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Yuan-Yuan Gao,Wen Tian,Hui-Nan Zhang,Yang Sun,Jing-Ru Meng,Wei Cao,Xiao-Qiang Li 대한약학회 2021 Archives of Pharmacal Research Vol.44 No.4
Canonical transient receptor potential channels(TRPCs) are nonselective, high calcium permeability cationicchannels. The TRPCs family includes TRPC1, TRPC2,TRPC3, TRPC4, TRPC5, TRPC6, and TRPC7. These channelsare widely expressed in the cardiovascular and nervoussystems and exist in many other human tissues and celltypes, playing several crucial roles in the human physiologicaland pathological processes. Hence, the emergenceof TRPCs modulators can help investigate these channels’applications in health and disease. It is worth noting that theTRPCs subfamilies have structural and functional similarities,which presents a signifi cant diffi culty in screening anddiscovering of TRPCs modulators. In the past few years,only a limited number of selective modulators of TRPCswere detected; thus, additional research on more potent andmore selective TRPCs modulators is needed. The presentreview focuses on the striking desired therapeutic eff ectsof TRPCs modulators, which provides intel on the structuralmodifi cation of TRPCs modulators and further pharmacologicalresearch. Importantly, TRPCs modulators cansignifi cantly facilitate future studies of TRPCs and TRPCsrelated diseases.
Research on Thymopentin Loaded Oral N-Trimethyl Chitosan Nanoparticles
Yuan, Xiao-Jia,Zhang, Zhi-Rong,Song, Qing-Guo,He, Qin The Pharmaceutical Society of Korea 2006 Archives of Pharmacal Research Vol.29 No.9
Peptides, although high efficacy and specificity in their physiological function, usually have low therapeutical activities due to their poor bioavailability when administrated orally. Nanoparticles have been regarded as a useful vector for targeted drug delivery system because they can protect drug from being degraded quickly and pass the gastrointestinal barriers. Here we described a novel oral N-trimethyl chitosan nanoparticles formulation containing thymopentin (Tp5-TMC-NP). N-trimethyl chitosan (TMC) was synthesized and then used to prepare Tp5-TMC-NP by ionotropic gelation. A three-factor, five-level CCD (Central Composite Design) design was used in the optimization procedure, with HPLC as the analyzing method. The resulting Tp5-TMC-NP had a regular spherical surface and a narrow particle size range with a mean diameter of 110.6 nm. The average entrapment efficiency was 78.8%. The lyophilized Tp5-TMC-NP formulation was stable in $4^{\circ}C\;or\;-20^{\circ}C$ after storage of 3 months without obvious changes in morphology, particle size, pH and entrapment ratio. The results of the flow cytometer determination showed that the ratio of $CD4^+/CD8^+$ of Wistar female rat given Tp5-TMC-NP (ig) was 2.59 time that of the group given Tp5 (ig).
Cinnamaldehyde Derivatives Inhibit Coxsackievirus B3-Induced Viral Myocarditis
( Xiao-qiang Li ),( Xiao-xiao Liu ),( Xue-ying Wang ),( Yan-hua Xie ),( Qian Yang ),( Xin-xin Liu ),( Yuan-yuan Ding ),( Wei Cao ),( Si-wang Wang ) 한국응용약물학회 2017 Biomolecules & Therapeutics(구 응용약물학회지) Vol.25 No.3
The chemical property of cinnamaldehyde is unstable in vivo, although early experiments have shown its obvious therapeutic effects on viral myocarditis (VMC). To overcome this problem, we used cinnamaldehyde as a leading compound to synthesize derivatives. Five derivatives of cinnamaldehyde were synthesized: 4-methylcinnamaldehyde (1), 4-chlorocinnamaldehyde (2), 4-methoxycinnamaldehyde (3), α-bromo-4-methylcinnamaldehyde (4), and α-bromo-4-chlorocinnamaldehyde (5). Neonatal rat cardiomyocytes and HeLa cells infected by coxsackievirus B3 (CVB3) were used to evaluate their antiviral and cytotoxic effects. In vivo BALB/c mice were infected with CVB3 for establishing VMC models. Among the derivatives, compound 4 and 5 inhibited the CVB3 in HeLa cells with the half-maximal inhibitory concentrations values of 11.38 ± 2.22 μM and 2.12 ± 0.37 μM, respectively. The 50% toxic concentrations of compound 4 and 5-treated cells were 39-fold and 87-fold higher than in the cinnamaldehyde group. Compound 4 and 5 effectively reduced the viral titers and cardiac pathological changes in a dose-dependent manner. In addition, compound 4 and 5 significantly inhibited the secretion, mRNA and protein expressions of inflammatory cytokines TNF-α, IL-1β and IL-6 in CVB3-infected cardiomyocytes, indicating that brominated cinnamaldehyde not only improved the anti-vital activities for VMC, but also had potent anti-inflammatory effects in cardiomyocytes induced by CVB3.
Yuan, Yuan,Cai, Hui,Yang, Xiao-Jun,Li, Wei,He, Jin,Guo, Tian-Kang,Chen, Yi-Rong Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.14
Background: The aim of this study was to investigate the effect of a c-myc antisense oligodeoxynucleotide and 5-fluorouracil on the expression of c-myc, invasion and proliferation of HEPG-2 liver cancer cells. Materials and Methods: HEPG-2 cells were treated with lipiosome-mediated c-myc ADSON and 5-fluorouracil. The proliferation inhibition rate and invasion were measured by MTT and invasion assay, respectively. Cell apoptosis was detected by flow cytometry and expression of c-myc by RT-PCR and immunohistochemistry. Results: The proliferation inhibition rate was significantly higher in the antisense oligodeoxynucleotide added-5-fluorouracil group than single antisense oligodeoxynucleotide or 5-fluorouracil group (p<0.05). G0/G1 cells in the antisense oligodeoxynucleotide group and S cells in the 5-fluorouracil groups were significantly increased than that in the control group, respectively (P<0.01). The amplification strips of PCR products in 5-FU, ASODN and combination groups were significantly weaker than that in the control group (P<0.01). The percentage of c-myc-protein-positive cells were significantly lower in antisense oligodeoxynucleotide, 5-fluorouracil and combination groups than that in the control group (P<0.01). Conclusions: A liposome-mediated c-myc antisense oligodeoxynucleotide and 5-fluorouracil can inhibit the proliferation and invasion of liver cancer cells by reducing the expression of c-myc. A c-myc antisense oligodeoxynucleotide can increase the sensitivity of liver cancer cells to 5-fluorouracil and decrease the dosage of the agent necessary for efficacy, providing an experimental basis for the clinical therapy of liver cancer.
Xiao-Lin Yuan,Lipo Mo,Yongguang Yu,Guo-Jian Ren 제어·로봇·시스템학회 2020 International Journal of Control, Automation, and Vol.18 No.7
This paper mainly considers the distributed containment control problem for continuous-time fractionalorder multi-agent systems (FOMASs) with double-integrator, where the control input of each agent is constrained to lie in a nonconvex set. A distributed projection containment control algorithm is designed for each follower. To finish the convergence analysis, the original closed-loop system is first changed into an equivalent one by a proper model transformation and the method of the L1 interpolation approximation is introduced to deal with the projection operator. Then, by using the properties of the convex hull and the Mittag-Leffler function, it is shown that the largest distance between the followers and the convex hull spanned by leaders tends to zero asymptotically, while all agents’ control inputs are constrained to stay in their corresponding nonconvex constraint sets. Finally, numerical simulations are provided to verify the effectiveness of the theoretical results.
Relationship Between the SER Treatment Period and Prognosis of Patients with Small Cell Lung Cancer
Xiao, Xiao-Guang,Wang, Shu-Jing,Hu, Li-Ya,Chu, Qian,Wei, Yao,Li, Yang,Mei, Qi,Chen, Yuan Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.15
Purpose: To explore the relationship between SER (time between the start of any treatment and the end of radiation therapy) and the survival of patients with limited-stage small cell lung cancer. Materials and Methods: Between 2008 and 2013, 135 cases of limited-stage small cell lung cancer (LS-SCLC) treated with consecutively curative chemoradiotherapy were included in this retrospective analysis. In terms of SER, patients were divided into early radiotherapy group (SER<30 days, n=76) and late radiotherapy group ($SER{\geq}30$ days, n=59) with a cut-off of SER 30 days. Outcomes of the two groups were compared for overall survival. Results: For all analyzable patients, median follow-up time was 23.8 months and median overall survival time was 16.8 months. Although there was no significant differences in distant metastasis free survival between the two groups, patients in early radiotherapy group had a significantly better PFS (p=0.003) and OS (p=0.000). Conclusions: A short SER may be a good prognostic factor for LD-SCLC patients treated with concurrent chemoradiotherapy.
SOFTWARE PERFORMANCE TESTING BASED ON LINUX KERNEL
Yuan Yuan Li,Peng Xiao,Huimin Meng 한국멀티미디어학회 2006 한국멀티미디어학회 국제학술대회 Vol.2006 No.-
Linux has created a huge new playing field for enterprises, academia, and governments. But lack and instability of applications have stopped many users from strategic, wholesale migrations to Linux. With more and more applications running on Linux system, for example mozilla fire fox, openoffice, GCC, etc. the software performance testing is becoming important on Linux platform. The kernel of an operating system has a significant impact on the overall performance of a computer system [1]. To test a software performance based on system kernel can give us a unique insight into the software, provide us useful information in determining the bottlenecks and weaknesses of the software, and thus enable us to improve it. This paper discusses the methodologies of software performance testing based on Linux kernel, which include design workload, get system parameter, time measurement and CPU utilized. We have done experiments on a computer running Linux; experiment results show that the methodologies of software performance testing based on Linux kernel is completely realizable and efficacious. Even though this paper is not intended to provide a comprehensive software test suite, the methodologies presented here can be extended to build such programs.
Xiao, Juan,Zhang, Tao,Xu, Daichao,Wang, Huibing,Cai, Yu,Jin, Taijie,Liu, Min,Jin, Mingzhi,Wu, Kejia,Yuan, Junying Cold Spring Harbor Laboratory Press 2015 Genes & development Vol.29 No.2
<P>Vps34, the catalytic subunit in the class III phosphatidylinositol 3 kinase complexes, mediates the production of PtdIns3P, a key intracellular lipid involved in regulating autophagy and receptor degradation. Xiao et al. show that DNA damage-activated mitotic arrest and CDK activation lead to the phosphorylation of Vps34. This provides a signal to promote Vps34 ubiquitination and proteasomal degradation mediated by FBXL20, leading to inhibition of autophagy and receptor endocytosis. Importantly, they also find that expression of FBXL20 is regulated by p53-dependent transcription.</P><P>Vacuolar protein-sorting 34 (Vps34), the catalytic subunit in the class III PtdIns3 (phosphatidylinositol 3) kinase complexes, mediates the production of PtdIns3P, a key intracellular lipid involved in regulating autophagy and receptor degradation. However, the signal transduction pathways by which extracellular signals regulate Vps34 complexes and the downstream cellular mechanisms are not well understood. Here we show that DNA damage-activated mitotic arrest and CDK activation lead to the phosphorylation of Vps34, which provides a signal to promote its ubiquitination and proteasomal degradation mediated by FBXL20 (an F-box protein) and the associated Skp1 (S-phase kinase-associated protein-1)–Cullin1 complex, leading to inhibition of autophagy and receptor endocytosis. Furthermore, we show that the expression of FBXL20 is regulated by p53-dependent transcription. Our study provides a molecular pathway by which DNA damage regulates Vps34 complexes and its downstream mechanisms, including autophagy and receptor endocytosis, through SCF (Skp1–Cul1–F-box)-mediated ubiquitination and degradation. Since the expression of FBXL20 is regulated by p53-dependent transcription, the control of Vps34 ubiquitination and proteasomal degradation by FBXL20 and the associated SCF complex expression provides a novel checkpoint for p53 to regulate autophagy and receptor degradation in DNA damage response.</P>
Xiao-Yong Gao,Hong-Liang Feng,Zeng-Yuan Zhang,Jiao-Min Ma,Meng-Ke Zhao,Chao Chen,Jin-Hua Gu,Shi-E Yang,Yong-Sheng Chen,Jing-Xiao Lu 한국물리학회 2011 THE JOURNAL OF THE KOREAN PHYSICAL SOCIETY Vol.58 No.2
Using values of the oxygen flux ratio (OFR = [O2]/[Ar]) ranging from 0 to 0.5, authors deposited a series of silver-oxide (Ag_xO) films on glass substrates by direct-current reactive magnetron sputtering (DC sputtering) at a substrate temperature of 150 ℃. The effect of the OFR on the film’s structural and optical properties was systematically investigated by using X-ray diffractometry, scanning electron microscopy and spectrophotometry. The Ag_xO films deposited clearly show an evolution of the film’s phase structure from the biphased (Ag + Ag_2O) structure to the biphased (AgO + Ag_2O) structure and then to the single-phased (Ag_2O) structure as value of the OFR increases. Accordingly, the film’s surface morphology, related to the film’s crystalline structure, clearly changes from a loose and porous surface structure to a compact surface structure and then to a pyramid-like surface structure with increasing value of the OFR. The novel porous structure may be attributed to the interruption of the silver’s growth course by the AgO on the film’s surface. Notably, a single-phased Ag_2O film is deposited by DC-sputtering at OFR = 0.5 due to the dual effects of thermal decomposition of the AgO phase and a combination reaction of AgO and Ag to Ag_2O. The oscillations both in the film’s reflectivity and transmissivity spectra are strengthened with increasing OFR, indicating an evolution from the metallic behavior of the biphased (Ag + Ag_2O) film to the dielectric behavior of the biphased (Ag_2O + AgO) film and the single-phased Ag2O film. The fitted optical absorption edges of the Ag_2O and the Ag_xO films deposited at values of the OFR of 0.5 and 0.33 are approximately 2.43 eV and 2.34 eV, respectively. The absorption edges are closely related to the direct interband transitions.