Search Results:　 1-20 of 146

1

Homoisoflavonoids from Caesalpinia sappan Displaying Viral Neuraminidases Inhibition

Jeong Hyung Jae , Kim Young Min , Kim Jang Hoon , Kim Ji Young , Park Ji-Young , Park Su-Jin , Ryu Young Bae , Lee Woo Song

… Of isolated homoisoflavonoids, sappanone A (2) showed the most potent NAs inhibitory activities with IC50 values of 0.7 µM [H1N1], 1.1 µM [H3N2], and 1.0 µM [H9N2], respectively, whereas saturated homoisoflavonoid (3) did not show significantly inhibition. … In our enzyme kinetic study, all NA inhibitors screened were found to be reversible noncompetitive types. …

Biological and Pharmaceutical Bulletin 35(5), 786-790, 2012

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2

Protein Tyrosine Phosphatase 1B and α-Glucosidase Inhibitory Phlorotannins from Edible Brown Algae, Ecklonia stolonifera and Eisenia bicyclis

MOON Hye Eun , ISLAM Md. Nurul , AHN Bo Ra , CHOWDHURY Sabiha Sultana , SOHN Hee Sook , JUNG Hyun Ah , CHOI Jae Sue

… Phlorotannins 3–6 were potent and noncompetitive PTP1B inhibitors with IC50 … 4–6 exhibited the most potent α-glucosidase inhibition with IC50 … Interestingly, 4 and 6 were noncompetitive, while 5 exhibited competitive inhibition in an α-glucosidase assay. …

Bioscience, Biotechnology, and Biochemistry 75(8), 1472-1480, 2011-08-23

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3

Effects of Grape Seed Proanthocyanidin on 5-Hydroxytryptamine3 Receptors in NCB-20 Neuroblastoma Cells

Li Qing-Zhong , Cho Hyeong-Seok , Jeun Seung-Hyun , Kim Ki Jung , Choi Se Joon , Sung Ki-Wug

… Co-treatment of proanthocyanidin (0.3—100 μg/ml) and 3 μM 5-HT (near EC50) produced a slight inhibition of 5-HT-induced inward peak current (I5-HT) in NCB-20 cells, but pretreatment with proanthocyanidin for 30 s before application of 5-HT induced a much larger inhibition of I5-HT in an irreversible, concentration- and time-dependent manner (IC50=6.5±0.4 μg/ml, Hill coefficient=2.5±0.1). …

Biological and Pharmaceutical Bulletin 34(7), 1109-1115, 2011

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4

.BETA.-Sitosteryl (6'-O-linoleoyl)-glucoside of Soybean (Glycine max L.) Crude Extract Inhibits Y-Family DNA Polymerases

Horie Sho , Okuda Chiaki , Yamashita Takatoshi , Watanabe Kenichi , Sato Yoshihiro , Yamaguchi Yasuhiro , Takeuchi Toshifumi , Sugawara Fumio , Yoshida Hiromi , Mizushina Yoshiyuki

… Kinetic studies showed that the inhibition of pol κ activity by compound 1 was noncompetitive with both the DNA template-primer and nucleotide substrate, whereas compound 3-induced inhibition was competitive with the DNA template-primer and noncompetitive with the nucleotide substrate. … The relationship between the structure of compound 1 and the selective inhibition of eukaryotic Y-family pols is discussed. …

Journal of Oleo Science 59(11), 621-630, 2010

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5

Rat Aldose Reductase-Like Protein (AKR1B14) Efficiently Reduces the Lipid Peroxidation Product 4-Oxo-2-nonenal

Endo Satoshi , Matsunaga Toshiyuki , Fujita Anna , Tajima Kazuo , El-Kabbani Ossama , Hara Akira

… AKR1B14 was inhibited by aldose reductase inhibitors such as tolrestat and epalrestat, and their inhibition patterns were noncompetitive versus the aldehyde substrate and competitive with respect to the alcohol substrate. … Kinetic analyses of the oxidoreduction and dead-end inhibition suggest that the reaction follows an ordered sequential mechanism. …

Biological and Pharmaceutical Bulletin 33(11), 1886-1890, 2010

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6

Aldose Reductase Inhibitory Compounds from Glycyrrhiza uralensis

Lee Yeon Sil , Kim Seon Ha , Jung Sang Hoon , Kim Jin Kyu , Pan Cheol-Ho , Lim Soon Sung

… From the 10 isolated compounds, semilicoisoflavone B showed the most potent inhibition, with the IC50 values of rAR and rhAR at 1.8 and 10.6μM, respectively. … In the kinetic analyses using Lineweaver.Burk plots of 1/velocity and 1/concentration of substrate, semilicoisoflavone B showed noncompetitive inhibition against rhAR. …

Biological and Pharmaceutical Bulletin 33(5), 917-921, 2010

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7

Selective Cholinesterase Inhibitory Activities of a New Monoterpene Diglycoside and Other Constituents from Nelumbo nucifera Stamens

Jung Hyun Ah , Jung Yu Jung , Hyun Sook Kyung , Min Byung-Sun , Kim Dong-Wook , Jung Jee H. , Choi Jae Sue

… The chemical structure of 5 was elucidated as 1-hydroxymethyl-2,6,6-trimethyl-1-cyclohexene 9-O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside (nuciferoside) on the basis of chemical and spectroscopic evidence, including 1D, 2D NMR, and MS. The anti-Alzheimer effects of 1—5 were evaluated via the acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) inhibition assays. …

Biological and Pharmaceutical Bulletin 33(2), 267-272, 2010

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8

Inhibitory Effects of Ketoconazole, Cimetidine and Erythromycin on Hepatic CYP3A Activities in Cats

SHAH Syed Sher , SASAKI Kazuaki , HAYASHI Yuhei , MOTOYAMA Seiko , HELMI Abdou Rania , KHALIL Waleed Fathy , SHIMODA Minoru

… The results showed that, all the examined drugs inhibited the reactions in a noncompetitive manner. … Mechanism-based inhibition was also examined in this study. … In clinical practice, therefore, KTZ may result in inhibition based drug-drug interaction with CYP3A substrates in cat patients, whereas CIM and ERY are unlikely to lead to interaction involving CYP3A substrates. …

Journal of Veterinary Medical Science 71(9), 1151-1159, 2009

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9

Isolation of Human Renin Inhibitor from Soybean : Soyasaponin I Is the Novel Human Renin Inhibitor in Soybean

TAKAHASHI Saori , HORI Kazuyuki , SHINBO Mamoru , HIWATASHI Kazuyuki , GOTOH Takeshi , YAMADA Seihan

… SRI showed significant inhibition against recombinant human renin, with an IC50 … Kinetic studies with SRI indicated partial noncompetitive inhibition, with a Ki …

Bioscience, Biotechnology, and Biochemistry 72(12), 3232-3236, 2008-12-23

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10

Some Selective Serotonin Reuptake Inhibitors Inhibit Dynamin I Guanosine Triphosphatase (GTPase)(Biochemistry)

OTOMO Masahiro , TAKAHASHI Kiyofumi , MIYOSHI Hiroshi , OSADA Kenichi , NAKASHIMA Hideki , YAMAGUCHI Noboru

… Kinetic analyses revealed that fluvoxamine is a noncompetitive inhibitor of dynamin I guanosine triphosphatase (GTPase) with respect to guanosine 5'-triphosphate (GTP) and a competitive inhibitor with respect to L-phosphatidylserine (PS). … On the other hand, sertraline was a mixed type inhibitor with respect to both GTP and PS. Our results indicate that sertraline and fluvoxamine may regulate the transportation of neurotransmitters by modulating synaptic vesicle endocytosis via the inhibition of dynamin I GTPase. …

Biological & pharmaceutical bulletin 31(8), 1489-1495, 2008-08-01

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11

The Mechanisms by Which Latanoprost Free Acid Inhibits Human Carbonic Anhydrase I and II(Biochemistry)

SUGIMOTO Ayako , IKEDA Hiroaki , TSUKAMOTO Hidetoshi , KIHIRA Kenji , TAKEDA Chiho , HIROSE Junzo , HATA Toshiyuki , BABA Eiko , ONO Yukio

… Latanoprost free acid inhibited the hydration activity of HCA I or II by a noncompetitive mechanism. … The inhibition constants (K_i) of latanoprost free acid for HCA I and II were 0.22 and 2.3 mM, respectively. … The noncompetitive inhibition mechanism and the binding mode of latanoprost free acid indicate that the behavior of latanoprost free acid is very similar to that of simple anions. …

Biological & pharmaceutical bulletin 31(5), 796-801, 2008-05-01

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12

Direct Inhibition of N-Methyl-D-Aspartate (NMDA)-Receptor Function by Antiglaucomatous β-Antagonists

NAGATA Tatsuo , UENO Susumu , MORITA Hirofumi , KUBOTA Toshiaki , TOYOHIRA Yumiko , TSUTSUI Masato , TAWARA Akihiko , YANAGIHARA Nobuyuki

… In oocytes expressing wild-type NMDA (NR1a/NR2A) receptors, timolol and betaxolol significantly inhibited glutamate-evoked currents, whereas less inhibition was obtained with pilocarpine, and latanoprost had few effects. … Moreover, the effect of timolol and betaxolol was noncompetitive with respect to glutamate. …

Journal of Pharmacological Sciences 106(3), 423-434, 2008-03-20

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13

Novel Inhibitors of Phenylalanine Ammonia-lyase: 5-Aryl-1, 3, 4-oxathiazol-2-ones

YAMADA Naotaka , HONG Soonsung , KUWANO Eiichi

… A series of 5-aryl-1,3,4-oxathiazol-2-ones was synthesized and tested for inhibition against phenylalanine ammonia-lyase (PAL) derived from the yeast Rhodotorula glutinis. … Compound 19 behaved as a noncompetitive inhibitor of PAL. … When potato tuber disks were treated with 19 in the presence of laminarin, a β-1,3-glucooligosaccharide elicitor, the amount of trans-cinnamic acid diminished after 48 hr, being consistent with an effective inhibition of PAL. …

Journal of the Faculty of Agriculture, Kyushu University 51(2), 309-313, 2006-10-00

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14

Glycosidase Inhibitory Flavonoids from Sophora flavescens(Medicinal Chemistry)

KIM Jin Hyo , RYU Young Bae , KANG Nam Suk , LEE Byong Won , HEO Jong Soo , JEONG Ill-Yun , PARK Ki Hun

… value of 57μM against β-glucosidase, which is the first report of a chalcone displaying glycosidase inhibition. … The inhibition pattern was noncompetitive for α-glucosidase, whereas mixed inhibition was observed for β-amylase. …

Biological & pharmaceutical bulletin 29(2), 302-305, 2006-02-01

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15

Xanthine Oxidase Inhibitors from the Heartwood of Vietnamese Caesalpinia sappan

NGUYEN Mai Thanh Thi , AWALE Suresh , TEZUKA Yasuhiro , TRAN Quan Le , KADOTA Shigetoshi

… The kinetic study of these inhibitors indicated that they are competitive inhibitors, the same as allopurinol, except for 1 and 16 which are noncompetitive inhibitors. …

Chemical & pharmaceutical bulletin 53(8), 984-988, 2005-08-01

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16

Inhibition of Tyrosinase Activity by N, N-Unsubstituted Selenourea Derivatives(Medicinal Chemistry)

HA Sang Keun , KOKETSU Mamoru , LEE Kunho , CHOI Sang Yoon , PARK Ji Ho , ISHIHARA Hideharu , KIM Sun Yeou

… Compound D at a concentration of 200μM exhibited 55.5% of inhibition on dopa oxidase activity of mushroom tyrosinase. … Moreover, the compound D identified as a noncompetitive inhibitor by Lineweaver-Burk plot analysis. …

Biological & pharmaceutical bulletin 28(5), 838-840, 2005-05-01

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17

Different Effects of Desipramine on Bufuralol 1"-Hydroxylation by Rat and Human CYP2D Enzymes(Pharmacology)

ISOBE Takashi , HICHIYA Hiroyuki , HANIOKA Nobumitsu , YAMAMOTO Shigeo , SHINODA Sumio , FUNAE Yoshihiko , SATOH Tetsuo , YAMANO Shigeru , NARIMATSU Shizuo

… Inhibition was examined under the following two conditions : 1) DMI was coincubated with BF and NADPH in the reaction mixture containing rat or human liver microsomes or yeast cell microsomes expressing rat CYP2D1, CYP2D2 or human CYP2D6 (co-incubation) ; …

Biological & pharmaceutical bulletin 28(4), 634-640, 2005-04-01

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18

A new graphical method for estimation of enzyme inhibition constants [in Japanese]

Hijikata-Okunomiya Akiko

本論文の目的は50%阻害を示すインヒビター濃度I_<50>と基質濃度[S]との間に導かれる関係式から酵素阻害定数K_iを求める新しい作図法を紹介することにある。まず、競合的阻害の場合I_<50>は[numerical formula]とあらわされる。ここでK_mはMichaelis定数を表す。一方、非競合的阻害の場合はI_<50>=K_iとなる。したがって、縦軸 …

神戸大学医学部保健学科紀要 21, 79-83, 2005-00-00

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19

Strong Antihyperglycemic Effects of Water-Soluble Fraction of Brazilian Propolis and Its Bioactive Constituent, 3,4,5-Tri-O-caffeoylquinic Acid(Medicinal Chemistry)

MATSUI Toshiro , EBUCHI Sumi , FUJISE Tomoko , ABESUNDARA Kanthi J. M. , Doi Shima , YAMADA Hideo , MATSUMOTO Kiyoshi

… Among the active compounds isolated from the fraction, 3,4,5-tri-caffeoylquinic acid was found to be a prominent candidate that exerts the effect and shows a strong maltase-specific inhibition with an IC_<50> … In addition, the noncompetitive inhibition power apparently increased with the number of caffeoyl groups bound to quinic acid. …

Biological & pharmaceutical bulletin 27(11), 1797-1803, 2004-11-01

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20

Noncompetitive Inhibition by L-Cysteine and Activation by L-Glutamate of the Iron-Oxidizing Activity of a Mixotrophic Iron-Oxidizing Bacterium Strain OKM-9(MICROBIAL PHYSIOLOGY AND BIOTECHNOLOGY)

SUGIO TUSYOSHI , INOUE TAKAO , KITANO YOSIKI , TAKEUCHI FUMIAKI , KAMIMURA KAZUO

… was 12.6 mM and the inhibition constant for L-cysteine was 41.6 mM. … A marked inhibition of iron oxidase by 50 mM L-cysteine was completely reversed by the addition of 60 mM L-glutamate. …

Journal of bioscience and bioengineering 98(2), 85-91, 2004-08-25

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