparison with sildenafil by performing 100 ns molecular dynamics (MD) simulation using Desmond. Among 109 bioactive compounds screened, nine (9) molecules were predicted as potent inhibitors of PDE-5 with binding affinities comparable to the co-crystalized ligand (sildenafil). 1,7-bis(3,4-dihyroxy-5-methoxyphenyl)heptane-3,5-diyldiacetate was observed to have the best docking score (-11.522 kcal/mol) among the hit compounds which is very close to the co-crystalized ligand (-11.872 kcal/mol). Validation using pharmacophore hypothesis and QSAR modeling further confirmed the prediction of the hit compounds with fitness score ranging from 0.754 to 2.605 and predicted pIC50 of 3.835 to 7.976 µM. All the hit compounds obeyed Lipinski's rule of five and within the reference range of the pharmacokinetics parameters. The MD simulation result predicted the stability of 1,7-bis(3,4-dihydroxy-5-methoxyphenyl)heptane-3,5-diyldiacetate-PDE-5 complex comparable to the sildenafil-PDE-5 complex. The outcome of this study predicted nine molecules from A. melegueta as potent PDE-5 antagonists which required isolation and experimental validation for the management of erectile dysfunction. SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1007/s40203-024-00284-3. © The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature 2024. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law. DOI: 10.1007/s40203-024-00284-3 PMCID: PMC11549073 PMID: 39524458 Conflict of interest statement: Conflict of interestThe authors declare no conflict of interest.

Aframomum Melegueta: Evaluation of Chronic Toxicity, HPLC Profiling, and In Vitro/In Vivo Antioxidant Assessment of Seeds Extracts.

11. Chem Biodivers. 2025 Jan;22(1):e202400942. doi: 10.1002/cbdv.202400942. Epub 2024 Oct 31. Aframomum Melegueta: Evaluation of Chronic Toxicity, HPLC Profiling, and In Vitro/In Vivo Antioxidant Assessment of Seeds Extracts. Mounia L(1), Ismail E(1), Othman EF(1), Hicham W(1), Rajaa E(1), El Mostafa M(1), Mounia O(1), Samira R(1)(2). Author information: (1)Immunology and Biodiversity Laboratory, Faculty of Sciences Ain Chock, Hassan II University, Casablanca, Morocco. (2)Department of Biology, Faculty of Sciences Ben M'Sick, Hassan II University, Casablanca, Morocco. Aframomum melegueta, commonly known as grains of paradise, is a medicinal plant celebrated for its rich phytochemical content and therapeutic properties. This study evaluated the antioxidant and cytotoxic potentials of its ethanolic and methanolic extracts, both in vitro and in vivo, while also analyzing their chemical profiles. HPLC analysis identified key compounds, including gallic acid, caffeic acid, caffeine, coumarin, rutin, catechin, ferulic acid, and quercetin. Chronic toxicity assessments confirmed the safety of the extracts, with no adverse effects on animal health, particularly in liver histopathology. Cytotoxicity results indicated reduced splenocyte viability at the highest concentrations. The extracts exhibited significant antioxidant activity in DPPH•, FRP, and phosphomolybdate assays, demonstrating their effectiveness as antiradical agents. In vivo antioxidant results showed a reduction in lipid peroxidation levels in serum and liver, highlighting the extracts' ability to mitigate oxidative stress. Additionally, the extracts provided protection against H2O2-induced erythrocyte hemolysis and modulated NO production in peritoneal macrophages. These findings underscore the therapeutic potential of A. melegueta extracts, suggesting their promise in developing preventive strategies for oxidative stress-related chronic diseases. © 2024 Wiley-VHCA AG, Zurich, Switzerland. DOI: 10.1002/cbdv.202400942 PMID: 39271457 [Indexed for MEDLINE]

Light-emitting diode irradiation at 590 nm combined with active substances modulates ultraviolet B radiation-induced keratinocyte inflammation.

12. Lasers Med Sci. 2024 Sep 3;39(1):231. doi: 10.1007/s10103-024-04178-w. Light-emitting diode irradiation at 590 nm combined with active substances modulates ultraviolet B radiation-induced keratinocyte inflammation. Qin Y(1), Jiang B(2)(3), Yuan C(1), Cui L(4), Lu M(5), Zheng X(5), Yu M(5). Author information: (1)Flossom Research Laboratories, 2601 Yingfeng Center, 3378 Binhai Avenue, Yuehai Street, Shenzhen, Guangdong, China. (2)Flossom Research Laboratories, 2601 Yingfeng Center, 3378 Binhai Avenue, Yuehai Street, Shenzhen, Guangdong, China. dr.j@flossom.com. (3)Shenzhen Rawskin Dermatology, Shenzhen, China. dr.j@flossom.com. (4), 22/F, Yingfeng Business Center, No.8 Yixing Road, Junlan Community, Beijiao Town, Shunde District, Foshan City, Guangdong, China. (5), 702, Building B, Hongqiao International Business Plaza, 2679 Hechuan Road, Minhang District, Shanghai, China. To evaluate the efficacy of yellow light-emitting diode (LED) irradiation at 590 nm, alone or in combination with anti-inflammatory active substances against ultraviolet (UV)-induced inflammation in keratinocytes. HaCaT keratinocytes were pretreated with LED yellow light (590 nm) alone or in combination with an antiinflammatory active substance such as glycerophosphoinositol choline (GC), extract of grains of paradise (Aframomum melegueta Schum, AM), or a bisabolol and ginger root extract mixture (Bb-GE) before UVB irradiation. Following each treatment, we measured the levels of inflammatory mediators secreted by keratinocytes. HaCaT keratinocytes treated with UVB (300 mJ cm-²) and then cultured for 24 h exhibited significantly upregulated expression of proinflammatory factors, including interleukin (IL)-1α, prostaglandin E2 (PGE2), and IL-8. After pretreatment with 590 nm LED, UVB-induced inflammatory responses were significantly inhibited. Co-pretreatment with 590 nm LED irradiation and GC further inhibited the expression of IL-1α and IL-8. IL-8 expression was inhibited by co-pretreatment with 590 nm LED irradiation and AM, whereas PGE2 expression was inhibited by co-pretreatment with 590 nm LED irradiation and Bb-GE. Co-treatment with 590 nm LED irradiation and various active substances modulated UVB-induced inflammation in keratinocytes, suggesting the potential application of this approach to prevent damage caused by voluntary sun exposure in daily life. © 2024. The Author(s), under exclusive licence to Springer-Verlag London Ltd., part of Springer Nature. DOI: 10.1007/s10103-024-04178-w PMID: 39223344 [Indexed for MEDLINE]

Phytochemical analysis and immunomodulatory activities in vitro and in vivo of Aframomum melegueta K Schum seed extracts.

13. Inflammopharmacology. 2024 Apr;32(2):1621-1631. doi: 10.1007/s10787-023-01422-7. Epub 2024 Feb 6. Phytochemical analysis and immunomodulatory activities in vitro and in vivo of Aframomum melegueta K Schum seed extracts. Latif M(1), Elkoraichi I(1), El Faqer O(1), Wahnou H(1), Mtairag EM(1), Oudghiri M(1), Rais S(2)(3). Author information: (1)Immunology and Biodiversity Laboratory, Faculty of Sciences Ain Chock, Hassan II University, Casablanca, Morocco. (2)Immunology and Biodiversity Laboratory, Faculty of Sciences Ain Chock, Hassan II University, Casablanca, Morocco. samirarais03@gmail.com. (3)Department of Biology, Faculty of Sciences Ben M'Sick, Hassan II University, Casablanca, Morocco. samirarais03@gmail.com. Aframomum melegueta K Schum (A. melegueta), an herbaceous plant renowned for its medicinal seeds, was investigated for its potential immunomodulatory effects in vitro and in vivo using ethanolic and methanolic extracts. The immunomodulatory effect was evaluated by measuring antibody titers using the agglutination technique, while anti-inflammatory activity was assessed in a carrageenan-induced mouse paw edema model. In vitro immunomodulatory activity was measured by lysozyme release from neutrophils. Additionally, white blood cell counts were analyzed post-extracts treatment. The MTT assay was employed to determine cytotoxicity, and the biochemical parameters of liver toxicity were evaluated. Remarkably, both extracts exhibited a dose-dependent reduction in paw edema (p < 0.001), with the most significant reduction observed at 1 g/kg (78.13 and 74.27% for ethanolic and methanolic extracts, respectively). Neutrophil degranulation was significantly inhibited in a dose-dependent manner (p < 0.003), reaching maximal inhibition at 100 μg/mg (60.78 and 39.7% for ethanolic and methanolic extracts, respectively). In comparison to the control group, both antibody production and white blood cell counts were reduced. Neither of the extracts showcased any cytotoxicity or toxicity. These findings suggest that A. melegueta extracts exhibit immunosuppressive and anti-inflammatory activities due to the presence of various biomolecules. © 2024. The Author(s), under exclusive licence to Springer Nature Switzerland AG. DOI: 10.1007/s10787-023-01422-7 PMID: 38319475 [Indexed for MEDLINE]

Antimicrobial and anti-virulence activities of 4-shogaol from grains of paradise against gram-negative bacteria: Integration of experimental and computational methods.

14. J Ethnopharmacol. 2024 Apr 6;323:117611. doi: 10.1016/j.jep.2023.117611. Epub 2023 Dec 27. Antimicrobial and anti-virulence activities of 4-shogaol from grains of paradise against gram-negative bacteria: Integration of experimental and computational methods. Koshak AE(1), Okairy HM(1), Elfaky MA(2), Abdallah HM(3), Mohamed GA(1), Ibrahim SRM(4), Alzain AA(5), Abulfaraj M(6), Hegazy WAH(7), Nazeih SI(8). Author information: (1)Department of Natural Products and Alternative Medicine, King Abdulaziz University, Jeddah, 21589, Saudi Arabia. (2)Department of Natural Products and Alternative Medicine, King Abdulaziz University, Jeddah, 21589, Saudi Arabia; Centre for Artificial Intelligence in Precision Medicines, King Abdulaziz University, Jeddah, 21589, Saudi Arabia. (3)Department of Natural Products and Alternative Medicine, King Abdulaziz University, Jeddah, 21589, Saudi Arabia. Electronic address: hmafifi@kau.edu.sa. (4)Preparatory Year Program, Department of Chemistry, Batterjee Medical College, Jeddah, 21442, Saudi Arabia; Department of Pharmacognosy, Assiut University, Assiut, 71526, Egypt. (5)Department of Pharmaceutical Chemistry, University of Gezira, Wad Madani, 21111, Sudan. (6)Department of Surgery, King Abdulaziz University, Jeddah, 21589, Saudi Arabia. (7)Department of Microbiology and Immunology, Zagazig University, Zagazig, 44519, Egypt; Pharmacy Program, Department of Pharmaceutical Sciences, Oman College of Health Sciences, Muscat, 113, Oman. (8)Department of Microbiology and Immunology, Zagazig University, Zagazig, 44519, Egypt. ETHNOPHARMACOLOGICAL RELEVANCE: Bacterial resistance to antibiotics is a growing global concern, highlighting the urgent need for new antimicrobial candidates. Aframomum melegueta was traditionally used for combating urinary tract and soft tissue infections, which implies its potential as an antimicrobial agent. AIM OF STUDY: This study was designed to explore the antibacterial and anti-virulence capabilities of 4-shogaol isolated from A. melegueta seeds versus gram-negative bacteria: Serratia marcescens, Klebsiella pneumoniae, Acinetobacter baumannii, and the clinically important pathogen Pseudomonas aeruginosa. MATERIALS AND METHODS: 4-Shogeol was isolated from A. melegueta seeds and its MICs were determined for Acinetobacter baumannii (ATCC-17978), Pseudomonas aeruginosa (ATCC-27853), Klebsiella pneumoniae (ATCC-700603), and Serratia marcescens clinical isolate. The anti-efflux activity and effect on the bacterial cell membrane for the compound were evaluated. Furthermore, the anti-virulence activities of the compound were evaluated. The effects of 4-shogeol at sub-MIC on bacterial motility, biofilm formation, and production of virulent enzymes and pigments were assessed. The anti-quorum sensing activities of 4-shogeol were evaluated virtually and by quantification its effect on the expression of quorum sensing encoding genes. The in vivo protection assay was conducted to evaluate the effect of 4-shogaol on the P. aeruginosa capacity to induce pathogenesis in mice. Finally, the effect of shogaol-antibiotics combination was assessed. RESULTS: The research revealed that 4-shogaol's antibacterial action primarily involves disrupting the bacterial cell membrane and efflux pumps. It also exhibited significant anti-virulence effects by reducing biofilm development and repressing virulence factors production, effectively protecting mice against P. aeruginosa infection. Furthermore, when combined with antibiotics, 4-shogaol demonstrated synergistic effects, leading to reduced minimum inhibitory concentrations (MICs) against P. aeruginosa. Its anti-virulence properties were linked to its ability to disrupt bacterial quorum sensing (QS) mechanisms, as evidenced by its interaction with QS receptors and downregulation of QS-related genes. Notably, in silico analysis indicated that 4-shogaol exhibited strong binding affinity to different P. aeruginosa QS targets. CONCLUSION: These findings suggest that 4-shogaol holds promise as an effective anti-virulence agent that can be utilized in combination with antibiotics for treating severe infections caused by gram-positive bacteria. Copyright © 2023 Elsevier B.V. All rights reserved. DOI: 10.1016/j.jep.2023.117611 PMID: 38158095 [Indexed for MEDLINE] Conflict of interest statement: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Phytochemical profiling and anthelmintic potential of extracts of selected tropical plants on parasites of fishes in Epe Lagoon.

15. Sci Rep. 2023 Dec 20;13(1):22727. doi: 10.1038/s41598-023-48164-8. Phytochemical profiling and anthelmintic potential of extracts of selected tropical plants on parasites of fishes in Epe Lagoon. Ukwa UD(1), Saliu JK(2), Akinsanya B(3). Author information: (1)Department of Zoology, Eco-Toxicology Unit, University of Lagos, Akoka, Lagos, Nigeria. ukwadavid@gmail.com. (2)Department of Zoology, Eco-Toxicology Unit, University of Lagos, Akoka, Lagos, Nigeria. (3)Department of Zoology, Environmental Parasitology Unit, University of Lagos, Akoka, Lagos, Nigeria. This research aims to study the anthelmintic properties of selected five (5) tropical plant extracts, ascertained margin of fish host safety in reference with praziquantel, a commonly used chemo-therapeutics. Qualitative and quantitative analysis of Alligator pepper seeds (Aframomum melegueta), Moringa leaves (Moringa oleifera), Neem leaves (Azadirachta indica), Ginger bulbs (Zingiber officinale) and Garlic (Allium sativum) and their potencies in reference to praziquantel against Clarias gariepinus and different classes of helminth parasites were investigated. The results obtained show that the 70% ethanol extract had 80 to 100% presence of the phytochemical content, compared with the 100% aqueous and 100% ethanol extracts with 50 to 80% and 50 to 90%, respectively. Among the five tropical plants, the richest in saponin and flavonoids are alligator pepper and neem with alkaloids, tannin, flavonoid and saponin in ratios 1:1:3:9 and 1:1:4:3 respectively. While, moringa, garlic and ginger are rich in alkaloids with alkaloids, tannin, flavonoid and saponin in ratios, 8:1:10:1, 6:2:1:4 and 6:3:2:1, respectively. Aframomum melegueta and praziquantel showed above 70% potency (at 96 h LC5) against all the classes of parasites; Wenyonia spp (cestode), Procamallanus spp (nematode), Tenuisentis spp (acanthocephalan), and Electrotaenia sp (cestode) as compared to the other plant extracts that showed above 70% potency (at 96 h LC5) only against Electrotaenia spp. Sub-lethal Concentrations (96 h LC5) of praziquantel and Aframomum melegueta on the juvenile fish host (12.36 mg/l and 9.9 mg/l respectively) were found to be 90.9% and 93.5% effective against adult Electrotaenia spp after 8 to 10 min of exposure. These concentrations were 78 to 85.7% and 89.7 to 88.4%, respectively, effective against the other classes of parasites after 18 to 25 min and 15 to 21 min of exposure. These concentrations were tested on the post juvenile of the fish to determine behavioral changes; there were no significant behavioral responses after 24 h of exposure. The effective concentrations indicate the widest margin of safety for the fish host. © 2023. The Author(s). DOI: 10.1038/s41598-023-48164-8 PMCID: PMC10733343 PMID: 38123590 [Indexed for MEDLINE] Conflict of interest statement: The authors declare no competing interests.

Bio-Guided Isolation of SARS-CoV-2 Main Protease Inhibitors from Medicinal Plants: In Vitro Assay and Molecular Dynamics.

16. Plants (Basel). 2022 Jul 24;11(15):1914. doi: 10.3390/plants11151914. Bio-Guided Isolation of SARS-CoV-2 Main Protease Inhibitors from Medicinal Plants: In Vitro Assay and Molecular Dynamics. Abdallah HM(1), El-Halawany AM(2), Darwish KM(3), Algandaby MM(4), Mohamed GA(1), Ibrahim SRM(5)(6), Koshak AE(1), Elhady SS(1), Fadil SA(1), Alqarni AA(1), Abdel-Naim AB(7), Elfaky MA(1). Author information: (1)Department of Natural Products and Alternative Medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia. (2)Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt. (3)Department of Medicinal Chemistry, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, Egypt. (4)Department of Biological Sciences, Faculty of Science, King Abdulaziz University, Jeddah 21589, Saudi Arabia. (5)Preparatory Year Program, Department of Chemistry, Batterjee Medical College, Jeddah 21442, Saudi Arabia. (6)Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt. (7)Department of Pharmacology and Toxicology, King Abdulaziz University, Jeddah 21589, Saudi Arabia. Since the emergence of the pandemic of the coronavirus disease (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the discovery of antiviral phytoconstituents from medicinal plants against SARS-CoV-2 has been comprehensively researched. In this study, thirty-three plants belonging to seventeen different families used traditionally in Saudi Arabia were tested in vitro for their ability to inhibit the SARS-CoV-2 main protease (MPRO). Major constituents of the bio-active extracts were isolated and tested for their inhibition potential against this enzyme; in addition, their antiviral activity against the SARS-CoV-2 Egyptian strain was assessed. Further, the thermodynamic stability of the best active compounds was studied through focused comparative insights for the active metabolites regarding ligand-target binding characteristics at the molecular level. Additionally, the obtained computational findings provided useful directions for future drug optimization and development. The results revealed that Psiadia punctulata, Aframomum melegueta, and Nigella sativa extracts showed a high percentage of inhibition of 66.4, 58.7, and 31.5%, against SARS-CoV-2 MPRO, respectively. The major isolated constituents of these plants were identified as gardenins A and B (from P. punctulata), 6-gingerol and 6-paradol (from A. melegueta), and thymoquinone (from N. sativa). These compounds are the first to be tested invitro against SARS-CoV-2 MPRO. Among the isolated compounds, only thymoquinone (THY), gardenin A (GDA), 6-gingerol (GNG), and 6-paradol (PAD) inhibited the SARS-CoV-2 MPRO enzyme with inhibition percentages of 63.21, 73.80, 65.2, and 71.8%, respectively. In vitro assessment of SARS-CoV-2 (hCoV-19/Egypt/NRC-03/2020 (accession number on GSAID: EPI_ISL_430820) revealed a strong-to-low antiviral activity of the isolated compounds. THY showed relatively high cytotoxicity and was anti-SARS-CoV-2, while PAD demonstrated a cytotoxic effect on the tested VERO cells with a selectivity index of CC50/IC50 = 1.33 and CC50/IC50 = 0.6, respectively. Moreover, GNG had moderate activity at non-cytotoxic concentrations in vitro with a selectivity index of CC50/IC50 = 101.3/43.45 = 2.3. Meanwhile, GDA showed weak activity with a selectivity index of CC50/IC50 = 246.5/83.77 = 2.9. The thermodynamic stability of top-active compounds revealed preferential stability and SARS-CoV-2 MPRO binding affinity for PAD through molecular-docking-coupled molecular dynamics simulation. The obtained results suggest the treating potential of these plants and/or their active metabolites for COVID-19. However, further in-vivo and clinical investigations are required to establish the potential preventive and treatment effectiveness of these plants and/or their bio-active compounds in COVID-19. DOI: 10.3390/plants11151914 PMCID: PMC9332707 PMID: 35893619 Conflict of interest statement: The authors declare no conflict of interest.

Anti-Th17 and anti-Th2 responses effects of hydro-ethanolic extracts of Aframomum melegueta, Khaya senegalensis and Xylopia aethiopica in hyperreactive onchocerciasis individuals' peripheral blood mononuclear cells.

17. PLoS Negl Trop Dis. 2022 Apr 25;16(4):e0010341. doi: 10.1371/journal.pntd.0010341. eCollection 2022 Apr. Anti-Th17 and anti-Th2 responses effects of hydro-ethanolic extracts of Aframomum melegueta, Khaya senegalensis and Xylopia aethiopica in hyperreactive onchocerciasis individuals' peripheral blood mononuclear cells. Katawa G(1), Ataba E(1), Ritter M(2), Amessoudji OM(1), Awesso ER(1), Tchadié PE(1), Bara FD(1), Douti FV(1), Arndts K(2), Tchacondo T(1), Batawila K(3), Ameyapoh Y(1), Hoerauf A(2)(4)(5), Karou SD(1), Layland LE(2)(4). Author information: (1)Unité de Recherche en Immunologie et Immunomodulation (UR2IM)/Laboratoire de Microbiologie et de Contrôle de Qualité des Denrées Alimentaires (LAMICODA)/Ecole Supérieure des Techniques Biologiques et Alimentaires (ESTBA), Université de Lomé, Lomé, Togo. (2)Institute for Medical Microbiology, Immunology and Parasitology (IMMIP), University Hospital Bonn (UKB), Bonn, Germany. (3)Laboratoire de Biologie et Écologie Végétale, Faculté des Sciences (FDS), Université de Lomé, Lomé, Togo. (4)German Center for Infection Research (DZIF), partner site Bonn-Cologne, Bonn, Germany. (5)German-West African Centre for Global Health and Pandemic Prevention (G-WAC), Partner Site Bonn, Bonn, Germany. Hyperreactive onchocerciasis (HO) is characterized by a severe skin inflammation with elevated Th17-Th2 combined responses. We previously demonstrated the anthelminthic activity of Aframomum melegueta (AM), Xylopia aethiopica (XA) and Khaya senegalensis (KS) used by traditional healers to treat helminthiasis in the endemic area of Togo. However, their effect on severe onchocerciasis is poorly investigated. The present study aimed to investigate the anti-Th17 and anti-Th2 effects of hydro-ethanolic extracts of AM, XA and KS during HO. Onchocerca volvulus-infected individuals were recruited in the Central region of Togo in 2018. Isolated peripheral blood mononuclear cells (PBMCs) from both generalized onchocerciasis (GEO) and HO forms were activated with anti-CD3 and anti-CD28 monoclonal antibodies in the presence or absence of the hydro-ethanolic extracts of AM, XA and KS as well as their delipidated, deproteinized and deglycosylated fractions. After 72 hours, cytokines were assayed from cell culture supernatants. Then, flow cytometry was used to investigate the effects of the extracts on cell activation, proliferation, intracellular cytokines and T cells transcription factors. The production of both Th17 and Th2 cytokines IL-17A and IL-5 were significantly inhibited upon T-cell receptor (TCR) activation in the presence of the hydro-ethanolic extracts of AM, XA and KS in HO individuals' PBMCs in vitro. AM and XA inhibited CD4+RORC2+IL-17A+ and CD4+GATA3+IL-4+ cell populations induction. This inhibition was not Th1 nor Treg-dependent since both IFN-γ and IL-10 were also inhibited by the extracts. AM and XA did not interfere with T cell activation and proliferation for their inhibitory pathways. Lipid and protein compounds from AM and XA were associated with the inhibition of IL-17A. This study showed that in addition to their anthelminthic effects, hydro-ethanolic extracts of Aframomum melegueta, Xylopia aethiopica and Khaya senegalensis could downregulate both Th17 and Th2 responses and prevent the severe skin disorder observed. DOI: 10.1371/journal.pntd.0010341 PMCID: PMC9071127 PMID: 35468134 [Indexed for MEDLINE] Conflict of interest statement: The authors have declared that no competing interests exist.

Cameroonian Spice Extracts Modulate Molecular Mechanisms Relevant to Cardiometabolic Diseases in SW 872 Human Liposarcoma Cells.

18. Nutrients. 2021 Nov 26;13(12):4271. doi: 10.3390/nu13124271. Cameroonian Spice Extracts Modulate Molecular Mechanisms Relevant to Cardiometabolic Diseases in SW 872 Human Liposarcoma Cells. Atchan Nwakiban AP(1), Passarelli A(2), Da Dalt L(2), Olivieri C(2), Demirci TN(2), Piazza S(2), Sangiovanni E(2), Carpentier-Maguire E(3), Martinelli G(2), Shivashankara ST(4), Manjappara UV(4), Tchamgoue AD(5), Agbor GA(5), Kuiate JR(1), Daglia M(6)(7), Dell'Agli M(2), Magni P(2)(8). Author information: (1)Department of Biochemistry, Faculty of Science, University of Dschang, Dschang P.O. Box 96, Cameroon. (2)Department of Pharmacological and Biomolecular Sciences, Università degli Studi di Milano, 20133 Milan, Italy. (3)Department of Science and Technology, University of Lille, Rue de Lille, 59160 Lille, France. (4)Department of Lipid Science, CSIR-Central Food Technological Research Institute (CFTRI), Mysore 570 020, India. (5)Institute of Medical Research and Medicinal Plants Studies (IMPM), Yaoundé 4123, Cameroon. (6)Department of Pharmacy, University of Naples Federico II, 80131 Naples, Italy. (7)International Research Center for Food Nutrition and Safety, Jiangsu University, Zhenjiang 212013, China. (8)IRCCS MultiMedica, Sesto San Giovanni, 20099 Milan, Italy. The molecular pathophysiology of cardiometabolic diseases is known to be influenced by dysfunctional ectopic adipose tissue. In addition to lifestyle improvements, these conditions may be managed by novel nutraceutical products. This study evaluatedthe effects of 11 Cameroonian medicinal spice extracts on triglyceride accumulation, glucose uptake, reactive oxygen species (ROS) production and interleukin secretion in SW 872 human adipocytes after differentiation with 100 µM oleic acid. Triglyceride content was significantly reduced by all spice extracts. Glucose uptake was significantly increased by Tetrapleura tetraptera, Aframomum melegueta and Zanthoxylum leprieurii. Moreover, Xylopia parviflora, Echinops giganteus and Dichrostachys glomerata significantly reduced the production of ROS. Concerning pro-inflammatory cytokine secretion, we observed that Tetrapleura tetraptera, Echinops giganteus, Dichrostachys glomerata and Aframomum melegueta reduced IL-6 secretion. In addition, Xylopia parviflora, Monodora myristica, Zanthoxylum leprieurii, and Xylopia aethiopica reduced IL-8 secretion, while Dichrostachys glomerata and Aframomum citratum increased it. These findings highlight some interesting properties of these Cameroonian spice extracts in the modulation of cellular parameters relevant to cardiometabolic diseases, which may be further exploited, aiming to develop novel treatment options for these conditions based on nutraceutical products. DOI: 10.3390/nu13124271 PMCID: PMC8706885 PMID: 34959824 [Indexed for MEDLINE] Conflict of interest statement: This study is an original research carried out by the mentioned authors and, thus, the authors declare that there is no conflict of interests regarding the publication of this paper.

Antiviral activity of aframomum melegueta against severe acute respiratory syndrome coronaviruses type 1 and 2.

19. S Afr J Bot. 2022 May;146:735-739. doi: 10.1016/j.sajb.2021.12.010. Epub 2021 Dec 18. Antiviral activity of aframomum melegueta against severe acute respiratory syndrome coronaviruses type 1 and 2. Mahoney O(1), Melo C(2), Lockhart A(3), Cornejal N(4), Alsaidi S(5), Wu Q(3), Simon J(3), Juliani R(3), Zydowsky TM(6), Priano C(1), Koroch A(1), Fernández Romero JA(1)(6). Author information: (1)Science Department, Borough of Manhattan Community College, The City University of New York, NY, 199 Chambers Street, Science Department room N699, New York, NY 10007, USA. (2)George Washington University, Washington DC USA. (3)Rutgers University, New Brunswick, NJ USA. (4)Brooklyn College, The City University of New York, NY USA. (5)Lehman College, The City University of New York, NY USA. (6)Center for Biomedical Research, Population Council, New York, NY USA. Plant-based compounds with antiviral properties against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) have been identified in Aframomum melegueta through computational models. The seed extract have been traditionally used to treat different illnesses. In this study, ethanolic extracts were prepared for six commercial samples of A. melegueta seeds. Antiviral activity was tested using the XTT cytotoxicity assay and cell-based SARS-CoV-1 and 2 pseudoviral models. The presence of gingerols and other non-volatile components in the seed extracts was determined using an Agilent 1290 UPLC/DAD in tandem with an Agilent 6546 QTOF-MS. Our results showed selective antiviral activity with TI values as high as 13.1. Fifteen gingerols were identified by chromatographic analysis, with 6-gingerol being the dominant component in each seed extract. A combination of 6-gingerol with techtochrysin, previously identified in computational models as a potential active ingredient against SARS-CoV-2, demonstrated additive antiviral activity with CI values between 0.8715 and 0.9426. We confirmed the antiviral activity of A. melegueta predicted through computational models and identified a different compound, 6-gingerol, as a potential active ingredient. © 2021 The Author(s). DOI: 10.1016/j.sajb.2021.12.010 PMCID: PMC8683269 PMID: 34955582 Conflict of interest statement: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Prolonged Treatment with Grains of Paradise (Aframomum melegueta) Extract Recruits Adaptive Thermogenesis and Reduces Body Fat in Humans with Low Brown Fat Activity.

20. J Nutr Sci Vitaminol (Tokyo). 2021;67(2):99-104. doi: 10.3177/jnsv.67.99. Prolonged Treatment with Grains of Paradise (Aframomum melegueta) Extract Recruits Adaptive Thermogenesis and Reduces Body Fat in Humans with Low Brown Fat Activity. Yoneshiro T(1)(2), Matsushita M(1), Sugita J(1)(3), Aita S(4), Kameya T(5), Sugie H(5), Saito M(1)(6). Author information: (1)Department of Nutrition, School of Nursing and Nutrition, Tenshi Collage. (2)Division of Metabolic Medicine, Research Center for Advanced Science and Technology, The University of Tokyo. (3)R&D Management, Kao Corporation. (4)Department of Food and Health Sciences, College of Life Sciences, Ibaraki Christian University. (5)LSI Sapporo Clinic. (6)Faculty of Veterinary Medicine, Hokkaido University. Increasing adaptive thermogenesis through the activation of brown adipose tissue (BAT) is a promising practical strategy for preventing obesity and related disorders. Ingestion of a single dose of 40 mg of an extract of Grains of Paradise (GP), a ginger family species, reportedly triggers BAT thermogenesis in individuals with high but not in those with low BAT activity. We hypothesized that prolonged treatment with GP might revive BAT in individuals who have lost active BAT. In the present study, we recruited 9 healthy young male volunteers with reduced BAT that was assessed by fluorodeoxyglucose positron emission tomography and computed tomography (FDG-PET/CT) following 2-h cold exposure at 19ºC. The subjects ingested GP extract (40 mg/d) or placebo every day for 5 wk. Before and after the treatment with either GP or placebo, their body composition and BAT-dependent cold-induced thermogenesis (CIT)-a non-invasive index of BAT-were measured in a single-blinded, randomized, placebo-controlled cross-over design. Their whole-body resting energy expenditure at a thermoneutral condition remained unchanged following GP treatment. However, CIT after treatment was significantly higher in GP-treated individuals than in placebo-treated individuals. Body weight and fat-free mass did not change significantly following GP or placebo treatment. Notably, body fat percentage slightly but significantly decreased after GP treatment but not after placebo treatment. These results suggest that repeated ingestion of GP elevates adaptive thermogenesis through the re-activation of BAT, thereby reducing body fat in individuals with low BAT activity. DOI: 10.3177/jnsv.67.99 PMID: 33952741 [Indexed for MEDLINE]

Extract of grains of paradise and its active principle 6-paradol trigger thermogenesis of brown adipose tissue in rats.

21. Auton Neurosci. 2011 Apr 26;161(1-2):63-7. doi: 10.1016/j.autneu.2010.11.012. Epub 2010 Dec 23. Extract of grains of paradise and its active principle 6-paradol trigger thermogenesis of brown adipose tissue in rats. Iwami M(1), Mahmoud FA, Shiina T, Hirayama H, Shima T, Sugita J, Shimizu Y. Author information: (1)Department of Basic Veterinary Science, Laboratory of Physiology, The United Graduate School of Veterinary Sciences, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan. Grains of paradise (GP) is a species of the ginger family, Zingiberaceae, extracts of which have a pungent, peppery taste due to an aromatic ketone, 6-paradol. The aim of this study was to explore the thermogenic effects of GP extracts and of 6-paradol. Efferent discharges from sympathetic nerves entering the interscapular brown adipose tissue were recorded. Intragastric injection of a GP extract or 6-paradol enhanced the efferent discharges of the sympathetic nerves in a dose-dependent manner. The enhanced nerve discharges were sustained for as long as 3h. The rats did not become desensitized to the stimulatory effects these compounds on sympathetic nerve activity. The tissue temperature of brown adipose tissue showed significant increase in rats injected with 6-paradol. These results demonstrate that GP extracts and 6-paradol activate thermogenesis in brown adipose tissue, and may open up new avenues for the regulation of weight loss and weight maintenance. Copyright © 2010 Elsevier B.V. All rights reserved. DOI: 10.1016/j.autneu.2010.11.012 PMID: 21185236 [Indexed for MEDLINE]