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多环笼状杂环杂化物的半胱天冬酶依赖性凋亡活性。

Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids.

作者信息

Kumar Raju Suresh, Almansour Abdulrahman I, Arumugam Natarajan, Kotresha D, Balakrishna Janardhana Papayya

机构信息

Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.

Department of Botany, Davangere University, Shivagangothri, Davangere- 577007, Karnataka, India.

出版信息

Saudi J Biol Sci. 2020 Dec;27(12):3290-3300. doi: 10.1016/j.sjbs.2020.09.042. Epub 2020 Sep 25.

DOI:10.1016/j.sjbs.2020.09.042
PMID:33304134
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7715051/
Abstract

A small library of cage-like heterocyclic hybrids encompassing pyrroloisoquinolines, pyridinone and acenaphthene structural moieties have been synthesized and tested for their potential as anticancer agents against HCT116 and JURKAT cell lines. The results revealed that these cell lines are more sensitive towards compound and it showed dose dependent cytotoxic effect at 48 hrs of incubation. The IC values of compound against HCT116 and JURKAT cell lines are 12.14 ± 1.53 and 10.68 ± 0.68 µM, respectively. Further studies on the determination of mechanism of action of compound discovered that it brought the cell death by inducing Caspase 3 dependent apoptosis and also by arresting the cell cycle at S phase. These studies revealed that compound can be recommended as a potential anti-cancer agent.

摘要

已合成了一个包含吡咯并异喹啉、吡啶酮和苊结构部分的笼状杂环混合物小型文库，并测试了它们作为抗癌剂针对HCT116和JURKAT细胞系的潜力。结果显示，这些细胞系对化合物 更敏感，并且在孵育48小时时表现出剂量依赖性细胞毒性作用。化合物 针对HCT116和JURKAT细胞系的IC值分别为12.14±1.53和10.68±0.68μM。对化合物 作用机制的进一步研究发现，它通过诱导半胱天冬酶3依赖性凋亡以及使细胞周期停滞在S期来导致细胞死亡。这些研究表明，化合物 可被推荐为一种潜在的抗癌剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/5aaf15c177b6/gr11.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/1826ba3e9f0b/gr12.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/c4d224741570/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/855c9d84f77d/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/162b588f9ae3/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/e1f10bfcc16b/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/25aab68de589/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/d47db67f649a/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/259a4d88b01a/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/595b2b3456a1/gr8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/25d25c27c24c/gr9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/98909da9e7d1/gr10.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/5aaf15c177b6/gr11.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/1826ba3e9f0b/gr12.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/c4d224741570/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/855c9d84f77d/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/162b588f9ae3/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/e1f10bfcc16b/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/25aab68de589/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/d47db67f649a/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/259a4d88b01a/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/595b2b3456a1/gr8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/25d25c27c24c/gr9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/98909da9e7d1/gr10.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75e9/7715051/5aaf15c177b6/gr11.jpg

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