Kaempferitrin can activate insulin signaling pathway, phosphorylateAkt kinase and exert the transloocation of GLUT4, thus has antitumor, antidepressant and antidiabetic effects. Kaempferitrin is a natural product isolated and purified from the root of Kaempferia galangal L..
Kaempferitrin (KM) is a natural flavonoid, possesses antinociceptive, anti-inflammatory, anti-diabetic, antitumoral and chemopreventive effects, and activates insulin signaling pathway. Kaempferitrin causes survival rates higher than 90% at 1-20 μM in matured 3T3-L1 adipocyte, and the survival rates decline rapidly at 25 and 50 μM. Kaempferitrin (15 μM) increases insulin receptor beta tyrosine phosphorylation and tyrosine phosphorylation of the insulin receptor substrate 1, and such effects are similar to that of 10 nM insulin. In addition, Kaempferitrin increases the total levels of Glu4 protein in differentiated cells and secreted adiponectin in mature 3T3-L1 adipocytes[3]. KM induces high cytotoxic effects in vitro and in vivo against HeLa cells. Kaempferitrin (2.5, 10 and 25 mg/kg, i.p.) markedly suppresses the growth of tumor by 40%, 87% and 97%, and decreases tumor weight by 37%, 81% and 95%, respectively in nu/nu mice bearing HeLa tumor[4]. Kaempferitrin decreased the levels of interleukin (IL)-1β, IL-6, tumor necrosis factor (TNF)-α, matrix metalloproteinase (MMP)-1, and MMP-3 in MH7A cells. Moreover, kaempferitrin blocked the activation of nuclear factor-κB (NF-κB) and protein kinase B (Akt)/mammalian target of rapamycin (mTOR) pathways. Furthermore, treatment with kaempferitrin decreased paw thickness and arthritis scores, and reduced the serum levels of IL-1β, IL-6, and TNF-α in a collagen-induced arthritis mouse model[5]. KM effectively increased SOD (Superoxide dismutase) activity, decreased MDA (malondialdehyde) levels, suppressed ROS (Reactive oxygen species) generation, and protected against OS (oxidative stress) in AGE-induced (Advanced glycation end products) GMCs[6].
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