SYNTHETIC COMMUNICATIONS
·
2023
·
IF 2.1
Jun Yang,Guang-Ping Liang,Xiong-Li Liu
To investigate the effects and mechanisms of 4-(1H-indol-1-yl)-4-oxobutanoic acid spliced podophyllotoxin derivatives (3a–3l) on tumor cells. The MTT method was adopted to evaluate (3a–3l) antitumor activity in vitro against A549 cells, A549/DDP cells, MCF-7 cells. The results showed that compound 3l had the most prominent inhibitory effect and high selectivity with IC50 18.53 ± 1.51 µM against A549/DDP cells. Meanwhile, the effects of compound 3l on the nuclear state, cell cycle and apoptosis of A549/DDP cells showed that compound 3l induced apoptosis by delaying the G2/M phase of A549/DDP cell cycle. In addition, molecular docking of compound 3l also showed that it could form a good hydrogen bond with ARG-158 (d = 2.6, 2.7 Å) and HIS-406 (d = 2.5 Å) at the colchicine site of tubulin. Compound 3l could provide lead compound for the development of new multi-drug resistant anti-tumor drugs.
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INDUSTRIAL & ENGINEERING CHEMISTRY RESEARCH
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2019
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IF 3.375
Yunpeng Hu,Kai Wang,Chunli Han,Tao Wang,Guangsheng Luo
A novel liquid–liquid microdispersion method for the synthesis of TS-1 has been developed by continuous preparation of the precursor. In the novel process, the solution of TBOT in n-hexane could be very uniformly dispersed into the oligomeric silicate prehydrolysis mixture to form microdroplets by a microsieve pore reactor. Due to the fast mixing and very high mass transfer performance of the microdispersion process, the Ti species could be uniformly distributed into the mixture and were more likely to condense into the oligomeric silicate precursor species rather than appear with self-condensation. The prepared samples had a minimum molar ratio of Si/Ti at 51 without extra-framework Ti species. Furthermore, the solvent of n-hexane can be recycled by simple phase separation rather than evaporation under the conditions of using isopropanol, which reduced energy consumption. This continuous microdispersion technology could be controllable and a reliable scaling-up for the preparation of TS-1.
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BIOSENSORS & BIOELECTRONICS
·
2019
·
IF 9.518
Xiaoxue Fu,Junlin He,Chengli Zhang,Jun Chen,Yilin Wen,Jia li,Weiran Mao,Hangtian Zhong,Jiahao Wu,Xingduo Ji,Chao Yu
In this work, an aptamer was used as the target capturing agent and a trimetallic signal amplification strategy based on [email protected] and AuPtRu NPs was demonstrated for the sensitive detection of TSP-1. Herein, the synthesized AuPtRu nanocomposite (AuPtRu NPs) not only acts as the catalyst for catalyzing hydrogen peroxide but also acts as a nanocarrier for capturing the -NH 2 termination single strand DNA (S1) to obtain the signal probe (SP, AuPtRu nanocomposite/S1). Then, SP was efficiently linked into TSP-1 aptamers with the addition of complementary linking strands to form M1 (SP/aptamer). The [email protected] nanocomposites were obtained by in situ reduction and used as GCE electrode modification materials. The -NH 2 -modified capture probe (CP) DNA was immobilized on the surface of [email protected] nanocomposites for hybridizing SP. In the presence of the target TSP-1, the aptamer recognizes the target and binds strongly so that SP is released from the prepared M1 and then hybridized with CP. When the detection solution contains an electrochemical matrix of H 2 O 2 , AuPtRu NPs can oxidize H 2 O 2 to obtain an enhanced signal. Furthermore, the proposed aptasensor has a very low LOD of 0.13 fg mL −1 TSP-1 in the detection range of 1 fg mL −1 to 10 ng mL −1 . Moreover, the proposed platform also has application implications for other potential targets.
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高影响因子
CARBOHYDRATE POLYMERS
·
2018
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IF 5.158
Guoyu Li,Kungang Chai,Liqin Zhou,Zhangfa Tong,Hongbing Ji
A novel aromatic-rich cellulose-urethane polymer (ACUP) was easily fabricated by crosslinking cellulose with 4,4’,4’’-triphenylmethane triisocyanate for preferential adsorption of acetophenone (AP) over 1-phenyethanol (PE). The successful synthesis of ACUP was confirmed by the instrumental analyses, e.g., FTIR, TG, XPS, FE-SEM, 13 C CP/MAS NMR and XRD. For single-solute adsorption of AP or PE onto ACUP, the effects of adsorbent dosage, agitation speed, time, solute concentration and temperature were systematically investigated. The overall adsorption process was exothermal and spontaneous in nature, and followed the pseudo-second-order kinetic rate equation and Freundlich isotherm model. Competitive adsorption studies concerning the effects of phenyl content in ACUP adsorbent, pH and ionic strength were also presented, in which ACUP showed much higher affinity for AP over PE. In addition, ACUP was examined as a column packing material for adsorptive separation of the equimolar mixture of AP-PE, showing excellent separation capability. The easily-regenerated and recyclable features of ACUP were demonstrated by adsorption-desorption cycles in both batch and continuous modes. Furthermore, a possible mechanism for the preferential adsorption of AP over PE, which may be associated with π-π and hydrogen bonding interactions was suggested on the basis of experimental and theoretical results.
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高影响因子
BRITISH JOURNAL OF PHARMACOLOGY
·
2018
·Vol. 176
·期 3
·416-435
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IF 6.81
Jingyan Li,Junying Huang,Jing Lu,Zhen Guo,Zhuoming Li,Hui Gao,Panxia Wang,Wenwei Luo,Sidong Cai,Yuehuai Hu,Kaiteng Guo,Luping Wang,Zhenzhen Li,Minghui Wang,Xiaolei Zhang,Peiqing Liu
Background and Purpose Activation of PKC-ζ is closely linked to the pathogenesis of cardiac hypertrophy. PKC-ζ can be activated by certain lipid metabolites such as phosphatidylinositol (3,4,5)-trisphosphate and ceramide. However, its endogenous negative regulators are not well defined. Here, the role of the sirtuin1-PKC-ζ signalling axis and the underlying molecular mechanisms were investigated in cardiac hypertrophy. Experimental Approach Cellular hypertrophy in cultures of cardiac myocytes, from neonatal Sprague-Dawley rats, was monitored by measuring cell surface area and the mRNA levels of hypertrophic biomarkers. Interaction between sirtuin1 and PKC-ζ was investigated by co-immunoprecipitation and confocal immunofluorescence microscopy. Sirtuin1 activation was enhanced by resveratrol treatment or Ad-sirtuin1 transfection. A model of cardiac hypertrophy in Sprague-Dawley rats was established by abdominal aortic constriction surgery or induced by isoprenaline in vivo . Key Results Overexpression of PKC-ζ led to cardiac hypertrophy and increased activity of NF-κB, ERK1/2 and ERK5, which was ameliorated by sirtuin1 overexpression. Enhancement of sirtuin1 activity suppressed acetylation of PKC-ζ, hindered its binding to phosphoinositide-dependent kinase 1 and inhibited PKC-ζ phosphorylation in cardiac hypertrophy. Consequently, the downstream pathways of PKC-ζ' were suppressed in cardiac hypertrophy. This regulation loop suggests a new role for sirtuin1 in mediation of cardiac hypertrophy. Conclusions and Implications Sirtuin1 is an endogenous negative regulator for PKC-ζ and mediates its activity via regulating the acetylation and phosphorylation in the pathogenesis of cardiac hypertrophy. Targeting the sirtuin1-PKC-ζ signalling axis may suggest a novel therapeutic approach against cardiac hypertrophy.
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Molecular Medicine Reports
·
2019
·Vol. 19
·期 5
·3658-3666
·
IF 1.851
Jin Xu,Yin Ying,Gaoyun Xiong,Liqin Lai,Qingliang Wang,Yue Yang
Nasopharyngeal carcinoma (NPC) is a type of cancer originating in the nasopharynx. There are no NPC‑specific treatments available at present. Serpin peptidase inhibitor clade C member 1 (SERPINC1) serves roles in anticoagulation and anti‑inflammation. The aim of the present study was to investigate the role of SERPINC1 in the proliferation and apoptosis of NPC cells. Tumor and adjacent healthy tissue samples were collected from patients with NPC. Additionally, the SERPINC1 gene was silenced in the HNE3 cell line using short interfering RNA targeted against SERPINC1 (SERPINC1‑siRNA). Cell viability was determined via a Cell Counting Kit‑8 assay; furthermore, proliferation and apoptosis were investigated via flow cytometry. Western blotting and reverse transcription‑quantitative polymerase chain reaction analysis were performed to determine the expression levels of protein and mRNA. It was revealed that the expression levels of SERPINC1 mRNA and protein were increased in NPC tumor tissues compared with in adjacent healthy tissues. The expression of SERPINC1 mRNA and protein in HNE3 cells decreased following SERPINC1‑siRNA transfection. Furthermore, knockdown of SERPINC1 promoted apoptosis and inhibited proliferation. It was also demonstrated that silencing SERPINC1 upregulated the expression of B‑cell lymphoma-2 (Bcl‑2)‑associated X protein and p53 mRNA and protein, and downregulated that of Bcl‑2, survivin and cyclin D1. Downregulation of SERPINC1 reduced the phosphorylation of phosphatidylinositol 3‑kinase (PI3K), protein kinase B (Akt) and mammalian target of rapamycin (mTOR). Thus, SERPINC1 knockdown may promote the apoptosis of HNE3 cells and inhibit proliferation via the suppression of the PI3K/Akt/mTOR signaling pathway.
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JOURNAL OF CHEMICAL TECHNOLOGY AND BIOTECHNOLOGY
·
2019
·Vol. 94
·期 6
·1951-1957
·
IF 2.659
Zhimin Ou,Jiaying Pan,Lan Tang,Hanbing Shi
BACKGROUND Magnetic nanoparticle immobilized enzymes are attractive owing to their potential applications in many biological fields. When an alternating magnetic field is applied, the magnetic moments of the magnetic nanoparticles are apt to align in the direction of the field, and the magnetic nanoparticles experience force in the direction of the field. Thus, the magnetic nanoparticles behave like microscopic stirrers. RESULTS In this study, (R)- N -(1-phenylethyl)acetamide was prepared continuously using immobilized lipase in an alternating magnetic field. The effect of several factors on the acylation reaction were investigated. A kinetic model of the continuous acylation reaction process also was developed. The conversion of 1-phenylethanamine reached a maximum value of 41.8% with lipase concentration 75 mg mL −1 (dry weight/reaction volume), substrate concentration 500 mmol L −1 and flow rate 25 μL min −1 The enantiomeric excess of (R)- N -(1-phenylethyl)acetamide was > 98.4%. The kinetic constants of the continuous reduction were r m = 2.25 × 10 −2 mmol L –1 min −1 , k cat = 6 × 10 −4 mmol L –1 min −1 , K A = 0.75 mmol L –1 , K B = 4.36 × 10 −3 , K QA = 2.43 × 10 −2 and K BQA = 6.2 × 10 −4 mmol L –1 . The kinetic model was in good agreement with the experimental data obtained during continuous acylation reaction. CONCLUSION The results revealed that the inhibition of the acylation reaction at high substrate concentrations was eliminated during the continuous reaction. Compared with the batch acylation reaction, the continuous acylation reaction showed significantly improved lipase catalyst efficiency. © 2019 Society of Chemical Industry
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AUSTRALIAN JOURNAL OF CHEMISTRY
·
2019
·Vol. 72
·期 7
·533-541
·
IF 1.226
Sai Huang,Mei Yang,Xin-Yu Deng,Qian Jiang Zhu,Ying Huang,Zhu Tao,Kai Chen
In the present work, a host–guest system of a hemimethyl-substituted cucurbit[6]uril derived from 3α-methyl-glycoluril (HMeQ[6]) and a hemicyanine dye, trans-4-[4-(dimethylamino)styryl]-1-methylpyridinium iodide (t-DSMI) showing strong fluorescence emission has been evaluated as a fluorescent probe. The results of a preliminary systematic study on the detection of a series of inorganic anions have revealed that this Q[n]-based host–guest fluorescent probe shows clear responses to BF4− and H2PO4− anions through distinct fluorescence quenching. Application of this Q[n]-based host–guest interaction system in anion recognition or detection opens a new avenue in Q[n] chemistry.
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Materials Science & Engineering C-Materials for Biological Applications
·
2018
·
IF 5.08
Yiqun Wang,Yi Lu,Jinkang Gong,Yuan Yao
Intermediate filaments, together with actin microfilaments and microtubules constituent the cytoskeleton of mammalian cells, involving in various cellular activities. The roles of intermediate filaments in cell skeleton reorganization when responding with extracellular matrix (ECM) nanostructure are poorly understood yet. To unveil the effects of fibrous composition and orientation on cells, we developed electrospun nanofibers of varying topology and components, and the effects on assembly of intermediate filaments as keratin and vimentin were investigated in detail. We found that aligned nanofibers enhanced expression of E-cadherin and promoted assembly of keratin intermediate filaments. Meanwhile, the compositional variation show different preference on up-regulation of the two intermediate filaments. Compared to keratin, the assembly of vimentin intermediate filaments were promoted by incorporating bovine serum albumin (BSA) functionalized graphene oxide (BSA-GO) into polycaprolactone (PCL) nanofibers. Thus, our findings elucidate how the different physical factors of fibrous extracellular matrix affect the reorganization of cytoskeleton by assembly of keratin and vimentin intermediate filaments.
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ACS Sustainable Chemistry & Engineering
·
2018
·
IF 6.14
Yufang Wu,Yiwei Sun,Jing Xiao,Xun Wang,Zhong Li
In this work, a novel Gly@HKUST-1 with simultaneously enhanced moisture stability and improved adsorption capacity was developed by grafting glycine (Gly) onto the open metal sites of HKUST-1, in order to recover light hydrocarbons from natural gas efficiently. The resultant Gly@HKUST-1 had higher C2H6 and C3H8 adsorption capacities compared to HKUST-1 and some other metal–organic frameworks, which reached as high as 6.47 and 7.80 mmol/g at ambient conditions. Its C2H6/CH4 and C3H8/CH4 adsorption selectivities were up to 12.6 and 173.5, respectively. Fixed-bed experiments showed that 0.3Gly@HKUST-1 could separate the CH4/C2H6/C3H8 mixtures completely at ambient conditions, showing excellent separation property toward the light hydrocarbons. More importantly, stability experiments confirmed that after the two samples were exposed to moist air (RH of 55%) for 20 days, 0.3Gly@HKUST-1 still remained its crystal structure, while parent HKUST-1 lost most of its crystallinity. Computational simulations showed that Gly grafting onto unsaturated Cu site played a critical role in enhancing stability against water vapor and improving capacity due to its shielding of unsaturated Cu site as well as introduction of −COOH or −NH2 as the H-binding sites. Gly@HKUST-1 is promising for practical application of efficiently recovering ethane and propane from natural gas by adsorption.
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International Journal of Polymer Science
·
2019
·
IF 1.892
Wei Xiong,Yue-kun Shen,Peng Dong,Ying Xiao,Xiong-qing Huang,Wen-qi Huang,Lu Yang,Xia Feng
Sustained release of anesthesia has shown great promise in the treatment of chronic pain in patients. In this research, we used neutralized ropivacaine as an anesthesia and poly(ε-caprolactone) (PCL) with different architectures to systematically study how these architectures affect the release of ropivacaine. After optimizing the parameters of the preparation of microspheres, ropivacaine-loaded 1-PCL microspheres and 4-PCL microspheres were obtained. Fourier Transform infrared spectra (FT-IR) and X-ray diffraction spectra (XRD) confirmed that ropivacaine was encapsulated within the microsphere rather than inserted on the surface of the microsphere. Ropivacaine was found to be buried deeper in the 1-PCL microsphere than in the 4-PCL microsphere. In vitro release assay revealed that small crystalline grains interfered with ropivacaine release in 4-PCL microspheres during the initial release period, but then two kinds of microspheres showed a similar ropivacaine release rate. We basically proved that the architecture of PCL has a negligible effect on ropivacaine release. Cell proliferation test revealed that the release of products from the microspheres resulted in insignificant toxicity towards mammalian cells.
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SENSORS AND ACTUATORS B-CHEMICAL
·
2019
·
IF 6.393
Ensheng Xu,Haitang Yang,Lina Wu,Jin Chen,Wei Wei,Yong Liu,Songqin Liu
Since the expression of poly(ADP-ribose) polymerase-1 (PARP-1) was significantly up-regulated in several primary malignancies, it was important to construct a sensitive and rapid PARP-1 assay for early diagnosis of cancer. When PARP-1 was activated by active dsDNA, it generates a number of negatively charged poly(ADP-ribose) (PAR) polymers, which can be readily detected. Here, we developed a label-free electrochemical (EC) biosensor for PARP-1 activity based on the electrostatic attraction between negatively charged PAR and positively charged amino-functioned mesoporous silica films (NH 2 -MSFs). Negatively charged PAR was absorbed on the NH 2 -MSFs surface and suppressed the electrochemical signal as the PAR prevented the electroactive probe reaching to the ITO electrode. The electrochemical signal for PAR linearly decreased from 0.01 U to 1.2 U with a detection limit of 0.005 U, which is comparable to the PARP-1 biosensors reported before. The strategy has been used to evaluate PARP-1 inhibitors and to detect PARP-1 activity in human serum and real cancer cells lysate with satisfactory results, indicating that it was a promising candidate for point-of-care diagnostics.
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