Design and Development of Water-Soluble Curcumin Conjugates as Potential Anticancer Agents

• Published in: Journal of medicinal chemistry Vol. 50; no. 24; pp. 6284 - 6288
• Main Authors: Safavy, Ahmad, Raisch, Kevin P, Mantena, Sushma, Sanford, Leisa L, Sham, Simon W, Krishna, N. Rama, Bonner, James A
• Format: Journal Article
• Language: English
• Published: Washington, DC American Chemical Society 29-11-2007
• Subjects: Antineoplastic agents; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Biological and medical sciences; Cell Line, Tumor; Curcumin - chemistry; Drug Design; Drug Screening Assays, Antitumor; General aspects; Humans; Medical sciences; Pharmacology. Drug treatments; Polyethylene Glycols - chemistry; Solubility; Structure-Activity Relationship; Water; Antineoplastic agent; Human; Cytotoxicity; Drug carrier; Molecular size; In vitro; Biological activity; Ethylene oxide polymer; Water soluble compound; Cell line; Internalization; Water solubility; Active ingredient; Curcumin; Kinetics; Colon; Conjugated compound; Pancreas; Chemical synthesis; Prostate; Tumor cell; Release
• ISSN: 0022-2623; 1520-4804
• DOI: 10.1021/jm700988f

Conjugates of curcumin to two differently sized poly(ethylene glycol) molecules were synthesized in an attempt to overcome the low aqueous solubility of this natural product with cytotoxic activity against some human cancer cell lines. The soluble conjugates exhibited enhanced cytotoxicity as compared to that of the parent drug. Synthesis, analyses of the rate of drug release, and cytotoxicity studies are herein reported. The water-soluble conjugates may provide information useful for the development of injectable curcumin conjugates.