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三种来自 的新二氢菲衍生物及其对癌细胞的细胞毒性。

Three New Dihydrophenanthrene Derivatives from and Their Cytotoxicity against Cancer Cells.

机构信息

Pharmaceutical Sciences and Technology Program, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand.

Department of Biochemistry, Faculty of Health Sciences, Islamic University in Uganda, Kampala P.O. Box 7689, Uganda.

出版信息

Molecules. 2022 Mar 29;27(7):2222. doi: 10.3390/molecules27072222.

DOI:10.3390/molecules27072222
PMID:35408617
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9000781/
Abstract

From the aerial parts of Cymbidium ensifolium, three new dihydrophenanthrene derivatives, namely, cymensifins A, B, and C (1−3) were isolated, together with two known compounds, cypripedin (4) and gigantol (5). Their structures were elucidated by analysis of their spectroscopic data. The anticancer potential against various types of human cancer cells, including lung, breast, and colon cancers as well as toxicity to normal dermal papilla cells were assessed via cell viability and nuclear staining assays. Despite lower cytotoxicity in lung cancer H460 cells, the higher % apoptosis and lower % cell viability were presented in breast cancer MCF7 and colon cancer CaCo2 cells treated with 50 µM cymensifin A (1) for 24 h compared with the treatment of 50 µM cisplatin, an available chemotherapeutic drug. Intriguingly, the half-maximum inhibitory concentration (IC50) of cymensifin A in dermal papilla cells at >200 µM suggested its selective anticancer activity. The obtained information supports the further development of a dihydrophenanthrene derivative from C. ensifolium as an effective chemotherapy with a high safety profile for the treatment of various cancers.

摘要

从 Cymbidium ensifolium 的地上部分分离得到三种新的二氢菲衍生物,分别为 cymensifins A、B 和 C(1-3),以及两种已知化合物 cypripedin(4)和 gigantol(5)。通过分析它们的光谱数据确定了它们的结构。通过细胞活力和核染色测定评估了它们对各种类型的人类癌细胞(包括肺癌、乳腺癌和结肠癌)的抗癌潜力以及对正常真皮乳头细胞的毒性。尽管在肺癌 H460 细胞中细胞毒性较低,但与可用化疗药物顺铂(50 μM)处理相比,用 50 μM cymensifin A(1)处理 24 小时后,乳腺癌 MCF7 和结肠癌 CaCo2 细胞中的凋亡率更高,细胞活力更低。有趣的是,cymensifin A 在真皮乳头细胞中的半最大抑制浓度(IC50)>200 μM 表明其具有选择性抗癌活性。获得的信息支持进一步开发来自 C. ensifolium 的二氢菲衍生物作为一种有效的化疗药物,具有高安全性,可用于治疗各种癌症。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ec8/9000781/c95ba6117730/molecules-27-02222-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ec8/9000781/bf31789ba1cb/molecules-27-02222-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ec8/9000781/fad76ae833a8/molecules-27-02222-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ec8/9000781/aadeebf2efbb/molecules-27-02222-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ec8/9000781/4886fdac919b/molecules-27-02222-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ec8/9000781/211839a558a8/molecules-27-02222-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ec8/9000781/c95ba6117730/molecules-27-02222-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ec8/9000781/bf31789ba1cb/molecules-27-02222-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ec8/9000781/fad76ae833a8/molecules-27-02222-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ec8/9000781/aadeebf2efbb/molecules-27-02222-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ec8/9000781/4886fdac919b/molecules-27-02222-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ec8/9000781/211839a558a8/molecules-27-02222-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ec8/9000781/c95ba6117730/molecules-27-02222-g006.jpg

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