1.福建中医药大学药学院,福州 350122
2.福建中医药大学科技创新与转化中心,福州 350122
3.泉州光前医院药剂科,福建 泉州 362321
Received:11 January 2023,
Revised:2023-06-02,
Accepted:07 June 2023,
Published:30 June 2023
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陈惠娴,王文义,檀兴慧,等.钩吻总生物碱及常绿钩吻碱的体外抗肿瘤作用及机制[J].中国药房,2023,34(12):1437-1442.
CHEN Huixian,WANG Wenyi,TAN Xinghui,et al.Antitumor effect and mechanism of total alkaloids of Gelsemium elegans and sempervirine in vitro[J].ZHONGGUO YAOFANG,2023,34(12):1437-1442.
陈惠娴,王文义,檀兴慧,等.钩吻总生物碱及常绿钩吻碱的体外抗肿瘤作用及机制[J].中国药房,2023,34(12):1437-1442. DOI: 10.6039/j.issn.1001-0408.2023.12.06.
CHEN Huixian,WANG Wenyi,TAN Xinghui,et al.Antitumor effect and mechanism of total alkaloids of Gelsemium elegans and sempervirine in vitro[J].ZHONGGUO YAOFANG,2023,34(12):1437-1442. DOI: 10.6039/j.issn.1001-0408.2023.12.06.
目的
2
探讨钩吻总生物碱(TA)和常绿钩吻碱(SPV)的体外抗肿瘤作用及机制。
方法
2
观察低、中、高浓度TA(50、100、200 μg/mL)和SPV(10、30、50 μmol/L)对人肝癌细胞(HepG2、Bel-7402)、人肺癌细胞(A549)、人结肠癌细胞(HCT-8)形态的影响并实时监测TA和SPV对4种肿瘤细胞的毒性;检测TA和SPV对HCT-8细胞上清液中胱天蛋白酶3(caspase-3)、caspase-9含量和细胞中磷酸化蛋白激酶B(p-Akt)(Thr308、Ser473)、B细胞淋巴瘤2(Bcl-2)、Bcl-2相关X蛋白(Bax)、生存素、C/EBP-同源蛋白(CHOP)、免疫球蛋白结合蛋白(Bip)、微管相关蛋白1轻链3Ⅱ(LC3Ⅱ)蛋白表达的影响。
结果
2
TA和SPV干预后的4种肿瘤细胞形态均出现体积缩小、细胞核皱缩的现象,细胞活性均出现不同程度的降低,其中TA和SPV对HCT-8细胞的抑制效果最好。TA和SPV干预后的HCT-8细胞上清液中caspase-3、caspase-9含量和细胞中Bax、CHOP、Bip、LC3Ⅱ蛋白表达水平均不同程度升高,p-Akt(Thr308、Ser473)、Bcl-2、生存素蛋白表达水平均不同程度降低。
结论
2
TA和SPV对上述4种肿瘤细胞均具有抑制作用,其对HCT-8细胞的抑制效果最好;二者对HCT-8细胞的作用机制可能与促进细胞凋亡、激活内质网应激和细胞自噬有关。
OBJECTIVE
2
To explore the antitumor effect and mechanism of total alkaloids of
Gelsemium elegans
(TA) and sempervirine (SPV)
in vitro
.
METHODS
2
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
2
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
2
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.
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