Abstract
Different approaches have been reported to enhance penetration of small drugs through physiological barriers, among them is the self-assembly drug conjugates preparation that shown to be a promising approach to improve activity and penetration, as well as to reduce any side effects. In recent years, the use of drug-conjugates, usually obtained by covalent coupling of the drug with biocompatible lipid moieties to form nanoparticles, has gained considerable attention. Natural products isolated from plants have been a successful source of potential drug leads with unique structural diversity. In the present work, three molecules derived from natural products were employed as lead molecules for the synthesis of self-assembled nanoparticles. The royleanones were conjugated with squalene, oleic acid, and/or 1-bromododecane self-assembly inducers, and conjugates were successfully synthesized and characterized. Bioactivity was assessed suggesting these nano assemblies can act as prodrugs for the release of cytotoxic lead molecules.
Highlights
Natural products remain a good source of bioactive compounds for the treatment of diseases including cancer [2]
In this work 7α-acetoxy-6β-hydroxyroyleanone (Roy), 7α-acetoxy-6β-hydroxy-12-benzoyloxyroyleanone (12BzRoy), and 6,7dehydroroyleanone (DHR) from Plectranthus species with cytotoxicity were used as lead compounds for the synthesis of self-assembled conjugates
Roy-oleic acid (OA) NPs had a low release of Roy at physiological pH 7.4 after 24 h
Summary
Natural products remain a good source of bioactive compounds for the treatment of diseases including cancer [2]. In this work 7α-acetoxy-6β-hydroxyroyleanone (Roy), 7α-acetoxy-6β-hydroxy-12-benzoyloxyroyleanone (12BzRoy), and 6,7dehydroroyleanone (DHR) from Plectranthus species with cytotoxicity were used as lead compounds for the synthesis of self-assembled conjugates. These royleanones were conjugated to squalene (sq), oleic acid (OA), and/or 1-bromododecane (BD) self-assembly inducers. Roy-OA, DHR-sq, and 12BzRoy-sq conjugates were successfully synthesized and characterized. Roy-OA NP and DHR-sq NP assemblies show promising size, Pdl, zeta potential, and spherical morphology from SEM.
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