Prostaglandin-synthesis inhibitory activity from the leaves of Siphonochilus aethiopicus used in the treatment of dysmenorrhoea.

Abstract

Plants used by southern African traditional healers for the treatment of menstrual pains were screened for prostaglandin-synthesis inhibitors and the ability to reduce isolated uterine muscle contraction using the cyclooxygenase (Cox-1) and in vitro uterine bioassays respectively. Prostaglandins are synthesized from arachidonic acid and the enzyme that drives this reaction is cyclooxygenase. The excessive production of prostaglandins by the myometrium and endometrium induces uterine contractions. Inhibition of cyclooxygenase and hence of the prostaglandin biosynthetic pathway may lead to relief of menstrual pain. Nine plants used by traditional healers for menstrual pains were assayed for cyclooxygenase inhibitory activity. Several plant extracts exhibited high inhibitory activity in the assay. The highest activities were obtained with ethanolic extracts of Siphonochilus aethiopicus, Cenchrus cilliaris and Solanum mauritianum. None of the ethanolic plant extracts were able to relax or reduce the contractions of a precontracted guinea pig uterus. Bioassay guided fractionation was used in an attempt to isolate the active compound(s) from the leaves of Siphonochilus aethiopicus. Isolation techniques employed were serial solvent extraction, bulk extraction, silica gel, Sephadex LH20 column, and high pressure liquid chromatography. Biological activity was followed through each purification step using the cyclooxygenase bioassay as a guide with respect to anti-inflammatory activity.