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茴三硫的代谢产物及其相互转化研究 被引量:2

Anethol trithione metabolites and their mutual transformation
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摘要 目的:研究茴三硫的代谢产物及其相互转化。方法:采用大鼠肝微粒体体外温孵,结合液相色谱质谱联用技术推测代谢物结构,并用高效液相色谱法测定原型药物与代谢产物的相互转化关系。结果:温孵体系中,茴三硫迅速脱甲基代谢为对羟基苯基三硫酮,并且均存在氧化产物,随后茴三硫及其氧化产物峰面积之和与代谢物对羟基苯基三硫酮及其氧化产物的峰面积之和是基本恒定的,而这时原型药物及3种代谢产物峰面积随时间的变化,是由于原型药物及脱甲基代谢物的氧化产物在温孵体系中被重新还原所引起的。结论:在体外温孵体系中,茴三硫存在脱甲基化、氧化和氧化产物的再还原3种反应。 Objective: To study anethol trithione metabolites and their mutual transformation. Methods: Rat liver microsomes were incubated in vitro. The metabolite structures were determined by liquid chromatography combined with mass spectrometry. Concentrations of the drug and metabolites were detected by high performance liquid chromatography to clarify the relationship of their mutual transformation. Results: In the in vitro incubation system, anethol trithione was rapidly demethylated and converts to 4-hydroxy-anethol trithione. The oxidation prod- ucts of both anethol trithione and 4-hydroxy-anethol trithione existed as well. The peak areas of anethol trithione, 4- hydroxy-anethol trithione and their oxidation products was basically constant. Meanwhile the peak areas of anethol trithione and its three metabolites were varying due to reduction of the oxidation products of anethol trithione and its demethylated metabolites. Conclusion: Three metabolic pathways of anethol trithione, namely demethylation, oxi- dation and reduction of the oxidation products, have been detected in the in vitro incubation system.
出处 《中国新药杂志》 CAS CSCD 北大核心 2013年第19期2328-2331,共4页 Chinese Journal of New Drugs
关键词 茴三硫 对羟基苯基三硫酮 代谢产物 anethol trithione hydroxyphenyl thione metabolites
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  • 1余佳芮,蒋学华,杨俊毅.HPLC测定人血浆中茴三硫浓度[J].药物分析杂志,2005,25(8):970-971. 被引量:7
  • 2DANIEL M, AMOR S, PATRICK M. Dansette, michel plat, a new potent inhibitor of lipid peroxidation in vitro and in vivo, the hepatoprotective drug anisyldithol thione [ J ]. Biochem Biophy Res Comun, 1986,135 (2) : 1015-1021.
  • 3Bagheri H,Schmitt L,Berlan M,et al.A comparative study of the effects of yohimbine and anethol trithione on salivary secretion in depressed patients treated with psychotropic drugs.Eur J Clin Pharmacol,1997,52:339.
  • 4Hamada T,Nakane T,Kimura T,et al.Treatment of xerostomia with the bile secretion-stimulating drug anethole trithione:a clinical trial.Am J Med Sci,1999,318:146.
  • 5Gmelin R,Lagler F.Vertr glichkeit und Ausschidung von Anethotrithion.Arzneim Forsch,1963,13:130.
  • 6Jing Qiufang,Shen Yongjia,Ren Fuzheng,et al,HPLC determination of anethole trithione and its application to pharmacokinetics in rabbits.J Pharm Biomed Anal,(2006,42:613.
  • 7Woodworth JR,Dennis RK,Hinsvark ON,et al.Bioavailability evaluation of a controlled-release dextromethorphan liquid.J Clin Pharmacol,1987,27(2):133.
  • 8Pfaff G,Briegel P,Lamprecht I.Inter-individual variation in the metabolism of dextromethorphan.Int J Pharm,1983,14(2-3):173.
  • 9陈新谦,金有豫,汤光.新编药物学[M].15版,北京:人民卫生出版社,2003:479.
  • 10BAGHERI H, SCHMITT L, BERLAN M. et al. A comparative study of the effects of yohimbine and anethole trithione on salivary secretion in depressed patients treated with psychotropic drugs [J]. Eur J Clin Pharmacol, 1997, 52(5) :339 -42.

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  • 1刘春晖,林巧平,山莽挺,祁智,许向阳.茴三硫固体分散体的体内外评价[J].中国现代应用药学,2013,30(1):47-52. 被引量:3
  • 2刘绛光,王俊敏,何应.微乳在口服多肽类药物中的应用[J].中国生化药物杂志,2006,27(1):56-58. 被引量:8
  • 3毕崇才,张兰荣,朱红玲.国产环戊硫酮片对生理性口干症的疗效观察[J].中国老年学杂志,2006,26(10):1405-1406. 被引量:6
  • 4刘春晖,陈云,于霞,许向阳.茴三硫微粉化片剂的研制[J].海峡药学,2007,19(4):21-23. 被引量:4
  • 5SHARMA S ,PU G,VERNON E S. Quantitative mor- phometry of respiratory tract epithelial cells as a tool for testing chemopreventive agent efficacy [ J ]. Anti- cancer Research,2010,30 ( 3 ) :737 - 742.
  • 6KHOSROW K, KENNETH R O. Biology and thera- peutic potential of hydrogen sulfide and hydrogen sul- fide - releasing chimeras [ J ]. Biochemical Pharmacol- ogy, 2013,85 ( 5 ) : 689 - 703.
  • 7BRUCE K S. Potential biological chemistry of hydro- gen sulfide(H < sub > 2 </sub > S)with the nitro- gen oxides [ J ]. Free Radical Biology and Medicine, 2013,55:1 -7.
  • 8MITALI C, RAVINDER K, KENNETH R O, et al. NOSH-aspirin( NBS- 1120 ), a novel nitric oxide-and hydrogen sulfide-releasing hybrid is a potent inhibitor of colon cancer cell growth < i > in vitro </i > and in a xenograft mouse model[ J]. Biochemical and Bio- physical Research Communications, 2012,419 ( 3 ) : 523 - 528.
  • 9HAN Si-fei, YAO Ting-fing, ZHANG Xin-xin, et al. Lipid-based formulations to enhance oral bioavailability of the poorly water-soluble drug anethol trithione:effects of lipid composition and formulation [ J ]. International Journal of Pharmaceutics,2009,379(1 ) : 18 - 24.
  • 10邓意辉,赵静,董晓辉,等.一种复合型乳化剂及用其制备的乳剂及其制备方法:中国.200710012275.7[P].2007-07-26.

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