Antiplasmodial Activity shown by Secondary Metabolites Extracted from the Seeds ofPentaclethramacrophyllaBenth

Oil extracts from the African oil bean seed (PentaclethramacrophyllaBenth.) was analyzed for its phytochemical and mineral content and proximate, physicochemical and antimicrobial analyses were also performed. Phytochemical analysis showed the presence of tannins, saponins, quinones, terpenoids, phenols and coumarins in the oil sample. Mineral determination of the cotyledon showed the presence of iron (Fe) (with the highest concentration), Cu, Zn, Mn, Cr, Pb and Cd; while proximate analysis gave the following result: moisture (14.2%), ash content (1.5%), crude fibre (4.9%), crude proteins (12.8%), oil contents (4.9%), and carbohydrate (61.8%). GC-MS analysis of the partitioned petroleum ether and chloroform fractions of the oil revealed the presence of 9-Octadecenoic acid, 9,12- Octadecadienoic acid and their methyl esters,cis-9-Hexadecenal among the many components of the oil extract. Physicochemical analysis of the oil indicateda saponification value (148.67 mg KOH/g), peroxide value(8.0 meq/g), iodine value (10.41 mg iodine/g) and free fatty acid (8.98 mg KOH/g). The need for the development of new drugs for malaria led to our study of the antiplasmodial activity of the oil from the seeds of Pentaclethramacrophylla. Toxicological studies were carried out to determine the LD50with chloroquinediphosphate as positive control and normal saline as negative control. Using the Peter’s 4 day suppressive test a parasite inhibition rate of 47.72% (25 mg/kg), 63.63% (50 mg/kg) and 61.36% (100 mg/kg) on day 4 after treatment was recorded. A 95.45% chemo-suppression was observed for animals treated with 10 mg/kg chloroquine. This resultis an indication that the extract had appreciable signs of chemosuppression

Structure-Based Design Synthesis of Functionalized 3-(5-(s- Phenyl)-4H-pyrazol-3-yl)-2H-chromen-2-one Motifs and Indigenous Plant Extracts and Their Antimalarial Potential

Resistance of the malaria parasite to conventional therapeutic agents calls for increased efforts in antimalarial drug discovery. Current efforts should be targeted at developing safe and affordable new agents to counter the spread of malaria parasites that are resistant to existing therapy. In this study, toxicological and in vivo antiplasmodial properties of 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-42H-chromen-2, Mangifera indica and Tithonia diversifolia in swiss albino mice models, Musmusculus were investigated. 2H-Chromen-2-one also known as coumarin is highly privileged oxygencontaining heterocyclic entity which are present in plant kingdom as secondary metabolites. The maceration technique of crude drug extraction was employed using cold water extraction. Toxicological analysis was carried out using Lorke’s method for acute toxicity testing while the chemosuppressive activity was carried out using Peter’s four day test on early infection. We also report the synthesis of functionalized 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-2H-chromen-2-one motifs via microwave assisted synthetic approach and isolation of indigenous plant extract in order to investigate their antimalarial efficacy. The condensation reaction of 3-acetylcoumarin with various benzaldehyde derivatives resulted in the formation of 3-[3-acryloyl]-2H-chromen-2-one which was subsequently reaction the hydrazine hydrate via microwave assisted hydrazinolysis to afford the targeted 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-2H-chromen-2-one motifs. The chemical structures were confirmed by analytical data and spectroscopic means such as FT-IR, UV, 1H NMR, 13C NMR and DEPT-135. The microwave assisted reaction was remarkably successful and gave targeted 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-2H-chromen- 2-one motifs in higher yields at lesser reaction time compared to conventional heating method. The LD50 of the aqueous extracts of the leaves and stem bark Mangifera indica was established to be ± 707.11 mg/kg b.w., p.o. (body weight, administered orally) in mice. Tithonia diversifolia aqueous leaf extracts is non-toxic at doses as high as 1000 mg/kg while the LD50 of the ethanolic leaf extracts was established to be ± 707.11 mg/kg b.w., p.o. in mice. The in vivo antiplasmodial activity was studied in chloroquine-sensitive Plasmodium berghei berghei - NK65 infected mice. All the plant extracts, at the doses (100, 200 and 400 mg/kg b.w., p.o.) used, produced significant (p 80% inhibition of parasitaemia at maximum dose) against the parasite in the suppressive tests. The in vitro antimalarial screening of the synthesized compounds is presently on-going and the finding will be reported in due course