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Andrographolide, 14-deoxyandrographolide, andrograpanin, andrographiside, deoxyandrographiside, and neoandrographolide were isolated from the leaves of A. paniculata and evaluated for their spermimmobilizing activity. The mode of spermicidal action was assessed by (a) supravital and double fluoroprobe staining of sperm, (b) hypo-osmotic swelling test, and (c) transmission electron microscopy. Contraceptive efficacy was evaluated by intrauterine application in rat followed by mating, and subsequent assessment of the pregnancy outcome. 14-Deoxyandrographolide with MEC of 200 mg/ml was found to be the most active among the six compounds. It is comparable in activity to nonoxynol (N-9) and exerts its effect in a dose dependent manner. Intra-vaginal administration of 10% 14-deoxyandrographolide did not cause any significant vaginal irritation in rat. The findings strongly suggest that 14-deoxyandrographolide may be used as a nondetergent type spermicidal agent. Key words: sperm-immobilizing activity; andrographolide; 14-deoxyandrographolide.

Evaluation of spermicidal potential of labdane diterpenes from Andrographis paniculata