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Journal articles on the topic 'Antitrypanosomal'

Author: Grafiati

Published: 4 June 2021

Last updated: 13 February 2022

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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 (July 25, 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, subsequently, investigated in Trypanosoma brucei (T. brucei), one of the causative species of African trypanosomiasis (AT). The novel compounds 2 and 3 displayed significant antitrypanosomal potencies in terms of half-maximal effective concentrations (EC50) and selectivity indices (SI) (compound 1, EC50 = 7.3 μM, SI = 29.5; compound 2, EC50 = 3.2 μM, SI = 91.3; compound 3, EC50 = 4.5 μM, SI = 69.9). Microscopic analysis indicated that at the EC50 values, the compounds resulted in the coiling and clumping of parasite subpopulations without significantly affecting the normal ratio of nuclei to kinetoplasts. In contrast to the animal antitrypanosomal drug diminazene, compounds 1, 2 and 3 exhibited antioxidant absorbance properties comparable to the standard antioxidant Trolox (Trolox, 0.11 A; diminazene, 0.50 A; compound 1, 0.10 A; compound 2, 0.09 A; compound 3, 0.11 A). The analysis of growth kinetics suggested that the compounds exhibited a relatively gradual but consistent growth inhibition of T. brucei at different concentrations. The results suggest that further pharmacological optimization of compounds 2 and 3 may facilitate their development into novel AT chemotherapy.

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2

Steverding, Dietmar, and Kevin M. Tyler. "Novel antitrypanosomal agents." Expert Opinion on Investigational Drugs 14, no. 8 (July 29, 2005): 939–55. http://dx.doi.org/10.1517/13543784.14.8.939.

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3

Sealey-Cardona, Marco, Simon Cammerer, Simon Jones, Luis M. Ruiz-Pérez, Reto Brun, Ian H. Gilbert, Julio A. Urbina, and Dolores González-Pacanowska. "Kinetic Characterization of Squalene Synthase from Trypanosoma cruzi: Selective Inhibition by Quinuclidine Derivatives." Antimicrobial Agents and Chemotherapy 51, no. 6 (March 19, 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 the amino terminus. Deletions of both the amino- and carboxyl-terminal regions generated active and soluble forms of the enzyme. The highest levels of soluble protein were achieved when 24 and 36 amino acids were eliminated from the amino and carboxyl regions, respectively, yielding a protein of 41.67 kDa. The Michaelis-Menten constants of the purified enzyme for farnesyl diphosphate and NAD (NADPH) were 5.25 and 23.34 μM, respectively, whereas the V max was 1,428.56 nmol min−1mg−1. Several quinuclidine derivatives with antiprotozoal activity in vitro were found to be selective inhibitors of recombinant T. cruzi SQS in comparative assays with the human enzyme, with 50% inhibitory concentration values in the nanomolar range. These data suggest that selective inhibition of T. cruzi SQS may be an efficient strategy for the development of new antitrypanosomal agents.

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4

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

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5

Nenortas, Elizabeth, Christian Burri, and Theresa A. Shapiro. "Antitrypanosomal Activity of Fluoroquinolones." Antimicrobial Agents and Chemotherapy 43, no. 8 (August 1, 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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6

Scovill, John, Elizabeth Blank, Michael Konnick, Elizabeth Nenortas, and Theresa Shapiro. "Antitrypanosomal Activities of Tryptanthrins." Antimicrobial Agents and Chemotherapy 46, no. 3 (March 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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7

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 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.

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8

Dofuor, Aboagye Kwarteng, Frederick Ayertey, Peter Bolah, Georgina Isabella Djameh, Kwaku Kyeremeh, Mitsuko Ohashi, Laud Kenneth Okine, and Theresa Manful Gwira. "Isolation and Antitrypanosomal Characterization of Furoquinoline and Oxylipin from Zanthoxylum zanthoxyloides." Biomolecules 10, no. 12 (December 13, 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 of action investigated in Trypanosoma brucei (T. brucei), the species responsible for AT. Both compounds resulted in a selectively significant growth inhibition of T. brucei (compound 1, half-maximal effective concentration EC50 = 1.7 μM, selectivity indices SI = 74.9; compound 2, EC50 = 1.2 μM, SI = 107.3). With regards to effect on the cell cycle phases of T. brucei, only compound 1 significantly arrested the second growth-mitotic (G2-M) phase progression even though G2-M and DNA replication (S) phase arrest resulted in the overall reduction of T. brucei cells in G0-G1 for both compounds. Moreover, both compounds resulted in the aggregation and distortion of the elongated slender morphology of T. brucei. Analysis of antioxidant potential revealed that at their minimum and maximum concentrations, the compounds exhibited significant oxidative activities in T. brucei (compound 1, 22.7 μM Trolox equivalent (TE), 221.2 μM TE; compound 2, 15.0 μM TE, 297.7 μM TE). Analysis of growth kinetics also showed that compound 1 exhibited a relatively consistent growth inhibition of T. brucei at different concentrations as compared to compound 2. The results suggest that compounds 1 and 2 are promising antitrypanosomals with the potential for further development into novel AT chemotherapy.

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9

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

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10

Nkemgu-Njinkeng, Joseph, Vera Rosenkranz, Michael Wink, and Dietmar Steverding. "Antitrypanosomal Activities of Proteasome Inhibitors." Antimicrobial Agents and Chemotherapy 46, no. 6 (June 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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11

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

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12

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

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13

Nnadi, CO, J. Nwodo Ngozi, R. Brun, M. Kaiser, and TJ Schmidt. "Antitrypanosomal alkaloids from Holarrhena africana." Planta Medica 81, S 01 (December 14, 2016): S1—S381. http://dx.doi.org/10.1055/s-0036-1596866.

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14

Croft, Simon L., Eric Chatelain, and Michael P. Barrett. "Antileishmanial and antitrypanosomal drug identification." Emerging Topics in Life Sciences 1, no. 6 (December 22, 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 trials for CD. Several other novel and diverse candidates are moving through the pipeline; sustained funding for their clinical development will now be the key to bring new safe, oral, shorter-course treatments to the clinic.

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15

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

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16

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

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17

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

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18

Londero, Vinicius S., Thais A. Costa-Silva, Guilherme M. Antar, João B. Baitello, Larissa V. F. de Oliveira, Fernanda F. Camilo, Andrea N. L. Batista, Joao M. Batista, Andre G. Tempone, and Joao Henrique G. Lago. "Antitrypanosomal Lactones from Nectandra barbellata." Journal of Natural Products 84, no. 5 (April 15, 2021): 1489–97. http://dx.doi.org/10.1021/acs.jnatprod.0c01303.

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19

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 (February 3, 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 suggests that the antitrypanosomal activity of this compound class is amenable to substituents at N1 and C6 positions. Compound 14 having a molecular weight of 238Da, ClogP value of 1 and a total polar surface area of 49 was identified as the most active, exhibiting an IC50 value of 0.093 µM Graphical Abstract.

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20

Begolo, Daniela, Esteban Erben, and Christine Clayton. "Drug Target Identification Using a Trypanosome Overexpression Library." Antimicrobial Agents and Chemotherapy 58, no. 10 (July 21, 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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21

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 (May 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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22

Singh, Nidhi, Priyanka Shah, Hemlata Dwivedi, Shikha Mishra, Renu Tripathi, Amogh A. Sahasrabuddhe, and Mohammad Imran Siddiqi. "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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23

Waleguele, Christine C., Brice M. Mba’ning, Angelbert F. Awantu, Jean J. K. Bankeu, Yannick S. F. Fongang, Augustin S. Ngouela, Etienne Tsamo, Norbert Sewald, Bruno N. Lenta, and Rui W. M. Krause. "Antiparasitic Constituents of Beilschmiedia louisii and Beilschmiedia obscura and Some Semisynthetic Derivatives (Lauraceae)." Molecules 25, no. 12 (June 21, 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, 6, and 7 were isolated for the first time from the Beilschmiedia genus. Additionally, the NMR data of compound 4 are given here for the first time. The isolates were evaluated for their antitrypanosomal and antimalarial activities against Tb brucei and the Plasmodium falciparum chloroquine-resistant strain Pf3D7 in vitro, respectively. From the tested compounds, the mixture of new compounds 1 and 2 exhibited the most potent antitrypanosomal activity in vitro with IC50 value of 4.91 μM.

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24

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 (May 27, 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 highlighted eight particular constituents that were likely to account for the major part of the bioactivity. These compounds were then purified and identified and their activity against the pathogen tested. All identified compounds (one flavonoid and eight diterpenes) displayed significant activity against Tbr, in some cases higher than that of the total tincture. From the overall results, it can be concluded that the antitrypanosomal activity of S. officinalis L. is, for the major part, caused by abietane-type diterpenes of the rosmanol/rosmaquinone group.

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25

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

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26

Bern, Caryn. "Antitrypanosomal Therapy for Chronic Chagas' Disease." New England Journal of Medicine 364, no. 26 (June 30, 2011): 2527–34. http://dx.doi.org/10.1056/nejmct1014204.

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27

Ryczak, Jasmin, Ma'ayan Papini, Annette Lader, Abedelmajeed Nasereddin, Dmitry Kopelyanskiy, Lutz Preu, Charles L. Jaffe, and Conrad Kunick. "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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28

Muth, Mathias, Verena Hoerr, Melanie Glaser, Alicia Ponte-Sucre, Heidrun Moll, August Stich, and Ulrike Holzgrabe. "Antitrypanosomal activity of quaternary naphthalimide derivatives." Bioorganic & Medicinal Chemistry Letters 17, no. 6 (March 2007): 1590–93. http://dx.doi.org/10.1016/j.bmcl.2006.12.088.

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29

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

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30

Hata, Yoshie, Samad Nejad Ebrahimi, Maria De Mieri, Stefanie Zimmermann, Tsholofelo Mokoka, Dashnie Naidoo, Gerda Fouche, 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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31

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 (November 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 > 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.

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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 (December 15, 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 (<20 µM). Compound 4e was 2-fold more active than primaquine and was also the most active (IC50 = 7.01 µM) against T. b. rhodesiense and also exhibited excellent aqueous solubility (>200 µM) at pH 7.

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33

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 (August 20, 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 (The half maximal inhibitory concentration) and IC0.5 values of 0.022 ± 0.003 mg/mL and 0.036 ± 0.007 mg/mL, and 0.518 ± 0.044 mg/mL and 1.076 ± 0.136 mg/mL, respectively. Spegatrine (4) was identified as the main antioxidant compound in R. caffra with IC50 and IC0.5 values of 0.119 ± 0.067 mg/mL and 0.712 ± 0 mg/mL, respectively. One fraction displayed high antitrypanosomal activity with an IC50 value of 18.50 μg/mL. However, the major constituent of this fraction, raucaffricine (2), was not active. The crude extract, fractions and pure compounds did not display any cytotoxic effect at a concentration of 50 μg/mL against HeLa cells. This study shows directions for further in vitro studies on the antioxidant and antitrypanosomal activities of Rauvolfia caffra Sond.

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Gamaleldin, Noha M., Walid Bakeer, Ahmed M. Sayed, Yara I. Shamikh, Ahmed O. El-Gendy, Hossam M. Hassan, Hannes Horn, Usama Ramadan Abdelmohsen, and Wael N. Hozzein. "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 (September 22, 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-fermentation with a mycolic acid-containing strain, namely Nocardia sp. UR23. Each treatment was found to affect these actinomycetes differently in terms of biological activity (i.e., antitrypanosomal activity) and chemical profiles evidenced by LC-HRES-MS-based metabolomics and multivariate analysis. Thereafter, orthogonal projections to latent structures discriminant analysis (OPLS-DA) suggested a number of metabolites to be associated with the antitrypanosomal activity of the active extracts. The subsequent in silico screenings (neural networking-based and docking-based) further supported the OPLS-DA results and prioritized desferrioxamine B (3), bafilomycin D (10), and bafilomycin A1 (11) as possible antitrypanosomal agents. Our approach in this study can be applied as a primary step in the exploration of bioactive natural products, particularly those from actinomycetes.

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35

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 (October 7, 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 against human cervix adenocarcinoma (HeLa cells) and their antiparasitic activities were investigated against Plasmodium falciparum strain 3D7 and Trypanosoma brucei brucei. GCMS analyses of the crude extracts revealed the bioactive compounds that could be responsible for the biological activities. The extracts had no cytotoxic effect on HeLa cells and demonstrated good antiplasmodial activity (chloroform extract: IC50 = 11.6 µg∙mL−1, ethyl acetate extract: IC50 = 3.3 µg∙mL−1 and ethanol extract: IC50 = 3.7 µg∙mL−1). Likewise, they showed excellent antitrypanosomal activity with IC50 = 0.5 µg∙mL−1 for chloroform and ethyl acetate extracts and IC50 = 0.4 µg∙mL−1 for the ethanol extract. Findings from the present study indicated that O. genistifolia could be a good source of strong antiplasmodial and antitrypanosomal agents.

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Osuna, Antonio, Luis M. Ruiz-Perez, Manuel C. Lopez, Santiago Castanys, Francisco Gamarro, Dan G. Craciunescu, and Carlos Alonso. "Antitrypanosomal Action of Cis-Diamminedichloroplatinum (II) Analogs." Journal of Parasitology 73, no. 2 (April 1987): 272. http://dx.doi.org/10.2307/3282078.

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37

Pathiranage, Anuradha Liyana, Jeannie Moore Stubblefield, Xiaolei Zhou, Jianhua Miao, Anthony L. Newsome, and Norma Dunlap. "Antitrypanosomal activity of iridals from Iris domestica." Phytochemistry Letters 18 (December 2016): 44–50. http://dx.doi.org/10.1016/j.phytol.2016.08.025.

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38

Rassi, Anis, Anis Rassi, and José Antonio Marin-Neto. "Antitrypanosomal agents: treatment or threat? – Authors' reply." Lancet 376, no. 9743 (September 2010): 768–69. http://dx.doi.org/10.1016/s0140-6736(10)61373-6.

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39

Nenortas, Elizabeth, Tomasz Kulikowicz, Christian Burri, and Theresa A. Shapiro. "Antitrypanosomal Activities of Fluoroquinolones with Pyrrolidinyl Substitutions." Antimicrobial Agents and Chemotherapy 47, no. 9 (September 2003): 3015–17. http://dx.doi.org/10.1128/aac.47.9.3015-3017.2003.

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ABSTRACT Fluoroquinolones with pyrrolidinyl substitutions were tested against Trypanosoma brucei and mammalian cells. Bulky substituents at C-7 or a 1-2-bridging thiazolidine ring increased antitrypanosomal activity and selective toxicity. These compounds trap protein-DNA complexes and inhibit nucleic acid biosynthesis in trypanosomes, characteristics of topoisomerase II inhibition.

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40

Keiser, J., and C. Burri. "Evaluation of quinolone derivatives for antitrypanosomal activity." Tropical Medicine and International Health 6, no. 5 (May 2001): 369–89. http://dx.doi.org/10.1046/j.1365-3156.2001.00713.x.

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41

Zuma, Aline A., and Wanderley de Souza. "Histone deacetylases as targets for antitrypanosomal drugs." Future Science OA 4, no. 8 (September 2018): FSO325. http://dx.doi.org/10.4155/fsoa-2018-0037.

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42

Bhambra, Avninder S., Ketan C. Ruparelia, Hoon L. Tan, Deniz Tasdemir, Hollie Burrell-Saward, Vanessa Yardley, Kenneth J. M. Beresford, and Randolph R. J. Arroo. "Synthesis and antitrypanosomal activities of novel pyridylchalcones." European Journal of Medicinal Chemistry 128 (March 2017): 213–18. http://dx.doi.org/10.1016/j.ejmech.2017.01.027.

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43

Venkatraj, Muthusamy, Irene G. Salado, Jan Heeres, Jurgen Joossens, Paul J. Lewi, Guy Caljon, Louis Maes, Pieter Van der Veken, and Koen Augustyns. "Novel triazine dimers with potent antitrypanosomal activity." European Journal of Medicinal Chemistry 143 (January 2018): 306–19. http://dx.doi.org/10.1016/j.ejmech.2017.11.075.

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Pomel, S., F. Dubar, D. Forge, P. M. Loiseau, and C. Biot. "New heterocyclic compounds: Synthesis and antitrypanosomal properties." Bioorganic & Medicinal Chemistry 23, no. 16 (August 2015): 5168–74. http://dx.doi.org/10.1016/j.bmc.2015.03.029.

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45

Mohamed, Shaymaa M., Enaam Y. Bachkeet, Soad A. Bayoumi, Surendra Jain, Stephen J. Cutler, Babu L. Tekwani, and Samir A. Ross. "Potent antitrypanosomal triterpenoid saponins from Mussaenda luteola." Fitoterapia 107 (December 2015): 114–21. http://dx.doi.org/10.1016/j.fitote.2015.10.011.

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46

Boberg, Mikael, Monica Cal, Marcel Kaiser, Rasmus Jansson-Löfmark, Pascal Mäser, and Michael Ashton. "Enantiospecific antitrypanosomal in vitro activity of eflornithine." PLOS Neglected Tropical Diseases 15, no. 7 (July 12, 2021): e0009583. http://dx.doi.org/10.1371/journal.pntd.0009583.

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The polyamine synthesis inhibitor eflornithine is a recommended treatment for the neglected tropical disease Gambian human African trypanosomiasis in late stage. This parasitic disease, transmitted by the tsetse fly, is lethal unless treated. Eflornithine is administered by repeated intravenous infusions as a racemic mixture of L-eflornithine and D-eflornithine. The study compared the in vitro antitrypanosomal activity of the two enantiomers with the racemic mixture against three Trypanosoma brucei gambiense strains. Antitrypanosomal in vitro activity at varying drug concentrations was analysed by non-linear mixed effects modelling. For all three strains, L-eflornithine was more potent than D-eflornithine. Estimated 50% inhibitory concentrations of the three strains combined were 9.1 μM (95% confidence interval [8.1; 10]), 5.5 μM [4.5; 6.6], and 50 μM [42; 57] for racemic eflornithine, L-eflornithine and D-eflornithine, respectively. The higher in vitro potency of L-eflornithine warrants further studies to assess its potential for improving the treatment of late-stage Gambian human African trypanosomiasis.

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47

Twumasi, Emmanuella Bema, Pearl Ihuoma Akazue, Kwaku Kyeremeh, Theresa Manful Gwira, Jennifer Keiser, Fidelis Cho-Ngwa, Adrian Flint, et al. "Antischistosomal, antionchocercal and antitrypanosomal potentials of some Ghanaian traditional medicines and their constituents." PLOS Neglected Tropical Diseases 14, no. 12 (December 31, 2020): e0008919. http://dx.doi.org/10.1371/journal.pntd.0008919.

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Background Ghana is endemic for some neglected tropical diseases (NTDs) including schistosomiasis, onchocerciasis and lymphatic filariasis. The major intervention for these diseases is mass drug administration of a few repeatedly recycled drugs which is a cause for major concern due to reduced efficacy of the drugs and the emergence of drug resistance. Evidently, new treatments are needed urgently. Medicinal plants, on the other hand, have a reputable history as important sources of potent therapeutic agents in the treatment of various diseases among African populations, Ghana inclusively, and provide very useful starting points for the discovery of much-needed new or alternative drugs. Methodology/Principal findings In this study, extracts of fifteen traditional medicines used for treating various NTDs in local communities were screened in vitro for efficacy against schistosomiasis, onchocerciasis and African trypanosomiasis. Two extracts, NTD-B4-DCM and NTD-B7-DCM, prepared from traditional medicines used to treat schistosomiasis, displayed the highest activity (IC50 = 30.5 μg/mL and 30.8 μg/mL, respectively) against Schistosoma mansoni adult worms. NTD-B2-DCM, also obtained from an antischistosomal remedy, was the most active against female and male adult Onchocera ochengi worms (IC50 = 76.2 μg/mL and 76.7 μg/mL, respectively). Antitrypanosomal assay of the extracts against Trypanosoma brucei brucei gave the most promising results (IC50 = 5.63 μg/mL to 18.71 μg/mL). Incidentally, NTD-B4-DCM and NTD-B2-DCM, also exhibited the greatest antitrypanosomal activities (IC50 = 5.63 μg/mL and 7.12 μg/mL, respectively). Following the favourable outcome of the antitrypanosomal screening, this assay was selected for bioactivity-guided fractionation. NTD-B4-DCM, the most active extract, was fractionated and subsequent isolation of bioactive constituents led to an eupatoriochromene-rich oil (42.6%) which was 1.3-fold (IC50 <0.0977 μg/mL) more active than the standard antitrypanosomal drug, diminazene aceturate (IC50 = 0.13 μg/mL). Conclusion/Significance These findings justify the use of traditional medicines and demonstrate their prospects towards NTDs drug discovery.

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48

Nandikolla, Adinarayana, Singireddi Srinivasarao, Banoth Karan Kumar, Sankaranarayanan Murugesan, Himanshu Aggarwal, Louise L. Major, Terry K. Smith, and Kondapalli Venkata Gowri Chandra Sekhar. "Synthesis, study of antileishmanial and antitrypanosomal activity of imidazo pyridine fused triazole analogues." RSC Advances 10, no. 63 (2020): 38328–43. http://dx.doi.org/10.1039/d0ra07881f.

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Thirty-five novel 1,2,3-triazole analogues of imidazo-[1,2-a]-pyridine-3-carboxamides were designed, synthesized and evaluated for in vitro antileishmanial and antitrypanosomal activity against L. major and T. brucei parasites, respectively.

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Cunha, André Barreto, Ronan Batista, María Ángeles Castro, and Jorge Mauricio David. "Chemical Strategies towards the Synthesis of Betulinic Acid and Its More Potent Antiprotozoal Analogues." Molecules 26, no. 4 (February 18, 2021): 1081. http://dx.doi.org/10.3390/molecules26041081.

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Betulinic acid (BA, 3β-hydroxy-lup-20(29)-en-28-oic acid) is a pentacyclic triterpene acid present predominantly in Betula ssp. (Betulaceae) and is also widely spread in many species belonging to different plant families. BA presents a wide spectrum of remarkable pharmacological properties, such as cytotoxic, anti-HIV, anti-inflammatory, antidiabetic and antimicrobial activities, including antiprotozoal effects. The present review first describes the sources of BA and discusses the chemical strategies to produce this molecule starting from betulin, its natural precursor. Next, the antiprotozoal properties of BA are briefly discussed and the chemical strategies for the synthesis of analogues displaying antiplasmodial, antileishmanial and antitrypanosomal activities are systematically presented. The antiplasmodial activity described for BA was moderate, nevertheless, some C-3 position acylated analogues showed an improvement of this activity and the hybrid models—with artesunic acid—showed the most interesting properties. Some analogues also presented more intense antileishmanial activities compared with BA, and, in addition to these, heterocycles fused to C-2/C-3 positions and amide derivatives were the most promising analogues. Regarding the antitrypanosomal activity, some interesting antitrypanosomal derivatives were prepared by amide formation at the C-28 carboxylic group of the lupane skeleton. Considering that BA can be produced either by isolation of different plant extracts or by chemical transformation of betulin, easily obtained from Betula ssp., it could be said that BA is a molecule of great interest as a starting material for the synthesis of novel antiprotozoal agents.

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Cerecetto, H., R. Di Maio, G. Seoane, A. Denicola, G. Peluffo, and C. Quijano. "Synthetic Modifications of Lead Compounds as Antitrypanosomal Drugs." Molecules 5, no. 12 (March 22, 2000): 497–98. http://dx.doi.org/10.3390/50300497.

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