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利托阿莫醇 A:一种来自红海软珊瑚的未被描述的倍半萜,具有抗疟活性评价。

Litoarbolide A: an undescribed sesquiterpenoid from the Red Sea soft coral with an anti-malarial activity evaluation.

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.

National Center for Natural Products Research, School of Pharmacy, The University of Mississippi, University, Mississippi, United States.

出版信息

Nat Prod Res. 2023 Feb;37(4):542-550. doi: 10.1080/14786419.2022.2071268. Epub 2022 May 2.

DOI:10.1080/14786419.2022.2071268
PMID:35491702
Abstract

Soft corals distributed across the Red Sea coasts are a rich source of diverse and bioactive natural products. Chemical probing of the Red Sea soft coral led to isolation and structural characterization of an undescribed sesquiterpenoid, litoarbolide (), along with 14 previously reported metabolites (). The chemical structures of the isolates were assigned based on NMR as well as high resolution electrospray ionization mass spectrometry (HR-ESI-MS) data. Litoarbolide A is supposed to be the biosynthetic precursor to other sesquiterpenoids, which formed further post-translational modifications. Furthermore, these metabolites were evaluated for anti-malarial activity, where only the acyclic sesquiterpenoid of a -germacrane nucleus () showed an activity against chloroquine-sensitive (D6) and chloroquine-resistant (W2) strains of with IC at 3.7 and 2.2 mg/mL, respectively. Moreover, the isolated metabolites were all non-toxic to the Vero cell line. These findings support the consideration of in further natural anti-malarial studies.

摘要

红海沿岸分布的软珊瑚是具有多种生物活性的天然产物的丰富来源。对红海软珊瑚的化学研究导致了一种未被描述的倍半萜内酯 litoarbolide ()的分离和结构表征,以及 14 种以前报道过的代谢物 ()。根据 NMR 以及高分辨率电喷雾电离质谱 (HR-ESI-MS) 数据确定了这些分离物的化学结构。litoarbolide A 被认为是其他倍半萜的生物合成前体,这些倍半萜形成了进一步的翻译后修饰。此外,还评估了这些代谢物的抗疟活性,只有具有 a - germacrane 核的无环倍半萜 ()对氯喹敏感 (D6) 和氯喹耐药 (W2) 株表现出活性,IC 值分别为 3.7 和 2.2mg/mL。此外,分离出的代谢物对 Vero 细胞系均无毒性。这些发现支持进一步的天然抗疟研究中考虑使用 。

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