title: Curcumin-based anti-prostate cancer agents.
abstract: Prostate cancer possesses the highest occurrence rate and is the second-paramount disease that causes cancer-affiliated death among men in the United States. Approximately 30,000 men die each year of castration-resistant prostate cancer due to the inevitable progression of resistance to first-line treatment with docetaxel. The safety profile of dietary curcumin in humans has been well-documented, and its therapeutic prospect in treating prostate cancer, especially for castration-resistant prostate cancer, has been evidenced in several cell culture systems and human xenograft mouse models. The critical disadvantage of curcumin as a drug candidate is its low bioavailability caused by poor water solubility and rapid in vivo metabolism. Curcumin is characteristic of regulating multiple targets, representing a good example for the philosophy to search for multitargeted drugs in the realm of drug design and drug development. This feature, together with its potential in treating castration-resistant prostate cancer and its safety profile, enables curcumin to serve as an ideal lead compound for the design and syntheses of curcumin-based agents with improved potential for the clinical therapies of prostate cancer. Several researches aiming to improve its bioavailability and potency resulted in the discovery and development of a wealth of curcumin-based compounds with an enhanced anticancer potential and/or an improved pharmacokinetic profile. This review starts with a brief summarization of the prospect of curcumin in treating prostate cancer and its mechanisms of action, then provides an in-depth overview of current development of curcumin-based anti-prostate cancer agents and their structure-activity relationships, and ends with the syntheses and pharmacokinetic studies of curcumin.
authors.affiliation: California State University Fresno, Department of Chemistry, 2555 E. San Ramon Avenue M/S SB 70. qchen@csufresno.edu.
authors.forename: Qiao-Hong
authors.initials: QH
authors.lastname: Chen
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D001682:Biological Availability; D003474:Curcumin / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D006801:Humans; D008297:Male; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D012995:Solubility; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D003474:Curcumin