Browsing by Subject "Antitumor activity"

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    Antitumor activity of rosmarinic acid-loaded silk fibroin nanoparticles on HeLa and MCF-7 cells
    (MDPI, 2021-09-18) Fuster, Marta G.; Carissimi, Gúzmán; García Montalbán, Mercedes; Víllora Cano, Gloria; Ingeniería Química
    Rosmarinic acid (RA), one of the most important polyphenol-based antioxidants, has drawn increasing attention because of its remarkable bioactive properties, including anti-inflammatory, anticancer and antibacterial activities. The aim of this study was to synthesize and characterize RA-loaded silk fibroin nanoparticles (RA-SFNs) in terms of their physical–chemical features and composition, and to investigate their antitumor activity against human cervical carcinoma and breast cancer cell lines (HeLa and MCF-7). Compared with the free form, RA bioavailability was enhanced when the drug was adsorbed onto the surface of the silk fibroin nanoparticles (SFNs). The resulting particle diameter was 255 nm, with a polydispersity index of 0.187, and the Z-potential was −17 mV. The drug loading content of the RA-SFNs was 9.4 wt.%. Evaluation of the in vitro drug release of RA from RA-SFNs pointed to a rapid release in physiological conditions (50% of the total drug content was released in 0.5 h). Unloaded SFNs exhibited good biocompatibility, with no significant cytotoxicity observed during the first 48 h against HeLa and MCF-7 cancer cells. In contrast, cell death increased in a concentration-dependent manner after treatment with RA-SFNs, reaching an IC50 value of 1.568 and 1.377 mg/mL on HeLa and MCF-7, respectively. For both cell lines, the IC50 of free RA was higher. The cellular uptake of the nanoparticles studied was increased when RA was loaded on them. The cell cycle and apoptosis studies revealed that RA-SFNs inhibit cell proliferation and induce apoptosis on HeLa and MCF-7 cell lines. It is concluded, therefore, that the RA delivery platform based on SFNs improves the antitumor potential of RA in the case of the above cancers.
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    Antitumor Activity of Rosmarinic Acid-Loaded Silk Fibroin Nanoparticles on HeLa and MCF-7 Cells
    (MDPI, 2021-09-18) Fuster, M. G.; Carissimi, G.; Montalbán, M. G.; Víllora Cano, Gloria; Ingeniería Química; Facultad de Química
    Rosmarinic acid (RA), one of the most important polyphenol-based antioxidants, has drawn increasing attention because of its remarkable bioactive properties, including anti-inflammatory, anticancer and antibacterial activities. The aim of this study was to synthesize and characterize RA-loaded silk fibroin nanoparticles (RA-SFNs) in terms of their physical–chemical features and composition, and to investigate their antitumor activity against human cervical carcinoma and breast cancer cell lines (HeLa and MCF-7). Compared with the free form, RA bioavailability was enhanced when the drug was adsorbed onto the surface of the silk fibroin nanoparticles (SFNs). The resulting particle diameter was 255 nm, with a polydispersity index of 0.187, and the Z-potential was 􀀀17 mV. The drug loading content of the RA-SFNs was 9.4 wt.%. Evaluation of the in vitro drug release of RA from RA-SFNs pointed to a rapid release in physiological conditions (50% of the total drug content was released in 0.5 h). Unloaded SFNs exhibited good biocompatibility, with no significant cytotoxicity observed during the first 48 h against HeLa and MCF-7 cancer cells. In contrast, cell death increased in a concentration-dependent manner after treatment with RA-SFNs, reaching an IC50 value of 1.568 and 1.377 mg/mL on HeLa and MCF-7, respectively. For both cell lines, the IC50 of free RA was higher. The cellular uptake of the nanoparticles studied was increased when RA was loaded on them. The cell cycle and apoptosis studies revealed that RA-SFNs inhibit cell proliferation and induce apoptosis on HeLa and MCF-7 cell lines. It is concluded, therefore, that the RA delivery platform based on SFNs improves the antitumor potential of RA in the case of the above cancers.
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    Potent anticancer activity of a novel iridium metallodrug via oncosis
    (Springer, 2022-09-06) Ortega Forte, Enrique; Hernández García, Samanta; Vigueras, Gloria; Henarejos Escudero, Paula; Cutillas, Natalia; Ruiz, José; Gandía Herrero, Fernando; Bioquímica y Biología Molecular A
    Oncosis (from Greek ónkos, meaning “swelling”) is a non-apoptotic cell death process related to energy depletion. In contrast to apoptosis, which is the main form of cell death induced by anticancer drugs, oncosis has been relatively less explored but holds potential to overcome drug resistance phenomena. In this study, we report a novel rationally designed mitochondriatargeted iridium(III) complex (OncoIr3) with advantageous properties as a bioimaging agent. OncoIr3 exhibited potent anticancer activity in vitro against cancer cells and displayed low toxicity to normal dividing cells. Flow cytometry and fluorescence-based assays confirmed an apoptosis-independent mechanism involving energy depletion, mitochondrial dysfunction and cellular swelling that matched with the oncotic process. Furthermore, a Caenorhabditis elegans tumoral model was developed to test this compound in vivo, which allowed us to prove a strong oncosis-derived antitumor activity in animals (with a 41% reduction of tumor area). Indeed, OncoIr3 was non-toxic to the nematodes and extended their mean lifespan by 18%. Altogether, these findings might shed new light on the development of anticancer metallodrugs with nonconventional modes of action such as oncosis, which could be of particular interest for the treatment of apoptosis-resistant cancers.