Sclerin, a New Cytotoxic Cyclononapeptide from Annona scleroderma

Sclerin,一种来自硬皮番荔枝的新型细胞毒性环肽

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作者:Francisco Cen-Pacheco, Gerardo Valerio-Alfaro, Dalia Santos-Luna, José Javier Fernández

Abstract

A new cytotoxic cyclononapeptide, sclerin, cyclo(⁻Dab¹⁻Ser²⁻Tyr³⁻Gly&sup4;⁻Thr&sup5;⁻Val&sup6;⁻Ala&sup7;⁻ Ile&sup8;⁻Pro&sup8;⁻) (1), was isolated from the methanol extract of the seeds of Annona scleroderma, together with the known metabolite, cyclosenegalin A, cyclo(⁻Pro¹⁻Gly²⁻Leu³⁻Ser&sup4;⁻Ala&sup5;⁻Val&sup6;⁻Thr&sup7;⁻) (2). The planar structures for the two compounds were established by comprehensive analysis of NMR and ESI-HRMS data, and the absolute stereochemistry was stablished by Marfey's method. Compound 1 showed moderate cytotoxic activity against the human prostate carcinoma cell line DU-145 at µM concentration.

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