First Total Synthesis and Pharmacological Potential of a Plant Based Hexacyclopeptide

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DAHIYA RAJIV; SINGH SUNIL; Gupta Sheeba Varghese; Sutariya Vijaykumar B.; Bhatia Deepak; Mourya Rita; Chennupati Suresh V.; SHARMA AJAY

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Journal: Iranian Journal of Pharmaceutical Research Year:2019 | Volume:18 | Issue:2 Page(s): 938-947

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Title

First Total Synthesis and Pharmacological Potential of a Plant Based Hexacyclopeptide

Author(s)

Keywords

Diandrine C

Proline-rich cyclic peptide

Solution-phase peptide synthesis

Drymaria diandra

Antimicrobial activity

Antihelmintic activity

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 μ g/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.

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APA: Copy

DAHIYA, RAJIV, SINGH, SUNIL, Gupta, Sheeba Varghese, Sutariya, Vijaykumar B., Bhatia, Deepak, Mourya, Rita, Chennupati, Suresh V., & SHARMA, AJAY. (2019). First Total Synthesis and Pharmacological Potential of a Plant Based Hexacyclopeptide. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 18(2), 938-947. SID. https://sid.ir/paper/289117/en

Vancouver: Copy

DAHIYA RAJIV, SINGH SUNIL, Gupta Sheeba Varghese, Sutariya Vijaykumar B., Bhatia Deepak, Mourya Rita, Chennupati Suresh V., SHARMA AJAY. First Total Synthesis and Pharmacological Potential of a Plant Based Hexacyclopeptide. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2019;18(2):938-947. Available from: https://sid.ir/paper/289117/en

IEEE: Copy

RAJIV DAHIYA, SUNIL SINGH, Sheeba Varghese Gupta, Vijaykumar B. Sutariya, Deepak Bhatia, Rita Mourya, Suresh V. Chennupati, and AJAY SHARMA, “First Total Synthesis and Pharmacological Potential of a Plant Based Hexacyclopeptide,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 18, no. 2, pp. 938–947, 2019, [Online]. Available: https://sid.ir/paper/289117/en

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