dla nienapromieniowanej i napromieniowanej promieniami X ludzkiej reduktazy aldozy[2]
w celu przetestowania jego działania ochronnego u myszy ze zwłóknieniem płuc wywołanym bleomycyną[3]
Działania biochem./fizjol.
Epalrestat hamuje reduktazę aldozy (AR) zaangażowaną w ograniczający szybkość etap konwersji glukozy do sorbitolu w warunkach hiperglikemii. Reduktaza aldozy była celem wielu badań klinicznych w leczeniu neuropatii cukrzycowej i retinopatii. Epalrestat jest lekiem zatwierdzonym w Japonii i Indiach, stosowanym w leczeniu neuropatii cukrzycowej.
Epalrestat is a carboxylic acid derivative which inhibits aldose reductase, an enzyme of the sorbitol (polyol) pathway. Under hyperglycaemic conditions epalrestat reduces intracellular sorbitol accumulation, which has been implicated in the pathogenesis of late-onset complications of diabetes mellitus. Epalrestat 150
Diabetic neuropathy is one of the most common long-term complications in patients with diabetes mellitus, with a prevalence of 60-70% in the United States. Treatment options include antidepressants, anticonvulsants, tramadol, and capsaicin. These agents are modestly effective for symptomatic relief
Drug development research, 83(3), 586-604 (2021-09-30)
A series of novel sulfonates containing quinazolin-4(3H)-one ring derivatives was designed to inhibit aldose reductase (ALR2, EC 1.1.1.21). Novel quinazolinone derivatives (1-21) were synthesized from the reaction of sulfonated aldehydes with 3-amino-2-alkylquinazolin-4(3H)-ones in glacial acetic acid with good yields (85%-94%).
The American journal of Chinese medicine, 41(4), 801-815 (2013-07-31)
The lignan extracts from the tree bark of Eucommia ulmoides Oliv., a famous traditional Chinese medicine, have been demonstrated to have inhibitory effects on aldose reductase activity in spontaneously hypertensive rat myocardium. This study was aimed to investigate the hypertensive
Alzheimer disease is characterized by pathological aggregation of two proteins, tau and Abeta-amyloid, both of which are considered to be toxic to neurons. In this review we summarize recent advances on small molecule inhibitors of protein aggregation with emphasis on
Nasz zespół naukowców ma doświadczenie we wszystkich obszarach badań, w tym w naukach przyrodniczych, materiałoznawstwie, syntezie chemicznej, chromatografii, analityce i wielu innych dziedzinach.
