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Wen C.,Fuzhou University | Zhan X.,Fuzhou University | Huang X.,Fuzhou University | Xu F.,Fuzhou University | And 2 more authors.
Surface and Coatings Technology | Year: 2017

A biodegradable hydroxyapatite/graphene oxide bio-composite (HA/GO) coating has been fabricated on magnesium (Mg) alloy by a convenient one-step method of micro-arc oxidation (MAO) for biodegradable implants. The microstructure and phase constituents of the obtained powders and coatings were characterized by XRD, SEM, TEM, FT-IR, XPS and the corrosion resistance in vitro has been investigated by electrochemical measurements in simulated body fluid (SBF). The results suggested that HA/GO powder has been successfully prepared and filled into the discharging pores of the coating during MAO process. The electrochemical measurements in SBF indicated that the corrosion current of Mg substrate has been significantly decreased by the HA/GO coating. Furthermore the EIS measurement suggested that the HA/GO coating more effectively inhibited the Mg substrate from corrosion compared to pure MAO coating. These results suggested that HA/GO coating on Mg alloy could be a promising candidate for biomedical application. © 2017 Elsevier B.V.


Huang W.,Fujian Medical University | Huang W.,Fujian Institute of Microbiology | Ye M.,Fujian Medical University | Ye M.,Fuijan Provincial Key Laboratory of Natural Medicine Pharmacology | And 7 more authors.
Molecular Cancer | Year: 2014

Background: Heat shock protein 90 (Hsp90) is a promising therapeutic target and inhibition of Hsp90 will presumably result in suppression of multiple signaling pathways. FW-04-806, a bis-oxazolyl macrolide compound extracted from China-native Streptomyces FIM-04-806, was reported to be identical in structure to the polyketide Conglobatin.Methods: We adopted the methods of chemproteomics, computational docking, immunoprecipitation, siRNA gene knock down, Quantitative Real-time PCR and xenograft models on the research of FW-04-806 antitumor mechanism, through the HER2-overexpressing breast cancer SKBR3 and HER2-underexpressing breast cancer MCF-7 cell line.Results: We have verified the direct binding of FW-04-806 to the N-terminal domain of Hsp90 and found that FW-04-806 inhibits Hsp90/cell division cycle protein 37 (Cdc37) chaperone/co-chaperone interactions, but does not affect ATP-binding capability of Hsp90, thereby leading to the degradation of multiple Hsp90 client proteins via the proteasome pathway. In breast cancer cell lines, FW-04-806 inhibits cell proliferation, caused G2/M cell cycle arrest, induced apoptosis, and downregulated Hsp90 client proteins HER2, Akt, Raf-1 and their phosphorylated forms (p-HER2, p-Akt) in a dose and time-dependent manner. Importantly, FW-04-806 displays a better anti-tumor effect in HER2-overexpressed SKBR3 tumor xenograft model than in HER2-underexpressed MCF-7 model. The result is consistent with cell proliferation assay and in vitro apoptosis assay applied for SKBR-3 and MCF-7. Furthermore, FW-04-806 has a favorable toxicity profile.Conclusions: As a novel Hsp90 inhibitor, FW-04-806 binds to the N-terminal of Hsp90 and inhibits Hsp90/Cdc37 interaction, resulting in the disassociation of Hsp90/Cdc37/client complexes and the degradation of Hsp90 client proteins. FW-04-806 displays promising antitumor activity against breast cancer cells both in vitro and in vivo, especially for HER2-overexpressed breast cancer cells. © 2014 Huang et al.; licensee BioMed Central Ltd.


Huang W.,Fujian Medical University | Wu Q.-D.,Fujian Medical University | Zhang M.,Fujian Medical University | Kong Y.-L.,Fujian Medical University | And 7 more authors.
Cancer Letters | Year: 2015

Human epidermal growth factor receptor 2 (HER2), a member of the HER family of tyrosine kinases and a binding partner of Heat shock protein 90 (Hsp90), is found amplifies in approximately 25% breast cancers. Treatment of HER2+ breast cancers has been greatly improved in recent years, but the accompanying upregulation of HER3 induced by HER2 blockade has subdued the therapeutic effect. FW-04-806, a novel Hsp90 N-terminal inhibitor that disassociates the Hsp90/Cdc37/client complex and degrades Hsp90 clients, was studied alone or in combination with the EGFR/HER2 tyrosine kinase inhibitor lapatinib in HER2+ breast cancer cells. We found that FW-04-806 alone or with laptinib inhibits cell proliferation, induces cell apoptosis and reduces the total and activated HER3 levels in these cells, while lapatinib has been reported to increase HER3 expression followed HER2 inhibition. The combination of FW-04-806 and lapatinib showed synergistic reduction of HER2 expression and the downstream PI3K/Akt and Ras/MEK/ERK pathways, enhanced suppression of Akt-mediated FOXO3a inactivation and augmented antitumor efficacy on SKBR3 xenografts with a favorable toxicity profile, suggesting its viability as a combination therapy for clinical studies in HER2+ breast cancer patients. © 2014 Elsevier Ireland Ltd.


Zheng Y.,Fujian Medical University | Huang Z.,Fujian Medical University | Huang Z.,Fujian Academy of Medical science | Zhao C.,Fujian Medical University | And 3 more authors.
Microchimica Acta | Year: 2013

We have developed a facile method for the preparation of a gold electrode modified with a flower-like gold nanostructure using potentiostatic electrodeposition. Its formation, morphology, and electrochemical properties were studied by scanning electron microscopy and cyclic voltammetry. The resulting nanostructures possess rough and enlarged surface areas and enable fast electron transfer in the selective and sensitive detection of ascorbic acid (AA) and dopamine (DA) in phosphate-buffered saline without disturbance by common interferents. The differential pulse voltammetry anodic peak currents at approximately -0.03 V and 0.16 V are strongly enhanced in the presence of AA and DA, respectively. The electrode responds linearly to AA in the concentration range from 60 μM to 500 μM, with a limit of detection at 10 μM. The respective data for DA are 1 μM to 150 μM, and the limit of detection is 0.2 μM. © 2013 Springer-Verlag Wien.


PubMed | Fuzhou University and Fujian Institute of Microbiology
Type: Journal Article | Journal: Bioprocess and biosystems engineering | Year: 2016

The objective of this study was to investigate the fundamental question of biofilm formation. First, a drum biofilm reactor was introduced. The drums were coated with three porous substrates (cotton rope, canvas, and spandex), respectively. The relationships among the substrate, extracellular polymeric substances (EPS), and adhesion ratio were analyzed. Second, a plate biofilm reactor (PBR) was applied by replacing the drum with multiple parallel vertical plates to increase the surface area. The plates were coated with porous substrates on each side, and the nutrients were delivered to the cells by diffusion. The influence of nitrogen source and concentration on compositions of EPS and biofilm formation was analyzed using PBR under sunlight. The results indicated that both substrate and nitrogen were critical on the EPS compositions and biofilm formation. Under the optimal condition (glycine with concentration of 1gl(-1) and substrate of canvas), the maximum biofilm productivity of 54.46gm(-2) d(-1) with adhesion ratio of 84.4% was achieved.


PubMed | Fuzhou University and Fujian Institute of Microbiology
Type: Journal Article | Journal: Journal of bioscience and bioengineering | Year: 2016

The objective of this study was to investigate the effects of culture conditions, including carbon sources and concentration, culture period, and precondition time, on the production of extracellular polymeric substances (EPS) and its influence on microalgal flocculation. EPS are natural high molecule polymer, excreted by microalgae themselves. EPS can accelerate the formation of microbial aggregates through binding cells closely. Organic carbon sources, such as glucose, glycerol, acetate and glycine were compared to select the optimal source to stimulate EPS accumulation. Subsequently, the effect of culture period, glycine dose and precondition time on EPS production and its influence on biomass growth and flocculation efficiency were investigated. As the main parts of EPS, tightly bound EPS were found positively related to suspended solids concentration. However, the loosely bound EPS may weaken the floc structure, leading to poor water-cells separation. Under the optimal condition with culture period of 16 days, glycine dose of 0.5 g l(-1) and precondition time of 5 days, the biomass concentration increased from 1.49 to 2 g l(-1), and the maximum suspended solids concentration of 7.06% with biomass recovery rate of 70.6% was achieved.


Jiang H.,Fujian Institute of Microbiology
Wei sheng wu xue bao = Acta microbiologica Sinica | Year: 2010

OBJECTIVE: The aim of this study was to investigate actinobacterial diversity in Chilean marine sediments. METHODS: Actinobacterial diversity in these sediments was investigated by selective isolation method, culture-independent method and phylogenetic analysis based on 16S rRNA gene sequences. Six selective media were used to isolate actinomycetes from sediment samples. The primers for the class Actinobacteria were used for Actinobacterial 16S rRNA gene amplification and then a clone library was constructed for the sediment sample btt. Twenty-two strains with different culture characteristics and 59 clones from sample btt were selected for 16S rRNA gene sequences analysis. To determine requirement for seawater each strain was grown on oatmeal agar prepared with deionized water and with seawater, respectively. Strains were screened for antibiotic activity against bacteria and fungi. RESULTS: In total 328 actinomycetes were obtained. Twenty-two strains which were selected belonged to Streptomyces, Micromonospora, Polymorphospora, Aeromicrobium and Brachybacterium. Fifty-nine clones (40 OTUs) were sequenced, and 60% OTUs belonged to Actinobacteridae, Acidimicrobidae and Rubrobacteridae. The other 40% OTUs, which formed several distinct clades in phylogenetic tree among phylum Actinobacteria may represent new taxonomical groups. 50% of the 47 sea water dependant strains and nineteen strains out of the above 22 strains exhibited antimicrobial activity. CONCLUSION: There was abundant actinobacterial diversity in the marine sediments of Chile, and the result implied that there were large numbers of unknown actinobacterial groups in the sediments. Actinomycetes from Chilean marine sediments had the potential of producing bioactive secondary metabolites.


PubMed | Hangzhou Huadong Medicine Group Pharmaceutical Research Institute Co. and Fujian Institute of Microbiology
Type: Journal Article | Journal: Archiv der Pharmazie | Year: 2016

Rapamycin, a potent antifungal antibiotic, was approved as immunosuppressant, and lately its derivatives have been developed into mTOR targeting anticancer drugs. Structure modification was performed at the C-42 position of rapamycin, and a novel series of rapamycin triazole hybrids (4a-d, 5a-e, 8a-e, and 9a-e) was facilely synthesized via Huisgens reaction. The anticancer activity of these compounds was evaluated against the Caski, H1299, MGC-803, and H460 human cancer cell lines. Some of the derivatives (8a-e, 9a-e) appeared to have stronger activity than that of rapamycin; however, 4a-d and 5a-e failed to show potential anticancer activity. Compound 9e with a (2,4-dichlorophenylamino)methyl moiety on the triazole ring was the most active anticancer compound, which showed IC50 values of 6.05 (Caski), 7.89 (H1299), 25.88 (MGC-803), and 8.60M (H460). In addition, research on the mechanism showed that 9e was able to cause cell morphological changes and to induce apoptosis in the Caski cell line. Most importantly, 9e can decrease the phosphorylation of mTOR and of its downstream key proteins, S6 and P70S6K1, indicating that 9e can effectively inhibit the mTOR signaling pathway. Thus, it may have the potential to become a new mTOR inhibitor against various cancers.


PubMed | Fujian Institute of Microbiology
Type: Journal Article | Journal: Chemical & pharmaceutical bulletin | Year: 2016

The immunosuppressant drug rapamycin, was firstly identified as a mammalian target of rapamycin (mTOR) allosteric inhibitor, and its derivatives have been successfully developed as anti-cancer drugs. Therefore, finding rapamycin derivatives with better anti-cancer activity has been proved to be an effective way to discover new targeted anti-cancer drugs. In this paper, structure modification was performed at the C-43 position of rapamycin using bioisosterism and a hybrid approach: a series of novel rapamycin-benzothiazole hybrids 4a-e, 5a-c, and 9a, b have been designed, synthesized and evaluated for their anti-cancer activity against Caski, CNE-2, SGC-7901, PC-3, SK-NEP-1 and A-375 human cancer cell lines. Some of these compounds (4a-e, 9a, b) displayed good to excellent potency against the Caski and SK-NEP-1 cell line as compared with rapamycin. Compound 9b as the most active compound showed IC50 values of 8.3 (Caski) and 9.6M (SK-NEP-1), respectively. In addition, research on the mechanism showed that 9b was able to cause G1 phase arrest and induce apoptosis in the Caski cell line. Most importantly, it significantly decreased the phosphorylation of S6 ribosomal protein, p70S6K1 and 4EBP1, which indicated that 9b inhibited the cancer cell growth by blocking the mTOR pathway and may have the potential to become a new mTOR inhibitor.


PubMed | Fujian Institute of Microbiology and Shenyang Pharmaceutical University
Type: | Journal: Archiv der Pharmazie | Year: 2017

A series of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing (E)-3-hydrosulfonylacrylamido or 1H-imidazole-4-carboxamido moieties were designed, synthesized and evaluated for their cytotoxicity against A549, MKN-45, and HT-29 cancer cell lines in vitro. All the target compounds showed moderate to significant cytotoxic activity against the tested cells with IC

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