Anti‐Initiating Activity of 3β‐Methoxy‐13α,14α‐epoxyserratan‐21β‐ol (PJJ‐34) from the Stem Bark of Picea jezoensis Carr. var. jezoensis

Abstract

Ultraviolet light is the major cause of skin cancers in human, and several effects of ultraviolet light B (UVB) are thought to contribute to skin photocarcinogenesis. 3Beta-methoxy-13alpha,14alpha-epoxyserratan-21beta-ol (PJJ-34; 1) isolated from Picea jezoensis Carr. var. jezoensis showed the strongest antitumor-promoting activity among naturally occurring triterpenoids in the in vivo two-stage mouse skin-carcinogenesis test. To investigate the anti-initiating activity, we further studied mouse models initiated with ultraviolet-B (UVB) and promoted with 12-O-tetradecanoylphorbol-13-acetate (TPA). Oral administration of the PJJ-34 (1) during a period before and after the three times of UVB irradiation led to a remarkable effect: oral administration of a 0.0025% solution of 1 only to the test group, which started one week before and ended one week after the irradiation, showed less than half papillomas, and inhibition of tumor incidence and tumor multiplicity in comparison to the control group. Therefore, it was recognized that PJJ-34 (1) showed strong anti-initiating activity as well as anti-promoting activity. After all, 1 seems to be useful as cancer-chemopreventive agent.

New Serratene Triterpenoids from Palhinhaea cernua and Their Cytotoxic Activity

“…The complement system plays a significant role in the host defense. It can be activated by a cascade mechanism involving either the classical pathway (CP), the alternative pathway (AP), or the mannan binding lectin/MBL-associated serine protease (MBL/MASP) pathway [1]. The 30 odd complement fragments that make up the system include proteolytic pro-enzymes, nonenzymatic components that form functional complexes, cofactors, regulators, and receptors [2].…”

“…The serratene group is a unique family of pentacyclic triterpenoids possessing seven to five tertiary methyl groups and a central seven-membered ring C, some of which showed important pharmacological activities [1][2][3]. This group of triterpenoids was mainly discovered from plants belonging to the Pinaceae, Huperziaceae, and Lycopodiaceae families, together with a few other plant species, e.g., Primula rosea [4], Imperata cylindrical [5], Polypodium vulgare [6], and Lemmaphyllum microphyllum [7].…”

Anti‐Tumor‐Initiating Effects of Spiro‐biflavonoids from Abies sachalinensis

“…jezoensis (Japanese name: Ezomatsu), and have isolated several triterpenoids including 13a,14a-epoxy-3b-methoxyserratan-21b-ol (PJJ-34) from the CHCl 3 extract [3 -5], and 23 phenolic compounds, including flavonostilbenes and stilbene dimers [6] [7]. In our previous publication of their biological activities, we have reported that PJJ-34 can inhibit carcinogenesis in both cancer initiation and promotion periods in the in vivo two-stage mouse skin carcinogenesis test [8] [9], and that the phenolic compounds have potent radical-scavenging activities against 1,1-diphenyl-2-picrylhydrazyl (DPPH) and superoxide anion radicals [6], and the anti-tumor-initiating activity [7]. Our continuing…”