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Setosphapyrone C and D accelerate macrophages cholesterol effl ux by promoting LXRa/ABCA1 pathway
Ting Li,Jiayu Yin,Yubin Ji,Ping Lin,Yanjie Li,Zixun Yang,Shumei Hu,Jin Wang,Baihui Zhang,Saloni Koshti,Junfeng Wang,Chenfeng Ji,Shoudong Guo 대한약학회 2020 Archives of Pharmacal Research Vol.43 No.8
LXRα agonists have attracted signifi cant attentiondue to their potential biological activities on promotingcholesterol effl ux. This study was designed to investigatewhether setosphapyrone C and D have potential lipid-loweringcapacity and the underlying mechanisms in vitro. Ourdata showed that setosphapyrone C and D had weak cytotoxicitycompared to the liver X receptor α (LXRα) agonistT0901317. In RAW 264.7 macrophages, setosphapyroneC and D signifi cantly enhanced [ 3 H]-cholesterol effl ux by~ 21.3% and 32.4%, respectively; furthermore, setosphapyroneC and D enhanced the protein levels of ATP-bindingcassette transporter (ABC) A1 and LXRα by 58% and 69%,and 60% and 70% (8 μM), respectively; however, they had noeff ect on the protein levels of ABCG1 and scavenger receptorB type 1; additionally, they had minor eff ect on the mRNAexpression of lipogenic genes. Of note, setosphapyrone C and D signifi cantly enhanced LXRα/ABCA1pathway inmice primary macrophages. In BRL cells, setosphapyroneC and D signifi cantly improved the protein levels of ABCA1and ABCG1; setosphapyrone D signifi cantly enhanced theprotein expression of low-density lipoprotein. Collectively,setosphapyrone C and D with weak cytotoxicity exhibitedeff ective lipid-lowering eff ect via enhancing LXRα/ABCpathways. Setosphapyrones possess potential applicationfor the treatment of hyperlipidemic diseases.
Yin Hu,Hai-Xia Ma,Jun-Feng Li,Rong Gao,Ji-Rong Song 대한화학회 2010 Bulletin of the Korean Chemical Society Vol.31 No.10
Seven fully optimized geometries of 3,6-dihydrazino-1,2,4,5-tetrazine (DHT) dimers have been obtained with density functional theory (DFT) method at the B3LYP/6-311++G** level. The intermolecular interaction energy was calculated with zero point energy (ZPE) correction and basis set superposition error (BSSE) correction. The greatest corrected intermolecular interaction energy of the dimers is ‒23.69 kJ·mol‒1. Natural bond orbital (NBO) analysis is performed to reveal the origin of the interaction. Based on the vibrational analysis, the changes of thermodynamic properties from the monomers to dimer with the temperature ranging from 200.0 K to 800.0 K have been obtained using the statistical thermodynamic method. It was found that the hydrogen bonds dominantly contribute to the dimers,while the binding energies are not only determined by hydrogen bonding. The dimerization process can not occur spontaneously at given temperatures.
Yin Yang,Qian Li,Qi-Hua He,Ji-Sheng Han,Li Su,You Wan 생화학분자생물학회 2018 Experimental and molecular medicine Vol.50 No.-
Activation of the cholecystokinin type B receptor (CCKBR) by cholecystokinin octapeptide (CCK-8) inhibits opioid analgesia. Chronic opiate treatment leads to an increase in the CCK-8 concentration and thus enhances the antagonism of CCK-8 against opioid analgesia; the underlying molecular mechanisms remain of great interest. In the present study, we validated the colocalization of the μ-opioid receptor (MOR) and CCKBR in pain signal transmissionrelated spinal cord dorsal horn and dorsal root ganglion neurons of rats. Co-immunoprecipitation (Co-IP) and fluorescence lifetime-imaging-microscopy-based fluorescence resonance energy transfer (FLIM-FRET) assays showed that MOR heteromerized with CCKBR directly in transfected HEK293 cells. Combined with MOR mutant construction, the third transmembrane domain of MOR (TM3MOR) was demonstrated to participate in heteromerization with CCKBR. Receptor ligand binding, ERK phosphorylation and cAMP assays showed that MOR heteromerization with CCKBR weakened the activity of MOR. A cell-penetrating interfering peptide consisting of TM3MOR and TAT (a transactivator of HIV-1) sequences from the N terminal to the C terminal disrupted the MOR–CCKBR interaction and restored the activity of MOR in transfected HEK293 cells. Furthermore, intrathecal application of the TM3MOR-TAT peptide alleviated CCK-8-injection-induced antagonism to morphine analgesia in rats. These results suggest a new molecular mechanism for CCK-8 antagonism to opioid analgesia in terms of G-protein-coupled receptor (GPCR) interaction through direct heteromerization. Our study may provide a potential strategy for pain management with opioid analgesics.
Li, Wei,Zheng, Chang-Ji,Sun, Liang-Peng,Song, Ming-Xia,Wu, Yan,Li, Yin-Jing,Liu, Yi,Piao, Hu-Ri 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.7
A series of arylhydrazone derivatives bearing a rhodanine moiety have been synthesized, characterized, and evaluated as antibacterial agents. Some of these compounds showed potent antibacterial activities against several different strains of Gram-positive bacteria, including multidrug-resistant clinical isolates. Of the compounds tested, IIk and IIIk were identified as the most effective, with minimum inhibitory concentration values of $2-4{\mu}g/mL$ against multidrug-resistant Gram-positive organisms, including methicillin-resistant and quinolone-resistant Staphylococcus aureus. None of the compounds exhibited any activity against the Gram-negative bacteria Escherichia coli 1356 at $64{\mu}g/mL$.
Chronic Hepatitis B Virus Infection and Risk of Pancreatic Cancer: A Meta-analysis
Li, Lei,Wu, Bo,Yang, Li-Bo,Yin, Guan-Cheng,Liu, Ji-Yong Asian Pacific Journal of Cancer Prevention 2013 Asian Pacific journal of cancer prevention Vol.14 No.1
Objectives: A number of studies have shown that chronic hepatitis B virus infection is implicated in susceptibility to pancreatic cancer. However, the results are still controversial. This meta-analysis aimed to quantitatively assess the relationship between chronic hepatitis B virus infection and incidence of pancreatic cancer of cohort and case-control studies. Methods: A literature search was performed for entries from 1990 to 2012 using PUBMED and EMBASE. Studies were included if they reported odds ratios (ORs) and corresponding 95% CIs of pancreatic cancer with respect to the infection of hepatitis B virus. Results: Eight studies met the inclusion criteria, which included five case-control studies and three cohort studies. Compared with individuals who have not infection of hepatitis B virus, the pooled OR of pancreatic cancer was 1.403 (95%CI: 1.139-1.729, P=0.001) for patients with hepatitis B virus infection. Sub-group analysis by study design showed that the summary OR was 1.43 (95%CI: 1.06-1.94, P=0.021) when pooling case-control studies and 1.31 (95%CI: 1.00-1.72, P=0.05) when pooling cohort studies. Conclusion: Findings from this meta-analysis suggest that chronic hepatitis B virus infection may increase the risk of pancreatic cancer. This relationship needs to be confirmed by further follow-up studies.
이백수,윤길봉,한천수 대한건축학회 2001 대한건축학회 학술발표대회 논문집 - 계획계/구조계 Vol.21 No.1
In this paper, prescription on the architectural standard specifications between China(CASS) and Korea(KASS) are compared focused on the part of transportation, placing, compacting and curing. According to the research, there are a lot of differences between KASS and CASS. In CASS, time limitation from discharging concrete to completing placement of concrete, transportation, placing and continuous placing time limit are provided in accordance with strength level such as below C30 and above C30. There are no provisions related to special purpose concrete in CASS.