Estrogenic and Anti-Inflammatory Activities of a Steroidal Indoxyl

F N Kamau; I O Kibwage; G Muriuki; A N Guantai; J Hoogmartens; E Roets; C Govaerts; H Chepkwony; R Busson

F N Kamau Department of Pharmaceutical Chemistry, University of Nairobi
I O Kibwage Department of Pharmaceutical Chemistry, University of Nairobi
G Muriuki Department of Pharmacology and Pharmacognosy, University of Nairobi
A N Guantai Department of Pharmacology and Pharmacognosy, University of 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
R Busson Katholieke Universiteit Leuven, Faculteit Farmaceutische Wetenschappen, Van Evenstraat 4, B-3000 Leuven, Belgium

Keywords: Steroidal indoxyl, synthesis, estrogenic, anti-inflammatory

Abstract

The estrogenic and anti-inflammatory activities of 3-methoxy-16,17-seco-16-norestra-
1,3,5-trien-15-(2'-indoxy1iden)-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 mglkg using the carrageenan-induced rat paw oedema antiinflammatory
assay method. Indomethacin had an of 3.2 mglkg in this assay while
dexamethasone had an EDs0 of 1.7 mglkg. 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 mglkg.