The influence of biologically active compounds from Salsola tuberculatiformis Botsch. on steroid protein interactions

[摘要] ENGLISH ABSTRACT: This study forms part of an ongoing investigation into the syndrome of prolonged gestation in sheep and contraception in rats, caused by Namibian shrub, Salsola tuberculatiformis Botsch. Evidence was obtained from studies with A. tuberculatiformis extracts, that compounds in the shrub pertrubed adrenal steroidogenesis in the rat and interfered with the binding of the natural subtrate, deoxicortocosterone, to sheep adrenal cytochrome P450c11. Swart described the isolation o fone of the active compounds from the shrub, named S2. The S2 fraction was found to consist of a mixture of an extremely labile compound plus one or more stable components, one of which is synephrine. In an aqueous medium synephrine is a breakdown product of the S2 fraction. Derivitization studies suggested that the active component in S2 was a labile hydroxyphenyl-aziridine or the corresponding open chain precursor. A more stable acetoxy-aziridine precursor analogue, 2-(4-aceroxyphenyl1)-2-chloro-N-methyl-ethylammoniumchloride (Compound A) was synthesised, and found to be contraceptive in rats and to inhibit adrenal P450c11, like S2. An ethanolic extract from the plant, the active fraction from the plant, S2, and Compound A, the chemical analogue, were prepared and tested in the present study.

[发布机构] Stellenbosch University