Recent Advances in Berberine Inspired Anticancer Approaches: From Drug Combination to Novel Formulation Technology
1Pharmacognosy Research Laboratories & Herbal Analysis Services UK, University of Greenwich, Chatham-Maritime, ME4 4TB Kent, UK.
Abstract:
Berberine is multifunctional natural product with potential to treat diverse pathological conditions. Its broad-spectrum anticancer effect through direct effect on cancer cell growth and metastasis have been established both in vitro and in vivo. The cellular targets that account to the anticancer effect of berberine are incredibly large and range from kinases (protein kinase B (Akt), mitogen activated protein kinases (MAPKs), cell cycle checkpoint kinases, etc.) and transcription factors to genes and protein regulators of cell survival, motility and death. The direct effect of berberine in cancer cells is however relatively weak and occur at moderate concentration range (10-100 µM) in most cancer cells. The poor pharmacokinetics profile resulting from poor absorption, efflux by permeability-glycoprotein (P-gc) and extensive metabolism in intestinal and hepatic cells are other dimensions of berberine's limitation as anticancer agent. This communication addresses the research efforts during the last two decades that were devoted to enhancing the anticancer potential of berberine. Strategies highlighted include using berberine in combination with other chemotherapeutic agents either to reduce toxic side effects or enhance their anticancer effects; the various novel formulation approaches which by order of magnitude improved the pharmacokinetics of berberine; and semisynthetic approaches that enhanced potency by up to 100-fold.
Insights
Berberine shows anticancer potential but has limitations. Research has focused on enhancing its effectiveness through combination therapies, novel formulations, and semi-synthetic modifications to improve its pharmacokinetic profile and potency.
Area of Science:
- Pharmacology
- Natural Products Chemistry
- Cancer Biology
Background:
- Berberine exhibits broad-spectrum anticancer properties by targeting various cellular pathways involved in cancer growth and metastasis.
- Its clinical application is limited by a weak direct effect on cancer cells and poor pharmacokinetic properties, including low absorption and rapid metabolism.
Purpose of the Study:
- To review research efforts over the past two decades aimed at enhancing the anticancer potential of berberine.
- To highlight strategies for overcoming berberine's limitations as an anticancer agent.
Main Methods:
- Review of scientific literature focusing on combination therapies, novel drug delivery systems, and semi-synthetic modifications of berberine.
- Analysis of studies investigating improved pharmacokinetic profiles and enhanced anticancer potency.
Main Results:
- Combination therapy with berberine can reduce side effects and enhance anticancer efficacy.
- Novel formulations significantly improve berberine's pharmacokinetics, increasing its bioavailability.
- Semi-synthetic derivatives of berberine have demonstrated up to 100-fold increase in potency.
Conclusions:
- Strategic approaches, including combination therapies, advanced formulations, and semi-synthetic modifications, have successfully enhanced berberine's anticancer potential.
- These advancements offer promising avenues for developing berberine-based cancer therapeutics with improved efficacy and bioavailability.
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