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.

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.

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 In Vitro and In Vivo Antitrypanosomal Activities of Methanol Extract of Echinops kebericho Roots

2020 ◽  
Vol 2020 ◽  
pp. 1-6
Author(s):  
Debela Abdeta ◽  
Nigatu Kebede ◽  
Mirutse Giday ◽  
Getachew Terefe ◽  
Solomon Mequanente Abay
Keyword(s):  
Body Weight ◽  
Neglected Tropical Diseases ◽  
Field Isolate ◽  
Parasite Load ◽  
Phytochemical Analysis ◽  
Isolation And Purification ◽  
Discovery Research ◽  
Drug Discovery Research

Microbial resistance to the few conventional antitrypanosomal drugs, increasing resistance of vectors to insecticides, lack of effective vaccines, and adverse effects of the existing antitrypanosomal drugs justify the urgent need for effective, tolerable, and affordable drugs. We assessed antitrypanosomal effects of the hydromethanolic extract of Echinops kebericho Mesfin roots against Trypanosoma congolense field isolate using in vitro and in vivo techniques. Parasite load, packed cell volume (PCV), body weight, and rectal temperature in Swiss albino mice were assessed. This finding is part of the outcomes of drug discovery research for neglected tropical diseases. The extract arrested the motility of trypanosomes within 40 min at 4 and 2 mg/mL concentration, whereas in the untreated control, motility continued for more than 160 min. The extract also reduced parasitemia and prevented drop in PCV and body weight significantly (p<0.05), as compared to control. Phytochemical analysis showed the presence of flavonoids, triterpenes, steroids, saponins, glycosides, tannins, and alkaloids. It is observed that this extract has activity against the parasite. Isolation and purification of specific compounds are required to identify hit compounds responsible for the antitrypanosomal activity of the studied medicinal plant.

scholarly journals Ajuga Bracteosa Transgenic Regenerants Display Better Pharmacological Potential

2021 ◽  
Author(s):  
Samina Rubnawaz ◽  
Waqas Khan Kayani ◽  
Nosheen Akhtar ◽  
Rashid Mahmood ◽  
Furrukh Mehmood ◽  
...  
Keyword(s):  
Plant Extracts ◽  
Antioxidant Activities ◽  
Reducing Power ◽  
Abnormal Behavior ◽  
Mice Model ◽  
Hydroxyl Ion ◽  
Total Antioxidant ◽  
Endangered Medicinal Herb

Abstract Ajuga bracteosa Wall. ex Benth is an endangered medicinal herb used against different ailments in folklore medicines. Here, we aimed to create a new insight to the fundamental mechanisms of genetic transformation in the ethnomedicinal usage of this plant. We transformed the plant with rol genes of Agrobacterium rhizogenes and raised the regenerants from the hairy roots. The transgenic regenerants were screened for in vitro antioxidant activities, a range of in vivo assays, and linked the activities with elemental analysis, polyphenol content and different phytochemicals found through HPLC. Among 18 polyphenolic standards, kaempferol was found most abundant in all transgenic lines (up to 101.26 ± 6 µg/mg). Furthermore, among all tested plant extracts, transgenic line 3 (ABRL3) showed maximum phenolics (13.39 ± 2µg GAE/mg) and flavonoids content (4.75 ± 0.16 µg QE/mg). ABRL3 also demonstrated potent total antioxidant capacity (8.16 ± 1 µg AAE/mg), total reducing power, (6.60 ± 1.17 µg AAE/mg), DPPH activity (IC50 = 59.5 ± 0.8µg/mL), hydroxyl ion scavenging (IC50 = 122.5 ± 0.90 µg/mL), and iron chelating power (IC50 = 154.8 ± 2 µg/mL) among all plants. Transformed plant extracts also produced significant analgesic, anti-inflammatory, anticoagulant, and antidepressant properties in in vivo mice model as compared to control untransformed plant material. Additionally, no abnormal behavior or lethality was observed in any animal tested. In conclusion, transgenic regenerants of A. bracteosa pose better pharmacological properties under the effect of rol genes as compared to wild type plants.

scholarly journals Evaluating the Antifungal Activity of Some Traditional Medicinal Plant Extracts against Alternaria solani (Tomato Early Blight Pathogen) in Ethiopia

2022 ◽  
Author(s):  
Meseret Tadelo ◽  
Tamirat Wato ◽  
Tilahun Negash
Keyword(s):  
Medicinal Plants ◽  
Plant Extracts ◽  
Early Blight ◽  
Allium Sativum ◽  
Alternaria Solani ◽  
Significant Inhibition ◽  
Crude Extracts ◽  
Medicinal Plant Extracts

Background: Tomato (Lycopersicon esculentum Mill.) belongs to the family Solanaceae. In Ethiopia, control of early blight is largely dependent on fungicidal application. There is a research need to identify effective botanical extracts to control Alternaria solani that cause early blight of tomato and for evaluation of plant extracts through different solvents on the target pathogen. Methods: In vitro experiment was conducted to evaluate the effectiveness of crude extracts of 16 selected medicinal plants against Alternaria solani. Thus, crude extracts were extracted from medicinal plants with different solvents (methanol, ethanol and petroleum at (25%, 50% and 100%) concentrations. The Alternaria solani was isolated from infected tomato leaves showing early blight symptoms. Evaluation of plant extracts was carried out against Alternaria solani using food poisoned technique on PDA. Result: Results showed that most of the methanolic extract plants were showed significant inhibition of the mycelial growth as compared to ethanolic and petroleum ether extracts. A higher rate of mycelial reduction was recorded by ethanol extracts of Allium sativum at all concentrations (100%) followed by methanol extracts of Allium sativum at 25%, 50%, 100% concentration (90.02%, 97.01%, 100% respectively). The effectiveness of extracts against Alternaria solani depends on use at the higher concentrations and various solvents. For crude extracts that have shown higher inhibitory effects against Alternaria solani in vitro conditions, actual chemical compounds should be identified. Furthermore, it is also important to evaluate these plants on other microbes, study to test in vivo and to assess their real potential field condition wherever early blight is an important disease of tomato.

scholarly journals IGFBP7 As a Potential Therapeutic Target for AML

Blood ◽  
2018 ◽  
Vol 132 (Supplement 1) ◽  
pp. 5134-5134
Author(s):  
Yina Niu ◽  
Shuiyan Wu ◽  
Shaoyan Hu
Keyword(s):  
Cell Lines ◽  
Conflicts Of Interest ◽  
Fold Increase ◽  
Dependent Manner ◽  
Mice Model ◽  
Cell Counts ◽  
And Migration ◽  
Proliferation And Migration

Abstract Insulin-like growth factor binding proteins (IGFBPs) are secretory factors that play essential roles in regulation of insulin-like growth factors (IGFs) in tissue as well as in modulating IGF binding to its receptors. IGFBP7, known as IGFBP-related protein 1 (IGFBP-rP1), mac25/angiomodulin, function as a potential tumor suppressor in various human solid cancers, including breast, prostate, gastric and liver cancer. We have reported the overexpression of IGFBP7 in the context of acute myeloid leukemia (AML), showing that IGFBP7 expression level in AML patients is significantly increased compared with controls (P<0.001). IGFBP7 expression was obviously decreased in AML patients achieving complete remission (P<0.01), and was significantly increased in relapsed AML patients (P<0.01). In addition, AML patients with high expression of IGFBP7 had shorter overall survival. Here, we investigate the role and mechanism of IGFBP7 in the development and progression of AML. In order to study the role of IGFBP7 in AML, stable cell lines expressing IGFBP7 and control in AML cells were constructed using lentiviral packaging system. Expression microarray assay was carried out to analyze the global gene level changes driven by IGFBP7. MTT and transwell assays were performed to evaluate the effect of IGFBP7 on cell proliferation and migration. Bioinformatics results found that IGFBP7 appeared to utilize multiple cellular processes for its oncogenic roles, including adhesion, migration, and proliferation. Experimental data showed overexpression of IGFBP7 in K562 cells resulted in a 2-3 fold increase in migration in contrast to control cells. Moreover, enforced expression of IGFBP7 also led to phosphorylation of Akt and Erk, whose activities inactivation by pharmacologically inhibitors resulted in the loss of ability to migrating. Finally, knockdown of IGFBP7 in cells with high IGFBP7 level, their migration abilities were significantly decreased. To assess the role of IGFBP7 in leukemogenesis in vivo, the same numbers of K562/IGFBP7 and K562-Vector cells, U937-shIGFBP7 and U937-shNEG cells were injected into NOD-SCID mice by tail vein injection, respectively. About two weeks later, it was showed that mice of K562/IGFBP7 and U937 groups displayed higher white blood cell counts compared with mice of K562-Vector and U937-shIGFBP7 groups, respectively. Mice of K562/IGFBP7 and U937 groups had more severe splenomegaly and hepatomagaly compared with its corresponding control groups. We further characterized the molecular mechanism underlying leukemogenesis driven by IGFBP7 in AML cell lines. The global expression profiling and molecular biological experiments showed PI3K/AKT signaling was activated by overexpression of IGFBP7, and knockdown of IGFBP7 in AML cells led to a decrease of PI3K/AKT activity in PTEN-dependent manner. IGFBP7 promotes proliferation and migration of AML cells, the promotion could be suppressed by both RNA interference and pharmacological inhibition of PI3K/AKT pathway. Immuno-precipitation assay showed that IGFBP7 associated with AXAN2 and induced PTEN degradation. The expression of ANXA2 was significantly positive correlated with the expression ANXA2 in AML patients. The expression of IGFBP7 in AML, overexpression as well as knockdown of IGFBP7 in leukemia cells and in mice model, all suggest that IGFBP7 is a potential proto-oncogene. Collectively this work suggests that targeting IGFBP7 activity may be an effective therapeutic strategy for AML. Disclosures No relevant conflicts of interest to declare.

scholarly journals Antiprotozoal activities of Triterpenic Acids and Ester Derivatives Isolated from the Leaves of Vitellaria paradoxa

Planta Medica ◽  
2020 ◽  
Author(s):  
Lucy Catteau ◽  
Laura Schioppa ◽  
Claire Beaufay ◽  
Cynthia Girardi ◽  
Marie-France Hérent ◽  
...  
Keyword(s):  
Shea Butter ◽  
Vitellaria Paradoxa ◽  
Mice Model ◽  
Efficacy Evaluation ◽  
Antitrypanosomal Activity ◽  
Triterpenic Acids ◽  
Low Cytotoxicity ◽  
First Time

AbstractLeaves of Vitellaria paradoxa, also called “Shea butter tree”, are used in traditional medicine to treat various symptoms including malaria fever, dysentery, or skin infections. Composition of the dichloromethane extract of V. paradoxa leaves possessing antiparasitic activities was investigated. Five pentacyclic triterpenic acids together with 6 ester derivatives were isolated and identified by standards comparison, MS and 1H-NMR analysis. Corosolic, maslinic, and tormentic coumaroyl esters and their corresponding triterpenic acids were isolated from this plant for the first time. The antiparasitic activities of the 11 isolated compounds were evaluated in vitro on Plasmodium falciparum, Trypanosoma brucei brucei, and Leishmania mexicana mexicana and their selectivity determined by cytotoxicity evaluation on WI38 cells. None of the isolated compounds showed good antiplasmodial activity. The antitrypanosomal activity of individual compounds was in general higher than their antileishmanial one. One isolated triterpenic ester mixture in equilibrium, 3-O-p-E/Z-coumaroyltormentic acids, showed an attractive promising antitrypanosomal activity (IC50 = 0.7 µM) with low cytotoxicity (IC50= 44.5 µM) compared to the corresponding acid. Acute toxicity test on this ester did not show any toxicity at the maximal cumulative dose of 100 mg/kg intraperitoneally on mice. In vivo efficacy evaluation of this compound, at 50 mg/kg by intraperitoneal route on a T. b. brucei-infected mice model, showed a significant parasitemia reduction on day 4 post-infection together with 33.3% survival improvement. Further bioavailability and PK studies are needed along with mode of action investigations to further assess the potential of this molecule.

scholarly journals In vitro and in vivo antitrypanosomal activities of Echinops kebericho root extract

2019 ◽  
Author(s):  
Debela Abdeta ◽  
Nigatu Kebede ◽  
Mirutse Giday ◽  
Getachew Terefe ◽  
Solomon Mequanente Abay
Keyword(s):  
Body Weight ◽  
Neglected Tropical Diseases ◽  
Field Isolate ◽  
Phytochemical Analysis ◽  
Root Extract ◽  
Isolation And Purification ◽  
Discovery Research ◽  
Drug Discovery Research

Abstract Objective: Microbial resistance to the few conventional antitrypanosomal drugs, increasing resistance of vectors to insecticides, lack of effective vaccines and adverse effects of the existing antitrypanosomal drugs justifies the urgent need for effective, tolerable and affordable drugs. We assessed antitrypanosomal effect of hydromethanolic extract of Echinops kebericho Mesfin roots against Trypanosoma congolense field isolate using in vitro and in vivo techniques. Parasite load, packed cell volume (PCV), body weight and rectal temperature in Swiss albino mice were assessed. This finding is part of the outcomes of drug discovery research for neglected tropical diseases. Result: The extract ceased motility of the trypanosomes within 40 min at 4 and 2 mg/ml concentration whereas in the untreated control motility continued for more than 160 min. The extract also reduced parasitemia, prevented drop in PCV and body weight significantly (p<0.05), as compared to control. Phytochemical analysis showed the presence of flavonoids, triterpines, steroids, saponins, glycosides, tannins and alkaloids. It is observed that this extract has activity against the parasite. Isolation and purification of specific compounds are required to identify hit compounds responsible for the antitrypanosomal activity of the studied medicinal plant.

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