Toxicity and potential anti-trypanosomal activity of ethanolic extract of Azadirachta indica (Maliacea) stem bark: An in vivo and in vitro approach using Trypanosoma brucei

2010 ◽  
Vol 128 (2) ◽  
pp. 495-500 ◽  
Author(s):  
Albert Wulari Mbaya ◽  
Umar Isah Ibrahim ◽  
Onyiche Thank God ◽  
Sanya Ladi
Keyword(s):  
Trypanosoma Brucei ◽  
Azadirachta Indica ◽  
Ethanolic Extract ◽  
Stem Bark

scholarly journals In vivo Neurological, Analgesic and In vitro Antioxidant and Cytotoxic Activities of Ethanolic Extract of Leaf and Stem Bark of Wedelia chinensis

2019 ◽  
Vol 22 (1) ◽  
pp. 18-26
Author(s):  
Sayema Khanum ◽  
Md Shahid Sarwar ◽  
Mohammad Safiqul Islam
Keyword(s):  
Body Weight ◽  
Oral Administration ◽  
Radical Scavenging ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
Pharmaceutical Journal ◽  
Stem Bark ◽  
Cytotoxic Activities

Wedelia chinensis is a widely used anti-inflammatory and hepatoprotective medicinal plant in Bangladesh. In this study, analgesic, neurological, antioxidant and cytotoxic activities of the ethanolic extract of leaf and stem bark of W. chinensis were investigated. Oral administration of the ethanolic extract of W. chinensis (200- and 300-mg/kg body weight) was investigated on animal model for neurological activity using open field test and hole cross test. Acetic acid induced writhing method was used to assess the analgesic activity. DPPH (1,1-diphenyl, 2-picryl hydrazyl) radical scavenging assay was used for determining the antioxidant activity, while brine shrimp lethality bioassay was used for investigating cytotoxicity. The ethanol extract of the plant produced significant reduction (P<0.05) of locomotion in both doses (200- and 300-mg/kg body weight) indicating pronounced neurological activity. Oral administration of alcoholic leaves and stem extracts significantly (p < 0.05) inhibited writhing response in mice. The percentage of scavenging of DPPH free radical was found to be concentration dependent with IC50 value of 44.10 ± 0.65 and 38.96 ± 0.50 μg/ml for leaves and stem extracts, respectively. Our findings indicate that W. chinensis may be a source of natural antioxidant with potent analgesic, neurological and cytotoxic activities. Bangladesh Pharmaceutical Journal 22(1): 18-26, 2019

scholarly journals IN VITRO AND IN VIVO ANTI-TRYPANOSOMAL ACTIVITIES OF METHANOL EXTRACT OF AZADIRACHTA INDICA STEM-BARK

2017 ◽  
Vol 14 (6) ◽  
pp. 72-77
Author(s):  
Everlyne N Wanzala ◽  
Nicholas K Gikonyo ◽  
Grace Murilla ◽  
Mercy Githua ◽  
Ahmed Hassanali
Keyword(s):  
Azadirachta Indica ◽  
Methanol Extract ◽  
Stem Bark

Antiinflammatory and immunomodulatory activity of an ethanolic extract from the stem bark of Terminalia catappa L. (Combretaceae): In vitro and in vivo evidences

2016 ◽  
Vol 192 ◽  
pp. 309-319 ◽  
Author(s):  
Oyindamola O. Abiodun ◽  
Alba Rodríguez-Nogales ◽  
Francesca Algieri ◽  
Ana Maria Gomez-Caravaca ◽  
Antonio Segura-Carretero ◽  
...  
Keyword(s):  
Ethanolic Extract ◽  
Stem Bark ◽  
Immunomodulatory Activity ◽  
Terminalia Catappa

Anti-parasitic activity of Annona muricata L. leaf ethanolic extract and its fractions against Toxoplasma gondii in vitro and in vivo

2021 ◽  
pp. 114019
Author(s):  
Natália Carnevalli Miranda ◽  
Ester Cristina Borges Araujo ◽  
Allisson Benatti Justino ◽  
Yusmaris Cariaco ◽  
Caroline Martins Mota ◽  
...  
Keyword(s):  
Toxoplasma Gondii ◽  
Ethanolic Extract ◽  
Annona Muricata ◽  
Parasitic Activity

scholarly journals Antitrypanosomal activity of purine nucleosides can be enhanced by their conversion to O-acetylated derivatives.

1996 ◽  
Vol 40 (11) ◽  
pp. 2567-2572 ◽  
Author(s):  
J R Sufrin ◽  
D Rattendi ◽  
A J Spiess ◽  
S Lane ◽  
C J Marasco ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Parent Compound ◽  
Nucleoside Analogs ◽  
Significant Activity ◽  
Structural Class ◽  
Antitrypanosomal Activity ◽  
Salvage Pathways ◽  
Purine Salvage Pathways

Fifteen purine nucleosides and their O-acetylated ester derivatives were examined for in vitro antitrypanosomal activity against the LAB 110 EATRO isolate of Trypanosoma brucei brucei and two clinical isolates of Trypanosoma brucei rhodesiense. Initial comparisons of activity were made for the LAB 110 EATRO isolate. Three nucleoside analogs exhibited no significant activity (50% inhibitory concentrations [IC50s] of > 100 microM), whether they were O acetylated or unacetylated; three nucleosides showed almost equal activity (IC50s of < 5 microM) for the parent compound and the O-acetylated derivative; nine nucleosides showed significantly improved activity (> or = 3-fold) upon O acetylation; of these nine analogs, six displayed activity at least 10-fold greater than that of their parent nucleosides. The most significant results were those for four apparently inactive compounds which, upon O acetylation, displayed IC50s of < or = 25 microM. When the series of compounds was tested against T. brucei rhodesiense isolates (KETRI 243 and KETRI 269), their antitrypanosomal effects were comparable to those observed for the EATRO 110 strain. Thus, our studies of purine nucleosides have determined that O acetylation consistently improved their in vitro antitrypanosomal activity. This observed phenomenon was independent of their cellular enzyme targets (i.e., S-adenosylmethionine, polyamine, or purine salvage pathways). On the basis of our results, the routine preparation of O-acetylated purine nucleosides for in vitro screening of antitrypanosomal activity is recommended, since O acetylation transformed several inactive nucleosides into compounds with significant activity, presumably by improving uptake characteristics. O-acetylated purine nucleosides may offer in vivo therapeutic advantages compared with their parent nucleosides, and this possibility should be considered in future evaluations of this structural class of trypanocides.

scholarly journals Characterization and selective inhibition of myristoyl-CoA:protein N-myristoyltransferase from Trypanosoma brucei and Leishmania major

2006 ◽  
Vol 396 (2) ◽  
pp. 277-285 ◽  
Author(s):  
Chrysoula Panethymitaki ◽  
Paul W. Bowyer ◽  
Helen P. Price ◽  
Robin J. Leatherbarrow ◽  
Katherine A. Brown ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Leishmania Major ◽  
Homo Sapiens ◽  
Selective Inhibition ◽  
Fungal Species ◽  
Chemotherapeutic Agents ◽  
Human Pathogens ◽  
Ic50 Values

The eukaryotic enzyme NMT (myristoyl-CoA:protein N-myristoyltransferase) has been characterized in a range of species from Saccharomyces cerevisiae to Homo sapiens. NMT is essential for viability in a number of human pathogens, including the fungi Candida albicans and Cryptococcus neoformans, and the parasitic protozoa Leishmania major and Trypanosoma brucei. We have purified the Leishmania and T. brucei NMTs as active recombinant proteins and carried out kinetic analyses with their essential fatty acid donor, myristoyl-CoA and specific peptide substrates. A number of inhibitory compounds that target NMT in fungal species have been tested against the parasite enzymes in vitro and against live parasites in vivo. Two of these compounds inhibit TbNMT with IC50 values of <1 μM and are also active against mammalian parasite stages, with ED50 (the effective dose that allows 50% cell growth) values of 16–66 μM and low toxicity to murine macrophages. These results suggest that targeting NMT could be a valid approach for the development of chemotherapeutic agents against infectious diseases including African sleeping sickness and Nagana.

scholarly journals Cross-Resistance to Nitro Drugs and Implications for Treatment of Human African Trypanosomiasis

2010 ◽  
Vol 54 (7) ◽  
pp. 2893-2900 ◽  
Author(s):  
Antoaneta Y. Sokolova ◽  
Susan Wyllie ◽  
Stephen Patterson ◽  
Sandra L. Oza ◽  
Kevin D. Read ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Human African Trypanosomiasis ◽  
Parent Drug ◽  
Cross Resistance ◽  
Pharmacokinetic Studies ◽  
African Trypanosomiasis ◽  
Trypanosoma Brucei Brucei ◽  
Resistant Lines

ABSTRACT The success of nifurtimox-eflornithine combination therapy (NECT) for the treatment of human African trypanosomiasis (HAT) has renewed interest in the potential of nitro drugs as chemotherapeutics. In order to study the implications of the more widespread use of nitro drugs against these parasites, we examined the in vivo and in vitro resistance potentials of nifurtimox and fexinidazole and its metabolites. Following selection in vitro by exposure to increasing concentrations of nifurtimox, Trypanosoma brucei brucei nifurtimox-resistant clones designated NfxR1 and NfxR2 were generated. Both cell lines were found to be 8-fold less sensitive to nifurtimox than parental cells and demonstrated cross-resistance to a number of other nitro drugs, most notably the clinical trial candidate fexinidazole (∼27-fold more resistant than parental cells). Studies of mice confirmed that the generation of nifurtimox resistance in these parasites did not compromise virulence, and NfxR1 remained resistant to both nifurtimox and fexinidazole in vivo. In the case of fexinidazole, drug metabolism and pharmacokinetic studies indicate that the parent drug is rapidly metabolized to the sulfoxide and sulfone form of this compound. These metabolites retained trypanocidal activity but were less effective in nifurtimox-resistant lines. Significantly, trypanosomes selected for resistance to fexinidazole were 10-fold more resistant to nifurtimox than parental cells. This reciprocal cross-resistance has important implications for the therapeutic use of nifurtimox in a clinical setting and highlights a potential danger in the use of fexinidazole as a monotherapy.

scholarly journals Atividade do óleo de Eucalyptus citriodora e Azadirachta indica no controle de Colletotrichum acutatum em morangueiro

2010 ◽  
Vol 36 (3) ◽  
pp. 228-232 ◽  
Author(s):  
Cláudia Regina Dias-Arieira ◽  
Lucas da Rocha Ferreira ◽  
Jailson de Oliveira Arieira ◽  
Edenilson Gonçalves Miguel ◽  
Mateus Augusto Donega ◽  
...  
Keyword(s):  
Azadirachta Indica ◽  
Colletotrichum Acutatum ◽  
Eucalyptus Citriodora

A flor-preta é uma das doenças mais importantes do morangueiro e a busca por alternativas de controle tem sido uma constante, principalmente em áreas de cultivo orgânico. Assim, objetivou-se avaliar a eficiência, in vitro e in vivo, dos óleos de Eucalyptus citriodora e Azadirachta indica no controle de Colletotrichum acutatum em morangueiro. No experimento in vitro determinou-se a inibição do crescimento micelial quando o fungo foi submetido aos extratos nas concentrações de 0; 0,25; 0,5; 1,0 e 1,5%. No campo, avaliou-se o controle da doença com a aplicação dos óleos nas concentrações de 0, 0,5 e 1,0%, pulverizados em intervalos de 7, 15 e 30 dias, em plantas inoculadas com suspensão de 10(6) conídios/mL. As avaliações foram realizadas semanalmente, observando-se a ocorrência e tamanho de lesões no pedúnculo e nos frutos, abortamento floral, produtividade, e ocorrência natural da doença. In vitro todos os tratamentos apresentaram redução significativa do crescimento micelial do fungo quando comparados ao controle. No campo, apenas o óleo de nim apresentou efeito significativo, reduzindo o abortamento floral e a ocorrência de frutos doentes advindos de flores inoculadas. Porém, maior ocorrência natural de doença foi observada quando a dosagem de 1,0% foi aplicada semanalmente.

Sign in / Sign up

Export Citation Format

Share Document