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Evaluating the Effectiveness of Cancer Drug Sensitization In Vitro and In Vivo
Published on: February 6, 2015
Chemoprotective and chemosensitizing effects of apigenin on cancer therapy
Zahra Nozhat1,2, Shabnam Heydarzadeh2,3, Zahra Memariani4
1Institute of Smart Biomedical Materials, School of Materials Science and Engineering, Zhejiang Sci-Tech University, Hangzhou, 310018, China.
Background:
Therapeutic resistance to radiation and chemotherapy is one of the major obstacles in cancer treatment. Although synthetic radiosensitizers are pragmatic solution to enhance tumor sensitivity, they pose concerns of toxicity and non-specificity. In the last decades, scientists scrutinized novel plant-derived radiosensitizers and chemosensitizers, such as flavones, owing to their substantial physiological effects like low toxicity and non-mutagenic properties on the human cells. The combination therapy with apigenin is potential candidate in cancer therapeutics. This review explicates the combinatorial strategies involving apigenin to overcome drug resistance and boost the anti-cancer properties.
Methods:
We selected full-text English papers on international databases like PubMed, Web of Science, Google Scholar, Scopus, and ScienceDirect from 1972 up to 2020. The keywords included in the search were: Apigenin, Chemoprotective, Chemosensitizing, Side Effects, and Molecular Mechanisms.
Results:
In this review, we focused on combination therapy, particularly with apigenin augmenting the anti-cancer effects of chemo drugs on tumor cells, reduce their side effects, subdue drug resistance, and protect healthy cells. The reviewed research data implies that these co-therapies exhibited a synergistic effect on various cancer cells, where apigenin sensitized the chemo drug through different pathways including a significant reduction in overexpressed genes, AKT phosphorylation, NFκB, inhibition of Nrf2, overexpression of caspases, up-regulation of p53 and MAPK, compared to the monotherapies. Meanwhile, contrary to the chemo drugs alone, combined treatments significantly induced apoptosis in the treated cells.
Conclusion:
Briefly, our analysis proposed that the combination therapies with apigenin could suppress the unwanted toxicity of chemotherapeutic agents. It is believed that these expedient results may pave the path for the development of drugs with a high therapeutic index. Nevertheless, human clinical trials are a prerequisite to consider the potential use of apigenin in the prevention and treatment of various cancers. Conclusively, the clinical trials to comprehend the role of apigenin as a chemoprotective agent are still in infancy.
Insights
Apigenin, a plant-derived compound, enhances chemotherapy effectiveness by reducing drug resistance and toxicity. Further clinical trials are needed to confirm its role in cancer treatment.
Area of Science:
- Oncology
- Pharmacology
- Natural Products
Background:
- Therapeutic resistance to conventional cancer treatments like radiation and chemotherapy remains a significant clinical challenge.
- Plant-derived compounds, such as flavones like apigenin, are being investigated as potential radiosensitizers and chemosensitizers due to their low toxicity and non-mutagenic properties.
- Apigenin shows promise as a combinatorial agent to enhance anti-cancer therapies and overcome drug resistance.
Purpose of the Study:
- To review and explicate combinatorial strategies involving apigenin to overcome drug resistance and enhance anti-cancer properties.
- To investigate apigenin's role in augmenting the efficacy of chemotherapy drugs.
- To assess apigenin's potential in reducing chemotherapy side effects and protecting healthy cells.
Main Methods:
- A comprehensive literature search was conducted on major scientific databases (PubMed, Web of Science, Google Scholar, Scopus, ScienceDirect) from 1972 to 2020.
- Keywords used in the search included: Apigenin, Chemoprotective, Chemosensitizing, Side Effects, and Molecular Mechanisms.
- Full-text English papers were selected for review.
Main Results:
- Combination therapy with apigenin demonstrated synergistic effects on various cancer cells, enhancing anti-cancer drug efficacy.
- Apigenin sensitized cancer cells to chemotherapy through multiple molecular pathways, including modulation of gene expression (AKT, NFκB, Nrf2, p53, MAPK) and caspase activity.
- Combined treatments significantly induced apoptosis in cancer cells, unlike monotherapies with chemotherapy drugs alone.
Conclusions:
- Combinatorial therapies incorporating apigenin show potential in mitigating the adverse toxicity associated with chemotherapeutic agents.
- These findings suggest the development of drugs with a higher therapeutic index, potentially improving cancer treatment outcomes.
- Further human clinical trials are essential to validate apigenin's efficacy and safety as a chemoprotective and anti-cancer agent.
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