2. Academic Validation
  3. Hybrids of 3alpha-methoxyserrat-14-en-21beta-ol (PJ-1) and 3beta-methoxyserrat-14-en-21beta-ol (PJ-2) and various anti-oxidants as cancer chemopreventive agents

Hybrids of 3alpha-methoxyserrat-14-en-21beta-ol (PJ-1) and 3beta-methoxyserrat-14-en-21beta-ol (PJ-2) and various anti-oxidants as cancer chemopreventive agents

  • Eur J Med Chem. 2010 Jun;45(6):2191-7. doi: 10.1016/j.ejmech.2010.01.057.
Hiroko Tsujii 1,  Takeshi Yamada,  Tetsuya Kajimoto,  Reiko Tanaka,  Harukuni Tokuda,  Junya Hasegawa,  Yoshio Hamashima,  Manabu Node
Affiliations

Affiliation

  • 1 Laboratory of Medicinal Chemistry, Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
PMID: 20153563 DOI: 10.1016/j.ejmech.2010.01.057
Abstract

3alpha-methoxyserrat-14-en-21beta-ol (1) and 3beta-methoxyserrat-14-en-21beta-ol (2) and their conjugates with curcumin, kojic acid, quercetin, and baicalein (3-18), as well as new analogs (19-24) derived from 1 and 2, were tested for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA). The inhibitory effects of 16 (IC50=330 mol ratio/32 pmol/TPA), 9 (IC50=335), 10 (IC50=338), and 15 (IC50=350) were stronger than those of the Other compounds and the positive control, oleanolic acid (IC50=449). Compounds 15 and 16, which are conjugates of one molecule each of 1 or 2 and quercetin, inhibited mouse skin tumor promotion in an in vivo two-stage carcinogenesis model. The in vivo two-stage mouse skin carcinogenesis test employed 7,12-dimethylbenz[a]anthracene (DMBA) as an initiator and TPA as a promoter.

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