Four new neo-clerodane diterpenoid alkaloids from Scutellaria barbata with cytotoxic activities.


:Four new neo-clerodane diterpenoid alkaloids, named scutebarbatines C-F (1-4), were isolated from the whole plants of Scutellaria barbata D. DON. Their structures were elucidated by spectral analyses (UV, IR, FAB-MS, 1D-NMR and 2D-NMR). In vitro, compounds 1-4 showed significant cytotoxic activities against three human cancer cell lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, and gave IC(50) values in the range 3.9-7.8 muM.


Dai SJ,Chen M,Liu K,Jiang YT,Shen L




Has Abstract


2006-06-01 00:00:00














  • Benzoxazines. II. Synthesis, conformational analysis, and structure--activity relationships of 3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide derivatives as potent and long-acting serotonin-3 (5-HT3) receptor antagonists.

    abstract::A series of 3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide derivatives was synthesized and evaluated for serotonin-3 (5HT3) receptor antagonistic activities by means of assays of 5-HT3 receptor binding and the ability to antagonize the von Bezold-Jarisch reflex in rats. Replacement of the 1,4-benzoxazine ring with a 1,4...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kuroita T,Marubayashi N,Sano M,Kanzaki K,Inaba K,Kawakita T

    更新日期:1996-11-01 00:00:00

  • Comparative pharmacokinetics of acetohexamide and its metabolite, hydroxyhexamide in laboratory animals.

    abstract::The pharmacokinetic profiles of the hypoglycemic agent, acetohexamide (AH) and its major active metabolite, hydroxyhexamide (HH) were studied in three species of laboratory animals after intraperitoneal (ipl) administration in comparison with those after intravenous (iv) administration of AH and of the preformed metab...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Asada S,Nagamine S,Nakae H

    更新日期:1989-03-01 00:00:00

  • New bicyclic taxane diterpenoids from Taxus sumatrana.

    abstract::Investigation of an acetone extract of the leaves and twigs of Taxus sumatrana has resulted in the isolation of two new bicyclic taxoids, tasumatrols M (1), and N (2) and a new baccatin III derivative, tasumatrol O (3) together with the previous known 7-deacetylcanadensene (4) and 2alpha,7beta,13alpha-triacetoxy-5alph...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Shen YC,Hsu SM,Lin YS,Cheng KC,Chien CT,Chou CH,Cheng YB

    更新日期:2005-07-01 00:00:00

  • Two new acylated flavonol glycosides from Vicia amurensis.

    abstract::Two new acylated flavonol glycosides, named amurenosides A and B, together with quercetin 3-(2,6-di-O-alpha-rhamnopyranosyl-beta-galactopyranoside), have been isolated from the whole plant of Vicia amurensis. Their structures were elucidated as quercetin 3-O-alpha-L-(3-feruloylrhamnopyranosyl)(1-->6)-[alpha-L-rhamnopy...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kang SS,Chang YS,Kim JS

    更新日期:2000-08-01 00:00:00

  • Hopeafuran and a C-glucosyl resveratrol isolated from stem wood of Hopea utilis.

    abstract::A new resveratrol dimer and a new C-glucosyl resveratrol were isolated from stem wood of Hopea utilis along with nine stilbenoid derivatives comprising bergenin and (+)-lyoniresinol. The structures have been elucidated on the basis of the spectroscopic evidence. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Tanaka T,Ito T,Ido Y,Nakaya K,Iinuma M,Chelladurai V

    更新日期:2001-06-01 00:00:00

  • Synthesis and in vitro antioxidant activity of glycyrrhetinic acid derivatives tested with the cytochrome P450/NADPH system.

    abstract::Five glycyrrhetinic acid (Ib) derivatives have been synthesized to try to improve the antioxidant activity. Their in vitro antioxidant activities were studied using a cytochrome P450/NADPH reductase system from rat liver microsomes. The generation of microsomal free radicals was followed by oxidation of the DCFH-DA pr...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Ablise M,Leininger-Muller B,Wong CD,Siest G,Loppinet V,Visvikis S

    更新日期:2004-12-01 00:00:00

  • Binding properties of adenosine deaminase interacted with theophylline.

    abstract::Thermodynamic studies were carried out to evaluate the binding of theophylline on adenosine deaminase (ADA) in 50 mM sodium phosphate buffer pH 7.5, at 300 K, using isothermal titration calorimetry (ITC). A simple method for determination of binding isotherm in the drug--ADA interaction was applied using ITC data. ADA...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Saboury AA,Bagheri S,Ataie G,Amanlou M,Moosavi-Movahedi AA,Hakimelahi GH,Cristalli G,Namaki S

    更新日期:2004-10-01 00:00:00

  • Three new glycosides from the leaves of Hydrangea macrophylla subsp. serrata (THUNB.) MAKINO.

    abstract::Three new glycosides, 7-deoxyloganic acid beta-D-glucopyranosyl ester (1), (3R)-hydrangenol 8,4'-di-O-beta-D-glucopyranoside (2), and (6R,7E,9R)-megastigma-4,7-dien-3-one 9,13-di-O-beta-D-glucopyranoside (3), have been isolated from the leaves of Hydrangea macrophylla subsp. serrata (THUNB.) MAKINO (Saxifragaceae). Th...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kikuchi M,Kakuda R,Kikuchi M,Yaoita Y

    更新日期:2008-04-01 00:00:00

  • Absorption enhancement of polypeptide drugs by cyclodextrins. I. Enhanced rectal absorption of insulin from hollow-type suppositories containing insulin and cyclodextrins in rabbits.

    abstract::The absorption of insulin (from porcine pancreas) from the rectum of rabbits after the administration of hollow-type suppositories containing insulin and five kinds of cyclodextrins (CyDs) was investigated. Three types of suppositories were employed: suppository I containing insulin (approximately 26 IU/mg) and variou...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Watanabe Y,Matsumoto Y,Seki M,Takase M,Matsumoto M

    更新日期:1992-11-01 00:00:00

  • Selective Targeting of Cancer Stem Cells by 2-Aminodihydroquinoline Analogs.

    abstract::Many aminodihydroquinoline compounds have been studied to determine their cytotoxicity to cancer cells. However, anti-cancer stem cells (CSCs) activity of aminodihydroquinoline has not been tested in spite that CSC is believed to do an important roles in chemotherapy resistance and recurrence. The CSC selective target...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Park H,Yu Y,Kim H,Lee E,Lee H,Jeon R,Kim WY

    更新日期:2017-04-01 00:00:00

  • Cytotoxicity of asymmetric platinum complexes against L-1210 cells. Effect of bulky substituents.

    abstract::The asymmetric platinum complexes cis-Pt(LL')Cl2 (L = NH3, L' = CH3NH2, (CH3)2NH, C2H5NH2 and (C2H5)2NH and LL' = N,N-dimethylethylenediamine),--one of the NH3 groups of cis-Pt(NH3)2Cl2 was substituted by alkylamine--, were synthesized and their cytotoxic effects have been measured using L-1210 cells. The IC50 values ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Hirano T,Inagaki K,Fukai T,Alink M,Nakahara H,Kidani Y

    更新日期:1990-10-01 00:00:00

  • Effect of surface layering time of lactose carrier particles on dry powder inhalation properties of salbutamol sulfate.

    abstract::The effect of the surface layering time of lactose carrier particles on the dry powder inhalation properties of salbutamol sulfate was investigated. Lactose carrier particles were layered with vegetable magnesium stearate by physical mixing. In the present study, drug/carrier powder mixtures were designed consisting o...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Iida K,Hayakawa Y,Okamoto H,Danjo K,Luenberger H

    更新日期:2004-03-01 00:00:00

  • Evaluation of Weight Variation in Mini-Tablets Manufactured by a Multiple-Tip Tool.

    abstract::Recently, owing to their pharmaceutical and clinical utility, mini-tablets have been well studied by researchers. Mini-tablets are usually manufactured by compression molding using a multiple-tip tool in a rotary tableting machine. Owing to their special structure, ensuring uniformity is a very important challenge in ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kurashima H,Uchida S,Kashiwagura Y,Tanaka S,Namiki N

    更新日期:2020-01-01 00:00:00

  • Magnolin Inhibits Proliferation and Invasion of Breast Cancer MDA-MB-231 Cells by Targeting the ERK1/2 Signaling Pathway.

    abstract::The aim of this study was to evaluate the effects of Magnolin (MGL) on inhibition of human breast cancer cells, and explore the underlying molecular mechanisms. The viability of the treated cells was assessed with the Cell Counting Kit-8 (CCK-8) assay, and the proliferation was analyzed in terms of EdU uptake, colony ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Wang J,Zhang S,Huang K,Shi L,Zhang Q

    更新日期:2020-01-01 00:00:00

  • Synthesis and evaluation of pyrrolin-2-one compounds, a series of plasminogen activator inhibitor-1 inhibitors.

    abstract::A novel series of furan-2-one and pyrrolin-2-one derivatives having PAI-1 (plasminogen activator inhibitor-1) inhibitory activity were synthesized and evaluated for their antithrombotic activity in a rat arterial thrombosis model. Among the synthesized compounds, 5f (T-1776Na) was found to have good selectivity for PA...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Miyazaki H,Ogiku T,Sai H,Moritani Y,Ohtani A,Ohmizu H

    更新日期:2009-09-01 00:00:00

  • Synthesis and Biological Evaluation of N-Aryl-5-aryloxazol-2-amine Derivatives as 5-Lipoxygenase Inhibitors.

    abstract::We describe the synthesis and biological evaluation of N-aryl-5-aryloxazol-2-amine derivatives that are able to inhibit 5-lipoxygenase (5-LOX), a key enzyme of leukotriene synthesis, for the treatment of inflammation-related diseases including asthma and rheumatoid arthritis. A novel structural moiety containing oxazo...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Suh JH,Yum EK,Cho YS

    更新日期:2015-01-01 00:00:00

  • Inhibitory effects of 3-O-acyl-(+)-catechins on Epstein-Barr virus activation.

    abstract::In the course of an exploratory investigation of antitumor-promoting catechins, 3-O-acyl-(+)-catechins of varying carbon lengths from C(4) to C(18) were assessed for inhibitory effects on the activation of the Epstein-Barr virus early antigen. Like 3-O-acyl-(-)-epigallocatechins, the (+)-catechin derivatives showed pr...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Uesato S,Taniuchi K,Kumagai A,Nagaoka Y,Seto R,Hara Y,Tokuda H,Nishino H

    更新日期:2003-12-01 00:00:00

  • Effect of water content on the solid-state stability in two isomorphic clathrates of cephalosporin: cefazolin sodium pentahydrate (alpha form) and FK041 hydrate.

    abstract::This study clearly demonstrates that clathrated water molecules can contribute to both chemical stabilization and destabilization of clathrates. The solid-state stabilities for two isomorphic clathrates of cephalosporin, cefazolin sodium and FK041, were investigated in terms of the effects of water content. The isomor...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Mimura H,Gato K,Kitamura S,Kitagawa T,Kohda S

    更新日期:2002-06-01 00:00:00

  • Design, Synthesis and Antiproliferative Evaluation of Novel Disulfides Containing 1,3,4-Thiadiazole Moiety.

    abstract::A series of novel disulfides containing 1,3,4-thiadiazole moiety were designed, synthesized, and the structures of all products were identified by spectral data (IR, NMR, and high resolution (HR)-MS). Their in vitro antiproliferative activities were evaluated using 2-(2-methoxy-4-nitro-phenyl)-3-(4-nitro-phenyl)-5-(2,...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Zhang S,Liu XJ,Tang R,Wang HX,Liu HY,Liu YM,Chen BQ

    更新日期:2017-01-01 00:00:00

  • 1,4-Benzoxazine-3(4H)-ones as potent inhibitors of platelet aggregation: design, synthesis and structure-activity relations.

    abstract::A series of novel potentially platelet aggregation-inhibiting 1,4-benzoxazine-3(4H)-one derivatives was designed and synthesized through Smiles rearrangement, reduction and acetylation reactions. The antiaggregatory activities of the target molecules on arterial blood samples from rabbits, expressed by IC₅₀ values (μM...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Liu C,Tan JL,Xiao SY,Liao JF,Zou GR,Ai XX,Chen JB,Xiang Y,Yang Q,Zuo H

    更新日期:2014-01-01 00:00:00

  • Preparation and evaluation of proliposomes containing clotrimazole.

    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

    pub_type: 杂志文章


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

    更新日期:2005-06-01 00:00:00

  • Green and efficient synthesis of quinoxaline derivatives via ceric ammonium nitrate promoted and in situ aerobic oxidation of alpha-hydroxy ketones and alpha-keto oximes in aqueous media.

    abstract::The direct conversion of alpha-hydroxy ketones and alpha-keto oximes into quinoxaline derivatives in the presence of a catalytic amount of ceric ammonium nitrate via metal-catalyzed aerobic oxidation followed by in situ trapping with aromatic 1,2-diamines in water as a green and efficient reaction media, is reported. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Shaabani A,Maleki A

    更新日期:2008-01-01 00:00:00

  • Synthesis and pharmacological activities of novel bicyclic thiazoline derivatives as hepatoprotective agents. I. 8-Ethoxycarbonyl-5,6-dihydrothiazolo[2,3-c][1,4]thiazine derivatives.

    abstract::A series of bicyclic thiazoline derivatives (4a-s) was synthesized and evaluated for hepatoprotective activity against galactosamine-induced and monoclonal antibody-induced acute liver injuries in rats. The structure-activity relationships were investigated. Among the compounds synthesized, ethyl 3-(N-methylcarbamoyl)...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Hasegawa M,Nakayama A,Hosokami T,Kurebayashi Y,Ikeda T,Shimoto Y,Ide S,Honda Y,Suzuki N

    更新日期:1995-01-01 00:00:00

  • Mucoadhesive tablets for controlled release of acyclovir.

    abstract::Mucoadhesive chitosan (CS) and/or hydroxypropyl-methylcellulose (HPMC) tablets for gastric drug delivery of acyclovir (ACV) have been developed in order to improve the ACV oral bioavailability. Swelling, bioadhesive and dissolution studies were carried out in two acidic media (pH 1.5 and 4) in order to determine the t...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Ruiz-Caro R,Gago-Guillan M,Otero-Espinar FJ,Veiga MD

    更新日期:2012-01-01 00:00:00

  • Synthetic studies on (+)-biotin, part 15: A chiral squaramide-mediated enantioselective alcoholysis approach toward the total synthesis of (+)-biotin.

    abstract::An efficient stereocontrolled total synthesis of (+)-biotin (1) has been achieved via the intermediacy of Roche's lactone 5 starting from cis-1,3-dibenzyl-2-imidazole-4,5-dicarboxylic acid (2). The bifunctional cinchona alkaloid-derived squaramide-promoted enantioselective alcoholysis was utilizing as a tool for the c...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Chen XX,Xiong F,Fu H,Liu ZQ,Chen FE

    更新日期:2011-01-01 00:00:00

  • Application of a self-organizing map to quantitative structure-activity relationship analysis of carboquinone and benzodiazepine.

    abstract::Self-organizing map (SOM) of Kohonen seems to be a promising approach beyond the standard one to regression for some classification problems encountered in the field of pharmacy. We apply them, therefore, to the quantitative structure-activity relationship (QSAR) in carboquinones and benzodiazepines, and show their us...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kawakami J,Hoshi K,Ishiyama A,Miyagishima S,Sato K

    更新日期:2004-06-01 00:00:00

  • Sesquiterpenoids from the formosan soft coral Sinularia leptoclados.

    abstract::Chemical investigation of the soft coral Sinularia leptoclados has afforded three new sesquiterpenoids, leptocladols A (1), B (2), and 1-epi-chabrolidione A (3). The relative structures of 1-3 were determined on the basis of extensive spectroscopic analysis. The relative configuration of 1 was further confirmed by a s...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Su JH,Chiang MY,Wen ZH,Dai CF,Hsu CH,Sheu JH

    更新日期:2010-02-01 00:00:00

  • Effect of grinding with hydroxypropyl cellulose on the dissolution and particle size of a poorly water-soluble drug.

    abstract::A new benzofuroquinoline derivative, 3,9-bis(N,N-dimethylcarbamoyloxy)-5H-benzofuro[3,2-c]quinoli ne-6-one (KCA-098), shows poor oral absorption due to practical insolubility in water. In this study, a co-grinding technique employing a water-soluble polymer was used for improvement of the dissolution rate of KCA-098. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Yamada T,Saito N,Imai T,Otagiri M

    更新日期:1999-09-01 00:00:00

  • A novel fluorescent probe for zinc ion based on boron dipyrromethene (BODIPY) chromophore.

    abstract::ZnAB has the combined structure of N,N-bis(2-pyridylmethyl)ethylenediamine as a specific chelater for Zn(2+) and 1,3,5,7-tetramethyl-8-phenyl-boron dipyrromethene as a fluorophore. Complexation of ZnAB with Zn(2+) produces a remarkable enhancement of fluorescence intensity. ZnAB has the advantages of less sensitivity ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Koutaka H,Kosuge J,Fukasaku N,Hirano T,Kikuchi K,Urano Y,Kojima H,Nagano T

    更新日期:2004-06-01 00:00:00

  • Studies on antibacterial agents. I. Synthesis of substituted 6,7-dihydro-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acids.

    abstract::A series of substituted 6,7-dihydro-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acids was synthesized and tested for antibacterial activities. Among them, 9-fluoro-6,7-dihydro-5-methyl-8-(4-methyl-1-piperazinyl)-1-oxo-1H,5H- benzo[i,j]quinolizine-2-carboxylic acid (OPC-7241) exhibited potent antibacterial activity ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Ishikawa H,Tabusa F,Miyamoto H,Kano M,Ueda H,Tamaoka H,Nakagawa K

    更新日期:1989-08-01 00:00:00