Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of Rosuvastatin <italic style="font-style: italic">In Vivo</italic> and <italic style="font-style: italic">Vitro</italic><sup>△</sup>

Wen* Jin-hua; Wei Xiao-hua; Sheng Xiang-yuan; Zhou De-qing; Peng Hong-wei; Lu Yan-ni; Zhou Jian

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Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of Rosuvastatin In Vivo and Vitro^△

Chinese Medical Sciences Journal Vol. 30, Issue 4, Pages: 218-225(2015)

Orginal Article | Updated：2024-04-10

- Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of Rosuvastatin In Vivo and Vitro^△
- Affiliations：
  
  Department of Pharmacy, the First Affiliated Hospital of Nanchang University, Nanchang 330006, China
- Author bio：
- Funds：
- DOI：
  CLC：
- Published Online：20 August 2015，
  
  Published：2015-08
- Accepted：
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Wen* Jin-hua, Wei Xiao-hua, Sheng Xiang-yuan, et al. Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of Rosuvastatin In Vivo and Vitro^△[J]. Chinese medical sciences journal, 2015, 30(4): 218-225.
DOI：

Wen* Jin-hua, Wei Xiao-hua, Sheng Xiang-yuan, et al. Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of Rosuvastatin In Vivo and Vitro^△[J]. Chinese medical sciences journal, 2015, 30(4): 218-225. DOI：

摘要

Abstract

Objective

To evaluate whether ursolic acid can inhibit breast cancer resistance protein (BCRP)-mediated transport of rosuvastatin

in vivo

and

in vitro

Methods

Firstly

we explored the pharmacokinetics of 5-fluorouracil (5-FU

a substrate of BCRP) in rats in the presence or absence of ursolic acid. Secondly

we studied the pharmacokinetics of rosuvastatin in rats in the presence or absence of ursolic acid or Ko143 (inhibitor of BCRP). Finially

the concentration-dependent transport of rosuvastatin and the inhibitory effects of ursolic acid and Ko143 were examined in Madin-Darby Canine Kidney (MDCK) Ⅱ-BCRP421CC (wild type) cells and MDCKⅡ-BCRP421AA (mutant type) cells.

Results

As a result

significant changes in pharmacokinetics parameters of 5-FU were observed in rats following pretreatment with ursolic acid. Both ursolic acid and Ko143 could significantly affect the pharmacokinetics of rosuvastatin. The rosuvastatin transport in the BCRP overexpressing system was increased in a concentration-dependent manner. However

there was no statistical difference in BCRP-mediated transport of rosuvastatin betweent the wild type cells and mutant cells. The same as Ko143

ursolic acid inhibited BCRP-mediated transport of rosuvastatin

in vitro

Conclusion

Ursolic acid appears to be a potent modulator of BCRP that affects the pharmacokinetic of rosuvastatin

in vivo

and inhibits the transport of rosuvastatin

in vitro

关键词

Keywords

references

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Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of Rosuvastatin In Vivo and Vitro△

DOI：

摘要

Abstract

关键词

Keywords

references

Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of Rosuvastatin In Vivo and Vitro^△