RESUMEN
Chalcones are direct precursors in the biosynthesis of flavonoids. They have an α,ß-unsaturated carbonyl system which gives them broad biological properties. Among the biological properties exerted by chalcones, their ability to suppress tumors stands out, in addition to their low toxicity. In this perspective, the present work explores the role of natural and synthetic chalcones and their anticancer activity in vitro reported in the last four years from 2019 to 2023. Moreover, we carried out a partial least square (PLS) analysis of the biologic data reported for colon adenocarcinoma lineage HCT-116. Information was obtained from the Web of Science database. Our in silico analysis identified that the presence of polar radicals such as hydroxyl and methoxyl contributed to the anticancer activity of chalcones derivatives. We hope that the data presented in this work will help researchers to develop effective drugs to inhibit colon adenocarcinoma in future works.
Asunto(s)
Adenocarcinoma , Antineoplásicos , Chalconas , Neoplasias del Colon , Humanos , Chalconas/farmacología , Neoplasias del Colon/tratamiento farmacológico , Flavonoides/farmacología , Antineoplásicos/farmacologíaRESUMEN
This study aimed to evaluate the in silico, in vitro, and ex-vivo toxicity of vitexin, the flavonoid 5,7,4'- trihydroxyflavone-8-C-ß-glucopyranoside from Waltheria viscosissima. The chemical structure and predicted bioactive properties were also in silico analyzed. The in vitro and ex-vivo assays were performed according to the Ethics Code of the World Medical Association and were approved by the Ethics Committee of University Center of Patos (protocol number: 3.621.284). In silico analysis suggested that the molecule presents good oral bioavailability and good absorption; penetrating biological membranes. The toxicity tests revealed the potential effectiveness of the molecule in cellular protection against free radicals, in addition to possible antimutagenic, anticarcinogenic, antioxidant, antineoplastic, anti-inflammatory, anti-hemorrhagic and apoptosis agonist activity. Hemolytic and genotoxic assessment detected low hemolysis rates in human red blood cells and no cellular toxicity against oral mucosa cells. The data suggest that vitexin is a safe molecule for possible therapeutic application and its toxicity profile indicates viability for future studies.
RESUMEN
Abstract The species Waltheria viscosissima A.St.-Hil, Malvaceae, which is known as 'malva-branca', is traditionally used in the Brazilian northeast for the treatment of coughs. This research looks towards reporting the isolation of phytoconstituents of W. viscosissima, as well as the quantification of its phenolics, total flavonoid content, and free radical scavenging potential, along with an evaluation of its larvicidal activity against Aedes aegypti larvae. Chromatographic techniques were used to isolate the compounds and a structural elucidation was performed by 1D and 2D NMR. The quantification of total phenolics and flavonoids and the DPPH˙ radical scavenging activity was determined through spectrophotometric methods. Consequently, the phytochemical investigation led to the identification of fourteen compounds from the aerial parts of the W. viscosissima: steroids, triterpenes, alkaloids, and eight flavonoids previously reported in the literature. The quantification of compounds showed that the aerial parts extract possessed high concentration of flavonoids, while the roots extract were rich in other phenolic compounds. At the DPPH˙ free radical scavenging assay, the roots extract presented EC50 = 77.32 ± 4.37 µg/ml and the aerial parts extracts showed EC50 = 118.10 ± 1.21 µg/ml. W. viscosissima roots extract showed the most potent larvicidal activity against Ae. aegypti (LC50 = 4.78 mg/ml), with the potential of being used in effective and economically viable preparations that can be catered for domestic use towards controlling the vector insect of severe diseases, such as dengue and Zika.
RESUMEN
ABSTRACT Pilosocereus pachycladus F. Ritter, Cactaceae, popularly known as "facheiro", is used as food and traditional medicine in Brazilian caatinga ecoregion. The plant is used to treat prostate inflammation and urinary infection. The present work reports the first secondary metabolites isolated from P. pachycladus. Therefore, the isolated compound 4-hydroxy-3,5-dimethoxy benzaldehyde (syringaldehyde) was evaluated as modulator of Staphylococcus aureus pump efflux-mediated antibiotic resistance. The isolation of compounds was performed using chromatographic techniques and the structural elucidation was carried out by spectroscopic methods. In order to evaluate syringaldehyde ability to modulate S. aureus antibiotic resistance, its minimum inhibitory concentrations (µg/ml) was first determinate, then, the tested antibiotics minimum inhibitory concentrations were determined in the presence of the syringaldehyde in a sub-inhibitory concentration. The chromatographic procedures led to isolation of twelve compounds from P. pachycladus including fatty acids, steroids, chlorophyll derivatives, phenolics and a lignan. The syringaldehyde did not show any antibacterial activity at 256 µg/ml against S. aureus. On the other hand the compound was able to reduce the antibiotic concentration (tetracycline, norfloxacin, ethidium bromide) required to inhibit the growth of drug-resistant bacteria, showing the ability of syringaldehyde of inhibiting the efflux pump on these bacteria.