四种中药单体成分体外抑制沙眼衣原体作用的筛查

张燕; 鲜雨琦; 高磊琼; 沈犁; 华子瑜

doi:10.16016/j.1000-5404.201712245

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四种中药单体成分体外抑制沙眼衣原体作用的筛查

基础医学 | 更新时间：2026-01-09

- 四种中药单体成分体外抑制沙眼衣原体作用的筛查
- Comparison of inhibitory effects of 4 effective components of traditional Chinese drugs on Chlamydia trachomatis in vitro
- 第三军医大学学报 2018年40卷第14期页码：1271-1278
- 作者机构：
  
  重庆 400014，重庆医科大学附属儿童医院儿科研究所，儿童发育疾病研究教育部重点实验室；儿童发育重大疾病国家国际科技合作基地；儿科学重庆市重点实验室
- 作者简介：
  
  [华子瑜，E-mail: h_ziyu@163.com HUA Ziyu, E-mail: h_ziyu@163.com
- 基金信息：
  
  国家自然科学基金面上项目(81370777);重庆市卫生计生委中医药科技项目(ZY201702069)
- DOI：10.16016/j.1000-5404.201712245
  中图分类号： R285.5;R374.1
- 收稿：2017-12-27，
  
  修回：2018-04-13，
  
  纸质出版：2018-07-30
- 稿件说明：
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张燕, 鲜雨琦, 高磊琼, 等. 四种中药单体成分体外抑制沙眼衣原体作用的筛查[J]. 第三军医大学学报, 2018,40(14):1271-1278.

Yan ZHANG, Yuqi XIAN, Leiqiong GAO, et al. Comparison of inhibitory effects of 4 effective components of traditional Chinese drugs on Chlamydia trachomatis in vitro[J]. Journal of Third Military Medical University, 2018, 40(14): 1271-1278.
张燕, 鲜雨琦, 高磊琼, 等. 四种中药单体成分体外抑制沙眼衣原体作用的筛查[J]. 第三军医大学学报, 2018,40(14):1271-1278. DOI： 10.16016/j.1000-5404.201712245.

Yan ZHANG, Yuqi XIAN, Leiqiong GAO, et al. Comparison of inhibitory effects of 4 effective components of traditional Chinese drugs on Chlamydia trachomatis in vitro[J]. Journal of Third Military Medical University, 2018, 40(14): 1271-1278. DOI： 10.16016/j.1000-5404.201712245.

摘要

目的

利用沙眼衣原体(

Chlamydia trachomatis

Ct)菌株Ct-L2/PompA-GFP，快速筛查黄连素、雷公藤红素、黄芩苷、三羟黄酮体外抑制Ct作用。

方法

通过CCK-8检测药物细胞毒性作用，得出50%细胞毒性药物浓度(50% cytotoxic concentration，CC50)；通过菌株Ct-L2/PompA-GFP快速筛查四种中药体外抑制Ct的效果，得出50%抑制率药物浓度(50% inhibitory concentrations，IC50)；使用治疗指数(therapeutic index，TI)综合评估药物安全性和有效性。选择安全药物浓度(≥90%细胞存活率)，通过活细胞实时观察、免疫荧光染色和末端包涵体形成单位测定，再次确认药物的细胞毒性和体外抑制Ct作用。

结果

黄连素、雷公藤红素、黄芩苷、三羟黄酮的CC50(mean±SD)分别为(97.0±2.2)、(2.0±0.08)、(557.1±29.1)、(205.8±9.1)；IC50(mean±SD)分别为(2.73±0.09)、(0.60±0.02)、(260.0±10.2)、(60.9±3.8)；TI分别为35.5、3.3、2.1、3.4，提示黄连素更安全有效。黄连素、雷公藤红素、黄芩苷、三羟黄酮安全药物浓度分别为10.0、0.2、80.0、10.0 μmol/L，结果显示黄连素具有明显的Ct抑制作用(

＜0.000 1)，其他3种药物无明显抑制Ct作用。

结论

黄连素可能成为抑制Ct安全有效的药物。

Abstract

Objective

To compare the inhibitory effects of the effective components derived from 4 traditional Chinese drugs

namely berberine (BER)

celastrol (CEL)

baicalin

and baicalein

Chlamydia trachomatis

(Ct) Ct-L2/PompA-GFP strain

in vitro

Methods

CCK-8 assay was used to determine the 50% cytotoxic concentration (CC50) of the 4 agents in human cervical cancer HeLa 229 cells according to the dose-cytotoxicity curve. The inhibitory effect of each agent on Ct was estimated by observing the decrease in GFP intensity

and the 50% inhibitory concentration (IC50) of each agent was calculated based on the dose-inhibition curve. The therapeutic index (TI) was used to assess both the safety and efficacy of the 4 agents. Using the safe drug concentration (defined as a ≥90% cell viability in HeLa 229 cells)

the safety and efficacy of the agents for inhibiting Ct were further assessed by observing the live cells

immunofluorescence assay (IFA) and endpoint inclusion-forming unit assay (IFUs).

Results

The CC50s of BER

CEL

baicalin and baicalein were 97.0±2.2

2.0±0.08

557.1±29.1

and 205.8±9.1

respectively and their IC50s were 2.73±0.09

0.60±0.02

260.0±10.2

and 60.9±3.8

respectively. The TIs of BER

CEL

baicalin and baicalein were 35.5

3.3

2.1

and 3.4

respectively

showing a better safety and a stronger efficacy of BER among the 4 agents. The safe concentrations of BER

CEL

baicalin and baicalein in HeLa 229 cells were 10

0.2

and 10 μmol/L

respectively. The results showed that BER could markedly inhibit Ct (

0.0001)

while the other 3 agent did not produce obvious inhibitory effect on Ct.

Conclusion

BER can obviously inhibit Ct

in vitro

and may serve as a potent anti-chlamydia drug with a good safety profile.

关键词

Keywords

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