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1

Dofuor, Aboagye Kwarteng, Temitayo Samson Ademolue, Cynthia Mmalebna Amisigo, Kwaku Kyeremeh, and Theresa Manful Gwira. "Chemical Derivatization and Characterization of Novel Antitrypanosomals for African Trypanosomiasis." Molecules 26, no. 15 (2021): 4488. http://dx.doi.org/10.3390/molecules26154488.

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The search for novel antitrypanosomals and the investigation into their mode of action remain crucial due to the toxicity and resistance of commercially available antitrypanosomal drugs. In this study, two novel antitrypanosomals, tortodofuordioxamide (compound 2) and tortodofuorpyramide (compound 3), were chemically derived from the natural N-alkylamide tortozanthoxylamide (compound 1) through structural modification. The chemical structures of these compounds were confirmed through spectrometric and spectroscopic analysis, and their in vitro efficacy and possible mechanisms of action were, s
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2

O Igoli, John, Poorna Kantheti, and Rajeev K Singla. "Antitrypanosomal Activity of Extract Fractions of Cetraria Islandica." Indo Global Journal of Pharmaceutical Sciences 02, no. 04 (2012): 348–50. http://dx.doi.org/10.35652/igjps.2012.40.

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The antitrypanosomal activity of various extract fractions of C. islandica (Iceland moss) was evaluated by using the well-established Alamar blue™ 96 well microplate assay. The antitrypanosomal activity significantly increased with increasing amounts of fractions (from 10-20 µg/ml) and MIC of 12.5µg/ml were observed for certain fractions. The results obtained in the present study indicate that C. islandica is a potential source of natural antitrypanosomal agents. © 2011 IGJPS. All rights reserved.
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3

Steverding, Dietmar, and Kevin M. Tyler. "Novel antitrypanosomal agents." Expert Opinion on Investigational Drugs 14, no. 8 (2005): 939–55. http://dx.doi.org/10.1517/13543784.14.8.939.

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4

Sealey-Cardona, Marco, Simon Cammerer, Simon Jones, et al. "Kinetic Characterization of Squalene Synthase from Trypanosoma cruzi: Selective Inhibition by Quinuclidine Derivatives." Antimicrobial Agents and Chemotherapy 51, no. 6 (2007): 2123–29. http://dx.doi.org/10.1128/aac.01454-06.

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ABSTRACT The biosynthesis of sterols is a major route for the development of antitrypanosomals. Squalene synthase (SQS) catalyzes the first step committed to the biosynthesis of sterols within the isoprenoid pathway, and several inhibitors of the enzyme have selective antitrypanosomal activity both in vivo and in vitro. The enzyme from Trypanosoma cruzi is a 404-amino-acid protein with a clearly identifiable membrane-spanning region. In an effort to generate soluble recombinant enzyme, we have expressed in Escherichia coli several truncated versions of T. cruzi SQS with a His tag attached to t
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5

Kaminsky, R., E. Zweygarth, and E. De Clercq. "Antitrypanosomal Activity of Phosphonylmethoxyalkylpurines." Journal of Parasitology 80, no. 6 (1994): 1026. http://dx.doi.org/10.2307/3283453.

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6

Nenortas, Elizabeth, Christian Burri, and Theresa A. Shapiro. "Antitrypanosomal Activity of Fluoroquinolones." Antimicrobial Agents and Chemotherapy 43, no. 8 (1999): 2066–68. http://dx.doi.org/10.1128/aac.43.8.2066.

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ABSTRACT Six fluoroquinolones presently in clinical use and four investigational tetracyclic fluoroquinolones were tested for in vitro activity against bloodstream-form Trypanosoma brucei brucei. All compounds had measurable activity, but the tetracyclic analogs were most potent, with 50% effective concentrations in the low micromolar range. In general, trypanosomes were more susceptible than L1210 leukemia cells. Consistent with the notion that they target type II topoisomerase in trypanosomes, the fluoroquinolones promote the formation of protein-DNA covalent complexes.
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7

Scovill, John, Elizabeth Blank, Michael Konnick, Elizabeth Nenortas, and Theresa Shapiro. "Antitrypanosomal Activities of Tryptanthrins." Antimicrobial Agents and Chemotherapy 46, no. 3 (2002): 882–83. http://dx.doi.org/10.1128/aac.46.3.882-883.2002.

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ABSTRACT New drugs and molecular targets are needed against Trypanosoma brucei, the protozoan that causes African sleeping sickness. Tryptanthrin (indolo[2,1-b]quinazoline-6,12-dione), a traditional antifungal agent, and 11 analogs were tested against T. brucei in vitro. The greatest activity was conferred by electron-withdrawing groups in the 8 position of the tryptanthrin ring system; the most potent compound had a 50% effective concentration of 0.40 μM.
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8

Abdeta, Debela, Nigatu Kebede, Mirutse Giday, Getachew Terefe, and Solomon Mequanente Abay. "In Vitro and In Vivo Antitrypanosomal Activities of Methanol Extract of Echinops kebericho Roots." Evidence-Based Complementary and Alternative Medicine 2020 (September 22, 2020): 1–6. http://dx.doi.org/10.1155/2020/8146756.

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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 o
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9

Jesumoroti, Omobolanle J., Richard M. Beteck, and Lesetja J. Legoabe. "In-vitro Anti-trypanosomal and Cytotoxicity Evaluation of 3-methyl-3,4-dihydroquinazolin-2(1H)-one Derivatives." Drug Research 71, no. 06 (2021): 335–40. http://dx.doi.org/10.1055/a-1349-1256.

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Sleeping sickness, caused by trypanosomes, is a debilitating, neglected tropical disease wherein current treatments suffer from several drawbacks such as toxicity, low activity, and poor pharmacokinetic properties, and hence the need for alternative treatment is apparent. To this effect, we screened in vitro a library of 2-quinazolinone derivatives for antitrypanosomal activity against T.b. brucei and cytotoxicity against HeLa cells. Seven compounds having no overt cytotoxicity against HeLa cells exhibited antitrypanosomal activity in the range of 0.093–45 µM were identified. The activity data
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10

Nyunt, Khine Swe, Ahmed Elkhateeb, Yusuke Tosa, Kensuke Nabata, Ken Katakura, and Hideyuki Matsuura. "Isolation of Antitrypanosomal Compounds from Vitis repens, a Medicinal Plant of Myanmar." Natural Product Communications 7, no. 5 (2012): 1934578X1200700. http://dx.doi.org/10.1177/1934578x1200700516.

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Bioactivity-guided fractionation of an ethanolic extract of Vitis repens led to the isolation of resveratrol (1), 11- O-acetyl bergenin (2), and stigmast-4-en-3-one (3). The compounds were examined for their in vitro antitrypanosomal activities against trypomastigotes of Trypanosoma evansi. Resveratrol showed antitrypanosomal activity with an IC50 value of 0.13 μM, whereas 11- O-acetyl bergenin and stigmast-4-en-3-one exhibited IC50 values of 0.17 and 0.15 μM, respectively.
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11

Begolo, Daniela, Esteban Erben, and Christine Clayton. "Drug Target Identification Using a Trypanosome Overexpression Library." Antimicrobial Agents and Chemotherapy 58, no. 10 (2014): 6260–64. http://dx.doi.org/10.1128/aac.03338-14.

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ABSTRACTElucidation of molecular targets is very important for lead optimization during the drug development process. We describe a direct method to find targets of antitrypanosomal compounds againstTrypanosoma bruceiusing a trypanosome overexpression library. As proof of concept, we treated the library with difluoromethylornithine and DDD85646 and identified their respective targets, ornithine decarboxylase andN-myristoyltransferase. The overexpression library could be a useful tool to study the modes of action of novel antitrypanosomal drug candidates.
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12

Dofuor, Aboagye Kwarteng, Frederick Ayertey, Peter Bolah, et al. "Isolation and Antitrypanosomal Characterization of Furoquinoline and Oxylipin from Zanthoxylum zanthoxyloides." Biomolecules 10, no. 12 (2020): 1670. http://dx.doi.org/10.3390/biom10121670.

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In the absence of vaccines, there is a need for alternative sources of effective chemotherapy for African trypanosomiasis (AT). The increasing rate of resistance and toxicity of commercially available antitrypanosomal drugs also necessitates an investigation into the mode of action of new antitrypanosomals for AT. In this study, furoquinoline 4, 7, 8-trimethoxyfuro (2, 3-b) quinoline (compound 1) and oxylipin 9-oxo-10, 12-octadecadienoic acid (compound 2) were isolated from the plant species Zanthoxylum zanthoxyloides (Lam) Zepern and Timler (root), and their in vitro efficacy and mechanisms o
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13

Singh, Nidhi, Priyanka Shah, Hemlata Dwivedi, et al. "Integrated machine learning, molecular docking and 3D-QSAR based approach for identification of potential inhibitors of trypanosomal N-myristoyltransferase." Molecular BioSystems 12, no. 12 (2016): 3711–23. http://dx.doi.org/10.1039/c6mb00574h.

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14

Londero, Vinicius S., Thais A. Costa-Silva, Guilherme M. Antar, et al. "Antitrypanosomal Lactones from Nectandra barbellata." Journal of Natural Products 84, no. 5 (2021): 1489–97. http://dx.doi.org/10.1021/acs.jnatprod.0c01303.

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15

Croft, Simon L. "Pharmacological Approaches to Antitrypanosomal Chemotherapy." Memórias do Instituto Oswaldo Cruz 94, no. 2 (1999): 215–20. http://dx.doi.org/10.1590/s0074-02761999000200017.

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16

Nkemgu-Njinkeng, Joseph, Vera Rosenkranz, Michael Wink, and Dietmar Steverding. "Antitrypanosomal Activities of Proteasome Inhibitors." Antimicrobial Agents and Chemotherapy 46, no. 6 (2002): 2038–40. http://dx.doi.org/10.1128/aac.46.6.2038-2040.2002.

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ABSTRACT Seven peptidyl proteasome inhibitors were tested for in vitro activity against Trypanosoma brucei bloodstream forms. Two compounds showed activity in the low nanomolar range. In general, trypanosomes were more susceptible to the compounds than were human HL-60 cells. The data support the potential of proteasome inhibitors for rational antitrypanosomal drug development.
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17

Croft, Simon L., Eric Chatelain, and Michael P. Barrett. "Antileishmanial and antitrypanosomal drug identification." Emerging Topics in Life Sciences 1, no. 6 (2017): 613–20. http://dx.doi.org/10.1042/etls20170103.

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Although the treatments for human African trypanosomiasis (HAT), leishmaniasis and Chagas disease (CD) still rely on drugs developed several decades ago, there has been significant progress in the identification, development and use of novel drugs and formulations. Notably, there are now two drugs in clinical trial for HAT, fexinidazole and acoziborole; the liposomal amphotericin B formulation AmBisome has become an essential tool for both treatment and control of visceral leishmaniasis; and antifungal triazoles, posoconazole and ravuconazole, together with fexinidazole, have reached clinical
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18

Nkemngu, Njinkeng Joseph, Vera Rosenkranz, Michael Wink, and Dietmar Steverding. "Antitrypanosomal Activities of Proteasome Inhibitors." Antimicrobial Agents and Chemotherapy 47, no. 9 (2003): 3036. http://dx.doi.org/10.1128/aac.47.9.3036.2003.

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19

Issa, Victor Sarli, and Edimar Alcides Bocchi. "Antitrypanosomal agents: treatment or threat?" Lancet 376, no. 9743 (2010): 768. http://dx.doi.org/10.1016/s0140-6736(10)61372-4.

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20

Nnadi, CO, J. Nwodo Ngozi, R. Brun, M. Kaiser, and TJ Schmidt. "Antitrypanosomal alkaloids from Holarrhena africana." Planta Medica 81, S 01 (2016): S1—S381. http://dx.doi.org/10.1055/s-0036-1596866.

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21

Bodley, Annette L., Mansukh C. Wani, Monroe E. Wall, and Theresa A. Shapiro. "Antitrypanosomal activity of camptothecin analogs." Biochemical Pharmacology 50, no. 7 (1995): 937–42. http://dx.doi.org/10.1016/0006-2952(95)00215-l.

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22

Schmidt, Ines, Sarah Göllner, Antje Fuß, et al. "Bistacrines as potential antitrypanosomal agents." Bioorganic & Medicinal Chemistry 25, no. 16 (2017): 4526–31. http://dx.doi.org/10.1016/j.bmc.2017.06.051.

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23

Çalış, İhsan, Semra Koyunoğlu, Akgül Yeşilada, Reto Brun, Peter Rüedi, and Deniz Taşdemir. "Antitrypanosomal Cycloartane Glycosides fromAstragalus baibutensis." Chemistry & Biodiversity 3, no. 8 (2006): 923–29. http://dx.doi.org/10.1002/cbdv.200690094.

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24

Dofuor, Aboagye Kwarteng, Emmanuel Kofi Kumatia, Jersley Didewurah Chirawurah, and Frederick Ayertey. "Antiplasmodial, Antitrypanosomal, and Cytotoxic Effects of Anthonotha macrophylla, Annickia polycarpa, Tieghemella heckelii, and Antrocaryon micraster Extracts." Advances in Pharmacological and Pharmaceutical Sciences 2022 (July 23, 2022): 1–7. http://dx.doi.org/10.1155/2022/9195753.

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Malaria and trypanosomiasis are protozoan diseases which pose a devastating challenge to human health and productivity especially, in Africa where their respective vectors (female Anopheles mosquito and tsetse fly) abound. Various medicinal plants are used to treat these parasitic diseases. However, the scientific basis of their use and toxicological profiles have not been assessed. We have, therefore, evaluated the antiplasmodial, antitrypanosomal, and cytotoxic activities of four African medicinal plant extracts namely, Anthonotha macrophylla leaf (AML), Annickia polycarpa leaf (APLE), Tiegh
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25

Dize, Darline, Rolland Bantar Tata, Rodrigue Keumoe, et al. "Preliminary Structure–Activity Relationship Study of the MMV Pathogen Box Compound MMV675968 (2,4-Diaminoquinazoline) Unveils Novel Inhibitors of Trypanosoma brucei brucei." Molecules 27, no. 19 (2022): 6574. http://dx.doi.org/10.3390/molecules27196574.

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New drugs are urgently needed for the treatment of human African trypanosomiasis (HAT). In line with our quest for novel inhibitors of trypanosomes, a small library of analogs of the antitrypanosomal hit (MMV675968) available at MMV as solid materials was screened for antitrypanosomal activity. In silico exploration of two potent antitrypanosomal structural analogs (7-MMV1578647 and 10-MMV1578445) as inhibitors of dihydrofolate reductase (DHFR) was achieved, together with elucidation of other antitrypanosomal modes of action. In addition, they were assessed in vitro for tentative inhibition of
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Afolayan, Michael Olalekan, Sarah Abimbola Akande, and Blessing Sunday. "Assessment of Antimicrobial, Antimalarial, and Antitrypanosomal Activities of Crude Extracts and Fractions from Piliostigma thonningii Schum. Leaves in Vitro." Journal of Biochemicals and Phytomedicine 3, no. 1 (2024): 46–52. https://doi.org/10.34172/jbp.2024.10.

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Introduction: The plant Piliostigma thonningii (Milne-Redhead, Fabaceae) has been traditionally used as a medicinal remedy in several African countries. This study aimed to investigate and validate the antimalarial, antitrypanosomal, and antimicrobial potential of the crude methanolic extract and fractions of P. thonningii leaves through in vitro assays. Methods: Cold maceration of dried P. thonningii leaves in methanol produced crude extracts, which were then fractionated into dichloromethane (DCM), ethyl acetate (EtOAc), and butanol (BuOH) fractions. The extracts and fractions were subsequen
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Dofuor, Aboagye Kwarteng, Temitayo Samson Ademolue, Karen Nana Akua Kuampah, Frederick Ayertey, and Theresa Manful Gwira. "In Vitro Mechanism of Action of Acanthospermum hispidum in Trypanosoma brucei." Advances in Pharmacological and Pharmaceutical Sciences 2022 (October 18, 2022): 1–9. http://dx.doi.org/10.1155/2022/1645653.

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African trypanosomiasis is a major neglected tropical disease with significant health and economic concerns in sub-Saharan Africa. In the absence of vaccines for African trypanosomiasis, there is a consideration for alternative sources of chemotherapy. Acanthospermum hispidum DC (A. hispidum) is a herbal species of the Asteraceae family that is endowed with rich phytochemicals with unknown mechanisms of antitrypanosomal effects. This study aimed to investigate the cellular mechanisms of antitrypanosomal and antioxidant activities of A. hispidum against Trypanosoma brucei (T. brucei), a causati
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Llurba Montesino, Núria, Marcel Kaiser, Pascal Mäser, and Thomas J. Schmidt. "Salvia officinalis L.: Antitrypanosomal Activity and Active Constituents against Trypanosoma brucei rhodesiense." Molecules 26, no. 11 (2021): 3226. http://dx.doi.org/10.3390/molecules26113226.

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As part of our studies on antiprotozoal activity of approved herbal medicinal products, we previously found that a commercial tincture from Salvia officinalis L. (common Sage, Lamiaceae) possesses high activity against Trypanosoma brucei rhodesiense (Tbr), causative agent of East African Human Trypanosomiasis. We have now investigated in detail the antitrypanosomal constituents of this preparation. A variety of fractions were tested for antitrypanosomal activity and analyzed by UHPLC/+ESI QqTOF MS. The resulting data were used to generate a partial least squares (PLS) regression model that hig
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Waleguele, Christine C., Brice M. Mba’ning, Angelbert F. Awantu, et al. "Antiparasitic Constituents of Beilschmiedia louisii and Beilschmiedia obscura and Some Semisynthetic Derivatives (Lauraceae)." Molecules 25, no. 12 (2020): 2862. http://dx.doi.org/10.3390/molecules25122862.

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The MeOH/CH2Cl2 (1:1) extracts of the roots and leaves of Beilschmiedia louisii and B. obscura showed potent antitrypanosomal activity during preliminary screening on Trypanosoma brucei brucei. Phytochemical investigation of these extracts led to the isolation of a mixture of two new endiandric acid derivatives beilschmiedol B (1) and beilschmiedol C (2), and one new phenylalkene obscurene A (3) together with twelve known compounds (4–15). In addition, four new derivatives (11a–11d) were synthesized from compound 11. Their structures were elucidated based on their NMR and MS data. Compounds 5,
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30

Abdulkadir, Y. Sadiq, S. Bilbis1 Lawal, Andrew Onu, and Yusuf Hassan. "Synthesis and in vitro anti-trypanosomal activity of Vanillic Acid and Para- Hydroxybenzoic Acid on T. congolense." Pharmaceutical and Chemical Journal 8, no. 3 (2021): 77–85. https://doi.org/10.5281/zenodo.13962835.

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The reported toxicities of antitrypanosomal drugs and the emergence of drug resistant trypanosomes underscore the need for the development of new antitrypanosomal agents. We report herein the synthesis of phenolic acid derivatives (vanillic acid and <em>para</em>-hydroxybenzoic acid) and their antitrypanosomal potential against <em>Trypanosoma congolense</em>. The compounds were synthesized by oxidizing the aldehyde functional groups (-CHO) in the starting materials to the corresponding carboxylic acids (-CO<sub>2</sub>H) using Jones reagent and were then characterized by FTIR. <em>In vitro</e
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31

Abdeta, Debela, Solomon Mequanente Abay, Mirutse Giday, Nigatu Kebede, and Getechew Terefe. "Antitrypanosomal Effect of Hydromethanolic Extract of Solanum anguivi Lam on Field Isolates of Trypanosoma congolense Infected Mice." Journal of Parasitology Research 2021 (December 29, 2021): 1–8. http://dx.doi.org/10.1155/2021/1239379.

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Introduction. Trypanosomiasis is one of the world’s most serious infectious diseases caused by Trypanosoma parasites. Concern about resistance to conventional antitrypanosomal drugs, mosquito vector resistance to existing insecticide side effects of existing antitrypanosomal drugs justifies the urgent need for more effective, tolerable, and affordable drugs. Objective. The present study is aimed at determining the in vivo antitrypanosomal effect of the hydromethanolic extracts of Solanum anguivi fruit extracts against the field isolates of T. congolense. Methods. The 80% methanol extracts of S
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32

Chama, Mary Anti, Beverly Egyir, Kofi Baffour-Awuah Owusu, Jessica Asomaniwaa Armah, Michael Afiadenyo, and Samuel Kojo Kwofie. "Evaluation of the Antitrypanosomal Activity of the Crude Extracts of Uvaria Ovata: In vitro and In silico Approach." Biomedical and Biotechnology Research Journal 8, no. 2 (2024): 172–80. http://dx.doi.org/10.4103/bbrj.bbrj_11_24.

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Abstract Background: Human African trypanosomiasis is the third disease with most mortalities among the neglected tropical diseases. The absence of vaccines and the development of parasite resistance have necessitated the quest for new affordable and safe treatment options for the disease. This study aims to assess the potential of Uvaria ovata as an alternative new and safer antitrypanosomal therapeutics. Methods: Antitrypanosomal efficacies of extracts and fractions of U. ovata were determined by the Alamar Blue cell viability assay against Trypanosoma brucei brucei GUTat 3.1. Molecular dock
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Sufrin, J. R., D. Rattendi, A. J. Spiess, S. Lane, C. J. Marasco, and C. J. Bacchi. "Antitrypanosomal activity of purine nucleosides can be enhanced by their conversion to O-acetylated derivatives." Antimicrobial Agents and Chemotherapy 40, no. 11 (1996): 2567–72. http://dx.doi.org/10.1128/aac.40.11.2567.

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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 &gt; 100 microM), whether they were O acetylated or unacetylated; three nucleosides showed almost equal activity (IC50s of &lt; 5 microM) for the parent compound and the O-acetylate
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34

Chukwu, Ifeoma L., Malachy C. Ugwu, Ifeanyi R. Iroha, Ikechukwu S. Mbagwu, Ugochukwu U. Okafor, and Amara A. Ajaghaku. "Antitrypanosomal activity of Argemone mexicana extract and fractions in the animal model of Trypanosoma brucei brucei infection." Open Veterinary Science 3, no. 1 (2022): 20–34. http://dx.doi.org/10.1515/ovs-2022-0114.

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Abstract Background This study investigated the antitrypanosomal activity of Argemone mexicana extract and fractions in the animal model of Trypanosoma brucei brucei infection. Methods The whole plant was cold-macerated with methanol. The liquid–liquid partitioning of the extract with n-hexane, ethyl acetate, butanol, and water produced various fractions of the extract. Infection was established by the inoculation of T. brucei brucei-infected red blood cells in the animals. Treatment with the extract and fractions was done orally for 5 days postinfection at 200 and 400 mg/kg doses. Diminazene
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35

Hegazy, Mostafa M., Wael M. Afifi, Ahmed M. Metwaly, et al. "Antitrypanosomal, Antitopoisomerase-I, and Cytotoxic Biological Evaluation of Some African Plants Belonging to Crassulaceae; Chemical Profiling of Extract Using UHPLC/QTOF-MS/MS." Molecules 27, no. 24 (2022): 8809. http://dx.doi.org/10.3390/molecules27248809.

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In our continuous study for some African plants as a source for antitrypanosomally and cytotoxic active drugs, nine different plants belonging to the Crassulaceae family have been selected for the present study. Sedum sieboldii leaves extract showed an antitrypanosomal activity against Trypanosoma brucei with an IC50 value of 8.5 µg/mL. In addition, they have cytotoxic activities against (HCT-116), (HEPG-2) and (MCF-7), with IC50 values of 28.18 ± 0.24, 22.05 ± 0.66, and 26.47 ± 0.85 µg/mL, respectively. Furthermore, the extract displayed inhibition against Topoisomerase-1 with an IC50 value o
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36

Abubakar, Abdulazeez, Benjamin C. Onusiriuka, Abdullahi I. Alhaji, and Godson Ofobuike Eze. "Antitrypanosomal effect of ethanolic stem extract of Cassytha filiformis on Trypanosoma congolense infection in albino mice." Journal of Animal Science and Veterinary Medicine 10, no. 2 (2025): 185–96. https://doi.org/10.31248/jasvm2025.550.

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African trypanosomiasis is a parasitic infection caused by single-celled protozoan parasites of the genus Trypanosoma that is primarily transmitted by the bite of infected tsetse flies. This study aimed to investigate the antitrypanosomal effect of ethanolic stem extract of Cassytha filiformis on Trypanosoma congolense infection in albino mice. Crude extract of the plant was obtained by maceration in absolute ethanol, its phytochemical and acute toxicity studies were carried out following standard procedures. Thereafter, the antitrypanosomal effect of the extract was investigated in albino mic
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37

Githua, Mercy, and Ahmed Hassanali. "Antitrypanosomal Tetranotriterpenoids from Toona ciliata roots." Agriculture and Biology Journal of North America 2, no. 7 (2011): 1042–47. http://dx.doi.org/10.5251/abjna.2011.2.7.1042.1047.

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38

Bern, Caryn. "Antitrypanosomal Therapy for Chronic Chagas' Disease." New England Journal of Medicine 364, no. 26 (2011): 2527–34. http://dx.doi.org/10.1056/nejmct1014204.

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39

Muth, Mathias, Verena Hoerr, Melanie Glaser, et al. "Antitrypanosomal activity of quaternary naphthalimide derivatives." Bioorganic & Medicinal Chemistry Letters 17, no. 6 (2007): 1590–93. http://dx.doi.org/10.1016/j.bmcl.2006.12.088.

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Julianti, Tasqiah, Yoshie Hata, Stefanie Zimmermann, Marcel Kaiser, Matthias Hamburger, and Michael Adams. "Antitrypanosomal sesquiterpene lactones from Saussurea costus." Fitoterapia 82, no. 7 (2011): 955–59. http://dx.doi.org/10.1016/j.fitote.2011.05.010.

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Hata, Yoshie, Samad Nejad Ebrahimi, Maria De Mieri, et al. "Antitrypanosomal isoflavan quinones from Abrus precatorius." Fitoterapia 93 (March 2014): 81–87. http://dx.doi.org/10.1016/j.fitote.2013.12.015.

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42

Ryczak, Jasmin, Ma'ayan Papini, Annette Lader, et al. "2-Arylpaullones are selective antitrypanosomal agents." European Journal of Medicinal Chemistry 64 (June 2013): 396–400. http://dx.doi.org/10.1016/j.ejmech.2013.03.065.

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43

Tukulula, Matshawandile, Stefan Louw, Mathew Njoroge, and Kelly Chibale. "Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles." Molecules 25, no. 24 (2020): 5941. http://dx.doi.org/10.3390/molecules25245941.

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A second generation of 4-aminoquinoline- and 8-aminoquinoline-based tetrazoles and lactams were synthesized via the Staudinger and Ugi multicomponent reactions. These compounds were subsequently evaluated in vitro for their potential antiplasmodium activity against a multidrug-resistant K1 strain and for their antitrypanosomal activity against a cultured T. b. rhodesiense STIB900 strain. Several of these compounds (4a–g) displayed good antiplasmodium activities (IC50 = 0.20–0.62 µM) that were comparable to the reference drugs, while their antitrypanosomal activity was moderate (&lt;20 µM). Com
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Tlhapi, Dorcas B., Isaiah D. I. Ramaite, Chinedu P. Anokwuru, Teunis van Ree, and Heinrich C. Hoppe. "In Vitro Studies on Antioxidant and Anti-Parasitic Activities of Compounds Isolated from Rauvolfia caffra Sond." Molecules 25, no. 17 (2020): 3781. http://dx.doi.org/10.3390/molecules25173781.

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As part of an ongoing study of natural products from local medicinal plants, the methanol extract of stem bark of Rauvolfia caffra Sond was investigated for biological activity. Column chromatography and preparative thin-layer chromatography were used to isolate lupeol (1), raucaffricine (2), N-methylsarpagine (3), and spegatrine (4). The crude extract, fractions and isolated compounds were tested for anti-oxidant, antitrypanosomal and anti-proliferation activities. Two fractions displayed high DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging activity and reducing power with IC50 (
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Wahab Obeng, Ahmed, Yaw Duah Boakye, Theresa Appiah Agana, et al. "Antitrypanosomal and Anthelminthic Properties of Ethanol Extracts of Carica papaya Linn. and Ceiba pentandra (L) Gaertn." Journal of Chemistry 2022 (June 13, 2022): 1–11. http://dx.doi.org/10.1155/2022/5251930.

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The most common diseases that affect low-income countries are helminthosis and trypanosomosis. In Ghana, and in many other African countries, herbal treatment of various diseases is still common. In the present study, we sought to determine the antitrypanosomal and anthelminthic activities of Carica papaya and Ceiba pentandra. The ethanol extracts of Carica papaya stem bark (PPSe) and leaves (PPLe) and ethanol extracts of Ceiba pentandra stem bark (CPSe) and leaves (CPLe) were screened against Trypanosoma brucei brucei and Pheretima posthuma worms in vitro. CPSe exhibited strong antitrypanosom
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46

Okaiyeto, Kunle, and Anthony I. Okoh. "In Vitro Assessment of Antiplasmodial and Antitrypanosomal Activities of Chloroform, Ethyl Acetate and Ethanol Leaf Extracts of Oedera genistifolia." Applied Sciences 10, no. 19 (2020): 6987. http://dx.doi.org/10.3390/app10196987.

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The high resistance evolution of protozoans to the existing antiparasitic drugs has necessitated the quest for novel and effective drugs against plasmodium and trypanosome parasites. As a result, this study aimed to assess the antiplasmodial and antitrypanosomal potentials of chloroform, ethyl acetate and ethanol leaf extracts of Oedera genistifolia. Standard biochemical procedures were explored for the plant extraction and gas chromatography-mass spectroscopy (GCMS) was used to identify the bioactive compounds in the crude extracts. The cytotoxic effects of the crude extracts were assessed ag
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Gamaleldin, Noha M., Walid Bakeer, Ahmed M. Sayed, et al. "Exploration of Chemical Diversity and Antitrypanosomal Activity of Some Red Sea-Derived Actinomycetes Using the OSMAC Approach Supported by LC-MS-Based Metabolomics and Molecular Modelling." Antibiotics 9, no. 9 (2020): 629. http://dx.doi.org/10.3390/antibiotics9090629.

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In the present study, we investigated the actinomycetes associated with the Red Sea-derived soft coral Sarcophyton glaucum in terms of biological and chemical diversity. Three strains were cultivated and identified to be members of genera Micromonospora, Streptomyces, and Nocardiopsis; out of them, Micromonospora sp. UR17 was putatively characterized as a new species. In order to explore the chemical diversity of these actinobacteria as far as possible, they were subjected to a series of fermentation experiments under altering conditions, that is, solid and liquid fermentation along with co-fe
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Bamidele, Osho Innocent, and Durojaye Catherine Olusunmibola. "In vitro and in vivo Antitrypanosomal Activities of Annona muricata Leaf Extracts in Trypanosoma brucei brucei Experimentally Infected Albino Rats." International Journal of TROPICAL DISEASE & Health 44, no. 8 (2023): 23–32. http://dx.doi.org/10.9734/ijtdh/2023/v44i81424.

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Aims: Trypanosomiasis is an important protozoan disease that affects domestic and wild animals as well as man. It is caused by the tsetse fly-transmitted extracellular hemo-flagellates that belong to the genus, Trypanosoma. In East and Southern Africa, Human African Trypanosomiasis (HAT) is caused by Trypanosoma brucei rhodesiense while in West and Central Africa, it is caused by T. b. gambiense. Animal trypanosomiasis on the other hand is caused by T. b. brucei, T. vivax, and T. congolense. In sub-Saharan Africa, about sixty million people are at risk of infection. This current study evaluate
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Madaki, Fatima, Adamu Kabiru, Ogunrombi Clinton, Sakariyau Waheed, and Yunusa Ibrahim. "Evaluating the influence of Trypanosomiasis on murine model using Corchorus olitorius leaf extract as a trypanocidal agent." Bulletin of Natural Sciences Research, no. 00 (2024): 14. http://dx.doi.org/10.5937/bnsr14-51999.

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Trypanosomiasis, a parasitic disease caused by trypanosomes, which are flagellate protozoa transmitted through the bite of the tsetse fly, manifests with symptoms including substantial weight loss, anemia, fever, edema, adenitis, dermatitis, and nervous disorders. This research investigated the impact of trypanosomiasis on a murine model while utilizing Corchorus olitorius leaf extract as a potential trypanocidal agent. An acute toxicity analysis was conducted following Lorke's method, and the antitrypanosomal efficacy was assessed in rats at doses of 100, 200, and 400 mg/kg over three weeks,
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Alanazi, Samyah. "Antineoplastic and Antitrypanosomal Properties of Propolis from Tetragonula biroi Friese." Molecules 27, no. 21 (2022): 7463. http://dx.doi.org/10.3390/molecules27217463.

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Propolis, popularly known as bee glue, is a resinous, sticky substance produced by different bee species across the globe. Studies on the biological properties of propolis from the Philippines are rare. Hence, the current study aims at the chemical characterization of propolis produced by the stingless bees Tetragonula biroi Friese from the Philippines and to investigate its antitrypanosomal and anticancer properties. The determination of the chemical composition and characterization of propolis samples was achieved using liquid chromatography–mass spectrometry (LC-MS), -high-performance liqui
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