PMID- 24647337 OWN - NLM STAT- MEDLINE DCOM- 20150120 LR - 20190720 IS - 1347-5215 (Electronic) IS - 0918-6158 (Linking) VI - 37 IP - 6 DP - 2014 TI - Effects of curcumin analogues for inhibiting human prostate cancer cells and the growth of human PC-3 prostate xenografts in immunodeficient mice. PG - 1029-34 AB - 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-kappaB) 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 microg/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. FAU - Zhou, Dai-Ying AU - Zhou DY AD - Guangdong Food and Drug Vocational College. FAU - Ding, Ning AU - Ding N FAU - Van Doren, Jeremiah AU - Van Doren J FAU - Wei, Xing-Chuan AU - Wei XC FAU - Du, Zhi-Yun AU - Du ZY FAU - Conney, Allan H AU - Conney AH FAU - Zhang, Kun AU - Zhang K FAU - Zheng, Xi AU - Zheng X LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20140319 PL - Japan TA - Biol Pharm Bull JT - Biological & pharmaceutical bulletin JID - 9311984 RN - 0 (NF-kappa B) RN - 0 (Receptors, Androgen) RN - 3XMK78S47O (Testosterone) RN - IT942ZTH98 (Curcumin) SB - IM MH - Animals MH - Apoptosis/*drug effects MH - Cell Line, Tumor MH - Cell Survival/drug effects MH - Curcumin/*analogs & derivatives/chemistry/*pharmacology/therapeutic use MH - Dose-Response Relationship, Drug MH - Gene Expression/drug effects MH - Genes, Reporter MH - Humans MH - Male MH - Mice, SCID MH - Molecular Structure MH - NF-kappa B/genetics/metabolism MH - Prostatic Neoplasms/*drug therapy/metabolism/pathology MH - Receptors, Androgen/genetics/metabolism MH - Structure-Activity Relationship MH - Testosterone/pharmacology MH - Xenograft Model Antitumor Assays EDAT- 2014/03/22 06:00 MHDA- 2015/01/21 06:00 CRDT- 2014/03/21 06:00 PHST- 2014/03/21 06:00 [entrez] PHST- 2014/03/22 06:00 [pubmed] PHST- 2015/01/21 06:00 [medline] AID - DN/JST.JSTAGE/bpb/b14-00044 [pii] AID - 10.1248/bpb.b14-00044 [doi] PST - ppublish SO - Biol Pharm Bull. 2014;37(6):1029-34. doi: 10.1248/bpb.b14-00044. Epub 2014 Mar 19.