RESUMO
Herein, we explore the biological properties of curcumin, quercetin, and rutin by loading them onto porous CuO nanorods (NRs). The CuO NRs were synthesized using the microwave irradiation method through a chemical reaction between CuSO4·5H2O and NaOH in the presence of the anionic stabilizer sodium dodecyl sulfate. The shape and surface morphology of CuO NRs were examined with two microscopic techniques: high-resolution transmission electron microscopy (HR-TEM) and field emission scanning electron microscopy (FESEM). Their average diameter was measured by TEM to be 15 ± 2 nm. The porosity and interfacial area of the fabricated material were determined by Brunauer-Emmett-Teller analysis. After successful synthesis, CuO NRs were loaded with polyphenolic curcumin, quercetin, and rutin, with the loading efficiency of 57.8, 62.2, and 81.2%, respectively, which was confirmed by UV-visible and infra-red spectroscopy and finally with a thermal gravimetric technique. Their radical scavenging activity was measured with the 2,2-diphenyl-1-picrylhydrazyl radical and compared with the control (ascorbic acid). Further, good bactericidal effects were observed against both Gram-positive bacterial strains, including Staphylococcus aureus and Bacillus subtilis, and Gram-negative bacterial strains, including Salmonella typhi, Pseudomonas aeruginosa, Escherichia coli, and Klebsiella pneumoniae. Excellent anticancer activity was observed against normal skin cells and breast cancer cells T-47D and MCF-7.
Assuntos
Anti-Infecciosos , Neoplasias da Mama , Curcumina , Nanotubos , Humanos , Feminino , Antioxidantes/farmacologia , Quercetina/farmacologia , Curcumina/farmacologia , Testes de Sensibilidade Microbiana , Rutina/farmacologia , Micro-Ondas , Células MCF-7 , Neoplasias da Mama/tratamento farmacológico , Anti-Infecciosos/farmacologia , Nanotubos/química , Escherichia coliRESUMO
Colorectal cancer (CRC) is a major cause of morbidity and mortality worldwide. Despite the critical involvement of epigenetic modifications in CRC, the studies on the chemotherapeutic efficacy of various epigenetic regulators remain limited. Considering the key roles of histone deacetylases (HDACs) in the regulation of diverse cellular processes, several HDAC inhibitors are implied as effective therapeutic strategies. In this context, suberoylanilide hydroxamic acid (SAHA), a 2nd-generation HDAC inhibitor, showed limited efficacy in solid tumors. Also, side effects associated with SAHA limit its clinical application. Based on the redox-modulatory and HDAC inhbitiory activities of essential trace element selenium (Se), the anti-carcinogenic potential of Se substituted SAHA, namely, SelSA-1 (25 mg kg-1), was screened for it enhanced anti-tumorigenic role and wider safety profiles in DMH-induced CRC in Balb/c mice. A multipronged approach such as in silico, biochemical, and pharmacokinetics (PK) has been used to screen, characterize, and evaluate these novel compounds in comparison to existing HDAC inhibitor SAHA. This is the first in vivo study indicating the chemotherapeutic potential of Se-based novel epigenetic regulators such as SelSA-1 in any in vivo experimental model of carcinogenesis. Pharmcological and toxicity data indicated better safety margins, bioavailability, tolerance, and elimination rate of SelSA-1 compared to classical HDAC inhibitor SAHA. Further, histological and morphological evidence demonstrated enhanced chemotherapeutic potential of SelSA-1 even at lower pharmacological doses than SAHA. This is the first in vivo study suggesting Se-based novel epigenetic regulators as potential chemotherapeutic alternatives with wider safety margins and enhanced anticancer activities.