School of Chinese Materia Medica & School of Life Sciences, Beijing University of Chinese Medicine, Beijing, 100029, People's Republic of China; Department of Pharmacy & Institute of Clinical Medical Sciences, China-Japan Friendship Hospital, Beijing, 100029, People's Republic of China.
Department of Pharmacy & Institute of Clinical Medical Sciences, China-Japan Friendship Hospital, Beijing, 100029, People's Republic of China.
J Ethnopharmacol. 2024 Jan 30;319(Pt 1):117130. doi: 10.1016/j.jep.2023.117130. Epub 2023 Sep 9.
Cornus officinalis Sieb. et Zucc. is a medicinal and edible homolog in traditional Chinese medicine. Loganin, an iridoid glycoside, is one of the main active components of Cornus officinalis Sieb. et Zucc. Loganin has been demonstrated to improve depression-like behavior and may be a potential antidepressant candidate. However, the pharmacokinetic characteristics and tissue distribution of loganin, especially in the brain region, are still unclear.
This study aims to investigate the pharmacokinetic characteristics and tissue distribution after oral administration of loganin in rats.
A simple, rapid and reproducible UPLC-MS/MS method was developed and validated for the determination of loganin in rat plasma and tissues. The samples were prepared by acetonitrile precipitation with chloramphenicol as internal standard (IS). Loganin was separated by gradient elution on ACQUITY UPLC®BEH C18 (2.1 × 50 mm, 1.7 μm) using multiple reactions monitoring (MRM) mode. Concentration-time data was subjected to pharmacokinetic analysis. The pharmacokinetic parameters of loganin in rat plasma were analyzed by compartment model using DAS 2.0 software.
The established UPLC-MS/MS method was accurate and reliable with a good linearity (R > 0.99) in the respective concentration range, satisfying the quantitative requirements. This method was successfully used to study the pharmacokinetics and tissue distribution after oral administration of loganin in rats. The peak time (T) of oral administration was about 40 min, and the half-life (t) was about 50 min, indicating that loganin was quickly absorbed and eliminated in rats. Oral bioavailability was 5.50%. The dose correlation results showed that AUC had a poor correlation with dose, while C had a good correlation with dose. In tissues, loganin (35 mg/kg) was highly distributed in the stomach, small intestine, kidney, liver and lung. When the dose was 70 mg/kg, loganin had significant distribution in the cortex.
In this study, a simple and sensitive UPLC-MS/MS method was developed and validated for the determination of loganin in rat plasma and tissues. Loganin was absorbed quickly, eliminated quickly, and had low bioavailability. The distribution of loganin in the cortex was higher than that in the hippocampus. We hope that our results can provide a reference for loganin to become a new antidepressant.
山茱萸是传统中药中的一种药用和食用同源物。马钱苷，一种环烯醚萜糖苷，是山茱萸的主要活性成分之一。马钱苷已被证明可以改善抑郁样行为，可能是一种有潜力的抗抑郁候选药物。然而，马钱苷的药代动力学特征和组织分布，特别是在脑区，仍不清楚。
本研究旨在研究马钱苷灌胃给药后在大鼠体内的药代动力学特征和组织分布。
建立并验证了一种简单、快速、重现性好的 UPLC-MS/MS 方法，用于测定大鼠血浆和组织中的马钱苷。样品经乙腈沉淀，以氯霉素为内标（IS）。马钱苷在 ACQUITY UPLC®BEH C18（2.1×50mm，1.7μm）上采用梯度洗脱，以多反应监测（MRM）模式进行分离。采用 DAS 2.0 软件对马钱苷在大鼠血浆中的浓度-时间数据进行药代动力学分析。
所建立的 UPLC-MS/MS 方法准确可靠，在各自的浓度范围内线性良好（R>0.99），满足定量要求。该方法成功用于研究大鼠灌胃给予马钱苷后的药代动力学和组织分布。口服给药的达峰时间（T）约为 40min，半衰期（t）约为 50min，表明马钱苷在大鼠体内吸收迅速，消除较快。口服生物利用度为 5.50%。剂量相关性结果表明，AUC 与剂量相关性差，而 C 与剂量相关性好。在组织中，马钱苷（35mg/kg）在胃、小肠、肾、肝和肺中分布较高。当剂量为 70mg/kg 时，马钱苷在皮质中有明显分布。
本研究建立并验证了一种用于测定大鼠血浆和组织中马钱苷的简单、灵敏的 UPLC-MS/MS 方法。马钱苷吸收迅速，消除迅速，生物利用度低。马钱苷在皮质中的分布高于在海马中的分布。我们希望我们的研究结果可以为马钱苷成为一种新型抗抑郁药提供参考。
