Abstract

Cancer is the second leading cause of death in the world and one of the major public health problems. Despite the great advances in cancer therapy, the incidence and mortality rates of cancer remain high. Therefore, the quest for more efficient and less toxic cancer treatment strategies is still at the forefront of current research. Curcumin, the active ingredient of the Curcuma longa plant, has received great attention over the past two decades as an antioxidant, anti-inflammatory, and anticancer agent. In this review, a summary of the medicinal chemistry and pharmacology of curcumin and its derivatives in regard to anticancer activity, their main mechanisms of action, and cellular targets has been provided based on the literature data from the experimental and clinical evaluation of curcumin in cancer cell lines, animal models, and human subjects. In addition, the recent advances in the drug delivery systems for curcumin delivery to cancer cells have been highlighted.

Highlights

  • Cancer is the second most life-threatening disease and one of the main public health problems worldwide

  • This review focuses on the recent literature on the structure activity relationship (SAR) of curcumin and its analogues and their anticancer activity in different cancer cell lines, animal models, and human clinical trials as well as different types of curcumin delivery systems that have been used for cancer therapy

  • In vitro studies of curcumin in different head and neck cancer cell lines have proven its ability to inhibit cell growth due to its effects on a number of cellular pathways involved in cell proliferation, most notably NF-κB and STAT3, which are found to be overexpressed in several head and neck carcinomas [109,110]

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Summary

Introduction

Cancer is the second most life-threatening disease and one of the main public health problems worldwide. The curcumin molecule tends to penetrate into the cell membrane and bind to the fatty acyl chains of membrane lipids through hydrogen binding and hydrophobic interactions, resulting in low availability of curcumin inside the cytoplasm [12,13] To overcome these obstacles and improve the overall anticancer activity of curcumin, several structural modifications have been suggested to enhance selective toxicity towards specific cancer cells [14], increase bioavailability, or enhance stability [4,15]. Another approach is to use different delivery systems to improve curcumin’s physiochemical properties and anticancer activity. This review focuses on the recent literature on the SAR of curcumin and its analogues and their anticancer activity in different cancer cell lines, animal models, and human clinical trials as well as different types of curcumin delivery systems that have been used for cancer therapy

Structure Activity Relationship of Curcumin and Its Derivatives
Introduction of cyclohexane bridge
Different Types of Curcumin Delivery Systems Used in Cancer Therapy
Liposomes
Peptide and Protein Formulations
Colorectal Cancer
Head and Neck Squamous Cell Carcinoma
Breast Cancer
Brain Cancer and Glioblastoma
Clinical Studies
Results
Pancreatic Cancer
Prostate Cancer
Head and Neck Cancer
Findings
Conclusions and Future Perspectives

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