Frontiers in Plant Science
·
2022
·
IF 6.627
Lei Wenli,Song Yuyang,Long Ai,Que Yanyan,He Shuzhong,Zhong Hang,Chen Yang
The medicinal plants were wildly library of natural products in drug discovery. The most active molecules with seven-membered rings skeleton represent a challenge for construction. A stereoselectivity (4 + 3) cycloadditions between allenyl ethers and substituted furans induced by chiral auxiliaries has been investigated. And the results showed significant stereoselectivities and regioselectivities. The optical cycloadducts with an oxygen-substituted seven-membered ring framework were generated by removing chiral auxiliaries under acidic conditions. The antiproliferative activity of the novel compounds displayed moderate antiproliferative effects toward T47D cells.
研究领域:
有机化学
·
药物化学
·
癌症研究
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DOI
PubMed
高影响因子
Bioresources and Bioprocessing
·
2018
·Vol. 5
·期 1
·1-11
·
IF 0
Liu Xin,Wang Weiwei,Hu Haiyang,Lu Xinyu,Zhang Lige,Xu Ping,Tang Hongzhi
Background Benzofuran and its derivatives contain central pharmacophores and are important structures in medicinal chemistry. Chemical synthesis of benzofuran rings often requires expensive catalysts and stringent operational conditions. Biosynthesis is recognized as a promising way to save energy and produce valuable compounds. Dioxin biodegradation pathways can form several benzofuran derivatives, and these pathways may be a better choice for further synthesis of important biological compounds. 2-Hydroxy-4-(3′-oxo-3′ H -benzofuran-2′-yliden)but-2-enoic acid (HOBB), a benzofuran derivative, can be biosynthesized from dibenzofuran (DBF) through co-metabolic degradation in a lateral dioxygenation pathway. Results Efficient biosynthesis of HOBB was observed using whole cells of Pseudomonas putida strain B6-2. After cultivation in LB medium containing biphenyl, the cells were suspended to an OD 600 of 5 to conduct biosynthesis in the presence of 0.5-mM DBF at pH 7 for 8 h. The bacterial cells were used twice to degrade approximately 0.70-mM DBF, and in batch process, accumulated about 0.29-mM HOBB. HOBB could be easily purified from the reaction with ethyl acetate using the neutral-acid extraction method, and 13.58 ± 0.31 mg of HOBB was obtained from 22.49 ± 0.74-mg DBF with an overall production yield of 60.4% (w/w). The product HOBB, which is a yellow powder, could be detected and identified by LC–MS, GC–MS, and NMR. Conclusions In this study, a new biological route was developed to produce HOBB from DBF using whole cells of P. putida B6-2 (DSM 28064). The biosynthesis of HOBB may contribute to studies of the DBF lateral pathway and provide a new green route for synthesizing benzofuran derivatives with pharmacological activities.
研究领域:
环境生物学
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药学
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微生物学
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产品关联
DOI
JOURNAL OF POLYMER SCIENCE PART A-POLYMER CHEMISTRY
·
2015
·Vol. 53
·期 21
·2469-2480
·
IF 3.113
Yong Deng,Xi Wang,Qiulin Yuan,Mengxiang Zhu,Ying Ling,Haoyu Tang
A series of side-chain-functionalized α-helical polypeptides, i.e., poly(γ-4-(3-chloropropoxycarbonyl)benzyl- L -glutamate) (6) have been prepared from n-butylamine initiated ring-opening polymerization (ROP) of γ-4-(3-chloropropoxycarbonyl)benzyl- L -glutamic acid-based N -carboxyanhydride. Polypeptides bearing oligo-ethylene-glycol (OEG) groups or 1-butylimidazolium salts were prepared from 6 via copper-mediated [2+3] alkyne-azide 1,3-dipolar cycloaddition or nuleophilic substitution, respectively. CD and FTIR analysis revealed that the polymers adopt α-helical conformations both in solution and the solid state. Polymers bearing OEG (m = 3) side-chains showed reversible LCST-type phase transition behaviors in water while polymers bearing 1-butylimidazolium and I − counter-anions exhibited reversible UCST-type transitions in water. Variable-temperature UV-vis analysis revealed that the phase transition temperatures ( T pt s) were dependent on the main-chain length and polymeric concentration. © 2015 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2015 , 53 , 2469–2480
研究领域:
高分子化学
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生物材料
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产品关联
DOI
高影响因子
MOLECULES
·
2023
·Vol. 28
·期 23
·7876
·
IF 4.6
Zhang Hu,Hongrui Dong,Zhenyu Si,Yurong Zhao,Yuanwei Liang
Infectious diseases pose a major challenge to human health, and there is an urgent need to develop new antimicrobial agents with excellent antibacterial activity. A series of novel triazolo[4,3-a]pyrazine derivatives were synthesized and their structures were characterized using various techniques, such as melting point,1H and13C nuclear magnetic resonance spectroscopy, mass spectrometry, and elemental analysis. All the synthesized compounds were evaluated for in vitro antibacterial activity using the microbroth dilution method. Among all the tested compounds, some showed moderate to good antibacterial activities against both Gram-positiveStaphylococcus aureusand Gram-negativeEscherichia colistrains. In particular, compound2eexhibited superior antibacterial activities (MICs: 32 μg/mL againstStaphylococcus aureusand 16 μg/mL againstEscherichia coli), which was comparable to the first-line antibacterial agent ampicillin. In addition, the structure–activity relationship of the triazolo[4,3-a]pyrazine derivatives was preliminarily investigated.Keywords:nitrogen-containing heterocycles;triazole compounds;triazolo[4,3-a]pyrazine derivatives;antibacterial activity
研究领域:
药物化学
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微生物学
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有机合成
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DOI
PubMed
高影响因子
ENERGY & FUELS
·
2024
·
IF 5.2
Li Zhao,Hao Fu,Yuan-gu Xia,Ji Liu,Bin Hu,Zhan-jun Cheng,Xi Luo,Dan Yan,Ji-hong Li,Qiang Lu
Pyrolysis is a promising thermochemical conversion technology, which can convert biomass and cellulose into value-added products. Herein, a new approach of oxalic acid-assisted staged fast pyrolysis (OASFP) of cellulose was developed, achieving the coproduction of 1,4:3,6-dianhydro-α-d-glucopyranose (DGP), furfural (FF), and formic acid (FA) in separated pyrolysis stages. The lab-scale tests demonstrated that a selectivity of 71.6% and a yield of 31.5 wt % for FA in the aqueous phase, as well as a selectivity of 55.6% and a yield of 1.2 wt % for FF in the organic phase, were achieved in the primary pyrolysis stage under the optimized conditions (primary pyrolysis temperature of 220 °C and cellulose-to-oxalic acid (OA) ratio of 1:3). During the subsequent secondary pyrolysis process at 400 °C, the decomposition of the solid residue achieved a yield of 7.2 wt % and a selectivity of 32.7% for DGP. The interaction between OA and cellulose during the primary pyrolysis stage was essential for DGP generation. The formation mechanism of major products and the role of OA were revealed based on experiments and density functional theory calculations. In total, the OASFP of cellulose offers new possibilities and opportunities for biomass utilization.
研究领域:
生物质能
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化学工程
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热化学转化
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DOI
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2016
·
IF 1.78
Zhi-Jian Chen,Ya-Na Chen,Chun-Na Xu,Shan-Shan Zhao,Qi-Yue Cao,Shao-Song Qian,Jie Qin,Hai-Liang Zhu
Three novel mononuclear complexes, [M Ⅱ ( L ) 2 ·2H 2 O], (M = Cu, Ni or Cd; HL = 4-(3,4-dichlorophenyl)piperazine-1-carboxylic acid)were synthesized and structurally determined by single-crystal X-ray diffraction. Molecular docking study preliminarily revealed that complex 1 had potential urease inhibitory activity. In accordance with the result of calculation, in vitro tests of the inhibitory activities of complexes 1–3 against jack bean urease showed complex 1 (IC 50 = 8.17 ± 0.91 μ M) had better inhibitory activities than the positive reference acetohydroxamic acid (AHA) (IC 50 = 26.99 ± 1.43 μ M), while complexes 2 and 3 showed no inhibitory activities., kinetics study was carried out to explore the mechanism of the inhibiting of the enzyme , and the result indicated that complex 1 was a competitive inhibitor of urease. Albumin binding experiment and in vitro toxicity evaluation of complex 1 were implemented to explore its Pharmacological properties .
研究领域:
生物无机化学
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药物化学
·
酶学
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DOI
高影响因子
MEDICINAL CHEMISTRY RESEARCH
·
2018
·Vol. 28
·期 2
·133-142
·
IF 1.607
Feng Yu,Teng Xingxing,Gu Jinhua,Yu Bangwei,Luo Yan,Ye Lianbao
In the previous research, our group designed and synthesized 2,3,4,5-tetrahydro-1 H -pyrido-[4,3-b] indoles, which showed high anti-tumor activity. In this study, a series of novel 2,3,4,5-tetrahydro-1 H -pyrido-[4,3-b] indole derivatives were designed by introducing an alkyl or aralkyl and a sulfonyl group, which are considered as the pharmacophores of some antitumor drugs based on the combination principles, and synthesized. The antiproliferative activity of all the target compounds were evaluated against Hela, A549, HepG2, and MCF-7 cell lines using the MTT assay in vitro. The results were represented by IC 50 values. All compounds showed moderate to excellent antiproliferative activity with IC 50 values between 0 μM and 100 μM against cancer cells. The proliferations of Hela, A549, HepG2, and MCF-7 cell lines were inhibited in a dose-dependent manner, and the cytolytic activity was markedly inhibited at the same time. The IC 50 values of intermediate 3 inhibited against Hela, A549, HepG2, and MCF-7 cell lines were 52.75, 50.30, 60.31, and 54.39 μM, respectively, which were higher than the new compounds that we expected. The compounds 4a – 4d bearing sulfonyl, substituted by electron donating group, showed moderate to significant antiproliferative activity, in which compound 4c was the best with the IC 50 values of 13.71, 9.42, 15.06, and 14.77 μM, and these results suggested that the introduction of sulfonyl could increase the antiproliferative activity of 2,3,4,5-tetrahydro-1 H -pyrido-[4,3-b]indole. Compounds 4e – 4g bearing alkyl, phenyl, and arylated alkyl produced good antiproliferative activity and the IC 50 value of 4 g was lower than 30 μM. The target compounds were more potent against A549 compared to the other three cell lines. Molecular docking studies revealed the binding orientations of all the synthesized compounds in the active site of c-Met. Moreover, molecular dynamics simulations have been performed to evaluate the binding stabilities between the synthesized compounds and their receptors.
研究领域:
药物化学
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肿瘤学
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计算生物学
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DOI
高影响因子
ANALYST
·
2010
·Vol. 135
·期 8
·2139-2143
·
IF 3.272
Lun Wang,Cai-Ling Zhou,Hong-Qi Chen,Jing-Guo Chen,Jie Fu,Bo Ling
An efficient fluorescence energy transfer (FET) system between CePO4:Tb3+ nanocrystals as donor and 6-mercapto-5-triazole[4,3-b]-S-tetrazine as acceptor was built. CePO4:Tb3+ nanocrystals were synthesized in aqueous solutions, and characterized by transmission electron microscopy, electron diffraction pattern spectroscopy and spectrofluorometry. Under alkaline conditions, 6-mercapto-5-triazole[4,3-b]-S-tetrazine was generated by redox reaction of formaldehyde (HCHO) with 4-amino-3-hydrazino-5-mercapto-1,2,4-triazole (AHMT) at room temperature. The degree of the overlap was effective for FET between the emission spectrum of CePO4:Tb3+ and the absorption spectrum of 6-mercapto-5-triazole[4,3-b]-S-tetrazine. Based on this system, a simple and sensitive fluorescence method for the selective determination of formaldehyde in aqueous solutions was developed. Under optimal conditions, the quenched fluorescence intensity increased linearly with the concentration of HCHO ranging from 1.03 × 10−9 to 1.03 × 10−5 mg mL−1 with a correlation coefficient of 0.9976. The limit of detection was 1.65 × 10−10 mg mL−1. Compared with several methods, the proposed method had a wider linear range, higher selectivity and sensitivity. Moreover, analytical application of the method was demonstrated by water samples.
研究领域:
分析化学
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环境监测
·
纳米材料
·
生物传感
·
分子探针
✓ 已验证
DOI
高影响因子
Biofabrication
·
2012
·Vol. 4
·期 3
·035007
·
IF 3.48
Zhengjian Chen,Liqun Wang,Hongliang Jiang
In this study, the effect of different crosslinkers including glutaraldehyde (GTA), genipin (GIP) and procyanidine (PA) on the properties of the electrospun gelatin membranes was compared. The water-resistant ability of the membranes could be significantly improved after being crosslinked with PA at T > 40 °C. In contrast with GTA and GIP, the PA-crosslinking process did not apparently affect the fibrous structure, and induced the lowest shrinkage of the membranes. At the concentration of 5% of PA, the ultimate tensile strength and elongation of the hydrated membrane were 0.87 MPa and 148%, respectively, which were higher than those of the GIP-crosslinked counterparts. In addition, the PA-crosslinked membranes displayed the highest resistance to pepsin degradation, and fibroblast cells could migrate deeper into the interior of the membranes due to the good preservation of the fibrous structure during the cell culture process.
研究领域:
生物材料学
·
组织工程学
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产品关联
DOI
PubMed
高影响因子
APPLIED SURFACE SCIENCE
·
2023
·
IF 6.7
Yitian Su,Hongmin Jiang,Qiaoling Kang,Xianhe Meng,Xiaomei Zheng,Jianfei Lu,Xingkun Mei,Xiangdong Sun,Lijing Yan,Tingli Ma
All-organic aqueous batteries are deemed attractive energy storage systems for some application scenarios demanding recyclability or wearability. The efficient redox activity of quinone/hydroquinone-derived couples in biosystems inspires us to develop advanced batteries based on them. However, designing such an all-organic aqueous battery is challenging in selecting suitable electrolytes and active materials. A possible battery configuration consisting of the 9, 10-anthraquinone (AQ) anode, hydroquinone derivatives cathode, and weak acid metal-ion aqueous electrolyte is demonstrated herein. The molecular configuration of quinones and ionic type of electrolytes affect the redox behaviors of electrodes. Gratifyingly, a combination of AQ-tetrachlorohydroquinone-Al 2 (SO 4 ) 3 exhibits optimal performance. The underlying work mechanism of this full-battery configuration is disclosed by electrochemical and structural characterizations, finding that H + and Al 3+ are jointly involved in the redox reaction of quinone electrodes, and Al 3+ plays a crucial role. This work inaugurates a new framework for designing an all-organic aqueous battery.
研究领域:
能量存储系统
·
电化学
·
材料科学
✓ 已验证
DOI
高影响因子
Molecular Catalysis
·
2023
·
IF 4.6
Jiangwen Guo,Songbo Zhang,Juntao Ren,He Li,Shuwei Wang,Yanming Hu,Guangyuan Zhou
A series of pyridylbenzotriazole iron (II) complexes with general formula (L 2 FeCl 2 ) were synthesized and characterized by IR, ESI-MS, and elemental analysis . Determined by single-crystal X-ray crystallography, complex Fe1 adopts a distorted octahedral geometry. Upon activation with methylaluminoxane (MAO), the activity of the complex for isoprene polymerization decreased as the bulkiness of the substituent at 6-position of the pyridyl ring of the ligand increased. Notably, Fe1 exhibited excellent activity of 4.1 × 10 6 g/(mol (Fe)•h), affording polymers with ultra-high molecular weight ( M n = 2380 × 10 3 g/mol) and narrow distributions ( M w / M n = 1.72). The resulting polyisoprenes possessed predominantly cis -1,4/3,4 alternating structure and short cis -1,4 and 3,4 sequences, irrespective of the reaction conditions, indicating high thermal stability of the catalyst. Moreover, the prepared polyisoprene composite showed higher mechanical properties compared to SSBR-2466 and SSBR-5025 which are the key components of current commercial tread rubber, and had comparable wet traction and superior rolling resistance.
研究领域:
催化
·
高分子科学
·
材料科学
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产品关联
DOI
高影响因子
JOURNAL OF MATERIALS SCIENCE & TECHNOLOGY
·
2024
·
IF 11.2
Ce Zhu,Miaomiao He,Juehan Wang,Yong Huang,Wei Deng,Limin Liu,Ganjun Feng,Li Zhang,Yueming Song
Photothermal therapy (PTT) is a desirable way to attain on-demand hyperthermia owing to the heat generated by photothermal materials absorbing near-infrared) light. The mild heat (42 ± 0.5 °C) can not only accelerate bone tissue regeneration but also promote the release of bioactive ions from biomaterials. Based on this one-stone-two-birds strategy, a 3D printed PEEK-graphene composite scaffold (PG) with hydroxyapatite (HA) coating (PGH) for photothermally remote control of bone regeneration was well designed in this study. The results showed that the HA coating on PGH could release Ca 2+ and PO 4 3– ions easily under NIR irradiation, which was ascribed to the mild heat generated from graphene in the composite scaffold. The mild heat and the boosted Ca 2+ /PO 4 3– release could synergistically enhance the bone regeneration ability both in vitro and in vivo . The underlying mechanism was further explored and confirmed to be closely related to the upregulation of HSP 70, by which the MAPK/ERK signaling pathway was activated selectively. The favorable results demonstrate that the 3D-printed PEEK/graphene composite scaffold is promising in the applications of bone defect repair.
研究领域:
生物材料
·
组织工程
·
生物医学工程
·
光热疗法
·
骨再生
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）