Gallein acts as a G protein βγ (Gβγ) subunit signaling inhibitor, disrupting the interaction between Gβγ subunits and PI3Kγ, and is recognized as an anticancer agent[1]. Gallein is employed as a red dye, an acid-base indicator, and as a detection reagent for phosphates[2].
Gallein/茜素紫 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Adult mouse cardiomyocytes
10 μM
Reduced β-AR-mediated membrane recruitment of GRK2
Circ Res. 2010 Aug 20;107(4):532-9
HL-60 cells
10 μM
10 minutes
Inhibited fMLP-induced PIP3 production
Arthritis Rheumatol. 2016 Sep;68(9):2244-56
Human T cells
10 μM
10 minutes
Inhibited CXCL12-dependent chemotaxis
Arthritis Rheumatol. 2016 Sep;68(9):2244-56
cultured human pheochromocytoma slices
10 µmol/l
48 hours
attenuates catecholamine secretion, inhibits GRK2 expression and membrane translocation
J Am Coll Cardiol. 2014 Jun 17;63(23):2549-2557
Mouse neutrophils
10 μM
10 minutes
Inhibited fMLP-dependent chemotaxis but not GM-CSF-dependent chemotaxis
Arthritis Rheumatol. 2016 Sep;68(9):2244-56
Mesenteric artery smooth muscle cells
50µmol/L
30 minutes
To investigate the effect of Gβγ inhibition on the association between Kv7.4 and Gβ subunits, results showed that gallein treatment had no significant effect on the number of Kv7.4-Gβ puncta in MA.
To investigate the effect of Gβγ inhibition on the association between Kv7.4 and Gβ subunits, results showed that gallein treatment reduced the number of Kv7.4-Gβ puncta.
Proc Natl Acad Sci U S A. 2015 May 19;112(20):6497-502
HEK293 cells
100 μM
10 minutes
Gallein completely abolished Kv7.4 currents
Proc Natl Acad Sci U S A. 2015 May 19;112(20):6497-502
Gallein/茜素紫 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rats
Right ventricular hypertrophy induced by pulmonary arterial hypertension (PAH-RVH) and pulmonary artery banding (PAB-RVH)
Intraperitoneal injection
1.8 mg/kg/day
Once daily for 2 weeks
To evaluate the therapeutic effects of Gallein on cardiac function and exercise capacity in RVH models. Results showed that Gallein treatment increased cardiac output and exercise capacity, and reduced GRK2 expression and activity.
Circulation. 2012 Dec 11;126(24):2859-69
Mice
Myocardial ischemia-reperfusion injury model
Intraperitoneal injection
2.5 mg/kg/day titrated to 10 mg/kg/day
Once daily for 3 weeks
To evaluate the effect of Gallein on cardiac function and fibrotic remodeling post-myocardial ischemia-reperfusion injury. Results showed that Gallein significantly preserved cardiac contractility, reduced cardiac fibrotic remodeling, and decreased expression of fibrotic markers.
J Am Coll Cardiol. 2017 Aug 22;70(8):958-971
Mice
Pressure-overload model of HF
Intraperitoneal injection
10 mg/kg/day
Daily administration for 8 weeks
Improved survival and cardiac function, attenuated cardiac remodeling, reduced plasma catecholamine levels, restored adrenal α2-AR feedback inhibitory function
J Am Coll Cardiol. 2014 Jun 17;63(23):2549-2557
NZB/NZW F1 female mice
Lupus-prone mouse model
Intraperitoneal injection
20 mg/kg or 35 mg/kg
3 times/week for 20 weeks
Reduced accumulation of T cells and germinal center B cells in the spleen, decreased accumulation of auto-reactive antibody-secreting cells in the kidneys, reduced immune complex deposition, inhibited kidney inflammation, prevented glomerular damage, and decreased proteinuria
Arthritis Rheumatol. 2016 Sep;68(9):2244-56
Mice
CSQ overexpressing mice
Peritoneal injection
30 mg/kg/day
Once daily for 28 days
Halted HF progression, and partially normalized heart size, morphology and cardiac expression of HF marker genes
Circ Res. 2010 Aug 20;107(4):532-9
Wistar rats
Renal, mesenteric and cerebral arteries
In vitro myography
50µmol/L
Single administration, duration not specified
To investigate the effect of Gβγ inhibition on isoproterenol and CGRP-induced relaxations in different arteries, results showed that gallein significantly inhibited isoproterenol-induced relaxations in renal arteries but had no significant effect in mesenteric arteries.
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