Synthesis, Structural Elucidation, and Anti-Inflammatory Activity of a Water-Soluble Derivative of Arctiin

被引：1

作者：

Xu, Xia ^{[1
]}

Huang, Xiaofeng ^{[1
]}

Zheng, Yuedan ^{[1
]}

Wang, Xiaoling ^{[1
]}

Xie, Jing ^{[2
]}

Liu, Sha ^{[2
,3
]}

Guo, Kun ^{[1
]}

机构：

[1] Southwest Minzu Univ, Coll Pharm, Chengdu 610200, Peoples R China

[2] Chengdu Med Coll, Sch Pharm, Chengdu 610500, Peoples R China

[3] Chengdu Med Coll, Affiliated Hosp 2, China Natl Nucl Corp Hosp 416, Chengdu 610066, Peoples R China

来源：

MOLECULES | 2023年 / 28卷 / 04期

关键词：

arctigenin-4 ' -O-glucuronide; arctiin; water-soluble derivative; anti-inflammatory activity; DIBENZYLBUTYROLACTONE LIGNANS; PRODRUG; FRUITS; LAPPA;

D O I：

10.3390/molecules28041789

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The poor oral bioavailability of arctiin caused by its low water solubility is the biggest obstacle in developing it as a drug. In this work, a new water-soluble glucuronide derivative of arctiin (arctigenin-4 '-O-glucuronide) was synthesized through 2,2,6,6-tetramethylpiperidine 1-oxyl mediated oxidation reaction. Subsequently, its anti-inflammatory effect was evaluated by mice acute lung injury model in vivo. The results showed that the glucuronide derivative of arctiin not only had better water solubility but also displayed improved anti-inflammatory activity in vivo, thus serving as an innovative compound in the drug development of arctiin.

引用

页数：11

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