FN Kamau
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Nairobi, P.O. Box 19676-00202, Nairobi.
IO Kibwage
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Nairobi, P.O. Box 19676-00202, Nairobi.
G Muriuki
Department of Pharmacology and Pharmacognosy, Faculty of Pharmacy, University of Nairobi, P.O. Box 1967-00202, Nairobi
AN Guantai
Department of Pharmacology and Pharmacognosy, Faculty of Pharmacy, University of Nairobi, P.O. Box 1967-00202, Nairobi
J Hoogmartens
Katholieke Universiteit Leuven, Faculteit Farmaceutische Wetenschappen, Van Evenstraat 4, B-3000 Leuven, Belgium
E Roets
Katholieke Universiteit Leuven, Faculteit Farmaceutische Wetenschappen, Van Evenstraat 4, B-3000 Leuven, Belgium
C Govaerts
Katholieke Universiteit Leuven, Faculteit Farmaceutische Wetenschappen, Van Evenstraat 4, B-3000 Leuven, Belgium
H Chepkwony
National Quality Control Laboratory, P.O. Box 29726-00202, Nairob
R Busson
Katholieke Universiteit Leuven, Faculteit Farmaceutische Wetenschappen, Van Evenstraat 4, B-3000 Leuven, Belgium
Abstract
The estrogenic and anti-inflammatory activities of 3-methoxy-16, 17-seco-16-norestra-1,3,5-trien-15-(2'-indoxyliden)-17-oic acid is reported. After intraperitoneal administration, the dose of this compound required to reduce swelling of the rat paw by 50% (ED50) was 14.1 mg/kg using the carrageenan-induced rat paw oedema anti-inflammatory assay method. Indomethacin had an ED50 of 3.2 mg/kg in this assay while dexamethasone had an ED50 of 1.7 mg/kg. The estrogenic activity of the compound after intramuscular administration in rats was 0.72 relative to diethylstilbestrol, when the two compounds were assayed at three dose levels of 1.0, 0.3 and 0.1 mg/kg.
Key Words: Steroidal indoxyl, synthesis, estrogenic, anti-inflammatory
East and Central African Journal of Pharmaceutical Sciences Vol.5(3) 2002: 44-48