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

Abstract

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

• Authors: S N Singh, S Bhatnagar, N Fatma, P M Chauhan, R K Chatterjee
• Journal: Tropical medicine & international health : TM & IH (Trop Med Int Health) Vol. 2 Issue 6 Pg. 535-43 (Jun 1997) ISSN: 1360-2276 [Print] England
• PMID: 9236820 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• CDRI 92-138
• Filaricides
• Imidazoles
• Indoles

Topics

• Animals
• Dipetalonema Infections (drug therapy)
• Drug Evaluation, Preclinical
• Filariasis (drug therapy)
• Filaricides (pharmacology, therapeutic use)
• Filarioidea (drug effects)
• Imidazoles (pharmacology, therapeutic use)
• Indoles (pharmacology, therapeutic use)
• Male
• Muridae
• Sigmodontinae