@conference{
author = "Bangay, Gabrielle and Isca, Vera and Domínguez-Martín, Eva María and Santos, Daniel J.V.A. and Díaz-Lanza, Ana María and Saraiva, Lucília and Afonso, Carlos A.M. and Jovanović, Mirna and Pešić, Milica and Rijo, Patricia",
year = "2023",
abstract = "Multidrug resistant (MDR) cancer cases continue to increase, such that the search for novel and more effective anti-cancer therapeutics is of high priority. In some MDR cancers, the overexpression of membrane transport proteins, like P-glycoprotein (P-gp), continues to be a major impediment to successful therapy. Plectranthus genus (Lamiaceae), known for their medicinal and therapeutic properties, is a well-known source of bioactive diterpenoids, such as 7α-acetoxy-6β-hydroxyroyleanone (Roy) and 6,7- dehydroroyleanone (DeRoy). Based on in silico molecular docking studies, a small library of semi-synthetic derivates was prepared. The antitumoural activity of the compounds was assessed in resistant human cancer cell lines NCI-H460/R and DLD1-TxR. Cell viability was assessed using MTT assay and cell death induction by Annexin V/PI. Overall, it was demonstrated that three of the abietane diterpenoid analogues induced P-gp inhibition in MDR cancer cell lines, presenting novel selective compounds for the possible treatment of lung and colon cancer. Moreover, Roy and DeRoy nano-formulations were successfully prepared. DeRoy hybrid nanoparticles significantly increased the efficacy of DeRoy in NCI-H460 and NCI- H460/R. Roy, conjugated with oleic acid afforded self-assembly nanoparticles, to improve aqueous solubility and bioavailability of Roy. This new nano formulation did not decrease cell viability of Vero-E6 cells when compared to Roy with potential as a pro-drug delivery system. Currently, top hit derivatives are being prepared into nano-formulations for prospective pharmaceutical use as P-gp modulators.",
publisher = "Georg Thieme Verlag KG",
journal = "71st International Congress and Annual Meeting of the Society for Medicinal Plant and Natural Product Research (GA); 2023 Jul 2-5; Dublin, Ireland",
title = "New formulations with royleanone derivatives from Plectranthus spp. to inhibit P-glycoprotein activity",
doi = "10.1055/s-0043-1774270",
pages = "1424"
}