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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 | Association of ABO blood group and Plasmodium falciparum malaria in Dore Bafeno Area,Southern Ethiopia显示文摘Objective:To assess the distribution of ABO blood group and their relationship with Plasmodium falciparum(P.falciparum) malaria among febrile outpatients who sought medical attention at Dore Bafeno Health Center,Southern Ethiopia.Methods:A total of 269 febrile outpatients who visited Dore Bafeno Health Center,Southern Ethiopia,were examined for malaria and also tested for ABO blood groups in January 2010.The blood specimens were collected by finger pricking,stained with Geimsa,and examined microscopically.Positive cases of the parasitemia were counted.CareStart^(TM) Malaria PflPv Combo was also used to test the blood specimens for malaria.ABO blood groups were determined by agglutination test using ERYCLONE antisera.Data on socio-demographic characteristics and treatment status of the participants were also collected.Chi-square and ANOVA tests were used to assess the difference between frequencies and means,respectively.Results:Out of a total of 269 participants,178(66.2%) febrile patients were found to be infected with Plasmodium parasites,among which 146(54.3%),28(10.4%),and 4(1.5%) belonged to P.falciparum,P.vivax,and mixed infections,respectively.All febrile patients were also tested for ABO blood groups and 51.3%,23.5%,21.9%and 3.3%were found to be blood types of 0,A,B and AB,respectively.Both total malaria infection and P.falciparum infection showed significant association with blood types(P<0.05).The proportion of A or B but not 0 phenotypes was higher(P<0.05) in individuals with P.falciparum as compared with non-infected individuals.The chance of having P.falciparum infection in patients with blood groups A,B and AB was 2.5,2.5 and 3.3times more than individuals showing blood 0 phenotypes,respectively.The mean P.falciparum malaria parasitemia for blood groups A,B,AB,and 0 were 3 744/μ L,1 805/ μ L,5 331/μ L,and1 515/μ L,respectively(P<0.01).Conclusions:The present findings indicate that individuals of blood groups A,B and AB are more susceptible to P.falciparum infection as compared with individuals of blood group O.Nevertheless,further in depth studies are required to clearly establish the role that ABO blood group plays in P.falciparum malaria. | Tewodros Zerihun Abraham Degarege Berhanu Erko | 2011 | Asian Pacific Journal of Tropical Biomedicine2011，1，4： | 10 |
| 3 | In vitro larvicidal potential against Anopheles stephensi and antioxidative enzyme activities of Ginkgo biloba,Stevia rebaudiana and Parthenium hysterophorous显示文摘Objective:To investigate in vitro larvicidal and antioxidant enzymes potential of the medicinal plants Ginkgo biloba(G.biloba),Stevia rebaudiana(S.rebaudiana) and Parthenium hysterophorous(P.hysterophorous) against Anopheles stephensi(An.stephensi) 4th instars larvae. Methods:For evaluation of larvicidal potential,the ethanolic,methanolic and dichloromethane leaves extracts of three different plants were used in dose-dependent experiments in two media, while the antioxidant enzymes activities were investigated using four different methods viz., superoxide dismutase,peroxidase,ascorbate and catalase.Results:An.stephensi has developed resistance to various synthetic insecticides,making its control increasingly difficult.The comparative performance of ethanolic extracts(65%-90%) was found better than the methanolic extract(70%-87%) and dichloromethane extract(60%-70%).Among the three plants extracts tested in two media,S.rebaudiana exhibited higher larvicidal activity with LC50(24 h) in methanolic extract than P.hysterophorous and G.biloba.G.biloba and P.hysterophorous exhibited the strongest antioxidative enzymes activity and S.rebaudiana were less active and no significant difference was observed.Conclusions:These three plants exhibit larvicidal potential and can be further used for vector control alternative to synthetic insecticide due to eco-friendly and diseases control,furthermore these plant species have potent antioxidative enzyme activities, therefore,making them strong natural candidate particularly for diseases which are caused due to free radicals. | Nisar Ahmad Hina Fazal Bilal H Abbasi Mazhar Iqbal | 2011 | Asian Pacific Journal of Tropical Medicine2011，4，3： | 2 |
| 4 | Comparison of protein patterns between Plasmodium falciparum mutant clone T9/94-M1-1(b3) induced by pyrimethamine and the original parent clone T9/94显示文摘Objective:To compare the protein patterns from the extracts of the mutant clone T9/94-M1-1(b3)induced by pyrimethamine,and the original parent clone T9/94 following separation of parasite extracts by two-dimensional electrophoresis(2-DE).Methods:Proteins were solubilized and separated according to their charges and sizes.The separated protein spots were then detected by silver staining and analyzed for protein density by the powerful image analysis software.Results:Differentially expressed protein patterns(up—or down-regulation)were separated from the extracts from the two clones.A total of 223 and 134 protein spots were detected from the extracts of T9/94 and T9/94-M1-1(b3)clones,respectively.Marked reduction in density of protein expression was observed with the extract from the mutant(resistant)clone compared with the parent(sensitive)clone.A total of 25 protein spots showed at least two-fold difference in density,some of which exhibited as high as ten-fold difference.Conclusions:These proteins may be the molecular targets of resistance of Plasmodium falciparum to pyrimethamine.Further study to identify the chemical structures of these proteins by mass spectrometry is required. | Kanchana Rungsihirunrat Wanna Chaijaroenkul Napapom Siripoon Aree Seugorn Sodsri Thaithong Kesara Na-Bangchang | 2012 | Asian Pacific Journal of Tropical Biomedicine2012，2，1： | 0 |
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