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Synthesis and Identification of Novel Berberine Derivatives as Potent Inhibitors against TNF-?-Induced NF-?B Activation.

ABSTRACT: Twenty-three new berberine (BBR) analogues defined on substituents of ring D were synthesized and evaluated for their activity for suppression of tumor necrosis factor (TNF)-?-induced nuclear factor (NF)-?B activation. Structure-activity relationship (SAR) analysis indicated that suitable tertiary/quaternary carbon substitutions at the 9-position or rigid fragment at position 10 might be beneficial for enhancing their anti-inflammatory potency. Among them, compounds 2d, 2e, 2i and 2j exhibited satisfactory inhibitory potency against NF-?B activation, with an inhibitory rate of around 90% (5 ?M), much better than BBR. A preliminary mechanism study revealed that all of them could inhibit TNF-?-induced NF-?B activation via impairing I?B kinase (IKK) phosphorylation as well as cytokines interleukin (IL)-6 and IL-8 induced by TNF-?. Therefore, the results provided powerful information on further structural modifications and development of BBR derivatives into a new class of anti-inflammatory candidates for the treatment of inflammatory diseases.

SUBMITTER: Wang YX 

PROVIDER: S-EPMC6152030 | biostudies-literature | 2017 Jul

REPOSITORIES: biostudies-literature

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Synthesis and Identification of Novel Berberine Derivatives as Potent Inhibitors against TNF-α-Induced NF-κB Activation.

Wang Yan-Xiang YX   Liu Lu L   Zeng Qing-Xuan QX   Fan Tian-Yun TY   Jiang Jian-Dong JD   Deng Hong-Bin HB   Song Dan-Qing DQ  

Molecules (Basel, Switzerland) 20170727 8

Twenty-three new berberine (BBR) analogues defined on substituents of ring D were synthesized and evaluated for their activity for suppression of tumor necrosis factor (TNF)-α-induced nuclear factor (NF)-κB activation. Structure-activity relationship (SAR) analysis indicated that suitable tertiary/quaternary carbon substitutions at the 9-position or rigid fragment at position 10 might be beneficial for enhancing their anti-inflammatory potency. Among them, compounds <b>2d</b>, <b>2e</b>, <b>2i</  ...[more]

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