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Synthesis and Cytotoxicity of Novel 3-Amino-4-indolylmaleimide Derivatives
Sheng-Yin Zhao,Yan-Wu Yang,Hai-Quan Zhang,Yun Yue,Mei Fan 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.4
In an attempt to develop potent and selective antitumor agents, a series of novel 3-amino-4-indolylmaleimides were designed and synthesized. The reaction showed high regioselectivity. The structure of compound 7a was determined by an X-ray single crystal diffraction method. The cytotoxicities of the title compounds were evaluated against HeLa, SMMC 7721 and HL 60 cancer cell lines by a standard MTT assay in vitro. The pharmacological results showed that some of the title compounds displayed moderate or high cytotoxic activity against the tested cell lines. Compound 7d was the most promising compound against the tested cancer cell lines. Structure-activity relationships are discussed based on the experimental data obtained. A hydroxyethylamino group at the 3-position in the side chain of indolylmaleimide is associated with an increase in cytotoxicity.
Aberrant microRNAs Expression in CD133+/CD326+ Human Lung Adenocarcinoma Initiating Cells from A549
Sheng Lin,Zheng-tang Chen,Jian-guo Sun,Jing-bo Wu,Hai-xia Long,Cong-hui Zhu,Tong Xiang,Hu Ma,Zhong-quan Zhao,Quan Yao,An-mei Zhang,Bo Zhu 한국분자세포생물학회 2012 Molecules and cells Vol.33 No.3
Increasing evidence demonstrates that miRNAs are in-volved in the dysregulation of tumor initiating cells (TICs) in various tumors. Due to a lack of definitive markers, cell sorting is not an ideal separation method for lung adeno-carcinoma initiating cells. In this study, we combined pa-clitaxel with serum-free medium cultivation (inverse-induc-tion) to enrich TICs from A549 cells, marked by CD133/ CD326, defined features of stemness. We next investigated aberrant microRNAs in this subpopulation compared to normal cells with miRNA microarray and found that 50 miRNAs exhibited a greater than 2-fold change in expres-sion. As further validation, 10 miRNAs were chosen to perform quantitative RT-PCR on the A549 cell line and primary samples. The results suggest that aberrant ex-pression of miRNAs such as miR-29ab, miR-183, miR-17-5p and miR-127-3P may play an important role in regulat-ing the bio-behavior of TICs.
Xiao-Quan Xu,Sheng Liu,Qing-Quan Zu,Lin-Bo Zhao,Jin-Guo Xia,Chun-Gao Zhou,Wei-Zhong Zhou,Hai-Bin Shi 대한신경과학회 2013 Journal of Clinical Neurology Vol.9 No.2
Background and Purpose This study evaluated the clinical value of detachable-balloon embolization for traumatic carotid-cavernous fistula (TCCF), focusing on the frequency, risk factors, and retreatment of recurrence. Methods Fifty-eight patients with TCCF underwent transarterial detachable-balloon embolization between October 2004 and March 2011. The clinical follow-up was performed every 3months until up to 3 years postprocedure. Each patient was placed in either the recurrence group or the nonrecurrence group according to whether a recurrence developed after the first procedure. The relevant factors including gender, fistula location, interval between trauma and the interventional procedure, blood flow in the carotid-cavernous fistula, number of balloons, and whether the internal carotid artery (ICA) was sacrificed were evaluated. Results All 58 TCCFs were successfully treated with transarterial balloon embolization, including 7 patients with ICA sacrifice. Recurrent fistulas occurred in seven patients during the follow-up period. Univariate analysis indicated that the interval between trauma and the interventional procedure (p=0.006) might be the main factor related to the recurrence of TCCF. The second treatments involved ICA sacrifice in two patients, fistula embolization with balloons in four patients, and placement of a covered stent in one patient. Conclusions Detachable balloons can still serve as the first-line treatment for TCCFs and recurrent TCCFs despite having a nonnegligible recurrence rate. Shortening the interval between trauma and the interventional procedure may reduce the risk of recurrence.
Yuan, Sheng-Guang,Liao, Wei-Jia,Yang, Jian-Jun,Huang, Guo-Jin,Huang, Zhao-Quan Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.24
Background: This study was conducted to determine DEPDC1 expression in hepatocelluar carcinomas (HCCs) and to reveal its potential role in diagnosis and prognosis of affected patients. Materials and Methods: DEPDC1 expression at the mRNA level was detected by quantitative real-time PCR (qRT-PCR) in 205 cases of HCC and paired adjacent normal liver tissues, and by semi-quantitative RT-PCR in 20 cases. Survival curves were obtained by using Kaplan-Meier method and Log-rank test. Independent predictors associated with regard to disease free survival (DFS) and overall survival (OS) were identified using the Cox proportional hazard model. Results: High DEPDC1 mRNA levels were detected in 144 out of 205 cases (70.24%) of HCC, significantly associated with clinicopathological parameters, including tumor size (${\geq}4cm$), alpha-fetoprotein (${\geq}100ng/ml$), B-C of BCLC stage and recurrence. Kaplan-Meier survival analysis revealed that HCC patients with high DEPDC1 expression had poor OS and DFS. Multivariate analysis demonstrated that high DEPDC1 expression was an independent predictor for OS (HR=1.651; 95% 95%CI, 1.041-2.617; p=0.033) and DFS (HR=1.583; 95%CI, 1.01-2.483; p=0.045). Conclusions: Our results indicate DEPDC1 might be a novel diagnostic marker and an independent prognostic predictor for HCC patients.
Directed Evolution of Beta-galactosidase from Escherichia coli into Beta-glucuronidase
Xiong, Ai-Sheng,Peng, Ri-He,Zhuang, Jing,Liu, Jin-Ge,Xu, Fang,Cai, Bin,Guo, Zhao-Kui,Qiao, Yu-Shan,Chen, Jian-Min,Zhang, Zhen,Yao, Quan-Hong Korean Society for Biochemistry and Molecular Biol 2007 Journal of biochemistry and molecular biology Vol.40 No.3
In vitro directed evolution through DNA shuffling is a powerful molecular tool for creation of new biological phenotypes. E. coli $\beta$-galactosidase and $\beta$-glucuronidase are widely used, and their biological function, catalytic mechanism, and molecular structures are well characterized. We applied an in vitro directed evolution strategy through DNA shuffling and obtained five mutants named YG6764, YG6768, YG6769, YG6770 and YG6771 after two rounds of DNA shuffling and screening, which exhibited more $\beta$-glucuronidase activity than wild-type $\beta$-galactosidase. These variants had mutations at fourteen nucleic acid sites, resulting in changes in ten amino acids: S193N, T266A, Q267R, V411A, D448G, G466A, L527I, M543I, Q626R and Q951R. We expressed and purified those mutant proteins. Compared to the wild-type protein, five mutant proteins exhibited high $\beta$-glucuronidase activity. The comparison of molecular models of the mutated and wildtype enzymes revealed the relationship between protein function and structural modification.
( Xiao Juan Xing ),( Yong Sheng Tian ),( Ri He Peng ),( Jing Xu ),( Wei Zhao ),( Quan Hong Yao ),( Sheng Sun ) 한국미생물 · 생명공학회 2014 Journal of microbiology and biotechnology Vol.24 No.10
Although a large number of AroA enzymes (EPSPS: 5-enopyruvylshikimate-3-phosphate synthase) have been identified, cloned, and tested for glyphosate resistance, only two AroA variants, derived from Agrobacterium tumefaciens strain CP4 and Zea mays, have been utilized to produce the commercial glyphosate-resistant crops. Here, we have used a PCR-based twostep DNA synthesis method to synthesize an aroA gene (aroAA. metalliredigens) from Alkaliphilus metalliredigens, encoding a new EPSPS. Furthermore, transgenic Arabidopsis with the new aroAA. metalliredigens gene was obtained to confirm the potential of the novel aroA gene in developing glyphosate-resistant crops.
Dan Ni Li,Jing Huang,Zhao Hua Ren,Rui Sheng,Zheng Bo Qian,Bei Bei Li,Xiao Feng Quan,Ye Xi Zhang,Jun Ru Wang,Huan Tian 한국공업화학회 2021 Journal of Industrial and Engineering Chemistry Vol.99 No.-
The phase separationphenomena or cloud points (CP) behaviorof nonionic octylphenol polyoxyethylene etherwith oxyethylene glycol ether unit of 15 (OP-15) were investigated in aqueous micellar solutions containinghigh concentrations of inorganic salts including NaCl, KCl, MgCl2, CaCl2, BaCl2, AlCl3, FeCl3, Na2SO4and Na2SiO3. The change in CP induced by salts and its mechanism are discussed theoretically. In aqueous solutionscontaining high concentration of salt, for thefirst time the linear relationship between CP and saltconcentrationiswellestablishedtocharacterizethedepressionofCP.Basedonpseudophaseseparationmodel,thermodynamic parameters are estimated and adopted to further describe the phase separation process andthe interactions between OP-15 molecules or the OP-15/water interactions. Thermodynamic parametersincluding standard Gibbs energy change (DG0CP), enthalpy change (DH0CP) and entropy change (DS0CP)indicate that the additions of different salts result in the change in entropy-driven nonspontaneousprocess of phase separation. These data, which are from the compensation temperatures and the changeof molar heat capacity, also prove that different ions induce the change in the interactions betweensurfactant molecules or the surfactant–water interaction and thus affect the depression of CP. Thesefindings help with understanding the effect of inorganic salts, especially the high concentration of salt, onCP of nonionic surfactant and then broadening the application of nonionic surfactant based on CP such asthe extraction of biomaterials in biological samples derived from animals or plants, etc.