Controlled nano-particle dyeing of cotton can ensure low cytotoxicity risk with multi-functional property enhancement

The Nanoparticle (NP) and their oxides are being progressively used and expected to be more frequently used in textiles. Nanoparticle (NP) has higher toxicological risk than larger particles because of their physicochemical properties, chemical reactivity and biological activity. In fact, the stability of nano-oxide particles in the medium is always challenging as they lack functional groups to leverage upon textile materials directly. Thus, in many finishing processes, cross-linkers and/or adhesives are applied together with NP at the cost of inferior comfort, feel and fastness which tends to be toxic and prone to release NPs under common laundering, physical stress and sweat. This study shows that the diffusion of NPs into the fibre polymer matrix via dyeing technique could be much durable, safer in terms of cytotoxicity levels and easy to process for tailoring desired functional attributes. We studied the possibility of a simple application technique via dyeing of vinyl sulphone based reactive dye with four kinds of NPs followed by their cytotoxicity test using cell line A431.1% silica dyed sample have shown highest (198.5%) increase in tensile strength followed by 2% silica and 2% CNT whereas a decrease in elongation is highest in the case of CNT 2% (5.31%) and significantly enhancing the moisture management properties in case of CNT and silica. The study showed promising results in dyeing with TiO2, CNT (Carbon nanotubes), Silica and Alumina NPs in enhancing the mechanical, moisture management, and surface frictional properties to ensure comfortable and safe wear.     

Pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine Sulfonamides as Novel Potential Anticancer Agents: Cytotoxic and Genotoxic Activities In Vitro

In this paper, we present for the first time the evaluation of cytotoxicity and genotoxicity of de novo synthesized pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine sulfonamides MM129, MM130, and MM131 in human tumor cell lines: HeLa, HCT 116, PC-3, and BxPC-3. Cytotoxic and genotoxic properties of the tested compounds were estimated using the MTT assay, comet assay (alkaline and neutral version), and γ-H2AX immuno-staining. Examined sulfonamides exhibited strong anticancer properties towards tested cells in a very low concentration range (IC₅₀ = 0.17–1.15 μM) after 72 h exposure time. The results of the alkaline and neutral version of the comet assay following 24 h incubation of the cells with tested compounds demonstrated the capability of heterocycles to induce significant DNA damage in exposed cells. HCT 116 cells were the most sensitive to the genotoxic activity of novel tricyclic pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine sulfonamides in the neutral version of the comet assay. Immunocytochemical detection of γ-H2AX showed an increase in DNA DSBs level in the HCT 116 cell line, after 24 h incubation with all tested compounds, confirming the results obtained in the neutral comet assay. Among all investigated compounds, MM131 showed the strongest cytotoxic and genotoxic activity toward all tested cell types. In conclusion, our results suggest that MM129, MM130, and MM131 exhibit high cytotoxic and genotoxic potential in vitro, especially towards the colorectal cancer cell line HCT 116. However, further investigations and analyses are required for their future implementation in the field of medicine.     

Design and Synthesis of Hsp90 Inhibitors with B-Raf and PDHK1 Multi-Target Activity

The design of multi-target ligands has become an innovative approach for the identification of effective therapeutic treatments against complex diseases, such as cancer. Recent studies have demonstrated that the combined inhibition of Hsp90 and B-Raf provides synergistic effects against several types of cancers. Moreover, it has been reported that PDHK1, which presents an ATP-binding pocket similar to that of Hsp90, plays an important role in tumor initiation, maintenance and progression, participating also to the senescence process induced by B-Raf oncogenic proteins. Based on these premises, the simultaneous inhibition of these targets may provide several benefits for the treatment of cancer. In this work, we set up a design strategy including the assembly and integration of molecular fragments known to be important for binding to the Hsp90, PDHK1 and B-Raf targets, aided by molecular docking for the selection of a set of compounds potentially able to exert Hsp90-B-Raf-PDHK1 multi-target activities. The designed compounds were synthesized and experimentally validated in vitro. According to the in vitro assays, compounds 4 a , 4 d and 4 e potently inhibited Hsp90 and moderately inhibited the PDHK1 kinase. Finally, molecular dynamics simulations were performed to provide further insights into the structural basis of their multi-target activity.     

6,7-二甲氧基-4-哌嗪喹唑啉缩氨基硫脲衍生物的合成及体外抗肿瘤活性研究

以4,5-二甲氧基-2-氨基苯甲酸和醋酸甲眯为起始原料,经环化、氯化、取代和缩合四步反应,设计、合成了六个未见文献报道的含有缩氨基硫脲的喹唑啉衍生物4a～4f,其结构用1H NMR,13C NMR,ESI-MS,IR及元素分析测试技术进行了表征.采用MTT法测试了化合物4a～4f对人胃癌SGC-7901、人口腔表皮样癌KB和人纤维肉瘤HT-1080的体外抗肿瘤活性.初步的测试结果表明,化合物4a和4f对HT1080表现出显著的抗肿瘤活性.     

Detecting Cytosolic Peptide Delivery with the GFP Complementation Assay in the Low Micromolar Range

Transfection of cells with a plasmid encoding for the first ten strands of the GFP protein (GFP1‐10) provides the means to detect cytosolic peptide import at low micromolar concentrations. Cytosolic import of the eleventh strand of the GFP protein either by electroporation or by cell‐penetrating peptide‐mediated import leads to formation of the full‐length GFP protein and fluorescence. An increase in sensitivity is achieved through structural modifications of the peptide and the expression of GFP1‐10 as a fusion protein with mCherry.     

姜黄素联合顺铂对卵巢癌细胞COC1的体外抗肿瘤作用

利用MTT比色法研究了姜黄素(Cur)联合顺铂（DDP）对卵巢癌COC1细胞的抑制作用。 结果表明,当ρ(DDP)为2.5~10 mg/L,ρ(Cur)=5 mg/L时,与DDP相比,二者联合用药对卵巢癌COC1细胞可产生协同抑制作用;ρ(Cur)=5 mg/L就可明显增强COC1细胞对顺铂的敏感性,增敏倍数为2.66倍;光学显微镜观察发现,药物作用后COC1细胞的形态发生了改变,细胞折光度下降,大小不一、形态各异、排列疏散和胞浆空泡化严重。 为探讨姜黄素协同顺铂抑制肿瘤的机制,本研究采用高效液相色谱法测定姜黄素辅助用药前后细胞内DDP含量的变化。 结果表明,在加入姜黄素前后,COC1细胞内顺铂含量虽然略有下降,但差异无统计学意义（P＞0.05）。 由此可见,姜黄素与顺铂联合用药对人卵巢癌COC1细胞增殖具有协同抑制作用,且姜黄素可同时增加COC1细胞对顺铂的敏感性,但姜黄素可能并未明显改变顺铂在细胞内的含量,即姜黄素可能不是通过影响顺铂进入细胞的通路而起协同抑制作用的。     

Porous GdIII‐Organic Framework as a Dual‐Functional Material for Cyanosilylation of Aldehydes and Ablation of Human Liver Cancer Cells

Metal‐organic frameworks (MOFs) have gained great attention in recent years because they could behave as multifunctional materials which combine the advances of porous solids and coordination complexes. With the aim of constructing multifunctional MOFs, in this study, we choose a Y‐shaped tricarboxylic ligand biphenyl‐3,4′,5‐tricarboxylic acid (H₃bpt) to react with Gd^III ions to afford a new dual‐functional lanthanide‐organic framework with the chemical formula of [Gd₂(bpt)₂(H₂O)₂] · (DMF)₂(H₂O)₆ ( 1 ) (DMF = N,N‐dimethylformamide) under solvothermal condition. The title complex was characterized by means of elemental analysis, FT‐IR spectroscopy, thermogravimetric and X‐ray diffraction analyses. Crystal structure analysis reveals that compound 1 is composed of 1D helical chain secondary building units that connect by the bpt^3– ligands into a 3D framework with 1D nanosized channels running along the b axis. In view of its high porosity and accessible open metal sites, the activated 1 ( 1a ) was studied for the cyanosilylation of aldehydes under solvent‐free conditions. The catalytic activity of 1a is much higher than that of compound 1 , indicating that the exposed open metal sites of 1a is beneficial to the cyanosilylation reaction. In connection to these, the different cytotoxicities of 1 and 1a were also evaluated on four human liver cancer cells (SMMC‐7721, Bel‐7402, MHCC97 and Hep3B) by the MTT assay.     

(E)-3-Arylidene-4-diazopyrrolidine-2,5-diones conveniently elaborated into cytotoxic compounds bearing primary sulfonamide and Michael acceptor moieties

The earlier described (E)-3-arylidene-4-diazopyrrolidine-2,5-diones have been elaborated into two distinct series of compounds both bearing a primary sulfonamide moiety and an electrophilic ‘Michael acceptor’ motif. These compounds demonstrated cytotoxicity against colorectal cancer cell line HCT 116.     

Anti-Cancer Effect of Kaffir Lime (Citrus Hystrix DC) Leaf Extract in Cervical Cancer and Neuroblastoma Cell Lines

Previous study showed that kaffir lime leaf contains alkaloid, flavonoid, terpenoid, tannin and saponin. The objective of this study was to examine the cytotoxic effect of kaffir lime leaf extract on cervical cancer and neuroblastoma cell lines. The method used for this research to determine cell viability was an 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results showed that an ethyl acetate extract had an IC50 for HeLa cells, UKF-NB3, IMR-5 and SK-N-AS parental cells of 40.7 μg · mL^–1, 28.4 μg · mL^–1, 14.1 μg · mL^–1, and 25.2 μg · mL^–1 respectively. Furthermore, the IC50 of chloroform extracts for HeLa cells, UKF-NB3, IMR-5 and SK-N-AS parental were 17.6 μg · mL^–1, 18.9 μg · mL^–1, 6.4 μg · mL^–1, and 9.4 μg · mL^–1 respectively. These data showed that kaffir lime extract reduces the viability of cervical and neuroblastoma cell lines and may have potential as anti-cancer compounds.