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The Search for antimalarial drugs and the Discovery of Artemisinin

Chinese Annals of History of Science and Technology 2020年第2期4卷 73-134页

作者： LI Runhong ZHANG Daqing The School of Health Humanities Peking UniversityBeijing 100191China

With its novel chemical structure, artemisinin is an antimalarial component isolated from the traditional Chinese medicine qinghao(Artemisia annua L.). Nowadays, artemisinin and its derivatives are used compatibly with new synthesized chemical antimalarial compounds to create artemisinin-based combination therapies(ACTs). These have become the first choice in treating malaria p.f. all over the world, providing an effective solution for the global challenge of curing drug-resistant malaria. Among the five ACTs recommended by the WHO, two were initiated in China and are used as the first-line treatment of falciparum malaria in all malaria endemic areas. As the use of artemisinin-based compound drugs have made such significant contributions to rolling back malaria, regarded as one of the great achievements globally in public health of the early twenty-first century, Tu Youyou, one of the most important researchers in the discovery of artemisinin, was made the first Nobel Prize laureate in Physiology or Medicine from the Chinese mainland. Artemisinin was discovered in a special social and cultural context through a combination of the exploration of traditional Chinese medical literature with the modern research approach of pharmaceutical sciences. This(Project 523) is a typical case of goal-oriented research leading to scientific advance, and the result of scientific research driven by the national needs.

关键词： antimalarial drugs artemisinin artemisinin-based compound drugs Tu Youyou

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Surveillance of antimalarial drug resistance in China in the 1980s–1990s

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Infectious Diseases of Poverty 2014年第1期3卷 62-69页

作者： De-quan Liu National Institute of Parasitic Diseases Chinese Center for Disease Control and Prevention200025 ShanghaiChina

Since the successful preparation of the microplates and the medium for field application,the resistance degree and its geographical distribution of chloroquine-resistant Plasmodium falciparum,the fluctuation of the resistance degree of *** to chloroquine,and the sensitivity of the parasite to commonly used antimalarial drugs were investigated between 1980 and 2003 by the in vitro microtest and the in vivo four-week test recommended by the World Health Organization(WHO).The results indicated that chloroquine-resistant falciparum malaria was present in all eight provinces/autonomous regions endemic for falciparum malaria in China,and the resistance was high and widely distributed in the Hainan and Yunnan *** the use of chloroquine was stopped or administered in a decreased quanity,the drug resistance gradually *** Hainan and Yunnan,*** was still highly resistant to chloroquine,amodiaquine and piperaquine,and sensitive to pyronaridine and artemisinin derivatives,but the sensitivity was gradually *** on these results,principles and therapeutic regimens for antimalarial drug use in China were formulated,the use of the antimalarials which had already developed resistance was stopped or reduced,and recommendations to use artemisinin derivatives or compound pyronaridine to promote a rational use of antimalarials and strengthen malaria control were *** results showed that malaria incidence had declined,and endemic areas of falciparum malaria have been gradually reducing since the mid-1980s.

关键词： Plasmodium falciparum Resistance Sensitivity antimalarial drugs in vivo in vitro Surveillance

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Mass media exposure and its impact on malaria prevention behaviour among adult women in sub-Saharan Africa:results from malaria indicator surveys

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Global Health Research and Policy 2018年第1期3卷 175-183页

作者： Sanni Yaya Olalekan A.Uthman Agbessi Amouzou Ghose Bishwajit School of International Development and Global Studies University of Ottawa120University PrivateOttawaON K1N 6N5Canada Warwick Centre for Applied Health Research and Delivery(WCAHRD) Division of Health SciencesWarwick Medical SchoolUniversity of WarwickCoventry CV47ALUK Bloomberg School of Public Health Johns Hopkins University615 N Wolfe StBaltimoreMD 21205USA

Background:Mass media exposure plays a pivotal role in health communication and adoption of a healthy *** this study,we aimed to measure the prevalence of malaria prevention behaviour among adult women in eight malariaendemic countries in sub-Saharan Africa(SSA),and assess the influence of mass media exposure in the adoption of those ***:For this study,we collected cross-sectional data on 46,822 women aged between 15 and 49 years from the Malaria Indicator Surveys(MIS)conducted in Burkina Faso,Ghana,Mali,Malawi,Kenya,Nigeria,Sierra Leone and *** the outcome variable,malaria prevention behaviour was proxied by the use of insecticide treated nets(ITNs)and uptake of antimalarial drugs in last ***:The overall prevalence of sleeping under ITN and that of taking antimalarial drug during the last pregnancy was respectively 67.9%(95%CI=66.6-69.2)and 72.8%(95%CI=71.3-74.2).However,there were disparities in the prevalence of using ITN and antimalarial drug use across the study *** the multivariable regression analysis,not receiving malaria related information from radio,poster/billboards,community events,and health workers were found to be significantly associated with reduction in the odds of using ITN the previous *** the use of antimalarial drugs during last pregnancy,the odds were 23%[OR=0.773,95%CI=0.625-0.956]lower for those who did not receive malaria information on radio compared with those who ***:These findings indicate a potentially important role of malaria information received through mass media on utilisation of ITN among women in *** research is needed to explore the factors that limit the accessibility to malaria information through mass media.

关键词： Malaria prevention behaviour Insecticide treated nets antimalarial drugs Global health Sub-Saharan Africa

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Expanding the Therapeutic Spectrum of Artemisinin:Activity Against Infectious Diseases Beyond Malaria and Novel Pharmaceutical Developments

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World Journal of Traditional Chinese Medicine 2016年第2期2卷 1-23页

作者： Thomas Efferth Marta R.Romero Anna Rita Bilia Ahmed Galal Osman Mahmoud ElSohly Michael Wink Rudolf Bauer Ikhlas Khan Maria Camilla Bergonzi Jose J.G.Marin Department of Pharmaceutical Biology Institute of Pharmacy and Biochemistry Johannes Gutenberg University Experimental Hepatology and Drug Targeting (HEVEFARM) CIBERehd IBSAL University of SalamancaCampus Miguel de Unamuno Department of Chemistry "Ugo Schiff" University of Florence National Center for Natural Products Research School of Pharmacy University of Mississippi ElSohly Laboratories Inc. Department of Pharmaceutics University of Mississippi Institute of Pharmacy and Molecular Biotechnology Ruprecht-Karls University Institute of Pharmaceutical Sciences Department of Pharmacognosy University of Graz Devision of Pharmacognosy Department of Biomolecular Sciences University of Mississippi

The interest of Western medicine in Traditional Chinese Medicine(TCM) as a source of drug leads/new drugs to treat diseases without available efficient therapies has been dramatically augmented in the last decades by the extensive work and the outstanding findings achieved within this kind of medicine. The practice of TCM over thousands of years has equipped scientists with substantial experience with hundreds of plants that led to the discovery of artemisinin(qinghaosu), which is extracted from the medicinal plant Artemisia annua L.(qinghao). The unexpected success of artemisinin in combating malaria has drawn strong attention from the scientific community towards TCM. Artemisinin was discovered by Youyou Tu in 1972. Since then, several novel pharmacological activities based on the well-known properties of the sesquiterpene lactone structure with the oxepane ring and an endoperoxide bridge have been unravelled. Beyond malaria, artemisinin and its derivatives(artemisinins) exert profound activities towards other protozoans(Leishmania, Trypanosoma, amoebas, Neospora caninum, and Eimeria tenella), trematodes(Schistosoma, liver flukes), and viruses(human cytomegalovirus, hepatitis B and C viruses). Less clear is the effect against bacteria and fungi. Based on the promising results of artemisinin and the first generation derivatives(artesunate, artemether, arteether), novel drug development strategies have been *** included the synthesis of acetal-and non-acetal-type artemisinin dimeric molecules as well as developing nanotechnological approaches, ***-based liposomes, niosomes, micelles, solid lipid nanocarriers, nanostructured lipid carriers, nanoparticles, fullerenes and nanotubes. The current review presents an overview on different aspects of artemisinins, including sources, chemistry, biological/pharmacological properties, types of infectious pathogens that are susceptible to artemisinins in vitro and in vivo, in addition to the advancement in

关键词： Artemisinin derivatives Artemisia annua Asteraceae antimalarial drugs Anti-pathogen activity Antiviral properties Artemisinin-loaded nanocarriers Traditional Chinese Medicine

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Studies on Toxicity of Nitroquine-Dapsone Compound and Therapeutic Effects of Folic or Folinic Acid on Toxicated Animals

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Journal of Medical Colleges of PLA 1986年第3期 225-231页

作者：胡友梅程天民李先珍况明书朱青平刘富安吴廷璜 Department of Pharmacology Third Military Medical College Chongqing Department of medical protection Department of parasitology

The toxic effects of nitroquine-dapsone compound(NQD)in mice and dogs were *** therapeutic index of NQDin mice is 1911,the greatest among the 6 antimalarials *** effects of NQD(50 mg/kg/day for 3 days per os)and nitro-quine in dogs were manifested by injuries on the adrenal cortexand intestinal *** folic acid(4 mg/kg/day for 4 days)or calcium leucovorinum(0.3 mg/kg/day for 4 days)were usedconcomitantly with NQD,the death rate and the incidence of dia-rrhea in the toxicated dogs were greatly reduced,the injury on theintestinal epithelium was much milder,and the goblet cells weremuch more numerous than those without *** results suggestthat folic acid and calcium leucovorinum can protect the undifferen-tiated cells in the intestinal crypts from being injured by NQD.

关键词： antimalarial drugs nitroquine(NQ) nitroquinedapsone(NQD) folic acid calcium leucovorinum(folinic acid)

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