Neothalfine, a potent natural anti-tumor agent against metastatic colorectal cancer and its primary mechanism

doi:10.1016/j.bmc.2020.115849

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	Neothalfine, a potent natural anti-tumor agent against metastatic colorectal cancer and its primary mechanism
	Zhu,Yan-Yan ; Jin,Qiong ; Chen,Shan-Shan ; Jin,Dan-Ni ; Wang,Zhao-Jie ; He,Ying-Jie ; Chen,Hui-Cheng ; Zhao,Yun-Li ; Zhao,Li-Xing ; Dai,Zhi ; Luo,Xiao-Dong
	2021
发表期刊	BIOORGANIC & MEDICINAL CHEMISTRY
ISSN	0968-0896
卷号	29 页码:115849
摘要	Neothalfine is a natural bisbenzylisoquinoline alkaloid with the abundant resource in medicinal plants and has not been reported its anti-tumor efficacy. In the present study, the anti-tumor efficacy was investigated and it showed broad-spectrum activity against several cancer cell lines, especially metastatic colorectal cancer (HCT116, SW620, T84) with the IC50 values of 7.2, 5.9, 8.2 nM, respectively, roughly equal to well-known antitumor agent docetaxel (4.0, 4.7, 2.7 nM) and nearly 1000 folds than CPT-11 (4.4, 5.1, 6.9 mu M). Furthermore, neothalfine inhibited colorectal cell proliferation by resulting in cell cycle arrest at the G2/M phase and induced apoptosis through the dysfunction of mitochondria to trigger intrinsic apoptotic pathway by untargeted metabolomic method, mitochondrial membrane potential, and caspase-3/7 activity assay. Moreover, neothalfine damaged colorectal cancer clonal spheres expansion significantly at the concentration of 3.5 nM with nearly 1000 folds efficacy than CPT-11 (3.0 mu M). The results supported that neothalfine might be an anti-tumor lead for further investigation.
关键词	Neothalfine Bisbenzylisoquinoline alkaloid Metastatic colorectal cancer Metabolomic Mitochondrial apoptosis SMALL MOLECULES IRINOTECAN RESISTANCE CELL IMMUNOTHERAPY OPPORTUNITIES CHEMOTHERAPY VINORELBINE ALKALOIDS PATHWAY
DOI	10.1016/j.bmc.2020.115849
WOS记录号	WOS:000612172300009
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/73730
专题	中国科学院昆明植物研究所
作者单位	1.[Zhu, Yan-Yan 2.Chen, Shan-Shan 3.Jin, Dan-Ni 4.Wang, Zhao-Jie 5.He, Ying-Jie 6.Chen, Hui-Cheng 7.Zhao, Yun-Li 8.Zhao, Li-Xing 9.Dai, Zhi 10.Yunnan Univ, Sch Chem Sci & Technol, Key Lab Med Chem Nat Resource, Minist Educ & Yunnan Prov, Kunming 650091, Yunnan, Peoples R China 11.[Jin, Qiong 12.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China
推荐引用方式 GB/T 7714	Zhu,Yan-Yan,Jin,Qiong,Chen,Shan-Shan,et al. Neothalfine, a potent natural anti-tumor agent against metastatic colorectal cancer and its primary mechanism[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2021,29:115849.
APA	Zhu,Yan-Yan.,Jin,Qiong.,Chen,Shan-Shan.,Jin,Dan-Ni.,Wang,Zhao-Jie.,...&Luo,Xiao-Dong.(2021).Neothalfine, a potent natural anti-tumor agent against metastatic colorectal cancer and its primary mechanism.BIOORGANIC & MEDICINAL CHEMISTRY,29,115849.
MLA	Zhu,Yan-Yan,et al."Neothalfine, a potent natural anti-tumor agent against metastatic colorectal cancer and its primary mechanism".BIOORGANIC & MEDICINAL CHEMISTRY 29(2021):115849.

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