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-β-D-glucuronide (OAG), an active principle isolated from root extracts of Sesbania sesban, was evaluated.


METHODS
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.


CONCLUSIONS
OAG has significant spermicidal activity that may be explored further.
Reproductive Biology Research Department, Cell-Biology and Physiology Division, Indian Institute of Chemical Biology (A Unit of CSIR), Kolkata-700 032, India.
Nilanjana
N
Das
Poornima
P
Chandran
Smritinath
S
Chakraborty
D000818:Animals; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D003267:Contraception; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D005260:Female; D005306:Fertilization / Q000187:drug effects; D005965:Glucuronates / Q000494:pharmacology* / Q000633:toxicity; D007779:Lactobacillus acidophilus / Q000187:drug effects; D008297:Male; D008315:Malondialdehyde / Q000378:metabolism; D008826:Microbial Sensitivity Tests; D009152:Mutagenicity Tests; D009828:Oleanolic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000633:toxicity; D010936:Plant Extracts; D018517:Plant Roots; D051381:Rats; D017207:Rats, Sprague-Dawley; D049931:Sesbania; D013081:Sperm Motility / Q000187:drug effects*; D013089:Spermatocidal Agents / Q000494:pharmacology* / Q000633:toxicity; D013094:Spermatozoa / Q000187:drug effects* / Q000648:ultrastructure
D005965:Glucuronates; D010936:Plant Extracts; D013089:Spermatocidal Agents; C077716:oleanolic acid 3-O-monoglucuronide; D008315:Malondialdehyde; D009828:Oleanolic Acid