Author/Authors :
Dahiya, Rajiv Laboratory of Peptide Research and Development - School of Pharmacy - Faculty of Medical Sciences - The University of the West Indies,Tobago, West Indies , Singh, Sunil Department of Pharmacy - Faculty of Pharmaceutical Science - Mewar University, Rajasthan, India , Varghese Gupta, Sheeba Department of Pharmaceutical Sciences - USF College of Pharmacy - University of South Florida, Tampa, FL , USA , Sutariya, Vijaykumar B Department of Pharmaceutical Sciences - USF College of Pharmacy - University of South Florida, Tampa, FL , USA , Bhatia, Deepak Department of Pharmacogenomics - Bernard J. Dunn School of Pharmacy - Shenandoah University- ICPH Fairfax, Fairfax, VA , USA , Mourya, Rita School of Pharmacy - College of Medicine and Health Sciences - University of Gondar, Gondar, Ethiopia , Chennupati, Suresh V Department of Pharmacy - College of Medical and Health Sciences - Wollega University, Nekemte, Ethiopia , Sharma, Ajay Department of Pharmacognosy - Amity Institute of Pharmacy - Amity University, Gwalior, Madhya Pradesh, India
Abstract :
A new bioactive proline-rich cyclohexapeptide - diandrine C (6), previously isolated
from whole plant of Drymaria diandra (Caryophyllaceae), was synthesized through coupling
reactions of tetrapeptide unit Boc-Gly-l-Pro-l-Tyr-l-Trp-OH with dipeptide unit l-Pro-
Gly-OMe using N,N-diisopropylcarbodiimide (DIPC) as the coupling agent, followed by
cyclization of linear hexapeptide unit under alkaline condition. Structure of cyclohexapeptide
was confirmed by means of chemical, and spectroscopic analyses and also was screened for
its antimicrobial and anthelmintic properties. Bioevaluation results indicated that the newly
synthesized hexacyclopeptide exhibited potent antimicrobial activity against Gram-negative
bacteria Pseudomonas aeruginosa, Klebsiella pneumoniae and pathogenic Candida albicans
at 6 μg/mL. Moderate to good level of antihelmintic activity against three earthworm species
Megascoplex konkanensis, Pontoscotex corethruses and Eudrilus eugeniae was also observed
at concentration of 2 mg/mL.
Keywords :
Antihelmintic activity , Antimicrobial activity , Drymaria diandra , Solution-phase peptide synthesis , Proline-rich cyclic peptide , Diandrine C
