著者
Satoshi Yamaori Yoshimi Okushima Kazufumi Masuda Mika Kushihara Takashi Katsu Shizuo Narimatsu Ikuo Yamamoto Kazuhito Watanabe
出版者
公益社団法人日本薬学会
雑誌
Biological and Pharmaceutical Bulletin (ISSN:09186158)
巻号頁・発行日
vol.36, no.7, pp.1197-1203, 2013-07-01 (Released:2013-07-01)
参考文献数
39
被引用文献数
2 or 0

Our recent work has shown that cannabidiol (CBD) exhibits the most potent direct inhibition of human cytochrome P450 1A1 (CYP1A1) among the CYP enzymes examined. However, the mechanism underlying this CBD inhibition remains to be clarified. Thus, to elucidate the structural requirements for the potent inhibition by CBD, the effects of CBD and its structurally related compounds on CYP1A1 activity were investigated with recombinant human CYP1A1. Olivetol, which corresponds to the pentylresorcinol moiety of CBD, inhibited the 7-ethoxyresorufin O-deethylase activity of CYP1A1; its inhibitory effect (IC50=13.8 µM) was less potent than that of CBD (IC50=0.355 µM). In contrast, d-limonene, which corresponds to the terpene moiety of CBD, only slightly inhibited CYP1A1 activity. CBD-2′-monomethyl ether (CBDM) and CBD-2′,6′-dimethyl ether inhibited CYP1A1 activity with IC50 values of 4.07 and 23.0 µM, respectively, indicating that their inhibitory effects attenuated depending on the level of methylation on the free phenolic hydroxyl groups in the pentylresorcinol moiety of CBD. Cannabidivarin inhibited CYP1A1 activity, although its inhibitory potency (IC50=1.85 µM) was lower than that of CBD. The inhibitory effects of Δ9-tetrahydrocannabinol and cannabielsoin (IC50s ≈10 µM), which contain a free phenolic hydroxyl group and are structurally constrained, were less potent than that of CBDM, which contains a free phenolic hydroxyl group and is rotatable between pentylresorcinol and terpene moieties. These results suggest that the pentylresorcinol structure in CBD may have structurally important roles in direct CYP1A1 inhibition, although the whole structure of CBD is required for overall inhibition.
著者
柴田 承二
出版者
公益社団法人日本薬学会
雑誌
ファルマシア (ISSN:00148601)
巻号頁・発行日
vol.34, no.2, pp.156-161, 1998-02-01
被引用文献数
1 or 0
著者
大橋 一智 上田 浩史 山崎 正利 木村 貞夫 安部 茂 山口 英世
出版者
公益社団法人日本薬学会
雑誌
藥學雜誌 (ISSN:00316903)
巻号頁・発行日
vol.112, no.12, pp.919-925, 1992-12-25
被引用文献数
19 or 0

The biological activity of a preparation of heat killed cells of Enterococcus faecalis, FK-23 which was isolated from the feces of a healthy human, was investigated in C3H/He mice. Intraperitoneal injection of the preparation caused an accumulation of neutrophils and macrophages in the peritoneal cavity of the mice 6 h later. As a parameter of the activation of macrophages, the effect of the FK-23 preparation on the production of tumor necrosis factor (TNF) was examined. The mice were given two consecutive intravenous injections of the preparation at a dose of 10μg/mouse and, 3 h later, of 300μg/mouse. The TNF level in the sera reached 99 U/ml in mice 2 h after the second injection. This preparation also stimulated peritoneal macrophages to produce TNF in vitro and increased the capacity of neutrophils to adhere to plastic plates and to release active oxygens, but did not induce blastogenic transformation of lymphocytes. These results suggest that the FK-23 preparation is a biological response modifier (BRM) with various activities on phagocytes similar to a streptococcal antitumor agent, OK432.
著者
金庭 延慶
出版者
公益社団法人日本薬学会
雑誌
ファルマシア (ISSN:00148601)
巻号頁・発行日
vol.15, no.10, pp.936-940, 1979-10-01
著者
野口 照久 原 博
出版者
公益社団法人日本薬学会
雑誌
ファルマシア (ISSN:00148601)
巻号頁・発行日
vol.32, no.1, pp.19-23, 1996-01-01
著者
乙黒 一彦
出版者
公益社団法人日本薬学会
雑誌
ファルマシア (ISSN:00148601)
巻号頁・発行日
vol.41, no.6, pp.551-554, 2005-06-01
著者
手塚 雅勝 鈴木 弘美 鈴木 康夫 原 征彦 岡田 昌二
出版者
公益社団法人日本薬学会
雑誌
衛生化学 (ISSN:0013273X)
巻号頁・発行日
vol.43, no.5, pp.311-315, 1997-10-31
被引用文献数
10 or 0

The effects of catechins obtained from the hot water extract of green tea leaves on two human type-A influenza virus strains of Aichi/2/68 and PR/8/34 were studied. In this study, (-)-epicatechin (EC), (-)-epigallocatechin (EGC), (-)-epicatechin gallate (ECg), (-)-epigallocatechin gallate (EGCg), the crude catechins containing these catechins and (+)-catechin were used. Consequently it was observed that catechins used in this study had an inhibitory effect on the hemolytic activity to red blood cells induced by these two type-A virus strains under acidic conditions (pH 5.1 or 5.4) although they did not have an influence on the agglutination activity to red blood cells induced by the same virus strains. After incubation of (-)-ECg and (-)-EGCg with A/Aichi/2/68 virus, MDCK cells, virus-sensitive cells, were infected with the virus and the ability of virus proliferation was measured in terms of an index of the agglutination activity of the virus to red blood cells. The used two catechins, (-)-ECg and (-)-EGCg, inhibited the virus proliferation at concentrations of 100μg/ml and 50μg/ml, respectively. Furthermore, at a concentration of 2.0 mg/ml these two catechins were found to inhibit the activity of neuraminidase on the surface of the virus membrane by 71.3% and 60.8%, respectively. From the above-mentioned results, it is considered that among the catechins contained in green tea leaves, such two catechins as (-)-ECg and (-)-EGCg inhibit the activity of neuraminidase present on the surface of human influenza virus in order to block the invasion of the influenza virus into virus-sensitive cells.
著者
木曽 良明
出版者
公益社団法人日本薬学会
雑誌
ファルマシア (ISSN:00148601)
巻号頁・発行日
vol.36, no.7, pp.652-653, 2000-07-01
著者
久保寺 昭子 毛利 哲郎 鶴藤 丞
出版者
公益社団法人日本薬学会
雑誌
藥學雜誌 (ISSN:00316903)
巻号頁・発行日
vol.87, no.5, pp.511-515, 1967-05-25

Effect of 10 chelating agents on the excretion of radiostrontium from the body was investigated in mice. Sodium salts and/or monocalcium-sodium salts of these chelating agents were used as test materials. Preliminery toxicity tests were carried out to estimate their approximate maximum safety doses. The sodium salts were generally more toxic and brought about some convulsion with occasional death which were attributed to the decrease of Ca^<2+> ion in the blood. The monocalcium-sodium salts were applicable in 10-folds as compared with their equivalent sodium salts. The chelating agents and radioactive strontium were simultaneously injected into different parts of the body. The animals were killed 24 hours after the injection, and then reduced to ashes individually in an electric furnace after removing the digestive tracts and bladders. Radioactivity of the ashes was assayed to determine the percentage retention of radioactive strontium in the carcasses. Monocalcium-disodium salt of bis(dicarboxyaminoethyl) ether was found to be one of the most effective agents, same as calcium sodium citrate which had been previously reported.
著者
瀬川
出版者
公益社団法人日本薬学会
雑誌
藥學雜誌 (ISSN:00316903)
巻号頁・発行日
no.224, pp.1001-1002, 1900-10-26
著者
高橋 三雄 大沢 啓助 蔡 哲宗 阿部 昌宏
出版者
公益社団法人日本薬学会
雑誌
藥學雜誌 (ISSN:00316903)
巻号頁・発行日
vol.100, no.2, pp.221-223, 1980-02-25

Nine kinds of fatty acids, fifteen hydrocarbons, three sterols, and six amino acids were detected by gas chromatography-mass spectrometry and amino acid analysis, from the dried fruits of Capsicum annuum L. var. fasciculatum IRISH. The distribution of N-(13-methyltetradecyl) acetoamide isolated from Capsicum annuum L., and named Capsi-amide, was investigated in four varieties of Capsicum annuum L., i.e. C. annuum L. var. fasciculatum IRISH, var. grossum SENDT., var. longum SENDT., and var. minimum ROXB. Capsi-amide was detected in all four varieties.
著者
上杉 志成
出版者
公益社団法人日本薬学会
雑誌
ファルマシア (ISSN:00148601)
巻号頁・発行日
vol.44, no.5, pp.463-464, 2008-05-01