Synthesis and Blastocyst Implantation Inhibition Potential of Lupeol Derivatives in Female Mice Anita Mahapatra, Purvi Shah, Mehul Jivrajani, and Manish Nivsarkar Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), S.G. Highway, Thaltej, Ahmedabad, 380054, India Department of Pharmacology and Toxicology, B. V. Patel PERD Centre, S.G. Highway, Thaltej, Ahmedabad, 380054, India Abstract: Blastocyst implantation which is analogous to pro-inflammatory response, mediated by different inflammatory mediators and ovarian hormones found to be an effective target for the development of emergency contraceptives. In the present study, a series of derivatives an anti-inflammatory natural scaffold, lupeol were synthesized under mild reaction conditions and good yield. All the compounds were evaluated for acute anti-inflammation. The three active compounds with 62-92% edema protection were screened for chronic anti-inflammation. The analogue 3-(p-chlorocinnamoyl) lupeol ( 2) with potent anti-inflammatory activity (85% protection) was evaluated for t he anti-implantation activity by studying changes in superoxide dismutase (SOD) and lipid peroxidation (LPO) levels, visualization of implantation site and anti-estrogenic activity. As expected, a sharp decrease in superoxide anion radical and increase in SOD activity was seen in the endometrium of treated animals. Also no implantation sites were observed in the uterus of treated animals. The active compound also exhibited anti-estrogenic activity.
Keywords: Lupeol; contraceptive; anti-inflammatory; blastocyst implantation; anti-estrogenic. © 2015 ACG Publications. All rights reserved. |
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