Antifilarial activity of a synthetic marine alkaloid, aplysinopsin (CDRI Compound 92/138)

摘要: CDRI Compound 92/138, a synthetic analogue of aplysinopsin, was evaluated in experimental filarial infections, Litomosoides carinii cotton rats (Sigmodon hispidus) and Acanthocheilonema viteae Mastomys coucha. The compound killed 63.8 90% adult L. A. at doses 30 50 mg/kg (i.p.) respectively given for 5 days. By the oral route, 100 days caused 50.9 57% mortality viteae, respectively. At 200 administered orally on 0, 10 25 post-infection, it reduced establishment by 68.5%. We also found 43.7 37.8% effect vivo L3 L4 stages single dose 250 mg/kg, p.o. active vitro micrograms/ml concentration significant decline MTT reduction 14C-glucose uptake filariids. Thus marine aplysinopsin could provide new pharmacophore development antifilarial agents.