Description
Statil is an aldose reductase inhibitor that blocks the conversion of glucose to sorbitol. It demonstrates selectivity for aldose reductase 2 over aldose reductase 1 with K
i values of 7.7 nM and 60 μM, respectively. Statil has been shown to prevent diabetes-induced alterations of the cardiovascular system in 14-day streptozotocin-diabetic rats. Aldose reductase inhibition by statil has also been used to impair the synthesis of prostaglandin F
2α by human cultured preadipocytes.
Uses
Inhibitor (aldose reductase).
Uses
Statil is a knon aldose reductase inhibitor which blocks the conversion of glucose to sorbitol. In addition it suppresses cell cancer growth
Definition
ChEBI: 2-[3-[(4-bromo-2-fluorophenyl)methyl]-4-oxo-1-phthalazinyl]acetic acid is a member of phthalazines.
Biological Activity
Potent aldose reductase inhibitor.
in vivo
Ponalrestat (ICI 128436; 10, 50 mg/kg; orally; daily; 8 weeks) reduces sorbitol accumulation indicating efficacy of aldose reductase inhibition[3].
| Animal Model: | Adult female Sprague-Dawley rats[3] |
| Dosage: | 10, 50 mg/kg |
| Administration: | Orally; daily; 8 weeks |
| Result: | Reduced sorbitol accumulation.
|
References
[1] WALTER H.J. WARD . Ponalrestat: A potent and specific inhibitor of aldose reductase[J]. Biochemical pharmacology, 1990, 39 2: Pages 337-346. DOI:
10.1016/0006-2952(90)90033-h[2] DONNA J. OTTER Russell C W. The effects of aldose reductase inhibition with ponalrestat on changes in vascular function in streptozotocin diabetic rats[J]. British Journal of Pharmacology, 1994, 113 2: 576-580. DOI:
10.1111/j.1476-5381.1994.tb17028.x[3] ANDRéANNE MICHAUD. Prostaglandin (PG) F2 alpha synthesis in human subcutaneous and omental adipose tissue: modulation by inflammatory cytokines and role of the human aldose reductase AKR1B1.[J]. PLoS ONE, 2014: e90861. DOI:
10.1371/journal.pone.0090861
