Anti-inflammatory effects of indomethacin's methyl ester derivative and induction of apoptosis in HL-60 Cells.


:Indomethacin is used as an anti-inflammatory drug and a nonselective cyclooxygenase inhibitor. When indomethacin in methanol was photo-irradiated with an Hg lamp, methyl ester, ethyl ester, and gamma-lactone derivatives of indomethacin were produced. In the present study, we found that the methyl ester derivative of indomethacin (M-IN) could more potently inhibit prostaglandin E(2) (PGE(2)) and nitric oxide (NO) production and inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX 2) protein expression from lipopolysaccharide (LPS)-stimulated RAW 264.7 cells than indomethacin, similar to the effect of a non-steroidal anti-inflammatory drugs (NSAID). On the other hand, the results showed that M-IN with an IC(50) value maintained at 36.9 microg/ml for 12 h exhibited stronger cytotoxicity than ethyl ester, gamma-lactone derivatives of indomethacin, and indomethacin in promyelocytic leukemia HL-60 cells. Moreover, a series of biochemical analyses determined that M-IN caused apoptotic bodies, DNA fragmentation, and enhanced PARP and pro-caspase 3 degradation in HL-60 cells. These above results indicate that the photosynthesized product, M-IN, had stronger anti-inflammatory effects in LPS-stimulated RAW 264.7 cells and cytotoxicity effects in HL-60 cells than the parent drug, indomethacin.


Biol Pharm Bull


Chao SH,Wu AB,Lee CJ,Chen FA,Wang CC




Has Abstract


2005-12-01 00:00:00














  • Effect of Shosaikoto (Kampo medicine) on the adherence of monocytes in hypercholesterolemic rabbit.

    abstract::Monocytes/macrophages are known to be involved in atherogenesis, and the adherence of monocytes to the endothelium is considered an earliest characteristic of atherogenesis. Therefore, we studied the mechanism by which Shosaikoto, a Kampo medicine, shows anti-atherosclerotic action, which has been already shown in hyp...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Shen YR,Inoue M,Ogihara Y

    更新日期:1996-01-01 00:00:00

  • Modulation of vacuolar H+ -pumps and aquaporin by phytohormones in rice seedling leaf sheaths.

    abstract::The effects of exogenously applied gibberellic acid (GA(3)) or brassinolide (BL) on the H(+)-pumps and aquaporin in the vacuolar membrane of rice seedling leaf sheath were investigated. Antibodies against mung bean H(+)-PPase, the B subunit of V-ATPase, and radish tonoplast intrinsic protein (TIP) cross-reacted with t...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Yang S,Maeshima M,Tanaka Y,Komatsu S

    更新日期:2003-01-01 00:00:00

  • Kinetic characterization of carrier-mediated transport systems for D-glucose and taurocholate in the everted sacs of the rat colon.

    abstract::The present study was aimed at kinetically characterizing the carrier-mediated transport systems for D-glucose and taurocholate in the rat colon, compared with their respective counterparts in the small intestine. The transport of these compounds was evaluated by measuring the initial uptake into everted intestinal ti...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Tomei S,Torimoto M,Hayashi Y,Inoue K,Yuasa H,Watanabe J

    更新日期:2003-06-01 00:00:00

  • Reduced plasma glucose by asparagine synthetase knockdown in the mouse liver.

    abstract::Expression of the asparagine synthetase gene is dependent on extracellular glucose concentration. This gene was knocked-down in livers of male Balb/c mice by a hydrodynamic tail vein injection of small interfering RNA (siRNA) against the gene. This knockdown resulted in a significant decrease in plasma glucose concent...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Iida S,Kamiya H,Nakaya A,Hayashi Y,Sawada A,Kaji N,Baba Y,Harashima H

    更新日期:2013-01-01 00:00:00

  • Oxidation of flavonoids which promote DNA degradation induced by bleomycin-Fe complex.

    abstract::Sixteen flavonoids including quercetin and kaempferol and their relatives were examined for their ability to promote DNA degradation induced by the bleomycin (BLM)-Fe complex. Three hydroxyl groups in the flavonoidal nucleus were proposed as a crucial structural requirement for effectively promoting DNA degradation: 1...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Sugihara N,Kaneko A,Furuno K

    更新日期:2003-08-01 00:00:00

  • Simultaneous determination of 25-hydroxyvitamin D2 and 25-hydroxyvitamin D3 in human plasma by liquid chromatography-tandem mass spectrometry employing derivatization with a Cookson-type reagent.

    abstract::A rapid and highly sensitive LC-MS-MS method for simultaneous determination of 25-hydroxyvitamin D2 125(OH)D21 and 25-hydroxyvitamin D3 125(OH)D3] in human plasma has been developed using derivatization with a Cookson-type reagent, 4-12-(6,7-dimethoxy-4-methyl-3-oxo-3,4-dihydroquinoxalyl)ethyll-1,2,4-triazoline-3,5-di...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 临床试验,杂志文章


    authors: Higashi T,Awada D,Shimada K

    更新日期:2001-07-01 00:00:00

  • Topology of Surface Ligands on Liposomes: Characterization Based on the Terms, Incorporation Ratio, Surface Anchor Density, and Reaction Yield.

    abstract::The surface topology of ligands on liposomes is an important factor in active targeting in drug delivery systems. Accurately evaluating the density of anchors and bioactive functional ligands on a liposomal surface is critical for ensuring the efficient delivery of liposomes. For evaluating surface ligand density, it ...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Lee SH,Sato Y,Hyodo M,Harashima H

    更新日期:2016-01-01 00:00:00

  • Comparative absorption of 5-aminosalicylic acid (5-ASA) after administration of a 5-ASA enema and salazosulfapyridine (SASP) after an SASP suppository in Japanese volunteers.

    abstract::Salazosulfapyridine (SASP) is widely used orally and rectally in the treatment of ulcerative colitis. SASP is mainly metabolized by hydrolysis and the main active metabolite, 5-aminosalicylic acid (5-ASA), has an antiinflammatory effect. In the present study, we prepared suppositories containing 6.5 mmol of SASP and a...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Tokui K,Asai Y,Arakawa T,Matsumoto T,Nabeshima T

    更新日期:2002-02-01 00:00:00

  • Examination of stability of anticonvulsants in a protease solution and assay of anticonvulsants in hairs.

    abstract::For analyzing the concentrations of drugs in hairs, a new method of digestion of hairs with Biopurase, a protease obtained from Bacillus subtilis, was examined. The concentrations of drugs in hairs were then determined in order to examine the usefulness of the protease for the digestion of hairs. The stability of five...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 临床试验,杂志文章


    authors: Fujii J,Higashi A,Nakano M

    更新日期:1996-12-01 00:00:00

  • Sex difference in ischemic acute renal failure in rats: approach by proteomic analysis.

    abstract::It is known that female rats are resistant to ischemic acute renal failure (ARF), compared with male rats. To elucidate sex differences in ischemic ARF, we searched global protein expression in post-ischemic kidneys using proteomic techniques. Ischemic ARF was induced by 45-min ischemia followed by reperfusion. By pro...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Takayama J,Takaoka M,Sugino Y,Yamamoto Y,Ohkita M,Matsumura Y

    更新日期:2007-10-01 00:00:00

  • Ninety-Day Subchronic Oral Toxicity Study of Senecio scandens Extract in Rats.

    abstract::The present study assessed the safety/toxicity of Senecio scandens, a well-known Chinese herb that is used as an anti-inflammatory, antibiosis, and antipyretic drug. A 90-d subchronic oral toxicity study of S. scandens was performed in Wistar rats. The extract of S. scandens was administered orally to male and female ...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Wang XK,Zhao Y,Liu T,Yi Y,Li CY,Wang HJ,Wang CH,Wang ZT,Ye ZG,Liang AH

    更新日期:2015-01-01 00:00:00

  • Suppression of N-myc downstream-regulated gene 2 is associated with induction of Myc in colorectal cancer and correlates closely with differentiation.

    abstract::NDRG2, a new member of the N-Myc downstream-regulated gene (NDRG) family, is a focus for study at present. Up to now, its expression and function in carcinoma remain to be elucidated. In this study, using a colorectal cancer tissue array and a series of 213 colorectal cancer samples, the relationship between Ndrg2 and...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Shi H,Jin H,Chu D,Wang W,Zhang J,Chen C,Xu C,Fan D,Yao L

    更新日期:2009-06-01 00:00:00

  • Pharmacological and pharmaceutical properties of freeze-dried formulations of egg albumin, indomethacin, olive oil, or fatty acids.

    abstract::Formulations consisting of egg albumin, indomethacin (IND), and olive oil or fatty acids, were prepared by vigorous stirring using a high-speed homogenizer and subsequent freeze-drying. To confirm the anti-inflammatory properties and ulcerogenic effects of the formulations, we examined the action of the formulations o...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Tsuji Y,Kakegawa H,Miyataka H,Matsumoto H,Satoh T

    更新日期:1993-07-01 00:00:00

  • Effects of prednisolone on the cutaneous reaction and skin barrier function in mice treated with a hapten.

    abstract::Glucocorticoids are effective drugs for the treatment of allergic skin diseases. In the present study, we observed the effects of prednisolone on the cutaneous reaction and skin barrier function in mice treated with a hapten, 2,4-dinitrofluorobenzene. Repeated hapten application onto the mouse ear resulted in a potent...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Ueda Y,Sone T,Inagaki N,Nagai H

    更新日期:2003-05-01 00:00:00

  • In vitro response of immunoregulatory cytokine expression in human monocytic cells to human parvovirus B19 capsid.

    abstract::Human parvovirus B19 is a clinically important pathogen in both children and adults. In adults, it frequently causes acute and chronic arthritis, which may be related to persistent infection. The effect of the capsid of human parvovirus B19 on monocytes, which are thought to be responsible for the first line of defens...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Fujita T,Ikejima H,Yamagata N,Kudo Y,Hoshi K

    更新日期:2007-11-01 00:00:00

  • A redox-silent analogue of tocotrienol inhibits cobalt(II) chloride-induced VEGF expression via Yes signaling in mesothelioma cells.

    abstract::Vascular endothelial growth factor (VEGF) plays a crucial role in tumor angiogenesis and represents an attractive anticancer target. We have previously demonstrated that a redox-silent analogue of α-tocotrienol, 6-O-carboxypropyl-α-tocotrienol (T3E) exhibits potent anti-carcinogenic property in human malignant mesothe...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Sato A,Virgona N,Ando A,Ota M,Yano T

    更新日期:2014-01-01 00:00:00

  • Structure-activity relationship of (1-->3)-beta-D-glucans in the induction of cytokine production from macrophages, in vitro.

    abstract::In a previous study, we reported that one of the gel-forming (1-->3)-beta-D-glucans, grifolan (from Grifola frondosa, GRN), stimulated cytokine production from macrophages in vitro. However, several other gel-forming (1-->3)-beta-D-glucans, such as sonifilan (SPG) and SSG, did not induce cytokine production from macro...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Okazaki M,Adachi Y,Ohno N,Yadomae T

    更新日期:1995-10-01 00:00:00

  • An Ophthalmic Formulation of Disulfiram Nanoparticles Prolongs Drug Residence Time in Lens.

    abstract::Disulfiram (DSF) is a dimer of diethyldithiocarbamate (DDC) that we previously added to a solution of 2-hydroxypropyl-β-cyclodextrin (DSF solution). We found that the instillation of this DSF solution delayed lens opacification in a hereditary cataractous ICR/f rat. In this study, we attempted to design an ophthalmic ...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Nagai N,Mano Y,Ito Y

    更新日期:2016-01-01 00:00:00

  • Effects of Ramelteon and Other Sleep-Promoting Drugs on Serum Low-Density Lipoprotein and Non-high-density Lipoprotein Cholesterol: A Retrospective Comparative Pilot Study.

    abstract::Melatonin has been suggested to play important roles in lipid metabolism as well as circadian rhythm; however, very few studies explored the effects of ramelteon, a selective melatonin receptor agonist, on serum lipid profiles. In this study effects of ramelteon on serum lipid profiles were explored, comparing to thos...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Torii H,Shimizu R,Tanizaki Y,Omiya Y,Yamamoto M,Kamiike S,Yasuda D,Hiraoka Y,Hashida T,Kume N

    更新日期:2018-01-01 00:00:00

  • Gambogic acid inhibits proliferation of human lung carcinoma SPC-A1 cells in vivo and in vitro and represses telomerase activity and telomerase reverse transcriptase mRNA expression in the cells.

    abstract::We determined the in vivo and in vitro antitumor activities of gambogic acid (GA) and one of the possible mechanisms for its inhibitory activities. In vivo antitumor activity of GA was evaluated by the relative tumor growth ratio (T/C) in nude mice, and in vitro inhibition of SPC-A1 cells was measured by 3-(4,5-dimeth...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Wu ZQ,Guo QL,You QD,Zhao L,Gu HY

    更新日期:2004-11-01 00:00:00

  • Separation of phospholipase A2 in Habu snake venom by glycyrrhizin (GL)-affinity column chromatography and identification of a GL-sensitive enzyme.

    abstract::By means of glycyrrhizin (GL)-affinity and Mono S column chromatographies (HPLC), at least four GL-binding proteins (p25, p17, p15-1 and p15-2) in the two Superdex fractions (P-II and P-III fractions) from Habu snake venom were selectively purified. By determination of their N-terminal partial amino acid sequences, a ...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Ohtsuki K,Abe Y,Shimoyama Y,Furuya T,Munakata H,Takasaki C

    更新日期:1998-06-01 00:00:00

  • Effect of a Dynorphin A analog, E2078, on phospholipid membrane properties.

    abstract::The effect of the Dynorphin A analog, E2078, on the physicochemical properties of lipid membranes was investigated. E2078 induces the leakage of calcein, especially out of negatively-charged vesicles. The peptide binds to dipalmitoylphosphatidylglycerol sonicated vesicles according to the Lamgmuir isotherm, with a bin...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Asai Y,Watanabe S

    更新日期:1999-05-01 00:00:00

  • Therapeutic Effect of Gypenosides on Nonalcoholic Steatohepatitis via Regulating Hepatic Lipogenesis and Fatty Acid Oxidation.

    abstract::Nonalcoholic steatohepatitis (NASH) is the most frequent cause of liver dysfunction and a common global problem. Gypenosides can decrease pathological modifications of high-fat diet-induced rat atherosclerosis; however, its effect and mechanism on NASH remain unclear. In this study, rats were randomly divided into nor...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Li H,Ying H,Hu A,Hu Y,Li D

    更新日期:2017-01-01 00:00:00

  • Detecting mRNA Predictors of Acetaminophen-Induced Hepatotoxicity in Mouse Blood Using Quantitative Real-Time PCR.

    abstract::Acetaminophen (APAP) is a widely used analgesic and antipyretic drug. Drug-induced liver injury from agents such as APAP is known to vary between individuals within a species. To avoid liver injury and ensure the proper use of pharmaceutical products, it is important to be able to predict such risks using genetic info...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kanno S,Tomizawa A,Yomogida S

    更新日期:2016-01-01 00:00:00

  • Evaluation of the anti-inflammatory, analgesic and antipyretic activities of the natural polyphenol chlorogenic acid.

    abstract::Phenolic compounds are numerous and ubiquitous in the plant kingdom, being particularly present in health-promoting foods. Epidemiological evidences suggest that the consumption of polyphenol-rich foods reduces the incidence of cancer, coronary heart disease and inflammation. Chlorogenic acid (CGA) is one of the most ...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: dos Santos MD,Almeida MC,Lopes NP,de Souza GE

    更新日期:2006-11-01 00:00:00

  • Effects of 3-O-methyldopa, L-3,4-dihydroxyphenylalanine metabolite, on locomotor activity and dopamine turnover in rats.

    abstract::It has been well known that 3-O-methyldopa (3-OMD) is a metabolite of L-3,4-dihydroxyphenylalanine (L-DOPA) formed by catechol O-methyltransferase (COMT), and 3-OMD blood level often reaches higher than physiological level in Parkinson's disease (PD) patients receiving long term L-DOPA therapy. However, the physiologi...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Onzawa Y,Kimura Y,Uzuhashi K,Shirasuna M,Hirosawa T,Taogoshi T,Kihira K

    更新日期:2012-01-01 00:00:00

  • Evaluation of Proteinuria Using Urine Protein : Creatine Ratio in Treatment with Molecular Targeted Agents for Advanced Renal Cell Carcinoma.

    abstract::The usefulness of the urine protein : creatine ratio (UPCR) in management of molecular targeted therapy and immunotherapy has not been studied, although urine protein dipstick testing (uPr) is widely used in the clinical setting. The aim of this study was to investigate the usefulness of UPCR as compared to uPr in pat...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Nakamura K,Tanaka T,Masumori N,Miyamoto A,Hirano T

    更新日期:2020-01-01 00:00:00

  • Real time measurement of nitric oxide released from cultured endothelial cells.

    abstract::Direct detection of nitric oxide (NO) is essential for understanding the precise mechanism of its production from endothelial cells. Previously, we developed an NO detection system based on the chemiluminescence reaction between NO and luminol-H2O2. Here, we have applied this system to cultured endothelial cells for t...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kurumatani H,Kikuchi K,Nagano T,Hirobe M,Yamazaki J,Nagao T

    更新日期:1998-12-01 00:00:00

  • The Activity of Fungichromin against the Formation of Candida albicans Biofilm.

    abstract::The effect of fungichromin (FC) on the formation of Candida albicans biofilm was assessed using 2,3-bis(2-methoxy-4-nitro-5-sulfo-phenyl)-2H-tetrazolium-5-carboxanilide (XTT) reduction method, scanning electron microscopy (SEM) and confocal laser scanning microscopy (CLSM). Results showed that FC revealed an inhibitor...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: An D,Wang X,Li J,Jiang S,Ma X,Zhang H,Shi H,Sun H,Ye L,Li J

    更新日期:2016-12-01 00:00:00

  • Amelioration of CIA by Asarinin Is Associated to a Downregulation of TLR9/NF-κB and Regulation of Th1/Th2/Treg Expression.

    abstract::To study the role of asarinin on collagen-induced arthritis (CIA) and its treatment mechanism on dendritic cells (DCs) and T cells. Before the onset of arthritis, asarinin were given orally to CIA mouse. Macroscopic scoring and micrometer caliper measurement were used to assess arthritis. The occurrence of cartilage d...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Dai Q,Wang M,Li Y,Li J

    更新日期:2019-07-01 00:00:00