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白头翁中的 23-羟基白桦酸(Bunge)与多柔比星在体内外协同抗肿瘤活性。

23-Hydroxybetulinic acid from Pulsatilla chinensis (Bunge) Regel synergizes the antitumor activities of doxorubicin in vitro and in vivo.

机构信息

Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, Jiangsu, China.

出版信息

J Ethnopharmacol. 2010 Apr 21;128(3):615-22. doi: 10.1016/j.jep.2010.02.004. Epub 2010 Feb 20.

Abstract

UNLABELLED

ETHNOPHARMACOLOGICAL REVELANCE: Pulsatilla chinensis (Bunge)Regel has been used as adjuvant in chemotherapy in traditional Chinese medicine. 23-Hydroxybetulinic acid, an isolated pentacyclic triterpene, is the major active constituent of Pulsatilla chinensis (Bunge) Regel.

AIM OF THIS STUDY

To evaluate the combinational anticancer effect of 23-hydroxybetulinic acid and doxorubicin in vitro and in vivo.

MATERIALS AND METHODS

The effect of combination treatment with 23-hydroxybetulinic acid and doxorubicin was evaluated with a quantitative combination index method based on the median-effect analysis in various cancer cell lines. And in vivo efficacy of combination chemotherapy was also evaluated using ICR mice bearing sarcoma 180 carcinoma tumors.

RESULTS

23-Hydroxybetulinic acid showed a synergistic cytotoxic effect on multiple cancer cell lines by combined use with doxorubicin. In vivo studies further demonstrated that co-administration of 23-HBA significantly improved the sensitivity of the tumor to doxorubicin through increasing intra-tumor doxorubicin concentration and inhibiting doxorubicin-induced up-regulation of P-gp in tumor.

CONCLUSION

These results suggest that the combined therapy with 23-hydroxybetulinic acid and doxorubicin may be a new promising strategy to promote the clinical chemotherapy, which needs further verification.

摘要

目的

评估 23-羟基白桦酸与阿霉素联合在体内外的抗癌作用。

材料和方法

采用基于中值效应分析的定量组合指数方法,评估 23-羟基白桦酸与阿霉素联合治疗的效果,在各种癌细胞系中。并采用 ICR 小鼠肉瘤 180 荷瘤模型评估联合化疗的体内疗效。

结果

23-羟基白桦酸与阿霉素联合使用对多种癌细胞系具有协同细胞毒性作用。体内研究进一步表明,23-HBA 的联合给药通过增加肿瘤内阿霉素浓度和抑制阿霉素诱导的 P-糖蛋白在肿瘤中的上调,显著提高了肿瘤对阿霉素的敏感性。

结论

这些结果表明,23-羟基白桦酸与阿霉素联合治疗可能是一种提高临床化疗效果的新策略,值得进一步验证。

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