Journal of Bioequivalence & Bioavailability

Design, synthesis and studies of delta and Cox-2 receptor specific analgesic anti-inflammatory activity of some linear and cyclic peptides

6^th World Congress on Bioavailability & Bioequivalence: BA/BE Studies Summit

August 17-19, 2015 Chicago, USA

Subir Samantha, Lipika Roy and D Maji

Scientific Tracks Abstracts: J Bioequiv Availab

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.

Biography :

S Samanta is Professor in the Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Jharkhand India. He is having 29 years of teaching
and research experience and presently guiding 7 PhD students. He established CADD lab for the department. He is supported by UGC-MRP project for installation of FlexX
and Reaction station in Medicinal Chemistry Research Labs. His area of interest includes anti-diabetics, analgesics, anti-inflammatory agents. He has a patent on product
and process on peptide based oral anti-diabetic compounds. He has number of International publications and recognition in the field of research and teaching.