Natural products are widely recognized as an important source of new therapeutic molecules and inspiration for drug development. Medicinal plants are traditionally used to treat several serious diseases. In particular, Plectranthus spp., usually used in folk medicine, is an important source bioactive molecules, namely diterpenoids. Abietane diterpenoids, widely found in Plectranthus spp. have a broad spectrum of biological activities.

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 7α-acetoxy-6β-hydroxyroyleanone (Roy) isolated from P. grandidentatus. A particular example is the patented diterpenoid dibenzoylroyleanone (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 investigate 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.

Patrícia Rijo has a degree in chemistry from the Faculty of Sciences of the University of Lisbon (FCUL), and a Master and PhD in Pharmaceutical and Therapeutic Chemistry from the Faculty of Pharmacy of the University of Lisbon (FFUL). She is currently an associate professor at the School of Health Sciences and Technologies (ECTS) at Universidade Lusófona (ULHT, Lisbon, Portugal) where she is responsible for Organic Medicinal Chemistry and Pharmacognosy and the international coordinator. The main area of research are medicinal chemistry, phytochemistry, and pharmacognosy, with an emphasis on the chemistry of natural products. She is the director of Research and Innovation at CBIOS (Research Center for Biosciences and Health Technologies at Universidade Lusófona), where she leads the laboratory of natural bioactives (Bio. Natural). She has published more than one hundred and forty articles in international journals, has more than three hundred communications (oral and panel) presented at national and international meetings and conferences, and has three registered patents.