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笼状多聚异戊烯基黄酮及其生物活性。

Caged Polyprenylated Xanthones in and the Biological Activities of Them.

机构信息

School of Pharmacy, Anhui University of Chinese Medicine, Hefei, People's Republic of China.

出版信息

Drug Des Devel Ther. 2023 Dec 5;17:3625-3660. doi: 10.2147/DDDT.S426685. eCollection 2023.

Abstract

The previous phytochemical analyses of revealed that the main structural characteristic associated with its biological activity is the caged polyprenylated xanthones with a unique 4-oxatricyclo [4.3.1.0] dec-2-one scaffold, which contains a highly substituted tetrahydrofuran ring with three quaternary carbons. Based on the progress in research of the chemical constituents, pharmacological effects and modification methods of the caged polyprenylated xanthones, this paper presents a preliminary predictive analysis of their drug-like properties based on the absorption, distribution, metabolism, excretion and toxicity (ADME/T) properties. It was found out that these compounds have very similar pharmacokinetic properties because they possess the same caged xanthone structure, the 9,10-double bond in a,b-unsaturated ketones are critical for the antitumor activity. The author believes that there is an urgent need to seek new breakthroughs in the study of these caged polyprenylated xanthones. Thus, the research on the route of administration, therapeutic effect, structural modification and development of such active ingredients is of great interest. It is hoped that this paper will provide ideas for researchers to develop and utilize the active ingredients derived from natural products.

摘要

先前对 的植物化学分析表明,与其生物活性相关的主要结构特征是笼状聚戊烯基黄酮,具有独特的 4-氧杂三环[4.3.1.0]癸-2-酮支架,其中包含一个高度取代的四氢呋喃环,具有三个季碳原子。基于笼状聚戊烯基黄酮的化学成分、药理作用和修饰方法的研究进展,本文基于吸收、分布、代谢、排泄和毒性(ADME/T)性质对其类药性进行了初步预测分析。结果发现,由于这些化合物具有相同的笼状黄酮结构,因此具有非常相似的药代动力学性质,在 a,b-不饱和酮中的 9,10-双键对于抗肿瘤活性至关重要。作者认为,迫切需要在这些笼状聚戊烯基黄酮的研究中寻求新的突破。因此,对这些活性成分的给药途径、治疗效果、结构修饰和开发的研究具有重要意义。希望本文能为研究人员开发和利用天然产物衍生的活性成分提供思路。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/006f/10710250/40974697fdab/DDDT-17-3625-g0001.jpg

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