In Silico Identification of Six Mushroom-Derived Sterol and Triterpenoid Compounds as Potential P-Glycoprotein Modulators in Multidrug Resistance

The overexpression of P-glycoprotein (P-gp) is often directly related to multidrug resistance (MDR), one of the greatest challenges in cancer treatment. This transmembrane efflux pump decreases the intracellular concentrations of chemotherapy drugs, reducing their effectiveness and resulting in treatment failure. This work used in silico methods to assess the potential of bioactive chemicals produced from mushrooms as P-gp modulators. A database comprising 211 bioactive compounds from mushrooms was investigated using molecular docking and virtual screening techniques against the P-gp structure. The compounds ergosta-4,6,8(14),22-tetraen-3-one, lucidumol A, (22E,24S)-ergosta-4,22-dien-3-one, antcin K, 3,11-dioxolanosta-8,24(Z)-diene-26-oic acid, and (22E)-19-norergosta-5,7,9,22-tetraen-3β-ol were identified as the six best candidates from our database of mushroom compounds based on their binding affinities, toxicity predictions, and pharmacological properties assessed through ADME analyses (absorption, distributions, metabolism, and excretion). These six compounds exhibited strong binding affinities, with binding energies ranging from −12.31 kcal/mol to −10.93 kcal/mol, all showing higher affinities than the control, tariquidar, which had a binding energy of −10.78 kcal/mol. Toxicity predictions indicated favorable safety profiles for all six, while ADME analyses found that all six compounds had high oral bioavailability and a low probability of acting as P-gp substrates. These results position bioactive mushroom compounds, particularly these six, as promising P-gp modulators, suggesting positive outcomes in cancer treatment.

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Journal
Applied Sciences
Published
2025-08-08
DOI
https://doi.org/10.3390/app15168772
Primary Topic
Drug Transport and Resistance Mechanisms
Type
article
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article

In Silico Identification of Six Mushroom-Derived Sterol and Triterpenoid Compounds as Potential P-Glycoprotein Modulators in Multidrug Resistance

Rui M.V. Abreu, Sara Ricardo, Carlos S. H. Shiraishi, Josiana A. Vaz et al.
Applied Sciences
Drug Transport and Resistance Mechanisms
article

In Silico Identification of Six Mushroom-Derived Sterol and Triterpenoid Compounds as Potential P-Glycoprotein Modulators in Multidrug Resistance

Rui M.V. Abreu, Sara Ricardo, Carlos S. H. Shiraishi, Josiana A. Vaz, Jéssica Fonsêca
article en

Abstract

The overexpression of P-glycoprotein (P-gp) is often directly related to multidrug resistance (MDR), one of the greatest challenges in cancer treatment. This transmembrane efflux pump decreases the intracellular concentrations of chemotherapy drugs, reducing their effectiveness and resulting in treatment failure. This work used in silico methods to assess the potential of bioactive chemicals produced from mushrooms as P-gp modulators. A database comprising 211 bioactive compounds from mushrooms was investigated using molecular docking and virtual screening techniques against the P-gp structure. The compounds ergosta-4,6,8(14),22-tetraen-3-one, lucidumol A, (22E,24S)-ergosta-4,22-dien-3-one, antcin K, 3,11-dioxolanosta-8,24(Z)-diene-26-oic acid, and (22E)-19-norergosta-5,7,9,22-tetraen-3β-ol were identified as the six best candidates from our database of mushroom compounds based on their binding affinities, toxicity predictions, and pharmacological properties assessed through ADME analyses (absorption, distributions, metabolism, and excretion). These six compounds exhibited strong binding affinities, with binding energies ranging from −12.31 kcal/mol to −10.93 kcal/mol, all showing higher affinities than the control, tariquidar, which had a binding energy of −10.78 kcal/mol. Toxicity predictions indicated favorable safety profiles for all six, while ADME analyses found that all six compounds had high oral bioavailability and a low probability of acting as P-gp substrates. These results position bioactive mushroom compounds, particularly these six, as promising P-gp modulators, suggesting positive outcomes in cancer treatment.

Applied SciencesVol. 15(16)
Universidade Politécnica de Bragança (PT), Cooperativa de Ensino Superior Politécnico e Universitário (PT), i3S - Instituto de Investigação e Inovação em Saúde, Universidade do Porto (PT), Unidade em Ciências Biomoleculares Aplicadas, Universidade de Vigo (ES)
Openalex Percentile: Top 71%
Drug Transport and Resistance Mechanisms
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