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仙茅苷的降脂作用及口服转运特性研究

Lipid-lowering effect and oral transport characteristics study of curculigoside.

作者信息

Wang Aiping, Ning Jie, Zhao Lu, Xu Renjie

机构信息

Shaoxing Maternity and Child Health Care Hospital, Shaoxing, China.

Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou, China.

出版信息

Front Cardiovasc Med. 2024 Jul 2;11:1426379. doi: 10.3389/fcvm.2024.1426379. eCollection 2024.

Abstract

INTRODUCTION

The incidence of metabolic disorders during pregnancy is increasing year by year, with diseases including hypertension and hyperlipidemia. Statins are the primary drugs for treating hyperlipidemia or atherosclerosis, yet some patients remain unresponsive to them, and pregnant women are prohibited from taking statins. Curculigoside is the major biologically active natural product present in .

METHODS

In this study, A high-fat mice model was developed to study the lipid-lowering effect of curculigoside. Using intestinal Caco-2 cell monolayer, the curculigoside transport properties at two temperatures and possible transporters were systemically studied.

RESULTS

Curculigoside at concentrations used during the experiments have no toxic effect to Caco-2 cells. The curculigoside transfer from the apical to the basolateral side was strongly influenced by temperature. P-glycoprotein, breast cancer resistance protein, and efflux transporters are crucial components of the human intestinal cell line Caco-2. The curculigoside can significantly affect the contents of total cholesterol, triglycerides, high-density lipoprotein cholesterol, and low-density lipoprotein cholesterol in mice.

DISCUSSION

The transport properties and potential mechanism of curculigoside offer valuable insights for the design of development of hypolipidemic drugs like anti-atherosclerotic drugs and also be helpful to the further study of the pharmacological activity of curculigoside.

摘要

引言

孕期代谢紊乱的发病率逐年上升,包括高血压和高脂血症等疾病。他汀类药物是治疗高脂血症或动脉粥样硬化的主要药物,但一些患者对其仍无反应,且孕妇禁止服用他汀类药物。仙茅苷是[具体来源未给出]中主要的生物活性天然产物。

方法

本研究建立了高脂小鼠模型以研究仙茅苷的降脂作用。利用肠Caco-2细胞单层,系统研究了仙茅苷在两个温度下的转运特性及可能的转运体。

结果

实验所用浓度的仙茅苷对Caco-2细胞无毒性作用。仙茅苷从顶端向基底外侧的转运受温度影响很大。P-糖蛋白、乳腺癌耐药蛋白和外排转运体是人类肠细胞系Caco-2的关键组成部分。仙茅苷可显著影响小鼠血清中总胆固醇、甘油三酯、高密度脂蛋白胆固醇和低密度脂蛋白胆固醇的含量。

讨论

仙茅苷的转运特性及潜在机制为抗动脉粥样硬化等降血脂药物的设计开发提供了有价值的见解,也有助于进一步研究仙茅苷的药理活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2d28/11249560/4cdf124414dd/fcvm-11-1426379-g001.jpg

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