PLECTRANTHUS: A VALUABLE SOURCE OF BIOACTIVE COMPOUNDS FOR THERAPEUTIC APPLICATIONS

Herein, it is reported several approaches using these bioactive lead molecules obtained from Plectranthus spp. for therapeutics applications, such as Parvifloron D (ParvD) isolated from P. ecklonii, , or 7 alpha-acetoxy-6 beta-hydroxyroyleanone (Roy) isolated from P. grandidentatus. . A particular example is the patented diterpenoid benzoylroyleanone (RoyBz), prepared from natural Roy. RoyBz was identified as a PKC-selective activator with potent anti-proliferative activity in colon cancer by stimulating a PKC-dependent mitochondrial apoptotic pathway. Notably, the PKCd-dependent anticancer activity was recapitulated in vivo using xenograft mouse models of control and PKCd-knockdown human colon cancer cells. We further investigate the molecular mechanism underlying the reported antitumor activity of Roy-Bz, and herein, we investigated the impact of Roy-Bz on glucose metabolism of colon cancer cells. This work provides insights into the role of PKC in tumor cell metabolism. Moreover, it strongly supports the ability of Roy-Bz to target both ATP producing pathways of glucose metabolism in cancer cells, thereby reinforcing its potential as an anticancer agent.