@conference{
author = "Isca, Vera and Duro, Ana and Bangay, Gabrielle and Princiotto, Salvatore and Dinić, Jelena and Pešić, Milica and Saraiva, Lucilia and Afonso, Carlos and Rijo, Patricia",
year = "2022",
abstract = "Nature is the most important source of novel pharmacologically active compounds for cancer
treatment. Plectranthus genus (Lamiaceae) has been widely used in traditional medicine and
seems to be promising for the research of new drug leads. In fact, Plectranthus spp. are rich in
cytotoxic diterpenoids, such as the 6,7-dehydroroyleanone (DeRoy) and the 7α-acetoxy-6β-
hydroxyroyleanone (Roy). (1) Royleanone diterpenoids are commonly very low water-soluble
compounds and nanotechnology can be employed to improve drug solubility and targeted
delivery: moreover, nanoformulations are often able to decrease the most frequent side effects
associated to chemotherapy. (2) Hybrid nanoparticles of DeRoy have shown an increased efficacy
of the natural royleanone on NCI-H460 and NCI-H460/R cell lines. (3) Additionally, self-
assembling nanoparticles combined with Roy reduced the cytotoxicity against normal cells (Vero-
E6) compared to parent compound (Roy) and displayed a low release of Roy at physiological pH.
(2) These results suggest that nano-assemblies of royleanones may act as a promising anticancer
strategy.
In this report, we describe the extraction and isolation of Roy from P. grandidentatus. Also, Roy
was derivatized with the goal of improving its antitumoral proprieties. Several derivatives were
prepared with overall good yields and are currently under in vitro antitumoral evaluation. So far,
two benzoylated derivatives revealed promising cytotoxic properties to be further exploited in
nanoformulations. Overall, we expect that derivatives in nanosystems can improve the drug
delivery and lead to an enhanced anticancer activity.",
publisher = "ALIES - Associação Lusófona para o Desenvolvimento da Investigação e do Ensino das Ciências da Saúde",
journal = "Book of abstracts: InnovDelivery '22; I Lusophone Meeting on Innovative Delivery Systems; 2022 Jun 30; Virtual Meeting",
title = "Nanosystem of royleanone diterpenoids from Plectranthus spp to improve targeted delivery into cancer cells",
doi = "10.19277/bbr.19.2.289",
pages = "28"
}
