Covid-19 treatment: Investigation on the phytochemical constituents of Vernonia amygdalina as potential Coronavirus-2 inhibitors.

The upsurge in the current cases of COVID-19 poses a major threat on human health and population all over the globe. The emergence of new infectious diseases and increase in frequency of drug resistant viruses demand effective and novel therapeutic agents. In this study, we used bioinformatics approach to investigate the possible inhibitory potentials of phytochemical constituents of Vernonia amygdalina towards coronavirus-2 major protease. Pharmacodynamics, pharmacokinetics and toxicological profiles of the compounds were also examined using the pkCSM server. All the phytochemicals showed good binding affinity to the binding pocket of PDB ID 6LU7. It was observed that veronicoside A exhibited the highest binding affinity when compared to remdesivir, hydroxy-vernolide, vernodalin, vernodalol, and vernolide. The amino acids LEU272, LEU287, GLY275, TYR237, LYS236, THR198, THR199, ARG131, and LYS5 were showed as the key residues for veronicoside A binding to human SARS-COV2 major protease. The Pharmacodynamics and pharmacokinetics results suggested that all the tested phytochemicals have significant drug likeness properties and they could be absorbed through the human intestine. Furthermore, all the tested phytochemicals are not hepatoxic and also exhibited non or relatively low toxic effects in human. Taken together, the results of this study indicated that all the tested phytochemicals are potential putative inhibitors of SARS-COV2 major protease with non or low toxicity effects. However, further experimental and clinical studies are needed to further explore their activities and validate their efficacies against COVID-19.

Lophirones B and C prevent aflatoxin B1-induced oxidative stress and DNA fragmentation in rat hepatocytes.

Context Despite the reported anticarcinogenic activity of lophirones B and C, no scientific information exists for its activity in rat hepatocytes. Objective Effect of lophirones B and C on aflatoxin B1 (AFB1)-induced oxidative stress, and DNA fragmentation in rat hepatocytes was investigated. Materials and methods Wistar rat hepatocytes were incubated with lophirones B and C (1 mg/mL) or sylimarin (1 mg/mL) in the presence or absence of AFB1. For an in vivo study, rats were orally administered with lophirones B and C, and/or AFB1 (20 µg/d) for 9 weeks. Results Lophirones B and C lowered AFB1-mediated increase in nitric oxide, superoxide anion radicals, caspase-3 and fragmented DNA. Lophirones B and C attenuated AFB1-mediated decrease in superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase, and reduced glutathione. Also, lophirones B and C attenuated AFB1-mediated increase in conjugated dienes, lipid hydroperoxides and malondialdehyde in rat hepatocytes. Furthermore, AFB1-mediated alterations in alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase, albumin, total bilirubin and globulin in rat serum were significantly annulled in lophirones B and C-treated rats. Conclusion This study revealed that lophirones B and C prevented AFB1-induced oxidative damage in rat hepatocytes.

Cytotoxic activity of aqueous extracts of Anogeissus leiocarpus and Terminalia avicennioides root barks against Ehrlich ascites carcinoma cells.

OBJECTIVES: Folkloric claims on the use of a mixture of Anogeissus leiocarpus and Terminalia avicennioides root barks in tumor management exist without scientific evidence. This study aimed at investigating the phytochemical constituents and in vitro antiproliferative activity of these plants and their mixture. MATERIALS AND METHODS: Phytochemical screening was carried out on the aqueous extracts after which various concentrations (0 to 1 000 µg/ml) were incubated with Ehrlich ascites carcinoma cell lines for 3 and 24 hours. RESULTS: The extracts contained alkaloids, tannins, flavonoids, phenolics, saponins, phlobatannins, and terpenes. The separate extracts and their 1:1 mixture significantly (P<0.05) decreased the computed percentage viability of the cell lines in a dose- and time-dependent manner. CONCLUSIONS: The antiproliferative activity may be due to the presence of the bioactive compounds in the extracts and has a potential in the management of tumor.

Diethylnitrosamine-induced redox imbalance in rat microsomes: protective role of polyphenolic-rich extract from Sorghum bicolor grains.

BACKGROUND: This study investigates the protective role of polyphenolic-rich extract from Sorghum bicolor against diethylnitrosamine (DEN)-induced redox imbalance in rat microsomes. METHODS: Reactive oxygen species (ROS) scavenging potentials of the polyphenolic extract from S. bicolor (0.2-1.0 mg/mL) was investigated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical, superoxide ion, hydrogen peroxide, hydroxyl radical, and ferric ion reducing system. The detoxification of ROS was evaluated in DEN-induced redox imbalance in rat microsomes. RESULTS: Sorghum bicolor polyphenolic extract at 1.0 mg/mL scavenged the DPPH, superoxide ion, hydrogen peroxide, and hydroxyl radical at 75%, 76%, 79%, and 81%, respectively; it also reduced ferric ion significantly. The polyphenolic extract significantly (p<0.05) attenuated DEN-mediated decrease in the activities of ROS detoxifying enzymes (superoxide dismutase, catalase, glutathione peroxidase and reductase, and glucose-6-phosphate dehydrogenase). The concentrations of malondialdehyde, conjugated dienes, lipid hydroperoxide, protein carbonyl, and percentage DNA fragmentation in DEN-treated microsomes were significantly reduced by the polyphenolic extract. CONCLUSIONS: The results of the present study indicated that S. bicolor polyphenolic extract possessed in vitro antioxidant activity and protected microsomes from DEN-mediated oxidative stress by scavenging free radicals and ROS scavenger and inducer of ROS detoxifying enzymes.

Androgenic potentials of aqueous extract of Massularia acuminata (G. Don) Bullock ex Hoyl. stem in male Wistar rats.

UNLABELLED: The use of medicinal plants in the management of several ailments is gaining popularity nowadays. Massularia acuminata, one of such plants is commonly used as chewing sticks due to its antimicrobial activity and the aqueous extract of its stem as an aphrodisiac. Aphrodisiac activity in some plants may be due to androgen increasing property of its phytochemicals. AIM OF THE STUDY: This study therefore sought to assess the androgenic potentials of aqueous extract of Massularia acuminata stem in male rats for 21 days. MATERIALS AND METHODS: Male rats weighing between 220 and 260 g were completely randomized into four groups: A, B, C and D. Group A, the control received orally 1 ml of distilled water (the vehicle) while groups B, C and D were orally administered with 1 ml each corresponding to 250, 500 and 1000 mg/kg body weight of the plant extract, respectively for 21 days. Rats were sacrificed 24h after 1, 7 and 21 days. RESULTS: Compared with the control, extract administration at all the doses produced significant increase (P<0.05) in testes-body weight ratio, testicular protein, glycogen, sialic acid, cholesterol, testosterone, luteinizing and follicle stimulating hormone concentrations throughout the period of administration. Testicular gamma glutamyl transferase activities were decreased significantly (P<0.05) after the first dose and was sustained throughout the experimental period. CONCLUSION: The available evidence in this study suggests that aqueous extract of Massularia acuminata stem has androgenic potential which may stimulate male sexual maturation and enhance normal testicular function.

Effects of oral administration of aqueous extract of Fadogia agrestis (Schweinf. Ex Hiern) stem on some testicular function indices of male rats.

AIM OF THE STUDY: The effects of administration of aqueous extract of Fadogia agrestis (Schweinf. Ex Hiern) stem on some testicular function indices of male rats (Rattus norvegicus) and their recovery potentials for 10 days were investigated. MATERIALS AND METHODS: Rats were grouped into four: A, B, C and D where A (the control) received orally 1 ml of distilled water (the vehicle), B, C and D (the test groups) received orally on daily basis graded doses of 18, 50 and 100mg/kg body weight of the plant extract, respectively, for 28 days. RESULTS: Compared with the control, extract administration for 28 days at all the doses resulted in significant increase (P<0.05) in percentage testes-body weight ratio, testicular cholesterol, sialic acid, glycogen, acid phosphatase and gamma-glutamyl transferase activities while there was significant decrease (P<0.05) in the activities of testicular alkaline phosphatase, acid phosphatase, glutamate dehydrogenase and concentrations of protein. Recoveries were made by the animals on some of the testicular function indices mainly at 18 mg/kg body weight. CONCLUSIONS: The alterations brought about by the aqueous extract of Fadogia agrestis stem are indications of adverse effects on the male rat testicular function and this may adversely affect the functional capacities of the testes. The recovery made at the dose of 18 mg/kg body weight as used in folklore medicine suggests that it does not exhibit permanent toxicity at this dose.