Ponalrestat: A potent and specific inhibitor of aldose reductase

Ward, Walter H.J.; Sennitt, Christopher M.; Ross, Helen S.; Dingle, Anthony; Timms, David; Mirrlees, Donald J.; Tuffin, D.P.

doi:10.1016/0006-2952(90)90033-h

Cited by 45 publications

(38 citation statements)

References 19 publications

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“…Rat kidney ALR1 was prepared in accordance with a previously reported method [26]. Kidneys were quickly removed from normal killed rats and homogenized (Glas-Potter) in three volumes of 10 mM sodium phosphate buffer, pH ¼ 7.2, containing 0.25 M sucrose, 2.0 mM EDTA dipotassium salt, and 2.5 mM b-mercaptoethanol.…”

Section: Aldehyde Reductase (Alr1)mentioning

confidence: 99%

“…IC 50 values were determined by linear regression analysis of the log of the concentration-response curve. Compounds PS01-PS12 were also assayed for their potency to inhibit SD [25] and two other enzymes not involved in the polyol pathway, namely, ALR1 [26] and GR [27]. Sorbinil [28] and tolrestat [29] were used as the reference standards.…”

Section: Biochemistry and Pharmacologymentioning

confidence: 99%

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RETRACTED: Synthesis and biological evaluation of [1,2,4]triazino[4,3-a] benzimidazole acetic acid derivatives as selective aldose reductase inhibitors

Sahoo

Behera²

2010

European Journal of Medicinal Chemistry

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Section: Aldehyde Reductase (Alr1)mentioning

confidence: 99%

Section: Biochemistry and Pharmacologymentioning

confidence: 99%

RETRACTED: Synthesis and biological evaluation of [1,2,4]triazino[4,3-a] benzimidazole acetic acid derivatives as selective aldose reductase inhibitors

Sahoo

Behera²

2010

European Journal of Medicinal Chemistry

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“…Rat kidney ALR1 was prepared in accordance with a previously reported method. 53 Kidneys were quickly removed from normal killed rats and homogenized (GlasPotter) in three volumes of 10 mM sodium phosphate buffer, pH 7.2, containing 0.25 M sucrose, 2.0 mM EDTA dipotassium salt, and 2.5 mM -mercaptoethanol. The homogenate was centrifuged at 12 000 rpm at 0-4°C for 30 min and the supernatant was subjected to a 40-75% ammonium sulfate fractionation, following the same procedure previously described for ALR2.…”

Section: General Procedures For the Synthesis Of 2-phenylpyrido[12-a]mentioning

confidence: 99%

Pyrido[1,2-a]pyrimidin-4-one Derivatives as a Novel Class of Selective Aldose Reductase Inhibitors Exhibiting Antioxidant Activity

et al. 2007

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pyrimidin-4-one derivatives bearing a phenol or a catechol moiety in position 2 were tested as aldose reductase (ALR2) inhibitors and exhibited activity levels in the micromolar/submicromolar range. Introduction of a hydroxy group in position 6 or 9 gave an enhancement of the inhibitory potency (compare 18, 19, 28, and 29 vs 13 and 14). Lengthening of the 2-side chain to benzyl determined a general reduction in activity. The lack or the methylation of the phenol or catechol hydroxyls gave inactive (10-12, 21, 22, 25-27) or scarcely active (15, 17, 20) compounds, thus demonstrating that the phenol or catechol hydroxyls are involved in the enzyme pharmacophoric recognition. Moreover, all the pyridopyrimidinones displayed significant antioxidant properties, with the best activity shown by the catechol derivatives. The theoretical binding mode of the most active compounds obtained by docking simulations into the ALR2 crystal structure was fully consistent with the structure-activity relationships in the pyrido[1,2-a]pyrimidin-4-one series.

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“…This was done according to Hayman [17] with minor modification; the modification to the method was done by adding different mass of ammonium sulphate to the supernatant depending on the volume of supernatant collected as percentage of saturation increases.…”

Section: Isolation and Purification Of Aldose Reductase Enzyme (Alr2)mentioning

confidence: 99%

Characterization and Evaluation of Vernonia amygdalina Extracts for its Antidiabetic Potentials

E¹,

A²,

O.T³

et al. 2018

ijSciences

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Abstract:Background: There is increase in the demand for the use of medicinal plants for the treatment of various ailments such as cancer, hypertension and diabetes locally as a result of the inability of the synthesized drugs to completely eradicate the ailments and also with the attendant side effects attached to the use of drugs. Objective: The aim of this research work was to investigate the Aldose reductase, α-glucosidase, β -glucosidase and maltase glucoamylase inhibitory potential of the crude extracts of Vernonia amygdalina, and characterizing the extracts. Materials and method:The leaves of the plant was obtained, air dried and turned to powdered form using commercial grinding machine with dimension 34×38×75. The extracted crudes were subjected into in-vitro studies of the inhibitory potentials using recommended protocols. The IC 50 values were calculated using Graph pad prism 5.0 software and the identified compounds were screened for drug properties using ONLINE OSIRIS server explorer. Results: The (IC 50 0.6 ± 0.03 μg/mL) of the chloroform extract was better than the methanolic extract of IC 50 (1.532±0.63μg/mL) and the results were better than the acarbose standard (IC 50 234.6 + 2.01μM). The maltase glucoamylase inhibitory potentials of the chloroform and methanolic extracts in the range of IC 50 1.112 ± 0.90 μg/mL and 1.315 ± 0.7 μg/mL. The β-glucosidase screening of the extracts results indicated that they do not have good selective inhibitor properties. IC 50 of Aldose reductase (ALR2) of chloroform extract IC 50 (1.339+0.264μg/mL) was better than that of methanolic extract of IC 50 (1.437+0.6μg/mL) and these values were better when compared with the standard, sorbinil of IC 50 (3.10 +0.20μM).The aldehyde reductase (ALR1) of methanolic extract IC 50 (0.325+0.02μg/mL) was better than that of chloroform extract of IC 50 (0.964+0.16μg/mL) and when compared with standard 10mM vaproic acid IC 50 (57.4 +10μM).The GC-MS of the chloroform extract revealed compounds which were screened computationally to for various drug properties such as drug likeness, cLogS, cLogP, H-bond acceptor and H-bond Donor. Conclusion: The promising inhibitory potential of the plant extracts and characterization of the extract is an indication of the usefulness of the plant for the treatment of diabetes.

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Ponalrestat: A potent and specific inhibitor of aldose reductase

Cited by 45 publications

References 19 publications

RETRACTED: Synthesis and biological evaluation of [1,2,4]triazino[4,3-a] benzimidazole acetic acid derivatives as selective aldose reductase inhibitors

RETRACTED: Synthesis and biological evaluation of [1,2,4]triazino[4,3-a] benzimidazole acetic acid derivatives as selective aldose reductase inhibitors

Pyrido[1,2-a]pyrimidin-4-one Derivatives as a Novel Class of Selective Aldose Reductase Inhibitors Exhibiting Antioxidant Activity

Characterization and Evaluation of Vernonia amygdalina Extracts for its Antidiabetic Potentials

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