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Cytotoxic Evaluation of (2S)-5,7-Dihydroxy-6-prenylflavanone Derivatives Loaded PLGA Nanoparticles against MiaPaCa-2 Cells.

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2017-09-15

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Andrade-Carrera, Berenice
Clares, Beatriz
Noé, Véronique
Mallandrich, Mireia
Calpena, Ana C
García, María Luisa
Garduño-Ramírez, María Luisa

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The search for new alternatives for the prevention and treatment of cancer is extremely important to minimize human mortality. Natural products are an alternative to chemical drugs, since they are a source of many potential compounds with anticancer properties. In the present study, the (2S)-5,7-dihydroxy-6-prenylflavanone (semi-systematic name), also called (2S)-5,7-dihydroxy-6-(3-methyl-2-buten-1-yl)-2-phenyl-2,3-dihydro-4H-1-Benzopyran-4-one (CAS Name registered) (1) was isolated from Eysenhardtia platycarpa leaves. This flavanone 1 was considered as the lead compound to generate new cytotoxic derivatives 1a, 1b, 1c and 1d. These compounds 1, 1a, 1b, 1c, and 1d were then loaded in nanosized drug delivery systems such as polymeric nanoparticles (NPs). Small homogeneous spherical shaped NPs were obtained. Cytotoxic activity of free compounds 1, 1a, 1b, 1c, and 1d and encapsulated in polymeric NPs (NPs1, NPs1a, NPs1b, NPs1c and NPs1d) were evaluated against the pancreatic cancer cell line MiaPaCa-2. The obtained results demonstrated that NPs1a and NPs1b exhibited optimal cytotoxicity, and an even higher improvement of the cytotoxic efficacy was exhibited with the encapsulation of 1a. Based on these results, NPs1a were proposed as promising anticancer agent candidates.

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Antineoplastic Agents
Cell Line, Tumor
Cell Survival
Drug Carriers
Drug Liberation
Drug Screening Assays, Antitumor
Fabaceae
Flavanones
Humans
Kinetics
Nanoparticles
Pancreatic Neoplasms
Particle Size
Plant Extracts
Plant Leaves
Polylactic Acid-Polyglycolic Acid Copolymer
Surface Properties
Thermodynamics

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Keywords

Eysenhardtia, MiaPaCa-2, cytotoxic activity, flavanone

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