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Corosolic acid β is a synthetic pentacyclic triterpenoid and derivative of corosolic acid (Item No. 27887) that has been used in the generation of lipid nanoparticles (LNPs) for the delivery of mRNA and siRNA in vitro and in vivo.1 It also inhibits glycogen phosphorylase (IC50 = 82.5 µM for the rabbit muscle enzyme).2 LNPs containing corosolic acid β and encapsulating an mRNA reporter show greater transfection efficiency than those containing cholesterol (Item Nos. 9003100 | 39088) in 4T1, B16/F10, and HeLa cells.1 Corosolic acid β-containing LNPs selectively accumulate in tumors and do not accumulate in the liver compared with cholesterol-containing LNPs, which accumulate in both, following intratumoral injection. LNPs containing corosolic acid β and encapsulating siRNA targeting mRNA encoding Bcl-2 decrease tumor volume and lung metastasis and increase survival in a 4T1 murine mammary carcinoma model.
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1. Corosolic acid derivative-
2. Pentacyclic triterpenes. Part 5: Synthesis and SAR study of corosolic acid derivatives as inhibitors of glycogen phosphorylases. Bioorg. Med. Chem. Lett. 17(21), 5777-5782 (2007).