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Phakellisins A-E,由 LC-MS 指导的海洋海绵 Phakellia sp. 中分离得到的环肽。

Phakellisins A-E, cyclopeptides from a marine sponge Phakellia sp. guided by LC-MS.

机构信息

Engineering Research Center of Zebrafish Models for Human Diseases and Drug Screening of Shandong Province, Key Laboratory for Biosensor of Shandong Province, Biology Institute, Qilu University of Technology (Shandong Academy of Sciences), Jinan 250103, Shandong, People's Republic of China.

Research Center for Marine Drugs, State Key Laboratory of Oncogene and Related Genes, Department of Pharmacy, Ren Ji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200127, People's Republic of China.

出版信息

Bioorg Chem. 2023 Oct;139:106699. doi: 10.1016/j.bioorg.2023.106699. Epub 2023 Jun 23.

DOI:10.1016/j.bioorg.2023.106699
PMID:37390633
Abstract

A chemical investigation of the marine sponge Phakellia sp. from the South China Sea yielded five new cyclopeptides, phakellisins A-E (1-5). Structures of these compounds were determined by comprehensive analysis of 1D/2D NMR, HRESIMS/MS spectroscopic data and the advanced Marfey's method. All compounds were evaluated for their cytotoxic activity. Compound 1 showed a strong inhibitory activity against WSU-DLCL-2 cells with an IC value of 5.25 ± 0.2 μM by induction of G0/G1 cell cycle arrest and apoptosis.

摘要

对南海海绵 Phakellia sp. 的化学研究得到了五个新的环肽,分别为 phakellisins A-E(1-5)。通过全面分析 1D/2D NMR、HRESIMS/MS 光谱数据和先进的 Marfey 方法确定了这些化合物的结构。所有化合物均进行了细胞毒性活性评价。化合物 1 通过诱导 G0/G1 细胞周期停滞和细胞凋亡,对 WSU-DLCL-2 细胞表现出强烈的抑制活性,IC 值为 5.25±0.2 μM。

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