Antitumor agents. 169 Dysoxylum cumingianum. V. Cumingianosides P and Q, new cytotoxic triterpene glucosides with an apotirucallane-type skeleton from Dysoxylum cumingianum.

abstract：:Bromination of 17-O-acetyltestosterone (17beta-acetoxyandrost-4-en-3-one) (1) was performed with 1, 5, and 10 eq of Br2 in AcOH-Et2O at room temperature. In all cases 2alpha,6beta- (2) and 2alpha,6beta-dibromo-17beta-acetoxyandrost-4-en-3-one (3) were obtained, although the yields were dependent upon the conditions us...

journal_title：Chemical & pharmaceutical bulletin

authors： Shimizu T,Tobari A,Koyanagi J,Kawase M,Saito S

更新日期：2001-01-01 00:00:00

abstract：:Biological activity of thioaurones was not tested so far and the group constitute completely unexplored source of new molecules of pharmacological interest. We report synthesis and evaluation of cytotoxic activity of thioaurone derivatives bearing p-hydroquinone system in ring A. Their activity was found to depend str...

journal_title：Chemical & pharmaceutical bulletin

authors： Konieczny MT,Konieczny W,Okabe S,Tsujimoto H,Suda Y,Wierzba K

更新日期：2006-03-01 00:00:00

abstract：:Two new flavonoid glycosides, 5-hydroxy-7,8-dimethoxy (2R)-flavanone-5-O-beta-D-glucopyranoside (1) and 5-hydroxy-7,8,2',5'-tetramethoxy-flavone-5-O-beta-D-glucopyranoside (2), and a new diterpenoid, andrographic acid (3), along with andrographidine A (4) were isolated from Andrographis paniculata, and their structure...

journal_title：Chemical & pharmaceutical bulletin

authors： Li W,Xu X,Zhang H,Ma C,Fong H,van Breemen R,Fitzloff J

更新日期：2007-03-01 00:00:00

abstract：:Isoliquiritigenin, glabridin, licoarylcoumarin and licoricidin were identified as strong inhibitors of adenosine 3',5'-cyclic monophosphate (cAMP) phosphodiesterase in waste materials which were obtained during the industrial extraction of glycyrrhizin from licorice roots. The structure-activity relationships of 12 fl...

journal_title：Chemical & pharmaceutical bulletin

authors： Kusano A,Nikaido T,Kuge T,Ohmoto T,Delle Monache G,Botta B,Botta M,Saitoh T

更新日期：1991-04-01 00:00:00

abstract：:A novel cytolytic factor, dolabellanin P, was purified to apparent homogeneity from the purple fluid of the sea hare, Dolabella auricularia. Purified dolabellanin P is a single polypeptide of 60 kDa. The amino acid composition and the N-terminus of the factor were also determined. This factor nonspecifically lysed all...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamazaki M,Tansho S,Kisugi J,Muramoto K,Kamiya H

更新日期：1989-08-01 00:00:00

abstract：:A novel lead compound, N-(3-[4-(4-fluorobenzoyl)piperidin-1-yl]propyl)-1-methyl-5-oxo-N-phenylpyrrolidine-3-carboxamide (1), was identified as a CCR5 antagonist by high-throughput screening using [(125)I]RANTES and CCR5-expressing CHO cells. The IC(50) value of 1 was 1.9 microM. In an effort to improve the binding aff...

journal_title：Chemical & pharmaceutical bulletin

authors： Imamura S,Ishihara Y,Hattori T,Kurasawa O,Matsushita Y,Sugihara Y,Kanzaki N,Iizawa Y,Baba M,Hashiguchi S

更新日期：2004-01-01 00:00:00

abstract：:A convenient synthesis of immunosuppressive agent FTY720 (1) using the Petasis reaction was developed. 4-Octylbenzaldehyde (9) was converted into 1-ethenyl-4-octylbenzene (11) by two-step synthesis. Hydroboration of 11 using catecholborane and hydrolysis gave (E)-2-(4-octylphenyl)vinylboronic acid (4). The Petasis rea...

journal_title：Chemical & pharmaceutical bulletin

authors： Sugiyama S,Arai S,Kiriyama M,Ishii K

更新日期：2005-01-01 00:00:00

abstract：:Simple one-pot methods for preparation of 2-oxazolines have been developed using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride (DMT-MM). Treatment of a mixture of carboxylic acids and 2-haloethylammonium salts with DMT-MM in methanol followed by refluxing in the presence of KOH gives oxazolines. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hioki K,Takechi Y,Kimura N,Tanaka H,Kunishima M

更新日期：2008-12-01 00:00:00

abstract：:Four new minor saponins, papyrioside LE-LH, were isolated from the leaves of Tetrapanax papyriferum, and their structures were determined on the basis of spectroscopic evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Mutsuga M,Kojima K,Saracoglu I,Ogihara Y

更新日期：1997-03-01 00:00:00

abstract：:Silver loaded zeolite (Ag-Z) was previously found to have effective bactericidal activity against Escherichia coli. To understand the mechanisms of bactericidal activity of Ag-Z, role of light irradiation was focused and investigated in this study. In this study, we focused on light irradiation. Antibacterial assay an...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue Y,Kogure M,Matsumoto K,Hamashima H,Tsukada M,Endo K,Tanaka T

更新日期：2008-05-01 00:00:00

abstract：:The analysis of genotoxic impurities (GTIs) in active pharmaceutical ingredients (APIs) is a challenging task. The target detection limit (DL) in an API is typically around 1 ppm (1 µg/g API). Therefore, a sensitive and selective analytical method is required for their analysis. 4-Chloro-1-butanol, an alkylating agent...

journal_title：Chemical & pharmaceutical bulletin

authors： Harigaya K,Yamada H,Yaku K,Nishi H,Haginaka J

更新日期：2014-01-01 00:00:00

abstract：:We used near infrared (NIR) spectroscopy to evaluate the degree of mixing of blended dry syrup (DS) products whose particle sizes are not specified in the Revised 16th Edition of the Japanese Pharmacopoeia, and also evaluated the degree of mixing when powder products or fine granule products were added to DS products....

journal_title：Chemical & pharmaceutical bulletin

authors： Yamamoto Y,Suzuki T,Matsumoto M,Ohtani M,Hayano S,Fukami T,Tomono K

更新日期：2012-01-01 00:00:00

abstract：:A new toxic neoanisatin-derivative (1) was isolated from the pericarps of Illicium majus. The structure of this compound was elucidated by spectroscopic data, including the 2D COSY NMR technique. The toxicity of compound 1 is also described. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yang CS,Hashimoto M,Baba N,Takahashi M,Kaneto H,Kawano N,Kouno I

更新日期：1990-01-01 00:00:00

abstract：:Four new lignans, 3',4'-O,O-demethylenehinokinin (1), chamalignolide (2), 8'beta-hydroxyhinokinin (3) and 7beta,8beta-epoxyzuonin A (4), as well as (-)-hinokinin (5), and (-)-zuonin A (6), were isolated from the heartwood of Chamaecyparis obtusa var. formosana. The structures of these lignans were unambiguously determ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuo YH,Chen CH,Lin YL

更新日期：2002-07-01 00:00:00

abstract：:3Beta,4beta:15,16-diepoxy-13(16),14-clerodadiene (1) and a new clerodane diterpenoid designated thysaspathone (2) were isolated from the liverwort Thysananthus spathulistipus, while Radula appressa produced radulannin A (3), radulannin L (4), 2-geranyl-3,5-dihydroxybibenzyl (5), 2(S)-2-methyl-2-(4-methyl-3-pentenyl)-7...

journal_title：Chemical & pharmaceutical bulletin

authors： Harinantenaina L,Takahara Y,Nishizawa T,Kohchi C,Soma G,Asakawa Y

更新日期：2006-07-01 00:00:00

abstract：:The aim of this study was to search for a novel choline acetyltransferase (ChAT) activator from plants traditionally grown in Korea. An ethanol extract from Chaenomeles sinensis Koehne showed the highest ChAT-activating effect in vitro in an assay that used human neuroblastoma cells and [(14)C]acetyl-CoA. The active c...

journal_title：Chemical & pharmaceutical bulletin

authors： Kwon YK,Choi SJ,Kim CR,Kim JK,Kim HK,Choi JH,Song SW,Kim CJ,Park GG,Park CS,Shin DH

更新日期：2015-01-01 00:00:00

abstract：:A one-pot conversion of allyl alcohols into selenochroman derivatives was achieved by treatment with a phenyl trimethylsilyl selenide (TMSSePh)-AIBr3 reagent system. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Abe H,Yamasaki A,Koshiba N,Takeuchi Y,Harayama T

更新日期：2001-09-01 00:00:00

abstract：:The in vitro percutaneous transport of sodium diclofenac from various oil vehicles was examined using rat abdominal skin as a model skin membrane. The overall transport of diclofenac through the skin from the oleaginous vehicles was very poor because of a poor solubility of sodium diclofenac in nonpolar oils. To incre...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi K,Tamagawa S,Katagi T,Yoshitomi H,Kamada A,Rytting JH,Nishihata T,Mizuno N

更新日期：1991-01-01 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：:An efficient synthesis of 5-bromo-2-methoxy-6-methylaminopyridine-3-carboxylic acid (1), a carboxylic acid moiety of a potent dopamine D2 and D3 and serotonin-3 (5-HT3) receptors antagonist, (R)-5-bromo-N-(1-ethyl-4-methylhexahydro-1 ,4-diazepin-6-yl)-2-methoxy-6-methylaminopyridine-3-carboxamide, is described. Reacti...

journal_title：Chemical & pharmaceutical bulletin

authors： Hirokawa Y,Horikawa T,Kato S

更新日期：2000-12-01 00:00:00

abstract：:Remote loading of insulin and bovine serum albumin (BSA) into neutral or positively-charged liposomes by incubation under a transmembrane pH gradient or non-pH gradient was investigated. Trapping efficiencies in several incubation conditions were compared with those of the conventional reverse-phase evaporation vesicl...

journal_title：Chemical & pharmaceutical bulletin

authors： Hwang SH,Maitani Y,Takayama K,Nagai T

更新日期：2000-03-01 00:00:00

abstract：:The binding of carprofen (CP) to human serum albumin (HSA) and bovine serum albumin (BSA) was compared using equilibrium dialysis method. The affinity of CP for the primary binding site was BSA > HSA. However, the number of primary binding sites (n1) was 1.94 on HSA, considerably greater than that on BSA (0.79). The d...

journal_title：Chemical & pharmaceutical bulletin

authors： Kohita H,Matsushita Y,Moriguchi I

更新日期：1994-04-01 00:00:00

abstract：:First, Raddeanin A, a cytotoxic oleanane-type triterpenoid saponin isolated from Anemone raddeana REGEL, was synthesized. Stepwise glycosylation was adopted in the synthesis from oleanolic acid, employing arabinosyl, glucosyl and rhamnosyl trichloroacetimidate as donors. The chemical structure of Raddeanin A was confi...

journal_title：Chemical & pharmaceutical bulletin

authors： Qian S,Chen QL,Guan JL,Wu Y,Wang ZY

更新日期：2014-01-01 00:00:00

abstract：:Different crystal packing of hydrates from anhydrate crystals leads to different physical properties, such as solubility and stability. Investigation of the potential of varied hydrate formation, and understanding the stability in an anhydrous/hydrate system, are crucial to prevent an undesired transition during the m...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeuchi S,Kojima T,Hashimoto K,Saito B,Sumi H,Ishikawa T,Ikeda Y

更新日期：2015-01-01 00:00:00

abstract：:A new dihydrobenzofuran neolignan, herpepropenal, was isolated from the seeds of Herpetospermum caudigerum. Its chemical structure was established based on spectroscopic analysis. In this work, the inhibitory effects of herpepropenal on hepatitis B virus DNA and on the replication and expression of hepatitis B surface...

journal_title：Chemical & pharmaceutical bulletin

authors： Yang F,Zhang HJ,Zhang YY,Chen WS,Yuan HL,Lin HW

更新日期：2010-03-01 00:00:00

abstract：:Hyaluronate-hydroxyethyl acrylate blend gel (HA-PHEA) were prepared to modify the brittleness of hyaluronate gel (HA) and the characteristics of HA-PHEA gel were compared with those of HA and polyhydroxyethyl acrylate (PHEA) gels. These gels were high in water content and transparent. HA-PHEA gel was improved in visco...

journal_title：Chemical & pharmaceutical bulletin

authors： Jin Y,Yamanaka J,Sato S,Miyata I,Yomota C,Yonese M

更新日期：2002-10-01 00:00:00

abstract：:Colon-specific drug delivery systems (CDDS) can improve the bioavailability of drug through the oral route. A novel formulation for oral administration using pH-enzyme Di-dependent chitosan mcirospheres (MS) and 5-Fu as a model drug has been investigated for colon-specific drug delivery by the emulsification/chemical ...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhao XL,Li KX,Zhao XF,Pang DH,Chen DW

更新日期：2008-07-01 00:00:00

abstract：:A major lysosomal membrane glycoprotein (LGP107) which has an apparent molecular weight (Mr) of 107 kilodaltons (kDa) was purified from rat liver by a simple method with a yield of 1 mg/87 g wet weight of liver. The purification procedures include; preparation of tritosomal membranes of triton-filled lysosomes (tritos...

journal_title：Chemical & pharmaceutical bulletin

authors： Akasaki K,Yamaguchi Y,Ohta M,Matsuura F,Furuno K,Tsuji H

更新日期：1990-10-01 00:00:00

abstract：:The purpose of this research is to investigate the applicability of terahertz (THz) reflectance spectroscopy for quantification of drug substance in tablets, so as to demonstrate the feasibility for applying this technique to tableting process monitoring. In order to acquire a suitable absorbance spectrum for this pur...

journal_title：Chemical & pharmaceutical bulletin

authors： Hisazumi J,Watanabe T,Suzuki T,Wakiyama N,Terada K

更新日期：2012-01-01 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