The Fourth Hospital of Hebei Medical University, Shijiazhuang, 050011, PR China.
The Second Hospital of Hebei Medical University, Shijiazhuang, 050000, PR China.
J Pharm Biomed Anal. 2021 Apr 15;197:113905. doi: 10.1016/j.jpba.2021.113905. Epub 2021 Jan 18.
Oroxin B, a flavonoid, is a major bioactive component form Oroxylum indicum (L.) Vent. with enormous anti-hepatoma effects. To data, the oroxin B metabolism studies remain underexplored. This study was designed to characterize oroxin B metabolism in vivo and in vitro by ultrahigh-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS/MS). Consequently, 30 metabolites in rats, 8 metabolites in liver microsomes and 18 metabolites in intestinal bacteria were identified, and 9 metabolites were recognized by comparison with standards. The biotransformation processes involved ketone, acetylation, loss of CHO, and loss of CHO. And baicalein and oroxin A were generated after loss of CHO, and loss of CHO, respectively, and further went through some other reactions, such as oxidation, methylation, internal hydrolysis, hydrogenation, loss of O, ketone, glycine conjugation, glucuronide conjugation and their composite reactions. The results provide valuable evidence for elucidation the potential mechanism of oroxin B pharmacological action, and offer reasonable guidelines for further investigations of oroxin B safety and efficacy.
奥洛林 B 是一种黄酮类化合物，是贯叶连翘（L.）Vent 的主要生物活性成分，具有巨大的抗肝癌作用。迄今为止，奥洛林 B 的代谢研究仍未得到充分探索。本研究旨在通过超高效液相色谱-四级杆飞行时间质谱联用（UHPLC-Q-TOF-MS/MS）对奥洛林 B 的体内和体外代谢进行表征。因此，在大鼠中鉴定出 30 种代谢物、肝微粒体中 8 种代谢物和肠道细菌中 18 种代谢物，并通过与标准品比较鉴定出 9 种代谢物。生物转化过程涉及酮、乙酰化、CHO 损失和 CHO 损失。在 CHO 损失和 CHO 损失后分别生成黄芩苷和奥洛林 A，并进一步经过氧化、甲基化、内水解、加氢、O 损失、酮化、甘氨酸结合、葡萄糖醛酸结合及其复合反应等反应。研究结果为阐明奥洛林 B 药理作用的潜在机制提供了有价值的证据，并为进一步研究奥洛林 B 的安全性和疗效提供了合理的指导。
