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疟疾和青蒿素衍生物:最新综述。

Malaria and artemisinin derivatives: an updated review.

机构信息

Department of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan, 60800.

出版信息

Mini Rev Med Chem. 2013 Nov;13(13):1879-902. doi: 10.2174/13895575113136660097.

Abstract

Malaria is the world's most prevalent disease that affects 515-600 million people each year and about 40% of the world's population live at risk for this infection. The prevalence of morbidity and mortality from drug resistant malaria (Plasmodium falciparum) is increasing in most of the developing countries, which is also a global threat because international travel is common now and imported malaria is increasingly a serious problem. Since rapid schizonticidal action of naturally occurring endoperoxides pharmacophore present in artemisinin against drug-resistant malaria has been documented, researchers have focused more on artemisinin analogs than any other antimalarials. In this review, drugs of choice about malaria i.e. artemisinin and its analogus/derivatives (arteether, artemether, artemiside, artemisinin, artemisone, artesunate, dihydroartemisinin) have been discussed in detail e.g. bioavailability, formulation development, stability, combination therapy, additional benefits, drug resistance and toxicity have been reviewed.

摘要

疟疾是世界上最流行的疾病,每年影响 5.15 亿至 6 亿人,约有 40%的世界人口面临这种感染的风险。在大多数发展中国家,抗药性疟疾(疟原虫)的发病率和死亡率呈上升趋势,这也是一个全球性的威胁,因为现在国际旅行很普遍,输入性疟疾日益成为一个严重的问题。由于已经证明天然内过氧化物药效团在青蒿素中对抗药性疟疾具有快速裂殖体杀伤作用,研究人员对青蒿素类似物的关注超过了任何其他抗疟药物。在这篇综述中,详细讨论了治疗疟疾的首选药物,即青蒿素及其类似物/衍生物(蒿甲醚、青蒿琥酯、青蒿素、蒿乙醚、青蒿素酮、青蒿琥酯、双氢青蒿素),例如生物利用度、制剂开发、稳定性、联合治疗、额外益处、耐药性和毒性。

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