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Gliotoxin和相关的环硫二酮哌嗪类化合物。

Gliotoxin and related epipolythiodioxopiperazines.

作者信息

Waring P, Beaver J

机构信息

Division of Cell Biology, John Curtin School, Canberra City, Australia.

出版信息

Gen Pharmacol. 1996 Dec;27(8):1311-6. doi: 10.1016/s0306-3623(96)00083-3.

DOI:10.1016/s0306-3623(96)00083-3
PMID:9304400
Abstract
  1. Gliotoxin belongs to the epipolythiodioxopiperazine class of secondary metabolites. These compounds show a diverse range of biological activity including antimicrobial, antifungal and antiviral properties. They also display potent in vitro and in vivo immunomodulating activity. 2. Their properties resulted in a number of early studies designed to exploit their possible chemotherapeutic value, although the general toxicity of most members of this class has precluded clinical use. 3. Most recently, their selective immunosuppressive properties have led to the possibility of ex vivo treatment of tissue to selectively remove immune cells responsible for tissue rejection. The mode of action of gliotoxin appears to be via covalent interaction to proteins through mixed disulphide formation and gliotoxin has been shown to inhibit a number of thiol requiring enzymes. 4. Gliotoxin is also a potent inducer of apoptotic cell death in a number of cells. Gliotoxin and other members of this class of toxins may be produced in vivo during the course of fungal infections and contribute to the aetiology of the disease.
摘要
  1. Gliotoxin属于次生代谢产物的表硫代二氧哌嗪类。这些化合物具有多种生物活性,包括抗菌、抗真菌和抗病毒特性。它们在体外和体内还表现出强大的免疫调节活性。2. 它们的特性促使了一些早期研究,旨在开发其潜在的化疗价值,尽管这类化合物中大多数成员的一般毒性使其无法用于临床。3. 最近,它们的选择性免疫抑制特性使得对组织进行离体处理以选择性去除负责组织排斥的免疫细胞成为可能。Gliotoxin的作用方式似乎是通过混合二硫键的形成与蛋白质发生共价相互作用,并且已证明Gliotoxin能抑制多种需要巯基的酶。4. Gliotoxin也是许多细胞中凋亡性细胞死亡的有效诱导剂。Gliotoxin和这类毒素的其他成员可能在真菌感染过程中在体内产生,并导致疾病的病因。

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Gliotoxin and related epipolythiodioxopiperazines.Gliotoxin和相关的环硫二酮哌嗪类化合物。
Gen Pharmacol. 1996 Dec;27(8):1311-6. doi: 10.1016/s0306-3623(96)00083-3.
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In vivo immunosuppressive activity of gliotoxin, a metabolite produced by human pathogenic fungi.Gliotoxin(一种由人类致病真菌产生的代谢产物)的体内免疫抑制活性。
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The immunomodulating agent gliotoxin causes genomic DNA fragmentation.免疫调节剂gliotoxin会导致基因组DNA片段化。
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Fungal metabolite gliotoxin blocks mast cell activation by a calcium- and superoxide-dependent mechanism: implications for immunosuppressive activities.真菌代谢产物gliotoxin通过一种依赖钙和超氧化物的机制阻断肥大细胞活化:对免疫抑制活性的影响。
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Structural relationship of epipolythiodioxopiperazines and their immunomodulating activity.环多硫代二氧哌嗪类化合物的结构关系及其免疫调节活性。
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Extracellular calcium is not required for gliotoxin or dexamethasone-induced DNA fragmentation: a reappraisal of the use of EGTA.
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Inactivation of rabbit muscle creatine kinase by reversible formation of an internal disulfide bond induced by the fungal toxin gliotoxin.真菌毒素gliotoxin诱导形成内部二硫键导致兔肌肉肌酸激酶失活,此失活过程可逆。
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[Chemistry and biological effects of gliotoxin].
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