Anti-onchocerca Metabolites from Cyperus articulatus:Isolation,In Vitro Activity and In Silico‘Drug-Likeness’

The aims of this investigation were to isolate active ingredients from the roots/rhizomes of Cyperus articulatus used as herbal medicine in Cameroon for the treatment of human onchocerciasis and to assess the efficacy of the metabolites on the Onchocerca worm.The antifilarial activity was evaluated in vitro on microfilariae(Mfs)and adult worms of the bovine derived Onchocerca ochengi,a close relative of Onchocerca volvulus.Cytotoxicity was assessed in vitro on monkey kidney epithelial cells.The structures of the active compounds were determined using spectroscopic methods and their drug-likeness evaluated using Lipinski parameters.Two secondary metabolites,AMJ1[containing mustakone(1)as the major component]and linoleic acid or(9Z,12Z)-octadeca-9,12-dienoic acid(2)were isolated.Both compounds were found to kill both the microfilariae and adult worms of O.ochengi in a dose dependent manner.The IC50s for AMJ1 were 15.7 lg/mL for Mfs,17.4 lg/mL for adult males and 21.9 lg/mL for adult female worms while for linoleic acid the values were,15.7 lg/mL for Mfs,31.0 lg/mL for adult males and 44.2 lg/mL for adult females.The present report provides the first ever evidence of the anti-Onchocerca efficacy of AMJ1 and linoleic acid.Thus,these secondary metabolites may provide a lead for design and development of new antifilarial agents.

A Bioactivity Versus Ethnobotanical Survey of Medicinal Plants from Nigeria, West Africa

Traditional medicinal practices play a key role in health care systems in countries with developing economies.The aim of this survey was to validate the use of traditional medicine within local Nigerian communities.In this review,we examine the ethnobotanical uses of selected plant species from the Nigerian flora and attempt to correlate the activities of the isolated bioactive principles with known uses of the plant species in African traditional medicine.Thirty-three(33)plant species were identified and about 100 out of the 120 compounds identified with these plants matched with the ethnobotanical uses of the plants.

Natural Products as Potential Lead Compounds for Drug Discovery Against SARS-CoV-2

For the past 2 years,the coronavirus responsible for the COVID-19 infection has become a world pandemic,ruining the lives and economies of several nations in the world.This has scaled up research on the virus and the resulting infection with the goal of developing new vaccines and therapies.Natural products are known to be a rich source of lead compounds for drug discovery,including against infectious diseases caused by microbes(viruses,bacteria and fungi).In this review article,we conducted a literature survey aimed at identifying natural products with inhibitory concentrations against the coronaviruses or their target proteins,which lie below 10μM.This led to the identification of 42 compounds belonging to the alkaloid,flavonoid,terpenoid,phenolic,xanthone and saponin classes.The cut off concentration of 10μM was to limit the study to the most potent chemical entities,which could be developed into therapies against the viral infection to make a contribution towards limiting the spread of the disease.