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紫金龙属植物全草中具有体外细胞毒性的 9 个新的裂环环烯醚萜苷类化合物 Ptehosides A-I

Ptehosides A-I: Nine undescribed iridoids with in vitro cytotoxicity from the whole plant of Pterocephalus hookeri (C.B. Clarke) Höeck.

机构信息

Chongqing Key Laboratory of New Drug Screening from Traditional Chinese Medicine, Integrative Science Center of Germplasm Creation in Western China (Chongqing) Science City & Southwest University, SWU-TAAHC Medicinal Plant Joint R&D Centre, College of Pharmaceutical Sciences, Southwest University, Chongqing, 400715, PR China; Key Laboratory of Luminescence Analysis and Molecular Sensing, Ministry of Education, College of Pharmaceutical Sciences, Southwest University, Chongqing, 400715, PR China.

Chongqing Key Laboratory of New Drug Screening from Traditional Chinese Medicine, Integrative Science Center of Germplasm Creation in Western China (Chongqing) Science City & Southwest University, SWU-TAAHC Medicinal Plant Joint R&D Centre, College of Pharmaceutical Sciences, Southwest University, Chongqing, 400715, PR China.

出版信息

Phytochemistry. 2024 Jul;223:114144. doi: 10.1016/j.phytochem.2024.114144. Epub 2024 May 15.

Abstract

Nine previously undescribed iridoids, ptehosides A-I (1-9), together with 12 known ones (10-21), were isolated from Pterocephalus hookeri (C.B. Clarke) Höeck. Their structures were elucidated using various spectroscopic methods including HR-ESI-MS, NMR, UV, IR and CD, etc. The cytotoxic activities of all isolates were evaluated using MTT method in three human cancer cell lines (Caco2, Huh-7, and SW982). As result, compound 9 exhibited substantial inhibitory activity on Caco2, Huh-7, and SW982 cells with IC values of 1.17 ± 0.05, 1.15 ± 0.05 and 1.14 ± 0.04 μM, respectively. A preliminary mechanism study showed that 9 arrested the cell cycle of SW982 cells in the G0/G1 phase and induced apoptosis by upregulating Bax expression and downregulating Bcl-2 expression.

摘要

从翼核果(Pterocephalus hookeri(C.B. Clarke)Höeck)中分离得到了 9 个以前未描述的环烯醚萜类化合物,即 ptehosides A-I(1-9),以及 12 个已知化合物(10-21)。采用 HR-ESI-MS、NMR、UV、IR 和 CD 等多种光谱方法阐明了它们的结构。采用 MTT 法在三种人癌细胞系(Caco2、Huh-7 和 SW982)中评价了所有分离物的细胞毒性。结果表明,化合物 9 对 Caco2、Huh-7 和 SW982 细胞具有显著的抑制活性,IC 值分别为 1.17±0.05、1.15±0.05 和 1.14±0.04 μM。初步机制研究表明,9 通过上调 Bax 表达和下调 Bcl-2 表达,将 SW982 细胞的细胞周期阻滞在 G0/G1 期并诱导细胞凋亡。

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