Larvicidal Properties Toxicological Effects And Characterisation Of Bioactive Principle(s) Of Garcinia Kola Seeds Fractions On Clarias Gariepinus

Malaria is a protozoan disease transmitted by the bite of an infected female Anopheles mosquito. Globally, there is a marked increase in resistance to well-known antimalaria drugs. The increasing drug resistance of the parasite and insecticide resistance of the vector dims the possibility of eradicating malaria in the tropics. Vector control are of the most successful method for reducing incidences of mosquito-borne diseases. Garcinia kola seeds (GKS) are used in Opi Nsukka for water guard to prevent Mosquito larvae in water. No literature has reported on the larvicidal property of GKS fractions. Therefore, this study was to investigate the larvicidal property, toxicological effect, and characterization of bioactive principles of GKS fractions with the view of providing a more cost effective method of malaria eradication. The specific objectives were to: (i) determine the presence of secondary metabolites and fractionate the aqueous and methanolic GKS. (ii) determine the larvicidal property of the aqueous and methanolic GKS fractions on mosquito larvae. (iii) identify the active components in the fractions with the highest larvicidal property (iv) characterize the bioactive principle(s) responsible for the larvicidal activity (v) propose a probable mechanism of action of the bioactive agent(s) (vi) determine the effect of GKS extracts on the Liver, brain and kidney function parameters, of Clarias gariepinus(vii) determine the binding conformations of the components of the extracts with mosquito larva acetylcholine esterase and Na+/K+-ATPase. rnScreening of the extracts for secondary metabolites and fractionation were done using standard methods. The larvicidal property of the GKS fractions on mosquito larvae were done using standard methods. Furthermore, the effects of the extracts on the rate of inhibition of mosquito larva acetylcholine esterase and Na+/K+-ATPase were done using standard methods. The components of the extracts were analysed by GC-MS and HPLC-DAD and in silico docking simulations were done on mosquito larva acetylcholine esterase and Na+/K+-ATPase. The toxicological effect on Clarias gariepinuswere done using standard methods. The data were subjected to analysis of variance and Duncan multiple range test and statistical significance was set at p˂0.05.rnThe results revealed that the aqueous and methanolic extracts of GKS contains alkaloids, tannins, phenolics, glycosides, saponin, flavonoids, steroids and HPLC-DAD revealed the presence of Apiginin, Ellagic acid and Luteolin. The larvicidal activities of 5th aqueous and 4th methanolic extracts of GKS fractions (96.92±0.42, and 89.72±0.03 respectively) were higher than the standard larvicide fenthione (81.27±0.24). Mosquito Larva Na+/K+-ATPase and AChE activity by GKS fractions were suppressed in dose dependent manner. In silico screening of GKS fractions suggested that Apiginin, Ellagic acid and Luteolin are potent inhibitor of Mosquito LarvaAcetylcholinesterase and Na+/K+-ATPase. The administration of GKS extracts had no toxic effect on the liver, brain and kidney function parameters, of Clarias gariepinus taking the waterrnThe study concluded that Apiginin, Ellagic acid and Luteolin effectively inhibited Na+/K+ ATPase and Acetylcholinesterase and thereby increasing the cholinergic response in the mosquito larva. The increase in cholinergic response may cause uncontrollable muscle contraction in the larva and its death

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