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Phase II trial of VEGFR2 inhibitor apatinib for metastatic sarcoma: focus on efficacy and safety
Zhichao Liao,Feng Li,Chao Zhang,Lei Zhu,Yehui Shi,Gang Zhao,Xu Bai,Shafat Hassan,Xinyue Liu,Ting Li,Peipei Xing,Jun Zhao,Jin Zhang,Ruwei Xing,Sheng Teng,Yun Yang,Kexin Chen,Jilong Yang 생화학분자생물학회 2019 Experimental and molecular medicine Vol.51 No.-
Apatinib (YN968D1) is a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor 2 (VEGFR- 2). We conducted a single-arm, nonrandomized phase II study (NCT03121846) to assess the efficacy and safety of apatinib in patients with stage IV sarcoma. We recruited 64 patients with stage IV sarcoma who had failed chemotherapy. The primary endpoint was progression-free survival (PFS), and the secondary endpoints were progression-free survival rate (PFR), objective response rate (ORR), and disease control rate (DCR) at week 12. Treatment-related adverse effects (AEs) were evaluated. Fifty-nine patients were assessed for efficacy and 64 patients for AEs. The median PFS was 7.93 months. At 12 weeks, the PFR was 74%, the ORR was 16.95% (10/59), and the DCR was 86.44% (51/59). The final ORR was 15.25% (9/59) and the DCR was 57.63% (34/59). Notably, 22 patients (34.38%) who developed hypertension, hand-foot-skin reaction, or proteinuria had significantly longer OS than those without these AEs (18.20 vs. 10.73 months; P = 0.002). We conclude that apatinib is effective and well tolerated in patients with advanced sarcoma. The development of hypertension, hand-foot-skin reaction, or proteinuria may indicate a favorable prognosis, representing a novel finding in sarcoma patients.
Peng Liao,Shi-Qin Hu,Hong Zhang,Liang-Bi Xu,Jing-Zi Liu,Bin He,Shang-Gao Liao,Yong-Jun Li 대한화학회 2018 Bulletin of the Korean Chemical Society Vol.39 No.3
In our previous studies, we have shown that thiourea compounds containing phosphate esters have potent antitumor activity and can be used as a novel strategy for the development of antitumor agents. Herein, a series of novel phosphonate thioureas 5–38 have been synthesized, which were fully characterized by 1H NMR, 13C NMR spectrum, elemental analysis. Three human cancer cell lines (Bcap-37, BGC-823, and PC-3) have been used to investigate these compounds’ antitumor activities. After the summarization of the structure–activity relationships, we found that the variation of R, R1, and R2 in these novel phosphonate thioureas contribute to the antitumor activities. All these SAR-guided efforts may lead to novel antitumor drugs in the market in the near future.
Recent Progress in Methods of Generating Water Mist for Fire Suppression
( Guang Xuan Liao ),( Xin Huang ),( Bei Hua Cong ),( Jun Qin ),( Jiang Hong Liu ),( Xi Shi Wang ) 한국액체미립화학회 2005 한국액체미립화학회 학술강연회 논문집 Vol.2005 No.-
To prevent the ozonosphere from being destroyed by Halon, it is an urgent task to find out Halon replacement. As one of the replacements water mist have showed broad applications by its advantages: little pollution to environment (not destroying the ozone layer or bring green house effect), extinguishing fire quickly, consuming a small quantity of water and having little damage to the protected objects. The methods of generating water mist strongly influence fire suppression effectiveness, which determine the cone angle, drop size distribution, flux uniformity, and momentum of the generating spray. The traditional water mist nozzle included pressure jet nozzles, impingement nozzles and twin-fluid nozzles. All of them have more or less disadvantages for fire suppression. Therefore, many research institutes and corporations are taking up with innovations in mist generation. This article provided some recent studies in State Key Laboratory of Fire Science (SKLFS) of University of Science and Technology of China. SKLFS have investigated new methods of generating water mist (i.e. effervescent atomization and ultrasonic atomization), and self developed a series of nozzles and developed advanced DPIVS (Digital Particle Image Velocimetry and Sizing) technique. Characteristics of water mist (the distribution of droplet sizes, flux density, spray dynamics and cone angle) produced by these nozzles were measured under different conditions (work pressure, nozzle geometry, etc.) using LDV/APV and DPIVS systems. A series of experiments were performed to study the fire suppression effectiveness in different fire scenario (different kinds of the fuel, fire size and ventilation conditions). The fire extinguishing mechanisms of water mist was also discussed.
( Chao Dong ),( Han Jun Li ),( Shi Chang ),( Hui Jun Liao ),( Zhi Peng Zhang ),( Peng Huang ),( Hui Huan Tang ) 대한간학회 2013 Gut and Liver Vol.7 No.2
Background/Aims: We aimed to investigate the correlation between a disintegrin and metalloprotease with thrombospondin motif 2 (ADAMTS-2) and transforming growth factor-β1 (TGF-β1) in clinical human cirrhotic tissues. Methods: The liver tissues of 24 patients (16 cases with cirrhotic portal hypertension as the cirrhosis group and eight cases with healthy livers as the normal group) were collected. Immunohistochemistry and Western blots were performed to evaluate the protein expression levels of ADAMTS-2 and TGF-β1. Western blots for other key mediators of cirrhotic progression, including SMAD2, SMAD3, TGF-β receptor II (TGFβRII), matrix metalloproteinases 2 (MMP2), and tissue inhibitor of matrix metalloproteinases 2 (TIMP2), were also performed. Results: Cirrhotic tissues showed higher percentages of collagen. The protein expression levels of ADAMTS-2 and TGF-β1 were significantly higher in the cirrhotic group as compared to the matched normal group (p<0.05), and there was a positive correlation between these two proteins (r=0.862, p<0.01). The protein expressions of MMP2, TIMP2, and TGFβRII, as well as the phosphorylated forms of SMAD2 and SMAD3, were significant higher in the cirrhotic group (p<0.01 or p<0.05). Conclusions: These findings suggested that ADAMTS-2 and TGF-β1 may play important roles in the pathogenesis of human cirrhosis; specifically, TGF-β1 may induce the expression of ADAMTS-2 through the TGFβ/SMAD pathway. (Gut Liver 2013;7:213-220)
Yu-Xiao Zou,Teng-Gen Hu,Ying Shi,Jun Liu,Li-Xia Mu,Yang Xiao,Sen-Tai Liao 한국응용곤충학회 2017 Journal of Asia-Pacific Entomology Vol.20 No.4
Silkworm pupae are a source of edible lipid with a high content of unsaturated fatty acids (UFAs) (70% of total lipid content) and are becoming a focus of pharmaceutical and dietary research in the functional oil field. To study the nutritional value of different silkworm strains, principal component analysis (PCA) was used to establish a mathematical model and cluster analysis on silkworm pupae lipid (SPL) in 90 strains based on Z-score. Single-factor correlation analysis indicated that the PUFAs content was significantly positively correlated with the α-linolenic acid (ALA) (ρ=0.98) and negatively correlated with the oleic acid (OA) (ρ=−0.73) contents, and comprehensive of principal components mathematical model (PC =0.148ZX1 +0.00 2ZX2 −0.197ZX3 −0.338ZX4 +0.220ZX5 +0.304ZX6 +0.314ZX7, ZXi is the standard score (Z-score) of X1, which was calculated as follow: ZXi = (Xi −−X )/S, where X1: palmitic acid, X2: palmitoleic acid, X3: stearic acid, X4: OA, X5: linoleic acid, X6: ALA, X7: PUFAs.−X is the arithmetic mean content of variable i, and S is the standard deviation of variable i for all samples included in the analysis.) showed the amount of ALA and PUFAs were the key factors determining the nutritional value of the pupae lipid. Cluster analysis on the composite scores calculated by the model of the principal component divided the 90 strains into three groups. A cluster of 6 strains (XHR, XIFF, ZX, YT, YO and BTN) with the best nutritional value was characterized by high contents of ALA and PUFAs and a low content of oleic acid.
Kim, Jae-Geun,Park, Min-Sik,Hwang, Soo Min,Heo, Yoon-Uk,Liao, Ting,Sun, Ziqi,Park, Jong Hwan,Kim, Ki Jae,Jeong, Goojin,Kim, Young-Jun,Kim, Jung Ho,Dou, Shi Xue Wiley (John WileySons) 2014 CHEM SUS CHEM Vol.7 No.5
<P>One-dimensional nanomaterials have short Li(+) diffusion paths and promising structural stability, which results in a long cycle life during Li(+) insertion and extraction processes in lithium rechargeable batteries. In this study, we fabricated one-dimensional spinel Li4Ti5O12 (LTO) nanofibers using an electrospinning technique and studied the Zr(4+) doping effect on the lattice, electronic structure, and resultant electrochemical properties of Li-ion batteries (LIBs). Accommodating a small fraction of Zr(4+) ions in the Ti(4+) sites of the LTO structure gave rise to enhanced LIB performance, which was due to structural distortion through an increase in the average lattice constant and thereby enlarged Li(+) diffusion paths rather than changes to the electronic structure. Insulating ZrO2 nanoparticles present between the LTO grains due to the low Zr(4+) solubility had a negative effect on the Li(+) extraction capacity, however. These results could provide key design elements for LTO anodes based on atomic level insights that can pave the way to an optimal protocol to achieve particular functionalities.</P>
Yan-Ni Wu,Hai-Fu Guo,Peng Hu,Xiao-Peng Xiao,Zhao-Wang Xiao,Shi-Jun Liao 성균관대학교(자연과학캠퍼스) 성균나노과학기술원 2016 NANO Vol.11 No.7
Three types of ternary low-platinum nanocatalysts, alloy PdPtIr/C, core–shell PdPt@PtIr/C and Pd@PtIr/C, have been prepared, and their catalytic behaviors toward methanol oxidation reaction (MOR)/oxygen reduction reaction (ORR) are comparatively investigated via cyclic voltammetry and chronoamperometry analysis in an acidic medium. Through a two-step colloidal technique, the synthesized core–shell structured catalyst PtPd@PtIr/C with alloy core and alloy shell show the best catalytic activity toward MOR and the best poisoning tolerance. The alloy PdPtIr/C catalyst prepared via a one-step colloidal technique exhibits the best performance toward ORR among the three catalysts. All the three catalysts are characterized by transmission electron microscopy (TEM), X-ray diffraction (XRD) and other characterization techniques.