scholarly journals Evaluation of in vivo antitrypanosomal activity of crude extracts of Artemisia abyssinica against aTrypanosoma congolense isolate

2014 ◽  
Vol 14 (1) ◽  
Author(s):  
Teka Feyera ◽  
Getachew Terefe ◽  
Workineh Shibeshi
Keyword(s):  
Antitrypanosomal Activity ◽  
Crude Extracts

scholarly journals Antitrypanosomal Activity of Hydromethanol Extract of Leaves of Cymbopogon Citratus and Seeds of Lepidium Sativum: in-vivo Mice Model

2021 ◽  
Author(s):  
Ayechew Yetayeh Emiru ◽  
Eyasu Makonnen Eshetu ◽  
Fikru Regassa Gari ◽  
Fekadu Regassa Gudeta ◽  
Takele Beyene Tufa
Keyword(s):  
Body Weight ◽  
Plant Extracts ◽  
Field Isolate ◽  
Lepidium Sativum ◽  
Mice Model ◽  
Cymbopogon Citratus ◽  
Cell Counts ◽  
Antitrypanosomal Activity ◽  
Crude Extracts

Abstract Background: Trypanosomiasis is one of the neglected tropical diseases of both humans and animals which decreases their productivity and causes death in the worst scenario. Unavailability of vaccine, low therapeutic index of trypanocidal drugs, and development of resistance lead to the need for research focused on developing alternative treatment options especially from medicinal plants. The present study was aimed to investigate antitrypanosomal activities of leaves of Cymbopogon citratus and seeds of Lepidium sativum in in vivo mice model. Methods: The plant extracts were prepared by maceration using 80% methanol and reconstituted with 10% dimethyl sulfoxide (DMSO) to have the desired concentration. The test doses were adjusted to 100, 200 and 400mg/kg based on the toxicity profile. The Plants extracts were administered to the respective groups of mice after the 12th day of field isolate T. congolense inoculation for seven consecutive days. The level of parasitemia, body weight, packed cell volume, and differential white blood cell counts were measured.Results: The in vivo test results revealed that both plant extracts had dose dependent antitrypanosomal activity. Both crude extracts showed a significant reduction in parasite load (P<0.05), ameliorate anaemia (increased or prevent the fall of PCV value) (P<0.05), decreased lymphocytosis and increased neutrophil counts (p<0.05) and improved body weight but significant body weight increment (P<0.05) was observed only in C. citratus treated mice compared to the negative and positive controls. Comparative results from all tested parameters showed that the best activities were observed with C. citratus treated groups of mice. Conclusion: The present study concluded that the crude extracts of leaves of C. citratus and seeds of L. sativum had antitrypanosomal effects and can be potential targets for further studies on the development of alternative antitrypanosomal agents.

scholarly journals Antitrypanosomal activity of hydromethanol extract of leaves of Cymbopogon citratus and seeds of Lepidium sativum: in-vivo mice model

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Ayechew Yetayeh Emiru ◽  
Eyasu Makonnen ◽  
Fikru Regassa ◽  
Fekadu Regassa ◽  
Takele Beyene Tufa
Keyword(s):  
Plant Extracts ◽  
Neglected Tropical Diseases ◽  
Field Isolate ◽  
Lepidium Sativum ◽  
Mice Model ◽  
Cymbopogon Citratus ◽  
Cell Counts ◽  
Antitrypanosomal Activity ◽  
Crude Extracts

Abstract Background Trypanosomiasis is one of the neglected tropical diseases of both humans and animals which decreases their productivity and causes death in the worst scenario. Unavailability of vaccines, the low therapeutic index of trypanocidal drugs, and the development of resistance lead to the need for research focused on developing alternative treatment options especially from medicinal plants. The present study was aimed to investigate antitrypanosomal activities of leaves of Cymbopogon citratus and seeds of Lepidium sativum in in-vivo mice model. Methods The plant extracts were prepared by maceration using 80% methanol and reconstituted with 10% dimethyl sulfoxide (DMSO) to have the desired concentration. The test doses were adjusted to 100, 200 and 400 mg/kg based on the toxicity profile. The plants extracts were administered to the respective groups of mice after the 12th day of field isolate T. congolense inoculation for seven consecutive days. The level of parasitemia, bodyweight, packed cell volume (PCV), and differential white blood cell counts were measured. Results The in -vivo test results revealed that both plant extracts had dose-dependent antitrypanosomal activity. Both crude extracts showed a significant reduction in parasite load (P < 0.05), increased or prevent the fall of PCV value (P < 0.05), decreased lymphocytosis and increased neutrophil counts (p < 0.05) and improved bodyweight but significant bodyweight increment (P < 0.05) was observed only in C. citratus treated mice compared to the negative and positive controls. Conclusion The present study concluded that the crude extracts of leaves of C. citratus and seeds of L. sativum had antitrypanosomal effects. Both plants extracts reduced parasitemia level, prevented anemia and improved bodyweight of treated mice. Comparative results from all tested parameters showed that the best activities were observed with C. citratus treated groups of mice.

The Role of nitro (NO2-), chloro (Cl), and fluoro (F) Substitution in the Design of Antileishmanial and Antichagasic Compounds

2020 ◽  
Vol 21 ◽  
Author(s):  
Boniface Pone ◽  
Ferreira Igne Elizabeth
Keyword(s):  
Chagas Disease ◽  
Mammalian Cells ◽  
Neglected Tropical Diseases ◽  
New Drugs ◽  
Pharmacokinetic Studies ◽  
Scientific Publications ◽  
Antitrypanosomal Activity ◽  
Chemical Groups

: Neglected tropical diseases (NTDs) are responsible for over 500,000 deaths annually and are characterized by multiple disabilities. Leishmaniasis and Chagas disease are among the most severe NTDs, and are caused by the Leishmania sp, and Trypanosoma cruzi, respectively. Glucantime, pentamidine and miltefosine are commonly used to treat leishmaniasis, whereas nifurtimox, benznidazole are current treatments for Chagas disease. However, these treatments are associated with drug resistance, and severe side effects. Hence, the development of synthetic products, especially those containing N02, F, or Cl, which chemical groups are known to improve the biological activity. The present work summarizes the information on the antileishmanial and antitrypanosomal activity of nitro-, chloro-, and fluoro-synthetic derivatives. Scientific publications referring to halogenated derivatives in relation to antileishmanial and antitrypanosomal activities were hand searched in databases such as SciFinder, Wiley, Science Direct, PubMed, ACS, Springer, Scielo, and so on. According to the literature information, more than 90 compounds were predicted as lead molecules with reference to their IC50/EC50 values in in vitro studies. It is worth to mention that only active compounds with known cytotoxic effects against mammalian cells were considered in the present study. The observed activity was attributed to the presence of nitro-, fluoro- and chloro-groups in the compound backbone. All in all, nitro and h0alogenated derivatives are active antileishmanial and antitrypanosomal compounds and can serve as baseline for the development of new drugs against leishmaniasis and Chagas disease. However, efforts on in vitro and in vivo toxicity studies of the active synthetic compounds is still needed. Pharmacokinetic studies, and the mechanism of action of the promising compounds need to be explored. The use of new catalysts and chemical transformation can afford unexplored halogenated compounds with improved antileishmanial and antitrypanosomal 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 Inhibition of In Vivo Growth of Plasmodium berghei by Launaea taraxacifolia and Amaranthus viridis in Mice

2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Adewale Adetutu ◽  
Olubukola S. Olorunnisola ◽  
Abiodun O. Owoade ◽  
Peter Adegbola
Keyword(s):  
Survival Time ◽  
Plasmodium Berghei ◽  
Packed Cell Volume ◽  
Haematological Parameters ◽  
Antimalarial Agents ◽  
Western Africa ◽  
Methanolic Extracts ◽  
Crude Extracts ◽  
In Vivo Growth

Launaea taraxacifolia and Amaranthus viridis used by people of Western Africa in the treatment of malaria and related symptoms were assessed for their antiplasmodial value against the chloroquine sensitive strain of Plasmodium berghei. Crude extracts (200 mg/kg) and chloroquine (5 mg/kg) were administered to different groups of Swiss mice. The percentage of parasitemia, survival time, and haematological parameters were determined. Both extracts significantly (p<0.05) inhibited parasitemia and improved survival time in infected mice. The crude extracts prevented loss of some haematological parameters. A. viridis had a distinct effect on the packed cell volume. The extract was able to protect the liver from some of the damage. This study however showed that the methanolic extracts of A. viridis and L. taraxacifolia possess antiplasmodial activity. The results of this study can be used as a basis for further phytochemical investigations in the search for new and locally affordable antimalarial agents.

scholarly journals THE EFFECTS OF ROENTGEN RAYS ON CELL-VIRUS ASSOCIATIONS

1943 ◽  
Vol 78 (4) ◽  
pp. 285-304 ◽  
Author(s):  
William F. Friedewald ◽  
Rubert S. Anderson
Keyword(s):  
X Rays ◽  
Pathological Changes ◽  
Cellular Division ◽  
Papilloma Virus ◽  
X Ray ◽  
Crude Extracts ◽  
Domestic Rabbits ◽  
Roentgen Rays

The virus-induced papillomas of cottontail as well as domestic rabbits regress completely within a few weeks when exposed to 5,000 r of x-ray irradiation. The x-rays do not immediately kill the papilloma cells, but lead to death by inhibiting cellular division and producing pathological changes in the cells which then continue to differentiate. The virus associated with the growths, however, not only persists in undiminished amount during regression, but often an increased yield of it can be obtained on extraction. The fibroma virus in crude extracts or in vivo is inactivated by far less irradiation than the papilloma virus. 10,000 r destroys 90 per cent or more of the infectivity of the fibroma virus, whereas at least 100,000 r is required to inactivate 50 per cent of the papilloma virus in extracts containing about the same amount of protein. No variant of the papilloma virus or fibroma virus has been encountered as a result of the irradiation.

scholarly journals In vivo validation of anti-malarial activity of crude extracts of Terminalia macroptera, a Malian medicinal plant

2018 ◽  
Vol 17 (1) ◽  
Author(s):  
Mahamane Haidara ◽  
Mohamed Haddad ◽  
Adama Denou ◽  
Guillaume Marti ◽  
Sandra Bourgeade-Delmas ◽  
...  
Keyword(s):  
Medicinal Plant ◽  
Crude Extracts ◽  
In Vivo Validation

scholarly journals Effect of China berry crude extracts on broad mites in vivo and in vitro

2008 ◽  
Vol 2 (1) ◽  
pp. 12-18
Author(s):  
Assma Gatta ◽  
Luaay K. Al – ani ◽  
Nabeel Al - ani
Keyword(s):  
Biological Control ◽  
Tissue Culture ◽  
Melia Azedarach ◽  
Concentration Increase ◽  
Water Extracts ◽  
Crude Extracts ◽  
Number Increase ◽  
Ethanol Extracts

Tissue culture were established from leaf and stem of china berry (Melia azedarach ) tree . Using MS media the best regulator to form callus were 6mg/l BAP, all other concentrations did not give callus . The crude extracts from leaves and callus established from leaves were extracted with water and ethanol with different concentrations. In ethanol extracts the least concentration 0.0001 half of the treated parasites were killed in 24 hours while the number increase as the concentration increase . However in callus the ethanol extracts were much higher about 8.5 were killed in the above concentration . In water extracts the least concentration 0.0001 killed half of the treated parasites in 24 hours .This number was increased 8 or 9 in 48 and 72 hours respectively . These results give us preliminary idea about the biological control of this dangerous parasite.

scholarly journals Indirubin Analogues Inhibit Trypanosoma brucei Glycogen Synthase Kinase 3 Short and T. brucei Growth

2019 ◽  
Vol 63 (6) ◽  
Author(s):  
Antonia Efstathiou ◽  
Nicolas Gaboriaud-Kolar ◽  
Vassilios Myrianthopoulos ◽  
Konstantina Vougogiannopoulou ◽  
Ines Subota ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Glycogen Synthase ◽  
Intracellular Localization ◽  
Protozoan Parasite ◽  
Glycogen Synthase Kinase ◽  
Glycogen Synthase Kinase 3 ◽  
Content Type ◽  
Antitrypanosomal Activity ◽  
Half Maximal Effective Concentration

ABSTRACT The protozoan parasite Trypanosoma brucei is the causative agent of human African trypanosomiasis (HAT). The disease is fatal if it remains untreated, whereas most drug treatments are inadequate due to high toxicity, difficulties in administration, and low central nervous system penetration. T. brucei glycogen synthase kinase 3 short (TbGSK3s) is essential for parasite survival and thus represents a potential drug target that could be exploited for HAT treatment. Indirubins, effective leishmanicidals, provide a versatile scaffold for the development of potent GSK3 inhibitors. Herein, we report on the screening of 69 indirubin analogues against T. brucei bloodstream forms. Of these, 32 compounds had potent antitrypanosomal activity (half-maximal effective concentration = 0.050 to 3.2 μM) and good selectivity for the analogues over human HepG2 cells (range, 7.4- to over 641-fold). The majority of analogues were potent inhibitors of TbGSK3s, and correlation studies for an indirubin subset, namely, the 6-bromosubstituted 3′-oxime bearing an extra bulky substituent on the 3′ oxime [(6-BIO-3′-bulky)-substituted indirubins], revealed a positive correlation between kinase inhibition and antitrypanosomal activity. Insights into this indirubin-TbGSK3s interaction were provided by structure-activity relationship studies. Comparison between 6-BIO-3′-bulky-substituted indirubin-treated parasites and parasites silenced for TbGSK3s by RNA interference suggested that the above-described compounds may target TbGSK3s in vivo. To further understand the molecular basis of the growth arrest brought about by the inhibition or ablation of TbGSK3s, we investigated the intracellular localization of TbGSK3s. TbGSK3s was present in cytoskeletal structures, including the flagellum and basal body area. Overall, these results give insights into the mode of action of 6-BIO-3′-bulky-substituted indirubins that are promising hits for antitrypanosomal drug discovery.

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