Alpinetin is a type of novel plant flavonoid derived from Alpinia katsumadai Hayata, possesses strong anti-hepatoma effects, can suppress HepG2 cell proliferation and arrested cells in the G0/G1 phase by up-regulating the expression levels of p-MKK7, and the antitumor effect of Alpinetin could be reversed by inhibiting the expression of MKK7; suggests that MKK7 may be a putative target for molecular therapy against hepatoma and Alpinetin could serve as a potential agent for the development of hepatoma therapy.[1]
Alpinetin has antiproliferative effect in BxPC-3 pancreatic cancer cells possibly through the regulation of the Bcl-2 family and XIAP expression, release of cytochrome C and the activation of caspases, it may serve as a potential agent for the development of pancreatic cancer cell therapies.[2]
Alpinetin and cardamonin have vascular effects to relax rat mesenteric arteries through multiple mechanisms; they induce both endothelium-dependent and -independent relaxation, the former is likely mediated by nitric oxide whereas the latter is probably mediated through nonselective inhibition of Ca2+ influx and intracellular Ca2+ release and inhibition of the protein kinase C-dependent contractile mechanism.[3]
Alpinetin has anti-inflammatory properties, can activate PPAR-γ, thereby attenuate TLR4 expression and TLR4 mediated NF-κB and MAPK activation and the release of pro-inflammatory cytokines, suggests that it may be a therapeutic agent against inflammatory diseases. [4]
Alpinetin has antioxidant effects, can protect LPS-induced kidney injury through activating Nrf2 and inhibiting TLR4 expression.[5]
Alpinetin suppresses T-cell-mediated delayed-type hypersensitivity reaction in mice, could shock the activation of NF-κB NFAT2 signal transduction pathways, indicates that it has potential effects in downregulating the immune system and might be developed as a useful immunosuppressive agent in treating undesired immune responses.[6]
[1] Tang B O, Jian D U, Wang J, et al. Oncol Rep, 2012, 27(4):1090-6.
[2] Du J, Tang B, Wang J, et al. Int J Mol Med, 2012, 29(4):607-12.
[3] Wang Z T, Lau C W, Chan F L, et al. J Cardiovasc Pharm, 2001, 37(5):596-606.
[4] Hu K, Yang Y, Tu QY, et al. Eur Journal of Pharmacol, 2013, 721(1-3):96–102.
[5] Huang Y, Zhou L S, Yan L, et al. Int Immunopharmacol, 2015, 28(2):1003-8.
[6] Guan S, Fang B, Song B, et al. Immunopharm Immunot, 2014, 36(4):1-7.
[7] Liu J, Feng Z, W U YH . Pharmacy Today, 2009, 19(4):46-8.
