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克罗托烷二萜类化合物和其他成分从 中分离得到。

Crotofolane Diterpenoids and Other Constituents Isolated from .

机构信息

Chemistry Department, College of Natural and Applied Sciences, University of Dar es Salaam, P.O. Box 35061, Dar es Salaam, Tanzania.

Department of Infectious Diseases/Virology, Institute of Biomedicine, Sahlgrenska Academy, University of Gothenburg, S-413 46 Gothenburg, Sweden.

出版信息

J Nat Prod. 2023 Feb 24;86(2):380-389. doi: 10.1021/acs.jnatprod.2c01007. Epub 2023 Feb 7.

Abstract

Six new crotofolane diterpenoids (-) and 13 known compounds (-) were isolated from the MeOH-CHCl (1:1, v/v) extracts of the leaves and stem bark of . The structures of the new compounds were elucidated by extensive analysis of spectroscopic and mass spectrometric data. The structure of crotokilwaepoxide A () was confirmed by single-crystal X-ray diffraction, allowing for the determination of its absolute configuration. The crude extracts and the isolated compounds were investigated for antiviral activity against respiratory syncytial virus (RSV) and human rhinovirus type-2 (HRV-2) in HEp-2 and HeLa cells, respectively, for antibacterial activity against the Gram-positive and the Gram-negative , and for antimalarial activity against the Dd2 strain. -3β,19-Dihydroxykaur-16-ene () and ayanin () displayed anti-RSV activities with IC values of 10.2 and 6.1 μM, respectively, while exhibiting only modest cytotoxic effects on HEp-2 cells that resulted in selectivity indices of 4.9 and 16.4. Compounds and exhibited modest anti-HRV-2 activity (IC of 44.6 μM for both compounds), while compound inhibited HRV-2 with an IC value of 1.8 μM. Compounds - showed promising antiplasmodial activities (80-100% inhibition) at a 50 μM concentration.

摘要

从 的叶和茎皮的甲醇 - 氯仿(1:1,v/v)提取物中分离得到了 6 个新的克罗托烷二萜(-)和 13 个已知化合物(-)。通过广泛的光谱和质谱数据分析,阐明了新化合物的结构。通过单晶 X 射线衍射确定了 crotokilwaepoxide A()的结构,从而确定了其绝对构型。对粗提取物和分离得到的化合物进行了抗呼吸道合胞病毒(RSV)和人鼻病毒 2 型(HRV-2)的抗病毒活性研究,分别在 HEp-2 和 HeLa 细胞中进行;对革兰氏阳性菌 和革兰氏阴性菌 进行了抗菌活性研究;对 株进行了抗疟原虫活性研究。-3β,19-二羟基贝壳杉-16-烯()和 ayanin()对 RSV 具有抗活性,IC 值分别为 10.2 和 6.1 μM,而对 HEp-2 细胞仅有适度的细胞毒性作用,导致选择性指数分别为 4.9 和 16.4。化合物 和 对 HRV-2 表现出适度的活性(对两种化合物的 IC 均为 44.6 μM),而化合物 对 HRV-2 的抑制作用的 IC 值为 1.8 μM。化合物 - 表现出有希望的抗疟原虫活性(在 50 μM 浓度下 80-100%抑制)。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e71/9972476/af13e3e0c5dd/np2c01007_0001.jpg

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