The in vitro activity of fatty diamines and amino alcohols against mixed amastigote and trypomastigote Trypanosoma cruzi forms

Júnior, Policarpo Ademar Sales; Júnior, Celso O. R.; Hyaric, Mireille Le; Almeida, Mauro Vieira de; Romanha, Álvaro J.

doi:10.1590/0074-0276130496

Cited by 9 publications

(5 citation statements)

References 14 publications

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“…It has been extensively used to determine the in vitro activity/toxicity of different drugs against different trypanosomatids such as T. cruzi, T. brucei and Leishmania spp. (Rolón et al., 2006, Sykes and Avery, 2009, Morais-Teixeira et al., 2011, Bowling et al., 2012, Sales Junior et al., 2014, Engel et al., 2015). A previous study found AlamarBlue ® was a good method to quantify the activity of different compounds against T. brucei gambiense and T. b. rhodesiense in vitro and demonstrated that results were comparable to those obtained with other fluorochrome dyes (Räz et al., 1997).…”

Section: Discussionmentioning

confidence: 99%

“…Several studies have revealed that some drugs or compounds, including benznidazole, are more active against T. cruzi intracellular amastigotes compared to epimastigotes and trypomastigotes (Freire-de-Lima et al., 2008, Luna et al., 2009, Sales Junior et al., 2014). This has also been shown with different species of Leishmania , where intracellular amastigotes showed greater susceptibility to miltefosine, than promastigotes (Obonaga et al., 2014).…”

Section: Discussionmentioning

confidence: 99%

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In vitro drug susceptibility of two strains of the wildlife trypanosome, Trypanosoma copemani : A comparison with Trypanosoma cruzi

Botero

Keatley

Peacock

et al. 2017

International Journal for Parasitology: Drugs and Drug Resistan

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Trypanosomes are blood protozoan parasites that are capable of producing illness in the vertebrate host. Within Australia, several native Trypanosoma species have been described infecting wildlife. However, only Trypanosoma copemani has been associated with pathological lesions in wildlife hosts and more recently has been associated with the drastic decline of the critically endangered woylie (Bettongia penicillata). The impact that some trypanosomes have on the health of the vertebrate host has led to the development of numerous drug compounds that could inhibit the growth or kill the parasite. This study investigated and compared the in vitro susceptibility of two strains of T. copemani (G1 and G2) and one strain of Trypanosoma cruzi (10R26) against drugs that are known to show trypanocidal activity (benznidazole, posaconazole, miltefosine and melarsoprol) and against four lead compounds, two fenarimols and two pyridine derivatives (EPL-BS1937, EPL-BS2391, EPL-BS0967, and EPL-BS1246), that have been developed primarily against T.cruzi. The in vitro cytotoxicity of all drugs against L6 rat myoblast cells was also assessed. Results showed that both strains of T. copemani were more susceptible to all drugs and lead compounds than T. cruzi, with all IC50 values in the low and sub-μM range for both species. Melarsoprol and miltefosine exhibited the highest drug activity against both T. copemani and T. cruzi, but they also showed the highest toxicity in L6 cells. Interestingly, both fenarimol and pyridine derivative compounds were more active against T. copemani and T. cruzi than the reference drugs benznidazole and posaconazole. T. copemani strains exhibited differences in susceptibility to all drugs demonstrating once again considerable differences in their biological behaviour.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

In vitro drug susceptibility of two strains of the wildlife trypanosome, Trypanosoma copemani : A comparison with Trypanosoma cruzi

Botero

Keatley

Peacock

et al. 2017

International Journal for Parasitology: Drugs and Drug Resistan

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“…Importantly, the amphiphilic character of the organic compounds reflects their ability to interact and penetrate biological membranes inducing different effects,29, 32, 46 such as increased antimicrobial activity 47 . Lipophilicity is an important characteristic of antifungal agents, such as terbinafine and ketoconazole, and is also evident in drugs like amphotericin B, which have proven effectiveness to treat systemic fungal infections 46 .…”

Section: Discussionmentioning

confidence: 99%

“…Amine and amide groups are significant functional groups in medications due to their reactive and chemical properties, 27 and these groups comprise peptides found in various proteins 28 . Our previous data show that amino alcohols have antimicrobial and immunological activities against Trypanosoma cruzi 29, 30, 31, 32. Thus, the present study evaluated the antifungal activities of amphiphilic aromatic amino alcohols and amides against different strains of fungi associated with onychomycosis.…”

Section: Introductionmentioning

confidence: 97%

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In vitro antifungal activity of organic compounds derived from amino alcohols against onychomycosis

Caneschi

Almeida

Martins

et al. 2017

Brazilian Journal of Microbiology

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Onychomycosis is a fungal infection of the nail caused by high densities of filamentous fungi and yeasts. Treatment for this illness is long-term, and recurrences are frequently detected. This study evaluated in vitro antifungal activities of 12 organic compounds derived from amino alcohols against standard fungal strains, such as Trichophyton rubrum CCT 5507 URM 1666, Trichophyton mentagrophytes ATCC 11481, and Candida albicans ATCC 10231. The antifungal compounds were synthesized from p-hydroxybenzaldehyde (4a–4f) and p-hydroxybenzoic acid (9a–9f). Minimum inhibitory concentrations and minimum fungicidal concentrations were determined according to Clinical and Laboratory Standards Institute protocols M38-A2, M27-A3, and M27-S4. The amine series 4b–4e, mainly 4c and 4e compounds, were effective against filamentous fungi and yeast (MIC from 7.8 to 312 μg/mL). On the other hand, the amide series (9a–9f) did not present inhibitory effect against fungi, except amide 9c, which demonstrated activity only against C. albicans. This allowed us to infer that the presence of amine group and intermediate carbon number (8C–11C) in its aliphatic side chain seems to be important for antifungal activity. Although these compounds present cytotoxic activity on macrophages J774, our results suggest that these aromatic compounds might constitute potential as leader molecules in the development of more effective and less toxic analogs that could have considerable implications for future therapies of onychomycosis.

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Antifungal activity of aminoalcohols and diamines against dermatophytes and yeast

et al. 2020

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The in vitro activity of fatty diamines and amino alcohols against mixed amastigote and trypomastigote Trypanosoma cruzi forms

Cited by 9 publications

References 14 publications

In vitro drug susceptibility of two strains of the wildlife trypanosome, Trypanosoma copemani : A comparison with Trypanosoma cruzi

In vitro drug susceptibility of two strains of the wildlife trypanosome, Trypanosoma copemani : A comparison with Trypanosoma cruzi

In vitro antifungal activity of organic compounds derived from amino alcohols against onychomycosis

Antifungal activity of aminoalcohols and diamines against dermatophytes and yeast

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