青蒿素类药物的抗疟机制及耐药性产生研究进展

doi:10.3969/j.issn.1000-8535.2018.02.032

广州医药 ›› 2018, Vol. 49 ›› Issue (2): 119-122.DOI: 10.3969/j.issn.1000-8535.2018.02.032

青蒿素类药物的抗疟机制及耐药性产生研究进展

杨美君¹, 于家瀛², 郄舒楠², 罗薇², 李学强^2,3, 魏梦雪^2,3

1 宁夏回族自治区人民医院西夏分院药剂科(银川750001)
2 宁夏天然药物工程技术研究中心(银川 750021)
3 省部共建煤炭高效利用与绿色化工国家重点实验室,宁夏大学化学化工学院(银川 750021)

收稿日期:2017-12-13 出版日期:2018-03-20 发布日期:2021-12-01
通讯作者: 李学强,E-mail:lixq@nxu.edu.cn;魏梦雪,E-mail:weimengxue@nxu.edu.cn
基金资助:
国家自然科学基金(21462032);宁夏自然科学基金(NZ17001);大学生创新创业训练计划项目(宁夏大学)(G201610749014,Q201710749028)

Advances in the synthesis and antimalarial study of artemisinin and its heteroatomic derivatives

YANG Meijun¹, YU Jiaying², QIE Shunan², LUO Wei², LI Xueqiang^2,3, WEI Mengxue^2,3

1. Department of Pharmacy, Xixia Branch, People's Hospital of Ningxia, Yinchuan 750001, China
2. Ningxia Engineering Research Center for Natural Medicines, Yinchuan 750021, China
3. State Key Laboratory of High-efficiency Utilization of Coal and Green Chemical Engineering, School of Chemistry and Chemical Engineering, Ningxia University, Yinchuan 750021, China

Received:2017-12-13 Online:2018-03-20 Published:2021-12-01

摘要/Abstract

摘要： 青蒿素类药物作为抗疟特效药,其特殊分子骨架和过氧基在抗疟中起着关键作用。通过损伤虫体的器膜、诱导蛋白变性、抑制ATP 蛋白6(Pf ATP6)活性等方式杀灭疟原虫。恶性疟原虫基因序列的突变和长期不规范用药均会使其产生耐药性。本文依据文献报道,对世界关于青蒿素类药物抗疟机制、耐药性的产生原因作一综述。

关键词: 青蒿素, 分子骨架, 过氧基, 抗疟活性, 耐药性

Abstract: Artemisinin is an effective anti-malaria drug, It's special molecular framework and peroxy group play a key role in antimalarial. Plasmodium falciparum was killed by the inducing cytoplasmic organelledamage protein denaturation, inhibiting ATP6 activity. Mutations in the genetic sequence of plasmodium falciparum and long-time using drugs without rule will develop drug resistance. This article is based on the literature, do a review of the world's causes for the resistance of artemisinin to antimalarial mechanisms.

Key words: Artemisinin, Molecular skeleton, Peroxide group, Antimalarial activity, Drug resistance

杨美君, 于家瀛, 郄舒楠, 罗薇, 李学强, 魏梦雪. 青蒿素类药物的抗疟机制及耐药性产生研究进展[J]. 广州医药, 2018, 49(2): 119-122.

YANG Meijun, YU Jiaying, QIE Shunan, LUO Wei, LI Xueqiang, WEI Mengxue. Advances in the synthesis and antimalarial study of artemisinin and its heteroatomic derivatives[J]. Guangzhou Medical Journal, 2018, 49(2): 119-122.

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青蒿素类药物的抗疟机制及耐药性产生研究进展

Advances in the synthesis and antimalarial study of artemisinin and its heteroatomic derivatives

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