Isoflavonoids and Epigenetic Modulation: Therapeutic Insights for Cancer Treatment

Isolavonoides represent the second largest subgroup of flavonoids and have an influence on critical molecular pathways and restore cellular homeostasis, through the reprogramming of epigenetic regulatory mechanisms. This feature indicates a crucial therapeutic potential that could be better explored to attend cancer treatment. Isoflavonoids, acting as epigenetic modulators, could contribute to the development of new therapeutic approaches in cancer, especially in onco-hematological diseases. Pterocarpans are a subgroup of isoflavonoids that have been extensively studied for their biological properties. The molecule (+)-2,3,9-trimethoxypterocarpan demonstrates high gastrointestinal (GI) absorption and the ability to cross the blood-brain barrier (BBB) in silico without violating Lipinski's rule, making it a desirable candidate in leukemia treatment. The synthesis of this molecule dates back more than a decade. In silico models, such as SwissADME, corroborate the notion of good intestinal absorption and the ability to cross the BBB. Also, it is suggested that P-glycoprotein is a substrate, which is related to its potential for active efflux from both the BBB and GI. This review highlights the biological mechanisms of this class of natural products from a translational perspective, emphasizing their chemical properties and epigenetic biological activities, which offer new therapeutic perspectives, particularly in oncology.

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Journal
Chemistry & Biodiversity
Published
2026-02-01
DOI
https://doi.org/10.1002/cbdv.202503446
Primary Topic
Histone Deacetylase Inhibitors Research
Type
article
Field-Weighted Citation Impact
0.00

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article

Isoflavonoids and Epigenetic Modulation: Therapeutic Insights for Cancer Treatment

Maria Cláudia dos Santos Luciano, Cristiana Libardi Miranda Furtado, GABRIEL CAETANO DE SOUZA, Cláudia do Ó Pessoa et al.
Chemistry & Biodiversity
Histone Deacetylase Inhibitors Research
article

Isoflavonoids and Epigenetic Modulation: Therapeutic Insights for Cancer Treatment

Maria Cláudia dos Santos Luciano, Cristiana Libardi Miranda Furtado, GABRIEL CAETANO DE SOUZA, Cláudia do Ó Pessoa, Sarah Sant'Anna Maranhão, Felipe Vasconcelos, Eduardo de Moraes e Sousa, Fátima de Cássia Evangelista de Oliveira, Maria Francilene Souza Silva
article en

Abstract

Isolavonoides represent the second largest subgroup of flavonoids and have an influence on critical molecular pathways and restore cellular homeostasis, through the reprogramming of epigenetic regulatory mechanisms. This feature indicates a crucial therapeutic potential that could be better explored to attend cancer treatment. Isoflavonoids, acting as epigenetic modulators, could contribute to the development of new therapeutic approaches in cancer, especially in onco-hematological diseases. Pterocarpans are a subgroup of isoflavonoids that have been extensively studied for their biological properties. The molecule (+)-2,3,9-trimethoxypterocarpan demonstrates high gastrointestinal (GI) absorption and the ability to cross the blood-brain barrier (BBB) in silico without violating Lipinski's rule, making it a desirable candidate in leukemia treatment. The synthesis of this molecule dates back more than a decade. In silico models, such as SwissADME, corroborate the notion of good intestinal absorption and the ability to cross the BBB. Also, it is suggested that P-glycoprotein is a substrate, which is related to its potential for active efflux from both the BBB and GI. This review highlights the biological mechanisms of this class of natural products from a translational perspective, emphasizing their chemical properties and epigenetic biological activities, which offer new therapeutic perspectives, particularly in oncology.

Chemistry & BiodiversityVol. 23(2)
Universidade Federal de Minas Gerais (BR), Universidade Federal do Ceará (BR), Universidade de Fortaleza (BR), Library Network (US), Hospital Haroldo Juaçaba (BR)
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior, Ministério da Ciência, Tecnologia e Inovação, Conselho Nacional de Desenvolvimento Científico e Tecnológico, Financiadora de Estudos e Projetos
Good health and well-being
Openalex Percentile: Top 54%
Histone Deacetylase Inhibitors Research
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