A Review of Curcumin and Its Derivatives as Anticancer Agents

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.

Synthesis of Curcumin Derivatives and Analysis of Their Antitumor Effects in Triple Negative Breast Cancer (TNBC) Cell Lines

“…13 C NMR spectrum of Compound 3 in CDCl 3 as solvent.4.1.3. (1E,6E)-1-(4-hydroxy-3-methoxyphenyl)-7-[3-methoxy-4(4-methylbromobenzyl)oxyphenyl]hepta-1,6-diene-3,5-dione (4) and (1E,6E)-1,7-bis [3-methoxy-4(4-methylbromobenzyl) oxyphenyl]hepta-1,6-diene-3,5-dione(5) …”

Curcumin as an Anticancer Agent in Malignant Mesothelioma: A Review

“…In fact, the glucuronidation and sulfation of curcumin happen very soon after in vivo administration and the produced metabolites are rapidly excreted from feces, urine and bile [57]. To have an idea of the low bioavailability of curcumin, these data are very indicative: ingestion of 2 g of pure curcumin results in the presence of only 10 ng/mL curcumin in plasma [58]. Indeed, its poor bioavailability and high potential to interfere with other drugs constitute real obstacles for precisely defining the real biological and clinical anti-cancer properties of curcumin.…”

“…In this regard, numerous attempts aimed at increasing the efficacy and bioavailability of curcumin have been made. In particular, attention has been paid to designing suitable formulations using nanocarriers for delivery and targeting [58][59][60].…”

“…Therefore, biodegradable synthetic polymers such as PLGA (poly (d, l-lactic-co-glycolic acid) and natural polymers such as silk fibroin and chitosan have become widely used in drug delivery [60]. Nevertheless, nanoscale liposomes are emerging as one of the most advantageous drug delivery systems for anticancer agents [58]. A liposome consists of a phospholipid bilayer shell and an aqueous core which makes it a superlative transporter for capturing both hydrophobic and hydrophilic compounds.…”

Cyclovirobuxine D inhibits colorectal cancer tumorigenesis via the CTHRC1‑AKT/ERK‑Snail signaling pathway

“…Accumulating evidence has shown that natural plant compounds (NPCs), such as curcumin, resveratrol and dictamnine, have significant clinical benefits in cancer, such as inhibiting cell proliferation, affecting the cell cycle, and promoting apoptosis and/or autophagy (6)(7)(8). In addition, bioactive natural components extracted from plants have received attention for their inhibition of epithelial-mesenchymal transformation (EMT) through anti-inflammatory, anti-fibrosis or anti-oxidant mechanisms (9).…”