Halofuginone - the multifaceted molecule.
Halofuginone - the multifaceted molecule.
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DOI：
10.3390/molecules20010573
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发表时间：
2015-01-05
期刊：
影响因子：
--
通讯作者：
Spector I
中科院分区：
文献类型：
--
作者：
Pines M;Spector I
Halofuginone是febrifugine的类似物，febrifugine是一种最初从植物Dichroa febrifuga中分离出来的生物碱。近年来，常山酮因其广泛的有益生物活性而引起了人们的广泛关注，包括疟疾、癌症、纤维化相关疾病和自身免疫性疾病。目前已经描述了常山酮的两种作用模式：（1）抑制TGFβ信号传导途径下游的Smad 3磷酸化导致成纤维细胞向肌成纤维细胞转化和纤维化的抑制。(2)在疟疾的血液阶段中抑制脯氨酰-tRNA合成酶（ProRS）活性和抑制Th 17细胞分化，从而通过激活氨基酸饥饿和整合的应激反应来抑制炎症和自身免疫反应。本文综述了这种天然产物的历史和起源，其合成，其已知的作用模式，以及它在临床前动物模型和人体中的各种生物活性。
Halofuginone is an analog of febrifugine—an alkaloid originally isolated from the plant Dichroa febrifuga. During recent years, halofuginone has attracted much attention because of its wide range of beneficial biological activities, which encompass malaria, cancer, and fibrosis-related and autoimmune diseases. At present two modes of halofuginone actions have been described: (1) Inhibition of Smad3 phosphorylation downstream of the TGFβ signaling pathway results in inhibition of fibroblasts-to-myofibroblasts transition and fibrosis. (2) Inhibition of prolyl-tRNA synthetase (ProRS) activity in the blood stage of malaria and inhibition of Th17 cell differentiation thereby inhibiting inflammation and the autoimmune reaction by activation of the amino acid starvation and integrated stress responses. This review deals with the history and origin of this natural product, its synthesis, its known modes of action, and it’s various biological activities in pre-clinical animal models and in humans.
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影响因子：
2.8
作者：
Gavish, Z;Pinthus, FH;Pines, M
通讯作者：
Pines, M
影响因子：
2.6
作者：
Daugschies, A;Gasslein, U;Rommel, M
通讯作者：
Rommel, M
影响因子：
2.6
作者：
FOLZ, SD;LEE, BL;CONDER, GA
通讯作者：
CONDER, GA
影响因子：
7.3
作者：
CHIEN, PL;CHENG, CC
通讯作者：
CHENG, CC
DOI：
10.1016/j.cvfa.2008.10.012
发表时间：
2009-03
期刊：
The Veterinary clinics of North America. Food animal practice
影响因子：
--
作者：
Constable PD
通讯作者：
Constable PD