Pharmacokinetics of Gingerols, Shogaols, and Their Metabolites in Asthma Patients.
Pharmacokinetics of Gingerols, Shogaols, and Their Metabolites in Asthma Patients.
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DOI：
10.1021/acs.jafc.2c03150
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发表时间：
2022-08-10
影响因子：
6.1
通讯作者：
Sang, Shengmin
中科院分区：
文献类型：
--
作者：
Zhang, Shuwei;DiMango, Emily;Zhu, Yingdong;Saroya, Tarnjot K.;Emala, Charles W.;Sang, Shengmin
6-姜辣素和6-姜烯酚是姜根中含量最丰富的姜辣素和姜烯酚，并已显示可减少哮喘小鼠模型中的哮喘表型。几项研究描述了姜辣素和姜烯酚在人类口服生姜后的药代动力学，而对这些成分在人类，特别是哮喘患者中的代谢知之甚少。在这项研究中，饮食补充剂1.0克生姜根提取物给予哮喘患者每天两次，共56天，血清样品在0.5-8小时的第0，28和56天。采用液相色谱-质谱法（LC-MS）分析了三次不同访视收集的哮喘患者血浆中姜辣素和姜烯酚的代谢谱以及姜辣素、姜烯酚及其代谢产物的动力学变化。酮还原是姜辣素和姜烯酚的主要代谢途径。姜二醇被鉴定为6-、8-和10-姜酚的主要代谢产物。M11和M9分别被鉴定为6-姜烯酚的双键还原代谢产物以及双键和酮还原代谢产物。半胱氨酸结合是6-姜烯酚在哮喘患者中的另一个主要代谢途径，并且两个半胱氨酸结合的6-姜烯酚，M1和M2，被鉴定为6-姜烯酚的主要代谢产物。此外，使用非常灵敏的高分辨率LC-MS方法，在三次访视期间的不同时间点收集的人血清中定量姜辣素、姜烯酚及其代谢物。结果表明，三分之一的6-姜酚被代谢产生其还原代谢产物6-姜二醇，超过90%的6-姜烯酚被代谢为其I相和半胱氨酸结合的代谢产物，这表明考虑这些代谢产物对姜酚和姜烯酚的生物利用度和健康有益作用的贡献的重要性。所有姜辣素、姜烯酚及其代谢产物在不到2小时内达到峰值浓度，其半衰期（t1/2）为0.6至2.4小时。此外，长期服用生姜补充剂，特别是治疗56天后，可以增加哮喘患者对生姜化合物及其代谢产物的吸收。
6-Gingerol and 6-shogaol are the most abundant gingerols and shogaols in ginger root and have been shown to reduce the asthmatic phenotype in murine models of asthma. Several studies have described the pharmacokinetics of gingerols and shogaols in humans following the oral ingestion of ginger, while little was known about the metabolism of these components in humans, particularly in patients with asthma. In this study, a dietary supplement of 1.0 g of ginger root extract was administered to asthma patients twice daily for 56 days and serum samples were drawn at 0.5–8 h on days 0, 28, and 56. The metabolic profiles of gingerols and shogaols in human plasma and the kinetic changes of gingerols, shogaols, and their metabolites in asthma patients collected on the three different visits were analyzed using liquid chromatography–mass spectrometry (LC–MS). Ketone reduction was the major metabolic pathway of both gingerols and shogaols. Gingerdiols were identified as the major metabolites of 6-, 8-, and 10-gingerols. M11 and M9 were identified as the double-bond reduction and both the double-bond and ketone reduction metabolites of 6-shogaol, respectively. Cysteine conjugation was another major metabolic pathway of 6-shogaol in asthma patients, and two cysteine-conjugated 6-shogaol, M1 and M2, were identified as the major metabolites of 6-shogaol. Furthermore, gingerols, shogaols, and their metabolites were quantitated in the human serum collected at different time points during each of the three visits using a very sensitive high-resolution LC–MS method. The results showed that one-third of 6-gingerol was metabolized to produce its reduction metabolites, 6-gingerdiols, and more than 90% of 6-shogaol was metabolized to its phase I and cysteine-conjugated metabolites, suggesting the importance of considering the contribution of these metabolites to the bioavailability and health beneficial effects of gingerols and shogaols. All gingerols, shogaols, and their metabolites reached their peak concentrations in less than 2 h, and their half-lives (t1/2) were from 0.6 to 2.4 h. Furthermore, long-term treatment of ginger supplements, especially after 56 days of treatment, increases the absorption of ginger compounds and their metabolites in asthma patients.
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DOI：
10.1016/j.jchromb.2012.09.020
发表时间：
2012-10-15
影响因子：
3
作者：
Chen, Huadong;Sang, Shengmin
通讯作者：
Sang, Shengmin
影响因子：
3.9
作者：
Chen, Huadong;Lv, Lishuang;Sang, Shengmin
通讯作者：
Sang, Shengmin
影响因子：
4.6
作者：
Mukkavilli, Rao;Yang, Chunhua;Aneja, Ritu
通讯作者：
Aneja, Ritu
影响因子：
7.4
作者：
Zhu, Yingdong;Wang, Pei;Sang, Shengmin
通讯作者：
Sang, Shengmin
影响因子：
4.1
作者：
Chen, Huadong;Soroka, Dominique N.;Sang, Shengmin
通讯作者：
Sang, Shengmin