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Self-assembly nanoparticles of 7α-acetoxy-6β-hydroxyroyleanone isolated from Plectranthus hadiensis
1, 2 , 3, 4 , 3, 5 , 6 , 3 , 3 , 3 , 3 , 4 , 6 , * 3, 5
1  CBIOS – Universidade Lusófona’s Research Center for Biosciences & Health Technologies, Campo Grande 376, 1749-024 Lisbon, Portugal.
2  University of Alcalá de Henares, Faculty of Pharmacy, Department of Biomedical Sciences, Pharmacology Area (Pharmacognosy Laboratory), New antitumor compounds: Toxic action on leukemia cells research group. Ctra. A2, Km 33.100 – Campus Universitario, 2880
3  CBIOS - Research Center for Biosciences & Health Technologies, Universidade Lusófona de Humanidades e Tecnologias, Campo Grande 376, 1749-024 Lisbon, Portugal
4  Department of Biomedical Sciences, Faculty of Pharmacy, University of Alcalá. Ctra. A2, Km 33.100 – Campus Universitario, 28805. Alcalá de Henares, Madrid, Spain.
5  Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, 1649-003 Lisbon, Portugal
6  Dipartimento di Chimica, Università degli Studi di Milano, Via Golgi 19, 20133 Milano, Italy

Abstract:

The Plectranthus genus belongs to the Lamiaceae family and consists of around 300 species distributed from Africa to Asia and Australia. Plectranthus spp. has been reported to be rich in diterpenoids, such as different types of royleanones. One of Plectranthus medicinal plant species is P. hadiensis (Forssk.) Schweinf. ex Sprenger, which contains diverse metabolites such as phenolic and diterpenoid compounds. Furthermore, this plant is widely used in an array of traditional and Ayurveda recipes for the treatment of diverse range of ailments like cancer.

Therefore, the aim of this work was to isolate large amounts of the cytotoxic royleanone
7α-acetoxy-6β-hydroxyroyleanone by fractionation of a P. hadiensis acetonic extract through an ultrasound-assisted extraction method. This royleanone was studied by cyclic voltammetry and employed as a starting material for the synthesis of self-assembled squalene nanoparticles. The obtained compound was characterized by spectroscopic methods, mainly NMR techniques. Additionally, the nanoparticles characterization, the ability to release the drug unit and the preliminary evaluation of their biological activity in different cell lines will be also tested in the future.

Acknowledgements: This project was funded by the Fundação para a Ciência e a Tecnologia (FCT, Portugal), through projects UIDP/04567/2020 and UIDB/04567/2020. E.M.D-M gratefully acknowledges had been the recipient of the grant UID/DTP/O4567/2019-CBIOS/BI1 and have, currently, a predoctoral FPU 2019 fellowship from the University of Alcalá de Henares.

Keywords: cancer, cyclic voltammetry, green-nanomedicine, Lamiaceae, lipid-drug conjugates, Plectranthus hadiensis, royleanone, self-assembly nanoparticles
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