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柏科植物双黄酮类化合物作为干预非小细胞肺癌的潜在抗肿瘤药物。

Biflavonoids from as Potential Antitumor Agents for Intervention of Non-Small Cell Lung Cancer.

机构信息

Xiangya School of Pharmaceutical Sciences, Central South University, Changsha 410013, China.

Xiangya Hospital of Central South University, Changsha 410008, China.

出版信息

Molecules. 2021 Sep 5;26(17):5401. doi: 10.3390/molecules26175401.

DOI:10.3390/molecules26175401
PMID:34500834
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8434134/
Abstract

Four new biflavonoids (-) were isolated from together with a known biflavonoid derivative (). Their structures contained a rare linker of individual flavones to each other by direct C-3-O-C-4''' bonds, and were elucidated by extensive spectroscopic data, including HRESIMS, NMR and ECD data. All isolates significantly inhibited the proliferation of NSCLC cells (IC = 2.3-8.4 μM) with low toxicity to non-cancer MRC-5 cells, superior to the clinically used drug DDP. Furthermore, the most active compound suppressed XIAP and survivin expression, promoted upregulation of caspase-3/cleaved-caspase-3, as well as induced cell apoptosis and cycle arrest in A549 cells. Together, our findings suggest that may be worth studying further for intervention of NSCLC.

摘要

从 中分离得到四个新的二氢黄酮类化合物 (-),以及一个已知的二氢黄酮类衍生物 ()。它们的结构包含通过直接 C-3-O-C-4'''键将单体黄酮彼此连接的罕见连接子,并通过广泛的光谱数据,包括 HRESIMS、NMR 和 ECD 数据进行阐明。所有分离物均显著抑制 NSCLC 细胞的增殖(IC = 2.3-8.4 μM),对非癌细胞 MRC-5 的毒性较低,优于临床使用的药物顺铂。此外,最活跃的化合物 抑制 XIAP 和 survivin 的表达,促进 caspase-3/cleaved-caspase-3 的上调,并诱导 A549 细胞凋亡和周期停滞。总之,我们的研究结果表明, 可能值得进一步研究以干预 NSCLC。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/a73b93469649/molecules-26-05401-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/7625e84be625/molecules-26-05401-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/f5d1c6431586/molecules-26-05401-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/b7897a74b9cc/molecules-26-05401-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/8731e16ee124/molecules-26-05401-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/ed9775573ab2/molecules-26-05401-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/c97b5fe90c53/molecules-26-05401-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/93aeecdfa347/molecules-26-05401-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/7164d1ac70fb/molecules-26-05401-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/a73b93469649/molecules-26-05401-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/7625e84be625/molecules-26-05401-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/f5d1c6431586/molecules-26-05401-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/b7897a74b9cc/molecules-26-05401-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/8731e16ee124/molecules-26-05401-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/ed9775573ab2/molecules-26-05401-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/c97b5fe90c53/molecules-26-05401-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/93aeecdfa347/molecules-26-05401-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/7164d1ac70fb/molecules-26-05401-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3810/8434134/a73b93469649/molecules-26-05401-g009.jpg

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