TRANSACTIONS OF TIANJIN UNIVERSITY
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2012
·Vol. 18
·期 5
·315-319
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IF 0
Feng Yakai,Chen Chengbin,Zhang Li,Tian Hong,Yuan Wenjie
A series of novel copolymers were successfully synthesized by ring-opening polymerization (ROP) of 3(S)-methyl-morpholine-2,5-dione (MMD) and 5-methyl-5-benzyloxycarbonyl-1,3-dioxan-2-one (MBC) using stannous octoate as catalyst. The copolymers were characterized by means of 1H-NMR and FT-IR spectroscopy. Gel permeation chromatography (GPC) test shows that the average-number relative molecular mass and average-weight relative molecular mass slightly increase with the increase of MBC content in feed. The results of differential scanning calorimetry (DSC) demonstrate that the glass transition temperature of copolymers increases with the increase of MBC content in copolymers. The copolymers of MMD and MBC are amorphous copolymers, as indicated by DSC results, while the homopolymer of MMD is semicrystalline.
研究领域:
高分子化学
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材料科学
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CURRENT ORGANIC SYNTHESIS
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2025
·Vol. 22
·期 5
·614-619
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IF 2.5
Dejun Zhou,Keyang Wang,Yuying Zhang,Xiaoyue Liu,Xiaoxia Mao
BackgroundTimolol maleate is clinically used for the treatment of hypertension, angina pectoris, tachycardia, and glaucoma.ObjectiveThe aim of this study was to enhance the safe use of timolol maleate and investigate a synthesis method for 3-S-timolol, a newly identified impurity in timolol API (Active Pharmaceutical Ingredients).Methods(S)-3-(tert-butylamino)propane-1,2-diol (1) was used as a raw material. 3-S-timolol maleate (7) was synthesized through a five-step reaction. Overall yield was 57.7%, with a purity of 98%.ResultsThe structure of the target compound was confirmed via analysis of its 1H nuclear magnetic resonance, 13C nuclear magnetic resonance, and high-resolution mass spectrometry spectra.ConclusionThe synthesis method was straightforward and yielded a high-purity product suitable for use as a reference in the analysis and identification of timolol maleate-related substances.
研究领域:
药物化学
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分析化学
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药物质控
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有机合成
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杂质研究
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药物代谢
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DOI
PubMed
高影响因子
MOLECULES
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2013
·Vol. 18
·期 4
·4158-4169
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IF 2.428
Luhui Ren,Xue Du,Mengnan Hu,Chaoqun Yan,Taigang Liang,Qingshan Li
An asymmetric synthesis of a series of novel 4-methyl-(3'S,4'S)-cis-khellactone derivatives3a–ois reported for the first time. Their structures were confirmed by1H-NMR,13C-NMR and MS. Their cytotoxic activity was evaluated by the MTT assay against three selected human cancer cell lines: HEPG-2 (human liver carcinoma), SGC-7901 (human gastric carcinoma), LS174T (human colon carcinoma). Some compounds showed high inhibitory activity against these human cancer cell lines. Among them, compound3aexhibited strong cytotoxicity, with IC50values ranging from 8.51 to 29.65 μM. The results showed that 4-methyl-cis-khellactone derivatives withS,Sconfiguration could be a potential antitumor agents.Keywords:4-methyl-(3'S,4'S)-cis-khellactone derivatives;asymmetric synthesis;antitumor activity
研究领域:
药物化学
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肿瘤学
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有机合成化学
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PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2022
·
IF 5.895
Hang-Zhi Zhu,Shan Jiang,Jun-Jie Wu,Xue-Rong Zhou,Peng-Yang Liu,Feng-Hong Huang,Xia Wan
Astaxanthin is a highly value-added keto-carotenoid compound. The astaxanthin 3S,3′S-isomer is more desirable for food additives, cosmetics, and pharmaceuticals due to health concerns about chemically synthesized counterparts with a mixture of three isomers. Biosynthesis of 3S,3′S-astaxanthin suffers from limited content and productivity. We engineered Yarrowia lipolytica to produce high levels of 3S,3′S-astaxanthin. We first assessed various β-carotene ketolases (CrtW) and β-carotene hydroxylases (CrtZ) from two algae and a plant. HpCrtW and HpCrtZ from Haematococcus pluvialis exhibited the strongest activity in converting β-carotene into astaxanthin in Y. lipolytica. We then fine-tuned the HpCrtW and HpCrtZ transcriptional expression by increasing the rounds of gene integration into the genome and applied a modular enzyme assembly of HpCrtW and HpCrtZ simultaneously. Next, we rescued leucine biosynthesis in the engineered Y. lipolytica, leading to a five-fold increase in biomass. The astaxanthin production achieved from these strategies was 3.3 g/L or 41.3 mg/g dry cell weight under fed-batch conditions, which is the highest level reported in microbial chassis to date. This study provides the potential for industrial production of 3S,3′S-astaxanthin, and this strategy empowers us to build a sustainable biorefinery platform for generating other value-added carotenoids in the future.
研究领域:
生物技术
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代谢工程
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微生物生物技术
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PubMed
高影响因子
Drug Design Development and Therapy
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2017
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IF 2.822
Jingrun Chen,Junjie Liu,Dongxiao Cui,Chaoqun Yan,Liqiang Meng,Liqian Sun,Shurong Ban,Rui Ge,Taigang Liang,Qingshan Li
This study deals with the design and synthesis of a series of novel 4-methoxy-substituted and 5-methyl-substituted (3′S,4′S)-(−)-cis-khellactones. The newly synthesized compounds were characterized by 1H nuclear magnetic resonance (NMR), 13C-NMR, mass spectrometry, and elemental analysis. All the derivatives were subjected to in vitro cytotoxicity screening against HEPG-2 (human liver carcinoma), SGC-7901 (human gastric carcinoma), and LS174T (human colon carcinoma), by using the MTT assay. The results revealed that several of the 4-methoxy-substituted compounds exhibited potent cytotoxicity. Among these, compound 12e showed the highest activity against cancer cells which 50% inhibitory concentration (IC50) values were in the range of 6.1–9.2 μM with low toxicity on normal human hepatocyte. Preliminary investigation of possible mechanisms of action of compound 12e against HEPG-2 cells indicated possible induction of apoptosis, as determined by morphological observations and Annexin V/propidium iodide (PI) double staining, in addition to apparent dissipation of mitochondrial membrane potential (MMP), as measured by 5,5′,6,6′-tetrachloro-1,1′,3,3′-tetraethyl-imidacarbocyanine iodide (JC-1) staining in combination with the activation of caspase-9 and caspase-3 by Western blot analysis. Overall, the data suggest that compound 12e may be a promising potential anti-cancer agent that could act primarily by inducing apoptosis through the mitochondria-mediated intrinsic pathway in human hepatoma cells.
研究领域:
药理学
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肿瘤学
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药物化学
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DOI
PubMed
高影响因子
Acta Pharmaceutica Sinica B
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2020
·
IF 7.097
Meng Yuan,Xiaobing Chen,Yitang Sun,Li Jiang,Zhongni Xia,Kaixiong Ye,Hong Jiang,Bo Yang,Meidan Ying,Ji Cao,Qiaojun He
The membrane protein claudin-3 (CLDN3) is critical for the formation and maintenance of tight junction and its high expression has been implicated in dictating malignant progression in various cancers. However, the post-translational modification of CLDN3 and its biological function remains poorly understood. Here, we report that CLDN3 is positively correlated with ovarian cancer progression both in vitro and in vivo. Of interest, CLDN3 undergoes S -palmitoylation on three juxtamembrane cysteine residues, which contribute to the accurate plasma membrane localization and protein stability of CLDN3 . Moreover, the deprivation of S -palmitoylation in CLDN3 significantly abolishes its tumorigenic promotion effect in ovarian cancer cells. By utilizing the co-immunoprecipitation assay, we further identify ZDHHC12 as a CLDN3-targating palmitoyltransferase from 23 ZDHHC family proteins. Furthermore, the knockdown of ZDHHC12 also significantly inhibits CLDN3 accurate membrane localization, protein stability and ovarian cancer cells tumorigenesis . Thus, our work reveals S -palmitoylation as a novel regulatory mechanism that modulates CLDN3 function, which implies that targeting ZDHHC12-mediated CLDN3 S -palmitoylation might be a potential strategy for ovarian cancer therapy.
研究领域:
癌症生物学
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细胞生物学
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分子生物学
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DOI
PubMed
高影响因子
FOOD CHEMISTRY
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2026
·
IF 10.4
Liru Liu,Ping Cheng,Yingxiao Xiao,Sijin Chen,Yiping Zhang,Weizhu Chen,Fengfu Fu,Zhenyu Lin,Yongqiang Dong
(3 S ,3′ S )-astaxanthin ((3 S ,3′ S )-AST) with excellent physiological activity demands accurate chiral-selective detection, yet conventional methods have inherent limitations and SERS technology lacks relevant applications here. In this study, a chiral-selective hydrogel-based SERS chip was prepared by immobilizing aggregated silver nanocages (a-AgNCs) in polyvinyl alcohol (PVA) hydrogel for specific and sensitive (3 S ,3′ S )-AST detection. The hydrogel realized selective adsorption of (3 S ,3′ S )-AST, and a-AgNCs provided strong SERS enhancement via electromagnetic-chemical synergistic effect. The sensing system showed excellent stability (intra/inter-chip RSD < 4.22%, signal loss <5% in 6 weeks), a semi-logarithmic linear response for (3 S ,3′ S )-AST in 0.5–500 ng/g. Practical detection in Haematococcus pluvialis (HP) and Phaffia rhodozyma yeast (PRY) powders confirmed no (3 S ,3′ S )-AST in PRY, and the detected contents in HP samples were consistent with HPLC results. This chip establishes a rapid and reliable chiral-selective detection method for (3 S ,3′ S )-AST, and expands SERS application in chiral analysis of food-related natural products. Hydrogel SERS chips enable direct chiral-selective detection of (3 S ,3′ S )-astaxanthin with high sensitivity and reliable real-sample applicability. Download: Download high-res image (202KB) Download: Download full-size image
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高影响因子
GREEN CHEMISTRY
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2026
·
IF 9.2
Yujie Yuan,Ziyu Yang,Hao Wang,Tong Wu,Xiaoyi Zhang,Lin Chen,Zhaohuan Wei,Rui Wang,C. Venkata Reddy,Jaesool Shim,Hui Tang
Electrocatalytic seawater splitting holds immense promise as a green hydrogen production technology; however, the anodic oxygen evolution reaction (OER) confronts formidable challenges arising from the high concentration of chloride ions (Cl -) and other impurities in seawater. Herein, we develop a facile two-step immersion corrosion strategy to successfully construct a Ni 3 S 2 @FeOOH heterojunction electrocatalyst on nickel foam (NF) tailored for industrial alkaline seawater oxidation. Integrating density functional theory (DFT) calculations and experimental characterizations, we demonstrate that Ni 3 S 2 @FeOOH selectively enriches OH -while repelling Cl -during OER in alkaline seawater electrolytes. Notably, in situ leaching of SO 4 2-from the electrode triggers efficient self-reconstruction, facilitating the generation of high-valence metal active sites. The asfabricated catalyst exhibits remarkable OER performance with a low overpotential of 390.5 mV at an ultrahigh current density of 1000 mA cm -2 in alkaline seawater. Moreover, it maintains exceptional electrochemical stability for over 1000 hours at the industrial current density of 1000 mA cm -2 . This work provides a scalable strategy for constructing self-reconstructing electrocatalysts that promote highvalence metal site formation and efficient Cl -repulsion in alkaline seawater oxidation.
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高影响因子
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