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Potential applications of artemisinins in ocular diseases 被引量:8
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作者 Bing-Wen Lu Li-Ke Xie 《International Journal of Ophthalmology(English edition)》 SCIE CAS 2019年第11期1793-1800,共8页
Artemisinin, also named qinghaosu, is a family of sesquiterpene trioxane lactone originally derived from the sweet wormwood plant(Artemisia annua), which is a traditional Chinese herb that has been universally used as... Artemisinin, also named qinghaosu, is a family of sesquiterpene trioxane lactone originally derived from the sweet wormwood plant(Artemisia annua), which is a traditional Chinese herb that has been universally used as anti-malarial agents for many years. Evidence has accumulated during the past few years which demonstrated the protective effects of artemisinin and its derivatives(artemisinins) in several other diseases beyond malaria, including cancers, autoimmune disorders, inflammatory diseases, viral and other parasiterelated infections. Recently, this long-considered antimalarial agent has been proved to possess anti-oxidant, anti-inflammatory, anti-apoptotic and anti-excitotoxic properties, which make it a potential treatment option for the ocular environment. In this review, we first described the overview of artemisinins, highlighting the activity of artemisinins to other diseases beyond malaria and the mechanisms of these actions. We then emphasized the main points of published results of using artemisinins in targeting ocular disorders, including uveitis, retinoblastoma, retinal neurodegenerative diseases and ocular neovascularization. To conclude, we believe that artemisinins could also be used as a promising therapeutic drug for ocular diseases, especially retinal vascular diseases in the near future. 展开更多
关键词 artemisinins UVEITIS RETINOBLASTOMA retinal NEURODEGENERATIVE diseases OCULAR NEOVASCULARIZATION
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Designing Artemisinins with Antimalarial Potential, Combining Molecular Electrostatic Potential, Ligand-Heme Interaction and Multivariate Models
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作者 Josué de Jesus Oliveira Araújo Ricardo Morais de Miranda +10 位作者 Jeferson Stiver Oliveira de Castro Antonio Florêncio de Figueiredo Ana Cecília Barbosa Pinheiro Sílvia Simone dos Santos Morais Marcos Antonio Barros dos Santos Andréia de Lourdes Ribeiro Pinheiro Andréia de Lourdes Ribeiro Pinheiro Fábio dos Santos Gil Heriberto Rodrigues Bitencourt Gustavo Nery Ramos Alves José Ciríaco Pinheiro 《Computational Chemistry》 CAS 2023年第1期1-23,共23页
Artemisinins tested against W-2 strains of malaria falciparum are investigated with molecular electrostatic potential (MEP), in an attempt to identify key features of the compounds that are necessary for their activit... Artemisinins tested against W-2 strains of malaria falciparum are investigated with molecular electrostatic potential (MEP), in an attempt to identify key features of the compounds that are necessary for their activities, as well as to investigate likely interactions with the receptor in a biological process and to use that information to propose new molecules. In order to discover the best geometry involving the ligand-receptor complexes (heme) studied and help in the proposition of the new derivatives, molecular simulations of interactions between the most negative charged region around the peroxide and heme locates (the ones around the Fe2+ ion) were carried out. In addition, PCA (principal components analysis), HCA (hierarchical cluster analysis), SDA (stepwise discriminant analysis), and KNN (K-nearest neighbor) multivariate models were employed to investigate which descriptors are responsible for the classification between the higher and lower antimalarial activity of the compounds, and also this information was used to propose new potentially active molecules. The information accumulated in studies of MEP, molecular docking, and multivariate analysis supported the proposal of new structures with potential antimalarial activities. The multivariate models constructed were applied to the new structures and indicated numbers 19 and 20 as the most prominent for syntheses and biological assays. 展开更多
关键词 artemisinins Antimalarial Potential Molecular Electrostatic Potential Ligand-Heme Interaction Multivariate Models
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More than anti-malarial agents: therapeutic potential of artemisinins in neurodegeneration 被引量:4
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作者 Bing-Wen Lu Larry Baum +2 位作者 Kwok-Fai So Kin Chiu Li-Ke Xie 《Neural Regeneration Research》 SCIE CAS CSCD 2019年第9期1494-1498,共5页
Artemisinin,also called qinghaosu,is originally derived from the sweet wormwood plant(Artemisia annua),which is used in traditional Chinese medicine.Artemisinin and its derivatives(artemisinins)have been widely used f... Artemisinin,also called qinghaosu,is originally derived from the sweet wormwood plant(Artemisia annua),which is used in traditional Chinese medicine.Artemisinin and its derivatives(artemisinins)have been widely used for many years as anti-malarial agents,with few adverse side effects.Interestingly,evidence has recently shown that artemisinins might have a therapeutic value for several other diseases beyond malaria,including cancers,inflammatory diseases,and autoimmune disorders.Neurodegeneration is a challenging age-associated neurological disorder characterized by deterioration of neuronal structures as well as functions,whereas neuroinflammation has been considered to be an underlying factor in the development of various neurodegenerative disorders,including Alzheimer’s disease.Recently discovered properties of artemisinins suggested that they might be used to treat neurodegenerative disorders by decreasing oxidation,inflammation,and amyloid beta protein(Aβ).In this review,we will introduce artemisinins and highlight the possible mechanisms of their neuroprotective activities,suggesting that artemisinins might have therapeutic potential in neurodegenerative disorders. 展开更多
关键词 artemisinin inflammation neuroinflammation NEURODEGENERATION Alzheimer’s DISEASE Parkinson’s DISEASE ANTI-OXIDATION neuroprotection neural regeneration
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GetArtemisininsByAnymeans (GABA): artemisinins path to conquer diabetes go through GABA receptors
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作者 Xiaojie Bai Suneng Fu 《Science Bulletin》 SCIE EI CAS CSCD 2017年第6期383-385,共3页
Diabetes is a chronic disease of elevated blood glucose levels that affects more than 400 million people worldwide.Complications of diabetes affect the neuronal and the vascular systems and causes diabetic kidney dise... Diabetes is a chronic disease of elevated blood glucose levels that affects more than 400 million people worldwide.Complications of diabetes affect the neuronal and the vascular systems and causes diabetic kidney disease,cardiovascular disease,hypertension,retinopathy,peripheral neuropathy,and diabetic food diseases.Diabetes is caused by either the body’s inability to 展开更多
关键词 GABA cell artemisinins path to conquer diabetes go through GABA receptors Get artemisinins By Anymeans
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From ancient herb to modern miracle:an in-depth analysis of the cardioprotective effects of artemisinin and its derivatives
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作者 Hao-Shuang LI Shu-Rong LI +6 位作者 Wen-Jue LIU Yuan ZHANG Rui WU Xu-Yang CUI Jia-Zheng SUN You-Wei MA Ying ZHAO 《Journal of Geriatric Cardiology》 2026年第1期45-64,共20页
Significant progress has been recently made in studying artemisinin and its derivatives for treating cardiovascular diseases,making this area a prominent research focus.Artemisinin,discovered with great acclaim,was in... Significant progress has been recently made in studying artemisinin and its derivatives for treating cardiovascular diseases,making this area a prominent research focus.Artemisinin,discovered with great acclaim,was initially and widely adopted in antimalarial treatments.As scientific research steadily progressed,its latent potential role in the cardiovascular system gradually captured the attention of the global scientific community.Artemisinin and its derivatives can reportedly play a protective role in the cardiovascular system through various mechanisms,including anti-inflammatory,anti-angiogenic,antioxidant,and anti-fibrotic effects,as well as the regulation of blood lipids and blood pressure.In particular,they have shown promising therapeutic effects in models of cardiovascular diseases such as atherosclerosis,myocardial ischaemia,and cardiac hypertrophy.In addition,artemisinin and its derivatives can improve cardiovascular function and prevent cardiovascular injury by regulating signalling pathways closely related to cardiovascular disease,such as AMPK and NF-kB.Although numerous ex vivo and in vivo experiments have verified the potential role of artemisinin in treating cardiovascular diseases,systematic studies to comprehensively elucidate its specific mechanism of action remain scarce.Further exploration of the precise roles of artemisinin and its derivatives in cardiovascular disease therapy,along with their potential clinical applications,could offer valuable insights for future research and treatment strategies. 展开更多
关键词 antimalarial treatmentsas ARTEMISININ cardiovascular diseasesmaking myocardial ischemia cardiac hypertrophy cardiovascular system cardioprotective effects ATHEROSCLEROSIS
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Nanocarriers to Enhance Solubility, Bioavailability, and Efficacy of Artemisinins 被引量:1
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作者 Anna Rita Bilia Maria Camilla Bergonzi +1 位作者 Joelle CBoulos Thomas Efferth 《World Journal of Traditional Chinese Medicine》 2020年第1期26-38,共13页
The therapeutic potential of artemisinin (ART) and its derivatives (ARTs) is not limited to malaria but has been recently expanded to other infections with protozoans, trematodes, or viruses as well as to cancer. Due ... The therapeutic potential of artemisinin (ART) and its derivatives (ARTs) is not limited to malaria but has been recently expanded to other infections with protozoans, trematodes, or viruses as well as to cancer. Due to their limited poor water and oil solubility, rapid degradation by the liver, and short half-life, they have a low bioavailability after oral administration. Consequently, there is a pressing necessity to formulate new ART preparations to raise its bioavailability and efficacy. Nanosized drug delivery systems represent important tools in modern medicine with wide clinical applications, because of their potential modulation of pharmacokinetic and biodistribution. This review focuses on polymer-based systems, lipid-based systems, and inorganic nanoparticles loaded with ARTs. The overall goal of this field of research is to enhance their solubility and stability to improve bioavailability at much lower doses and to increase long-term safety. In addition, the opportunity to reach highly specific site-targeted delivery by these nanocarriers confers a high medicinal value. Remarkably, most of the reported nanoparticulate drug delivery systems are biologically inactive or marginally immunogenic, generating no antigenic or pyrogenic reactions but only partial intrinsic toxicity. As clinical studies in human patients are available so far, there is a pressing need to translate preclinical results on ART-based nanosystems into clinical settings. 展开更多
关键词 ARTEMISININ Asteraceae derivatives inorganic nanocarriers lipid nanocarriers nanotechnology polymeric nanocarriers sesquiterpene lactones
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Interpersonal Sensitivity Prediction Based on Multi-strategy Artemisinin Optimization with Fuzzy K-Nearest Neighbor
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作者 Yiguo Tian Xiao Pan +2 位作者 Xinsen Zhou Lei Liu Da Wei 《Journal of Bionic Engineering》 2025年第3期1484-1505,共22页
The mental health issues of college students have become an increasingly prominent social problem,exerting severe impacts on their academic performance and overall well-being.Early identification of Interpersonal Sens... The mental health issues of college students have become an increasingly prominent social problem,exerting severe impacts on their academic performance and overall well-being.Early identification of Interpersonal Sensitivity(IS)in students serves as an effective approach to detect psychological problems and provide timely intervention.In this study,958 freshmen from higher education institutions in Zhejiang Province were selected as participants.We proposed a Multi-Strategy Artemisinin Optimization(MSAO)algorithm by enhancing the Artemisinin Optimization(AO)framework through the integration of a group-guided elimination strategy and a two-stage consolidation strategy.Subsequently,the MSAO was combined with the Fuzzy K-Nearest Neighbor(FKNN)classifier to develop the bMSAO-FKNN predictive model for assessing college students’IS.The proposed algorithm’s efficacy was validated through the CEC 2017 benchmark test suite,while the model’s performance was evaluated on the IS dataset,achieving an accuracy rate of 97.81%.These findings demonstrate that the bMSAO-FKNN model not only ensures high predictive accuracy but also offers interpretability for IS prediction,making it a valuable tool for mental health monitoring in academic settings. 展开更多
关键词 Interpersonal sensitivity Feature selection Metaheuristic algorithm Artemisinin optimization
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Traditional Chinese Medicine in Uganda:History,Present,and Future
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作者 LIN Jie HAN Xue Namusiitwa Resty 《Chinese Medicine and Culture》 2025年第4期431-440,共10页
In the context of globalization,traditional Chinese medicine(TCM)has transcended geographical boundaries to provide the world with Chinese philosophical principles and therapeutic methodologies,which have been welcome... In the context of globalization,traditional Chinese medicine(TCM)has transcended geographical boundaries to provide the world with Chinese philosophical principles and therapeutic methodologies,which have been welcomed by the people of the world.Similarly,Uganda’s indigenous medical traditions embody profound ethnomedical knowledge,creating a robust foundation for cross-cultural exchanges in phytotherapy between the two nations.The introduction of TCM to Uganda started in the 1980s,facilitated by successive Chinese medical teams dispatched under the framework of Sino-African health cooperation,and has engendered a gradual yet sustained trajectory of acceptance and integration within local healthcare systems.Empirical evidence indicates that TCM’s therapeutic efficacy,cultural adaptability,and cost-effectiveness have progressively contributed to its growing institutional recognition and community-level adoption across Uganda’s diverse demographic groups since its initial dissemination.Therapeutic approaches such as acupuncture and massage,along with the remarkable efficacy of artemisinin in combating malaria,offer local populations more options for disease prevention and health maintenance.This paper examines the historical development and current practices of TCM in Uganda,aiming to provide insights and recommendations for addressing challenges related to infectious disease control,chronic disease management,and health resource accessibility in Africa and other underdeveloped regions.Furthermore,it proposes cross-cultural implementation strategies for integrating traditional medicine into the global health governance framework,thereby contributing to the construction of a global community of health. 展开更多
关键词 Uganda Traditional Chinese medicine The Silk Road ACUPUNCTURE ARTEMISININ Forum on China-Africa Cooperation(FOCAC)
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Effects of Fungal Elicitors on Cell Growth and Artemisinin Accumulation in Hairy Root Cultures of Artemisia annua 被引量:13
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作者 王红 叶和春 +2 位作者 李国凤 刘本叶 种康 《Acta Botanica Sinica》 CSCD 2000年第9期905-909,共5页
The artemisinin accumulation in the hairy root cultures of Artemisia annua L. was enhanced via a treatment of three fungal elicitors separately ( Verticillium dahliae Kleb., Rhizopus stolonifer (Ehrenb. ex ... The artemisinin accumulation in the hairy root cultures of Artemisia annua L. was enhanced via a treatment of three fungal elicitors separately ( Verticillium dahliae Kleb., Rhizopus stolonifer (Ehrenb. ex Fr.) Vuill and Colletotrichum dematium (Pers.) Grove). Among these three elicitors, V. dahliae had the highest inducing efficiency, but none of them manifests any noticeable effects on the cell growth of the hairy root cultures. The artemisinin content of the hairy root cultures treated with V. dahliae elicitor was 1.12 mg/g DW, which was 45% higher than the control (0.77 mg/g DW). The results showed that elicitation was dependent on the elicitor concentration, the incubation period and the physiological stage at which the hairy root cultures were treated. In addition, the authors found that for V. dahliae , the optimum concentration was 0.4 mg carbohydrate per millilitre medium, the strongest response of A. annua hairy root cultures to the elicitation was at the late exponential growth stage, and the highest artemisinin content of the hairy root cultures was on the 4th day post treatment. 展开更多
关键词 Artemisia annua hairy root cultures ARTEMISININ fungal elicitor
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Elicitation on Artemisinin Biosynthesis in Artemisia annua Hairy Roots by the Oligosaccharide Extract from the Endophytic Colletotrichum sp. B501 被引量:12
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作者 王剑文 夏仲豪 谭仁祥 《Acta Botanica Sinica》 CSCD 2002年第10期1233-1238,共6页
The oligosaccharide elicitor from the mycelial wall of an endophytic Colletotrichum sp. B501 promoted the production of artemisinin in Artemisia annua L. hairy root culture. When hairy roots of 22-day-old cultures (la... The oligosaccharide elicitor from the mycelial wall of an endophytic Colletotrichum sp. B501 promoted the production of artemisinin in Artemisia annua L. hairy root culture. When hairy roots of 22-day-old cultures (later growth phase) were exposed to the elicitor (20 mg/L) for 4 d, the maximum content of artemisinin reached 1.15 mg/g, a 64.29% increment over the control. The electron X-ray microanalysis disclosed the rapid accumulation of Ca 2+ in the elicited cortical cells of hairy root. The electronic microscope observation revealed the high electron density area in vacuole of elicited cells. During the first day of elicitation the peroxidase activity of hairy roots was improved sharply. Some cellular morphological changes including cell shrinkage, condensation of cytoplasm and nuclear fragmentation, coincident with the appearance of DNA ladders, were observed after the third day of elicitation. It was suggested that the oligosaccharide elicitor triggered the programmed cell death, which may provide the substance or chemical signal for artemisinin biosynthesis. 展开更多
关键词 Artemisia annua Colletotrichum sp. B501 a fungal endophyte oligosaccharide elicitor ARTEMISININ eliciting response
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青蒿素之母——2015年诺贝尔生理学或医学奖新科得主屠呦呦(二) 被引量:11
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作者 朱安远 郭华珍 《中国市场》 2016年第14期186-194,共9页
2015年10月5日,中国中医科学院(原中国中医研究院)终身研究员兼首席研究员、女药学家、药物化学家、医学家和教育家屠呦呦以创制新型抗疟药物——青蒿素及其首个衍生物双氢青蒿素而赢得当年诺贝尔生理学或医学奖之殊荣,特大喜讯传来,国... 2015年10月5日,中国中医科学院(原中国中医研究院)终身研究员兼首席研究员、女药学家、药物化学家、医学家和教育家屠呦呦以创制新型抗疟药物——青蒿素及其首个衍生物双氢青蒿素而赢得当年诺贝尔生理学或医学奖之殊荣,特大喜讯传来,国内舆论媒体亢奋,国人无不欢欣鼓舞。屠呦呦先生是首位荣获诺贝尔科学奖的中国大陆本土科学家、首位华裔女性诺奖得主和诺医奖得主,这是中国医学界尤其是中医学界的重大历史性突破,这一荣耀将永远铭记在中国科技发展史上。详细介绍了屠呦呦女士的生平、主要学术成就与贡献、与疟疾直接相关的诺医奖以及青蒿素类抗疟药物获得的各种国内外奖项,简明扼要地阐述了青蒿素类抗疟药物的发现(发明)简史,不惜浓墨重彩全方位地展示了以屠呦呦为杰出代表的中国科学家群英谱的奋斗历程和辉煌成就。 展开更多
关键词 屠呦呦 寄生虫病 疟疾(malaria) 疟原虫 抗疟药物(antimalarial drug) 剂型 抗药性(耐药性) 中药 西药(化学药品) 青蒿 黄花蒿 青蒿素(artemisinin) 衍生物(derivative) 双氢青蒿素DHA(dihydroartemisinin) 蒿甲醚(artemether) 蒿乙醚(artemotil/arteether) 青蒿琥酯(artesunate) 卡罗琳医学院诺贝尔大会 生理学或医学奖诺贝尔委员会(医诺委) 诺贝尔生理学或医学奖(诺医奖)
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Selective Effect of Qinghaosu on Different Stages of Plasmodium falciparum in Vitro 被引量:1
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作者 叶祖光 CarolynDoak KnoxVanDyke 《Journal of Chinese Pharmaceutical Sciences》 CAS 1993年第1期64-68,共5页
Using highly synchronous cultures of Plasmodium falciparum in vitro,the susceptibi- lity of the different stages of the intraerythrocytic parasites to Qinghaosu (QHS) was assessed.The anti- parasitic effect of QHS was... Using highly synchronous cultures of Plasmodium falciparum in vitro,the susceptibi- lity of the different stages of the intraerythrocytic parasites to Qinghaosu (QHS) was assessed.The anti- parasitic effect of QHS was measured by comparing the changes of irradiation of^3 H-hypoxanthine in- corporated into the nucleic acids of parasites exposed to various concentrations of QHS at different stages of growth.It was found that the trophozoite stage of the parasite was the most sensitive to QHS, whereas the early ring stage was the least sensitive,and the sensitivities of the late ring and schizont stages fell between those of the early ring and trophozoite stages.The results revealed the correlation of stage-dependent effects of QHS with the blockade of the protein metabolism of the parasite. 展开更多
关键词 Qinghaosu(artemisinin) Antimalarial drug Plasmodium falciparum MALARIA
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青蒿素之母——2015年诺贝尔生理学或医学奖新科得主屠呦呦(一) 被引量:10
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作者 朱安远 郭华珍 《中国市场》 2016年第9期199-208,共10页
2015年10月5日,中国中医科学院(原中国中医研究院)终身研究员兼首席研究员、女药学家、药物化学家、医学家和教育家屠呦呦以创制新型抗疟药物——青蒿素及其首个衍生物双氢青蒿素而赢得当年诺贝尔生理学或医学奖之殊荣,特大喜讯传来,国... 2015年10月5日,中国中医科学院(原中国中医研究院)终身研究员兼首席研究员、女药学家、药物化学家、医学家和教育家屠呦呦以创制新型抗疟药物——青蒿素及其首个衍生物双氢青蒿素而赢得当年诺贝尔生理学或医学奖之殊荣,特大喜讯传来,国内舆论媒体亢奋,国人无不欢欣鼓舞。屠呦呦先生是首位荣获诺贝尔科学奖的中国大陆本土科学家、首位华裔女性诺奖得主和诺医奖得主,这是中国医学界尤其是中医学界的重大历史性突破,这一荣耀将永远铭记在中国科技发展史上。详细介绍了屠呦呦女士的生平、主要学术成就与贡献、与疟疾直接相关的诺医奖以及青蒿素类抗疟药物获得的各种国内外奖项,简明扼要地阐述了青蒿素类抗疟药物的发现(发明)简史,不惜浓墨重彩全方位地展示了以屠呦呦为杰出代表的中国科学家群英谱的奋斗历程和辉煌成就。 展开更多
关键词 屠呦呦 寄生虫病 疟疾(malaria) 疟原虫 抗疟药物(antimalarial drug) 剂型 抗药性(耐药性) 中药 西药(化学药品) 青蒿 黄花蒿 青蒿素(artemisinin) 衍生物(derivative) 双氢青蒿素DHA(dihydroartemisinin) 蒿甲醚(artemether) 蒿乙醚(artemotil/arteether) 青蒿琥酯(artesunate) 卡罗琳医学院诺贝尔大会 生理学或医学奖诺贝尔委员会(医诺委) 诺贝尔生理学或医学奖(诺医奖)
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青蒿素之母——2015年诺贝尔生理学或医学奖新科得主屠呦呦(三) 被引量:8
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作者 朱安远 郭华珍 《中国市场》 2016年第18期233-245,共13页
2015年10月5日,中国中医科学院(原中国中医研究院)终身研究员兼首席研究员、女药学家、药物化学家、医学家和教育家屠呦呦以创制新型抗疟药物——青蒿素及其首个衍生物双氢青蒿素而赢得当年诺贝尔生理学或医学奖之殊荣,特大喜讯传来,国... 2015年10月5日,中国中医科学院(原中国中医研究院)终身研究员兼首席研究员、女药学家、药物化学家、医学家和教育家屠呦呦以创制新型抗疟药物——青蒿素及其首个衍生物双氢青蒿素而赢得当年诺贝尔生理学或医学奖之殊荣,特大喜讯传来,国内舆论媒体亢奋,国人无不欢欣鼓舞。屠呦呦先生是首位荣获诺贝尔科学奖的中国大陆本土科学家、首位华裔女性诺奖得主和诺医奖得主,这是中国医学界尤其是中医学界的重大历史性突破,这一荣耀将永远铭记在中国科技发展史上。详细介绍了屠呦呦女士的生平、主要学术成就与贡献、与疟疾直接相关的诺医奖以及青蒿素类抗疟药物获得的各种国内外奖项,简明扼要地阐述了青蒿素类抗疟药物的发现(发明)简史,不惜浓墨重彩全方位地展示了以屠呦呦为杰出代表的中国科学家群英谱的奋斗历程和辉煌成就。 展开更多
关键词 屠呦呦 寄生虫病 疟疾(malaria) 疟原虫 抗疟药物(antimalarial drug) 剂型 抗药性(耐药性) 中药 西药(化学药品) 青蒿 黄花蒿 青蒿素(artemisinin) 衍生物(derivative) 双氢青蒿素DHA(dihydroartemisinin) 蒿甲醚(artemether) 蒿乙醚(artemotil/arteether) 青蒿琥酯(artesunate) 卡罗琳医学院诺贝尔大会 生理学或医学奖诺贝尔委员会(医诺委) 诺贝尔生理学或医学奖(诺医奖)
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青蒿素之母——2015年诺贝尔生理学或医学奖新科得主屠呦呦(四) 被引量:9
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作者 朱安远 郭华珍 《中国市场》 2016年第22期260-272,共13页
2015年10月5日,中国中医科学院(原中国中医研究院)终身研究员兼首席研究员、女药学家、药物化学家、医学家和教育家屠呦呦以创制新型抗疟药物——青蒿素及其首个衍生物双氢青蒿素而赢得当年诺贝尔生理学或医学奖之殊荣,特大喜讯传来,国... 2015年10月5日,中国中医科学院(原中国中医研究院)终身研究员兼首席研究员、女药学家、药物化学家、医学家和教育家屠呦呦以创制新型抗疟药物——青蒿素及其首个衍生物双氢青蒿素而赢得当年诺贝尔生理学或医学奖之殊荣,特大喜讯传来,国内舆论媒体亢奋,国人无不欢欣鼓舞。屠呦呦先生是首位荣获诺贝尔科学奖的中国大陆本土科学家、首位华裔女性诺奖得主和诺医奖得主,这是中国医学界尤其是中医学界的重大历史性突破,这一荣耀将永远铭记在中国科技发展史上。详细介绍了屠呦呦女士的生平、主要学术成就与贡献、与疟疾直接相关的诺医奖以及青蒿素类抗疟药物获得的各种国内外奖项,简明扼要地阐述了青蒿素类抗疟药物的发现(发明)简史,不惜浓墨重彩全方位地展示了以屠呦呦为杰出代表的中国科学家群英谱的奋斗历程和辉煌成就。 展开更多
关键词 屠呦呦 寄生虫病 疟疾(malaria) 疟原虫 抗疟药物(antimalarial drug) 剂型 抗药性(耐药性) 中药 西药(化学药品) 青蒿 黄花蒿 青蒿素(artemisinin) 衍生物(derivative) 双氢青蒿素DHA(dihydroartemisinin) 蒿甲醚(artemether) 蒿乙醚(artemotil/arteether) 青蒿琥酯(artesunate) 卡罗琳医学院诺贝尔大会 生理学或医学奖诺贝尔委员会(医诺委) 诺贝尔生理学或医学奖(诺医奖)
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Reversing artemisinin resistance by leveraging thermo-responsive nanoplatform to downregulating GSH
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作者 Yong-Dan Zhao Yidan Wang +9 位作者 Rongrong Wang Lina Chen Hengtong Zuo Xi Wang Jihong Qiang Geng Wang Qingxia Li Canqi Ping Shuqiu Zhang Hao Wang 《Chinese Chemical Letters》 SCIE CAS CSCD 2024年第6期392-397,共6页
Artemisinin(ART)resistance has been an emerging clinical problem,severely compromising antimalarial efficacy and threatening the global malaria elimination campaign.Albeit intensive studies about the molecular mechani... Artemisinin(ART)resistance has been an emerging clinical problem,severely compromising antimalarial efficacy and threatening the global malaria elimination campaign.Albeit intensive studies about the molecular mechanism for ART resistance are under way,no effective therapeutic targets for reversing resistance have been applied.Here,we explore glutathione(GSH)as a therapeutic target to develop a thermo-responsive nanoplatform to specifically co-deliver ART and GSH synthesis inhibitor(L-buthionine sulfoximine,BSO)in a sustained manner,effectively reversing ART resistance in vivo.By combining with BSO,ART exerts increased antimalarial activity with reduced half-maximal inhibitory concentration(IC50)by 7.43-fold in ART-resistant strains.This work reveals that the GSH in ART-resistant parasites can be a promising therapeutic target for reversing ART resistance,paving the way for developing drug candidates and intelligent nanomedicines in malaria therapy. 展开更多
关键词 NANOMEDICINES Drug delivery artemisinins resistance Malaria GLUTATHIONE
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Biotransformation of Artemisinin by Hairy Root Cultures of Rheum palmatum L. 被引量:3
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作者 李莉欣 苏艳芳 +1 位作者 刘晓峰 果德安 《Journal of Chinese Pharmaceutical Sciences》 CAS 2002年第4期122-124,共3页
The biotransformation of artemisinin by hairy root cultures ofRheum palmatum L. was investigated for the first time. The main product, deoxyartemisinin, was isolated and characterized on the basis of its spectral data.
关键词 ARTEMISININ Deoxyartemisinin Rheum palmatum hairy root cultures BIOTRANSFORMATION
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Preparation of the nanostructured lipid carriers of artemisinin and its pharmacokinetic evaluation 被引量:2
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作者 代华灵 高伟祺 +2 位作者 张国顺 王锐利 张淑秋 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2017年第3期180-186,共7页
Artemisinin(ART) is a widely used active drug for malaria, including severe and cerebral malaria. However, its therapeutic efficacy is affected by its lower bioavailability. In the present study, nanostructured lipi... Artemisinin(ART) is a widely used active drug for malaria, including severe and cerebral malaria. However, its therapeutic efficacy is affected by its lower bioavailability. In the present study, nanostructured lipid carriers(NLCs) were proposed as carrier of ART to improve pharmacokinetic properties of the drug. ART-NLC was prepared by high-pressure homogenization based on orthogonal design. The particle size, zeta potential, encapsulation efficiency(EE) and percentage of drug loading(DL) of ART-NLC were(53.06±2.11) nm,(–28.7±3.59) m V, 73.9%±0.5% and 11.23%±0.37%, respectively. ART-NLC showed the sustained release characteristics and scarcely the hemolysis effect on human red blood cells. The pharmacokinetics of ART-NLC for rats after tail intravenous injection(i.v) or intraperitoneal injection(i.p) were investigated by liquid chromatography-tandem mass spectroscopy(LC-MS/MS). And ART solution was designed as control preparation. For rats of i.v groups, the AUC0–∞((707.45±145.65) ng·h/m L) of ART-NLC were significantly bigger than that of ART((368.98±139.58) ng·h/m L). The MRT((3.38±0.46) h) of ART-NLC was longer than that of ART((1.39±0.61) h). And similar results were observed for rats of i.p groups. The AUC0–∞((1233.06±235.57) ng·h/m L) and MRT((4.97±0.69) h) of ART-NLC were both bigger than those of ART, which were(871.17±234.03) ng·h/m L) and(1.75±0.31) h), respectively. Compared with ART, ART-NLC showed a significant increase in AUC0–∞(P〈0.05) and MRT(P〈0.001) for both i.p and tail i.v administrations. 展开更多
关键词 ARTEMISININ Nanostructured lipid carriers PHARMACOKINETICS LC-MS/MS
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Research Progresses on Extraction and Detection Techniques of Artemisinin 被引量:2
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作者 廖巧 龙世平 杨春贤 《Agricultural Science & Technology》 CAS 2012年第8期1631-1636,共6页
[Objective] The aim was to make a summary on research progresses on extraction and detection techniques of artemisinin. [Method] In the research, the concerning progress was made based on physicochemical property, sou... [Objective] The aim was to make a summary on research progresses on extraction and detection techniques of artemisinin. [Method] In the research, the concerning progress was made based on physicochemical property, source, extraction methods and detection technology of artemisinin. [Result] Artemisinin is colorless acicular crystal and easier to be dissolved in organic solvent. The extraction methods of artemisinin include organic solvent extraction, ultrasonic extraction, microwave extraction and supercritical fluid extraction; the detection technologies include ultraviolet spectrophotometry, high performance liquid chromatography and HPLC-evaporative light-scattering. [Conclusion] The research laid foundation for further exploration and global market. 展开更多
关键词 ARTEMISININ EXTRACTION Content detection
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Artemisinin, the Magic Drug Discovered from Traditional Chinese Medicine 被引量:28
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作者 Jigang Wang Chengchao Xu +4 位作者 Yin Kwan Wong Yujie Li Fulong Liao Tingliang Jiang Youyou Tu 《Engineering》 SCIE EI 2019年第1期32-39,共8页
Artemisinin and its derivatives represent the most important and influential class of drugs in the fight against malaria. Since the discovery of artemisinin in the early 1970s, the global community has made great stri... Artemisinin and its derivatives represent the most important and influential class of drugs in the fight against malaria. Since the discovery of artemisinin in the early 1970s, the global community has made great strides in characterizing and understanding this remarkable phytochemical and its unique chemical and pharmacological properties. Today, even as artemisinin continues to serve as the foundation for antimalarial therapy, numerous challenges have surfaced in the continued application and development of this family of drugs. These challenges include the emergence of delayed treatment responses to artemisinins in malaria and efforts to apply artemisinins for non-malarial indications. Here, we provide an overview of the story of artemisinin in terms of its past, present, and future. In particular, we comment on the current understanding of the mechanism of action (MOA) of artemisinins, and emphasize the importance of relating mechanistic studies to therapeutic outcomes, both in malarial and non-malarial contexts. 展开更多
关键词 ARTEMISININ Mechanism of action MALARIA ANTI-CANCER
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