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Xiong, Shang-Ling,Lim, Gyu Tae,Yin, Shang-Jun,Lee, Jinhyuk,Si, Yue-Xiu,Yang, Jun-Mo,Park, Yong-Doo,Qian, Guo-Ying Elsevier 2019 INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES Vol.121 No.-
<P><B>Abstract</B></P> <P>Pyrogallol is naturally found in aquatic plant and has been proposed as a substrate of tyrosinase. In this study, we evaluated the dual effect of pyrogallol on tyrosinase as an inhibitor in the presence of L‑DOPA simultaneously via integrating methods of enzyme kinetics and computational molecular dynamics (MD) simulations. Pyrogallol was found to be a reversible inhibitor of tyrosinase in the presence of L‑DOPA and its induced mechanism was the parabolic non-competitive inhibition type (<I>IC</I> <SUB>50</SUB> = 0.772 ± 0.003 mM and <I>K</I> <SUB>i</SUB> = 0.529 ± 0.022 mM). Kinetic measurements by real-time interval assay showed that pyrogallol induced rapid inactivation process composing with slight activations at the low dose. Spectrofluorimetry studies showed that pyrogallol mainly induced regional changes in the active site of tyrosinase accompanying with hydrophobic disruption at high dose. The computational MD simulations further revealed that pyrogallol could interact with several residues near the tyrosinase active site pocket such as HIS61, HIS85, HIS259, ASN260, HIS263, VAL283, and ALA296. Our study provides insight into the mechanism by which hydroxyl group composing pyrogallol inhibit tyrosinase and pyrogallol is a potential natural anti-pigmentation agent.</P>
Piao, Shang Guo,Bae, Soo Kyung,Lim, Sun Woo,Song, Ji-Hyun,Chung, Byung Ha,Choi, Bum Soon,Yang, Chul Woo Lippincott Williams Wilkins, Inc. 2012 Transplantation Vol.93 No.4
BACKGROUND.: It is known that sirolimus (SRL) aggravates cyclosporine A (CsA)-induced nephrotoxicity and pancreatic injury, but the influence of everolimus (EVR) on CsA-induced organ injury is undetermined. METHODS.: Rats were treated with CsA (15 mg/kg) and EVR or SRL (0.3 mg/kg) subcutaneously for 4 weeks. The influences of EVR or SRL on CsA-induced nephrotoxicity and pancreatic islet dysfunction were compared, and drug interactions between CsA and EVR or SRL were evaluated at blood and tissue levels. RESULTS.: Treatment with EVR or SRL alone did not cause severe pancreatic dysfunction and renal injury, but when combined with CsA they aggravated CsA-induced pancreatic and renal injury. Drug interactions between CsA and EVR or SRL differed at the tissue level. Combined treatment with CsA and SRL significantly increased the CsA or SRL levels in kidney and pancreas compared with CsA or SRL alone. However, combined treatment with CsA and EVR did not increase CsA or EVR levels in kidney and pancreas. CONCLUSIONS.: Both EVR and SRL aggravate CsA-induced organ injury, but the pharmacologic interaction between EVR and CsA at the tissue level is less than that between CsA and SRL. This finding provides better understanding of the difference between EVR and SRL when combined with CsA treatment.
Influence of the MACC1 Gene on Sensitivity to Chemotherapy in Human U251 Glioblastoma Cells
Shang, Chao,Hong, Yang,Guo, Yan,Liu, Yun-Hui,Xue, Yi-Xue Asian Pacific Journal of Cancer Prevention 2015 Asian Pacific journal of cancer prevention Vol.16 No.1
Background: This study was conducted to determine the influence of MACC1 expression on chemotherapy sensitivity in human U251 glioblastoma cells. Materials and Methods: Expression of the MACC1 gene in 49 cases of human brain glioma was determined by quantitative real-time PCR. Silencing effects of RNA interference on MACC1 was detected by Western-blotting. Flow cytometry methods and methyl thiazolyl tetrazolium assay (MTT) were used to determine the apoptosis and growth inhibitory rates of the U251 cells with MACC1 silencing. before and after treatment with cisplatin (DDP). Results: MACC1 mRNA in gliomas was up-regulated remarkably, to 158.8% of that in peri-cancerous tissues (P<0.05). The siRNA-MACC1 could inhibit the expression of MACC1 protein significantly (p<0.05), associated with an increase in apoptosis rate from 2.57% to 5.39% in U251 cells and elevation of the growth inhibitory rate from 1.5% to 17.8% (p<0.05 for both). After treatment with DDP at various concentrations (1, 3, $5{\mu}g/ml$), compared with control U251 cells, the apoptosis rate of MACC1-silenced U251 cells rose from 8.41%, 13.2% and 19.5% to 12.8%, 17.8% and 25.8%; the growth inhibitory rate increased from 16.2%, 19.3% and 24.5% to 23.7%, 28.4% and 36.3%. Conclusions: There is a notable relationship between over-expression of MACC1 and the characteristics of glioma cells. Silencing of MACC1 was found to enhance the apoptosis and growth inhibitory rates of U251 glioma cells, and thereby increase their sensitivity to DDP chemotherapy.
Characterization and Mapping of the Bovine FBP1 Gene
Guo, H.,Liu, W-S.,Takasuga, A.,Eyer, K.,Landrito, E.,Xu, Shang-zhong,Gao, X.,Ren, H-Y. Asian Australasian Association of Animal Productio 2007 Animal Bioscience Vol.20 No.9
Fructose-1,6-bisphosphatase (FBP1) is a key regulatory enzyme of gluconeogenesis that catalyzes the hydrolysis of fructose-1,6-bisphosphate to generate fructose-6-phosphate and inorganic phosphate. Deficiency of fructose-1, 6-bisphosphatase is associated with fasting hypoglycemia and metabolic acidosis. The enzyme has been shown to occur in bacteria, fungi, plants and animals. The bovine FBP1 gene was cloned and characterized in this study. The full length (1,241 bp) FBP1 mRNA contained an open reading frame (ORF) encoding a protein of 338 amino acids, a 63 bp 5' untranslated region (UTR) and a 131 bp 3' UTR. The bovine FBP1 gene was 89%, 85%, 82%, 82% and 74% identical to the orthologs of pig, human, mouse, rat and zebra fish at mRNA level, and 97%, 96%, 94%, 93% and 91% identical at the protein level, respectively. This gene was broadly expressed in cattle with the highest level in testis, and the lowest level in heart. An intronic single nucleotide polymorphism (SNP) (A/G) was identified in the $5^{th}$ intron of the bovine FBP1 gene. Genotyping of 133 animals from four beef breeds revealed that the average frequency for allele A (A-base) was 0.7897 (0.7069-0.9107), while 0.2103 (0.0893-0.2931) for allele B (G-base). Our preliminary association study indicated that this SNP is significantly associated with traits of Average Daily Feed Intake (ADFI) and Carcass Length (CL) (p<0.01). In addition, the FBP1 gene was assigned on BTA8 by a hybrid radiation (RH) mapping method.
Xylaroisopimaranin A, a New Isopimarane Derivative from an Endophytic Fungus Xylaralyce sp.
Shang-Song Bao,Hui-Hui Liu,Xue-Qing Zhang,Cheng-Xiong Liu,Xiao-Cong Li,Zhi-Yong Guo 한국생약학회 2019 Natural Product Sciences Vol.25 No.3
Five secondary metabolites, including a new isopimarane derivative xylaroisopimaranin A (1), were isolated from the endophytic fungus Xylaralyce sp. (HM-1), and their structures were elucidated by 1D, 2D NMR, MS and CD spectra. Their bioactivities were performed to antibacterial, Hep G2 cells cytotoxicity and brine shrimp inhibition. The biological evaluation results showed that the xylaroisopimaranin A (1), xylabisboein B (2), griseofulvin (3) , 5-methylmellein (4) and mellein-5-carboxlic acid (5) displayed no significant Hep G2 cells cytotoxicity and antibacterial acitivity, but they inhibited the brine shrimp with IC50 from 0.5 to 25 μmol/mL.
Guo, Hong-Yan,Xing, Yue,Sun, Yu-Qiao,Liu, Can,Xu, Qian,Shang, Fan-Fan,Zhang, Run-Hui,Jin, Xue-Jun,Chen, Fener,Lee, Jung Joon,Kang, Dongzhou,Shen, Qing-Kun,Quan, Zhe-Shan The Korean Society of Ginseng 2022 Journal of Ginseng Research Vol.46 No.6
Background: Ginseng possesses antitumor effects, and ginsenosides are considered to be one of its main active chemical components. Ginsenosides can further be hydrolyzed to generate secondary saponins, and 20(R)-panaxotriol is an important sapogenin of ginsenosides. We aimed to synthesize a new ginsengenin derivative from 20(R)-panaxotriol and investigate its antitumor activity in vivo and in vitro. Methods: Here, 20(R)-panaxotriol was selected as a precursor and was modified into its derivatives. The new products were characterized by <sup>1</sup>H-NMR, <sup>13</sup>C-NMR and HR-MS and evaluated by molecular docking, MTT, luciferase reporter assay, western blotting, immunofluorescent staining, colony formation assay, EdU labeling and immunofluorescence, apoptosis assay, cells migration assay, transwell assay and in vivo antitumor activity assay. Results: The derivative with the best antitumor activity was identified as 6,12-dihydroxy-4,4,8,10,14-pentamethyl-17-(2,6,6-trimethyltetrahydro-2H-pyran-2-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl(tert-butoxycarbonyl)glycinate (A11). The focus of this research was on the antitumor activity of the derivatives. The efficacy of the derivative A11 (IC<sub>50</sub> < 0.3 µM) was more than 100 times higher than that of 20(R)- panaxotriol (IC<sub>50</sub> > 30 µM). In addition, A11 inhibited the protein expression and nuclear accumulation of the hypoxia-inducible factor HIF-1α in HeLa cells under hypoxic conditions in a dose-dependent manner. Moreover, A11 dose-dependently inhibited the proliferation, migration, and invasion of HeLa cells, while promoting their apoptosis. Notably, the inhibition by A11 was more significant than that by 20(R)-panaxotriol (p < 0.01) in vivo. Conclusion: To our knowledge, this is the first study to report the production of derivative A11 from 20(R)-panaxotriol and its superior antitumor activity compared to its precursor. Moreover, derivative A11 can be used to further study and develop novel antitumor drugs.
Design and theoretical analysis of a sliding valve distribution radial piston pump
Guo Tong,Zhao Shengdun,Yu Yanghuiwen,Shang Peng 대한기계학회 2016 JOURNAL OF MECHANICAL SCIENCE AND TECHNOLOGY Vol.30 No.1
A Sliding valve distribution radial piston pump (SVDRPP) is presented. In this pump, a new distribution method that uses slidingvalves to distribute oil for the piston chambers is developed. With this design, the disadvantages brought by the distribution shaft and thecheck valves (traditional distribution mechanisms), such as the poor stress state of the shaft and the energy waste for opening the checkvalves, are expected to be eliminated. In addition, a method of using pressure oil to accomplish the returning stroke of the piston is alsoproposed, which could be used to replace the usage of springs along with their shortcomings. A pump with five pistons is designed as anexample to elaborate the structure and the working principle of SVDRPP. Furthermore, the flow characteristics of SVDRPP are studied,and the formulas of the displacement, the average flow rate and the instantaneous flow rate are deduced.
Jasmine tea extract enhances human retinal pigment epithelial cells survival after UVB irradiation
Shang Hu,Guo Yaling,Wu Liangyu,Lin Jinke 한국응용생명화학회 2023 Applied Biological Chemistry (Appl Biol Chem) Vol.66 No.-
To examine the protecting effect of jasmine tea extract (JTE) against ultraviolet B (UVB) induced damage on human retinal pigment epithelial (RPE) cells, the RPE cells were subjected to UVB exposure and sequential JTE administration. The cell viability, intracellular reactive oxygen species (ROS), and apoptosis were determined by MTT, 2ʹ,7ʹ-dichlorodihydrofluorescein diacetate and flow cytometer assays, respectively. Further, the cells treated with UVB irradiation and sequential JTE administration were subjected to RNA-sequencing analysis in order to identify genes and pathways involved in the UVB-induced damage and JTE protecting mechanisms. The results showed that JTE effectively attenuated the UVB-induced cell injury by reducing the excessive intracellular ROS generation, and inhibiting the expression of apoptotic genes such as Bax, Caspase-3/9. This finding may offer a promising candidate for the prevention of UVB exposure related eye diseases.