REVIEW Harmine, a beta-carboline alkaloid has various types of pharmacological activities. It acts on gamma-aminobutyric acid type A and monoamine oxidase A or B receptor, enhances insulin sensitivity and also produces vasorelaxant effect. Harmine prevents bone loss by suppressing osteoclastogenesis Several potential molecular targets that have been identified for the central pharmacological effects of harmine include cyclin-dependent kinases CDKs (CDK1, 2 and 5), MAO A, 5-HT2A and imidazoline receptors I1 and I2 sites. Harmine is a highly potent inhibitor of dual-specificity tyrosine-phosphorylation regulated kinase (DYRK). Harmine possesses anxiolytic, behavioral effects and anti-tumor potential both in vitro and in vivo. Harmine has high inhibitory affinity of DYRK1A kinase activity, suggesting that harmine could alter tau phosphorylation. Harmine also has dual effects on the upstroke of the action potential of atrial muscle. Harmine was reported to have cytotoxic activity against human tumor cell lines. Harmine, has also been shown to be an antidiabeticis cell-type-specific regulator of PPAR-gamma expression.
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Egusa H, Doi M, Saeki M, Fukuyasu S, Akashi Y, Yokota Y, et al. et al. The small molecule harmine regulates NFATc1 and Id2 expression in osteoclast progenitor cells. Bone. 2011;49(2):264-274.
Réus GZ, Stringari RB, Gonçalves CL, Scaini G, Carvalho-Silva M, Jeremias GC, et al. et al. Administration of harmine and imipramine alters creatine kinase and mitochondrial respiratory chain activities in the rat brain. Depress Res Treat. 2012;2012:987397.
'Frost D, Meechoovet B, Wang T, Gately S, Giorgetti M, Shcherbakova I, et al. et al. Beta-carboline compounds, including harmine, inhibit DYRK1A and tau phosphorylation at multiple Alzheimer''s disease-related sites. PLoS One. 2011;6(5):e19264.'
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