Inhibitory effects of flavonoids on human immunodeficiency virus type-I integrase

スポンサーリンク

概要

• 論文の詳細を見る

• マルチプレートインテグレーション法を用いて183種のフラボノイド類のHIV-1インテグラーゼ阻害効果を検討した。これらのうち6-hydroxyluteolin, scutellarein, pedalitin, scutellarin, baicalein二量体,hypolaetin,7-O-benzyl-6-hydroxyluteolinおよびbaicaleinは強い阻害を示し,それらの50%阻害濃度はそれぞれ0.4, 0.6, 1.3, 1.7, 2.0 ,2.1 ,3.0および3.6μMであった。フラボノイド類による阻害には少なくとも一対の隣接したヒドロキシル基が必要であった。また,隣接したヒドロキシル基の数が増加するに従い,HIV-1インテダラーゼ阻害活性も上昇した。他方,ヒドロキシル基がmethoxyl基, acetoxyl基, isopropoxyl基, isopentenyl基, benzyloxyl基, glucuronyl基 及びglycosyl基に置換されると阻害活性は減少あるいは消失した。試験したフラバノン,フラバノール,カルコン類には顕著な阻害活性は認められなかった。

• 和漢医薬学会の論文
• 2001-12-31

著者

• 花岡 美代次

  金沢大学薬学部

• HATTORI Masao

  Institute of Natural Medicine, University of Toyama

• Hattori Masao

  Institute Of Natural Medicine University Of Toyama

• MIYASHIRO Hirotsugu

  Institute of Natural Medicine, University of Toyama

• TEWTRAKUL Supinya

  Faculty of Pharmaceutical Sciences, Prince of Songkla University

• TEWTRAKUL Supinya

  Institute of Natural Medicine, Toyama Medical and Pharmaceutical University

• FUJIWARA Tamio

  Shionogi Institute for Medical Science

• FUJIWARA Tamio

  b Shionogi Institute for Medical Science

• YOSHINAGA Tomokazu

  Shionogi Institute for Medical Science

• TOMIMORI Tsuyoshi

  School of Pharmacy, Hokuriku University

• KIZU Haruhisa

  School of Pharmacy, Hokuriku University

• MIYAICHI Yukinori

  School of Pharmacy, Hokuriku University

• Fujiwara T

  B Shionogi Institute For Medical Science

• Tewtrakul Supinya

  Faculty Of Pharmaceutical Sciences Prince Of Songkla University

• Tewtrakul Supinya

  Institute Of Natural Medicine Toyama Medical And Pharmaceutical University

• Hattori Masao

  Institute Of Natural Medicine Faculty Of Pharmaceutical Sciences

• Hattori Masao

  Metabolic Engineering Institute Of Natural Medicine University Of Toyama

• Miyashiro H

  Institute Of Natural Medicine University Of Toyama

• Miyaichi Y

  北陸大学 薬学科生薬学

• Miyaichi Yukinori

  School Of Pharmacy Hokuriku University

• Miyaichi Yukinori

  Department Of Pharmacognosy Pharmaceutical Sciences Hokuriku University

• Tomimori T

  Department Of Pharmacognosy Pharmaceutical Sciences Hokuriku University

• Kizu H

  Department Of Pharmacognosy Pharmaceutical Sciences Hokuriku University

• Tomimori Tsuyoshi

  School Of Pharmacy Hokuriku University

• Tomimori Tsuyoshi

  Research Institute For Wakan-yaku (traditional Sino-japanese Medicine) Toyama Medical And Pharmaceut

• 花岡 美代次

  Institute Of Natural Medicine University Of Toyama

• Kizu Haruhisa

  School Of Pharmacy Hokuriku University

関連論文

• Estrogenic and Antiestrogenic Activities of Phloridzin
• Studies on Antispasmodics. VI. Synthesis of N-Alkyl 6- and 7-Diarylmethyleneindolizidinium Bromides
• Studies on Antispasmodics. V. Synthesis and Anticholinergic Activity of N-Alkyl 1- and 2-Diarylmethylene-indolizidinium Bromides
• 鎮痙剤の研究(第4報)Diarylhydroxymethylquinolizidine Methohalidesの合成と抗アセチルコリン作用
• 鎮痙剤の研究(第3報)2位置換Quinolizidine類の簡便な新合成法とそれらの立体構造について
• 鎮痙剤の研究(第2報)3位置換Quinolizidine類の簡便な新合成法とそれらの立体構造について
• Studies on 1-Azabicyclo Compounds. XXVI. Synthesis of Ten-membered Ring Amines from 9a-Cyanomethyl-, 9a-Ethoxycarbonylmethyl-, and 1-Ethoxycarbonyl-octahydroquinolizine
• Synthesis of (±)-Methyldecamine
• Dacarbazineの光分解によって生成する発痛物質の探索
• Convenient Synthesis of 2,3,9,10-Tetraoxygenated Protoberberine Alkaloids and Their 13-Methyl Alkaloids
• 12-3-B3 ダカルバジン注射剤投与時における血管痛原因物質の探索
• 100(P24) 抗腫瘍性スチリルラクトン化合物の高立体選択的合成(ポスター発表の部)
• (o-トリメチルシリルベンズアルデヒド)クロム錯体を活用する高立体選択的反応の開発
• Erythro-Selective Aldol Reaction of Tricarbonyl(η^6-o-trialkylsilylbenzaldehyde)chromium(0) Complexes with Cyclic Ketene Silyl Acetals
• 18 Protoberberineアルカロイドの新規合成とBenzo[c]phenanthridineアルカロイド(±)-Ambinineの全合成(口頭発表の部)
• Chemical Transformation of Protoberberines. XVII. Biomimetic Introduction of an Oxy Functionality at the C-10 Position in the Benzo[c]phenanthridine Skeleton : Synthesis of 2,3,7,8,10-Pentaoxygenated Benzo[c]phenanthridine Alkaloids, Chelilutine and Sangu
• A FIRST TOTAL SYNTHESIS OF (±)-AMBININE
• Chemical Transformation of Protoberberines. XVI. Regioselective Introduction of an Oxy Functionality at the C_-Position of the Benzo[c]phenanthridine Skeleton : A Convenient Synthesis of Macarpine from Oxychelirubine
• Trimethylsilyl Trifluoromethanesulfonate-Catalyzed Aldol Reaction of Various Aldehydes with Silyl Enol Ethers
• A NOVEL DIASTEREOSELECTIVITY IN THE ALDOL REACTION OF CYCLIC KETENE SILYL ACETALS WITH COBALT-COMPLEXED AND UNCOMPLEXED PROPYNALS
• 学術貢献賞受賞 北 泰行氏の業績
• 故荒田義雄先生を偲んで
• イソキノリンアルカロイドの生合成的合成
• サマリーを重要視(キーワードの使い方)
• 科学研究費の配分について(文部省科学研究費申請と配分の問題点)
• 双環状アミン体から中環状アミン類の合成
• Synthetic Studies on Lythraceae Alkaloids. V. Total Synthesis of (±)-Vertaline
• Synthetic Studies on Lythraceae Alkaloids. IV. Total Synthesis of (±)-Methyldecinine
• Total Synthesis of (±)-Lagerine
• Synthetic Studies on Lythraceae Alkaloids. III. Stereoselective Total Synthesis of (±)-Decaline
• Synthetic Studies on Lythraceae Alkaloids. II. The Mannich Reaction of Isopelletierine with 3-Methoxybenzaldehyde and 3-Hydroxybenzaldehyde
• Studies on 1-Azabicyclo Compounds. XXIV. Synthesis and Stereochemistry of 10-Ethyl-, 10-Vinyl-, and 10-Ethynyl-quinolizidine Methiodides
• Studies on 1-Azabicyclo Compounds. XXII. Stereochemistry of 9a-Substituted Quinolizidine Methiodides
• Metabolism and pharmacokinetics in rats of ganoderiol F, a highly cytotoxic and antitumor triterpene from Ganoderma lucidum
• Pharmacokinetic study of benzoylmesaconine in rats using an enzyme immunoassay system
• Protective Effects of a Neutral Polysaccharide Isolated from the Mycelium of Antrodia cinnamomea on Propionibacterium acnes and Lipopolysaccharide Induced Hepatic Injury in Mice
• Quantitative Determination of Bitter Principles in Specimens of Ganoderma lucidum Using High-Performance Liquid Chromatography and Its Application to the Evaluation of Ganoderma Products
• Chemical Transformation of Protoberberines. XV. : A Novel and Efficient Method for the Introduction of Alkyl Groups on the C-13 Position in the Protoberberine Skeleton
• A NOVEL TOTAL SYNTHESIS OF (±)-CRYPTAUSTOLINE, A DIBENZOPYRROCOLINE ALKALOID
• A NOVEL AND BIOMIMETIC SYNTHESIS OF CHELILUTINE AND SANGUILUTINE
• A TOTAL SYNTHESIS OF (±)-CEPHALOTAXINAMIDE
• 64 ProtoberberineアルカロイドからBenzo [c] phenanthridineアルカロイドの生合成的合成(口頭発表の部)
• 58 ProtoberberineアルカロイドからBenzo[c]phenanthridineアルカロイドの高立体選択的合成
• 33 ProtoberberineからBenzo〔c〕phenanthridine及び3-Arylisoquinolineアルカロイドの合成
• Chemical Transformation of Protoberberines. VIII. A Novel Synthesis of (±)-Fumaricine and a Formal Synthesis of (±)-Alpinigenine
• Chemical Transformation of Protoberberines. VII. Efficient Conversion of Protoberberines into Benzindenoazepines via 8,14-Cycloberbines
• Chemical Transformation of Protoberberines. V. Photochemical Valence Isomerization of Berberinephenolbetaines to 8,14-Cycloberbines, Versatile Aziridine Derivatives for a Novel and Efficient Entry to Spirobenzylisoquinolines and Benzindenoazepines
• Chemical Transformation of Protoberberines. XIII. A Novel and Efficient Synthesis of Antitumor Benzo[c]phenanthridine Alkaloids, Nitidine and Fagaronine(Organic,Chemical)
• Chemical Transformation of Protoberberines. XI. A Novel Synthesis of 2,3,10,11-Tetraoxygenated Protoberberine Alkaloids from Corresponding 2,3,9,10-Tetraoxygenated Protoberberine Alkaloids(Organic,Chemical)
• SYNTHESIS OF FAGARIDINE, A PHENOLIC BENZO [c] PHENANTHRIDINE ALKALOID
• Two New Triterpenes from the Rhizome of Dryopteris crassirhizoma, and Inhibitory Activities of Its Constituents on Human Immunodeficiency Virus-1 Protease
• Enantioselective Dehydroxylation of Enterodiol and Enterolactone Precursors by Human Intestinal Bacteria(Pharmacognosy)
• Developing of anti-HIV agents from natural resources(Chemical & Pharmacological study)
• A New Enzyme Immunoassay for Aconitine and Its Application to Quantitative Determination of Aconitine Levels in Plasma(Pharmacognosy)
• Sesquiterpenes and Alkaloids from Lindera chunii and Their Inhibitory Activities against HIV-1 Integrase
• Flavanone and Flavonol Glycosides from the Leaves of Thevetia peruviana and Their HIV-1 Reverse Transcriptase and HIV-1 Integrase Inhibitory Activities
• Inhibition of Cytopathic Effect of Human Immunodeficiency Virus Type-1 by Various Phorbol Derivatives
• Inhibitory effects of flavonoids on human immunodeficiency virus type-I integrase
• The Heterocyclic Ring Fission and Dehydroxylation of Catechins and Related Compounds by Eubacterium sp.Strain SDG-2, a Human Intestinal Bacterium
• Triterpenes from the Spores of Ganoderma lucidum and Their Cytotoxicity against Meth-A and LLC Tumor Cells
• Inhibition of Human Immunodeficiency Virus Type 1 Reverse Transcriptase and Ribonuclease H Activites by Constituents of Juglans mandshurica
• Inhibitory Effects of Constituents from Cynomorium songaricum and Related Triterpene Derivatives on HIV-1 Protease
• Triterpenes from the Spores of Ganoderma lucidum and Their Inhibitory Activity against HIV-1 Protease
• Isolation and Characterization of a Human Intestinal Bacterium, Eubacterium sp. ARC-2, Capable of Demethylating Arctigenin, in the Essential Metabolic Process to Enterolactone(Pharmacology)
• Inhibitory effect of Yunnan traditional medicines on hepatitis C viral polymerase
• Isolation of a Human Intestinal Bacterium That Transforms Mangiferin to Norathyriol and Inducibility of the Enzyme That Cleaves a C-Glucosyl Bond(Pharmacognosy)
• An Improved Synthesis of Butyl 4-[(4-Amino-5-chloro-2-methoxybenzoyl)amino]-1-piperidineacetate (AU-224)
• Synthesis and Gastrointestinal Prokinetic Activity of Novel Benzamide Derivatives with Amphoteric Side Chains
• New Triterpenoid Saponins from the Roots of Sinocrassula asclepiadea
• INVERSION OF A HYDROXYL GROUP BY THE NEIGHBORING-GROUP PARTICIPATION OF A URETHANE : A GENERAL AND STEREOSELECTIVE SYNTHESIS OF (±)-RADDEANONE, (±)-YENHUSOMIDINE, AND RELATED SPIROBENZYLISOQUINOLINE ALKALOIDS
• A CONVENIENT TRANSFORMATION OF SPIROBENZYLISOQUINOLINES TO DEHYDROPHTHALIDEISOQUINOLINES
• Chemical Transformation of Protoberberines. XII. : A Novel Synthesis of Rhoeadine Alkaloids. : An Alternative Synthesis of a Key Intermediate, Benzindenoazepine, for a Synthesis of (±)-cis-Alpinigenine and (±)-cis-Alpinine from Palmatine(Organic,Chemical)
• A FIRST AND STEREOSELECTIVE SYNTHESIS OF (±)-RADDEANAMINE
• A NOVEL AND HIGHLY STEREOSELECTIVE SYNTHESIS OF (±)-SIBIRICINE
• Chemical Transformation of Protoberberines. VI. Ring D Inversion of Protoberberine Alkaloids. Conversion of Berberine into Non-naturally Occurring 11,12-Oxygenated Protoberberines via Spirobenzylisoquinolines
• 54 8,14-Cycloberbineを経由するProtoberberineアルカロイドからSpirobenzylisoquinoline及びBenzindenoazepineアルカロイドの合成
• 26 Lythraceaeアルカロイドの合成 : (±)-Decaline,(±)-Vertaline,(±)-Desmethyldecaline,(±)-Methyldecinine,(±)-Methyllagerineの全合成
• Withanolide Derivatives from the Roots of Withania somnifera and Their Neurite Outgrowth Activities
• Trigonelline-Induced Neurite Outgrowth in Human Neuroblastoma SK-N-SH Cells
• Biotransformation of Phorbol by Human Intestinal Bacteria
• 1-Azabicyclo化合物の研究(第21報)1,2,3,10,11,11a-Hexahydro-5H-pyrrolo-[2,1-c][1,4]benzodiazepin-11-oneおよび5,6,6a, 7,8,9,10,12-Octahydropyrido[2,1-c][1,4]benzodiazepin-6-oneから中環状AminolactamおよびSpiroaminolactam体の合成
• Synthesis of (±)-Desmethyldecaline
• Synthesis of the Compound proposed as the Structure of Lagerine and Its Non identity with Lagerine
• Synthesis of (±)-Methyldecinine
• Lythraceaeアルカロイドの合成研究(第1報)Isopelletierineの一改良合成
• Total Synthesis of (±)-Vertaline
• Studies on 1-Azabicyclo Compounds. XVIII. Synthesis of Fourteenmembered Ring Diamine, 1,8-Dimethyl-1,8-diazacyclotetradecane, and Related Compounds from Perhydrodipyrido [1,2-a : 1', 2'-d]-pyrazine via Ten-membered Ring Diamine, 2-Methyl-perhydro-2H-pyrid
• Studies on 1-Azabicyclo Compounds. XVI. Synthesis of 1'-Methylindan-2-spiro-2'-piperazine and Related Compounds
• Studies on 1-Azabicyclo Compounds. XV. Oxidation of 1,3,4,6,11,11a-Hexahydro-2H-pyrazino [1,2-b] isoquinolin-1-one Derivatives with Mercuric Acetate, and Their Conversion into 1,2,3,4,5,6,7,8-Octahydro-2-methyl-2,5-benzodiazecine and Related Compounds
• 1,6-Dihydro-3 (2H)-pyridinones. X. 2-Azabicyclo [2.2.2] octane Ring Formation via Intramolecular Michael Reaction : Total Synthesis of (±)-Ibogamine and (±)-Epiibogamine
• 1,6-Dihydro-3 (2H)-pyridinones. IX. A Regioselective Synthesis of Ethyl 3-Methoxycarbonylmethyl-4-oxopiperidine-1-carboxylate from Ethyl 3-Hydroxy-1,2,3,6-tetrahydropyridine-1-carboxylate
• Alkyne-Co2(CO)6錯体を用いる高立体選択的反応の開発
• ジヒドロピリジノンを共通出発原料としたアルカロイド類の合成
• 双環状アミン体から中環状アミン類の合成
• Constituents of the seeds of Glycyrrhiza uralensis
• Screening of Some Indonesian Medicinal Plants for Inhibitory Effects on HIV-1 Protease
• A Comparative Study on the Inhibitory Effects of Flavonoids and Alkaloids on Reverse Transcriptases of Different Retroviruses
• Effects of Flavonoids and Alkaloids on Reverse Transcriptase
• Effects of Ganoderma lucidum Extracts and Their Constituents on the Spontaneous Beating of Myocardial Cell Sheet in Culture
• ラクトン系ミソハギ科アルカロイドの合成

もっと見る 閉じる

スポンサーリンク