Tryptanthrin-loaded nanoparticles for delivery into cultured human breast cancer cells, MCF7: the effects of solid lipid/liquid lipid ratios in the inner core.

abstract：:We have identified a novel cardiac steroid, 11,19-epoxy-19-methoxytelocinobufagin, named marinosin (1), in the skin of the toad, Bufo marinus (L.) Schneider. The treatment of compound 1 with 50% CH3CN containing 0.1% trifluoroacetic acid yielded a 11 alpha-hydroxyhellebrigenin (2), which has not previously been isolat...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsukawa M,Akizawa T,Ohigashi M,Morris JF,Butler VP Jr,Yoshioka M

更新日期：1997-02-01 00:00:00

abstract：:To reverse the adverse reactions of alkylxanthines and to develop novel inhibitors of cyclic AMP phosphodiesterase 4 (PDE4), a series of heterocycle [a]-, [b]-, [c,d]-, and [i]-condensed purines were designed and synthesized. Although all compounds did not display PDE1 and PDE3 inhibitory activities, several heterocyc...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki H,Yamamoto M,Shimura S,Miyamoto K,Yamamoto K,Sawanishi H

更新日期：2002-09-01 00:00:00

abstract：:Orally disintegrating tablets (ODTs) are useful for improving benefits for patients of various ages. Masking the unpleasant taste of a drug is an important factor in the compliance of patients who take ODTs. We evaluated the taste acceptability effects of various taste-masking methods on bitter famotidine ODTs as a cl...

journal_title：Chemical & pharmaceutical bulletin

authors： Sugiura T,Uchida S,Namiki N

更新日期：2012-01-01 00:00:00

abstract：:The interaction of halofantrine with phosphatidylcholine and phosphatidylethanolamine bilayers has been investigated by differential scanning calorimetry. Halofantrine caused a broadening of the gel to liquid crystalline phase transition endotherm of the phosphatidylcholines. A decrease in the transition temperature T...

journal_title：Chemical & pharmaceutical bulletin

authors： Lim LY,Go ML

更新日期：1999-06-01 00:00:00

abstract：:New five seven-membered vibsane-type diterpenes named 5-epi-vibsanin C, 5-epi-vibsanin H, 5-epi-vibsanin K, 18-O-methyl-5-epi-vibsanin K and 5-epi-vibsanin E have been isolated from the leaves of Viburnum awabuki (Caplifoliaceae). Their structures have been elucidated by analyses of spectroscopic data and comparison o...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukuyama Y,Minami H,Matsuo A,Kitamura K,Akizuki M,Kubo M,Kodama M

更新日期：2002-03-01 00:00:00

abstract：:A series of 4-aza-5 alpha-androstane compounds with one or two aromatic moieties in the carbamoyl group at the C-17 position were synthesized and their inhibitory activities for rat and human prostatic testosterone 5 alpha-reductase were tested in vitro. Compounds with one aromatic moiety in the carbamoyl group showed...

journal_title：Chemical & pharmaceutical bulletin

authors： Kurata H,Ishibashi K,Saito S,Hamada T,Horikoshi H,Furukawa Y,Kojima K

更新日期：1996-01-01 00:00:00

abstract：:Alpha-trifluoromethyl allenol ethers 9a-e were prepared in moderate to good yields by the Julia-Lythgoe process using beta-ethoxy-beta-trifluoromethyl vinylic sulfone 3. Several reactions of 9c were examined to give alpha,beta-unsaturated trifluoromethyl ketone derivatives 11 and 12. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshimatsu M,Hibino M

更新日期：2000-09-01 00:00:00

abstract：:Thioglycosides are available donors in glycosylation due to the stability of the anomeric C-S bond under general reaction conditions of protection and deprotection, and offer orthogonality in their activation. We report now that the hypervalent iodine effectively induced glycosylation reaction of thioglycosides with v...

journal_title：Chemical & pharmaceutical bulletin

authors： Kajimoto T,Morimoto K,Ogawa R,Dohi T,Kita Y

更新日期：2016-01-01 00:00:00

abstract：:Two new iridoid glycosides, 7 beta,8 beta-epoxy-8 alpha-dihydrogeniposide (1) and 8-epiapodantheroside (2), were isolated, together with six known (3-8) and three artifact (9-11) iridoids, from the leaves of Gardenia jasminoides cv. fortuneana Hara. Their structures were established based on chemical and spectral data...

journal_title：Chemical & pharmaceutical bulletin

authors： Machida K,Takehara E,Kobayashi H,Kikuchi M

更新日期：2003-12-01 00:00:00

abstract：:The full structures of the two steroidal saponins from Narthecium asiaticum MAXIM. We previously identified as toxic substances by monitoring the toxicity in guinea pigs were phytochemically reinvestigation on the aerial parts of the plant. The desired toxic saponins (6,7) were isolated together with two known lignan ...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue T,Mimaki Y,Sashida Y,Kobayashi M

更新日期：1995-07-01 00:00:00

abstract：:To develop non-prodrugs of taxoids with satisfactory stability in vivo, high water-solubility, and potent antitumor activity, we prepared several 10-O-sec-aminoethyl docetaxel analogs (3) and evaluated their cytotoxicity against mouse leukemia and human tumor cell lines, microtubule disassembly-inhibitory activity, an...

journal_title：Chemical & pharmaceutical bulletin

authors： Uoto K,Takenoshita H,Yoshino T,Hirota Y,Ando S,Mitsui I,Terasawa H,Soga T

更新日期：1998-05-01 00:00:00

abstract：:We discovered that the reactivity of some conjugated and electron-deficient hydrocarbons was quite different in the presence of transition metal catalysts. In this review we report our development and applications of the highly selective palladium and nickel-catalyzed cycloaddition reactions of unsaturated hydrocarbon...

journal_title：Chemical & pharmaceutical bulletin

authors： Saito S

更新日期：2005-09-01 00:00:00

abstract：:A series of new (5R,8R,10R)-ergoline derivatives was synthesized, and their antihypertensive and dopaminergic activities were tested in conscious spontaneously hypertensive rats and in rats with unilateral 6-hydroxydopamine-induced lesions of the substantia nigra. (5R,8R,10R)-6-Alkyl-8-ergolinemethanols, prepared from...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohno S,Adachi Y,Koumori M,Mizukoshi K,Nagasaka M,Ichihara K,Kato E

更新日期：1994-07-01 00:00:00

abstract：:Fluorescence assays are useful tools for estimating enzymatic activity. Their simplicity and manageability make them suitable for screening enzyme inhibitors in drug discovery studies. However, researchers need to pay attention to compounds that show auto-fluorescence and quench fluorescence, because such compounds lo...

journal_title：Chemical & pharmaceutical bulletin

authors： Itoh Y,Suzuki M,Matsui T,Ota Y,Hui Z,Tsubaki K,Suzuki T

更新日期：2016-01-01 00:00:00

abstract：:Transfer of aprindine from the blood into the intestinal lumen or into the peritoneal cavity was examined after intravenous administration of the drug at a dose of 5 mg/kg in rats. The amount of the drug transferred from the blood into the intestinal lumen was much greater than into the peritoneal cavity. The average ...

journal_title：Chemical & pharmaceutical bulletin

authors： Arimori K,Hashimoto Y,Nakano M

更新日期：1991-12-01 00:00:00

abstract：:2,3-Epoxy-4-hydroxy-4-((E,E)-3,6-octadienyl)cyclopentanone (dl-carbacerulenin 5) was synthesized via the epoxyketones 15a and 15b as a mimic of the active form of the antibiotics cerulenin 1, a potent inhibitor of fatty acid synthetase (FAS). The monobenzyl ethers (12 and 13), synthetic intermediates of 15, were prepa...

journal_title：Chemical & pharmaceutical bulletin

authors： Shimazawa R,Ogawa Y,Morisaki N,Funabashi H,Kawaguchi A,Iwasaki S

更新日期：1992-11-01 00:00:00

abstract：:Clotrimazole (CT)-containing proliposomes were prepared by penetrating an ethanol solution of CT and Egg phosphatidylcholine (PC) into microporous sorbitol particles, followed by vacuum evaporation of the solvent. As a result, CT proliposomes with free-flowing flowability were obtained. On contact with water, the prol...

journal_title：Chemical & pharmaceutical bulletin

authors： Ning MY,Guo YZ,Pan HZ,Yu HM,Gu ZW

更新日期：2005-06-01 00:00:00

abstract：:Using CPG support linked with 5-deazaflavin, the 5-deazaflavin modified oligodeoxynucleotides at 3'-end(ODN-dF1) were synthesized. The thermal stability of the duplex of ODN-dF1 with its complement was higher than that of oligonucleotide linked to 5-deazaflavin at 5'-end internucleotide linkage. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakamura Y,Akiyama T,Bessho K,Yoneda F

更新日期：1993-07-01 00:00:00

abstract：:A model based on solubility parameters is proposed to predict the solubility curves of antihelmintic drugs at several temperatures, including aqueous and non-aqueous mixtures. The solubility of the drugs was measured in ethanol-water and ethanol-ethyl acetate mixtures at 15-35 degrees C (mebendazole) and at 25 degrees...

journal_title：Chemical & pharmaceutical bulletin

authors： Bustamante P,Muela S,Escalera B,Peña A

更新日期：2010-05-01 00:00:00

abstract：:Peptides mimicking chemokine receptor CCR5 were synthesized and their anti-HIV-1 activities evaluated. Prepared compounds, especially a sulfated derivatives, showed significant anti-HIV-1 activities. Furthermore, a hybrid molecule linked to an N-carbomethoxycarbonyl-prolyl-phenylalanine (CPF) moiety had a greater effe...

journal_title：Chemical & pharmaceutical bulletin

authors： Konishi K,Ikeda K,Achiwa K,Hoshino H,Tanaka K

更新日期：2000-02-01 00:00:00

abstract：:An antibiotic formycin A inhibited growth of Vibrio parahaemolyticus under certain conditions, which suggested that formycin A was taken up by cells under these conditions. We found that formycin A was transported via the adenosine transport system which we previously reported as a Na(+)-coupled cotransport system. We...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakai-Tomita Y,Mitani Y,Tsuda M,Tsuchiya T

更新日期：1991-05-01 00:00:00

abstract：:An effective procedure for decontamination of beta-lactam antibiotic residues or contaminants in the pharmaceutical manufacturing environment was investigated. Decontamination with solutions of hydrochloric acid, sodium hydroxide, hydrogen peroxide and hydroxylamine as agents for degradation was assessed. According to...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukutsu N,Kawasaki T,Saito K,Nakazawa H

更新日期：2006-09-01 00:00:00

abstract：:We designed and synthesized a new class of peptidomimetic human immunodeficiency virus protease inhibitors containing a unique unnatural amino acid, allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid], with a hydroxymethylcarbonyl isostere as the active moiety. From a structure-activity relatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Mimoto T,Hattori N,Takaku H,Kisanuki S,Fukazawa T,Terashima K,Kato R,Nojima S,Misawa S,Ueno T,Imai J,Enomoto H,Tanaka S,Sakikawa H,Shintani M,Hayashi H,Kiso Y

更新日期：2000-09-01 00:00:00

abstract：:To search for compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, ten 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline sulfonates (4a-j) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Some compounds demonstrated anti-HIV-1 activity, especially 5,...

journal_title：Chemical & pharmaceutical bulletin

authors： Zeng XW,Huang N,Xu H,Yang WB,Yang LM,Qu H,Zheng YT

更新日期：2010-07-01 00:00:00

abstract：:Inhibitors of delta 4-3-ketosteroid (5 alpha) reductase, which had been prepared from rat prostate and converted testosterone to 5 alpha-dihydrotestosterone and 4-androstene-3,17-dione, were isolated from 50% ethanol extract of Populus nigra. They were identified as pinobanksin (I, 3,5,7-trihydroxyflavanone), 3,7-dime...

journal_title：Chemical & pharmaceutical bulletin

authors： Komoda Y

更新日期：1989-11-01 00:00:00

abstract：:Mycalamide A and mycalamide B, isolated as antiviral and antitumor agents from a New Zealand sponge of the genus Mycale, converted the morphology of ras-transformed NRK-cells to normal morphology at 10 and 1 ng/ml, respectively. The effect on protein synthesis suggests that these agents converted the morphology by pre...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogawara H,Higashi K,Uchino K,Perry NB

更新日期：1991-08-01 00:00:00

abstract：:A fragment analog, [D-Arg30]prothymosin alpha fragment 1-30, containing D-arginine in place of arginine residue at position 30 was synthesized by the liquid phase procedure and studied for immunological effect on the impaired blastogenic response of T-lymphocytes isolated from uremic patients after treatment of human ...

journal_title：Chemical & pharmaceutical bulletin

authors： Abiko T,Sekino H

更新日期：1991-03-01 00:00:00

abstract：:A series of 2-(4-methylphenyl)benzothiazoles was synthesized and evaluated using an adjuvant-induced arthritic rat model. This class of desired compounds affecting the immune response was found using hemagglutination assay. 4-Acetoxy-2-(4-methylphenyl)benzothiazole (7m), KB-2683, was most potent in the adjuvant-induce...

journal_title：Chemical & pharmaceutical bulletin

authors： Hori N,Tsukamoto G,Imamura A,Ohashi M,Saito T,Yoshino K

更新日期：1992-09-01 00:00:00

abstract：:A powder solid dispersion system (SD) of indomethacin (IM) with crospovidone (CrosPVP) possesses good fluidity and can be used for tablet formulation. Tablets of SD can be prepared by direct compression and have adequate hardness and a small variation in weight. Forces during the tableting process were measured with a...

journal_title：Chemical & pharmaceutical bulletin

authors： Shibata Y,Fujii M,Okada H,Noda S,Kondoh M,Watanabe Y

更新日期：2005-07-01 00:00:00

abstract：:Several kinds of loline-type alkaloids, norloline, loline, N-acetylnorloline, N-acetylloline, N-formylnorloline, N-formylloline and N-methylloline were detected in the urine of race-horses. Furthermore, a new compound of the alkaloids, N-senecioylnorloline, was also found and identified. These compounds were mainly id...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeda A,Suzuki E,Kamei K,Nakata H

更新日期：1991-04-01 00:00:00