Potent spermicidal effect of oleanolic acid 3-beta-D-glucuronide, an active principle isolated from the plant Sesbania sesban Merrill.

BACKGROUND: The spermicidal activity of oleanolic acid 3-ß-D-glucuronide (OAG), an active principle isolated from root extracts of Sesbania sesban, was evaluated. STUDY DESIGN: Under the Sander-Cramer test criteria, the sperm-immobilizing activity of OAG was studied using highly motile rat sperm. Sperm mortality and membrane integrity were assessed by supravital staining, hypo-osmotic swelling (HOS), transmission electron microscopy (TEM) and sperm membrane lipid peroxidation (LPO). In vitro microbicidal potential and hemolytic index of OAG were examined in Lactobacillus culture and rat red blood corpuscles (RBCs), respectively. Post-intravaginal OAG application, the in vivo contraceptive efficacy was evaluated in rats. Ames test determined the carcinogenic potential of OAG. RESULTS: The minimum effective concentration (MEC) of OAG was 50 mcg/mL. More than 97% of the OAG-treated sperm lost their HOS responsiveness in a dose-dependent manner. TEM and LPO revealed that OAG affected the sperm membrane integrity. OAG declined fertility to zero, was nonmutagenic and was not harmful to lactobacillus. CONCLUSION: OAG has significant spermicidal activity that may be explored further.

Dual action microbicides: reappraisal of their roles in contraceptive research.

Of the variety of contraceptive options available for women, very few provide dual protection against sexually transmitted diseases. Due to increased incidence of human immunodeficiency virus type 1 (HIV-1), genital herpes, hepatitis B and human papilloma virus, development of novel contraceptive strategies that incorporate antiviral activity has become the top priority in contraceptive research. Topical microbicides are now considered to be the last ray of hope, as they would ideally provide protection against unwanted pregnancy, proper lubrication during sexual activity, and preclude the vaginal/rectal transmission of sexually transmitted diseases. A large number of vaginal microbicides are in the preclinical or clinical stages of evaluation for their safety, efficacy and acceptability. However, a major bottleneck in the development of novel mechanism-based dual microbicides has been their detergent-like effects, along with debilitating action on the vaginal microflora. Hence the search is still on for the ideal dual microbicide/s that may obliterate these disadvantages and provide an invincible shield to women in their crusade against unintended pregnancy as well as sexually transmitted diseases. The present review highlights the current scenario towards the development of novel contraceptive strategies to counteract the rampant spread of sexually transmitted diseases, with special reference to HIV/AIDS.