This page has only limited features, please log in for full access.
The preparation and characterization of ionic liquids and organic salts (OSILs) that contain anionic penicillin G [secoPen] and amoxicillin [seco-Amx] hydrolysate derivatives and their in vitro antibacterial activity against sensitive and resistant Escherichia coli and Staphylococcus aureus strains is reported. Eleven hydrolyzed β-lactam-OSILs were obtained after precipitation in moderate-to-high yields via the neutralization of the basic ammonia buffer of antibiotics with different cation hydroxide salts. The obtained minimum inhibitory concentration (MIC) data of the prepared compounds showed a relative decrease of the inhibitory concentrations (RDIC) in the order of 100 in the case of [C2OHMIM][seco-Pen] against sensitive S. aureus ATCC25923 and, most strikingly, higher than 1000 with [C16Pyr][seco-Amx] against methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300. These outstanding in vitro results showcase that a straightforward transformation of standard antibiotics into hydrolyzed organic salts can dramatically change the pharmaceutical activity of a drug, including giving rise to potent formulations of antibiotics against deadly bacteria strains.
Ricardo Ferraz; Dário Silva; Ana Rita Dias; Vitorino Dias; Miguel M. Santos; Luís Pinheiro; Cristina Prudêncio; João Paulo Noronha; Željko Petrovski; Luís C. Branco. Synthesis and Antibacterial Activity of Ionic Liquids and Organic Salts Based on Penicillin G and Amoxicillin hydrolysate Derivatives against Resistant Bacteria. Pharmaceutics 2020, 12, 221 .
AMA StyleRicardo Ferraz, Dário Silva, Ana Rita Dias, Vitorino Dias, Miguel M. Santos, Luís Pinheiro, Cristina Prudêncio, João Paulo Noronha, Željko Petrovski, Luís C. Branco. Synthesis and Antibacterial Activity of Ionic Liquids and Organic Salts Based on Penicillin G and Amoxicillin hydrolysate Derivatives against Resistant Bacteria. Pharmaceutics. 2020; 12 (3):221.
Chicago/Turabian StyleRicardo Ferraz; Dário Silva; Ana Rita Dias; Vitorino Dias; Miguel M. Santos; Luís Pinheiro; Cristina Prudêncio; João Paulo Noronha; Željko Petrovski; Luís C. Branco. 2020. "Synthesis and Antibacterial Activity of Ionic Liquids and Organic Salts Based on Penicillin G and Amoxicillin hydrolysate Derivatives against Resistant Bacteria." Pharmaceutics 12, no. 3: 221.
Brain tumor, as any type of cancer, is assumed to be sustained by a small subpopulation of stem-like cells with distinctive properties that allow them to survive conventional therapies and drive tumor recurrence. Thus, the identification of new molecules capable of controlling stemness properties may be key in developing effective therapeutic strategies for cancer by inducing stem-like cells differentiation. Spiropyrazoline oxindoles have previously been shown to induce apoptosis and cell cycle arrest, as well as upregulate p53 steady-state levels, while decreasing its main inhibitor MDM2 in the HCT116 human colorectal carcinoma cell line. In this study, we made modifications in this scaffold by including combinations of different substituents in the pyrazoline ring in order to obtain novel small molecules that could modulate p53 activity and act as differentiation inducer agents. The antiproliferative activity of the synthesized compounds was assessed using the isogenic pair of HCT116 cell lines differing in the presence or absence of the p53 gene. Among the tested spirooxindoles, spiropyrazoline oxindole 1a was selective against the cancer cell line expressing wild-type p53 and presented low cytotoxicity. This small molecule induced neural stem cell (NSC) differentiation through reduced SOX2 (marker of multipotency) and increased βIII-tubulin (marker of neural differentiation) which suggests a great potential as a non-toxic inducer of cell differentiation. More importantly, in glioma cancer cells (GL-261), compound 1a reduced stemness, by decreasing SOX2 protein levels, while also promoting chemotherapy sensitization. These results highlight the potential of p53 modulators for brain cell differentiation, with spirooxindole 1a representing a promising lead molecule for the development of new brain antitumor drugs.
Joana D. Amaral; Dário Silva; Cecilia Rodrigues; Susana Solá; Maria M. M. Santos. A Novel Small Molecule p53 Stabilizer for Brain Cell Differentiation. Frontiers in Chemistry 2019, 7, 15 .
AMA StyleJoana D. Amaral, Dário Silva, Cecilia Rodrigues, Susana Solá, Maria M. M. Santos. A Novel Small Molecule p53 Stabilizer for Brain Cell Differentiation. Frontiers in Chemistry. 2019; 7 ():15.
Chicago/Turabian StyleJoana D. Amaral; Dário Silva; Cecilia Rodrigues; Susana Solá; Maria M. M. Santos. 2019. "A Novel Small Molecule p53 Stabilizer for Brain Cell Differentiation." Frontiers in Chemistry 7, no. : 15.