转染结构性雄烷受体CAR对MMC和629的辐射增敏性的影响

张江虹; 郝福荣; 金一尊

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转染结构性雄烷受体CAR对MMC和629的辐射增敏性的影响

核化学、放射性药物和核医学 | 更新时间：2021-03-12

- 转染结构性雄烷受体CAR对MMC和629的辐射增敏性的影响
- Effect of constitutive androstane receptor on radiosensitization of mictomycin C and its homologoue—629
- 核技术 2008年31卷第8期
- 作者机构：
  
  1. 复旦大学放射医学研究所
  2. 潍坊市人民医院
- 作者简介：
- 基金信息：
  
  国家自然科学基金（30400089）资助()
- DOI：
  中图分类号： R730.5
- 纸质出版日期：2008-08-01
- 稿件说明：
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[1]张江虹,郝福荣,金一尊.转染结构性雄烷受体CAR对MMC和629的辐射增敏性的影响[J].核技术,2008,31(08):619-624.

ZHANG Jianghong1 HAO Furong2 JIN Yizun1 1. Effect of constitutive androstane receptor on radiosensitization of mictomycin C and its homologoue—629[J]. Nuclear techniques, 2008, 31(8): 619-624.
[1]张江虹,郝福荣,金一尊.转染结构性雄烷受体CAR对MMC和629的辐射增敏性的影响[J].核技术,2008,31(08):619-624. DOI：

ZHANG Jianghong1 HAO Furong2 JIN Yizun1 1. Effect of constitutive androstane receptor on radiosensitization of mictomycin C and its homologoue—629[J]. Nuclear techniques, 2008, 31(8): 619-624. DOI：

摘要

研究了丝裂霉素C（Mictomycin C

MMC）及其衍生物5-氮丙啶-3-羟甲基-1-甲基吲哚-4

7-二酮（5-（aziridin-1-yl）-3-hydroxymethyl-1-methylindole-4

7-dione

629）的乏氧辐射增敏效应

以及转染结构性雄烷受体（Constitutive androstane receptor

CAR）对它们的生物学效应的影响。采用RT-PCR（Reverse Transcriptase PCR）检测HepG2和g2car细胞中CAR mRNA和CYP2B6 mRNA的表达

应用体外细胞克隆培养法评价MMC和629对HepG2和g2car细胞在有氧和乏氧条件下的辐射增敏效应。同时

应用流式细胞技术检测629对两种细胞周期和细胞凋亡情况的影响。结果显示:在乏氧情况下

MMC和629对HepG2细胞的辐射增敏效应均高于单纯乏氧组

低于单纯有氧组

并且629的辐射增敏效应高于其母体化合物MMC

转染CAR后

两者的辐射增敏效应均增加;629在低浓度时对细胞周期和细胞凋亡的影响不大

高浓度时可改变细胞周期和诱导细胞凋亡的发生。表明:629较其母体化合物MMC具有较高的辐射增敏效应

并且转染CAR基因可在转录水平调节药物的代谢

以增加细胞的辐射增敏效应。

Abstract

The object of this work is to evaluate radiosensitization of MMC and its analogue 5-(aziridin-1-yl)-3- hydroxymethyl-1-methylindole-4

7-dione(629) and how transfection of constitutive androstane receptor (CAR) affect their biological effects. The expressions of CAR mRNA and CYP2B6 mRNA in HepG2 cells and g2car cells were detected by RT-PCR. The radiosensitization of MMC and 629 in vitro were evaluated in HepG2 cells and g2car cells by colony formation under anaerobic and aerobic condition. The effect of 629 on cell cycle and apoptosis of HepG2 cells and g2car cells were assayed by flow cytometry. It was found that plasmid mCAR1/pCR3 was transfected into g2car cells successfully and target CYP2B6 was transactivated by CAR. To compare with aerobic and anaerobic

the radiosensitization of MMC and 629 to HepG2 cells and g2car cells had significantly enhanced

the radiosensitization of 629 was stronger than its parent compound—MMC under aerobic and anaerobic condition

and transfect CAR gene could improve the radiosensitization of MMC and 629. Furthermore

CYP2B6 is one master enzyme for the metabolism of MMC and 629. Transfection of CAR can increase expression of CYP2B6 mRNA in HepG2 cells

and can affect radiosensitization of MMC and 629.

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