Design, Synthesis, and Biological Evaluation of Novel Quinazoline Derivatives Possessing a Trifluoromethyl Moiety as Potential Antitumor Agents.

A novel series of trifluoromethyl-containing quinazoline derivatives with a variety of functional groups was designed, synthesized, and tested for their antitumor activity by following a pharmacophore hybridization strategy. Most of the 20 compounds displayed moderate to excellent antiproliferative activity against five different cell lines (PC3, LNCaP, K562, HeLa, and A549). After three rounds of screening and structural optimization, compound 10 b was identified as the most potent one, with IC50 values of 3.02, 3.45, and 3.98 µM against PC3, LNCaP, and K562 cells, respectively, which were comparable to the effect of the positive control gefitinib. To further explore the mechanism of action of 10 b against cancer, experiments focusing on apoptosis induction, cell cycle arrest, and cell migration assay were conducted. The results showed that 10 b was able to induce apoptosis and prevent tumor cell migration, but had no effect on the cell cycle of tumor cells.

Optimization of Supercritical CO2 Extraction of Moringa oleifera Seed Oil Using Response Surface Methodological Approach and Its Antioxidant Activity.

Moringa (Moringa oleifera) seed oil is an edible vegetable oil rich in unsaturated fatty acids. In this study, the supercritical CO2 fluid extraction method was employed to obtain the maximum yield of moringa seed oil. The effects of temperature, time, and pressure, three characteristics of extractions, on the extraction rate of Moringa seed oil were investigated by single factor test and response surface methodological approach. The optimal process conditions of supercritical CO2 fluid extraction of moringa seed oil were determined as extraction temperature of 45°C, extraction time of 2.5 h, extraction pressure of 50 MPa, and CO2 flow rate of 240 L/h, resulting in a maximum yield of 38.54%. Composition analysis shows that the extracted moringa seed oil is rich in unsaturated fatty acids, including oleic acid, octadecanoic acid, palmitic acid, stearic acid, eicosanoic acid, etc. Furthermore, we found that Moringa seed oil exerted potent antioxidant activities on DPPH and hydroxyl radicals, and its efficacy was comparable to commercial peanut oil and tea oil. Overall, this novel extraction method of moringa seed oil may increase its potential value and application in the food and nutraceutical industries.