Gliquidone, a sulfonylurea class drug used for treating diabetes mellitus type 2. Gliquidone reduced the body weight and the kidney weight/body weight ratio of mice. Gliquidone improved the kidney function, indicated by reductions in urinary protein, blood urea nitrogen, and serum creatinine and triglyceride. Gliquidone can ameliorate the diabetic symptoms of diabetic nephropathy through inhibiting Notch/Snail1 signaling pathway, improving anti-oxidative response and delaying renal interstitial fibrosis[3]. Gliquidone treatment effectively reduced urinary protein in GK rats with diabetic nephropathy by improving glomerular lesions and promoting tubular reabsorption[4]. Moreover, using gliquidone nanoparticles revealed ~2.5-fold increase in Cmax when taken orally in the form of hard gelatin capsules in comparison to free gliquidone. The developed strategy of gliquidone nanoparticles possess a keen potential for exhibiting anti-diabetic effect[5].
Gliquidone/格列喹酮 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human foreskin fibroblasts 1 (HFF-1)
7.6 µM
5 days
Evaluation of Gliquidone's inhibitory effect on in vitro infection by T. cruzi Querétaro strain, IC50 of 7.6 µM
Pharmaceuticals (Basel). 2024 Dec 27;18(1):21.
Cos7 cells
1, 10, 30, 100 μM
24 hours
To evaluate the effect of gliquidone on PPARγ transcriptional activity. Results showed that gliquidone exhibited PPARγ agonistic activity at 1 μM, increased activity by 3-4 times at 10 μM, and nearly ten times at higher concentrations.
Diabetes Metab J. 2011 Aug;35(4):340-7.
Primary astrocytes
5 μM
5.5 h or 23.5 h
Gliquidone selectively affected LPS-mediated proinflammatory cytokine expression and decreased STAT3/NF-κB signaling in an NLRP3-independent manner.
Front Aging Neurosci. 2021 Oct 29;13:754123.
BV2 microglial cells
5 μM
5.5 h or 23.5 h
Gliquidone significantly decreased LPS-induced proinflammatory cytokine levels and inhibited ERK/STAT3/NF-κB phosphorylation by altering NLRP3 inflammasome activation.
Front Aging Neurosci. 2021 Oct 29;13:754123.
CA3 hippocampal neurons
10μM
Gliquidone significantly depressed the slowly inactivating outward current (ID) by 42·6±7·9% (n=13).
J Physiol. 1993 Jul;466:39-54.
Gliquidone/格列喹酮 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Tail flick test model
Intracerebroventricular injection
0.06-16 μg/mouse
Single injection, observed for 120 minutes
To evaluate the effects of gliquidone on the antinociception induced by different μ-opioid receptor agonists. Results showed that gliquidone antagonized the antinociception induced by buprenorphine, morphine, and methadone but did not affect the effects of fentanyl and levorphanol.
Br J Pharmacol. 1995 Mar;114(6):1296-302
Swiss albino mice
Forced swimming test
Intracerebroventricular injection
6 mg/mouse
Single dose, 20 min before the test
To evaluate the effect of gliquidone on immobility time in mice, results showed that gliquidone significantly reduced immobility time, comparable to tricyclic antidepressants.
Br J Pharmacol. 1999 Apr;126(7):1653-9
Mice
Tail flick test
Intracerebroventricular injection
4-8 μg/mouse
Single administration
Gliquidone significantly antagonized clonidine-induced antinociception but did not significantly modify baclofen-induced antinociception.
Br J Pharmacol. 1993 Nov;110(3):1049-54
Swiss albino mice
Hot-plate test model
Intracerebroventricular injection
6 mg/mouse
Single injection, 15 minutes before the test
Gliquidone, by blocking K ATP channels, prevented the antinociception induced by the α2-adrenoceptor agonists clonidine and guanabenz.
Br J Pharmacol. 1999 Mar;126(5):1214-20
C57BL6/N mice
Neuroinflammatory disease model
Intraperitoneal injection
10 or 20 mg/kg
Daily injections for 3 consecutive days
Gliquidone suppressed LPS-mediated microgliosis, microglial hypertrophy, and proinflammatory cytokine COX-2 and IL-6 levels in wild-type mice, with smaller effects on astrogliosis. Importantly, gliquidone downregulated the LPS-induced microglial NLRP3 inflammasome and peripheral inflammation in wild-type mice.
China, Shanghai
... 展开 >>
Novo Nordisk Investigational Site
Shanghai, Shanghai, China, 200025
Novo Nordisk Investigational Site
Shanghai, Shanghai, China, 200433
China, Sichuan
Novo Nordisk Investigational Site
Chengdu, Sichuan, China, 610041
China
Novo Nordisk Investigational Site
Beijing, China, 100029 收起 <<
China, Shanghai
... 展开 >>
Novo Nordisk Investigational Site
Shanghai, Shanghai, China, 200025
Novo Nordisk Investigational Site
Shanghai, Shanghai, China, 200433
China, Sichuan
Novo Nordisk Investigational Site
Chengdu, Sichuan, China, 610041
China
Novo Nordisk Investigational Site
Beijing, China, 100029 收起 <<
China, Shandong
... 展开 >>
Department of Hematology of the 2nd Hospital of Shandong University
Recruiting
Jinan, Shandong, China, 250033
Contact: chengyun zheng, Ph. D +86-531-85875635 chengyun.zheng@ki.se, kdx2002@126.com 收起 <<
搜索
