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环糊精在基于三萜的治疗剂设计与开发中的作用。

The Role of Cyclodextrins in the Design and Development of Triterpene-Based Therapeutic Agents.

作者信息

Prodea Alexandra, Mioc Alexandra, Banciu Christian, Trandafirescu Cristina, Milan Andreea, Racoviceanu Roxana, Ghiulai Roxana, Mioc Marius, Soica Codruta

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Victor Babes University of Medicine and Pharmacy, 2nd Eftimie Murgu Sq., 300041 Timisoara, Romania.

Research Centre for Pharmaco-Toxicological Evaluation, "Victor Babes" University of Medicine and Pharmacy, Eftimie Murgu Sq., No. 2, 300041 Timisoara, Romania.

出版信息

Int J Mol Sci. 2022 Jan 10;23(2):736. doi: 10.3390/ijms23020736.

Abstract

Triterpenic compounds stand as a widely investigated class of natural compounds due to their remarkable therapeutic potential. However, their use is currently being hampered by their low solubility and, subsequently, bioavailability. In order to overcome this drawback and increase the therapeutic use of triterpenes, cyclodextrins have been introduced as water solubility enhancers; cyclodextrins are starch derivatives that possess hydrophobic internal cavities that can incorporate lipophilic molecules and exterior surfaces that can be subjected to various derivatizations in order to improve their biological behavior. This review aims to summarize the most recent achievements in terms of triterpene:cyclodextrin inclusion complexes and bioconjugates, emphasizing their practical applications including the development of new isolation and bioproduction protocols, the elucidation of their underlying mechanism of action, the optimization of triterpenes' therapeutic effects and the development of new topical formulations.

摘要

三萜类化合物因其显著的治疗潜力而成为一类广泛研究的天然化合物。然而,它们的低溶解度以及随之而来的低生物利用度目前正阻碍着它们的应用。为了克服这一缺点并增加三萜类化合物的治疗用途,环糊精已被用作水溶性增强剂;环糊精是淀粉衍生物,具有可容纳亲脂性分子的疏水内腔以及可进行各种衍生化以改善其生物学行为的外表面。本综述旨在总结三萜类化合物与环糊精包合物和生物缀合物方面的最新研究成果,重点介绍它们的实际应用,包括新分离和生物生产方案的开发、作用机制的阐明、三萜类化合物治疗效果的优化以及新外用制剂的开发。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d460/8775686/fb4fcafcb15c/ijms-23-00736-g001.jpg

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