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Ze-Qin Dai,Hang Su,Min Luo,Yu Ou,Xiao-Zhong Fu,Yong-Xi Dong,Yu-Feng Cha,Shun Zhang,Yong Huang,Yong-Lin Wang 대한화학회 2015 Bulletin of the Korean Chemical Society Vol.36 No.8
A series of 4′-N-substituted (aminomethyl)benzoate derivatives of scutellarein were designed and synthesized. Evaluation of their physiochemical properties showed that the designed target compounds 5a–e exhibit higher chemical stability and aqueous solubility than scutellarin and scutellarein. The permeability (Papp AP to BL ) of 5c–e in Caco-2 cells were 2.8, 8.1, and 12.6 times higher than that of scutellarin and 1.3, 4.1, and 6.0 times higher than that of scutellarein; especially, 5e had the highest P app AP to BL value (7.19 ± 0.31 × 10−6 cm/s) and the lowest ER (P app BL to AP /P app AP to BL ) value of 0.17. In vitro antioxidative evaluation results revealed that 5e could protect against H2O2 -induced PC12 cells’ oxidative damage by attenuating mitochondrial membrane potential loss and decreasing H2O2 -induced reactive oxygen species (ROS) production.
Ying Yang,Dong Wang,Lei Cui,Hong-Hao Ma,Li Zhang,Hong-Yun Lian,Qing Zhang,Xiao-Xi Zhao,Li-Ping Zhang,Yun-Ze Zhao,Na Li,Tian-You Wang,Zhi-Gang Li,Rui Zhang 대한암학회 2021 Cancer Research and Treatment Vol.53 No.1
Purpose We sought to investigate the effectiveness and safety of dabrafenib in children with BRAFV600E-mutated Langerhans cell histiocytosis (LCH). Materials and Methods A retrospective analysis was performed on 20 children with BRAFV600E-mutated LCH who were treated with dabrafenib. Results The median age at which the patients started taking dabrafenib was 2.3 years old (range, 0.6 to 6.5 years). The ratio of boys to girls was 2.3:1. The median follow-up time was 30.8 months (range, 18.9 to 43.6 months). There were 14 patients (70%) in the risk organ (RO)+ group and six patients (30%) in the RO– group. All patients were initially treated with traditional chemotherapy and then shifted to targeted therapy due to poor control of LCH or intolerance to chemotherapy. The overall objective response rate and the overall disease control rate were 65% and 75%, respectively. During treatment, circulating levels of cell-free BRAFV600E (cfBRAFV600E) became negative in 60% of the patients within a median period of 3.0 months (range, 1.0 to 9.0 months). Grade 2 or 3 adverse effects occurred in five patients. Conclusion Some children with BRAFV600E-mutated LCH may benefit from monotherapy with dabrafenib, especially high-risk patients with concomitant hemophagocytic lymphohistiocytosis and intolerance to chemotherapy. The safety of dabrafenib is notable. A prospective study with a larger sample size is required to determine the optimal dosage and treatment duration.
Ding Sheng-Long,Zhang Tai-Wei,Zhang Qi-Chen,Ding Wang,Li Ze-Fang,Han Guan-Jie,Bai Jin-Song,Li Xi-Lei,Dong Jian,Wang Hui-Ren,Jiang Li-Bo 생화학분자생물학회 2021 Experimental and molecular medicine Vol.53 No.-
Night shift workers with disordered rhythmic mechanical loading are more prone to intervertebral disc degeneration (IDD). Our results showed that circadian rhythm (CR) was dampened in degenerated and aged NP cells. Long-term environmental CR disruption promoted IDD in rats. Excessive mechanical strain disrupted the CR and inhibited the expression of core clock proteins. The inhibitory effect of mechanical loading on the expression of extracellular matrix genes could be reversed by BMAL1 overexpression in NP cells. The Rho/ROCK pathway was demonstrated to mediate the effect of mechanical stimulation on CR. Prolonged mechanical loading for 12 months affected intrinsic CR genes and induced IDD in a model of upright posture in a normal environment. Unexpectedly, mechanical loading further accelerated the IDD in an Light-Dark (LD) cycle-disrupted environment. These results indicated that intrinsic CR disruption might be a mechanism involved in overloading-induced IDD and a potential drug target for night shift workers.
Hao Tang,Nian-Guang Li,Zhi-Hao Shi,Yu-Ping Tang,Qian-Ping Shi,Ze-Xi Dong,Peng-Xuan Zhang,Jin-ao Duan 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.10
The binding abilities of scutellarin (Scu) andscutellarein (Scue) with bovine serum albumin (BSA) wereinvestigated using equilibrium dialysis, high performanceliquid chromatography, fluorescence spectroscopy, competitivesite marker and molecular docking. The resultsshowed that the average protein binding ratios of Scu andScue with BSA were (79.85 ± 1.83) and (85.49 ± 1.21) %respectively. Under simulated physiological conditions, thefluorescence data indicated that Scu and Scue bound withBSA through a static mechanism. The thermodynamicparameters indicated that the interactions of Scu-BSA andScue-BSA mainly occurred by van der Waals forces andhydrogen bonds and it was easier for Scue to bind withBSA than Scu, indicating that the glucuronic acid moleculein Scu decreased the binding affinity. Site competitivemarker experiments showed that the binding sites of Scuand Scue mainly located within the sub-domain IIA ofBSA. Furthermore, molecular docking studies indicatedthat one BSA could bind three Scue, while one BSA couldcarry only two Scu. All these results clearly indicated theinteractions of Scu and Scue with BSA, which will lay thefoundation for further research to determine the pharmacologyand pharmacodynamics of Scu and Scue for treatingischemic cerebrovascular disease.