Subir Samanta
Birla Institute of Technology, India
Title: Design, synthesis and studies of delta and Cox-2 receptor specific analgesic anti-inflammatory activity of some linear and cyclic peptides
Biography
Biography: Subir Samanta
Abstract
Pain is the most common symptom for most diseases and there is an urgent need of more receptor specific, potent and safe analgesics. The present study is based on docking studies of 30 designed molecules both linear and cyclic small peptides. Using Glide software (version: 5.0), on receptor [pdb: 4COX & OPRD_HUMAN_AD_JOM-13 the ADME studies were done using QikProp (version: 3.1) software. The cyclic peptides have shown good % Human oral absorption. The toxicity studies were validated using OSIRIS Property Explorer. 14 designed ligands having best docking scores were synthesized and screened for anti-inflammatory, analgesic activity. Peripheral analgesic activity was significant in acetic acid induced writhing test in mice, for injectable compounds SSLR-9 (72% of inhibition) and SSLR-12 (61% of inhibition) while orally given compounds SSLR-12 showed good analgesic activity (45% of inhibition) compared to standard compound Aspirin (67% of inhibition). Also, injectable compounds SSLR-9 (43% inhibition) & SSLR-12 (35% inhibition) showed significant degree of anti- inflammatory activity compared to standard compound indomethacin (55% inhibition) in carrageenan induced anti-inflammatory study in rats. Thus this study infers that in the near future different combinations of amino acids will be suitable for peripheral analgesic and anti-inflammatory activity. Peptide combinations can also be attached with the non peptide NSAIDs such as indomethacin etc. and can prove to be more receptor specific, potent, and bio-friendly analgesic and anti- inflammatory agents.