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己酮可可碱

Pentoxifylline.

作者信息

Samlaska C P, Winfield E A

机构信息

Dermatology Service, Tripler Army Medical Center, Honolulu, Hawaii.

出版信息

J Am Acad Dermatol. 1994 Apr;30(4):603-21. doi: 10.1016/s0190-9622(94)70069-9.

Abstract

Pentoxifylline (oxpentifylline) is a methylxanthine derivative with potent hemorrheologic properties. In the United States it is marketed for the treatment of intermittent claudication. Human and animal studies have shown that pentoxifylline therapy results in a variety of physiological changes at the cellular level, which may be important in treating a diverse group of human afflictions. Immune modulation includes increased leukocyte deformability and chemotaxis, decreased endothelial leukocyte adhesion, decreased neutrophil degranulation and release of superoxides, decreased production of monocyte-derived tumor necrosis factor, decreased leukocyte responsiveness to interleukin 1 and tumor necrosis factor, inhibition of T and B lymphocyte activation, and decreased natural killer cell activity. Hypercoagulable states improve through decreased platelet aggregation and adhesion, increased plasminogen activator, increased plasmin, increased antithrombin III, decreased fibrinogen, decreased alpha 2-antiplasmin, decreased alpha 1-antitrypsin, and decreased alpha 2-macroglobulin. Wound healing and connective tissue disorders may respond to an increase in fibroblast collagenases and decreased collagen, fibronectin, and glycosaminoglycan production. Fibroblast responsiveness to tumor necrosis factor is also diminished. Potential medical uses of pentoxifylline are reviewed.

摘要

己酮可可碱(氧代己酮可可碱)是一种具有强大血液流变学特性的甲基黄嘌呤衍生物。在美国,它被用于治疗间歇性跛行。人体和动物研究表明,己酮可可碱治疗会在细胞水平上引发多种生理变化,这可能对治疗多种人类疾病具有重要意义。免疫调节包括增加白细胞变形性和趋化性、减少内皮细胞与白细胞的黏附、减少中性粒细胞脱颗粒和超氧化物释放、减少单核细胞衍生的肿瘤坏死因子生成、降低白细胞对白介素1和肿瘤坏死因子的反应性、抑制T和B淋巴细胞活化以及降低自然杀伤细胞活性。高凝状态通过减少血小板聚集和黏附、增加纤溶酶原激活物、增加纤溶酶、增加抗凝血酶III、降低纤维蛋白原、降低α2-抗纤溶酶、降低α1-抗胰蛋白酶以及降低α2-巨球蛋白而得到改善。伤口愈合和结缔组织疾病可能会因成纤维细胞胶原酶增加以及胶原蛋白、纤连蛋白和糖胺聚糖生成减少而得到改善。成纤维细胞对肿瘤坏死因子的反应性也会降低。本文对己酮可可碱的潜在医学用途进行了综述。

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