...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Journal of Pharmacy and Pharmaceutical Sciences >Interactions between Phytochemical Components of Sutherlandia Frutescens and the Antiretroviral, Atazanavir In Vitro: Implications for Absorption and Metabolism
【24h】

Interactions between Phytochemical Components of Sutherlandia Frutescens and the Antiretroviral, Atazanavir In Vitro: Implications for Absorption and Metabolism

机译：萨尔兰氏植物植物和抗逆转录病毒，atazanavir在体外相互作用：吸收和代谢的影响

获取原文
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Purpose. African traditional medicinal plants, such as Sutherlandia frutescens have the potential to interact pharmacokinetically with the protease inhibitor class of antiretrovirals, thereby impacting on their safety and efficacy. The effects of extracts and phytochemical components of Sutherlandia frutescens, on the in vitro absorption and metabolism of the protease inhibitor, atazanavir were thus investigated. Methods. Aqueous and methanolic extracts of Sutherlandia frutescens were prepared by freeze-drying of hot water and methanol decoctions of Sutherlandia frutescens plant material respectively, whilst crude triterpenoid glycoside and flavonol glycoside fractions were isolated by solvent extraction and subsequent column chromatography. Atazanavir was quantitated in the absence or presence of these compounds as well as commercially available purported constituents of Sutherlandia frutescens, namely, L-canavanine, L-GABA and D-pinitol, after a one hour co-incubation in Caco-2 cell monolayers and human liver microsomes. Results. The triterpenoid and flavonol glycoside fractions were found to be present in the aqueous and methanolic extracts of Sutherlandia frutescens and were shown to contain the sutherlandiosides and sutherlandins known to be present in Sutherlandia frutescens. The aqueous extract and D-pinitol significantly reduced atazanavir accumulation by Caco-2 cells, implying a decrease in atazanavir absorption, whilst the opposite was true for the triterpenoid glycoside fraction. Both the aqueous and methanolic extracts inhibited atazanavir metabolism in human liver microsomes, whilst enhanced atazanavir metabolism was exhibited by the triterpenoid glycoside fraction. Conclusions. The extracts and phytochemical components of Sutherlandia frutescens influenced the accumulation of atazanavir by Caco-2 cells and also affected ATV metabolism in human liver microsomes. These interactions may have important implications on the absorption and metabolism and thus the overall oral bioavailability of atazanavir. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on on the issue’s contents page.
机译：目的。非洲传统药用植物，如Sutherlandia Frutescens有可能用蛋白酶抑制剂类的抗逆转录患者药代动力学，从而影响它们的安全性和功效。因此，研究了Sutherlandia Frutescens的提取物和植物化学成分对蛋白酶抑制剂的体外吸收和代谢的影响。方法。通过分别冷冻干燥的热水和甲醇煎蛋醛酸盐的含水水和甲醇煎蛋醛分离，溶剂萃取和随后的柱色谱分离，通过腐牛草糖糖苷和黄酮醇糖苷级分分离，制备Sutherlandia Frutescens的水和甲醇溶液。在缺乏或存在这些化合物的情况下定量Atazanavir以及商业上可获得的Suthlandia Frutescens，即L- Canavanine，L-GABA和D-吡啶醇，在Caco-2细胞单层的一小时共培养后，人肝微粒体。结果。发现三萜和黄酮醇序列存在于萨尔兰·弗劳擦的含水和甲醇醇中，并且被证明含有撒丁香族和乳兰蛋白蛋白，并在萨尔兰菊属植物中存在。通过Caco-2细胞，水性提取物和D-吡啶醇显着降低了Atazanavir积累，暗示Atazanavir吸收的减少，而Triterpenoid糖苷级分相反。含水和甲醇醇提取物抑制了人肝微粒体的亚扎沙昔韦代谢，而Triterpenoid糖苷级分呈现出增强的Atazanavir代谢。结论。 Sutherlandia Frutescens的提取物和植物化学成分影响了Caco-2细胞的Atazanavir积累，并且在人肝微粒体中影响了ATV代谢。这些相互作用可能对吸收和新陈代谢具有重要意义，从而具有Atazanavir的整体口服生物利用度。本文对发布后审查开放。注册读者（参见“对于读者”）可以通过单击“问题的内容”页面进行评论。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号