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Mechanical evaluation of polymer microneedles for transdermal drug delivery: In vitro and in vivo
Rui Xuan Liu,Yu Ting He,Ling Liang,Liu Fu Hu,Yue Liu,Rui-xing Yu,Bo Zhi Chen,Yong Cui,Xin Dong Guo 한국공업화학회 2022 Journal of Industrial and Engineering Chemistry Vol.114 No.-
In this study, we reported two types of PMNs based on polylactic acid (PLA) and polyvinyl alcohol (PVA),respectively. Parafilm M film, porcine skin, and rats’ models were operated to evaluate the mechanicalproperties in vitro and in vivo to find optimal parameters for efficient insertion. Insertion depth was measuredusing Digital Force Gauge by changing insertion force and speed, respectively. Results showed thatincreasing the insertion force and speed used for PMNs application led to a significant increase in thedepth of insertion. A force of 18 N under a speed of 330 mm/min was the optimal condition for insertingPMNs array into ParafilmM film and porcine skin. In addition, PLA-MNs exhibited higher robustness andenhanced homogeneity in insertion depth compared with PVA-MNs, but PVA-MNs were able to reachmuch deeper insertion depth. Moreover, Sprague Dawley (SD) rat experiments confirmed the effectivenessof optimal insertion parameters for transdermal drug delivery. This study illustrated not only thedevelopment of novel PMNs but also the mechanical evaluation for the design of PMNs.
( Tian Zhou Liu ),( Bang Xing Wang ),( Jin Tao Guo ),( Yang Zhou ),( Mugweru Julius ),( Moses Njire ),( Yuan Yuan Cao ),( Tian Wu ),( Zhi Yong Liu ),( Chang Wei Wang ),( Yong Xu ),( Tian Yu Zhang ) 한국미생물 · 생명공학회 2015 Journal of microbiology and biotechnology Vol.25 No.9
The combination of trimethoprim (TMP) and sulfamethoxazole (SMX) has been shown to be active against Mycobacterium tuberculosis (Mtb) in clinical tuberculosis (TB) treatment. However, the mechanism of action of TMP-SMX against Mtb is still unknown. To unravel this, we have studied the effect of TMP and SMX by deleting the folP2 gene in Mycobacterium smegmatis (Msm), and overexpressing the Mtb and Msm folP1/2 genes in Msm. Knocking out of the folP2 gene in Msm reduced the minimum inhibitory concentration of SMX 8-fold compared with wild type. Overexpression of the folP1 genes from Mtb and Msm increased the MICs by 4- and 2-fold in Msm for SMX and TMP, respectively. We show a strong correlation between the expression of folP1 and folP2 genes and TMP-SMX resistance in mycobacteria. This suggests that a combination of FolP2 inhibitor and SMX could be used for TB treatment with a better outcome.
Ying-Hua Li,Yin-Yin Wang,Shan Zhong,Zhi-Li Rong,Yong-Ming Ren,Zhi-Yong Li,Shu-Ping Zhang,Zhi-Jie Chang,Li Liu 한국분자세포생물학회 2009 Molecules and cells Vol.27 No.1
Ligand-dependent or independent oligomerization of receptor protein tyrosine kinase (RPTK) is often an essential step for receptor activation and intracellular signaling. The novel oncogene with kinase-domain (NOK) is a unique RPTK that almost completely lacks an ectodomain, expresses intracellularly and activates constitutively. However, it is unknown whether NOK can form oligomer or what function oligomerization would have. In this study, two NOK deletion mutants were generated by either removing the ectodomain (NOKECD) or including the endodomain (NOK-ICD). Co-immunoprecipitation demonstrated that the transmembrane (TM) domain of NOK was essential for its intermolecular interaction. The results further showed that NOK aggregated more closely as lower order oligomers (the dimer- and trimer-sized) than either deletion mutant did since NOK could be cross-linked by both Sulfo-EGS and formaldehyde, whereas either deletion mutant was only sensitive to Sulfo-EGS. Removing the NOK TM domain (NOK-ICD) not only markedly promoted higher order oligomerization, but also altered the subcellular localization of NOK and dramatically elevated the NOK-mediated constitutive activation of extracellular signal-regulated kinase (ERK). Moreover, NOK-ICD but not NOK or NOKECD was co-localized with the upstream signaling molecule RAS on cell membrane. Thus, TM-mediated intermolecular contacting may be mainly responsible for the constitutive activation of NOK and contribute to the autoinhibitory effect on RAS/MAPK signaling.
Zhi-Rong Zhong,Zhi-rong Zhang,Ji Liu,Yong Deng,Hong-wei Zhang,Yao Fu,Qing-guo Song,Qin He 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.1
A novel non-viral gene delivery system, Procationic-Liposome-Protamine-DNA complexes (PLPD) which could further adsorb transferrin on the surface as a targeting ligand to form Tf- PLPD, was prepared and characterized before and after lyophilization. The size distribution of Tf-PLPD was in the range of 240 ± 12 nm and the zeta potential was -24.10 ± 2.5 mV. The transfection efficiencies of PLPD and Tf-PLPD were 12.18 ± 3.8 and 24.26 ± 2.6 mU β-galactosidase/ mg protein respectively. The lyophilization and the presence of serum didn’t affect the tansfectivities of PLPD or Tf-PLPD. Compared to LipofectamineTM 2000 (Invitrogen, U.S.A.), the procationic liposomes had less cytotoxicity to cells. In summary the procationic lipoplex described here, combining the condensing effect of protamine and the targeting capability of Tf, was a perspective non-viral vector for gene delivery system.
Abietane Diterpenoids from Perovskia atriplicifolia and Their Anti-HBV Activities
Zhi-Yong Jiang,Zhong-Qiu Li,Chao-Guan Huang,Jun Zhou,Qiu-Fen Hu,Wen-Xing Liu,Xiang-Zhong Huang,Wei Wang,Li-Zhu Zhang,Fu-Ting Xia 대한화학회 2015 Bulletin of the Korean Chemical Society Vol.36 No.2
Bioassay-guided phytochemical investigation on the 90% EtOH extract of Perovskia atriplicifolia resulted in the isolation of eight abietane diterpenoids, including three new ones (1–3). Based on spectroscopic methods involving 1D and 2D NMR spectroscopy techniques, mass spectrometry, and optical rotation, the structures of the new compounds (1–3) were unambiguously characterized. Compounds 1–2 and 4–8 were evaluated for their anti-HBV (hepatitis B virus) activity in HepG 2.2.15 cell line. Results suggested rosmadial (8) had the most anti-HBV potency, suppressing the secretion of HBsAg and HBeAg, with IC50 values of 0.09 and 0.34 mM, respectively.
Liu, Shi-Xin,Zhou, Zhi-Rui,Chen, Ling-Xiao,Yang, Yong-Jing,Hu, Zhi-De,Zhang, Tian-Song Asian Pacific Journal of Cancer Prevention 2015 Asian Pacific journal of cancer prevention Vol.16 No.14
Background: Short-course preoperative radiation (SCRT) with delayed surgery was found to increase pathologic complete response (pCR) rates in several trials. However, there was no clear answer on whether SCRT or long-course chemo-radiotherapy (LCRT) is more effective. Therefore we conducted this meta-analysis to evaluate the safety and efficacy of SCRT versus LCRT, both with delayed surgery, for treatment of rectal cancer. Materials and Methods: The literature was searched from PubMed, EMBASE, Web of Science, Cochrane Library and clinicaltrials.gov up to November, 2014. Quality of the randomized controlled trials (RCTs) was evaluated according to the Cochrane's risk of bias tool of RCT. The Grading of Recommendations Assessment, Development and Evaluation (GRADE) system was used to rate the level of evidence. Review Manager 5.3 was employed for statistical analysis. Pooled risk ratios (RRs) and 95% confidence intervals (CIs) were calculated. Results: Three RCTs, with a total of 357 rectal cancer patients, were included in this systematic review. Metaanalysis results demonstrated there were no significantly differences in sphincter preservation rate, local recurrence rate, grade 3~4 acute toxicity, R0 resection rate and downstaging rate. Compared with SCRT, LCRT was associated with significant increase in the pCR rate [RR=0.49, 95%CI (0.31, 0.78), P=0.003]. Conclusions: In terms of sphincter preservation rate, local recurrence rate, grade 3~4 acute toxicity, R0 resection rate and downstaging rate, SCRT with delayed surgery is as effective as LCRT with delayed surgery for management of rectal cancer. LCRT significantly increased pCR rate compared with SCRT. Due to risk of bias and imprecision, further multi-center large sample RCTs were needed to confirm this conclusion.
Current-voltage Characteristics of NdFeAsO0.85F0.15 and NdFeAsO0.85 Superconductors
Yong Liu,YiSheng Chai,Hyeong-Jin Kim,G.R. Stewart,김기훈,Zhi-An Ren,Zhong-Xian Zhao 한국물리학회 2009 THE JOURNAL OF THE KOREAN PHYSICAL SOCIETY Vol.55 No.2
The vortex phase diagrams of NdFeAsO0.85F0.15 and NdFeAsO0.85 superconductors are determined from an analysis of resistivity and current-voltage (I-V ) measurements in magnetic fields up to 9 T. A vortex glass to liquid transition can be identified only in the oxygen-deficient NdFeAsO0.85, for which the I-V curves can be well scaled onto liquid and glass branches consistent with the vortex glass theory. With increasing magnetic field, the activation energy, U0, deduced from the Arrhenius plots of the resistivity based on the thermally-activated flux-flow model decays more quickly for NdFeAsO0.85F0.15 than for NdFeAsO0.85. Moreover, the irreversibility field, Hirr, of NdFeAsO0.85 increases more rapidly than that of NdFeAsO0.85F0.15 with decreasing temperature. These observations imply strong vortex pinning effects in the oxygen-deficient NdFeAsO0.85, presumably caused by enhanced defects and disorders. We infer that the observation of a vortex glass to liquid transition in NdFeAsO0.85 may be also related to the enhanced defects and disorder in the specimen.