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Wang Z.,Chonnam National University | Liu Z.,Wenzhou Medical College | Liu Z.,Wenzhou Undersun Biotechnology Co. | Lee W.,Korea Institute of Science and Technology | And 3 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2014

A series of novel 5-(substituted benzylidene)thiazolidine-2,4-dione derivatives was designed, and synthesized based on our previous studies. Also their activities were evaluated as competitive inhibitors of protein tyrosine phosphatase 1B (PTP1B). Compounds 6d-6g, 7b, 7c, 7e, 7j, 7k, 7m, 14b and 14e-14f showed potent inhibitory effects against PTP1B, and compound 7e, the most potent among the series, had an IC50 of 4.6 μM. Also a Surflex-Dock docking model of 7e was studied. Compound 7e showed a negative binding energy of -7.35 kcal/mol and a high affinity to PTP1B residues (Gly220, Ala217, Arg221, Asp181, Ser216, Cys215, Phe182, Gln262 and Ile219) in the active sites, indicating that it may stabilize the open form and generate tighter binding to the catalytic sites of PTP1B. © 2014 Elsevier Ltd. All rights reserved.

Cong W.,Wenzhou Medical College | You W.,Wenzhou Medical College | Chen M.,Wenzhou Medical College | Ling J.,Wenzhou Medical College | And 6 more authors.
Analyst | Year: 2012

We report here a sensitive and environmentally benign technique for the visualization of DNA by using eosin Y, which appeared as a transparent and colorless band under the opaque gel matrix background. As low as 0.2-0.6 ng of DNA can be visualized within 1 h, similar to that of the most commonly used ethidium bromide stain. Furthermore, the mechanism of the newly developed method was also described. According to the results, it can be concluded that the complex between DNA and eosin Y is mainly formed by the function of groove binding, but not intercalate itself into the double helix structure of DNA. © 2012 The Royal Society of Chemistry.

Liu Z.,Wenzhou University | Liu Z.,Wenzhou Undersun Biotechnology Co. | Tang L.,Wenzhou University | Zou P.,Nanjing University of Science and Technology | And 8 more authors.
European Journal of Medicinal Chemistry | Year: 2014

Curcumin has been shown to possess anti-inflammatory activities but has been limited for its low stability and poor bioavailability. We have previously reported four series of 5-carbon linker-containing mono-carbonyl analogs of curcumin (MACs). In continuation of our ongoing research, we designed and synthesized 33 novel allylated or prenylated MACs here, and evaluated their anti-inflammatory effects in RAW 264.7 macrophages. A majority of them effectively inhibited the LPS-induced expression of TNF-α and IL-6, especially IL-6. The preliminary SAR and quantitative SAR analysis were conducted. Compound 14q is the most potent analog among them, and exhibits significant protection against LPS-induced death in septic mice. Together, these data present a series of new analogs of curcumin as promising anti-inflammatory agents. © 2013 Elsevier Masson SAS. All rights reserved.

Zhu Z.-X.,Wenzhou Medical College | Cong W.-T.,Wenzhou Medical College | Zhou X.,Wenzhou Medical College | Chen M.,Wenzhou Medical College | And 5 more authors.
Analytical Biochemistry | Year: 2012

A sensitive and simple technique for the negative detection of lipopolysaccharides (LPSs) following polyacrylamide gel electrophoresis (PAGE) using eosin B (EB) was developed. After electrophoresis, gels were fixed, stained, and developed within 30 min to achieve transparent and colorless LPS bands under opaque gel matrix background. As low as 20 to 40 ng of total LPSs could be detected, which is 4-fold more sensitive than those of the widely used silver stain developed by Fomsgaard and coworkers and imidazole-zinc (IZ) negative stain. For its sensitivity and brevity, this stain may be a practical method for LPS determination in the routine laboratory. © 2012 Elsevier Inc. All rights reserved.

Zhu Z.-X.,Wenzhou Medical College | Cong W.-T.,Wenzhou Medical College | Zhang P.-H.,Wenzhou Medical College | Ma W.-D.,Wenzhou Medical College | And 6 more authors.
Electrophoresis | Year: 2010

A sensitive and easy technique has been developed for the negative detection of DNA following PAGE using eosin Y. After electrophoresis, gels are fixed and stained within 40 min to provide a detection limit of 0.1-0.2 ng of single DNA band, which appears as transparent and colorless under the opaque gel matrix background. The sensitivity of the new stain is fourfold better than zinc-imidazole negative and ethidium bromide stains. Furthermore, the newly developed staining method has been successfully applied to RNA visualization in polyacrylamide gels. In addition, the inclusion of inorganic salts in staining solution was also investigated, which has great effect on the staining efficiency. Copyright © 2010 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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