Antitrypanosomal activity of new semi‐synthetic bergenin derivatives

2021 ◽  
Author(s):  
Seham S. El‐Hawary ◽  
Rabab Mohammed ◽  
Sameh AbouZid ◽  
Mohamed A. Zaki ◽  
Zeinab Y. Ali ◽  
...  
Keyword(s):  
Antitrypanosomal Activity ◽  
Bergenin Derivatives

Screening of medical plants from Mali for antitrypanosomal activity

Planta Medica ◽  
2006 ◽  
Vol 72 (11) ◽  
Author(s):  
B Aderbauer ◽  
PH Clausen ◽  
MF Melzig
Keyword(s):  
Antitrypanosomal Activity ◽  
Medical Plants

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.

Antitrypanosomal Activity & Docking Studies of Components of Crateva adansonii DC Leaves: Novel Multifunctional Scaffolds

2014 ◽  
Vol 14 (8) ◽  
pp. 981-990 ◽  
Author(s):  
Ngozichukwuka Igoli ◽  
Carol Clements ◽  
Rajeev Singla ◽  
John Igoli ◽  
Nzekwe Uche ◽  
...  
Keyword(s):  
Docking Studies ◽  
Antitrypanosomal Activity

Virtual Screening of Alkaloids from Apocynaceae with Potential Antitrypanosomal Activity

2015 ◽  
Vol 10 (5) ◽  
pp. 509-519 ◽  
Author(s):  
Marcus Scotti ◽  
Alejandro Speck-Planche ◽  
Josean Tavares ◽  
Marcelo da Silva ◽  
M. D. S. Cordeiro ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Antitrypanosomal Activity

scholarly journals Bufadienolides from the Skin Secretions of the Neotropical Toad Rhinella alata (Anura: Bufonidae): Antiprotozoal Activity against Trypanosoma cruzi

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4217
Author(s):  
Candelario Rodriguez ◽  
Roberto Ibáñez ◽  
Luis Mojica ◽  
Michelle Ng ◽  
Carmenza Spadafora ◽  
...  
Keyword(s):  
Vero Cells ◽  
Chemical Diversity ◽  
Hydroxyl Group ◽  
Antitrypanosomal Activity ◽  
The Family ◽  
Toad Venom ◽  
Skin Secretions ◽  
Pharmacological Potential ◽  
First Time ◽  
Mcf 7

Toads in the family Bufonidae contain bufadienolides in their venom, which are characterized by their chemical diversity and high pharmacological potential. American trypanosomiasis is a neglected disease that affects an estimated 8 million people in tropical and subtropical countries. In this research, we investigated the chemical composition and antitrypanosomal activity of toad venom from Rhinella alata collected in Panama. Structural determination using mass spectrometry (MS) and nuclear magnetic resonance (NMR) spectroscopy led to the identification of 10 bufadienolides. Compounds identified include the following: 16β-hydroxy-desacetyl-bufotalin-3-adipoyl-arginine ester (1), bufotalin (2), 16β-hydroxy-desacetyl-bufotalin-3-pimeloyl-arginine ester (3), bufotalin-3-pimeloyl-arginine ester (4), 16β-hydroxy-desacetyl-bufotalin-3-suberoyl-arginine ester (5), bufotalin-3-suberoyl-arginine ester (6), cinobufagin-3-adipoyl-arginine ester (7), cinobufagin-3-pimeloyl-arginine ester (8), cinobufagin-3-suberoyl-arginine ester (9), and cinobufagin (10). Among these, three new natural products, 1, 3, and 5, are described, and compounds 1–10 are reported for the first time in R. alata. The antitrypanosomal activity assessed in this study revealed that the presence of an arginyl-diacid attached to C-3, and a hydroxyl group at C-14 in the structure of bufadienolides that is important for their biological activity. Bufadienolides showed cytotoxic activity against epithelial kidney Vero cells; however, bufagins (2 and 10) displayed low mammalian cytotoxicity. Compounds 2 and 10 showed activity against the cancer cell lines MCF-7, NCI-H460, and SF-268.

scholarly journals Antitrypanosomal activity of purine nucleosides can be enhanced by their conversion to O-acetylated derivatives.

1996 ◽  
Vol 40 (11) ◽  
pp. 2567-2572 ◽  
Author(s):  
J R Sufrin ◽  
D Rattendi ◽  
A J Spiess ◽  
S Lane ◽  
C J Marasco ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Parent Compound ◽  
Nucleoside Analogs ◽  
Significant Activity ◽  
Structural Class ◽  
Antitrypanosomal Activity ◽  
Salvage Pathways ◽  
Purine Salvage Pathways

Fifteen purine nucleosides and their O-acetylated ester derivatives were examined for in vitro antitrypanosomal activity against the LAB 110 EATRO isolate of Trypanosoma brucei brucei and two clinical isolates of Trypanosoma brucei rhodesiense. Initial comparisons of activity were made for the LAB 110 EATRO isolate. Three nucleoside analogs exhibited no significant activity (50% inhibitory concentrations [IC50s] of > 100 microM), whether they were O acetylated or unacetylated; three nucleosides showed almost equal activity (IC50s of < 5 microM) for the parent compound and the O-acetylated derivative; nine nucleosides showed significantly improved activity (> or = 3-fold) upon O acetylation; of these nine analogs, six displayed activity at least 10-fold greater than that of their parent nucleosides. The most significant results were those for four apparently inactive compounds which, upon O acetylation, displayed IC50s of < or = 25 microM. When the series of compounds was tested against T. brucei rhodesiense isolates (KETRI 243 and KETRI 269), their antitrypanosomal effects were comparable to those observed for the EATRO 110 strain. Thus, our studies of purine nucleosides have determined that O acetylation consistently improved their in vitro antitrypanosomal activity. This observed phenomenon was independent of their cellular enzyme targets (i.e., S-adenosylmethionine, polyamine, or purine salvage pathways). On the basis of our results, the routine preparation of O-acetylated purine nucleosides for in vitro screening of antitrypanosomal activity is recommended, since O acetylation transformed several inactive nucleosides into compounds with significant activity, presumably by improving uptake characteristics. O-acetylated purine nucleosides may offer in vivo therapeutic advantages compared with their parent nucleosides, and this possibility should be considered in future evaluations of this structural class of trypanocides.

Prolylisoxazoles: Potent Inhibitors of Prolyloligopeptidase with Antitrypanosomal Activity.

ChemInform ◽  
2003 ◽  
Vol 34 (47) ◽  
Author(s):  
Gunther Bal ◽  
Pieter Van der Veken ◽  
Dimitri Antonov ◽  
Anne-Marie Lambeir ◽  
Philippe Grellier ◽  
...  
Keyword(s):  
Antitrypanosomal Activity

scholarly journals In vitro antitrypanosomal activity of African plants used in traditional medicine in Uganda to treat sleeping sickness

2007 ◽  
Vol 1 (6) ◽  
pp. 765-771 ◽  
Author(s):  
Franziska Freiburghaus ◽  
Elizabeth N. Ogwal ◽  
Mayunga H. H. Nkunya ◽  
Ronald Kaminsky ◽  
Reto Brun
Keyword(s):  
Traditional Medicine ◽  
Sleeping Sickness ◽  
Antitrypanosomal Activity ◽  
African Plants

In-vitro Anti-trypanosomal and Cytotoxicity Evaluation of 3-methyl-3-4-dihydroquinazolin-2(1H)-one Derivatives

Drug Research ◽  
2021 ◽  
Author(s):  
Omobolanle J. Jesumoroti ◽  
Richard M. Beteck ◽  
Lesetja J. Legoabe
Keyword(s):  
Hela Cells ◽  
Polar Surface Area ◽  
Activity Data ◽  
Antitrypanosomal Activity ◽  
Ic50 Value ◽  
Pharmacokinetic Properties ◽  
Quinazolinone Derivatives ◽  
Low Activity ◽  
As Toxicity

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.

Synthesis and biological evaluation of bergenin derivatives as new immunosuppressants

2021 ◽  
Author(s):  
Lihua Deng ◽  
Cheng-Cheng Song ◽  
Youhong Niu ◽  
Qin Li ◽  
Meng Wang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Pharmacological Properties ◽  
New Type ◽  
Bergenin Derivatives ◽  
Synthesis And Biological Evaluation

Bergenin, which is isolated from Bergenia species, exhibits various pharmacological properties. In the search for new type of immunosuppressants, a series of bergenin derivatives were designed and synthesized, and their...

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