The potential roles of gossypol as anticancer agent: advances and future directions

Abstract Gossypol, a polyphenolic aldehyde derived from cottonseed plants, has seen a transformation in its pharmaceutical application from a male contraceptive to a candidate for cancer therapy. This shift is supported by its recognized antitumor properties, which have prompted its investigation in...

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Main Authors: Danijela Paunovic, Jovana Rajkovic, Radmila Novakovic, Jelica Grujic-Milanovic, Reham Hassan Mekky, Dragos Popa, Daniela Calina, Javad Sharifi-Rad
Format: Article
Language:English
Published: BMC 2023-12-01
Series:Chinese Medicine
Subjects:
Online Access:https://doi.org/10.1186/s13020-023-00869-8
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author Danijela Paunovic
Jovana Rajkovic
Radmila Novakovic
Jelica Grujic-Milanovic
Reham Hassan Mekky
Dragos Popa
Daniela Calina
Javad Sharifi-Rad
author_facet Danijela Paunovic
Jovana Rajkovic
Radmila Novakovic
Jelica Grujic-Milanovic
Reham Hassan Mekky
Dragos Popa
Daniela Calina
Javad Sharifi-Rad
author_sort Danijela Paunovic
collection DOAJ
description Abstract Gossypol, a polyphenolic aldehyde derived from cottonseed plants, has seen a transformation in its pharmaceutical application from a male contraceptive to a candidate for cancer therapy. This shift is supported by its recognized antitumor properties, which have prompted its investigation in the treatment of various cancers and related inflammatory conditions. This review synthesizes the current understanding of gossypol as an anticancer agent, focusing on its pharmacological mechanisms, strategies to enhance its clinical efficacy, and the status of ongoing clinical evaluations. The methodological approach to this review involved a systematic search across several scientific databases including the National Center for Biotechnology Information (NCBI), PubMed/MedLine, Google Scholar, Scopus, and TRIP. Studies were meticulously chosen to cover various aspects of gossypol, from its chemical structure and natural sources to its pharmacokinetics and confirmed anticancer efficacy. Specific MeSH terms and keywords related to gossypol’s antineoplastic applications guided the search strategy. Results from selected pharmacological studies indicate that gossypol inhibits the Bcl-2 family of anti-apoptotic proteins, promoting apoptosis in tumor cells. Clinical trials, particularly phase I and II, reveal gossypol’s promise as an anticancer agent, demonstrating efficacy and manageable toxicity profiles. The review identifies the development of gossypol derivatives and novel carriers as avenues to enhance therapeutic outcomes and mitigate adverse effects. Conclusively, gossypol represents a promising anticancer agent with considerable therapeutic potential. However, further research is needed to refine gossypol-based therapies, explore combination treatments, and verify their effectiveness across cancer types. The ongoing clinical trials continue to support its potential, suggesting a future where gossypol could play a significant role in cancer treatment protocols.
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spelling doaj.art-a47b6226143b43679abc2bacdd7623812023-12-17T12:29:54ZengBMCChinese Medicine1749-85462023-12-0118111710.1186/s13020-023-00869-8The potential roles of gossypol as anticancer agent: advances and future directionsDanijela Paunovic0Jovana Rajkovic1Radmila Novakovic2Jelica Grujic-Milanovic3Reham Hassan Mekky4Dragos Popa5Daniela Calina6Javad Sharifi-Rad7Institute for Biological Research Sinisa Stankovic, National Institute of the Republic of Serbia, University of BelgradeInstitute for Pharmacology, Clinical Pharmacology and Toxicology, Medical Faculty, University of BelgradeCenter for Genome Sequencing and Bioinformatics, Institute of Molecular Genetics and Genetic Engineering, University of BelgradeInstitute for Medical Research, National Institute of the Republic of Serbia, Department for Cardiovascular Research, University of BelgradeDepartment of Pharmacognosy, Faculty of Pharmacy, Egyptian Russian UniversityDepartment of Plastic Surgery, University of Medicine and Pharmacy of CraiovaDepartment of Clinical Pharmacy, University of Medicine and Pharmacy of CraiovaFacultad de Medicina, Universidad del AzuayAbstract Gossypol, a polyphenolic aldehyde derived from cottonseed plants, has seen a transformation in its pharmaceutical application from a male contraceptive to a candidate for cancer therapy. This shift is supported by its recognized antitumor properties, which have prompted its investigation in the treatment of various cancers and related inflammatory conditions. This review synthesizes the current understanding of gossypol as an anticancer agent, focusing on its pharmacological mechanisms, strategies to enhance its clinical efficacy, and the status of ongoing clinical evaluations. The methodological approach to this review involved a systematic search across several scientific databases including the National Center for Biotechnology Information (NCBI), PubMed/MedLine, Google Scholar, Scopus, and TRIP. Studies were meticulously chosen to cover various aspects of gossypol, from its chemical structure and natural sources to its pharmacokinetics and confirmed anticancer efficacy. Specific MeSH terms and keywords related to gossypol’s antineoplastic applications guided the search strategy. Results from selected pharmacological studies indicate that gossypol inhibits the Bcl-2 family of anti-apoptotic proteins, promoting apoptosis in tumor cells. Clinical trials, particularly phase I and II, reveal gossypol’s promise as an anticancer agent, demonstrating efficacy and manageable toxicity profiles. The review identifies the development of gossypol derivatives and novel carriers as avenues to enhance therapeutic outcomes and mitigate adverse effects. Conclusively, gossypol represents a promising anticancer agent with considerable therapeutic potential. However, further research is needed to refine gossypol-based therapies, explore combination treatments, and verify their effectiveness across cancer types. The ongoing clinical trials continue to support its potential, suggesting a future where gossypol could play a significant role in cancer treatment protocols.https://doi.org/10.1186/s13020-023-00869-8GossypolAnticancer mechanismsApoptosisProliferationMolecular targetsMechanisms
spellingShingle Danijela Paunovic
Jovana Rajkovic
Radmila Novakovic
Jelica Grujic-Milanovic
Reham Hassan Mekky
Dragos Popa
Daniela Calina
Javad Sharifi-Rad
The potential roles of gossypol as anticancer agent: advances and future directions
Chinese Medicine
Gossypol
Anticancer mechanisms
Apoptosis
Proliferation
Molecular targets
Mechanisms
title The potential roles of gossypol as anticancer agent: advances and future directions
title_full The potential roles of gossypol as anticancer agent: advances and future directions
title_fullStr The potential roles of gossypol as anticancer agent: advances and future directions
title_full_unstemmed The potential roles of gossypol as anticancer agent: advances and future directions
title_short The potential roles of gossypol as anticancer agent: advances and future directions
title_sort potential roles of gossypol as anticancer agent advances and future directions
topic Gossypol
Anticancer mechanisms
Apoptosis
Proliferation
Molecular targets
Mechanisms
url https://doi.org/10.1186/s13020-023-00869-8
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