Phytochelators Intended for Clinical Use in Iron Overload, Other Diseases of Iron Imbalance and Free Radical Pathology.
Phytochelators Intended for Clinical Use in Iron Overload, Other Diseases of Iron Imbalance and Free Radical Pathology.
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DOI：
10.3390/molecules201119725
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发表时间：
2015-11-23
期刊：
影响因子：
--
通讯作者：
Kontoghiorghes GJ
中科院分区：
文献类型：
--
作者：
Kontoghiorghe CN;Kolnagou A;Kontoghiorghes GJ
铁螯合药物主要且广泛用于治疗地中海贫血和类似病症中的输血性铁过载。最近的体内和临床研究还表明，螯合剂，特别是去铁酮，可以有效地用于涉及自由基损伤和病理学的许多病症，包括神经变性、肾、肝、心脏病症和癌症。许多种类的植物螯合剂（希腊语：phyto（φ τ）-植物，chele（χηλ）-蟹爪）具有不同的螯合性能，包括类似于螯合药物的植物多酚，可以开发用于临床使用。植物螯合剂含羞草素和托酚酮已被鉴定为在治疗铁过载的动物模型中具有口服活性和有效性，并且麦芽酚用于治疗缺铁性贫血。开发临床使用的植物螯合剂需要许多关键参数，包括治疗靶点的表征、ADMET、治疗指数的鉴定以及与现有疗法相比的风险/获益评估。植物螯合剂可以被开发并用作主要、替代或辅助疗法，包括与合成螯合剂的组合疗法，以获得协同和/或互补的治疗效果。植物螯合剂的开发是一个具有挑战性的领域，用于引入新的药物，可用于许多疾病和衰老。与合成药物相比，这种开发的商业和其他考虑具有很大的优势，也可使发展中国家数百万病人受益。
Iron chelating drugs are primarily and widely used in the treatment of transfusional iron overload in thalassaemia and similar conditions. Recent in vivo and clinical studies have also shown that chelators, and in particular deferiprone, can be used effectively in many conditions involving free radical damage and pathology including neurodegenerative, renal, hepatic, cardiac conditions and cancer. Many classes of phytochelators (Greek: phyto (φυτό)—plant, chele (χηλή)—claw of the crab) with differing chelating properties, including plant polyphenols resembling chelating drugs, can be developed for clinical use. The phytochelators mimosine and tropolone have been identified to be orally active and effective in animal models for the treatment of iron overload and maltol for the treatment of iron deficiency anaemia. Many critical parameters are required for the development of phytochelators for clinical use including the characterization of the therapeutic targets, ADMET, identification of the therapeutic index and risk/benefit assessment by comparison to existing therapies. Phytochelators can be developed and used as main, alternative or adjuvant therapies including combination therapies with synthetic chelators for synergistic and or complimentary therapeutic effects. The development of phytochelators is a challenging area for the introduction of new pharmaceuticals which can be used in many diseases and also in ageing. The commercial and other considerations for such development have great advantages in comparison to synthetic drugs and could also benefit millions of patients in developing countries.
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影响因子：
11.4
作者：
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