A possibility of harvesting the physiologically-active compounds from the vegetable oils using bespoke resin and optimised solid-phase extraction (SPE) purification method is demonstrated. The paper describes the application of SPE protocol, which was originally developed, using sunflower oil as model biomass, for extraction of the valuable compounds from sesame, wheat germ, palm, olive and soybean oils. As a result, the extraction of three free fatty acids (palmitic, oleic and linoleic), α-tocopherol and three phytosterols (campesterol, stigmasterol and β-sitosterol) from six vegetable oils have been demonstrated. The comparison between the published data on the amount of the analysed compounds in the corresponding vegetable oils and presented here extraction results confirm that the developed method allowed not only quantitatively extract the physiologically-active components from various vegetable oils without any pre-treatment but also was reproducible, cost-effective and ecologically-conscious as consumed smaller volumes of organic solvents than commonly used protocols.
A new series of tetrasubstituted imidazole derivatives carrying pyrimidine sulfonamide pharmacophores has been synthesized and evaluated for their anticancer activities. In‐vitro screening of these hybrids against a full 60‐cell‐line panel at a single dose of 10 μM showed significant growth inhibition of up to 95 %. The most active compound showed in‐vitro anticancer activities against (i) abnormal HER2 and (ii) two mutants for EGFR. Apoptotic gene expression revealed that lead compounds induced MCF‐7 cell line apoptosis together with considerable change in the Bax/Bcl‐2 expression ratio. One lead compound led to a significant cell‐cycle S‐phase arrest, while another blocked the cell cycle at G1/S‐phase causing the accumulation of cells. Docking analysis of these two hybrids adopted the orientation and binding interactions with a higher liability to enter the active side pocket of HER2, L858R, and T790 M, preferable to that of co‐crystallized ligands. Modelling simulation was consistent with the acquired biological evaluation.
Bacterial secondary metabolites are a valuable source of various molecules that have antibacterial and anticancer activity. In this study, ten endosymbiotic bacteria of aphids, aphid predators and ants were isolated. Bacterial strains were identified according to the 16S rRNA gene. Ethyl acetate fractions of methanol extract (EA-ME) were prepared from each isolated bacterium and tested for their antibacterial activities using the disk diffusion method. The EA-ME of three bacterial species, Planococcus sp., Klebsiella aerogenes, Enterococcus avium, from the pomegranate aphids Aphis punicae, Chrysoperia carnea, and Tapinoma magnum, respectively, exhibited elevated antibacterial activity against one or several of the five pathogenic bacteria tested. The inhibition zones ranged from 10.00 ± 0.13 to 20.00 ± 1.11 mm, with minimum inhibitory concentration (MIC) values ranging from 0.156 mg/mL to 1.25 mg/mL. The most notable antibacterial activity was found in the EA-ME of K. aerogenes against Klebsiella pneumonia and Escherichia coli, with an MIC value of 0.156 mg/mL. The cytotoxic activity of EA-ME was dependent on the cell line tested. The most significant cytotoxicity effect was observed for extracts of K. aerogenes and E. avium, at 12.5 µg/mL, against the epithelial cells of lung carcinoma (A549), with a cell reduction of 79.4% and 67.2%, respectively. For the EA-ME of K. aerogenes and Pantoea agglomerans at 12.5 µg/mL, 69.4% and 67.8% cell reduction were observed against human colon cancer (Hct116), respectively. Gas chromatography–mass spectrometry (GC-MS) analysis of three EA-ME revealed the presence of several bioactive secondary metabolites that have been reported previously to possess antibacterial and anticancer properties. To the best of our knowledge, this is the first study to examine the biological activities of endosymbiotic bacteria in aphids, aphid predators and ants. The promising data presented in this study may pave the way for alternative drugs to overcome the continued emergence of multidrug-resistant bacteria, and find alternative drugs to conventional cancer therapies.
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