Antileishmanial Chemotherapy: A Literature Review

Bastos, Mônica M.; Boechat, Núbia; Hoelz, Lucas Villas Bôas; Oliveira, Andresa Pereira de

doi:10.21577/1984-6835.20160139

Cited by 11 publications

(15 citation statements)

References 37 publications

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“…Amphotericin B is a second-choice drug for the treatment of leishmaniasis in many places around the world. Combined drug therapy can be an important tool for reducing toxic effects, as well as reducing the duration of treatment and improving treatment compliance by the patient ( Bastos et al, 2016 ; Roatt et al, 2020 ). In this regard, some studies were caried out with the aim to associating promising compounds to amphotericin B ( Marinho et al, 2014 ; Mehrizi et al, 2019 ; Roatt et al, 2020 ; Silva et al, 2020 ).…”

Section: Discussionmentioning

confidence: 99%

A Betulinic Acid Derivative, BA5, Induces G0/G1 Cell Arrest, Apoptosis Like-Death, and Morphological Alterations in Leishmania sp

et al. 2022

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Leishmaniasis are endemic diseases caused by different species of intracellular parasites of the genus Leishmania. Due to the high toxicity and drug resistance of current antileishmanial drugs, it is necessary to identify new and more effective drugs. Previously, we investigated the immunomodulatory and anti-Trypanosoma cruzi action of BA5, a derivative of betulinic acid. In the present study, we investigated the in vitro activity of BA5 against different species of Leishmania and their action mechanism. BA5 exhibited low cytotoxicity against macrophages and inhibited the proliferation of promastigote forms of Leishmania amazonensis (IC50 = 4.5 ± 1.1 μM), Leishmania major (IC50 = 3.0 ± 0.8 μM), Leishmania braziliensis (IC50 = 0.9 ± 1.1 μM) and Leishmania infantum (IC50 = 0.15 ± 0.05 μM). Incubation with BA5 reduced the percentage of Leishmania amazonensis-infected macrophages and the number of intracellular parasites (IC50 = 4.1 ± 0.7 μM). To understand the mechanism of action underlying BA5 antileishmanial activity (incubation at IC50/2, IC50 or 2xIC50 values of the drug), we investigated ultrastructural changes by scanning electron microscopy and evaluated cell cycle, membrane mitochondrial potential, and cell death against promastigote forms of Leishmania amazonensis by flow cytometry. Promastigotes incubated with BA5 presented membrane blebbing, flagella damage, increased size, and body deformation. Flow cytometry analysis showed that parasite death is mainly caused by apoptosis-like death, arrested cell cycle in G0/G1 phase and did not alter the membrane mitochondrial potential of Leishmania amazonensis. Surprisingly, the combination of BA5 and amphotericin B, an assay used to determine the degree of drug interaction, revealed synergistic effects (CI = 0.15 ± 0.09) on promastigotes forms of Leishmania amazonensis. In conclusion, BA5 compound is an effective and selective antileishmanial agent.

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Section: Discussionmentioning

confidence: 99%

A Betulinic Acid Derivative, BA5, Induces G0/G1 Cell Arrest, Apoptosis Like-Death, and Morphological Alterations in Leishmania sp

et al. 2022

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“…Still, it has important adverse effects, the most frequent being nausea, headache, tachycardia, hypoglycemia, and hyperglycemia. Furthermore, parasitic resistance was observed, which reduces PT effectiveness. ,, PM is an aminoglycoside antibiotic produced by bacteria of the genus Streptomyces , with leishmanicidal activity. The drug can be administered parenterally and locally and is inexpensive and effective in the treatment.…”

Section: Leishmaniasis Therapymentioning

confidence: 99%

“…The drug can be administered parenterally and locally and is inexpensive and effective in the treatment. Common side effects are nausea, abdominal pain, nephrotoxicity, ototoxicity, and liver dysfunction . MT was first used as an anticancer drug.…”

Section: Leishmaniasis Therapymentioning

confidence: 99%

“…According to the World Health Organization (WHO), more than 1 billion people reside in endemic areas and are at risk of infection. The annual occurrence in the world is estimated between 700,000 to 1 million new cases, between 600,000 to 1 million LC, and between 50,000 and 90,000 of VL. − …”

Section: Introductionmentioning

confidence: 99%

“…Another factor of great concern is the high cost of certain formulations. The limitations of the available drugs indicate the need to develop new therapeutic strategies or new more effective and less toxic formulations. ,, …”

Section: Introductionmentioning

confidence: 99%

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A Systematic Review of Drug-Carrying Nanosystems Used in the Treatment of Leishmaniasis

et al. 2023

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Leishmaniasis is an infectious disease responsible for a huge rate of morbidity and mortality in humans. Chemotherapy consists of the use of pentavalent antimonial, amphotericin B, pentamidine, miltefosine, and paromomycin. However, these drugs are associated with some drawbacks such as high toxicity, administration by parenteral route, and most seriously the resistance of some strains of the parasite to them. Several strategies have been used to increase the therapeutic index and reduce the toxic effects of these drugs. Among them, the use of nanosystems that have great potential as a site-specific drug delivery system stands out. This review aims to compile results from studies that were carried out using first-and second-line antileishmanial drugcarrying nanosystems. The articles referred to here were published between 2011 and 2021. This study shows the promise of effective applicability of drug-carrying nanosystems in the field of antileishmanial therapeutics, with the perspective of providing better patient adherence to treatment, increased therapeutic efficacy, reduced toxicity of conventional drugs, as well as the potential to efficiently improve the treatment of leishmaniasis.

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Sixty years of Amphotericin B: An Overview of the Main Antifungal Agent Used to Treat Invasive Fungal Infections

Cavassin

Baú-Carneiro²,

Vilas-Boas³

et al. 2021

Infect Dis Ther

197

123

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Introduced in the late 1950s, polyenes represent the oldest family of antifungal drugs. The discovery of amphotericin B and its therapeutic uses is considered one of the most important scientific milestones of the twentieth century . Despite its toxic potential, it remains useful in the treatment of invasive fungal diseases owing to its broad spectrum of activity, low resistance rate, and excellent clinical and pharmacological action. The well-reported and defined toxicity of the conventional drug has meant that much attention has been paid to the development of new products that could minimize this effect. As a result, lipid-based formulations of amphotericin B have emerged and, even keeping the active principle in common, present distinct characteristics that may influence therapeutic results. This study presents an overview of the pharmacological properties of the different formulations for systemic use of amphotericin B available for the treatment of invasive fungal infections, highlighting the characteristics related to their chemical, pharmacokinetic structures, drug–target interactions, stability, and others, and points out the most relevant aspects for clinical practice.

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Antileishmanial Chemotherapy: A Literature Review

Cited by 11 publications

References 37 publications

A Betulinic Acid Derivative, BA5, Induces G0/G1 Cell Arrest, Apoptosis Like-Death, and Morphological Alterations in Leishmania sp

A Betulinic Acid Derivative, BA5, Induces G0/G1 Cell Arrest, Apoptosis Like-Death, and Morphological Alterations in Leishmania sp

A Systematic Review of Drug-Carrying Nanosystems Used in the Treatment of Leishmaniasis

Sixty years of Amphotericin B: An Overview of the Main Antifungal Agent Used to Treat Invasive Fungal Infections

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