College of Chinese Medicine, Zhejiang Pharmaceutical College, Ningbo, People's Republic of China.
College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, People's Republic of China.
Biomed Chromatogr. 2022 Feb;36(2):e5253. doi: 10.1002/bmc.5253. Epub 2021 Oct 28.
Saururus chinensis (SC) possesses significant anti-diabetic activity and lignans were its major bioactive compounds. In this study, a rapid and sensitive ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method was established for simultaneous quantification of six lignans, namely (-)-(7R,8R)-machilin D (1), verrucesin (2), rel-(7S,8S,7'R,8'R)-3,3',4,4',5,5'-hexamethoxy-7.O.7',8.8'-lignan (3), manassantin A (4), manassantin B (5), and saucerneol F (6) in rat's plasma. It was validated with acceptable linearity (r ≥ 0.9922), accuracy (80.42-95.17%), precision (RSD ≤ 12.08%), and extraction recovery (80.36-93.45%). The method was successfully applied to the comparative pharmacokinetic study of the six lignans in normal and diabetic rats after oral administration of SC extract. Results showed that the areas under the plasma concentration-time curve (AUC and AUC ) of (-)-(7R,8R)-machilin D, rel-(7S,8S,7'R,8'R)-3,3',4,4',5,5'-hexamethoxy-7.O.7',8.8'-lignan, manassantin B, and saucerneol F in diabetic rats were significantly increased, and the plasma clearance (CL) of (-)-(7R,8R)-machilin D in diabetic rats was significantly decreased. However, the AUC and AUC of verrucesin were significantly decreased, and its CL was significantly increased in diabetic rats compared with those in normal rats. These results indicated that there were remarkable differences in the pharmacokinetic parameters between the normal and diabetic rats. The pharmacokinetic studies might be beneficial for the clinical use of SC as hypoglycemic agent.
中华蛇菰(SC)具有显著的抗糖尿病活性,其主要生物活性化合物为木脂素。本研究建立了一种快速灵敏的超高效液相色谱-串联质谱(UHPLC-MS/MS)法,用于同时定量分析大鼠血浆中的 6 种木脂素,分别为(-)-(7R,8R)-马钱子素 D(1)、蛇菰宁(2)、(7S,8S,7'R,8'R)-3,3',4,4',5,5'-六甲氧基-7.O.7',8.8'-木脂素(3)、马桑亭 A(4)、马桑亭 B(5)和桑色醇 F(6)。该方法具有良好的线性(r≥0.9922)、准确度(80.42-95.17%)、精密度(RSD≤12.08%)和提取回收率(80.36-93.45%)。该方法成功应用于 SC 提取物灌胃后正常和糖尿病大鼠体内 6 种木脂素的比较药代动力学研究。结果表明,糖尿病大鼠体内(-)-(7R,8R)-马钱子素 D、(7S,8S,7'R,8'R)-3,3',4,4',5,5'-六甲氧基-7.O.7',8.8'-木脂素、马桑亭 B 和桑色醇 F 的血浆浓度-时间曲线下面积(AUC 和 AUC )显著增加,而糖尿病大鼠体内(-)-(7R,8R)-马钱子素 D 的血浆清除率(CL)显著降低。然而,与正常大鼠相比,糖尿病大鼠体内蛇菰宁的 AUC 和 AUC 显著降低,而其 CL 显著增加。这些结果表明,正常和糖尿病大鼠的药代动力学参数存在显著差异。药代动力学研究可能有助于 SC 作为降血糖药物的临床应用。