Leishmania: papel de la glicoproteína P en la mediación de resistencia a medicamentos y estrategias de reversión.

Osorio, Edison; Robledo, Sara M.; Arango, Gabriel Jaime Murillo; Muskus, Carlos

doi:10.7705/biomedica.v25i2.1347

Cited by 5 publications

(3 citation statements)

References 133 publications

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“…As Figure 13 shows, passive human gastrointestinal (GI) absorption data estimate that 97% of the 68 compounds present high absorption in the digestive tract, while the remaining 3%, corresponding to structures 17 and 43, would present low intestinal absorption. For its part, P-glycoprotein (PGP) is a permeability protein that pumps substances out of the body and prevents their absorption, which causes drug resistance to form [105,106]. It was found that none of the compounds behaved as a substrate for P-gp; therefore, they could conduct the function without any resistance [107].…”

Section: Adme Analysismentioning

confidence: 99%

In Silico Antiprotozoal Evaluation of 1,4-Naphthoquinone Derivatives against Chagas and Leishmaniasis Diseases Using QSAR, Molecular Docking, and ADME Approaches

et al. 2022

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Chagas and leishmaniasis are two neglected diseases considered as public health problems worldwide, for which there is no effective, low-cost, and low-toxicity treatment for the host. Naphthoquinones are ligands with redox properties involved in oxidative biological processes with a wide variety of activities, including antiparasitic. In this work, in silico methods of quantitative structure–activity relationship (QSAR), molecular docking, and calculation of ADME (absorption, distribution, metabolism, and excretion) properties were used to evaluate naphthoquinone derivatives with unknown antiprotozoal activity. QSAR models were developed for predicting antiparasitic activity against Trypanosoma cruzi, Leishmania amazonensis, and Leishmania infatum, as well as the QSAR model for toxicity activity. Most of the evaluated ligands presented high antiparasitic activity. According to the docking results, the family of triazole derivatives presented the best affinity with the different macromolecular targets. The ADME results showed that most of the evaluated compounds present adequate conditions to be administered orally. Naphthoquinone derivatives show good biological activity results, depending on the substituents attached to the quinone ring, and perhaps the potential to be converted into drugs or starting molecules.

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Section: Adme Analysismentioning

confidence: 99%

In Silico Antiprotozoal Evaluation of 1,4-Naphthoquinone Derivatives against Chagas and Leishmaniasis Diseases Using QSAR, Molecular Docking, and ADME Approaches

et al. 2022

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“…Hay, además, una modificación en el transporte del medicamento que frena su ingreso y acelera su salida del parásito disminuyendo, de esta manera, las concentraciones citoplasmáticas que podrían ser fatales para el microorganismo. Para una mayor ilustración al respecto se recomienda la revisión publicada por Osorio et al (56).…”

Section: Mecanismos De Resistencia a Antimoniales Pentavalentesunclassified

Estado actual y futuro de la terapia anti-leishmaniásica en Colombia

Soto¹,

Soto²

2012

biomedica

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Palabras clave: leishmaniasis/terapia, vigilancia epidemiológica, resistencia a las drogas, resultado del tratamiento, efectividad. Current situation and future of antileihmanial therapy in ColombiaPentavalent antimonials are the first choice to treat leishmaniasis in Colombia. However, a 600% increase in the total dose has been necessary in order to maintain their efficacy. Cure rates varying between 93 and 25% can reflect differences in parasite susceptibility, but are more likely secondary to deficiencies in compliance with treatment guidelines. We review the current situation of efficacy and use of pentavalent antimony compounds, amphotericin B, pentamidine and miltefosine and attempt a projection for the next following years. To determine the real situation of response to antileishmanial drugs and to extend their useful life, the establishment of surveillance mechanisms to cover all factors involved is necessary. A sentinel site surveillance strategy to allow punctual observations in time, in specific geographical areas and in particular local situations, is proposed.

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“…El tratamiento consiste en la administración de antimoniales pentavalentes pero su administración causa efectos secundarios como mialgia, pancreatitis, insuficiencia renal, neuropatía periférica, hepatotoxicidad, y cardiotoxicidad (Croft y Yardley, 2002). En la actualidad existen varias drogas que han sido ensayadas para el tratamiento quimioterápico de Leishmaniosis cutánea pero muchas de ellas son nuevas formulaciones de drogas diseñadas hace 50 años; además se ha presentado resistencia a las drogas clásicamente empleadas, lo cual hace necesaria la búsqueda de nuevos medicamentos que reemplacen o complementen el tratamiento actual (Croft y Yardley, 2002;Osorio et al, 2005).…”

Section: Introductionunclassified

Actividad leishmanicida de los extractos metanólicos de cuatro ecotipos de Lepidium peruvianum, Chacón (Brassicaceae)

et al. 2006

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ResumenEl tratamiento clásico de la leishmaniosis cutánea consiste en la inyección de 15-20 ampollas de Glucantine lo que ocasiona efectos secundarios, este hecho justifica la búsqueda de nuevos medicamentos motivando la presente investigación. El objetivo fue evaluar in vitro la actividad leishmanicida de los extractos metanólicos (EM) de los ecotipos blanco, rojo, morado y negro de Lepidium peruvianum, Chacón (también conocida como Lepidium meyenii Walp.), sobre el crecimiento de Leishmania braziliensis peruviana. Los promastigotes alcanzaron la fase de crecimiento exponencial al quinto día de cultivo a 27 ºC en el medio bifásico Columbia, suplementado con 15% de sangre desfibrinada de carnero, en ese momento se enfrentaron, por separado, con los EM a concentraciones de 50, 100, 200 y 400 μg/ml. Los recuentos se hicieron diariamente con cámara Neubauer. La máxima disminución de promastigotes se produjo al segundo día de enfrentamiento para el ecotipo morado (17,41% de viabilidad) empleando 400 μg/ml. El efecto leishmanicida estaría relacionado con los alcaloides imidazólicos presentes en el EM. Se concluye que al segundo día de enfrentamiento con el EM, el ecotipo morado presenta la mayor actividad leishmanicida seguido del ecotipo blanco.Palabras clave: Leishmania braziliensis peruviana, Lepidium peruvianum; Lepidium meyenii, actividad leishmanicida, plantas medicinales peruanas, ecotipos de Maca. AbstractThe classic treatment of the cutaneous leishmaniosis consists on the injection of 15-20 ampoule of Glucantine what causes serious secondary effects. This fact justifies the search of new medications what motivated the present investigation. The objective was to evaluate the leishmanicidal activity of the methanolic extracts (ME) of the white, red, purple and black ecotypes of Lepidium peruvianum Chacón (at present Lepidium meyenii Walp.) about the growth of Leishmania braziliensis peruviana in vitro. The promastigotes reached the logarithmic phase to the fifth day of cultivation at 27 ºC in the two-phase Columbia medium with 15% of defibrinated sheep blood and they faced, for separate, with the ME to concentrations of 50, 100, 200 and 400 μg/ml. The recounts were made daily with camera Neubauer. The maximum decrease of promastigotes (17.41% of viability) took place to the second day for the purple ecotype with the concentration of 400 μg/ml. The leishmanicidal effect would be related with the imidazolic alkaloids, glucosinolates, flavonoids, tannins and saponines present in the ME. The conclusion is that only ME of the white and purple ecotypes presents leishmanicidal activity, at second day of culture.

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Leishmania: papel de la glicoproteína P en la mediación de resistencia a medicamentos y estrategias de reversión.

Cited by 5 publications

References 133 publications

In Silico Antiprotozoal Evaluation of 1,4-Naphthoquinone Derivatives against Chagas and Leishmaniasis Diseases Using QSAR, Molecular Docking, and ADME Approaches

In Silico Antiprotozoal Evaluation of 1,4-Naphthoquinone Derivatives against Chagas and Leishmaniasis Diseases Using QSAR, Molecular Docking, and ADME Approaches

Estado actual y futuro de la terapia anti-leishmaniásica en Colombia

Actividad leishmanicida de los extractos metanólicos de cuatro ecotipos de Lepidium peruvianum, Chacón (Brassicaceae)

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