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Biotransformation, a Promising Technology for Anti-cancer Drug Development
Gao, Fei,Zhang, Jin-Ming,Wang, Zhan-Guo,Peng, Wei,Hu, Hui-Ling,Fu, Chao-Mei Asian Pacific Journal of Cancer Prevention 2013 Asian Pacific journal of cancer prevention Vol.14 No.10
With the high morbidity and mortality caused by cancer, finding new and more effective anti-cancer drugs is very urgent. In current research, biotransformation plays a vital role in the research and development of cancer drugs and has obtained some achievements. In this review, we have summarized four applications as follows: to exploit novel anti-cancer drugs, to improve existing anti-cancer drugs, to broaden limited anti-cancer drug resources and to investigate correlative mechanisms. Three different groups of important anti-cancer compounds were assessed to clarify the current practical applications of biotransformation in the development of anti-cancer drugs.
Variation of Urinary and Serum Trace Elements (Ca, Zn, Cu, Se) in Bladder Carcinoma in China
Guo, Kun-Feng,Zhang, Zhe,Wang, Jun-Yong,Gao, Sheng-Lin,Liu, Jiao,Zhan, Bo,Chen, Zhi-Peng,Kong, Chui-Ze Asian Pacific Journal of Cancer Prevention 2012 Asian Pacific journal of cancer prevention Vol.13 No.5
Backgrounds: Deficiency or excess of trace elements can induce body metabolic disorders and cellular growth disturbance, even mutation and cancerization. Since there are few studies of the effect of trace elements in bladder carcinoma in China, the aim of this study was thus to assess variation using a case control approach. Methods: To determine this, 81 patients with bladder carcinoma chosen as a study group and 130 healthy persons chosen as a control group were all assayed for urinary and serum trace elements (calcium [Ca], zinc [Zn], copper [Cu], selenium [Se]) using an atomic absorption spectrophotometer, and the results were analyzed by independent sample t tests. The correlative factors on questionnaires answered by all persons were analyzed by logistic regression. Results: The results showed urinary Ca, Zn and serum Cu levels of the study group to be significantly higher (P<0.05) than those of he control group. Serum Ca and Se levels of study group were significantly lower (P<0.05) than those of control group. Conclusion: There were higher urinary Zn and serum Cu concentrations in bladder carcinoma cases. Bladder carcinoma may be associated with Ca metabolic disorder, leading to higher urinary Ca and lower serum Ca. Low serum Se and smoking appear to be other risk factors for bladder carcinoma in China.
Zhan-Li Shi,Dao-Hui Xiang,Hao-Ren Feng,Bang-Fu Wu,Zhi-Meng Zhang,Guo-Fu Gao,Bo Zhao 한국정밀공학회 2021 International Journal of Precision Engineering and Vol.22 No.10
SiCp/Al composites have been widely used in many fields due to their excellent mechanical properties. However, the addition of reinforced phase SiC particles makes the overall properties of the composites hard and brittle, which brings great challenges to milling. Ultrasonic vibration-assisted processing technology has great advantages in processing hard and brittle materials. However, the process of rupture of SiC particles cannot be effectively observed during the test processing, and a large number of tests increase the cost of the test. The combination of finite element analysis and experiment was used to study the machining performance of High-volume fraction SiCp/Al composites in longitudinal-torsional ultrasonicassisted milling (LTUAM), and its feasibility was evaluated by comparing with conventional Milling (CM). By analyzing the trajectories of cutting edges in ultrasonic-assisted milling, It was found that ultrasonic frequency determines the time of periodic contact-separation between chisel edge and workpiece, and ultrasonic amplitude determines the maximum distance of contact-separation. Using ABAQUS finite element software, a polygon SiC particles model with a high-volume fraction was established to investigate the SiC particles crushing process under different ultrasonic-assisted milling conditions. The results showed that high-frequency ultrasonic-assisted milling could soften SiCp/Al composites, and the structural integrity of silicon carbide particles could be better maintained under appropriate ultrasonic amplitudes, reducing the probability of fragmentation. The removal mode was mainly plastic removal or crushing into small particles. The surface roughness value and milling force were reduced, improving the surface quality of the processed composite material. The conclusions of the milling test were basically consistent with the simulation results, which prove the correctness and feasibility of the simulation results
Peng, Yong,Guo, Cong-Shan,Li, Pan-Xia,Fu, Zhan-Zhao,Gao, Li-Ming,Di, Ya,Ju, Ya-Kun,Tian, Ru,Xue, Jia-Jia Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.10
Background: The objective was to study the effect of Scutellaria baicalensis Georgi ethanol extracts (SBGE) on immune and anti-oxidant function in U14 tumor-bearing mice. Materials and Methods: U14 tumor-bearing mice were randomly divided into eight groups: a control group, a cyclophosphamide (CTX) group, three dose groups of SBGEI (high, medium, low), and three dose groups of SBGEII (high, medium, low). After two weeks, the thymus and spleen weight indices of mice bearing U14 cervical cancer were calculated. Enzyme linked immunosorbent assays (ELISA) was used to determine the levels of serum IL-2, TNF-${\alpha}$, IL-8, and PCNA. MDA activity and SOD activity in plasma were measured with detection kits. Results: In the SBGE groups, thymus weight and spleen weight indices of U14 tumor-bearing mice were significantly higher than in the control group or CTX group (p<0.05). Compared to control group, the levels of serum IL-2 and TNF-${\alpha}$ in U14 tumor-bearing mice increased significantly, whereas the contents of serum IL-8 and PCNA decreased (p<0.05). The activity of SOD increased with the growing dose of SBGE, while the activity of MDA decreased significantly in the highe-rdose groups of SBGE. Conclusions: These findings suggested that SBGE, especially at high dose, 1000 mg/kg, showed significant immune and anti-oxidant effects infU14 tumor-bearing mice, which might be the mechanisms of SBGE inhibition of tumor growth.
Jeong, Lak Shin,Shantanu Pal,Choe, Seung Ah,Choi, Won Jun,Kenneth A. Jacobson,Zhan-Guo Gao,Athena M. Klutz,Xiyan Hou,Kim, Hea Ok,Lee, Hyuk Woo,Lee, Sang Kook,Dilip K. Tosh,Moon, Hyung Ryong 이화여자대학교 약학연구소 2009 藥學硏究論文集 Vol.- No.19
Novel D- and L-4´-thioadenosine derivatives lacking the 4´-hydroxymethyl moiety were synthesized, starting from D-mannose and D-gulonic γ-lactone, respectively, as potent and selective species-independent A₃ adenosine receptor (AR) antagonists. Among the novel 4´-truncated 2-H nucleosides tested, a N^(6)-(3-chlorobenzyl) derivative 7c was the most potent at the human A₃ AR (K_(i) = 1.5 nM), but a N^(6)-(3-bromobenzyl) derivative 7d showed the optimal species-independent binding affinity.
Lim, Moo Hong,Kim, Hea Ok,Moon, Hyung Ryoung,Lee, Seung Jin,Chun, Moon Woo,Gao, Zhan-Guo,Melman, Neli,Jacobson, Kenneth A.,Kim, Joong Hyup,Jeong, Lak Shin 梨花女子大學校 藥學硏究所 2003 藥學硏究論文集 Vol.- No.12
Several 3'-fluoro analogues, la, lb, and lc of selective and potent adenosine A₃ receptor agonist, Cl-IB-MECA were synthesized from D-xylose via highly regioselective opening of lyxo-epoxides, 8a and 8b with fluoride anion. Compared to the high binding affinity of CI-IB-MECA to the A₃ adenosine receptor, the corresponding 3'-fluoro derivative showed remarkably decreased binding affinity, indicating that 3'-hydroxyl group acts as hydrogen bonding acceptor, not hydrogen bonding donor like fluorineatom in binding to the A₃ adenosine receptor.
Jeong, Lak Shin,Choe, Seung Ah,Gunaga, Prashantha,Kim, Hea Ok,Lee, Hyuk Woo,Lee, Sang Kook,Tosh, Dilip K.,Patel, Amit,Palaniappan, Krishnan K.,Gao, Zhan-Guo,Jacobson, Kenneth A.,Moon, Hyung Ryong 이화여자대학교 약학연구소 2008 藥學硏究論文集 Vol.- No.18
Truncated D-4'-thioadenosine derivatives lacking the 4'-hydroxymethylene moiety were synthesized starting from D-mannose, using cyclization to the 4-thiosugar and one-step conversion of the diol to the acetate as key steps At the human A₃ adenosine receptor (AR), N^(6)-substituted purine analogues bound potently and selectively and acted as antagonists in a cyclic AMP functional assay An N^(6)-(3-chlorobenzyl)purine analogue 9b displayed a K, value of 1 66 nM at the human A₃ AR Thus, truncated D-4'-thioadenosine is an excellent template for Ihe design of novel A₃ AR antagonists to act at both human and murine species.
Stereoselective Synthesis of 1'-Functionalized-4'-Thionucleosides
Jeong, Lak Shin,Gunaga, Prashantha,Kim, Hea Ok,Tosh, Dilip K.,Lee, Hyuk Woo,Choe, Seung Ah,Moon, Hyung Ryong,Gao, Zhan-Guo,Jacobson, Kenneth A.,Chun, Moon Woo Taylor Francis 2007 NUCLEOSIDES NUCLEOTIDES AND NUCLEIC ACIDS Vol. No.
<P> Stereoselective functionalization of the 1'-position of 4'-thionucleosides was achieved using a stereoselective SN2 reaction controlled by 5-membered ring coordination.</P>
Nayak, Akshata,Chandra, Girish,Hwang, Inah,Kim, Kyunglim,Hou, Xiyan,Kim, Hea Ok,Sahu, Pramod K.,Roy, Kuldeep K.,Yoo, Jakyung,Lee, Yoonji,Cui, Minghua,Choi, Sun,Moss, Steven M.,Phan, Khai,Gao, Zhan-Guo American Chemical Society 2014 Journal of medicinal chemistry Vol.57 No.4
<P/><P>Truncated <I>N</I><SUP>6</SUP>-substituted-(<I>N</I>)-methanocarba-adenosine derivatives with 2-hexynyl substitution were synthesized to examine parallels with corresponding 4′-thioadenosines. Hydrophobic N<SUP>6</SUP> and/or C2 substituents were tolerated in A<SUB>3</SUB>AR binding, but only an unsubstituted 6-amino group with a C2-hexynyl group promoted high hA<SUB>2A</SUB>AR affinity. A small hydrophobic alkyl (<B>4b</B> and <B>4c</B>) or <I>N</I><SUP>6</SUP>-cycloalkyl group (<B>4d</B>) showed excellent binding affinity at the hA<SUB>3</SUB>AR and was better than an unsubstituted free amino group (<B>4a</B>). A<SUB>3</SUB>AR affinities of 3-halobenzylamine derivatives <B>4f</B>–<B>4i</B> did not differ significantly, with <I>K</I><SUB>i</SUB> values of 7.8–16.0 nM. <I>N</I><SUP>6</SUP>-Methyl derivative <B>4b</B> (<I>K</I><SUB>i</SUB> = 4.9 nM) was a highly selective, low efficacy partial A<SUB>3</SUB>AR agonist. All compounds were screened for renoprotective effects in human TGF-β1-stimulated mProx tubular cells, a kidney fibrosis model. Most compounds strongly inhibited TGF-β1-induced collagen I upregulation, and their A<SUB>3</SUB>AR binding affinities were proportional to antifibrotic effects; <B>4b</B> was most potent (IC<SUB>50</SUB> = 0.83 μM), indicating its potential as a good therapeutic candidate for treating renal fibrosis.</P>