Pharmacokinetics and Tissue Distribution Kinetics of Puerarin in Rats Using Indirect Competitive ELISA.

Hui Kong,Xin Yan,Jinjun Cheng,Rongfeng Shi,Meiling Zhang,Yongzhi Wang,Yan Zhao,Huihua Qu,Qingguo Wang,Xiaoman Liu,Xueqian Wang

doi:10.3390/molecules22060939

Abstract

Puerarin (PUE) is a compound isolated from the roots of Pueraria lobata. We studied the pharmacokinetics and tissue distribution kinetics of PUE in Sprague-Dawley rats following intraperitoneal administration of three concentrations. Indirect competitive ELISA based on an anti-PUE monoclonal antibody was used to determine the concentration of PUE in the blood, heart, liver, spleen, lung, kidney, hippocampus, cerebral cortex, and striatum. The plasma and tissue distribution kinetic characteristics following a single injection of PUE (20, 40 and 80 mg/kg) were calculated using a non-compartment model. In the high-dose (80 mg/kg) and medium-dose (40 mg/kg) groups, the kinetic profile of PUE in blood and kidney samples showed two absorption peaks, while that of the other tissues showed only one peak. In the low-dose (20 mg/kg) group, there was only one peak, irrespective of the sample type. Pharmacokinetic parameters, such as the area under the curve, Cmax, and Tmax varied according to the administered dose. AUC and Cmax values increased dose-dependently. PUE was widely distributed in areas of the brain such as the hippocampus, cerebral cortex, and striatum, providing a foundation for guiding the use of PUE in the treatment of cerebral ischaemic stroke and neurodegenerative diseases.

Highlights

Puerarin (PUE, Figure 1) is a major bioactive compound isolated from the dried roots of Pueraria lobata (Willd.) Ohwi (Fabaceae) [1]
The most widely used techniques in [11], chromatography coupled with tandem mass spectrometry
We developed an indirect competitive enzyme-linked immunosorbent to cognitive functions, such as the hippocampus, whether it can reach the effective concentration, assay based on monoclonal antibodies (MAbs), and successfully applied them to detect andPUE

Summary

Introduction

Puerarin (PUE, Figure 1) is a major bioactive compound isolated from the dried roots of Pueraria lobata (Willd.) Ohwi (Fabaceae) [1]. PUE has been widely used to treat ischaemic stroke in China [2]. It acts by dilating blood vessels, improving cerebral (pial) microcirculation and blood flow [3], reducing blood viscosity, platelet aggregation, and microintravascular fibrin precipitation, inhibiting thrombus formation [4], and attenuating neuronal apoptosis [5]. Pharmacokinetics and distribution is one of the key steps in elucidating mechanism far, high-performance liquid chromatography (HPLC). The most widely used techniques in [11], chromatography coupled with tandem mass spectrometry [10], gas chromatography studies. Sample pretreatment for the thesemost methods is complex, the in andpharmacokinetic gas chromatography-mass spectrometry [12] are widely usedrequiring techniques removal of proteins and a concentration step, which inevitably leads to sample loss

Objectives

Methods

Results