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及它们的抗动脉粥样硬化活性。

New Bisabolane-Type Sesquiterpenoids from and Their Anti-Atherosclerotic Activity.

机构信息

State Key Laboratory of Southwestern Chinese Medicine Resources, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.

School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.

出版信息

Molecules. 2023 Mar 16;28(6):2704. doi: 10.3390/molecules28062704.

Abstract

To explore the sesquiterpenoids in L. and their activity related to anti-atherosclerosis. The chemical compounds of the rhizomes of were separated and purified by multiple chromatography techniques. Their structures were established by a variety of spectroscopic experiments. The absolute configurations were determined by comparing experimental and calculated NMR chemical shifts and electronic circular dichroism (ECD) spectra. Their anti-inflammatory effects and inhibitory activity against macrophage-derived foam cell formation were evaluated by lipopolysaccharide (LPS) and oxidized low-density lipoprotein (ox-LDL)-injured RAW264.7 macrophages, respectively. This study resulted in the isolation of 10 bisabolane-type sesquiterpenoids (-) from , including two pairs of new epimers (curbisabolanones A-D, -). Compound significantly inhibited LPS-induced nitric oxide (NO), interleukin-1β (IL-1β), interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), and prostaglandin E2 (PGE2) production in RAW264.7 cells. Furthermore, compound showed inhibitory activity against macrophage-derived foam cell formation, which was represented by markedly reducing ox-LDL-induced intracellular lipid accumulation as well as total cholesterol (TC), free cholesterol (FC), and cholesterol ester (CE) contents in RAW264.7 cells. These findings suggest that bisabolane-type sesquiterpenoids, one of the main types of components in , have the potential to alleviate the atherosclerosis process by preventing inflammation and inhibiting macrophage foaming.

摘要

为了探索 中的倍半萜及其与抗动脉粥样硬化相关的活性。通过多种色谱技术分离和纯化 的根茎中的化学成分。通过各种光谱实验确定其结构。通过比较实验和计算 NMR 化学位移和电子圆二色性 (ECD) 光谱确定绝对构型。通过脂多糖 (LPS) 和氧化低密度脂蛋白 (ox-LDL) 损伤 RAW264.7 巨噬细胞分别评估其抗炎作用和抑制巨噬细胞源性泡沫细胞形成的活性。这项研究从 中分离出 10 种倍半萜 (-),包括两对新的差向异构体 (curbisabolanones A-D,-)。化合物 显著抑制 LPS 诱导的 RAW264.7 细胞中一氧化氮 (NO)、白细胞介素-1β (IL-1β)、白细胞介素-6 (IL-6)、肿瘤坏死因子-α (TNF-α) 和前列腺素 E2 (PGE2) 的产生。此外,化合物 对巨噬细胞源性泡沫细胞形成具有抑制活性,表现为明显减少 ox-LDL 诱导的 RAW264.7 细胞内脂质积累以及总胆固醇 (TC)、游离胆固醇 (FC) 和胆固醇酯 (CE) 含量。这些发现表明,倍半萜类化合物是 的主要成分之一,具有通过预防炎症和抑制巨噬细胞泡沫化来减轻动脉粥样硬化进程的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a448/10058791/d303c6b8ea69/molecules-28-02704-g001.jpg

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