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Antiprotozoal Effects of Wild Plants
Published in Mahendra Rai, Shandesh Bhattarai, Chistiane M. Feitosa, Ethnopharmacology of Wild Plants, 2021
Muhammad Subbayyal Akram, Rao Zahid Abbas, José L. Martinez
Trichilia emetica belongs to family Meliaceae and is natively found in the forests of Africa. It is traditionally used for the treatment of abdominal pain, jaundice, skin problems, chest pain and many more (Komane et al. 2015). Atindehou et al. (2004) evaluated 88 plants of Côte d’Ivoire and their 101 crude ethanol extracts to verify antitrypanosomal activity and he founded T. emetica to be the most promising one. The root bark extract shows IC50 value of 0.04 μg/ml against Trypanosoma brucei rhodensiense. Its leaf extracts also exhibited satisfactory results against Trypanosoma brucei brucei and Trypanosoma brucei rhodesiense with IC50value of 14.9 μg/ml and 8.6 μg/ml, respectively (Hoet et al. 2004). Phytochemical analyses reveal the presence of limonoids such as trichilins and seco-liminoids which show antitrypanosomal activity by damaging DNA (Atindehou et al. 2004).
Curcumin and Neglected Infectious Diseases
Published in Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay, Medicinal Chemistry of Neglected and Tropical Diseases, 2019
Francesca Mazzacuva, Agostino Cilibrizzi
Curcumin (1) also demonstrated cytotoxic effects in vitro against African trypanosomiasis (i.e., African sleeping sickness), with LD50 values of 4.77 μM and 46.52 μM for Trypanosoma brucei brucei (GUTat 3.1 clone) bloodstream and procyclic forms, respectively (Saleheen et al. 2002, Nose et al. 2006). Similarly, demethoxycurcumin (2) and bisdemetoxycurcumin (3) (see section 1.1 and Figure 1) exhibited the same level of antitrypanosomal activity on this parasite species, with EC50 values in the low micromolar range (Changtam et al. 2010). All the curcuminoids tested in the study displayed a higher toxicity for Tryoanosoma brucei brucei than HEK cells (i.e., selectivity indexes ranging from 3- to 1500-fold) (Lim 2016).
Design, synthesis, and antiprotozoal evaluation of new 2,4-bis[(substituted-aminomethyl)phenyl]quinoline, 1,3-bis[(substituted-aminomethyl)phenyl]isoquinoline and 2,4-bis[(substituted-aminomethyl)phenyl]quinazoline derivatives
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Jean Guillon, Anita Cohen, Clotilde Boudot, Alessandra Valle, Vittoria Milano, Rabindra Nath Das, Aurore Guédin, Stéphane Moreau, Luisa Ronga, Solène Savrimoutou, Maxime Demourgues, Elodie Reviriego, Sandra Rubio, Sandie Ferriez, Patrice Agnamey, Cécile Pauc, Serge Moukha, Pascale Dozolme, Sophie Da Nascimento, Pierre Laumaillé, Anne Bouchut, Nadine Azas, Jean-Louis Mergny, Catherine Mullié, Pascal Sonnet, Bertrand Courtioux
Furthermore, another neglected disease caused by Trypanosomatidae parasites of the Trypanosoma genus is the human African trypanosomiasis (HAT), or sleeping sickness, almost invariably fatal unless treated. This infection is transmitted to humans through the bite of an infected tsetse fly. Brain involvement causes various neurological disturbances, including sleep disorders, progression to coma and, ultimately, death. There are two clinical forms: the slowly progressing form (gambiense HAT), caused by infection with Trypanosoma brucei gambiense (currently 98% of cases), and the faster progressing form (rhodesiense HAT), caused by infection with Trypanosoma brucei rhodesiense. As a neglected tropical disease targeted by the WHO for elimination, a historically low number of cases (<1000) was reported in 2018. The recent approval of a new medicine (fexinidazole) for the treatment of gambiense HAT has opened new possibilities for the management of cases and thus led to recent WHO interim guidelines for this treatment27. A veterinary form of this parasitic disease exists. Named Nagana, it is caused by Trypanosoma brucei brucei which contaminates African livestock, thus having a significant economic impact.
Metal nanoparticles restrict the growth of protozoan parasites
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2018
Oluyomi Stephen Adeyemi, Nthatisi Innocentia Molefe, Oluwakemi Josephine Awakan, Charles Obiora Nwonuma, Omokolade Oluwaseyi Alejolowo, Tomilola Olaolu, Rotdelmwa Filibus Maimako, Keisuke Suganuma, Yongmei Han, Kentaro Kato
Trypanosoma and Toxoplasma are protozoan parasites responsible for diseases that cause significant morbidity, mortality and economic burden, predominantly in developing countries [1–3]. For example, African trypanosomosis is a lethal infectious disease for both humans and livestock; an epidemic of this infection would have a major impact on the economic development of sub-Saharan Africa [4]. The causative agents are hemoflagellated protozoan parasites (i.e. Trypanosoma species), which elicit fatal diseases in African mammalian hosts. The human African trypanosomiasis (HAT, also called sleeping sickness) is caused by Trypanosoma brucei rhodesiense and Trypanosoma brucei gambiense, whereas bovine Trypanosomosis or nagana is caused by Trypanosoma brucei brucei [5–7]. Trypanosoma infection is fatal if left untreated either in humans or animals. Chemotherapy is a major means of controlling the infection; however, the available treatment options have various shortcomings including limited efficacy, toxicity and the emergence of resistant strains of trypanosomes [2,8]. Melarsoprol, one of the few drugs effective against the second stage of the disease, is reported to cause encephalopathy in 10–15% of patients, and approximately 40% of these cases are fatal [9,10]. These highlight the need for innovative strategies to combat trypanosomosis, which puts the health of more than 60 million people in the sub-Saharan Africa at risk annually [11]. Consequently, the lack of effective anti-Trypanosoma therapies, coupled with unsuccessful attempts at vaccine development due to antigenic variation, has stimulated the search for new chemotherapy for trypanosomosis. Therefore, new candidate drugs against trypanosomosis are urgently needed.