Sustainable biomimetic solar distillation with edge crystallization for passive salt collection and zero brine discharge.

The urgency of addressing water scarcity and exponential population rise has necessitated the use of sustainable desalination for clean water production, while conventional thermal desalination processes consume fossil fuel with brine rejection. As a promising solution to sustainable solar thermal distillation, we report a scalable mangrove-mimicked device for direct solar vapor generation and passive salt collection without brine discharge. Capillarity-driven salty water supply and continuous vapor generation are ensured by anti-corrosion porous wicking stem and multi-layer leaves, which are made of low-cost superhydrophilic nanostructured titanium meshes. Precipitated salt at the leaf edge forms porous patch during daytime evaporation and get peeled by gravity during night when saline water rewets the leaves, and these salt patches can enhance vaporization by 1.6 times as indicated by our findings. The proposed solar vapor generator achieves a stable photothermal efficiency around 94% under one sun when treating synthetic seawater with a salinity of 3.5 wt.%. Under outdoor conditions, it can produce 2.2 L m-2 of freshwater per day from real seawater, which is sufficient for individual drinking needs. This kind of biomimetic solar distillation devices have demonstrated great capability in clean water production and passive salt collection to tackle global water and environmental challenges.

Multi-parametric arterial spin labelling and diffusion-weighted magnetic resonance imaging in differentiation of grade II and grade III gliomas.

PURPOSE: To assess arterial spin labelling (ASL) perfusion and diffusion MR imaging (DWI) in the differentiation of grade II from grade III gliomas. MATERIAL AND METHODS: A prospective cohort study was done on 36 patients (20 male and 16 female) with diffuse gliomas, who underwent ASL and DWI. Diffuse gliomas were classified into grade II and grade III. Calculation of tumoural blood flow (TBF) and apparent diffusion coefficient (ADC) of the tumoral and peritumoural regions was made. The ROC curve was drawn to differentiate grade II from grade III gliomas. RESULTS: There was a significant difference in TBF of tumoural and peritumoural regions of grade II and III gliomas (p = 0.02 and p =0.001, respectively). Selection of 26.1 and 14.8 ml/100 g/min as the cut-off for TBF of tumoural and peritumoural regions differentiated between both groups with area under curve (AUC) of 0.69 and 0.957, and accuracy of 77.8% and 88.9%, respectively. There was small but significant difference in the ADC of tumoural and peritumoural regions between grade II and III gliomas (p = 0.02 for both). The selection of 1.06 and 1.36 × 10-3 mm2/s as the cut-off of ADC of tumoural and peritumoural regions was made, to differentiate grade II from III with AUC of 0.701 and 0.748, and accuracy of 80.6% and 80.6%, respectively. Combined TBF and ADC of tumoural regions revealed an AUC of 0.808 and accuracy of 72.7%. Combined TBF and ADC for peritumoural regions revealed an AUC of 0.96 and accuracy of 94.4%. CONCLUSION: TBF and ADC of tumoural and peritumoural regions are accurate non-invasive methods of differentiation of grade II from grade III gliomas.

Design, synthesis and biological evaluation of some new 1,3,4-thiadiazine-thiourea derivatives as potential antitumor agents against non-small cell lung cancer cells.

New 1,3,4-thiadiazine-thiourea derivatives have been synthesized. All the synthesized compounds were examined for in vitro cytotoxic activity against Non-Small Cell Lung Cancer (NSCLC) cell line A549, using MTT bioassay. Compounds 5d, 5i, 5j showed the highest cytotoxic activity with IC50 values of 0.27 ±â€¯0.01, 0.30 ±â€¯0.02, and 0.32 ±â€¯0.012 µM respectively with sorafenib as reference (IC50 3.85 ±â€¯0.27 µM). These compounds were chosen for further investigations against various biological targets known to play roles in NSCLC specifically: vascular endothelial growth factor receptor 2 (VEGFR2), B-RAF and matrix metalloproteinase 9 (MMP9). Encouraging results were exhibited by the three compounds against the selected targets. Compound 5j was specially promising as it exhibited inhibitory activity of VEGFR2 close to sorafenib (IC50 0.11 ±â€¯0.01 µM), most potent B-RAF activity inhibition (IC50 0.178 ±â€¯0.004 µM) and MMP9 inhibition (IC50 0.08 ±â€¯0.004 µM). Moreover, cell cycle analysis of A549 cells treated with 5j exhibited cell cycle arrest at G2-M phase and pro-apoptotic activity as indicated by Annexin V-FITC staining. Also, it reflected antinvasive and antimigration properties to A549 cells. Additionally, docking study of 5j on VEGFR2, B-RAF and MMP9 revealed that it binds to the target enzymes in a similar way as the co-crystallized ligand. The three compounds exhibited significantly high selectivity to A549 cancer cells against the normal human fetal lung fibroblast cell line WI-38 with higher selectivity index compared to sorafenib (5d IC50 136.76 ±â€¯2.38 µM, SI = 506.52; 5i IC50 89.20 ±â€¯2.11 µM, SI = 297.33; 5j IC50 79.60 ±â€¯3.8 µM, SI = 248.75; sorafenib IC50 30.32 ±â€¯2.41 µM, SI = 7.88). In conclusion, compounds 5d, 5i and 5j, specially 5j are promising anticancer agents targeting important pathways in NSCLC and warrant further preclinical and clinical trials.

Design and synthesis of some ß-carboline derivatives as multi-target anticancer agents.

AIM: Some anticancer ß-carbolines exhibited dual inhibition of topo-I and KSP. METHODOLOGY/RESULTS: Novel ß-carbolines were synthesized and screened for their anticancer activity according to the NCI protocol. Five dose assays results indicated that compounds 9, 10, 12, 17 and 20 were potent and non selective anticancer agents; the sulfanyltriazole 12 was the most potent. Compounds 10, 12 and 20 showed dual topo-I and KSP inhibition with compound 12 being the most potent. Active compounds elicited Pre-G1 apoptosis and cell cycle arrest at G2/M phase of melanoma MDA-MB-435 cells. Docking results, in silico physicochemical and absorption, distribution, metabolism, excretion (ADME) properties were appropriate. CONCLUSION: Compounds 10, 12 and 20 are potent apoptosis-inducing multitarget anticancer agents that act via dual inhibition of topo-I and KSP-ATPase.

Design, synthesis, anticancer screening, docking studies and in silico ADME prediction of some ß-carboline derivatives.

BACKGROUND: Medicinal interest has focused on ß-carbolines as anticancer agents. METHODOLOGY/RESULTS: Several ß-carbolines were designed, synthesized and evaluated for their cytotoxic activity against MCF-7 and A-549 cancer cell lines using MTT assay. Compounds 13a, 13c, 13d and 20a were the most promising showing high selectivity indices. Compounds 13c and 20a showed potent inhibition of topoisomerase (topo-I) and kinesin spindle protein (KSP/Eg5 ATPase) which was confirmed by their docking results into the active site of both enzymes. In silico physicochemical calculations predicted that compounds 13a, 13d and 20a obeyed Lipinski's rule of five. CONCLUSION: Compounds 13c and 20a are multitarget anticancer leads that act as potent inhibitors for both topo-I and/or KSP ATPase.