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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
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY
ISSN0968-0896
Volume29Pages:115849
AbstractNeothalfine 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.
KeywordNeothalfine Bisbenzylisoquinoline alkaloid Metastatic colorectal cancer Metabolomic Mitochondrial apoptosis SMALL MOLECULES IRINOTECAN RESISTANCE CELL IMMUNOTHERAPY OPPORTUNITIES CHEMOTHERAPY VINORELBINE ALKALOIDS PATHWAY
DOI10.1016/j.bmc.2020.115849
WOS IDWOS:000612172300009
Citation statistics
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/73730
Collection中国科学院昆明植物研究所
Affiliation1.[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
Recommended Citation
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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