(4-Oxo-2-thioxothiazolidin-3-yl)acetic acids as potent and selective aldose reductase inhibitors.

Aldose reductase (AR) has been shown to play an important role in the development of diabetic complications. To search for AR inhibitors from Chinese plants, the ethanol extracts of Chinese plants was tested against an inhibition of rat lens AR in vitro. Among Chinese plants tested, Cissus assamica var. pilosissima and Syzygium oblatum showed highest inhibition of AR (IC50 values, 0.71 and 0.79 μg/ml, respectively). Cissus assamica var. pilosissima and Syzygium oblatum showed more potent inhibitory activity against AR than the positive control, TMG. Consequently, C. assamica var. pilosissima and S. oblatum have a possibility of new natural resources for the development of AR inhibitor for the prevention of diabetic complications.

Rat Lens Aldose Reductase Inhibitory Activities of Cissus assamica var. pilosissima and Syzygium oblatum

Background: Aldose Reductase (AR) enzyme and advanced glycation end products (AGEs) play an important role in diabetic complications. The AR and AGEs inhibitors are beneficial in prevention of diabetic complications. Objective: Aim of present study was to evaluate the in vitro and in vivo AR and AGEs inhibitory activity of an antidiabetic plant Butea monosperma. Methods: The methanolic extract, standardized extract of flower and the major constituent butein were studied for their inhibitory activity against Rat Lens AR (RLAR), rat kidney AR and generation of AGEs. In addition, in vivo inhibition of lens galactitol accumulation in galactose-fed rat model was studied. Results: The plant extracts and butein were shown to possess AR inhibitory activity in both in vitro and in vivo assays with equal potency to that of standard quercetin. In case of inhibited AGEs formation, the plant extracts showed insignificant activity where as butein was found to be potent. Conclusion: The results obtained in this study provide a new dimension to the hitherto unknown activity of the plant as possible protective agent against long-term diabetic complications.

/pdf/aldose-reductase-inhibitory-activity-of-butea-monosperma-for-11l4gddw9e.pdf

Aldose Reductase Inhibitory Activity of Butea monosperma for the Management of Diabetic Complications

/pdf/alterations-of-aldose-reductase-activity-by-indole-3-22b73yum4q.pdf

Alterations of aldose reductase activity by indole-3-carboxaldehyde derivatives

In diabetic conditions, aldose reductase (AR, EC 1.1.1.21) activity is significantly increased in lens, kidney and nerve tissues. Mainly in ocular and neural tissues increased levels of sorbitol is associated with diabetic complications such as retinopathy, nephropathy, neuropahty, cataract formation and also tissue damage via increased reactive oxygen speices. Recently, there are many studies that show the relationship between this enzyme family and cancer. Aldose reductase is important for the pathway and in turn has been a potential target for drug design. Great number of aldose reductase inhibitors (ARIs) are used for prevention or delay of these diabetic complications and cancer. However, effective ARIs which has benefits in diabetic complications are still under investigation. In this study aldose reductase was partially purified from bovine lens and the inhibitory effects of 16 different indol-3-carboxyaldehydederivatives on aldose reductase enzyme activities were examined by kinetic assays. These results suggested that N'-[(5-bromo-1H-indol-3-yl)methylidene]pyridine-4-carbohydrazide showed that the highest inhibitory activity on AR.

Method for isolating tight-binding inhibitors of rat lens aldose reductase.

Whether the inhomogeneity of mudstone foundation leads to abnormal bearing capacity of the driven pile remains controversial. This study introduces the standard penetration test hammering number and needle penetration strength for quantitative analysis by macroscopic observation of the engineering field on the mudstone stratum self-structure and microscopic observation by simple and feasible electronic magnification. The analysis of typical engineering examples demonstrated that the abnormal bearing capacity of piles in the mudstone stratum was related to mudstone inhomogeneity. This study also proposes a method of evaluating mudstone uniformity using the heterogeneous index η, in which η > 2 suggests the need for engineering measures. These findings assist in determining a reasonable solution to the problem of abnormal bearing capacity at driven piles in mudstone foundations.

https://www.frontiersin.org/articles/10.3389/feart.2022.1101955/pdf

Bearing capacity of driven pile and determination of inhomogeneous mudstone around the pile

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Method for isolating tight-binding inhibitors of rat lens aldose reductase.

Bearing capacity of driven pile and determination of inhomogeneous mudstone around the pile