Dang Y, Lin G, Xie Y, Duan J, Ma P, Li G, Ji G
Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
Drug Res (Stuttg). 2014 Oct;64(10):516-22. doi: 10.1055/s-0033-1363220. Epub 2013 Dec 19.
Myricetin is a widely distributed bioactive flavonoid with scientific interest attributed to its anti-oxidant, antitumor, and anti-inflammatory properties. A specific and sensitive ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method has been developed and validated for identification and quantification of myricetin in rat plasma after oral and intravenous administrations. Kaempferol was used as an internal standard. Followed by β-glucuronidase and sulfatase hydrolysis and liquid-liquid extraction with ethyl acetate, the analytes were separated on an Acquity UPLC BEH C18 column (2.1×50 mm, 1.7 μm) and analyzed in the selected ion recording with a negative electrospray ionization mode. The developed method was validated for selectivity, accuracy, precision, linearity, recovery, stability and matrix effect. The assay was validated over a wide concentration range of 2-4,000 ng/mL. Intra- and inter-day precisions were all less than 13.49% and accuracy ranged from 95.75 to 109.80%. The present method was successfully applied to investigate a pharmacokinetic study of myricetin following intravenous and oral administrations to rats. The absolute bioavailability was found to be 9.62% and 9.74% at 2 oral doses (50 mg/kg and 100 mg/kg, respectively), which indicated myricetin was poorly absorbed after oral administration. To our knowledge, this is the first pharmacokinetic evaluation of myricetin as a single active pharmaceutical ingredient in preclinical studies.
杨梅素是一种广泛分布的生物活性黄酮类化合物，因其抗氧化、抗肿瘤和抗炎特性而受到科学界的关注。已开发并验证了一种特定且灵敏的超高效液相色谱-串联质谱法（UPLC-MS/MS），用于在大鼠口服和静脉给药后血浆中杨梅素的鉴定和定量。山奈酚用作内标。在经β-葡萄糖醛酸酶和硫酸酯酶水解并用乙酸乙酯进行液-液萃取后，分析物在Acquity UPLC BEH C18柱（2.1×50 mm，1.7 μm）上分离，并在选择离子记录模式下以负电喷雾电离模式进行分析。所开发的方法在选择性、准确性、精密度、线性、回收率、稳定性和基质效应方面得到了验证。该测定法在2-4,000 ng/mL的宽浓度范围内得到验证。日内和日间精密度均小于13.49%，准确度范围为95.75%至109.80%。本方法成功应用于大鼠静脉和口服给药后杨梅素的药代动力学研究。在2个口服剂量（分别为50 mg/kg和100 mg/kg）下，绝对生物利用度分别为9.62%和9.74%，这表明杨梅素口服给药后吸收较差。据我们所知，这是临床前研究中对作为单一活性药物成分的杨梅素的首次药代动力学评估。
