Cytotoxicity and Reactive Oxygen Species Related Mechanism on HepG2 Cells of Two Benzofuran Derivatives

ZHAO Jing; PU Li-ping; YANG Jing-tao; LIU Quan; GAO Qing-xiang; Wang Qin; WANG Chun-ming

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Cytotoxicity and Reactive Oxygen Species Related Mechanism on HepG2 Cells of Two Benzofuran Derivatives

更新时间：2024-01-04

- Cytotoxicity and Reactive Oxygen Species Related Mechanism on HepG2 Cells of Two Benzofuran Derivatives
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 16, Issue 16, Pages: 105-108(2010)
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- Published：2010
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ZHAO Jing, PU Li-ping, YANG Jing-tao, et al. Cytotoxicity and Reactive Oxygen Species Related Mechanism on HepG2 Cells of Two Benzofuran Derivatives[J]. Chinese journal of experimental traditional medical formulae, 2010, 16(16): 105-108.
DOI：

ZHAO Jing, PU Li-ping, YANG Jing-tao, et al. Cytotoxicity and Reactive Oxygen Species Related Mechanism on HepG2 Cells of Two Benzofuran Derivatives[J]. Chinese journal of experimental traditional medical formulae, 2010, 16(16): 105-108. DOI：

摘要

目的 :比较离舌橐吾Ligularia veitchiana (Hemsl.) Greenm的2种苯并呋喃衍生物5

6-二甲氧基-2-异丙基-苯并呋喃(5

6-dimethoxy-2-isopropenyl-benzofuran

化合物1)

5-乙酰基-6-甲氧基-2-异丙基-苯并呋喃(5-acetyl-6-methoxy-2-isopropenyl-benzofuran

化合物2)对人肝癌细胞HepG2和正常肝细胞L02的毒性

并分析其可能机制。方法: 用台盼蓝排染法检测化合物细胞毒性、用DCFH-DA荧光分光光度计法检测细胞活性氧含量、用钼酸铵比色法检测过氧化氢酶活性。结果: 化合物1和2对L02的IC50分别为(171.2±3.3)mg ·L-1和(79.0±4.1) mg ·L-1

高于对HepG2的IC50(84.2±6.5)mg ·L-1和(65.2±1.9) mg ·L-1

表明肿瘤细胞比正常细胞对化合物更加敏感。用化合物1和2 IC50处理细胞48 h

测得HepG2细胞活性氧分别是对照组的1.6倍和3.2倍;L02细胞活性氧分别是对照组的1.2倍和1.8倍。化合物1和2处理后

HepG2细胞过氧化氢酶活力分别从对照组的(17.2±1.7)U ·mg-1下降到(12.8±0.4)和(6.4±0.1)U ·mg-1;L02细胞过氧化氢酶活力分别从对照组的(17.7±1.2) U ·mg-1下降到(14.3±1.5)和(8.6±0.5)U ·mg-1;HepG2过氧化氢酶活力降低幅度大于L02。结论: 2个化合物对HepG2的毒性和活性氧的增幅均大于L02

同时HepG2过氧化氢酶活力降幅也大于L02。据此推测2个化合物细胞毒性与活性氧有关。

Abstract

Objective: This study was to evaluate the effect of two benzofuran derivatives on human liver hepatocellular carcinoma cells HepG2 and human hepatic L02 cells in vitro. Method: 5

6-dimethoxy-2-isopropenyl-benzofuran (compound 1) and 5-acetyl-6-methoxy-2-isopropenyl-benzofuran (compound 2) were isolated from Ligularia veitchiana (Hemsl.) Greenm.Trypan blue exclusion staining

7'-dichlorofluorescin diacetate(DCFH-DA) fluorescence spectrophotometry

and ammonium molybdate colorimetric assay were used to evaluate cytotoxicity

reactive oxygen species (ROS) generation

and catalase activity respectively. Result: The results showed that IC50 of compound 1 and 2 on L02 cells are (171.2±3.3) mg ·L-1 and (79.0±4.1) mg ·L-1

higher than that on HepG2

(84.2±6.5) mg ·L-1 and (65.2±1.9) mg ·L-1

exhibited more potent cytotoxic effect on tumor cells.After treated with the half inhibitory concentration (IC50) of compound 1 and 2 for 48 hours

ROS generated in HepG2 cells were 1.6 and 3.2 folds to the control group

and 1.2 and 1.8 folds in L02 cells respectively.Higher ROS generations in HepG2 cells than L02 were found.The catalase activity decreased from the control group (17.2±1.7) U ·mg-1 to (12.8±0.4) and (6.4±0.1) U ·mg-1 after treated with compound 1 and 2 in HepG2 cell respectively

and decreased from the control group (17.7±1.2) U ·mg-1 to (14.3±1.5) and (8.6±0.5) U ·mg-1 in L02 cells. Higher catalase activity reduced in HepG2 cells than L02. Conclusion: According to the more potent cytotoxicity

the ROS generation increasing in HepG2 than L02

and the decreasing of catalase activity in HepG2 cells

we suppose that the mechanism of the cytotoxicity for these two benzofuran deravatives may relate to ROS theory.

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