In vitro Assessment of Camphor Hydrazone Derivatives as an Agent Against Leishmania amazonensis

Silva, Emerson Teixeira da; Andrade, Gabriel Fernandes de; Araújo, Adriele da Silva; Almeida, Ayla das Chagas; Coimbra, Elaine Soares; Souza, Marcus V. N. de

doi:10.2478/s11686-019-00146-5

Cited by 5 publications

(4 citation statements)

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“…Many other previous studies have evaluated a wide variety of herbal remedies such as the antioxidant effects of lemon, Cinnamomum camphora (L.) J. Presl, and Crocus sativus L., the anti-bacterial effects of lemon, Juniperus excelsa M. Bieb, and Vitriolum ( ferrous sulfate ), the anti-inflammatory and antiseptic properties of honey, lemon, Commiphora myrrha (Nees) Engl., Cuminum cyminum L., Aristolochia sp., and Boswellia sp., the antipruritic effect of topical camphor on leishmaniasis lesion, the antimicrobial effect of olibanum and cumin , and the anti-promastigote effect of mountain tea, M. germanica leaves, and calendula officinalis on leishmaniasis. [ 28 29 30 31 32 33 34 35 36 37 38 ]…”

Section: Discussionmentioning

confidence: 99%

Examination of the topical effect of the combination of Plantago ovata and vinegar on the improvement of rural cutaneous leishmaniasis lesions

et al. 2023

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Section: Discussionmentioning

confidence: 99%

Examination of the topical effect of the combination of Plantago ovata and vinegar on the improvement of rural cutaneous leishmaniasis lesions

et al. 2023

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“…In addition to triazole, compound 6 contains another important pharmacophoric group, the arylhydrazone. Hydrazones are important groups, known for their leishmanicidal properties and presence in many compounds used as antileishmanial agents [31,32]. The arylhydrazone may be related to the greater activity exhibited by compound 6 in comparison to the other compounds analyzed.…”

Section: Discussionmentioning

confidence: 99%

“…Compound 6, meanwhile, had the lowest cytotoxicity, possibly associated with the presence of the arylhydrazone group. Several studies have described the use of hydrazone derivatives with leishmanicidal activity, reporting their good selectivity rates and low cytotoxicity [31,32,35].…”

Section: Discussionmentioning

confidence: 99%

1,4-Disubstituted-1,2,3-Triazole Compounds Induce Ultrastructural Alterations in Leishmania amazonensis Promastigote: An in Vitro Antileishmanial and in Silico Pharmacokinetic Study

Almeida-Souza

Silva

et al. 2020

IJMS

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The current standard treatment for leishmaniasis has remained the same for over 100 years, despite inducing several adverse effects and increasing cases of resistance. In this study we evaluated the in vitro antileishmanial activity of 1,4-disubstituted-1,2,3 triazole compounds and carried out in silico predictive study of their pharmacokinetic and toxicity properties. Ten compounds were analyzed, with compound 6 notably presenting IC50: 14.64 ± 4.392 µM against promastigotes, IC50: 17.78 ± 3.257 µM against intracellular amastigotes, CC50: 547.88 ± 3.256 µM against BALB/c peritoneal macrophages, and 30.81-fold selectivity for the parasite over the cells. It also resulted in a remarkable decrease in all the parameters of in vitro infection. Ultrastructural analysis revealed lipid corpuscles, a nucleus with discontinuity of the nuclear membrane, a change in nuclear chromatin, and kinetoplast swelling with breakdown of the mitochondrial cristae and electron-density loss induced by 1,4-disubstituted-1,2,3-triazole treatment. In addition, compound 6 enhanced 2.3-fold the nitrite levels in the Leishmania-stimulated macrophages. In silico pharmacokinetic prediction of compound 6 revealed that it is not recommended for topical formulation cutaneous leishmaniasis treatment, however the other properties exhibited results that were similar or even better than miltefosine, making it a good candidate for further in vivo studies against Leishmania parasites.

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“…Many compound classes have exhibited activity in vitro against promastigotes or amastigotes, including thiophene-indole hybrids [82,83], 2-amino-thiophene derivatives [84], pyrazolothiophene hybrids [85], camphor hydrazone derivatives [86], tetroxanes [87], isoxazole derivatives and tetrahydrofuran neolignans [88], piperine derivatives [89], naphthotriazolyl-4-oxoquinolines [90], furazolidone-based cyclodextrins [91], 2-pyrimidinyl-hydrazone and N-acylhydrazone derivatives [92], piperidine-benzodioxole derivatives [93], and methyl gallate [94]. In vivo studies of these compounds are required to elucidate their activity and safety profiles before clinical development can begin.…”

Section: Drug Discovery Targeting a Single Leishmania Speciesmentioning

confidence: 99%

Drug Discovery for Cutaneous Leishmaniasis: A Review of Developments in the Past 15 Years

Corman,

McNamara,

Bakowski

2023

Microorganisms

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Leishmaniasis is a group of vector-borne, parasitic diseases caused by over 20 species of the protozoan Leishmania spp. The three major disease classifications, cutaneous, visceral, and mucocutaneous, have a range of clinical manifestations from self-healing skin lesions to hepatosplenomegaly and mucosal membrane damage to fatality. As a neglected tropical disease, leishmaniasis represents a major international health challenge, with nearly 350 million people living at risk of infection a year. The current chemotherapeutics used to treat leishmaniasis have harsh side effects, prolonged and costly treatment regimens, as well as emerging drug resistance, and are predominantly used for the treatment of visceral leishmaniasis. There is an undeniable need for the identification and development of novel chemotherapeutics targeting cutaneous leishmaniasis (CL), largely ignored by concerted drug development efforts. CL is mostly non-lethal and the most common presentation of this disease, with nearly 1 million new cases reported annually. Recognizing this unaddressed need, substantial yet fragmented progress in early drug discovery efforts for CL has occurred in the past 15 years and was outlined in this review. However, further work needs to be carried out to advance early discovery candidates towards the clinic. Importantly, there is a paucity of investment in the translation and development of therapies for CL, limiting the emergence of viable solutions to deal with this serious and complex international health problem.

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In vitro Assessment of Camphor Hydrazone Derivatives as an Agent Against Leishmania amazonensis

Cited by 5 publications

References 10 publications

Examination of the topical effect of the combination of Plantago ovata and vinegar on the improvement of rural cutaneous leishmaniasis lesions

Examination of the topical effect of the combination of Plantago ovata and vinegar on the improvement of rural cutaneous leishmaniasis lesions

1,4-Disubstituted-1,2,3-Triazole Compounds Induce Ultrastructural Alterations in Leishmania amazonensis Promastigote: An in Vitro Antileishmanial and in Silico Pharmacokinetic Study

Drug Discovery for Cutaneous Leishmaniasis: A Review of Developments in the Past 15 Years

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