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Anti-tumor activity screening and research on the primary mechanism of dicumarol in vitro
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Jing WEI1, Yue-ping FENG1, Xi ZHENG2, Qin WANG1, Chun ZHANG1, *
Acta Pharmaceutica Sinica | 2020, 55(12) : 2904 - 2910
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Acta Pharmaceutica Sinica | 2020, 55(12): 2904-2910
Original Articles
Anti-tumor activity screening and research on the primary mechanism of dicumarol in vitro
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Jing WEI1, Yue-ping FENG1, Xi ZHENG2, Qin WANG1, Chun ZHANG1, *
Affiliations
  • 1. Department of Pharmacy, Southwest Medical University, Luzhou 646000, China
  • 2. Sichuan Vacotional College of Health and Rehabilitation, Zigong 643000, China
Published: 2020-12-12 doi: 10.16438/j.0513-4870.2020-0598
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To study the anti-tumor activities and the related mechanisms of dicumarol, the CCK-8 method was used to identify anti-tumor activities of dicumarol. HepG2 cells were used to explore the anti-tumor mechanisms by measuring several physiological and biochemical indexes. The results show that dicumarol can significantly inhibit the growth of HepG2, Hccc-9810 and MDA-MB-231 cell lines in a dose-dependent and time-dependent manner, with HepG2 cells showing the greatest sensitivity to dicumarol (with an IC50 value of 3.19±0.68 µmol·L-1 at 48 h). Dicumarol arrested the cell cycle at S phase and down-regulated the expression of anti-apoptotic protein Bcl-2 while promoting the expression of the pro-apoptotic proteins Bax and cleaved caspase-9. Dicumarol significantly decreased the levels of glutathione (GSH) and superoxide dismutase (SOD) in HepG2 cells, and increased the levels of malonaldehyde (MDA) and reactive oxygen species (ROS). Dicumarol also down-regulated the protein levels of NAD(P)H quinone oxidoreductase 1, 3-phosphoinositide-dependent protein kinase 1, and hypoxia inducible factor-1α under hypoxic conditions. The above results show that dicumarol can inhibit the proliferation of HepG2 cells and induce cycle arrest and apoptosis. Dicumarol may down-regulate the expression of HIF-1α by inhibiting the activity of NQO1 and PDK1, which leads to the accumulation of ROS, thereby generating oxidative stress and inducing apoptosis in HepG2 cells.

dicumarol  /  HepG2  /  apoptosis  /  cell cycle  /  oxidative stress
Jing WEI, Yue-ping FENG, Xi ZHENG, Qin WANG, Chun ZHANG. Anti-tumor activity screening and research on the primary mechanism of dicumarol in vitro[J]. Acta Pharmaceutica Sinica, 2020 , 55 (12) : 2904 -2910 . DOI: 10.16438/j.0513-4870.2020-0598
Year 2020 volume 55 Issue 12
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Article Info
doi: 10.16438/j.0513-4870.2020-0598
  • Receive Date:2020-04-21
  • Online Date:2026-01-23
  • Published:2020-12-12
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  • Received:2020-04-21
  • Revised:2020-06-17
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    1. Department of Pharmacy, Southwest Medical University, Luzhou 646000, China
    2. Sichuan Vacotional College of Health and Rehabilitation, Zigong 643000, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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