Anhui Province Key Laboratory of Major Autoimmune Diseases, School of Pharmacy, Anhui Medical University, Hefei 230032, China.
Huainan Municipal Food and Drug Inspection Center, Huainan 232000, China.
Molecules. 2022 Jul 21;27(14):4657. doi: 10.3390/molecules27144657.
To understand that 18β-Glycyrrhetic acid 3-O-mono--D-glucuronide (GAMG) showed better pharmacological activity and drug-like properties than 18β-Glycyrrhizin (GL); a rapid and sensitive HPLC-MS/MS method was established for the simultaneous determination of GAMG and its metabolite 18β-Glycyrrhetinic acid (GA) in rat plasma and tissues after oral administration of GAMG or GL. This analytical method was validated by linearity, LLOQ, specificity, recovery rate, matrix effect, etc. After oral administration, GAMG exhibited excellent (2377.57 ng/mL), (5 min) and AUC (6625.54 mg/Lh), which was much higher than the (346.03 ng/mL), (2.00 h) and AUC (459.32 mg/Lh) of GL. Moreover, GAMG had wider and higher tissue distribution in the kidney, spleen, live, lung, brain, etc. These results indicated that oral GAMG can be rapidly and efficiently absorbed and be widely distributed in tissues to exert stronger and multiple pharmacological activities. This provided a physiological basis for guiding the pharmacodynamic study and clinical applications of GAMG.
为了理解 18β-甘草酸 3-O-单-β-D-葡萄糖醛酸苷（GAMG）比 18β-甘草酸苷（GL）具有更好的药理活性和类药性；建立了一种快速灵敏的 HPLC-MS/MS 方法，用于同时测定大鼠口服 GAMG 或 GL 后血浆和组织中的 GAMG 及其代谢物 18β-甘草次酸（GA）。该分析方法通过线性、LLOQ、特异性、回收率、基质效应等进行了验证。口服后，GAMG 表现出优异的（2377.57ng/mL）、（5 分钟）和 AUC（6625.54mg/Lh），明显高于 GL 的（346.03ng/mL）、（2.00 小时）和 AUC（459.32mg/Lh）。此外，GAMG 在肾脏、脾脏、肝脏、肺、大脑等组织中分布更广泛、更高。这些结果表明，口服 GAMG 能够快速有效地吸收，并广泛分布于组织中，发挥更强、更广泛的药理活性。这为指导 GAMG 的药效学研究和临床应用提供了生理学基础。
