HETEROCYCLIC COMMUNICATIONS
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2022
·Vol. 28
·期 1
·84-94
·
IF 2
Zhongyu Zhang,Meng Chen,Mingqiong Tong,Wan Sun,Pingxuan Dong,Xinfeng Song,Xiaoyue Wang
Three complexes, namely complex ( 1 ), complex ( 2 ), and complex ( 3 ), were synthesized and characterized by X-ray diffraction, thermogravimetric study, and elemental study. Complex ( 1 ) comprises discrete binuclear clusters, where two oxygen atoms of 2-chloro-5-nitrobenzoic acid bridge the two copper atoms. Complex ( 2 ) is a six-coordination structure consisting of four nitrogen atoms and two oxygen atoms in 2-chloro-5-nitrobenzoic acid and 1,10-phenanthroline to furnish a twisted octahedron. Complex ( 3 ) is a six-coordination structure consisting of four oxygen atoms and two nitrogen atoms from the 2-chloro-5-nitrobenzoic acid, methanol, and 2,2′-dipyridyl to furnish a distorted octahedral geometry. Metal complexes’ anti-tumor activity was also investigated by the MTT assay. Of the complexes tested, complex ( 1 ) could induce apoptosis in these A549 lung cancer and Caco-2 colon adenocarcinoma cells and complex ( 2 ) could induce apoptosis in Caco-2 colon adenocarcinoma cells. CCDC for complex ( 1 ) was 1543354, CCDC for complex ( 2 ) was 1546991, and CCDC for complex ( 3 ) was 1543417.
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FUEL PROCESSING TECHNOLOGY
·
2023
·
IF 7.5
Shanshan Shao,Xiankun Xia,Xiaohua Li,Huiyan Zhang,Rui Xiao
As the aviation sector grows and fossil fuels are utilized, the environment and economy depend on biomass-based aviation fuel . This study investigated acid sites in aldol condensation to produce aviation fuel from biomass-derived aldehydes and ketones over the bifunctional catalyst Ni/HZSM-5. Due to its excellent 10-member ring channels structure, HZSM-5 yielded 63.81% of the targeted condensates as aviation fuel precursor. At 200 °C for 9 h, aldehydes and ketones were converted to 90.32% and 69.53% of the required condensates. Sodium ion-exchange HZSM-5 with different Brönsted acid site quantities was tested for condensation . Brönsted acid sites were the active center for aldol condensation of aldehydes and ketones, increasing product yield. In γ-Al 2 O 3 , the overall amount of Brönsted acid and Lewis acid was equivalent to that of HZSM-5, the amount of Lewis acid was much more. The yield of the targeted condensates over γ-Al 2 O 3 was only 46.11%, much lower than that of HZSM-5 (69.53%). Thus, Brönsted acid sites were better than Lewis acid sites for aldol condensation of aldehydes and ketones. The balance of active sites for aldol condensation and hydrogenation increased the intended alkane yield to 62.91% with 20 wt% Ni loading. This study involves improving biomass-based aviation fuel generation.
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2019
·
IF 4.833
Zhang Li,Zhong-Chang Wang,Xin Li,Muhammad Abbas,Song-Yu Wu,Shen-Zhen Ren,Qi-Xing Liu,Yi Liu,Peng-Wen Chen,Yong-Tao Duan,Peng-Cheng Lv,Hai-Liang Zhu
In this paper, 41 hybrid compounds containing diaryl-1,5-diazole and morpholine structures acting as dual COX-2/5-LOX inhibitors have been designed, synthesized and biologically evaluated. Most of them showed potent antiproliferative activities and COX-2/5-LOX inhibitory in vitro. Among them, compound A33 displayed the most potency against cancer cell lines (IC 50 = 6.43–10.97 μ M for F10, HeLa, A549 and MCF-7 cells), lower toxicity to non-cancer cells than celecoxib ( A33 : IC 50 = 194.01 μ M vs. celecoxib : IC 50 = 97.87 μ M for 293T cells), and excellent inhibitory activities on COX-2 (IC 50 = 0.17 μ M) and 5-LOX (IC 50 = 0.68 μ M). Meanwhile, the molecular modeling study was performed to position compound A33 into COX-2 and 5-LOX active sites to determine the probable binding models. Mechanistic studies demonstrated that compound A33 could block cell cycle in G2 phase and subsequently induced apoptosis of F10 cells. Furthermore, compound A33 could significantly inhibit tumor growth in F10-xenograft mouse model, and pharmacokinetic study of compound A33 indicated that it showed better stability in vivo . In general, compound A33 could be a promising candidate for cancer therapy.
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SEPARATION AND PURIFICATION TECHNOLOGY
·
2023
·
IF 8.6
Wenqing Wang,Hao Li,Meiyao Li,Huiling Lu,Jianming Pan
Molecularly imprinted polymers (MIPs) are an effective method to accurately recognize and isolate targets. Adenosine 5′-monophosphate (AMPs) are typical nucleoside compounds widely used as intermediates and raw materials in the pharmaceutical field with high medicinal potential. In this work, molecularly imprinted adsorbents with fast magnetic response recovery were obtained for the selective separation of AMP by covering MIPs with AcrU and AM as functional monomers and AMP as a template molecule on the surfaces of Fe 3 O 4 NPs, and then by layer-by-layer (LBL) assembling of the MIPs realized through glutaraldehyde (GA) mediation. Static adsorption experiments have been utilized to explore the adsorption effects of different numbers of imprinted layers. The experimental results showed that the Fe 3 O 4 @MIPs-LBL2 covered with two layers of MIPs had the best imprinting effect (IF = 2.50), and the adsorption of AMP by Fe 3 O 4 @MIPs-LBL2 was dominated by chemisorption, with the saturation adsorption capacity reaching 105.72 μmol g −1 , it could adsorb and separate AMP efficiently from the actual sample (human urine). The magnetic responsiveness solves the problem of difficult recovery and high recovery loss of nano-imprinted adsorbents. Notably, this work not only proposes a magnetic imprinted adsorbent for selective separation of AMP, but also explores the structure-effect relationship between the number of layers of MIPs and adsorption performance, which provides a new inspiration for improving the performance of molecular imprinting techniques.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2023
·
IF 5.8
Yimin Wang,Yanan Zhang,Zhihui Yang,Lei Zhang,Xiangping Chen,Guliang Yang,Jianfeng Zhan,Shiming Li,Feng He,Guanwei Fan
Psoriasis is an inflammatory skin disease accompanied with chronic papulosquamous lesions and multiple comorbidities that considerably affect patients’ quality of life. In order to develop an enhanced therapeutic strategy for psoriasis, 5-demethylnobiletin (5-DN), a kind of polymethoxyflavones (PMFs) with high anti-inflammatory activity, was delivered in vitro and in vivo by the nanocarrier of mesoporous silica nanoparticles (MSNs) both in the human keratinocytes HaCaT cell line and the mouse model with psoriasis-like lesions. The drug-loaded nanocarrier system (MSNs@5-DN) significantly improved the biocompatibility and bioavailability of 5-DN. Investigations at cell biological, histopathological, and molecular levels revealed the pharmacological mechanism of the drug delivery system, including the inhibition of inflammatory responses by downregulating the proinflammatory cytokine levels of tumor necrosis factor α (TNF-α) and interleukin-6 (IL-6). The upregulation of anti‑inflammatory cytokine of transforming growth factor-β1 (TGF-β1) and microRNA-17-5p, a critical regulator of the PTEN/AKT pathway, was also observed. The psoriasis-like lesions were markedly ameliorated in the mouse models treated with MSNs@5-DN. The designed drug-loading system shows an enhanced therapeutic outcome for psoriasis-like lesion compared with free 5-DN. This study revealed the synergistic effect of functionalized MSNs loaded with PMFs on the clinical treatment of human psoriasis.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2021
·
IF 6.953
Junxin Zhao,Shichang Liu,Yifang Gao,Maomao Ma,Xianghui Yan,Ding Cheng,Dongman Wan,Zheling Zeng,Ping Yu,Deming Gong
Enzymatic degradation has become the most promising approach to degrading organic ester compounds. In this study, Bacillus licheniformis NCU CS-5 was isolated from the spoilage of Cinnamomum camphora seed kernel, and its extracellular lipase was purified, with a specific activity of 192.98 U/mg. The lipase was found to be a trimeric protein as it showed a single band of 27 kDa in SDS-PAGE and 81 kDa in Native-PAGE. It was active in a wide range of temperatures (5–55 °C) and pH values (6.0–9.0), and the optimal temperature and pH value were 40 °C and 8.0, respectively. The enzyme was active in the presence of various organic solvents, metal ions, inhibitors and surfactants. Both crude and purified lipase retained more than 80% activity after 5 h in the presence of commercial detergents, suggesting its great application potential in detergent industry. The highest activity was found to be towards medium- and long-chain fatty acids (C 6 -C 18 ). Peptide mass spectrometric analysis of the purified lipase showed similarity to the lipase family of B. licheniformis . Furthermore, it degraded more than 90% 2,4-D butyl ester to its hydrolysate 2,4-D within 24 h, indicating that the novel lipase may be applied to degrade organic ester pesticides.
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BIOSENSORS & BIOELECTRONICS
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2021
·
IF 10.618
Kai Zhang,Zhenqiang Fan,Bo Yao,Yuedi Ding,Jing Zhao,Minhao Xie,Jianbin Pan
Sialic acid-binding immunoglobulin (Ig)-like lectins (Siglecs) is a type I transmembrane receptor on the cell surface. Siglec-5, as one of the Siglecs family, play an important role as an inhibitory receptor for leukocytes in the human body. The development of novel siglec-5 assays can help to study the pathogenesis of related diseases as well as to develop novel therapeutic drugs. We use catalytic hairpin assembly (CHA) amplification strategy combined with CRISPR-Cas12a′s side-cutting feature to build a 2D ultra-thin Ti 3 C 2 T x (MXene) based electrochemiluminescence (ECL) biosensor for the detection of Siglec-5. By using this ECL biosensor, the cleavage of CRISPR-Cas12a is reasonably combined with CHA-mediated isothermal amplification, thereby realizing the sensitive amplification assay Siglec-5 with 20.22 fM sensitivity. By introducing pairs of sites that are not in the same double-stranded DNA into the DNA duplex, the hybridization sequence of CRISPR-Cas12a complements the targeting mechanism to enhance indirect Siglec-5 amplification assay. Also, the double-strand DNA (dsDNA) design based on CRISPR-Cas12a amplification allows the same CRISPR RNA (crRNA, also known as guide RNA (gRNA)) to detect the output of DNA duplexes from different intermediate DNAs, which provides a common way for biomarker detection based on the conversion of protein analytes to intermediate DNA strategy. This work extends the application scope of CRISPR-Cas12a to the construction of ECL biosensors, evaluates the role of lectins, which can be used for the biochemical research and clinical diagnosis of protein markers. This is the first investigative work exploring the Trans-Cleavage activity of CRISPR-Cas12a for Mxene-based ECL biosensor establishment to the best of our knowledge.
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FOOD CHEMISTRY
·
2021
·
IF 7.514
Li-Xin Ma,Xu-Hui Huang,Jie Zheng,Liu Dong,Jia-Nan Chen,Xiu-Ping Dong,Da-Yong Zhou,Bei-Wei Zhu,Lei Qin
Blue mussel ( Mytilus edulis L.) is a popular, nutritional, and tasty mollusk. To better understand the composition of nutrients and improve further processing of the mussels, metabolomic approaches were used to analyze the free amino acids, 5ʹ-nucleotides, and lipid compositions of different tissues. Our results showed that the viscera and gonad were rich in glutamine and glycine. Adenosine 5ʹ-monophosphate, uridine 5ʹ-monophosphate, guanosine 5ʹ-monophosphate, and inosine 5ʹ-monophosphate were abundant in the mantle, foot, and adductor muscle. Three main types of lipids, phospholipids (PLs), glycerides, and fatty acids (FAs), were semi-quantified. PLs were mainly distributed in the gonad of male mussels and viscera, gonad, and mantles of female mussels. FAs were relatively high in the viscera of males and in the gonad and viscera of females. The viscera of females were rich in phosphatidylcholine, such as 16:0/22:6 and 16:0/20:5. Triglycerides were the key lipids for distinguishing different tissues, especially 16:0/18:1/18:3 and 16:0/18:4/20:5.
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BIORESOURCE TECHNOLOGY
·
2021
·
IF 9.642
Jingyuan Shang,Guangbin Fu,Zhenping Cai,Xiang Feng,Yongxiao Tuo,Xin Zhou,Hao Yan,Chong Peng,Xin Jin,Yibin Liu,Xiaobo Chen,Chaohe Yang,De Chen
Valorization of biomass to olefin or aromatics harbours tremendous practical value due to growing concerns about sustainable production of chemicals. Herein, the olefin or aromatics yields of ex-situ catalytic pyrolysis of pine can be regulated by impregnating Sn on hollow-structured ZSM-5 (M-ZSM-5) and microporous ZSM-5 catalysts in fixed-bed reactor, respectively. Results showed that Sn/ZSM-5 catalyst simultaneously increased medium acidic sites and maintained strong acidic sites, which obtained the maximum carbon yield of aromatics (33.77%) due to enhanced cracking and deoxygenation reactions. In addition, Sn boosted alkylation between olefin and aromatics, generating more alkylbenzene. In contrast, Sn/M-ZSM-5 catalyst produced the highest olefins carbon yield (12.39%) because the reduction of strong acidic sites and microporous volume inhibited the olefin aromatization. Moreover, olefins were easier to desorb from Sn/M-ZSM-5 due to the enhanced mass transfer ability, which weakened the alkylation reactions. The synergistic effect harbours great significance to manipulate the distribution of products.
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JOURNAL OF DRUG TARGETING
·
2021
·
IF 5.121
Yongwei Hao,Cuixia Zheng,Qingxia Song,Hongli Chen,Wenbin Nan,Lei Wang,Zhenzhong Zhang,Yun Zhang
Drug delivery with the help of nanoparticles could transport more payloads to tumour site. Owing to their limited accumulation and penetration in the tumour tissues, to increase delivery efficiency is currently still required for applying nanomedicine to treat tumour. Here, we initially report a pressure-driven accumulation of drug-loaded nanoparticles to tumours for efficient tumour therapy with a dry cupping device. The mesoporous Mn-doped silica based nanoparticles delivering 5-aza-2-deoxycytidine and docetaxel were prepared, characterised and used as a model nanomedicine to investigate the potential of dry cupping treatment. For this system, the Mn doping not only endowed the mesoporous silica nanoparticles biodegradability, but also made it much easier to bind a tumour targeting group, which is a G-quadruplex-forming aptamer AS1411. On tumour-bearing mice, the in vivo results demonstrated that the dry cupping treatment could substantially improve the distribution of nanomedicines at tumour site, resulting in enhanced treatment efficacy. Overall, this method enables the therapeutical nanoparticles accumulate to tumour through increasing the blood perfusion as well as altering the biological barrier, which opened up possibilities for the development of pressure-driven nanomedicine accumulation at tumour site.
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RENEWABLE ENERGY
·
2021
·
IF 8.001
Nishu,Chong Li,Meiyun Chai,Md. Maksudur Rahman,Yingkai Li,Manobendro Sarker,Ronghou Liu
Hemicellulose was extracted from rice straw, and catalyst ZSM-5 was modified by NaOH and Ni over alkaline treatment and wet impregnation method, respectively. To investigate the effects of modified ZSM-5 on selectivity of aromatic hydrocarbons, catalytic pyrolysis of hemicellulose was studied via Py-GC/MS. Significant effect has been reported for product selectivity and composition over the modified catalysts. All the modified catalysts showed better aromatic selectivity than parent ZSM-5 (P-ZSM-5). Notably, alkali modified ZSM-5 with 0.4 M concentration of NaOH (0.4 M ZSM-5) showed 36% selectivity towards aromatics with the share of benzene, toluene, and xylene (58%) and share of polyaromatics (15%) compared to others. Meanwhile, 8 wt% Ni-ZSM-5 showed the highest selectivity of aromatic hydrocarbons of 54% where the share of benzene, toluene, and xylene was 70%. This research revealed that metal modified ZSM-5 significantly influences the aromatics yield, which is essential for the production of liquid fuels and chemicals.
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MOLECULES
·
2020
·Vol. 25
·期 4
·858
·
IF 3.267
Xiaojuan Liu,Yue Wang,Yezhi Chen,Shuting Xu,Qin Gong,Chenning Zhao,Jinping Cao,Chongde Sun
O-methylation of flavonoids is an important modification reaction that occurs in plants.O-methylation contributes to the structural diversity of flavonoids, which have several biological and pharmacological functions. In this study, anO-methyltransferase gene (CrOMT2) was isolated from the fruit peel ofCitrus reticulata, which encoding a multifunctionalO-methyltransferase and could effectively catalyze the methylation of 3’-, 5’-, and 7-OH of flavonoids with vicinal hydroxyl substitutions. Substrate preference assays indicated that this recombinant enzyme favored polymethoxylated flavones (PMF)-type substrates in vitro, thereby providing biochemical evidence for the potential role of the enzyme in plants. Additionally, the cytotoxicity of the methylated products from the enzymatic catalytic reaction was evaluated in vitro using human gastric cell lines SGC-7901 and BGC-823. The results showed that the in vitro cytotoxicity of the flavonoids with the unsaturated C2-C3 bond was increased after being methylated at position 3’. These combined results provide biochemical insight regarding CrOMT2 in vitro and indicate the in vitro cytotoxicity of the products methylated by its catalytic reaction.Keywords:citrus;flavonoids;O-methyltransferase;bioactivity;cytotoxicity
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