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从. 中提取的具有抗菌和调节 ATP 合成作用的化合物。

Antibacterial and ATP Synthesis Modulating Compounds from .

机构信息

Department of Pharmacy, University of Genova, Viale Cembrano 4, 16148 Genova, Italy.

Department of Integrated Surgical and Diagnostical Sciences, University of Genova, Largo Rosanna Benzi 8, 16145 Genova, Italy.

出版信息

J Nat Prod. 2020 Apr 24;83(4):1027-1042. doi: 10.1021/acs.jnatprod.9b01024. Epub 2020 Mar 17.

DOI:10.1021/acs.jnatprod.9b01024
PMID:32182064
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7997632/
Abstract

A surface extract of the aerial parts of afforded a nor-sesterterpenoid () and eight new sesterterpenoids (-̵), along with five known sesterterpenoids, five labdane and one abietane diterpenoid, one sesquiterpenoid, and four flavonoids. The structures of the new compounds were established by 1D and 2D NMR spectroscopy, HRESIMS, and VCD data and Mosher's esters analysis. The antimicrobial activity of compounds was evaluated against 30 human pathogens including 27 clinical strains and three isolates of marine origin for their possible implications on human health. The methyl ester of salvileucolide (), salvileucolide-6,23-lactone (), sclareol (), and manool () were the most active against Gram-positive bacteria. The compounds were also tested for the inhibition of ATP production in purified mammalian rod outer segments. Terpenoids , , , and inhibited ATP production, while only inhibited also ATP hydrolysis. Molecular modeling studies confirmed the capacity of to interact with mammalian ATP synthase. A significant reduction of ATP production in the presence of was observed in and isolates.

摘要

从 地上部分的表面提取物中分离得到了一个 nor-sesterterpenoid () 和八个新的甾体萜烯(-̵),以及五个已知的甾体萜烯、五个 labdane 和一个 abietane 二萜、一个倍半萜和四个类黄酮。新化合物的结构通过 1D 和 2D NMR 光谱、HRESIMS 和 VCD 数据以及 Mosher 酯分析确定。对 30 种人类病原体(包括 27 种临床分离株和 3 种海洋来源的分离株)进行了化合物的抗菌活性评估,以评估它们对人类健康的可能影响。 salvileucolide 的甲酯()、salvileucolide-6,23-lactone ()、sclareol () 和 manool () 对革兰氏阳性菌的活性最强。还测试了这些化合物对纯化的哺乳动物视杆外段中 ATP 产生的抑制作用。萜烯、、、和 抑制了 ATP 的产生,而只有 也抑制了 ATP 水解。分子建模研究证实了 与哺乳动物 ATP 合酶相互作用的能力。在 和 分离株中观察到 存在时 ATP 产生的显著减少。

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