In another context, cell viability significantly diminishes following a 1-hour exposure to 30% diluted diquafosol, and continues to decrease 6 hours after treatment with 10% and 20% diluted diquafosol. Additionally, 24 hours after wounding monolayers, treatments with 3% diquafosol and 0.3% HCECs demonstrate significantly enhanced wound healing compared to the control[1].
体内研究
In a rat dry eye model, the P2Y2 agonist diquafosol tetrasodium is observed to improve ocular surface health, marked by increases in tear fluid secretion, corneal epithelial resistance, and the release of glycoprotein-containing moieties from goblet cells. Notably, maximal reductions in dye penetrance of about 50% are recorded starting from 2 weeks and continuing for an additional 2 weeks, with effective doses as low as 1%[2].
INS365 effectively mitigates corneal damage at concentrations exceeding 0.1% w/v[3].
体外研究
In another context, cell viability significantly diminishes following a 1-hour exposure to 30% diluted diquafosol, and continues to decrease 6 hours after treatment with 10% and 20% diluted diquafosol. Additionally, 24 hours after wounding monolayers, treatments with 3% diquafosol and 0.3% HCECs demonstrate significantly enhanced wound healing compared to the control[1].
Diquafosol tetrasodium/地夸磷索四钠 细胞实验
Cell Line
Concentration
Treated Time
Description
References
human corneal epithelial cells (HCECs)
1 mM
4 or 6 days
Promoted MUC1 expression and impeded intracellular fluorescein ingress
Invest Ophthalmol Vis Sci. 2022 Feb 1;63(2):31
Human corneal epithelial cells (HCECs)
100 µM
8 hours
To evaluate the effect of Diquafosol on cell viability and wound healing under hyperosmotic stress. Results showed that Diquafosol restored cell viability, promoted wound healing, and reduced the expression of inflammation-related genes.
Cells. 2024 Jul 25;13(15):1251
rabbit meibomian gland cells
0.85%
4 hours
To investigate the effect of Diquafosol on total cholesterol release from rabbit meibomian gland cells, results showed that Diquafosol significantly increased total cholesterol release in a dose-dependent manner, and this effect was significantly inhibited by AR-C118925XX and the intracellular Ca2+ chelator BAPTA-AM.
Sci Rep. 2021 Mar 26;11(1):6989
rabbit meibomian gland cells
0.015% to 0.85%
To investigate the effect of Diquafosol on intracellular Ca2+ signaling in rabbit meibomian gland cells, results showed that Diquafosol significantly increased intracellular Ca2+ signaling in a dose-dependent manner, and this increase was almost completely inhibited by the selective P2Y2 receptor antagonist AR-C118925XX.
Sci Rep. 2021 Mar 26;11(1):6989
Diquafosol tetrasodium/地夸磷索四钠 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
Environmental dry eye stress model
Eye drops
3%
Twice daily for 3 days
To compare the therapeutic effects of 3% Diquafosol eye drops with different molecular weight hyaluronic acid eye drops in environmental dry eye stress model mice. Results showed that the DQ group did not show significant changes in tear secretion volume, but tear film breakup time (BUT) significantly decreased.
Int J Mol Sci. 2020 May 15;21(10):3516
NOD.B10.H2b mice
Desiccation stress-induced dry eye mouse model
Topical
3%
6 times per day for 10 days
To evaluate the effect of Diquafosol on dry eye symptoms including tear quantity, ocular surface stabilization, and inflammation. Results showed that Diquafosol significantly increased tear production and improved corneal epithelial stability, but had a weaker effect on suppressing inflammation in the lacrimal gland.
Sci Rep. 2017 Aug 7;7(1):7413
Mice
Dry eye model
Eye drops
3%
6 times daily for 14 days, then 6 times daily for 22 days
To evaluate the therapeutic effect of Diquafosol on dry eye, results showed that Diquafosol significantly reduced the fluorescein-stained area
Ophthalmol Sci. 2023 Oct 19;4(2):100414
C57BL/6 mice
Experimental dry eye model
Ophthalmic instillation
0.03
6 times daily for 10 days
To evaluate the therapeutic effect of Diquafosol on dry eye disease in vivo. Results showed that Diquafosol reduced corneal staining scores, increased NGF expression, and promoted corneal wound healing.
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