Antitumor effect and mechanism of total alkaloids of Gelsemium elegans and sempervirine in vitro
- VernacularTitle:钩吻总生物碱及常绿钩吻碱的体外抗肿瘤作用及机制
- Author:
Huixian CHEN
1
;
Wenyi WANG
2
;
Xinghui TAN
1
;
Gaopan LI
1
;
Xiaoqiong ZHANG
3
;
Desen LI
1
;
Shuisheng WU
1
Author Information
1. College of Pharmacy，Fujian University of Traditional Chinese Medicine，Fuzhou 350122，China
2. Innovation and Transformation Center，Fujian University of Traditional Chinese Medicine，Fuzhou 350122，China
3. Dept. of Pharmacy，Quanzhou Guangqian Hospital，Fujian Quanzhou 362321，China
- Publication Type:Journal Article
- Keywords:
Total alkaloids of Gelsemium elegans;
sempervirine;
antitumor;
apoptosis;
endoplasmic reticulum stress
- From:
China Pharmacy
2023;34(12):1437-1442
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To explore the antitumor effect and mechanism of total alkaloids of Gelsemium elegans （TA） and sempervirine （SPV） in vitro. METHODS The effects of low， medium and high concentrations of TA （50， 100， 200 μg/mL） and SPV （10， 30， 50 μmol/L） on the morphology of human hepatoma cells （HepG2， Bel-7402）， human lung cancer cells （A549） and human colon cancer cells （HCT-8） were observed， and the toxicity of TA and SPV to four tumor cells was monitored. The effects of TA and SPV on the contents of caspase-3 and caspase-9 in the supernatant of HCT-8 cells， the protein expressions of phosphorylated protein kinase B （p-Akt） （Thr308， Ser473）， B-cell lymphoma 2 （Bcl-2）， Bcl-2-related X protein （Bax）， survivin， C/EBP-homologous protein （CHOP）， immunoglobulin binding protein （Bip） and microtubule-associated protein 1 light chain 3Ⅱ （LC3Ⅱ） in HCT-8 cells were detected. RESULTS After the intervention of TA and SPV， the volume reduction and nuclear shrinkage were founded in four tumor cells； the cell activity decreased to varying degrees， among which TA and SPV had the best inhibitory effect on HCT-8 cells. After the intervention of TA and SPV， the contents of caspase-3 and caspase-9 in the supernatant of HCT-8 cells， the protein expressions of Bax， CHOP， Bip and LC3Ⅱ all increased to different degrees， while the protein expressions of p-Akt （Thr308， Ser473）， Bcl-2 and survivin in HCT-8 cells all decreased to different degrees. CONCLUSIONS TA and SPV have inhibitory effects on the above four tumor cells， and the inhibitory effect on HCT-8 cells is the best. The mechanism of their action on HCT-8 cells may be related to promoting apoptosis， activating endoplasmic reticulum stress and autophagy.
