Aims and Scope
Acridocarpus orientalis (AO) is a medicinal herb indigenous to tropical and subtropical Africa, Arabian Peninsula, and New Caledonia with reported anti-inflammatory and antioxidant properties.
To determine whether AO has any beneficial effects on diabetes-induced metabolic parameters in rats.
Materials and Methods:
Diabetes mellitus was induced in male Wistar rats by streptozotocin. Diabetic rats were treated with three doses of AO extract (50, 100, and 200 mg/kg BW) for 30 days. Kidney, liver, and pancreatic tissue samples were processed for histopathology to determine the effect of AO on the cells of these organs. The effect of AO on pancreatic islet cells and serum insulin levels was also examined using immunohistochemistry and enzyme-linked immunosorbent assay techniques, respectively.
AO (100 mg/kg BW) caused a marked reduction in blood glucose levels in diabetic rats compared to diabetic control on day 10 of the study. Moreover, AO (200 mg/kg BW) increased the number of insulin-positive cells with a concomitant reduction in the number of glucagon-immunoreactive cells in pancreatic islets. AO (100 mg/kg) also increased the serum level of superoxide dismutase significantly. Although the administration of AO was able to significantly decrease the diabetes-associated increases in serum creatinine and bilirubin levels, it had no effect on blood urea nitrogen, serum aspartate, or alanine aminotransferase levels. Histopathological examination showed that AO has no toxic effect on the structure of the pancreas, liver, and kidney.
Our findings showed that AO could alleviate some complications of diabetes mellitus.
November 27, 2020
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- July 30, 2020
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- June 29, 2020
Synthesis and Functional Evaluation of Novel Aldose Reductase Inhibitors Bearing a Spirobenzopyran ScaffoldMaria Digiacomo, Stefania Sartini, Giulia Nesi, Simona Sestito, Vito Coviello, Concettina La Motta, Simona Rapposelli
Aldose reductase, the first enzyme of the polyol pathway, is the key determinant for the pathogenesis of long term diabetic complications. Accordingly, its inhibition represents the major therapeutic strategy to treat this kind of pathologies.
In this work we describe the synthesis and the functional evaluation of a number of spiro-oxazolidinone and spiro-morpholinone acetic acid derivatives, and their benzyloxy analogs, developed as aldose reductase inhibitors.
Most of them proved to inhibit the target enzyme, showing IC50 values in the micromolar/low micromolar range. SARs observed among the three different series allowed to highlight their key pharmacophoric elements, thus creating sound basis for the design of novel and more effective inhibitors.
Although further substitution patterns are needed, the novel compounds here proposed represent a good starting point for the development of novel and effective ARIs.
January 31, 2017