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海洋来源放线菌中含吡咯生物碱及其抗微生物和细胞毒性活性。

Pyrrole-Containing Alkaloids from a Marine-Derived Actinobacterium and Their Antimicrobial and Cytotoxic Activities.

机构信息

Marine Natural Products Chemistry Laboratory, Korea Institute of Ocean Science and Technology, 385 Haeyang-ro, Yeongdo-gu, Busan 49111, Republic of Korea.

Department of Marine Biotechnology, University of Science and Technology (UST), 217 Gajungro, Yuseong-gu, Daejeon 34113, Republic of Korea.

出版信息

Mar Drugs. 2023 Mar 6;21(3):167. doi: 10.3390/md21030167.

Abstract

Two new alkaloids, streptopyrroles B and C ( and ), were discovered through a chemical investigation of the ethyl acetate (EtOAc) extract from a marine-derived actinomycete, , along with four known analogs (-). The structures of the new compounds were elucidated by spectroscopic analysis (HR-ESIMS, 1D, and 2D NMR) and a comparison of their experimental data with literature values. The new compounds were evaluated for their antimicrobial activity by standard broth dilution assay, and the tested compounds showed significant activity against Gram-positive bacteria with minimum inhibitory concentration (MIC) values ranging from 0.7 to 2.9 µM, and kanamycin was used as a positive control with MIC values ranging from <0.5 to 4.1 µM. Additionally, , , and were evaluated for their cytotoxicity against six tumor cell lines by sulforhodamine B (SRB) assay, and these compounds displayed cytotoxic activities against all the tested cell lines, with concentration causing 50% cell growth inhibition (GI) values ranging from 4.9 to 10.8 µM, while a positive control, adriamycin, showed GI values of 0.13-0.17 µM.

摘要

通过对海洋来源放线菌 中乙酸乙酯(EtOAc)提取物的化学研究,发现了两种新的生物碱,即链孢吡咯 B 和 C(和 ),以及四种已知类似物(-)。通过光谱分析(高分辨 ESIMS、1D 和 2D NMR)和与文献值的比较,确定了新化合物的结构。通过标准肉汤稀释法评估新化合物的抗菌活性,测试化合物对革兰氏阳性菌具有显著的活性,最小抑菌浓度(MIC)值范围为 0.7-2.9 μM,卡那霉素为阳性对照,MIC 值范围为<0.5-4.1 μM。此外,通过磺酰罗丹明 B(SRB)测定法评估 、 和 对六种肿瘤细胞系的细胞毒性,这些化合物对所有测试的细胞系均显示出细胞毒性活性,浓度引起 50%细胞生长抑制(GI)值范围为 4.9-10.8 μM,而阳性对照阿霉素的 GI 值为 0.13-0.17 μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2647/10054583/8aac7684a9e8/marinedrugs-21-00167-g001.jpg

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