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| 1 | 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 |
| 2 | Antimalarial potential of kolaviron,a biflavonoid from Garcinia kola seeds,against Plasmodium berghei infection in Swiss albino mice显示文摘Objective:To investigate the antimalarial potential of kolaviron(KV),a biflavonoid fraction from Garcinia kola seeds,against Plasmodium berghei(P.berghei)infection in Swiss albino mice.Methods:The study consists of seven groups of ten mice each.Groups I,II and III were normal mice that received com oil.KV1 and chloroquine(CQ),respectively.Groups IV,V,ⅥandⅦwere infected mice that received corn oil.CQ,KYI and KV2.respectively.CQ.KY1 and KV2were given at 10-,100-and 200-mg/kg daily,respectively for three consecutive days.Results:Administration of KV1 and KV2 significantly(P<0.05)suppressed P.berghei-infection in the mice by 85%and 90%.respectively,while CQ produced 87%suppression relative to untreated infected group after the fifth day of treatment.Also,KV2 significantly(P<0.05)increased the mean survival time of the infected mice by 175%.The biflavonoid prevented a drastic reduction in HCV from day4 of treatment,indicating its efficacy in ameliorating anaemia.Significant(P<0.05)oxidative stress assessed by the elevation of serum and hepatic malondialdehydewere observed in unlrealed P.berghei-infected mice.Specifically,senum and hepatic malondialdehyde levels increased by93%and 78%,resjiectively in the unlrealed infecled mice.Furlhennore,antioxidant indices,viz;superoxide dismutase.catalase,glutathione-s-transferasc.glualhione peroxidase and reduced gluathione decreased significantly(P<0.05)in the tissues of untreated P.berghei-infected mice.KV significantly(P<0.05)ameliorated the P.berghei-induced decrease in antioxidant status of the infected mice.Conclusions:This study shows that kolaviron,especially at 200 mg/kg,has high antimalarial activities in P.berghei-infected mice,in addition to its known antioxidant properties. | Adaramoyc Oluwatosin Akinpelu Tolulope Kosoko Ayokulchin Okoric Patricia Kehinde Aderemi Falade Catherine Ademowo Olusegun | 2014 | Asian Pacific Journal of Tropical Medicine2014，7，2： | 2 |
| 3 | Antimalarial potency of the leaf extract of Aspilia africana(Pers.) C.D.Adams显示文摘Objective:To investigate the antimalarial activity of ethanol extract of Aspilin africana (A.africana) leaf.Methods:The ethanol extract of A.africana leaf(100-400 mg/kg) was screened for blood schizonticidal effect against chloroquine-sensitive Plasmodium berghei(P. berghei) in mice both in early and established models of antimalarial studies.Results:The leaf extract exhibited significant(P<0.05) antiplasmodial activity in 4-day early infection and in established infection tests with a considerable mean survival time comparable to that of standard drug,chloroquine(10 mg/kg).Conclusions:The findings show thai ethanol extract of A.africana leaf possesses potent antiplasmodial activity which justify the use in ethnomedicine and can be developed in malaria therapy. | Akuodor Godwin Christian Amos Grace Mfon Essien Augustine Dick Essien David-Oku Akpan Joseph Linus Ezeokpo Basil Chukwuma | 2012 | Asian Pacific Journal of Tropical Medicine2012，5，2： | 2 |
| 4 | 为从变形体 berghei 的氮的氧化物 synthase 和类似的蛋白质的结构和功能的生物信息学分析和预言显示文摘 <正>Objective:To search and analyze nitric oxide synthase(NOS) and similar proteins from Plasmodium berghei(Pb).Methods:The structure and function of nitric oxide synthase and similar proteins from Plasmodium berghei were analyzed and predicted by bioinformatics. Results:P6NOS were not available,but nicotinamide adenine dinucleotide 2’-phosphate reduced tetrasodium(NADPH)-cytochrome p450 reductase(CPR) were gained.PiCPR was in the nucleus of Plasmodium berghei,while 134aa-229aa domain was localize in nucleolar organizer. The amino acids sequence of P6CPR had the closest genetic relationship with Plasmodium vivax showing a 73%homology.The tertiary structure of PbCPR displayed the forcep-shape with wings,but no wings existed in the tertiary structure of its’ host,Mus musculus(Mm).137aa-200aa, 201aa-218aa,220aa-230aa,232aa-248,269aa-323aa,478aa-501aa and 592aa-606aa domains of P6CPR showed no homology with MmCPRs’,and all domains were exposed on the surface of the protein.Conclusions:NOS can’t be found in Plasmodium berghei and other Plasmodium species.PbCPR may be a possible resistance site of antimalarial drug,and the targets of antimalarial drug and vaccine.It may be also one of the mechanisms of immune evasion.This study on Plasmodium berghei may be more suitable to Plasmodium vivax.And137aa-200aa, 201aa-218aa,220aa-230aa,232aa-248,269aa-323aa,478aa-501aa and 592aa-606aa domains of PbCPR are more ideal targets of antimalarial drug and vaccine. | Zhigang Fan Gang Lv Lingmin Zhang Xiufeng Gan Qiang Wu Saifeng Zhong Guogang Yan Guifen Lin | 2011 | Asian Pacific Journal of Tropical Medicine2011，4，1： | 2 |
| 5 | 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 |
| 6 | Comparative study of chloroquine and quinine on malaria rodents and their effects on the mouse testis显示文摘Objective:To evaluate the effects of quinine and chloroquine against mole mice infected with Plasmodium berghei and their adverse effects on the mice testes.Methods:In this study,48 adult male mice,(20-23 g).aged 8 to 12 weeks were divided into four groups.This study was carried out from December 2009 until May 2010 in the School of Public Health,Tehran University of Medical Sciences.Results:The results showed that 58.33%of mice treated with chloroquine were completely recovered.Parasitemia was 4%on day 8 when compared to that on day 0,whereas it was 9%on day 9.There was no orchitis found in this group.The mortality of mice after exposing to quinine on day 5 was 8.3%,whereas from day 10 to day 14 it was 91.7%.We found 73%orchitis occurred in quinine treated group.There was a significant difference between quinine and chloroquine effects on the parasite and also mice testes(P<0.05).Conclusions:In this study,It can be concluded that male mice have full resistance to the quinine.Quinine does not only make male mice recover completely,but also cause inflammation on mice testicles tissue. | Esmail Abolghasemi Seyed Hassan Moosa-Kazemi Maryam Davoudi Ahmad Reisi Mohammad Taghi Satvat | 2012 | Asian Pacific Journal of Tropical Biomedicine2012，2，4： | 1 |
| 7 | Immunogenicity and immunizing protection effect of GAMA gene DNA vaccine on Plasmodium berghei显示文摘Objective: To explore the effect of immunogenicity and immunizing protection of GAMA gene DNA vaccine, which was related with merozoite, ookinete and sporozoite invasion. Methods:Gene fragments were obtained using PCR technique and eukaryotic expression vector(containing immunostimulatory sequence) was built. BALB/c mice were divided into PBS control group, empty vector control group and study group and were immunized at week 0, 3 and 6 respectively. Blood was collected 2 weeks after each immunization and serum was separated to detect the Ig G, Ig G1 and Ig G2 a levels. Spleen of mice was obtained for preparation of splenic mononuclear cell and the cytokine IL-4 and IFN-αlevels were detected. Indirect immunofluorescence and western blot were employed to verify the specificity of antiserum. Sporozoite and merozoite invasion were used respectively to detect the immune protective effect 2 weeks after the third immunization. Ookinete conversion rate in vitro and oocyst numbers of mosquito stomach were observed to evaluate the transmission-blocking levels. Results: In GAMA DNA vaccine group: antiserum could be combined with recombinant protein specifically and green fluorescence signals of merozoite, ookinete and sporozoite were observable, while specific fragments and fluorescence signals were not observable in empty vector group. Compared with control group, specific Ig G in DNA vaccine immunity group significantly increased(P<0.01), and Ig G1 and Ig G2 a all increased(P<0.01). IL-4, IFN-αcontent in study group significantly increased, compared with control group(P<0.01). GAMA DNA vaccine immunity could not obviously block the erythrocyte-stage infection(caused by sporozoite invasion); compared with control group, liver worm load was slightly reduced(P<0.05), and antiserum ookinete numbers(cultured in vitro) had no significant difference with oocyst numbers of mosquito stomach in DNA vaccine group. Conclusions:GAMA has good antigenicity, which could stimulate the body to produce specific immune responses; while DNA vaccine immunity could not play a good protective effect, the effect of which is only limited to the slight reduction of liver worm load, and has no obvious erythrocytestage protective effect and transmission-blocking effect. Therefore, trying other immunization strategies for further research on the value of GAMA(as multi-stage antigen vaccine and multistage combined vaccine components of the life-cycle of plasmodium) is necessary. | Feng Du Si Wang Chen Zhao Ya-Ming Cao En-Jie Luo | 2016 | Asian Pacific Journal of Tropical Medicine2016，9，2： | 1 |
| 8 | Nauclea latifolia aqueous leaf extract eliminates hepatic and cerebral Plasmodium berghei parasite in experimental mice显示文摘Objective: To assess the effects of hot water leaf extract of Nauclea latifolia(N. latifolia) on antioxidant status, lipid peroxidation values and parasite levels in hepatic and brain tissue of experimental mice(BALB/c) infected with Plasmodium berghei(P. berghei) malaria.Methods: Forty nine mice were divided into seven groups(n = 7) and used for the study. Group A(control) were given 0.2 m L/kg phosphate buffer saline; Group B mice were infected with P. berghei and treated with phosphate buffer saline. Groups C and D mice were also infected but treated with 200 and 300 mg/kg body weight of leaf extract respectively. Groups E and F mice were not infected, but received 200 and 300 mg/kg of leaf extract respectively. Group G mice were infected and treated with chloroquine(5 mg/kg). Liver and brain tissues of mice were prepared for both biochemical assay and microscopic examination. Results: Results showed that P. berghei malaria infection induced oxidative stress in both liver and brain tissues as evidenced by the significant(P < 0.05) decrease in antioxidants: superoxide dismutase, reduced glutathione and catalase. These reductions perhaps caused compromise in membrane integrity as indicated by the significant increase in lipid peroxidation product malondialdhyde. Malaria parasites were also identified in these tissues. However, N. latifolia treatment eliminated the parasites in tissues and protected them from oxidative damage even better than chloroquine treatment did, whose anti-malarial potency also cleared tissue parasites. The measurement of protection by N. latifolia against damage was strengthened by the insignificant micro structural alterations.Conclusions: The bioactive phytochemical(s) in N. latifolia should be structured and the mechanism(s) of its antimalarial tendency should be further investigated. | Innocent Onyesom Ejovi Osioma Precious Chiamaka Okereke | 2015 | Asian Pacific Journal of Tropical Biomedicine2015，5，7： | 1 |
| 9 | 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 |
| 10 | Nano chloroquine delivery against Plasmodium berghei NK65 induced programmed cell death in spleen显示文摘Objective:To compare the protective effects of chitosan-trypolyphosphate(CS-TPP) nanoparticle conjugated chloroquine(CQ) with effect of CQ alone on the reversal of splenic damages and induction of apoptosis.Methods:Different researches have been carried out to explore the potential role of chitosan based drug delivery system against parasitic diseases.After successive Plasmodium berghei NK65 parasiste infection by intraperitoneal injection in Swiss mice and subsequent parasite development,the ROS generation,anti-apoptotic and pro apoptotic protein levels in spleen were measured.To analyze caspases,flow cytometry study was performed with annexin 桋-FITC and with PI staining.Results:The results revealed that ROS mediated caspase 3 and 9 activation and the induction of apoptosis occurred during the parasitic infection.However,CS-TPP conjugated CQ was relatively better in reversing the splenic damage compared with similar effects of CQ alone.Conclusions:This study indicates that Plasmodium berghei NK65 induces apoptosis in the spleen.The study further shows that CS-TPP nanoparticles conjugation with CQ have positive influence on the recovery of damaged host's system towards maintenance of normal homeostasis,and this is shown to be selective to CS-TPP conjugated CQ treated animals only. | Satyajit Tripathy Sourav Chattopadhyay Sandeep Kr.Dash Motlalepula G.Matsabisa Somenath Roy | 2018 | Asian Pacific Journal of Tropical Medicine2018，11，9： | 0 |
| 11 | Pharmacodynamic evaluation for antiplasmodial activity of Holarrhena antidysentrica(Kutaja) and Azadirachta indica(Neemb) in Plasmodium berghei infected mice model显示文摘Objective:To investigate in-vivo anti-plasmodial activity of aqueous extracts of plants selected based on the symptomology mentioned in Ayurveda.Methods:The aqueous extracts of Holarrhena antidysentrica(H.antidysentrica)(Kutaja) and Azadirachta indica(A.indica)(Neemb) for their antiplasmodial potential in Plasmodium berghei(P.berghei) infected mice was assessed using Peters four day suppressive test.Both the extracts were administered at 2 dose levels,full dose(1 000 mg/d) and minimized dose(200 mg/d).10~6 P.berghei infected RBCs were injected on day ’0’ and treated from day ’0’ till day ’3’ post-infection,Tail blood smears were collected, giemsa stained and analyzed.The mice were observed for survival and parasitemia was assessed till 50%of mice in control survived.Results:It was observed that the percentage of parasitemia increased gradually in all the groups,with maximum in control group(Day 3-35,Day 9-46.98) and minimum in Chloroquine arm(Day 3-14.06.Day 9-19.92).The percentage of parasitemia was compared using Mann-Whitney U test depicting that all test groups exhibited reduction in parasitemia as compared to control(P-value<0.002 for all groups).These groups showed similar percentage of survival as Chloroquine.Conclusions:The present investigation demonstrated the anti-plasmodial effects of H.antidysentrica and A.indica.which are two most commonly used medicinal plants in Ayurved for treatment of fever. | Jadhav Priyanka Lal Hingorani Kshirsagar Nilima | 2013 | Asian Pacific Journal of Tropical Medicine2013，6，7： | 0 |
| 12 | Effect of pre-existing Schistosoma haematobium infection on Plasmodium berghei multiplications in imprinting control region mice显示文摘Objective: To investigate the effect of pre-existing Schistosoma haematobium(S. haematobium) infection on malaria disease severity.Methods: The study involved the use of twenty-i ve imprinting control region mice, i fteen of which were initially infected with S. haematobium. Five of the remaining ten schistouninfected mice together with i ve schisto-infected mice were infected with Plasmodium berghei(P. berghei) after four weeks(acute stage) of schistosoma infection. The remaining i ve schisto-uninfected mice together with i ve schisto-infected mice were also infected with P. berghei after seven weeks(chronic stage) of schistosoma infection. The last i ve schistoinfected mice were used as control group. They were then monitored for changes in P. berghei parasitaemia on Days 3, 5, 7, 9 and 11 post-infection. Records on their survivability were also taken.Results: The co-infected mice had signii cantly higher malaria parasitaemia, compared with the mono-infected mice during acute S. haematobium infection. In contrast, the co-infected mice had signii cantly lower malaria parasitaemia during chronic S. haematobium infection and a higher survival rate.Conclusions: Co-infection of mice with P. berghei during acute S. haematobium infection resulted in rapid P. berghei development and increased malaria parasitaemia. However, the co-infection resulted in slower P. berghei development and decreased malaria parasitaemia with enhanced survivability of the mice during chronic S. haematobium infection. Therefore, pre-existing chronic S. haematobium infection may provide some protection to the host by reducing parasitaemia. | Benjamin Amoani Elvis Ofori Ameyaw Du-Bois Asante Francis Ackah Armah James Prah Collins Paa Kwesi Botchey Johnson Nyarko Boampong | 2015 | Asian Pacific Journal of Tropical Biomedicine2015，5，6： | 0 |
| 13 | Comparative effects of parenteral antimalarials in Swiss albino mice after chronic exposure to Plasmodium berghei显示文摘Mice are considered to be a similar model to humans in the pathogenesis of malaria. This study evaluates the effect of parenteral antimalarials on the spleen and liver of Swiss albino mice after chronic exposure to Plasmodium berghei. After chronic exposure to P. berghei NK65 strain, the level of parasitemia was assessed.The mice were treated for 3 days using chloroquine(5 mg/kg), quinine(10 mg/kg),and artemether(2 mg/kg). The effect of chronic exposure and the pattern of recovery were evaluated. There was significant decrease in total body weight after chronic exposure to P. berghei(P < 0.05). An increase in total weight recovery was seen after day 15 of treatment with the antimalarials; this was more pronounced with artemether. A significant increase in liver and spleen weights due to P. berghei infection was seen. There was a recovery pattern due to decrease in liver and spleen weights following antimalarial administration, which was greatest with artemether(P < 0.05). Significant changes were more in parasitized, quinine and artemether groups(P < 0.05). There was a significant decrease in total spleen protein due to chloroquine but a decrease due to quinine and artemether(P < 0.05). No significant changes in liver and spleen albumin were observed after treatment. The highest parasite clearance was observed with artemether, followed by quinine. Five mice died after chronic exposure in all the groups prior to treatment. There was significant enlargement and discoloration of spleen and liver after chronic exposure. This study showed that artemether aided recovery of the liver and spleen better than quinine and chloroquine in albino mice after chronic exposure to P. berghei. This suggests there is potential for improvement in antimalarial therapy. | Sylvester Aghahowa Kenka Okolocha | 2018 | Animal Models and Experimental Medicine2018，1，3： | 0 |
| 14 | Construction and identification of recombinant plasmid pUIS3-BLC^+显示文摘Objective:To construct and identify recombinant plasmid pUIS3-BLC^+.Methods:The cDNA of B-lymphocyte chemoattractant(BLC) was amplified from the total RNA of spleen tissues by PCR method,and were inserted into plasmid of Plasmodium berghei with U1S3 knockout by digestion of restrictive endonuclease and T7 ligation.The recombinant plasmids were screened,and then underwent restriction enzymatic digestion and DNA sequencing.Then the confirmed plasmid was further transfected into COS-1 cells by lipofectamine and the BLC expression was tested by RT-PCR and Western blotting.Results:The cDNA of BLC gene was correctively amplified by RT-PCR and the recombinant plasmid pUIS3-BLC^+ was constructed successfully,which was confirmed by restriction enzymatic digestion and DNA sequencing.RT-PCR and Western blotting also showed the BLC gene expression in COS-1 cells.Conclusions:The recombinant plasmid pUIS3-BLC^+ has BLC expression in COS-1 cells,and is useful for further study on BLC transgene and UIS3 gene knockout in Plasmodium berghei. | Yingzi Lin Shixiang Bao Guanghong Tan Fengying Huang Huiqin Huang | 2010 | Asian Pacific Journal of Tropical Medicine2010，3，10： | 0 |
| 15 | 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 |
| 16 | Effects of the methanolic seeds extract of Carica Papaya on plasmodium Berghei infected mice显示文摘Objective:The leaves extract of Carica Papaya(C.Papaya)papaya has been shown to possess antimalarial activity, thus this work aims at finding out if the plants antimalarial activity is present in or extended to the seeds.Methods:The seeds of C.papaya were collected from its fruit,air dried for 5 days and ground into fine powder.80.65 g of the powder was then soaked for 48hours in 300 mL of methanol.Filtration was carried out using Whatman No.1 filter paper.The filtrate was evaporated to dryness by a three-day continuous heating on a hot plate of 30℃.The dry extract yield was scraped out of the Petri dish weighed and refrigerated until required. The percentage extract yield was calculated out from the initial powder weight.A preliminary phytochemical study was done by re-dissolving the appropriate amount of the dry extract in distilled water and appropriate test reagent added.The LD50 of the seeds of C.papaya was carried out using arithmetic method.Swiss albino Mice of both sexes and of average weight of 18-25 g were used as animals for antimalarial activity.They were housed in standard animal house,fed on Rats/Mice pellets and had non restricted excess to both feed and water throughout the 60day study period.While the non pregnant female Mice were used as test animals,the male animals were used as malaria parasite donors.Precautions were taken to ensure that all animals in the study groups were free from infection with Eperythrozoon coocoides.The female animals were then divided into three main groups(A-C) of 25 animals per group.Group A was used for malaria suppressive study(early infection -day 0-3) and was further subdivided to 5 subgroups(a-e) of 5animals per group.Group B was used for malaria curative study(established malaria infection-day 3-7) and was further subdivided to 5subgroups(a-e) of 5animals per group.Group C was used for malaria prophylactic study(repository-4days treatment prior to malaria parasite infection) and was also further subdivided into 5subgroups(a-e) of 5animals per group.At the appropriate time,50 mg/kg/day,100 mg/kg/day and 200 mg/kg/day of crude extract of C.papaya were administered orally to the different subgroups(b-d) within the three main groups.One subgroup(a) in each main group also received orally,5 mg/kg/day of chloroquine phosphate as positive control while one subgroup (e) in each main group also received orally,0.2 mL/kg/day of distilled water as negative control.Malaria parasites infected red blood cells numbering 1×10 and suspended in 0.2 mL of physiological saline was inoculated intraperitoneally,to each animal of the subgroups(a-d) in each of the three main groups at the appropriate time.Blood smears were made from animals’tail,stained with Lieshman and examined microscopically at 100×for the presence of malaria parasite.Percentage malaria parastaemia was calculated as well as average percentage malaria parasitaemia suppression.Results:Extraction yield of 25.29%was obtained while the LD50 was 620 mg/kg.The phytochemistry showed the richly presence of alkaloids,as well as glycosides,carbohydrates, resins,fats and fixed oils.The suppressive study at doses of 200,100 and 50mg/kg/day showed 53.02%,43.43%and 19.83%suppressive activity against Plasmodium berghei respectively.This activity compared to that of chloroquine,a standard antimalaria drug that gave 95.95%suppressive anti-parasitaemia. The prophylactic study at doses of 200,100 and 50 mg/kg/day showed 63.85%,61.12%and 48.08%prevention to malaria parasitaemia respectively as against 94.78%showed by chloroquine.The curative study however,at doses of 200,100 and 50 mg/kg/day failed to suppress malaria parasitaemia with a mean survival range of 6-8days as against 27.2 days showed by chloroquine.The seeds extract of C.papaya showed a significant malaria parasitaemia suppressive activity(P≤0.05).These activities are dose dependent and comparable to those of Chloroquine phosphate.Conclusion:The results above suggest that the seeds extracts of C.papaya possess antimalarial activity like the leaf extracts.The antimalarial activity may be attributable to the richly presence of alkaloids and or the presence of its proteolytic enzyme(Papain).The present finding justifies the inclusion of the seeds of C.papaya in the treatment of malaria by local herbalists.The seeds extracts therefore,if well purified and characterized may be used in treatment of very early plasmodiasis as well as a good prophylactic drug in human.This work at the moment is limited to animals,thus clinical trials in humans is be recommended particularly,when C.papaya seeds are non harmful/non toxic. | Amazu LU Ebong OO Azikiwe CCA Unekwe PC Siminialayi MI Nwosu PJC Ezeani MC Obidiya OS Ajugwo AO | 2009 | Asian Pacific Journal of Tropical Medicine2009，2，3： | 0 |
| 17 | Antimalarial and analgesic activities of ethanolic leaf extract of Panicum maximum显示文摘Objective:To evaluate antiplasmodial and analgesic activities of ethanolic leaf extract/ fractions of Panicum maximum.Methods:The crude leaf extract(47-190 mg/kg) and fractions (chlor of orm,ethyl acqeous and methanol;96 mg/kg) of Panicum maximum were investigated for antiplasmodial activity against chloroquine sensitive Plasmodium berghei infections in mice and for analgesic activity against chemical and heat-induced pains.The antiplasmodial activity during early and established infections as well as prophylactic were investigated.Artesunate at 5 mg/kg and pyrimethamine at 1.2 mg/kg were used as positive controls.Analgesic activity of the crude extract/fractions was also evaluated against acetic acid,formalin and heat-induced pains.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<0.001).They also improved the mean survival time from 13 to 28 days compared with control(P<0.001).The activities of extract/ fractions were incomparable to that of the standard drugs(Artesunate and pyrimethamine).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.Condusions:Panicum maximum leaf extract has antiplasmodial and analgesic activities which may in part be mediated through the chemical constituents of the plant. | Jude E Okokon Paul A Nwafor Ukeme E Andrew | 2011 | Asian Pacific Journal of Tropical Medicine2011，4，6： | 0 |
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