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一种具有双Nrf2和Nf-κB调节活性的链格孢萜类化合物的鉴定

Identification of a Strigoterpenoid with Dual Nrf2 and Nf-κB Modulatory Activity.

作者信息

Rogati Federica, Millán Estrella, Appendino Giovanni, Correa Alejandro, Caprioglio Diego, Minassi Alberto, Muñoz Eduardo

机构信息

Dipartimento di Scienze del Farmaco, Università del Piemonte Orientale, Via Bovio 6, Novara 28100, Italy.

Maimonides Biomedical Research Institute of Córdoba, Avda Menendez Pidal s/n, 14004 Cordoba, Spain.

出版信息

ACS Med Chem Lett. 2019 Jan 8;10(4):606-610. doi: 10.1021/acsmedchemlett.8b00604. eCollection 2019 Apr 11.

DOI:10.1021/acsmedchemlett.8b00604
PMID:30996804
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6467025/
Abstract

The sesquiterpene-coumarin ether samarcandone provided a suitable framework to replace the apocarotenoid A-C ring system of strigol (), replicating, after linking to a butenolide moiety, the activity of the natural phytohormone on Nrf2 and also showing potent NF-kB inhibitory activity, overall modulating two critical pathways of inflammation and cancer.

摘要

倍半萜香豆素醚萨马坎酮提供了一个合适的骨架来取代独脚金内酯的类胡萝卜素A-C环系统，在与丁烯内酯部分连接后，复制了天然植物激素对Nrf2的活性，并且还表现出强大的NF-κB抑制活性，总体上调节炎症和癌症的两个关键途径。

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