PLECTRANTHUS: A VALUABLE SOURCE OF BIOACTIVE COMPOUNDS FOR THERAPEUTIC APPLICATIONS.

Plectranthus spp., commonly used in folk medicine, stands as a significant source of bioactive abietane diterpenoids with a broad spectrum of biological activities, supported by recent scientific studies. 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 7a-acetoxy-6ß-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. [ABSTRACT FROM AUTHOR]