Suppr超能文献

三种天然他汀类药物从内酯形式向相应羟基酸形式的转化及其在普洱茶中的测定研究

Study on the conversion of three natural statins from lactone forms to their corresponding hydroxy acid forms and their determination in Pu-Erh tea.

作者信息

Yang Deng-Jye, Hwang Lucy Sun

机构信息

Department of Health Diet and Restaurant Management, Chung Shan Medical University, Taichung, Taiwan.

出版信息

J Chromatogr A. 2006 Jun 30;1119(1-2):277-84. doi: 10.1016/j.chroma.2005.12.031. Epub 2006 Jan 18.

Abstract

Conversions of statins, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors, from lactone forms to their corresponding hydroxy acid form in 0.1 N NaOH or 0.05 N KOH (prepared with 25, 50, 75, 90% acetonitrile or methanol in water or 100% water) were evaluated. Results showed that lactone form statins could be transformed almost completely only in alkaline solutions prepared with 25 or 50% acetonitrile. In all methanolic alkaline solutions, lactone form statins could also be converted entirely, nevertheless, they would be further transformed to the methyl ester of the hydroxy acid form and the transformation increased as methanol rises. When lactone and hydroxy acid forms of statins were in methanol, ethyl acetate, 70% acetonitrile in water (with 0.5% acetic acid or no) for 0-48 h at room temperature or in 100 degrees C water for 0-2 h, lactone form statins were converted to their corresponding hydroxy acids, which were raised as time extends and the highest conversions of them were about 35% in 100 degrees C water and 70% acetonitrile, slightly transformed for lactone form statins in 70% acetonitrile (with 0.5% acetic acid) after 8 h, and the other treatments for all statins showed no significant changes. Interferences would be reduced efficiently when statins were extracted from Pu-Erh tea with methanol, ethyl acetate or 100 degrees C water followed by purifying through a C18 solid-phase extraction cartridge. Lovastatin was the only statin found in Pu-Erh tea and the highest content of it was found under ethyl acetate extraction. In ethyl acetate and methanol extracts, lovastatin existed merely as lactone form. The lowest content of lovastatin was found in the 100 degrees C water extract of Pu-Erh tea, however, both of lactone and hydroxy acid forms were found to exist in the extract.

摘要

对他汀类药物(3-羟基-3-甲基戊二酰辅酶A(HMG-CoA)还原酶抑制剂)在0.1 N NaOH或0.05 N KOH(用25%、50%、75%、90%乙腈或甲醇与水混合或100%水配制)中从内酯形式转化为相应的羟基酸形式进行了评估。结果表明,内酯形式的他汀类药物几乎只能在用25%或50%乙腈配制的碱性溶液中完全转化。在所有甲醇碱性溶液中,内酯形式的他汀类药物也能完全转化,不过,它们会进一步转化为羟基酸形式的甲酯,且随着甲醇比例升高转化程度增加。当他汀类药物的内酯和羟基酸形式在甲醇、乙酸乙酯、70%乙腈水溶液(含或不含0.5%乙酸)中于室温下放置0至48小时,或在100℃水中放置0至2小时时,内酯形式的他汀类药物会转化为相应的羟基酸,且随着时间延长转化率升高,在100℃水中和70%乙腈中的最高转化率约为35%,在70%乙腈(含0.5%乙酸)中8小时后内酯形式的他汀类药物略有转化,而其他处理对所有他汀类药物均无显著变化。当用甲醇、乙酸乙酯或100℃水从普洱茶中提取他汀类药物,然后通过C18固相萃取柱纯化时,干扰会有效降低。洛伐他汀是普洱茶中唯一检测到的他汀类药物,乙酸乙酯萃取时其含量最高。在乙酸乙酯和甲醇提取物中,洛伐他汀仅以内酯形式存在。普洱茶100℃水提取物中洛伐他汀含量最低,不过提取物中同时存在内酯和羟基酸两种形式。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验