Author: Hiroko Tsujii ; Harukuni Tokuda ; Reiko Tanaka ; Tetsuya Kajimoto ; Yoshio Hamashima ; Junya Hasegawa ; Nobutaka Suzuki ; Takeshi Yamada ; Takanari Arai ; Manabu Node

3α-Methoxyserrat-14-en-21β-ol (PJ-1) and 3β-methoxyserrat-14-en-21β-ol (PJ-2) were conjugated with well-known phenolic compounds, narigenin, hesperetin, genistein, and daidzein (1-8). Other conjugates of PJ-2-3,5-dihydroxy-4-methoxybenzoic acid (9), PJ-2-pyrogallol (10), and derivatives of PJ-1, PJ-2-3,3-dimethyl-succinates (11, 12), PJ-1, PJ-2-succinates (13, 14), PJ-2-glycine (15), PJ-2-piperidine acetic acid (16), and PJ-1 epoxy-3,3-dimethyl-succinate (17) 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 11 (IC(50) = 251), 12 (IC(50) = 248), and 17 (IC(50) = 230 mol ratio/32 pmol/TPA), were 2-fold stronger than those of the other compounds such as oleanolic acid (IC(50) = 449). Compounds 10, 11, and 17 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.

01 Jun 2008·Food and Chemical ToxicologyQ2 · MEDICINE

Chemopreventive effects of a serratane-type triterpenoid, 3α-methoxyserrat-14-en-21β-ol (PJ-1), against rat lung carcinogenesis

Q2 · MEDICINE

Article

Author: Shoji Fukushima ; Reiko Tanaka ; Chiharu Yamaguchi ; Hideki Wanibuchi ; Anna Kakehashi

Our efforts to search for cancer-chemopreventive agents have been focused on constituents from materials of trees such as leaves and bark as waste in the forestry industry. Cancer-chemopreventive effects of a serratane-type triterpenoid from the bark of Picea jezoensis, 3alpha-methoxyserrat-14-en-21beta-ol (PJ-1), were here examined in a revised rat multi-organ carcinogenesis (DMBDD) model. Male 6-week-old F344 rats received combined treatment with five different carcinogens and starting 1 week thereafter were administered PJ-1 at a dose of 2mg/kg or 6mg/kg body wt i.g. (five times/week) or the vehicle as a control (1ml of 0.5% CMC). At the termination at week 30, significant decrease of adenomas (P<0.01) and total tumors (P<0.01) and a trend for reduction of adenocarcinoma multiplicity in the lung were observed, but without any modulating influence in other major organs. The cell proliferation indices in the lungs tended to be decreased in the PJ-1 administered groups, with apparent induction of CYP2B1/2 mRNA expression to recover the values observed in non-initiated controls. These results indicate that PJ-1 exerts cancer-chemopreventive effects on rat lung carcinogenesis after multi-organ initiation.

01 Jan 1998·Biological and Pharmaceutical BulletinQ4 · MEDICINE

Antiplatelet Action of 3',4'-Diisovalerylkhellactone Diester Purified from Peucedanum japonicum Thunb.

Q4 · MEDICINE

Article

Author: Che Ming Teng ; Ting Ting Jong ; Feng Nien Ko ; George Hsiao

3',4'-Diisovalerylkhellactone diester (PJ-1) is a coumarin derivative purified from the medicinal herb Peucedanum japonicum Thunb. We examined its in vitro effects on various aspects of platelet reactivity. PJ-1 inhibited the aggregation and ATP release of rabbit platelets induced by PAF (platelet-activating factor) and collagen. The IC50 values of PJ-1 and BN52021 on PAF (2 ng/ml)-induced platelet aggregation were about 56.3 and 22.0 microM, respectively. And, the IC50 value of PJ-1 toward collagen (10 microg/ml)-induced platelet aggregation was 89.4 microM. Although the platelet aggregation caused by arachidonic acid and thrombin were barely inhibited by PJ-1, the release reactions were partially suppressed. PJ-1 also inhibited the thromboxane B2 formation caused by collagen, while formations of thromboxane B2 and prostaglandin D2 caused by arachidonic acid were not affected. The phosphoinositide breakdown caused by PAF was inhibited by PJ-1, but those by other inducers were not affected significantly. PJ-1 inhibited the intracellular Ca2+ increase caused by PAF in fura-2-loaded platelets. PJ-1 also concentration-dependently inhibited [3H]PAF (3.03 ng/ml) binding to washed platelets with an IC50 value of 3.9 microM. It is concluded that the main antiplatelet effect of PJ-1 may be due to dual activities on the blockade of PAF receptor-induced activation and also the inhibition of phospholipase A2 in rabbit platelets.

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Indication	Highest Phase	Country/Location	Organization	Date
Dermatitis, Atopic	Preclinical	China	Jiangnan University	29 Feb 2024

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