RESUMO
Natural products are closely associated with human health. Luteolin (LUT), a flavonoid polyphenolic compound, is widely found in fruits, vegetables, flowers, and herbs. It is noteworthy that LUT exhibits a variety of beneficial pharmacological properties and holds significant potential for clinical applications, particularly in antitumor, anti-convulsion, diabetes control, anti-inflammatory, neuroprotection, anti-oxidation, anti-cardiovascular, and other aspects. The potential mechanism of action has been partially elucidated, including the mediation of NF-κB, toll-like receptor, MAPK, Wnt/ß-catenin, PI3K/Akt, AMPK/mTOR, and Nrf-2, among others. The review that aimed to comprehensively consolidate essential information on natural sources, pharmacological effects, therapeutic and preventive potential, as well as potential mechanisms of LUT. The objective is to establish a theoretical basis for the continued development and application of LUT.
Assuntos
Luteolina , Humanos , Luteolina/farmacologia , Flavonoides/farmacologia , Flavonoides/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Animais , Antioxidantes/farmacologiaRESUMO
Free-falling cubic Test Masses (TMs) are a key component of the interferometer used for low-frequency gravitational wave (GW) detection in space. However, exposure to energetic particles in the environment can lead to electrostatic charging of the TM, resulting in additional electrostatic and Lorentz forces that can impact GW detection sensitivity. To evaluate this effect, the high-energy proton data set of the Geostationary Operational Environmental Satellite (GOES) program was used to analyze TM charging due to Solar Proton Events (SPEs) in the 24th solar cycle. Using the Geant4 Monte Carlo toolkit, the TM charging process is simulated in a space environment for SPEs falling into three ranges of proton flux: (1) greater than 10 pfu and less than 100 pfu, (2) greater than 100 pfu and less than 1000 pfu, and (3) greater than 1000 pfu. It is found that SPEs charging can reach the threshold within 535 s to 18.6 h, considering a reasonable discharge threshold of LISA and Taiji. We demonstrate that while there is a somewhat linear correlation between the net charging rate of the TM and the integrated flux of [Formula: see text] 10 MeV SPEs, there are many cases in which the integrated flux is significantly different from the charging rate. Therefore, we investigate the difference between the integral flux and the charging rate of SPEs using the charging efficiency assessment method. Our results indicate that the energy spectrum structure of SPEs is the most important factor influencing the charging rate. Lastly, we evaluate the charging probability of SPEs in the 24th solar cycle and find that the frequency and charging risk of SPEs are highest in the 3rd, 4th, 5th, 6th, and 7th years, which can serve as a reference for future GW detection spacecraft.
RESUMO
Pterostilbene (PTE) is known as resveratrol of the next generation and it has attracted extensive attention in recent years. PTE can inhibit the growth of a variety of tumor cells. To overcome the problem of insolubility, PTE was loaded into nanoparticles (NPs) by anti-solvent precipitation technique using soybean lecithin (SPC) and D-α-tocopheryl polyethylene glycol succinate (TPGS) as stabilizers. The obtained PTE-NPs had an average particle size of 71.0 nm, a polydispersity index ï¼PDIï¼ value of 0.258, and a high zeta potential of -40.8 mV. PTE-NPs can maintain particle size stability in various physiological media. The entrapment efficiency of PTE-NPs was 98.24%. And the apparently water solubility of PTE-NPs was about 53 times higher than the solubility of PTE (54.41µg ml-1v-1s-1. 2.89 mg ml-1). M-1T-1T-1assay showed that the antitumor activity of PTE-NPs on 4T1 breast cancer cells, MCF-7 breast cancer cells and Hela cervical cancer cells was significantly increased by 4, 6 and 8 times than that of free PTE, respectively.In vivostudies have shown that PTE-NPs has a certain dose dependence. When injected intraperitoneally, PTE-NPs showed a similar therapeutic effect as paclitaxel injection (TIR was 57.53% versus 57.23%) against 4T1 tumor-bearing mice. This should be due to the improved bioavailability of the drug caused by nano-drug delivery system (nano-DDS). These results indicate that PTE-NPs may be a clinically promising anti-tumor drug for breast cancer treatment.
Assuntos
Antineoplásicos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Nanopartículas/química , Paclitaxel/farmacologia , Estilbenos/farmacologia , Animais , Antineoplásicos/farmacocinética , Disponibilidade Biológica , Neoplasias da Mama/patologia , Composição de Medicamentos/métodos , Feminino , Células HeLa , Humanos , Lecitinas/química , Células MCF-7 , Camundongos , Camundongos Endogâmicos BALB C , Nanopartículas/administração & dosagem , Paclitaxel/farmacocinética , Tamanho da Partícula , Solubilidade , Estilbenos/farmacocinética , Resultado do Tratamento , Carga Tumoral/efeitos dos fármacos , Vitamina E/química , Ensaios Antitumorais Modelo de XenoenxertoRESUMO
Two new daphnane diterpenes named tianchaterpenes A and B were isolated from the roots of Stelleropsis tianschanica. Their structures were elucidated on the basis of chemical and spectral analysis, including 1D, 2D NMR analyses and HRESIMS. Compounds 1 and 2 were evaluated for their cytotoxic activities against HeLa and HCT-8 cell lines. The results showed that all compounds displayed weak cytotoxicities to the HeLa cells and were inactive to the HCT-8 cells.