Automating a 96-well microtiter plate assay for identification of AGEs inhibitors or inducers: application to the screening of a small natural compounds library

Abstract

Advanced glycation end-products (AGEs) are involved in the pathogenesis of numerous affections such as diabetes and neurological diseases. AGEs are also implied in various changes in tissues and organs. Therefore, compounds able to break them or inhibit their formation may be considered as potential drugs, dietary supplements, or bioactive additives. In this study, we have developed a rapid and reliable (Z' factor calculation) anti-AGEs activity screening based on the overall fluorescence of AGEs. This method was successfully evaluated on known AGEs inhibitors and on a small library of natural compounds, yielding coherent results when compared with literature data.

Antidiabetic property of Aerva lanata (L.) Juss. ex Schult. is mediated by inhibition of alpha glucosidase, protein glycation and stimulation of adipogenesis 软毛白花苋(L.)的降糖特性是通过对α葡萄糖甙酶与蛋白质糖基化的抑制以及脂肪生成的刺激达成的

“…Hyperglycemia induced oxidative stress is responsible for the early onset of secondary complications in diabetic patients . Increased ROS accelerate formation of AGEs leading to neuropathy, nephropathy and retinopathy …”

“…35 Increased ROS accelerate formation of AGEs leading to neuropathy, nephropathy and retinopathy. 27,36,36 Therefore, therapeutic measures to reduce hyperglycemia induced oxidative stress could be beneficial for diabetic patients. Exposure of HepG2 cells to high glucose stress (25 mM glucose) caused a significant increase in ROS.…”

Anti-Advanced glycation end-product and free radical scavenging activity of plants from the yucatecan flora

“…[21] In addition, since many plants are traditionally used to treat diseases such as diabetes and others disorders associated with AGE formation, these particular species constitute a potentially important source for the search of novel secondary metabolites with anti-AGE activity. [22] We wish to report herein on the results of evaluating the anti-AGEs and radical scavenging activity of the organic extracts and aqueous traditional preparations of nine plants used in Yucatecan traditional medicine to treat diabetes, hypertension, and obesity.…”

Preparative Isolation, Fast Centrifugal Partition Chromatography Purification and Biological Activity of Cajaflavanone from Derris ferruginea Stems

“…According to Matsuda, the anti‐AGE activity of flavonoids increased with the number of free hydroxyl groups in positions 3'‐, 4'‐, 5‐ and 7. However, although its oxygen in position 7 is integrated within a dihydropyran ring, 1 exhibited inhibition of AGE formation to a similar extent as naringenin (0.6 m m in the same assay; Derbré et al , ), which bears a free OH group in position 7. These findings suggest that 1 , with its prenyl groups, exerts its anti‐AGE properties through mechanisms that differ from radical scavenging.…”