Curcumin analogs as potent aldose reductase inhibitors.

Du ZY; Bao YD; Liu Z; Qiao W; Ma L; Huang ZS; Gu LQ; Chan AS

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Curcumin analogs as potent aldose reductase inhibitors.

机译：姜黄素类似物可作为有效的醛糖还原酶抑制剂。

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In the present study, curcuminoids isolated from curcuma longa were demonstrated to possess inhibitory activities on bovine lens aldose reductase. In order to find more potent aldose reductase inhibitor, curcumin analogs were synthesized and evaluated for their ability to inhibit bovine lens aldose reductase enzyme. The results indicated that the compounds with tetrahydroxyl groups, 2,6-bis(3,4-dihydroxybenzylidene)cyclohexanone (A(2)), 2,5-bis(3,4-dihydroxybenzylidene)cyclopentanone (B(2)), 1,5-bis(3,4-dihydroxyphenyl)-1,4-pentadiene-3-one (C(2)), and 3,5-bis(3,4-dihydroxybenzylidene)-4-piperidone (D(2)) showed remarkably potent inhibitory effects on aldose reductase with IC(50) of 2.9 microM, 2.6 microM, 3.4 microM, and 4.9 microM, respectively. The structure-activity relationship revealed that the curcumin analogs with ortho-dihydroxyl groups could form a more tight affinity with aldose reductase to exert more potential inhibitory activities.

机译：在本研究中，从姜黄中分离出的姜黄素被证明具有抑制牛晶状体醛糖还原酶的活性。为了找到更有效的醛糖还原酶抑制剂，合成了姜黄素类似物并评估了其抑制牛晶状体醛糖还原酶的能力。结果表明，具有四羟基的化合物，2,6-双（3,4-二羟基亚苄基）环己酮（A（2）），2,5-双（3,4-二羟基亚苄基）环戊酮（B（2））， 1,5-双（3,4-二羟基苯基）-1,4-戊二烯-3-酮（C（2））和3,5-双（3,4-二羟基苄叉）-4-哌啶酮（D（2 ））对醛糖还原酶具有显着的抑制作用，IC（50）分别为2.9 microM，2.6 microM，3.4 microM和4.9 microM。构效关系表明，具有邻二羟基基团的姜黄素类似物可与醛糖还原酶形成更紧密的亲和力，发挥更大的潜在抑制活性。

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《Archiv der Pharmazie》 |2006年第3期|共6页
作者
Du ZY; Bao YD; Liu Z; Qiao W; Ma L; Huang ZS; Gu LQ; Chan AS;
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正文语种 eng
中图分类药学;
关键词
Aldehyde Reductase; Curcumin; Enzyme Inhibitors; 醛还原酶; 姜黄素; 酶抑制剂;

机译：Aldehyde Reductase;Curcumin;Enzyme Inhibitors;醛还原酶;姜黄素;酶抑制剂;

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1. Curcumin analogs as potent aldose reductase inhibitors. [J] . Du ZY, Bao YD, Liu Z, Archiv der Pharmazie . 2006,第3期

机译：姜黄素类似物可作为有效的醛糖还原酶抑制剂。
2. Spirohydantoin derivatives of thiopyrano(2,3-b)pyridin-4(4H)-one as potent in vitro and in vivo aldose reductase inhibitors. [J] . Da Settimo F, Primofiore G, La Motta C, Bioorganic and Medicinal Chemistry . 2005,第2期

机译：硫吡喃（2,3-b）吡啶-4（4H）-的螺乙内酰脲衍生物作为有效的体外和体内醛糖还原酶抑制剂。
3. Synthesis, activity, and molecular modeling of new 2, 4-dioxo-5-(naphthylmethylene)-3-thiazolidineacetic acids and 2-thioxo analogues as potent aldose reductase inhibitors. [J] . Fresneau P, Cussac M, Morand JM, Journal of Medicinal Chemistry . 1998,第24期

机译：作为有效醛糖还原酶抑制剂的新型2,4-二氧代-5-（萘基亚甲基）-3-噻唑烷乙酸和2-thioxo类似物的合成，活性和分子模型。
4. Synthesis and Characterization of Lipid Nanoparticle Formulation of a Poorly Soluble, Highly Potent, Novel Synthetic Analog of Curcumin for Cancer Therapy [C] . Arpan Pradhan, Satyendra Mishra, Avadhesha Surolia, Society for Biomaterials annual meeting and exposition . 2018

机译：姜黄素的水溶性差，高强度，新型合成类似物的脂质纳米颗粒制剂的合成与表征
5. PART 1: SYNTHESIS OF IRREVERSIBLE INHIBITORS OF ALDOSE REDUCTASE WITH SUBSEQUENT DEVELOPMENT OF A CARBON-13 NMR PROTEIN PROBE. PART 2: SYNTHESIS OF SELENIUM ANALOGS OF DOPAMINE AS POTENTIAL DOPAMINE RECEPTOR AGONISTS. [D] . ARES, JEFFREY JOSEPH. 1986

机译：第1部分：合成具有碳13 NMR蛋白质探针的醛糖还原酶的不可逆抑制剂。第2部分：作为潜在的多巴胺受体激动剂的多巴胺硒类似物的合成。
6. Purified rat lens aldose reductase. Polyol production in vitro and its inhibition by aldose reductase inhibitors. [O] . P F Kador, J H Kinoshita, D R Brittain, 1986

机译：纯化的大鼠晶状体醛糖还原酶。多元醇的体外生产及其对醛糖还原酶抑制剂的抑制作用。
7. Curcumin analogs as potent aldose reductase inhibitors [O] . Du ZY, Bao YD, Liu Z, 2006

机译：姜黄素类似物可作为有效的醛糖还原酶抑制剂

Curcumin analogs as potent aldose reductase inhibitors.

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