title: Effects of curcumin analogues for inhibiting human prostate cancer cells and the growth of human PC-3 prostate xenografts in immunodeficient mice.
abstract: Four curcumin analogues ((2E,6E)-2,6-bis(thiophen-3-methylene) cyclohexanone (AS), (2E,5E)-2,5-bis(thiophen-3-methylene) cyclopentanone (BS), (3E,5E)-3,5-bis(thiophen-3-methylene)-tetrahydropyran-4-one (ES) and (3E,5E)-3,5-bis(thiophen-3-methylene)-tetrahydrothiopyran-4-one (FS) as shown in Fig. 1) with different linker groups were investigated for their effects in human prostate cancer CWR-22Rv1 and PC-3 cells. Compounds FS and ES had stronger inhibitory effects than curcumin, AS and BS on the growth of cultured CWR-22Rv1 and PC-3 cells, as well as on the androgen receptor (AR) and nuclear factor kappa B (NF-κB) activity. The strong activities of ES and FS may be correlated with a heteroatom linker. In animal studies, severe combined immunodeficient (SCID) mice were injected subcutaneously (s.c.) with PC-3 cells in Matrigel. After 4 to 6 weeks, mice with PC-3 tumors (about 0.6 cm wide and 0.6 cm long) received daily intraperitoneal (i.p.) injections of vehicle, ES and FS (10 µg/g body weight) for 31 d. FS had a potent effect in inhibiting the growth and progression of PC-3 tumors. Our results indicate that FS may be useful for inhibiting human prostate tumors growth.
authors.affiliation: Guangdong Food and Drug Vocational College.
authors.forename: Dai-Ying
authors.initials: DY
authors.lastname: Zhou
authors.forename: Ning
authors.initials: N
authors.lastname: Ding
authors.forename: Jeremiah
authors.initials: J
authors.lastname: Van Doren
authors.forename: Xing-Chuan
authors.initials: XC
authors.lastname: Wei
authors.forename: Zhi-Yun
authors.initials: ZY
authors.lastname: Du
authors.forename: Allan H
authors.initials: AH
authors.lastname: Conney
authors.forename: Kun
authors.initials: K
authors.lastname: Zhang
authors.forename: Xi
authors.initials: X
authors.lastname: Zheng
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003474:Curcumin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D015870:Gene Expression / Q000187:drug effects; D017930:Genes, Reporter; D006801:Humans; D008297:Male; D016513:Mice, SCID; D015394:Molecular Structure; D016328:NF-kappa B / Q000235:genetics / Q000378:metabolism; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D011944:Receptors, Androgen / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D013739:Testosterone / Q000494:pharmacology; D023041:Xenograft Model Antitumor Assays
chemical_list: D016328:NF-kappa B; D011944:Receptors, Androgen; D013739:Testosterone; D003474:Curcumin