Noscapine shows antimalarial activity against Plasmodium falciparum 3D7,its clinical isolate Pf140/SS,and Plasmodium berghei ANKA

Objective:To evaluate the antimalarial activity of noscapine against Plasmodium falciparum 3D7 strain(Pf3D7),its clinical isolate(Pf140/SS),and Plasmodium berghei ANKA(PbA).Methods:Using ring-stage survival assay,phenotypic assessments,and SYBR-green-based fluorescence assay,the antimalarial activities of noscapine were assessed compared with dihydroartemisinin(DHA)in in vivo and in vitro studies.In addition,hemolysis and cytotoxicity tests were carried out to evaluate its safety.RT-PCR assay was also conducted to determine the effect of noscapine on papain-like cysteine protease Plasmodium falciparum falcipain-2(PfFP-2).Results:The antimalarial efficacy of noscapine against Pf3D7 and Pf140/SS was comparable to DHA,with IC50 values of(7.68±0.88)and(5.57±0.74)nM/mL,respectively,and>95%inhibition of PbA infected rats.Noscapine also showed a safe profile,as evidenced by low hemolysis and cytotoxicity even at high concentrations.Moreover,PfFP-2 expression was significantly inhibited in both noscapine-treated Pf3D7 and Pf140/SS(P<0.01).Conclusions:Noscapine has antimalarial properties comparable to standard antimalarial DHA with better safety profiles,which may be further explored as a therapeutic candidate for the treatment of malaria.

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)

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。

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)

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。

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)

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。

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)

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。

科泰新~悬浊液稳定性试验

疟疾在全球尤其是热带亚热带地区广泛流行，是严重威胁人们健康的传染病。疟疾治疗药物在各种不同环境条件下的稳定性将直接影响其治疗效果。为此我们设计了该试验，通过对COTECXIN（Dihydroartemisinin）科泰新（双氢青蒿素）悬浊液在水中28天的稳定性研究分析，我们认为其性状是稳定的。

Development of nanoscale drug delivery systems of dihydroartemisinin for cancer therapy: A review

Dihydroartemisinin(DHA),a first-line antimalarial drug,has demonstrated great anticancer effects in many types of tumors,including liver cancer,glioblastoma,and pancreatic cancer.Due to its abilities to induce programmed cell death(PCD;apoptosis,autophagy and ferroptosis),inhibit tumor metastasis and angiogenesis,and modulate the tumor microenvironment,DHA could become an antineoplastic agent in the foreseeable future.However,the therapeutic efficacy of DHA is compromised owing to its inherent disadvantages,including poor stability,low aqueous solubility,and short plasma halflife.To overcome these drawbacks,nanoscale drug delivery systems(NDDSs),such as polymeric nanoparticles(NPs),liposomes,and metal-organic frameworks(MOFs),have been introduced to maximize the therapeutic efficacy of DHA in either single-drug or multidrug therapy.Based on the beneficial properties of NDDSs,including enhanced stability and solubility of the drug,prolonged circulation time and selective accumulation in tumors,the outcomes of DHA-loaded NDDSs for cancer therapy are significantly improved compared to those of free DHA.This reviewfirst summarizes the current understanding of the anticancer mechanisms of DHA and then provides an overview of DHA-including nanomedicines,aiming to provide inspiration for further application of DHA as an anticancer drug.

Inhibition of lymphangiogenesis,nodal and lung metastasis by dihydroartemisinin in mice bearing Lewis lung carcinoma

Objective:To investigate the activity of anti-malarial dihydroartemisinin (DHA) on tumor growth, lymphangiogenesis, nodal and lung metastasis and survival in mice bearing Lewis lung carcimoma (LLC). Methods: The models of C57BL/6 mice transplantation tumors were established via subcutaneous injection of LLC cells and divided into 4 groups: control group, DHA group, DHA+ferrous sulfate (FS) group and FS group, with 25 mice in each group. Tumor volumes and weights, nodal and lung metastasis, and survival were monitored. Tumor lymphatic microvessel density (LMVD) was determined by lymphatic vessel endothelial hyaluronan receptor-1 (LYVE-1) immnohistochemistry. After LLC cells were treated with DHA or DHA+FS, protein and mRNA levels of vascular endothelial growth factor (VEGF) -C were evaluated by Western blotting and real time quantitative RT-PCR, respectively. Results: Oral administration of DHA or DHA+FS inhibited lymph node and lung metastasis, and prolonged survival. However, no significant tumor growth retardation effect was observed when mice were treated with DHA alone. The inhibited tumor metastasis was related to the decreased LMVD in the peritumoral regions, but not in the intratumoral regions. DHA significantly down-regulated the expression of VEGF-C protein and mRNA in LLC cells. Conclusion: DHA effectively inhibits LLC transplantation tumor lymphangiogenesis, nodal and lung metastasis, and may be a promising chemotherapeutic agent for controlling lung cancer metastasis by decreasing VEGF-C expression.

pH-activatable oxidative stress amplifying dissolving microneedles for combined chemo-photodynamic therapy of melanoma

Photodynamic therapy(PDT)-mediated oxidation treatment is extremely attractive for skin melanoma ablation,but the strong hydrophobicity and poor tumor selectivity of photosensitizers,as well as the oxygen-consuming properties of PDT,leading to unsatisfactory therapeutic outcomes.Herein,a tumor acidic microenvironment activatable dissolving microneedle(DHA@HPFe-MN)was developed to realize controlled drug release and excellent chemo-photodynamic therapy of melanoma via oxidative stress amplification.The versatile DHA@HPFe-MN was fabricated by crosslinking a self-synthesized protoporphyrin(PpIX)-ADH-hyaluronic acid(HA)conjugate HA-ADH-PpIX with“iron reservoir”PA-Fe 3+complex in the needle tip via acylhydrazone bond formation,and dihydroartemisinin(DHA)was concurrently loaded in the hydrogel network.HA-ADH-PpIX with improved water solubility averted undesired aggregation of PpIX to ensure enhanced PDT effect.DHA@HPFe-MN with sharp needle tip,efficient drug loading and excellent mechanical strength could efficiently inserted into skin and reach the melanoma sites,where the acidic pH triggered the degradation of microneedles,enabling Fe-activated and DHA-mediated oxidation treatment,as evidenced by abundant reactive oxygen species(ROS)generation.Moreover,under light irradiation,a combined chemo-photodynamic therapeutic effect was achieved with amplified ROS generation.Importantly,the Fe-catalyzed ROS production of DHA was oxygen-independent,which work in synergy with the oxygen-dependent PDT to effectively destroy tumor cells.This versatile microneedles with excellent biosafety and biodegradability can be customized as a promising localized drug delivery system for combined chemo-photodynamic therapy of melanoma.

Topical dihydroartemisinin inhibits suture-induced neovascularization in rat corneas through ERK1/2 and p38 pathways

AIM: To determine if topical instillation of dihydroartemisinin (DHA) inhibits corneal neovascularization (NV) in rats and to investigate the role of the extracellular regulated kinases (ERK) 1/2 and p38 pathways in this process. O METHODS: Suture-induced corneal NV was produced in rats and the eyes were topically treated with different concentrations of DHA (20mg/L, 10mg/L or 5mg/L) or normal saline 4 times a day for 7 days. The corneal NV was quantified as the proportion of NV area to the whole cornea. Western blot was used to determine the expressions of vascular endothelial growth factor (VEGF) and the phosphorylation status of VEGF receptor-2, ERK1/2 and p38 in the corneas. Immunofluorescent staining was used to determine the expressions of phospho-ERK1/2 and phospho-p38 in the corneal tissues from the eyes treated with 20 mg/L DHA (DHA group) or normal saline (control group). RESULTS: The proportion of corneal NV area in the eyes treated with normal saline or DHA at dosages of 20mg/L, 10mg/L or 5mg/L was (23.74 +/- 3.00)%, (15.73 +/- 2.88)%, (19.53 +/- 2.42)%, and (23.38 +/- 2.79)%, respectively. In the eyes treated with 20mg/L or 10mg/L DHA, the corneal NV area was significantly reduced when compared to that in eyes with normal saline (P < 0.05). Western blot analyses revealed that 20mg/L DHA significantly inhibited the expressions of VEGF and phospho-VEGFR-2. Both 20mg/L and 10mg/L DHA inhibited the expressions of phospho-ERK1/2 and phospho-p38. Immunofluorescent staining further demonstrated that 20mg/L DHA lowered the Expression levels of phospho-ERK1/2 and phospho-p38 in the corneas with suture-induced NV. O CONCLUSION: Suture-induced NV in rat corneas was significantly inhibited by topical treatment with 20mg/L and 10mg/L DHA. The results suggest that the effects could be partially dependent on the DHA-mediated inhibitions of the ERK1/2 and p38 pathways.

The inhibitory effect of dihydroartemisinin on the growth of neuroblastoma cells

Objective:To evaluate the inhibitory effect of dihydroartemisinin on neuroblastoma cell line SH-SY5 Y,explore the possible mechanism of dihydroartemisinin against neuroblastoma cells.Methods:The cell viability of dihydroartemisinin treated SH-SY5 Y cells was examined by MTT assay and morphology of cells was observed by using inverted microscope.Cell cycle was examined with flowcytometry assay,then cyclin D1 and caspase-3 proteins expression was detected by ELISA and western blotting assay.Results:MTT analysis results showed that cell viability significantly decreased after exposure to 0.05,0.50,5.00 and 50.00 mmol/L dihydroartemisinin in a dose-dependent manner,and the lower density of cells was observed in treated groups.The number of cells in sub-G1 phase was increased after treatment with different doses of dihydroartemisinin compared with the control group.The expression of cyclin D1 protein was decreased,while the expression of caspase-3 protein was increased in treated group.Conclusions:Dihydroartemisinin could inhibit the proliferation through stopping the cell cycle and inducing the apoptosis in neuroblastoma SH-SY5 Y cells.

Dihydroartemisinin ameliorates innate inflammatory response induced by Streptococcus suis-derived muramidase-released protein via inactivation of TLR4-dependent NF-kB signaling

Muramidase-released protein(MRP)is now being recognized as a critical indicator of the virulence and pathogenicity of Streptococcus suis(S.suis).However,the identification of viable therapeutics for S.suis infection was hindered by the absence of an explicit mechanism for MRP-actuated inflammation.Dihydroartemisinin(DhA)is an artemisinin derivative with potential anti-inflammatory activity.The modulatory effect of DhA on the inflammatory response mediated by the virulence factor MRP remains obscure.This research aimed to identify the signaling mechanism by which MRP triggers the innate immune response in mouse spleen and cultured macrophages.With the candidate mechanism in mind,we investigated DhA for its ability to dampen the pro-inflammatory response induced by MRP.The innate immune response in mice was drastically triggered by MRP,manifesting as splenic and systemic inflammation with splenomegaly,immune cell infiltration,and an elevation in pro-inflammatory cytokines.A crucial role for Toll-like receptor 4(TLR4)in coordinating the MRP-mediated inflammatory response via nuclear factor-kappa B(NF-kB)activation was revealed by TLR4 blockade.In addition,NFkB-dependent transducer and activator of transcription 3(STAT3)and mitogen-activated protein kinases(MAPKs)activation was required for the inflammatory signal transduction engendered by MRP.Intriguingly,we observed an alleviation effect of DhA on the MRP-induced immune response,which referred to the suppression of TLR4-mediated actuation of NF-kB-STAT3/MAPK cascades.The inflammatory response elicited by MRP is relevant to TLR4-dependent NF-kB activation,followed by an increase in the activity of STAT3 or MAPKs.DhA mitigates the inflammation process induced by MRP via blocking the TLR4 cascade,highlighting the therapeutic potential of DhA in targeting S.suis infection diseases.

Dihydroartemisinin inhibits plasmid transfer in drug-resistant Escherichia coli via limiting energy supply

Conjugative transfer of antibiotic resistance genes(ARGs)by plasmids is an important route for ARG dissemination.An increasing number of antibiotic and nonantibiotic compounds have been reported to aid the spread of ARGs,highlighting potential challenges for controlling this type of horizontal transfer.Development of conjugation inhibitors that block or delay the transfer of ARG-bearing plasmids is a promising strategy to control the propagation of antibiotic resistance.Although such inhibitors are rare,they typically exhibit relatively high toxicity and low efficacy in vivo and their mechanisms of action are inadequately understood.Here,we studied the effects of dihydroartemisinin(DHA),an artemisinin derivative used to treat malaria,on conjugation.DHA inhibited the conjugation of the IncI2 and IncX4 plasmids carrying the mobile colistin resistance gene(mcr-1)by more than 160-fold in vitro in Escherichia coli,and more than two-fold(IncI2 plasmid)in vivo in a mouse model.It also suppressed the transfer of the IncX3 plasmid carrying the carbapenem resistance gene bla_(NDM-5)by more than twofold in vitro.Detection of intracellular adenosine triphosphate(ATP)and proton motive force(PMF),in combination with transcriptomic and metabolomic analyses,revealed that DHA impaired the function of the electron transport chain(ETC)by inhibiting the tricarboxylic acid(TCA)cycle pathway,thereby disrupting PMF and limiting the availability of intracellular ATP for plasmid conjugative transfer.Furthermore,expression levels of genes related to conjugation and pilus generation were significantly down-regulated during DHA exposure,indicating that the transfer apparatus for conjugation may be inhibited.Our findings provide new insights into the control of antibiotic resistance and the potential use of DHA.

Dihydroartemisinin enhances cell apoptosis in diffuse large B cell lymphoma by inhibiting the STAT3 activity

Background:Dihydroartemisinin(DHA)is reported to be a potential anticancer agent,and the mechanisms underlying the effects of DHA on diffuse large B cell lymphoma however are still obscure.This study aimed to assess the antitumor effect of DHA on diffuse large B cell lymphoma cells and to determine the potential underlying mechanisms of DHA-induced cell apoptosis.Methods:Here,the Cell Counting Kit 8 assay was conducted to study cell proliferation.We performed Annexin V-FITC/propidium iodide staining,real-time polymerase chain reaction,and western blot analysis to analyze cell apoptosis and potential molecular mechanisms.Results:The results showed that DHA substantially suppressed cell proliferation and induced cell apoptosis in vitro in a time-and concentration-dependent fashion.Moreover,STAT3 activity could be inhibited after stimulation with DHA.Conclusion:These results imply that the underlying anti-tumoral effect of DHA may increase apoptosis in diffuse large B cell lymphoma cells via the STAT3 signaling pathway.In addition,DHA might be an effective drug for diffuse large B cell lymphoma therapy.

A Comparative Study of Dihydroartemisin in Compounds in Treatment of Uncomplicated Falciparum Malaria in Kampong of Cambodia

Objective: To compare the safety and efficacy of two compounds of dihydroartemisinin(DHA) -Artekin and Artekin (T) in the treatment of uncomplicated falciparum malaria. Methods:The regimen of 8-tablet for 2 days of Artekin and Artekin (T) were applied to 100 patients with uncomplicated falciparum malaria, who were randomly divided into two groups. Each group contained 50 cases. The cure rate, the mean parasites clearance time, the mean fever clearance and side-effects were observed to assess the safety and efficacy of the compounds used. Results: The mean parasites clearance time was 31. 7±9.0 hours in the Artekin group and 32. 8±8. 8 hours in Artekin (T) group respectively; the mean fever clearance time was 12. 7±7. 2 hours in Artekin group and 16. 5±7. 9 hours in Artekin (T) group; there were no recrudescence case in both groups within the 28 days of follow-up, the cure rates in Artekin group and Artekin (T) groups were 100%. It indicated that the tolerability of both compounds were very good, the side-effects such as nausea, abdominal pain were mild and self-limited. Conclusion: The study preliminarily indicated that the DHA and PQ compounds were of high efficacy, rapid acting and low toxici-ty. Artekin is very promising as a cheap, simple, effective treatment for multi-resistance malaria in Cambodia.

Immune System and Body Defence Enhancement Effects of Oral Dihydroartemisinin in Wistar Albino Rats

Some drugs like clozapine, interferons and cyclosporine affect the number and function of white blood cells. This study examined the effect of oral dihydroartemisinin on the white blood cells; the lymph and intestinal glands of the intestinal wall and the open circulation of the spleen of Wistar albino rats. Five dosages of oral DHA （dihydroartemisinin）, 1, 2, 60 and 80 ms/ks were administered for 5 days or 7 days to 10 sets of 5 test rats weighing 104-106 grams. Equivalent doses of distilled water were given to 4 rats of similar weight and age to serve as controls in each of these tests. A group of five test and four control young adult albino rats which weighed 75-90 grams were given a repeated dose of the 1 ms/ks oral DHA with a rest period of 1 week between the two dosage regimens. The results of the study showed that oral dihydroartemisinin treatment produced highly statistically significant increases in the percentage neutrophil count （P 〈 0.01 ）; the percentage lymphocyte count （P 〈 0.01, P 〈 0.03）; the percentage monocyte count; the population of the cells of the intestinal glands and intestinal solitary and aggregated lymph glands; the number of the cells of the slow and open circulation of the spleen of the dihyrdroartemisinin-treated rats in comparism with the controls. These increases were dose, dose repetition and time dependent. The results suggest that oral dihydroartemisinin treatment had immune defence enhancement effects in the treated rats.

Mitochondria-targeted carrier-free nanoparticles based on dihydroartemisinin against hepatocellular carcinoma

Hepatocellular carcinoma is a common and fatal malignancy for which there is no effective systemic therapeutic strategy.Dihydroartemisinin(DHA),a derivative of artemisinin,has been shown to exert anti-tumor effects through the production of reactive oxygen species(ROS)and resultant mitochondrial damage.However,clinical translation is limited by several drawbacks,such as insolubility,instability and low bioavailability.Here,based on a nanomedicine-based delivery strategy,we fabricated mitochondria-targeted carrier-free nanoparticles coupling DHA and triphenylphosphonium(TPP),aiming to improve bioavailability and mitochondrial targeting.DHA-TPP nanoparticles can be passively delivered to the tumor site by enhanced penetration and retention and then internalized.Flow cytometry and Western blot analysis showed that DHA-TPP nanoparticles increased intracellular ROS,which increased mitochondrial stress and in turn upregulated the downstream Bcl-2 pathway,leading to apoptosis.In vivo experiments showed that DHA-TPP nanoparticles exhibited anti-tumor effects in a mouse model of hepatocellular carcinoma.These findings suggest carrier-free DHA-TPP nanoparticles as a potential therapeutic strategy for hepatocellular carcinoma.

Increased stability and solubility of dihydroartemisinin in aqueous solution through the formation of complexes with 2-hydroxypropyl-β-cyclodextrin

The effect of various concentrations of 2-hydroxypropyl-β-cyclodextrin （HP-β-CD） on the solubility of dihydroartemisinin （DHA） in aqueous solution at different pHs was investigated. The influence of different concentrations of 2-hydroxypropyl-β- eyclodextrin on the stability of dihydroartemisinin at 50, 60, 70 and 80 ℃ was also studied. Inclusion complex of dihydroartemisinin with 2-hydroxypropyl-β-cyclodextrin was prepared and characterized by X-ray diffraction and differential scanning calorimetry. The 2-hydroxypropyl-β-cyclodextrin effectively inhibited the hydrolysis of dihydroartemisinin and greatly increased its solubility. Furthermore, we showed that the higher concentrations of 2-hydroxypropyl-β-cyclodextrin, the better stability and solubility of dihydroartemisinin. When the temperature was increased, the stability of dihydroartemisinin decreased. Our results indicated that 2-hydroxypropyl-β-cyclodextrin can be used as a stabilizer and solubilizer of dihydroartemisinin.

Efficacy of dihydroartemisinin-mefloquine on acute uncomplicated falciparum malaria

Objective To evaluate the clinical efficacy of dihydroartemisinin-mefloquine on acute uncomplicated falciparum malaria. Methods Fifty-four patients with symptomatic falciparum malaria were allocated to receive oral dihydroartemisinin at a single dose of 120?mg on day 1, followed by mefloquine, 750?mg and 500?mg on days 2 and 3, respectively. Follow-up was performed on days 1,2,3,4,7,14,21, and 28. Results All patients had a rapid initial response to treatment. The parasite clearance time (PCT) after treatment was 30.7±3.6 hours. The fever subsidence time (FST) after treatment was 21.2±2.8 hours. Two patients had a recrudescence 21 and 25 days respectively after the disappearance of parasitemia, hence the recrudescence rate was 3.7% and the cure rate was 96.3%. No serious adverse effects were observed, only mild and transient nausea, vomiting and loss of appetite. Conclusion A combination of dihydroartemisinin and mefloquine is effective in the treatment of acute uncomplicated falciparum malaria.

Artemisinin anti-malarial drugs in China

Discovered by Youyou Tu, one of the 2015 Nobel Prize winners in Physiology or Medicine, together with many other Chinese scientists, artemisinin, artemether and artesunate, as well as other artemisinins, have brought the global anti-malarial treatment to a new era, saving millions of lives all around the world for the past 40 years. The discoveries of artemisinins were carried out beginning from the 1970s, a special period in China, by hundreds of scientists all together under the 'whole nation' system. This article focusing on medicinal chemistry research, briefly introduced the discovery and invention course of the scientists according to the published papers, and highlighted their academic contribution and achievements. (C) 2016 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.