Rottlerin, a principal phenolic compound isolated and purified from Kamala plant Mallotus philippinensis, exers its tumour-suppressive function in ACC.
Rottlerin is a compound extracted from Mallotus Philippinensis, functions as a selective inhibitor of Protein Kinase C (PKC), demonstrating IC50 values of 3-6 μM for PKCδ, 30-42 μM for PKCα,β,γ, and 80-100 μM for PKCε,η,ζ. Its mode of action includes acting as a direct mitochondrial uncoupler and promoting autophagy by acting on a signaling cascade upstream of mTORC1. Furthermore, Rottlerin triggers apoptosis through the activation of caspase 3[1].[2].[3].
体内研究
When administered via gavage at a dose of 20 mg/kg five days a week for a duration of six weeks, Rottlerin effectively curbs the growth of AsPC-1 pancreatic tumors in Balb C nude mice without inducing toxicity[3].
Its antitumor effects are attributed to the inhibition of tumor cell proliferation and the induction of apoptosis, facilitated by the activation of caspase-3 and the cleavage of poly(ADP-ribose) polymerase (PARP)[3].
体外研究
In primary Human Microvascular Endothelial Cells (HMVEC), treatment with Rottlerin at 20 μM for 2, 6, and 24 hours significantly reduces cyclin D-1 mRNA levels in a time-dependent manner. At the same concentration, Rottlerin also affects cell proliferation in HMVEC[2].
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