Plants are repository of important constituents with proven efficacy against many human diseases including viral diseases. The antiviral activity of many plants including Azadirachta indica, Xylopia aethiopica and Allium cepa has been reported. The novel coronavirus disease is no exception among viral diseases in which plant compounds could serve as potent antagonist. Therefore, our study investigated the inhibitory potentials of Azadirachta indica and Xylopia aethiopica isolates against SARS-CoV-2 viral accessory proteins and the host serine protease. The protein data (SARS-CoV-2 Papain like protease (PLpro) (PDB: 6wx4), Chymotrypsin-like main protease (3CLpro) (PDB:6YB7), SARS-CoV nsp 12 (PDB: 6nus), Host cell protease (TMPRSS1) (PDB:5ce1) were obtained from the protein data bank (PDB), while the SDS format of each Ligands were obtained from Pubchem database. Molecular docking analysis was performed with Auto Dock Vina 1.5.6 and visualization of the interaction between the ligands and protein was done with discovery studio 2019. The ADMET prediction of pharmacokinetics and toxicity properties of the ligands was obtained using vNN Web Server. Our result showed that all the plant isolates demonstrated negative Gibb’s free energy, indicating good binding affinity for both the viral and host protein. Overall, twenty-three of the forty-seven isolates showed good binding affinity comparable with dexamethasone that was used as reference drug. Although many of the compounds have good binding affinity for the viral and host proteins, based on the ADMET prediction, only Azadironic acid, Nimbionone, Nimbionol and Nimocinol all from A. indica could serve as potential drug candidate with good pharmacokinetics and toxicity profile. This study provides an insight into potential inhibitors and novel drug candidates for SARS-CoV-2. Further studies will look forward into the wet laboratory validation of Azadironic acid, Nimbionone, Nimbionol and Nimocinol against corona virus disease. Supplementary Information The online version contains supplementary material available at 10.1007/s13337-021-00682-7.

Launaea taraxacifolia and Amaranthus viridis used by people of Western Africa in the treatment of malaria and related symptoms were assessed for their antiplasmodial value against the chloroquine sensitive strain of Plasmodium berghei. Crude extracts (200 mg/kg) and chloroquine (5 mg/kg) were administered to different groups of Swiss mice. The percentage of parasitemia, survival time, and haematological parameters were determined. Both extracts significantly (p < 0.05) inhibited parasitemia and improved survival time in infected mice. The crude extracts prevented loss of some haematological parameters. A. viridis had a distinct effect on the packed cell volume. The extract was able to protect the liver from some of the damage. This study however showed that the methanolic extracts of A. viridis and L. taraxacifolia possess antiplasmodial activity. The results of this study can be used as a basis for further phytochemical investigations in the search for new and locally affordable antimalarial agents.

No abstract

SARS-CoV-2 has caused millions of infections and hundreds of thousands of deaths globally. Presently, no cure for SARS-CoV-2 infection is available; thus, all hands are on deck for new drug discovery. Although, several studies have reported the potentials of some already approved drugs for the treatment of COVID-19. This study attempted to compare the potency and safety of some these trial drugs via in silico methods. The binding affinity and interactions of the trial drugs with proteins involved in viral polyprotein processing (Papain like protease (PLpro) and Chymotrypsin like-protease (3-CLpro), viral replication (RNA dependent RNA polymerase (RdRp)) and host protease were studied in this work. The pharmacokinetic properties and toxicity potentials of the trial drugs were also predicted using vNN Web Server for ADMET Predictions. From the results, Merimepodib and Dexamethaxone demonstrated the most significant inhibitory potential against the PLpro. The binding affinity (∆G°) for merimepodib was − 7.2 kcal/mol while the inhibition constant was 6.3 µM. The binding affinity of the inhibitors for CLpro ranged from − 5.6 to − 9.5 kcal/mol. whereas Lopinavir (− 7.7 kcal/mol) exhibited the strongest affinity for RdRp. Overall, our results showed that all the ligands have a higher affinity for the 3-Chymotrypsin like protease than the other proteins (PLpro, RdRp, and Host protease). Among these compounds lopinavir, merimepodib and dexamethasone could be inhibitors with potentials for the treatment of SARS-CoV-2. However, the only dexamethasone has attractive pharmacokinetic and toxicity properties probable for drug development; therefore, our study provides a basis for developing effective drugs targeting a specific protein in the SARS-CoV-2 life cycle. Supplementary Information The online version contains supplementary material available at 10.1007/s40203-021-00105-x.

No abstract

No abstract

Aims: The toxicity of ethanol whole plant extract of Euphorbia lateriflora was assessed in Albino Wistar rats. Methodology: The LD50 was at single dose of 5000 mg/kg body weight, the sub-acute dosage of the extract was administered orally at 250 and 500 mg/kg b.w.t twice daily for 7 days and the effect of the extract on liver, kidney, and haematological parameters was assessed and recorded during these periods. Results: The result of the oral acute toxicity study at single high dose of 5000 mg/kg/bwt shows that the LD50 of the extract is greater than 5000 mg/kg/bwt. After 7 days of oral administration, 500 mg/kg/bwt of the extract caused a significant (p<0.05) decrease in the packed cell volume. At 500 mg/kg/bwt, the extract caused a significant (p<0.05) increase in ALP, total protein and albumin and decrease in serum electrolytes (Na+, k+ and Cl-). Histopathological analysis revealed the expansion of fibrous spaces in the liver and thickening of the glomerular basement of the kidney in the group fed with 500 mg/kg/b.w.t of extracts. Conclusion: In conclusion, the dose and time-dependent selective organ toxicity effect of this extract suggested that the extract might be relatively unsafe for consumption at especially high concentrations.

Background: The leaves of Thaumatococcus danielli (Benth.) have been traditionally used in folk medicine to treat malaria in Nigeria. However, there is no report on whether these leaves contain Nephroprotective activity. Thus, the ethanol leaf extract was investigated for Nephron-protective activity in Streptozotocin induced diabetic rats.Methods: First, the LD50 of the leaf was determined using standard procedure. Rats were assigned to 5 groups (A-E) of five rats. Except for the control group, each group was made diabetic using Streptozotocin (65 mg/kg/b.wt. i p). The treated groups received 0.5 ml of glibenclamide (25mg/kg/b.wt, o.p), 250 and 500 mg/kg/b.wt, o.p of Thaumatococcus danielli respectively. After 14 days of treatment, animals were sacrificed under light anaesthesia. Data were expressed as Means ± S.D (n=5) and were analyzed using one-way ANOVA followed by Dunnet’s test, values were considered significant at p<0.05. Results: The plant showed a LD50 greater than 5000 mg/kg/b.wt in albino rats observed for 72 hours. A significant (p<0.05) decreased in serum Na+, Cl-, HCO-3, total protein, and an insignificant increase in K+, urea and creatinine level were observed in the diabetic group when compared with the normal group. Oral administration of plant extract and glibenclamide significantly (p<0.05) restored the electrolytes to near normal. Histological alterations such as glomerulonephritis, and tubules infiltration by inflammatory cells observed in diabetic control were also reversed.Conclusion: This study suggests renal protective ability of the plant against impairment due to hyperglycemia.Keywords: Streptozotocin, Thaumatococcus danielli, Nephroprotective, Glibenclamide, serum electrolytes.