Peroxisome proliferator-activated receptor γ (PPARγ) is a central regulator of adipocyte differentiation and is the principle target of the thiazolidinedione (TZD) class of antidiabetic drugs.1 Harmine is a β-carboline alkaloid that was first isolated from seeds of Peganum harmala (Syrian rue) and Banisteriopsis caapi. Recent work indicates that harmine is a unique regulator of PPARγ expression that acts by inhibiting the Wnt signalling pathway in a cell-specific manner.2 Administration of harmine (30 mg/kg) to obese db/db mice resulted in reduced blood glucose, free fatty acids, and triglyceride levels, delayed hyperglycemia, and improved insulin sensitivity. Harmine also attenuates inflammatory gene expression (TNFα, IL-1β, iNOS) and macrophage accumulation in adipose tissue.2
1
Hauner, H. The mode of action of thiazolidinediones. Diabetes Metab Res Rev18S10-S15(2002).
2
Waki, H., Park, K.W., Mitro, N., et al. The small molecule harmine is an antidiabetic cell-type-specific regulator of PPARγ expression. Cell Metab5357-370(2007).
Formal Name
7-methoxy-1-methyl-9H-pyrido[3,4-b]indole
CAS Number
442-51-3
Molecular Formula
C13H12N2O
Formula Weight
212.1
Formulation
A crystalline solid
Purity
≥98%
λmax
242, 302 nm
Stability
2 years
Storage
-20°C
Shipping
Room temperature
in continental US; may vary elsewhere
SMILES
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COc1ccc2c(c1)[nH]c1c(C)nccc21
Background Reading
Waki, H., Park, K.W., Mitro, N., et al. The small molecule harmine is an antidiabetic cell-type-specific regulator of PPARγ expression. Cell Metab5357-370(2007).
Hauner, H. The mode of action of thiazolidinediones. Diabetes Metab Res Rev18S10-S15(2002).
Harmine is available in the following screening
library: