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| 1 | Malaria parasite carbonic anhydrase:inhibition of aromatic/heterocyclic sulfonamides and its therapeutic potential显示文摘Plasmodium falciparum(P.falciparum) is responsible for the majority of life-threatening cases of human malaria,causing 1.5-2.7 million annual deaths.The global emergence of drug-resistant malaria parasites necessitates identification and characterisation of novel drug targets and their potential inhibitors.We identified the carbonic anhydrase(CA) genes in P.falciparum.The pfGA gene encodes an α-carbonic anhydrase,a Zn^(2+)-metalloenzme,possessing catalytic properties distinct from that of the human host CA enzyme.The amino acid sequence of the pfCA enzyme is different from the analogous protozoan and human enzymes.A library of aromatic/heterocyclic sulfonamides possessing a large diversity of scaffolds were found to be very good inhibitors for the malarial enzyme at moderate-low micromolar and submicromolar inhibitions.The structure of the groups substituting the aromatic-ureido-or aromatic-azomethine fragment of the molecule and the length of the parent sulfonamide were critical parameters for the inhibitory properties of the sulfonamides.One derivative,that is,4-(3,4-dichlorophenylureido)thioureidobcnzcnesulfonamide(compound 10) was the most effective in vitro Plasmodium falciparum CA inhibitor,and was also the most effective antimalarial compound on the in vitro P.falciparum growth inhibition.The compound 10 was also effective in vivo antimalarial agent in mice infected with Plasmodium berghei,an animal model of drug testing for human malaria infection. It is therefore concluded that the sulphonamide inhibitors targeting the parasite CA may have potential for the development of novel therapies against human malaria. | Sudaratana R Krungkrai Jerapan Krungkrai | 2011 | Asian Pacific Journal of Tropical Biomedicine2011，1，3： | 10 |
| 2 | Quantum chemical studies on antimalarial of artemisinin (qinghaosu) derivatives显示文摘In this paper theoretical studies were performed on artemisinin (qinghaosu) derivatives with semiempirical quantum chemical methods AMI and PM3. The antimalarial activity -logC has an obvious correlation with the net charge of C(16) and bond orders of bonds O(1)-C(10), O(2)-C(6), O(1)-O(2) and O(5)-C(16). According to the calculation results, we derived structure-activity relationship, presented the probable pharmacophore of qinghaosu derivatives and the interaction fashion between the drugs and the plasmodium receptor. | JIANG, HL CHEN, KX TANG, Y CHEN, JZ JI, RY | 1995 | Chinese Journal of Chemistry1995，13，2： | 5 |
| 3 | Putative metabolic roles of the mitochondria in asexual blood stages and gametocytes of Plasmodium falciparum显示文摘Upon infection into human red cell,Plasmodium falciparum differentiates into asexual and sexual(gametocyte) stages.The mitochondrion is a tubular-cristate organelle,functionally and structurally different between the two stages.Genes and proteins involving metabolic and functional roles,protein targeting and import to this organelle, are comprehensively reviewed.The genes and proteins of the electron transport system are identified, partially characterized in human and rodent malaria parasites consisting of a single subunit of NADH dehydrogenase, two subunits of succinate dehydrogenase,cytochrome C reductase and cytochrome Coxidase.One of the primary functional roles of the mitochondrion in the parasite is the coordination of pyrimidine biosynthesis, the electron transport system and oxygen utilization through dihydroorotate dehydrogenase.All enzymes of tricarboxylic acid cycle,pyruvate dehydrogenase complex and some enzymes of ATP synthase,are identified and partially characterized using the completed P.falciparum genome.Some metabolic and functional roles of the organelle include oxidative phosphorylation,ubiquinone and heme biosynthesis,antioxidant defense and redox balance.Recent physiological studies involve membrane potential maintenance,cellular signaling and cation homeostasis.The organelle is a target for antimalarial drug,i.e.atovaquone.Based on the lines of evidence, we hypothesize that the parasite exhibits metabolic adaptation of the underdeveloped mitochondrial organelle to life in the mosquito vector and the human host. | Krungkrai J Kanchanaphum P Pongsabut S Krungkrai SR | 2008 | Asian Pacific Journal of Tropical Medicine2008，1，1： | 4 |
| 4 | Epilepsy triggered by mefloquine in an adult traveler to Uganda显示文摘We report a case of a traveler who visited Uganda for 8 d, and took mefloquine one tablet/week for malaria prophylaxis. After the second dose, he suffered from two episodes of loss of consciousness with seizures, therefore mefloquine was discontinued. During the flight back after full recovery, seizures reoccurred while he was on board, he was disembarked in Addis Ababa and then transferred to Nairobi. After repatriation to Italy, he experienced four other similar episodes. The patient was still on full dose anticonvulsant therapy one year and a half after, as any attempt at reduced dose was unsuccessful. Currently, three agents(mefloquine, atovaquone/proguanil, and doxycycline) are recommended for malaria chemoprophylaxis, with similar efficacy but different adverse event profiles, regimens, and prices. Considering that mefloquine is associated with a higher risk of neurologic and psychiatric adverse events than the alternative regimens, we suggest considering mefloquine as a second line choice after atovaquone/progua-nil and doxycycline for short-term travelers. | Federico Gobbi Andrea Rossanese Dora Buonfrate Andrea Angheben Chiara Postiglione Zeno Bisoffi | 2014 | World Journal of Clinical Cases2014，2，1： | 2 |
| 5 | Assessment of in vitro sensitivity of Plasmodium vivax fresh isolates显示文摘Objective:To compare the applicability of the SYBK Grcen-Ⅰ assay with the standard schizont maturalion assay,for determination of sensitivity of Plasmodium vivax(P.vivax) to chloroquine and a new antifolale WR 99210.Methods:The study was conducted at Mae Tao Clinic for migrant workers,Tak Province during April 2009 to July 2010.A total of 64 blood samples(1 mL blood collected into sodium heparinized plastic tube) were collected from patients with monoinfection with P.vivax malaria prior to treatment with standard regimen of a 3-day chloroquine. In vitro sensitivity of P.vivax isolates was evaluated by schizont maturation inhibition and SYBR Green-Ⅰ assays.Results:A total of 30 out of 64 blood samples collected from patients with P.vivax malaria were successfully analyzed using both the microscopic schizont maturation inhibition and SYBR Green-I assays.The failure rates of the schizont maturation inhibition assay(50%) and the SYBR Green-I assay(54%) were similar(P=0.51).The median IC_(10)s,IC_(50)s and IC_(90)s of both chloroquine and WR99210 were not significantly different from the clinical isolates of P.vivax tested.Based on the cut-off of 100 nM,the prevalences of chloroquine resistance determined by schizont maturation inhibition and SYBR Green-I assays were 19 and 11 isolates,respectively.The strength of agreement between the two methods was very poor for both chloroquine and WR992I0.Conclusions:On the basis of this condition and its superior sensitivity,the microscopic method appears better than the SYUK Green-I Green assay for assessing in vitro sensitivity of fresh P.vivax isolates to antimalarial drugs. | Poonuch Muhamad Wanna Chacharoenkul Kanchana Rungsihirunrat Ronnatrai Ruengweerayut Kesara NaBangchang | 2011 | Asian Pacific Journal of Tropical Biomedicine2011，1，1： | 2 |
| 6 | Antimalarial activity and toxicity of Garcinia mangostana Linn.显示文摘Objective:To investigate the antimalarial activity and toxicity of the crude ethanolic extract of its pericarp both in vitro and in vim.Methods:The antimalarial activity of Gareinja mangostana(G.mangostana)Linn.extract against 3D7 and Kl Plasmodium falciparum(P.falciparum)clone were assessed using SYBR green I-based assay.A 4-day suppressive test of Plasmodium berghei{P.berghei)infected mouse was performed to investigate in vivo antimalarial activity.Results:The in vitro antimalarial activity was seleclive(SI>5?and classified as weak and good lo moderate activity against both 3D7 and K1 P.falciparum,clones with median IC_(50)(range)values of 11.12(10.94-11.29)and 7.54(6.80-7.68)μg/mL,respectively.The extract was considered nontoxic to mice.The maximum tolerated doses for acute and subacute toxicity in mice were 5 000and 2 000 mg/kg,respectively.Median(range)parasite density on day 4 of the negative control group(25%Tween-80),mice treated with 250,500,1000,and 2 000 mg/kg body weight of the extract,and 10 mg/kg body weight of chloroquine for 14 d were 12.8(12.2-13.7),11.4(9.49-13.8),11.6(9.9-12.5),11.7(10.6-12.8),10.9(9.4-11.6)and 0(0-0)%respectively.Parasite density on day 4in the control group treated with Tween-80 was higher than the groups treated with chloroquine and all dose levels of the extract.Conclusions:G.mangostana linn,showed weak antimalarial activity of the extract both in vitro and in vivo could be due to limitation of absorption of the active compounds. | Ratchanu Bunyong Wanna Chaijaroenkul Tullayakorn Plengsuriyakarn Kesara Na-Bangchang | 2014 | Asian Pacific Journal of Tropical Medicine2014，7，9： | 2 |
| 7 | From control to eradication of malaria:the end of being stuck in second gear?显示文摘More than 2 billion people are at risk of malaria,which primarily affects poor populations in tropical and subtropical areas,including Southern Asia.As malaria incidence has been reduced strongly in some parts of endemic regions by combinations of interventions,including artemisinin-based therapies and insecticide-treated bed nets,a new goal has been established recently by charity foundations which support research on malaria:the worldwide eradication of the pathology.Doing away with control approaches which have been applied for the last 50 years and more focus on elimination objectives will deeply change priorities in the area of malaria treatment,chemoprevention,vector control,vaccine research and health system assessment.In this review,actual knowledge on pathogenesis and pharmacology is discussed,and new drugs, vaccines and insecticides are described. | Khadjavi Amina Giribaldi Giuliana Prato Mauro | 2010 | Asian Pacific Journal of Tropical Medicine2010，3，5： | 2 |
| 8 | Isolation of antileishmanial,antimalarial and antimicrobial metabolites from Jatropha multifida显示文摘Objective:To investigate the antileishinanial,antimicrobial and antimalarial activities of the pure metabolites from Jatropha multifida used in African ethnomedicine.Methods:The methanolic stem bark extract of Jatropha multifida used in Nigerian folk medicine as remedy against bacterial infections was subjected to column chromatography and HPLC analyses lo obtain three known metabolites,microcyclic lathyrane dilerpenoids(1-3).Structures were confirmed by comparison of 1D and 2D spectral data with literature.Results:The three compounds exhibited inhibition of antileishmanial,antimalarial and antimicrobial actions against the tested organisms with compouds 2 and 3 active against Cryptococcus neoformans at IC_(50)of 82 and 8.7 μg/ml,respectively.Conclusions:The research lends support to the ethnomedicinal use of the plant in combating microbial infections,leishmaniasis and malarial infections. | Abiodun Falodun Vincent Imieje Osayewenre Erharuyi Ahomafor Joy Peter Langer Melissa Jacob shabanna Khan Mohammed Abaldry Mark Hamann | 2014 | Asian Pacific Journal of Tropical Biomedicine2014，4，5： | 1 |
| 9 | Chemical proteomic profling with photoaffinity labeling strategy identifies antimalarial targets of artemisinin显示文摘Present research on the antimalarial mechanisms of artemisinin(ART)is mainly focused on covalent drug binding targets alkylated by free radicals,while non-covalent binding targets have rarely been reported.Here,we developed a novel photoaffinity probe of ART to globally capture and identify the antimalarial target proteins of ART through chemical proteomics.The results demonstrated that ART can bind to par-asite proteins by both covalent and non-covalent modification,and these may jointly contribute to the antimalarial effects.Our work enriches the research on the antimalarial targets of ART,and provides a new perspective for further exploring the antimalarial mechanism of ART. | Peng Gao Jiayun Chen Peng Sun Jianyou Wang Huan Tang Fei Xia Liwei Gu Huimin Zhang Chen Wang Yin Kwan Wong Yinhua Zhu Chengchao Xu Jigang Wang | 2023 | Chinese Chemical Letters2023，34，12： | 1 |
| 10 | In vivo antiplasmodial activities of ethanolic exract and fractions of Eleucine indica显示文摘Objective:To evaluate the in rivo antiplasmodial activities of the extract and fractions(n-hexane. chloroform,ethylacetate.butanol.aqueous) of the whole plant in Plasmodium berghei berghei infected mice.Methods:Oral administrations of the extract(200.400,and 600 my/kg) of Eleacine indica and fractions(400 mg/kg) were screened in the 4-day.repository and curative tests. Chloroquine(5 mg/kg).pyrimethamine(1.2 mg/kgi and artesunate(5 mg/kgi were used as controls. Results:The extract showed significant[P< 0.05-0.001) dose-dependent,antiplasmodial activity in the 4-day.repository and curative tests and increased the survival times of the infected mice. All the fractions exhibited significant antiplasmodial activity with the highest being ethylacetate fraction.Conclusions:Eleucine indica extract and fractions possess antimalarial activity which confirms the ethnobotanical use of this plant as a malarial remedy and opens a new highway to further investigate its potentials in the on-going fight against malaria. | Ettebong EO Nwafor PA Okokon JE | 2012 | Asian Pacific Journal of Tropical Medicine2012，5，9： | 1 |
| 11 | Antiplasmodial and analgesic activities of Clausena anisata显示文摘Objective:Antiplasmodial and analgesic activities of the leaf extract and fractions of Clausena anisata(C.anisata) were evaluated for antimalarial and analgesic activities.Methods:The crude leaf extract(39-117mg/kg) and fractions(chloroform and acqeous;78mg/kg) of C. anisata were investigated for antiplasmodial activity against chloroquine-sensitive Plasmodium berghei(P.berghei) infections in mice using suppressive,prophylactic and curative models and analgesic activity against acetic acid,formalin and heat-induced pains.Artesunate,5 mg/kg and pyrimethamine,1.2mg/kg were used as positive controls.Thin films made from tail blood of each mouse were used to assess the level of parasitaemia of the mice.Results:The extract and its fractions dose-dependently reduced parasitaemia induced by chloroquine-sensitive P.berghei in prophylactic,suppressive and curative models in mice.These reductions were statistically significant(P<0.001).They also improved the mean survival time(MST) from 17 to 21 days relative to control(P<0.01-0.001).On chemically and thermally-induced pains,the extract inhibited acetic acid and formalin-induced inflammation as well as hot plate-induced pain in mice.These inhibitions were statistically significant(P<0.001) and in a dose-dependent fashion. Conclusions:The antiplasmodial and analgesic effects of this plant may in part be mediated through its chemical constituents and it can be concluded that the C.anisata possess significant antimalarial and analgesic properties. | Jude E Okokon Ette O Etebong John A Udobang Grace E Essien | 2012 | Asian Pacific Journal of Tropical Medicine2012，5，3： | 1 |
| 12 | 三唑类的化学和生物活性进展(英文)显示文摘In recent years,heterocyclic compounds,analogs,and derivatives have attracted strong interest due to their useful biological and pharmacological properties.The small and simple triazole nucleus is present in compounds aimed at evaluating new entities that possess anti-microbial,anti-tumor,antitubercular,anti-convulsant,anti-depressant,antimalarial,and anti-inflammatory activities.Triazoles display a broad range of biological activities and are found in many potent,biologically active compounds,such as trazodone(antidepressant drug),rizatriptan(antimigrane drug),hexaconazole(antifungal drug) and alprazolam(hyptonic,sedative and tranquilizer drug).So far,modifications of the triazole ring have proven highly effective with improved potency and lesser toxicity.The present review highlights the recently synthesized triazoles possessing important biological activities. | Jagdish K. Sahu1 Swastika Ganguly Atul Kaushik | 2013 | 中国天然药物2013，11，5： | 1 |
| 13 | Antiplasmodial and antiulcer activities of Melanthera scadens显示文摘Objective:To evaluate the antimalarial and antiulcerogenic activities ofleaf exlracl and fractions of Melanthera scandens(M.scandens).Methods:The crude leaf extract(37-111 mg/kg)and fractions(chloroform,ethylacetale and methanol;78 mg/kg)of M.scadens were investigated for antiplasmodial activity against chloroquine-sensitive Plasmodium berghei infections in mice and for antiulcer activity against experimentally-induced ulcers.The antimalarial activity during early and established infections as well as prophylactic was investigated.Artesunate(5 mg/kg)and pyrimethamine(1.2 mg/kg)were used as positive controls.Thin films made from tail blood of each mouse were used to assess the level of parasitaemia of the mice.Antiulcer activity of the crude extract was also evaluated against indomethacin,ethanol and histamine induced ulcers.Results:The extract and its fractions dose-dependently reduced parasitaemia induced by chloroquine-sensitive Plasmodium berghei infection in prophylactic,suppressive and curative models in mice.These reductions were statistically significant(P<0.00l),They also improved the mean survival time(MST)from 9.28 to 17.73 days as compared with the control(P<0.0l-0.001).The activities of extract/fractions were incomparable to that of the standard drugs ie.artesunate and pyrimethamine.On experimentally-induced ulcers,the extract inhibited indomethacin,ethanol and histamine induced ulcers.These inhibitions were statistically significant(P<0.001)and in a dose-dependent fashion.Conclusions:The antiplasmodial and antiulcerogenic effects of this plant may in part be mediated through the chemical constituents of the plant. | Jude E Okokon Ette O Etebong John A Udobang Jackson Obot | 2012 | Asian Pacific Journal of Tropical Biomedicine2012，2，1： | 1 |
| 14 | Antimalarial activities of butanol and ethylacetate fractions of Combretum nigricans leaf显示文摘Objective: To evaluate the antimalarial activity of the ethylacetate and butanol fractions of Combretum nigricans(C. nigricans) leaf extract in mice. Methods: C. nigricans solvent(butanol and ethylacetate) fractions were screened for their phytochemical constituents using standard procedures illustrated by Harborne and Evans. The Peters' 4-day suppressive test against early malaria infection, Rane's curative test against established malaria and prophylactic test for residual activity were employed for evaluating the antimalarial potential in mice. Results: The phytochemical screening revealed the presence of alkaloids, terpenoids, saponins, and flavonoids in both fractions at different intensity. Both fractions exhibited significant antimalarial activity in all test models(P<0.05). The ethylacetate fraction of C. nigricans had better chemosuppressive and curative effects compared to the butanol fraction, which however, elicited a better chemoprophylactic effect. The chemosuppressive effect of C. nigricans ethylacetate fraction(200-800 mg/kg) was 77.6%, 69.1% and 86.1%; curative effect was 62.3%, 71.3% and 72.4%; while the chemoprophylactic activity was 32.1%, 48.6% and 61.2% respectively. C. nigricans butanol fraction(200-800 mg/kg) had 40.3%, 54.1% and 69.1% chemosuppression; 26.2%, 36.9% and 34.5% curative effect; and 48.4%, 70.0% and 87.4% chemoprophylaxis. Conclusions: Both solvent fractions of C. nigricans possess antimalarial activity, and may be useful at different stages of malaria therapy. | Enegide Chinedu Peter A.Akah Dabum L.Jacob Ifeoma A.Onah Chimere Y.Ukegbu Chukwuma K.Chukwuemeka | 2019 | Asian Pacific Journal of Tropical Biomedicine2019，9，4： | 0 |
| 15 | Chemical Composition of Gossypium herbaceum linn and its Antioxidant, Antibacterial, Cytotoxic and Antimalarial Activities显示文摘Background:Gossypium herbaceum(G.herbaceum),a plant commonly found in the wild in Nigeria,is said to possess some therapeutic activities.However,there is a dearth of information on its chemical constituents.Also,there is a need to investigate its therapeutic activities.Objective:To investigate the qualitative and quantitative phytochemical components of the leaf extracts of G.herbaceum,as well as its antioxidant,antimalarial and cytotoxic activity.Methods:Gas chromatography-mass spectrometry(GC-MS)analysis was used to determine the components of ethanol and hexane extracts of G.herbaceum leaf while 2,2-diphenyl-1-picrylhydrazyl(DPPH)and nitric oxide assays were used to determine the antioxidant potential.Malaria parasites viability was examined using parasite lactate dehydrogenase(pLDH)technique and HeLa cell was used for the cytotoxicity evaluation.Results:Bioactive compounds identified in ethanol and hexane extracts of G.herbaceum were 37 and 30 kinds,respectively,with major components as linoleic acid(36.10%and 33.82%),vitamin E(7.15%and 5.98%)and caryophyllene(4.21%and 5.08%).It also has tannins,saponins,alkaloids,flavonoids steroids,phenols and ter-penoids.In antibacterial test,significant inhibitory potentials against multidrug-resistant bacteria strains were present.In vitro antioxidant potentials(IC 50)of ethanol and hexane extracts were 3.33 and 4.12μg/mL for DPPH assays,and 3.87 and 5.00μg/mL for nitric oxide assays,respectively.Antiplasmodial activities(IC 50)were 9.99 and 9.76μg/mL for ethanol and hexane extracts,respectively.Conclusion:G.herbaceum leaf may provide novel plant-derived therapeutic agents,effective in treating infectious diseases arising from multiple drug-resistant bacteria and a target in the management of oxidative stress. | Rotimi Abisoye Larayetan Gideon Ayeni Abdulrazaq Yahaya Abayomi Ajayi Sunday Omale Umar Ishaq Dauda Joseph Abiodun Chijioke Olisah Julius Aigbogun Swesme Enyioma-Alozie | 2021 | Clinical Complementary Medicine and Pharmacology2021，1，1： | 0 |
| 16 | Role of traditional herbal medicine in the treatment of malaria显示文摘Malaria is one of the world's major public health concerns and numerous medicinal plants are commonly used for treating malaria.Traditional health care uses medicinal plants widely,but no scientific documentation is available and,there is a growing risk of losing this knowledge.Thus,this study aims to document the traditional use of medicinal plants in treating malaria and related conditions.In this review,numerous herbal medicines for antimalarial potential are explained.The literature survey was done using keywords i.e.,malaria,herbal,herbal,traditional use,antimalarial,quinine,artemisinin,and traditional medicine by using PubMed,Science Direct,Google Scholar,and HINARI database.This review discusses the life cycle of the malarial parasite,what makes you attractive to mosquitoes,and the role of traditional herbal medicine in malaria. | Virender Kumar Vandana Garg Harish Dureja | 2022 | TMR Modern Herbal Medicine2022，5，4： | 0 |
| 17 | Novel dual inhibitors against FP-2 and PfDHFR as potential antimalarial agents: Design, synthesis and biological evaluation显示文摘Resistance to malaria parasites has quickly developed to almost all used antimalarial drugs. Cysteine protease falcipain-2(FP-2) and Plasmodium falciparum dihydrofolate reductase(PfDHFR) have crucial roles, which are absolutely necessary, in the parasite life cycle. In this study, based on the uniform pharmacophores of reported PfDHFR inhibitors and the first-generation dual inhibitors against FP-2 and PfDHFR, we identified a novel series of dual inhibitors through fragments assembly. Lead optimization led to the identification of 14, which showed potent inhibition against FP-2 and PfDHFR enzyme(IC_(50)= 6.8 + 1.8 mmol/L and IC_(50)= 8.8 + 0.3 mmol/L) and P. falciparum 3D7 strain(IC50= 2.9mmol/L).Additionally, 14 exhibited more potent inhibition to the proliferation of chloroquine-resistant P.falciparum Dd2 strain(IC_(50)= 1.1 mmol/L) than pyrimethamine(IC_(50)>10 mmol/L), and 14 displayed micromolar inhibitory activities against two clinical isolated strains Fab9(IC_(50)= 2.6 mmol/L) and GB4(IC_(50)= 1.0 mmol/L). Collectively, these data demonstrated that 14 might be a good lead compound for the treatment of malaria. | Wenhua Chen Xue Yao Zhenghui Huang Fei Mao Longfei Guan Yun Tang Hualiang Jiang Jian Li Jin Huang Lubin Jiang Jin Zhu | 2019 | Chinese Chemical Letters2019，30，1： | 0 |
| 18 | Domestic trends in malaria research and development in China and its global influence显示文摘Background:Though many countries,including China,are moving towards malaria elimination,malaria remains a major global health threat.Due to the spread of antimalarial drug resistance and the need for innovative medical products during the elimination phase,further research and development(R&D)of innovative tools in both epidemic and elimination areas is needed.This study aims to identify the trends and gaps in malaria R&D in China,and aims to offer suggestions on how China can be more effectively involved in global malaria R&D.Methods:Quantitative analysis was carried out by collecting data on Chinese malaria-related research programmes between 1985 and 2014,invention patents in China from 1985 to 2014,and articles published by Chinese researchers in PubMed and Chinese databases from 2005 to 2014.All data were screened and extracted for numerical analysis and were categorized into basic sciences,drug/drug resistance,immunology/vaccines,or diagnostics/detection for chronological and subgroup comparisons.Results:The number of malaria R&D activities have shown a trend of increase during the past 30 years,however these activities have fluctuated within the past few years.During the past 10 years,R&D on drug/drug resistance accounted for the highest percentages of research programmes(32.4%),articles(55.0%in PubMed and 50.6%in Chinese databases)and patents(45.5%).However,these R&D activities were mainly related to artemisinin.R&D on immunology/vaccines has been a continuous interest for China’s public entities,but the focus remains on basic science.R&D in the area of high-efficiency diagnostics has been rarely seen or reported in China.Conclusions:China has long been devoted to malaria R&D in multiple areas,including drugs,drug resistance,immunology and vaccines.R&D on diagnostics has received significantly less attention,however,it should also be an area where China can make a contribution.More focus on malaria R&D is needed,especially in the area of diagnostics,if China would like to contribute in a more significant way to global malaria control and elimination. | Yang-Mu Huang Lu-Wen Shi Rui She Jing Bai Shi-Yong Jiao Yan Guo | 2017 | Infectious Diseases of Poverty2017，6，1： | 0 |
| 19 | Antimalarial activity of a novel series of artemisinin-derived 1, 2, 3-triazole dimers显示文摘Objective: To obtain suitable artimisinin-based drug candidates with high antimalarial activity.Methods: Three different reaction schemes were used to synthesize a total of 15 artemisininbased compounds.The first synthetic scheme involved the synthesis of diazido aliphatic and aromatic compounds from commercially available dihalides and azido derivatives of artemisinin.The second scheme consisted of the reaction of dibromoaliphatic compounds with sodium azide in dimethylformamide which yielded the desired compounds.Artemisinin-based compounds on treatment with sodium azide and bromotrimethylsilane in dichloromethane produced the most potent compound GB-2.Another potent compound GB-1 was synthesized from artemisinin by treatment with alcohols in the presence of Aberlyst-15 in anhydrous dichloromethane.The third scheme involved the Huisgen 1,3-dipolar cycloaddition between the synthesized aliphatic and aromatic diazides and two alkyne derivatives of artemisinin to obtain the desired artemisinin dimers with average yields.Results: The best in vitro antiplasmodial activity was shown by the compound GB-2 registering IC_(50) value 0.066 μg/mL against chloroquine-sensitive and 0.865 μg/mL against chloroquineresistant strains of Plasmodium falciparum.It suppressed 59.0% parasitaemia in vivo of rodent malaria parasite Plasmodium berghei in Swiss albino model at 50 μg/kg body weight dosage.Molecular docking interactions of Plasmodium falciparum ATP6(PfATP6) protein revealed strong bonding of GB-2 with Thr255 residue which is likely to be the reason for excellent antimalarial activity of this compound.Conclusion: Two compounds GB-1 and GB-2 exhibited excellent in vitro antiplasmodial activity and fair in vivo antimalarial activity.Of the two, GB-2 showed better activity which could be attributed to its strong bonding interactions with Thr255 as evidenced from the molecular docking study.Study helped in identifying artemisinin analogues possessing good antimalarial properties and further research in structural alterations of the selected molecules should be carried out which may result in obtaining potent drug candidates against the malarial parasite. | Kabita Gogoi Gokul Baishya Biswajit Saikia Nabin Chandra Barua Chandrajit Dohutia Akalesh Kumar Verma Anil Prakash | 2019 | Asian Pacific Journal of Tropical Medicine2019，12，5： | 0 |
| 20 | Antimalarial activity of Ageratum conyzoides in combination with chloroquine and artesunate显示文摘Objective:To determine the suppressive and curative activity of aqueous leaf extract of Ageratum conyzoides(A.conyzoides) in combination with chloroquine and artesunate, respectively against Plasmodium berghei infection in mice.Methods:Using malaria(Plasmodium berghei) infected albino mice of both sexes,aqueous extracts of A.conyzoides in combination with chloroquine and artesunate were tested for antimalarial activity,respectively.Four-day suppressive test and Rane’s curative test were carried out.Results:Suppressive tests showed significant dose dependent reduction in parasitemia level produced by the extract-chloroquine and extract-artesunate combinations.Suppressive activities of both extract-drug combinations were greater than the individual drugs alone.Extract-chloroquine(100:5) produced the highest suppressive effect(98%suppression).Curative tests showed absolute survival in two extract-drug combinations.Two extract-drug combinations produced higher curative effects than the individual drugs alone.The highest dose combinations of extract-chloroquine(100:5) and extract-artesunate(100:5) produced absolute parasitemia clearance(cure) in the infected mice. Conclusions:The study indicated that aqueous extract of A.conyzoides had the ability to potentiate the antimalarial activity of chloroquine and artesunate against induced plasmodiasis in mice.It contributes a lot in the malaria endemic and poverty stricken tropics. | Ukwe Chinwe V Ekwunife Obinna I Epueke Ebele A Ubaka Chukwuemeka M | 2010 | Asian Pacific Journal of Tropical Medicine2010，3，12： | 0 |
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