Ponente
Descripción
Betulinic acid, 3β-hydroxy-lup-20(29)-en-28-oic acid, is a naturally occurring pentacyclic triterpenoid widely distributed in the plant kingdom. It has been shown its variety of biological activities including antibacterial, antimalarial, antiinflammatory, anthelmintic and antioxidant properties. This compound is most highly regarded for its anti-HIV-1 activity and specific cytotoxicity against a variety of tumor cell lines (Rios et al., 2018). Betulinic acid has also been reported to inhibit in vitro enzymatic activity of aminopeptidase N (APN, EC 3.4.11.2) (Melzig & Bowman, 1998). APN is a metallo-type actopeptidase, which is involved in a number of processes such as cell survival, cell migration, blood pressure regulation, and viral uptake. This is also involved in the regulation of angiogenesis, being overexpressed in several cancers, and playing a role in metastasis of tumor cells (Barnieh et al., 2021). In the present work, the effects of betulinic acid on the cellular viability/metabolism of APN+ tumor cells have been studied. By a kinetic approach it was quantified the APN activity on different human and murine tumor cells, i.e. MB16F10, A549, NCI-H292, LL/2, CT26WT and MeWo. The effect of the betulinic acid on the cellular viability/metabolism was analyzed for these cellular lines using MTT assay. The results showed that the betulinic acid affected the cell viability in a dose-response manner. There was not found any correlation between the activity levels of the APN and the effects of the betulinic acid on the cellular viability/metabolism for these cellular lines.
References:
• Barnieh, F. M., Loadman, P. M., & Falconer, R. A. (2021). Is tumour-expressed aminopeptidase N (APN/CD13) structurally and functionally unique? Biochimica et Biophysica Acta (BBA)-Reviews on Cancer, 1876(2), 188641.
• Melzig, M. F., & Bormann, H. (1998). Betulinic acid inhibits aminopeptidase N activity. Planta medica, 64(07), 655-657.
• Ríos, J. L., & Máñez, S. (2018). New pharmacological opportunities for betulinic acid. Planta medica, 84(01), 8-19.
