The Experts below are selected from a list of 132 Experts worldwide ranked by ideXlab platform
Wei Tang - One of the best experts on this subject based on the ideXlab platform.
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Caffeoyl Pyrrolidine Derivative LY52 inhibits hepatocellular carcinoma invasion via suppressing matrix metalloproteinase-2
Hepatology international, 2010Co-Authors: Xin Zhao, Yoshinori Inagaki, Norihiro Kokudo, Jiahong Dong, Wei TangAbstract:Purpose In this study, we examined the effects of LY52, a caffeoyl Pyrrolidine Derivative designed to fit the S′1 active pocket of gelatinases, on the expressions of matrix metalloproteinases and invasion abilities of hepatocellular carcinoma cells.
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using caffeoyl Pyrrolidine Derivative ly52 a potential inhibitor of matrix metalloproteinase 2 to suppress tumor invasion and metastasis
International Journal of Molecular Medicine, 2006Co-Authors: Yunxia Yuan, Minghui Chen, Shuxiang Cui, Masatoshi Makuuchi, Munehiro Nakata, Zhigang Tian, Qian Guo, Ruoyan Gai, Wei TangAbstract:LY52 is a caffeoyl Pyrrolidine Derivative designed to fit the S'1 active pocket of gelatinases that act in tumor invasion and metastasis. Herein, we examined the effects of LY52 on expression of matrix metalloproteinase (MMP)-2 expression in human breast cancer MDA-MB-231 cells and on in vitro invasion and in vivo metastasis. LY52 significantly blocked MMP-2 activity as evidenced by a decrease in the degradation of succinylated gelatin. Gelatin zymography analysis showed that LY52 (0.1-200 microg/ml) inhibited expression of active MMP-2 in concanavalin A-stimulated MDA-MB-231 cells. Inhibition of MMP-2 expression was also observed in tissue of tumor xenografts in mice that were orally administered LY52 (25 or 100 mg/kg). Furthermore, LY52 displayed an inhibitory effect on in vitro invasion of MDA-MB-231 cells and pulmonary metastasis of B16F10 murine melanoma cells in mice without significant toxic effects. These results suggest that LY52 is a potential MMP-2 inhibitor that may effectively suppress tumor invasion and metastasis.
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caffeoyl Pyrrolidine Derivative ly52 inhibits tumor invasion and metastasis via suppression of matrix metalloproteinase activity
Anticancer Research, 2006Co-Authors: Yunxia Yuan, Minghui Chen, Shuxiang Cui, Hong Meng, Masatoshi Makuuchi, Munehiro Nakata, Wei TangAbstract:Background: LY52 is a caffeoyl Pyrrolidine Derivative designed to fit and extend into the active pocket of matrix metalloproteinase (MMP). In this study, the effects of LY52 on MMP-2 and MMP-9 activities and tumor invasion and metastasis were examined. Materials and Methods: MMP expression in SKOV3 cells was analyzed by gelatin zymography. The anti-invasion and anti-metastasis abilities of LY52 were evaluated with penetration of SKOV3 cells through Matrigel- coated membrane in vitro and pulmonary metastasis of Lewis lung carcinoma in mice, respectively. Results: LY52 significantly blocked the proteolytic activity of gelatinase. Gelatin zymography revealed that MMP-2 and MMP-9 expressions in SKOV3 cells were reduced in the presence of LY52. LY52 also suppressed SKOV3 cell invasion in vitro. Furthermore, a significant inhibition of pulmonary metastasis of Lewis lung carcinoma cells was observed in LY52-administrated mice. Conclusion: LY52 might suppress invasion and metastasis of carcinoma cells via inhibition of MMP-2 and MMP-9 proteolytic activities. Matrix metalloproteinases (MMPs) play a crucial role in the development and metastatic spread of cancer. One of the earliest events in the metastatic spread of cancer is invasion through basement membrane and proteolytic degradation of extracellular matrix (ECM) proteins, such as collagens,
Takeo Kawabata - One of the best experts on this subject based on the ideXlab platform.
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a cyclochiral conformational motif constructed using a robust hydrogen bonding network
Journal of the American Chemical Society, 2013Co-Authors: Kenji Mishiro, Takumi Furuta, Takahiro Sasamori, Kazuhiro Hayashi, Norihiro Tokitoh, Shiroh Futaki, Takeo KawabataAbstract:A novel conformational motif constructed with a robust intramolecular hydrogen-bonding (H-bonding) network was discovered. A Pyrrolidine Derivative possessing four identical amide substituents at C(2) and C(5) formed a strong intramolecular H-bonding network consisting of all the amide groups. This conformation yielded a cyclochiral structure with a handedness that depended on the directionality of the H-bonding network. The most stable compound was isolated and applied to the acylative kinetic resolution of secondary alcohol. The handedness of the H-bonding network was biased by the presence of chiral substituents, and the preferred direction could be switched under an external stimulus. A structural analysis using NMR, X-ray crystallography, and theoretical calculation techniques indicated that the conformation of the substituents was highly ordered and depended on the directionality of the H-bonding network.
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A Cyclochiral Conformational Motif Constructed Using a Robust Hydrogen-Bonding Network
2013Co-Authors: Kenji Mishiro, Takumi Furuta, Takahiro Sasamori, Kazuhiro Hayashi, Norihiro Tokitoh, Shiroh Futaki, Takeo KawabataAbstract:A novel conformational motif constructed with a robust intramolecular hydrogen-bonding (H-bonding) network was discovered. A Pyrrolidine Derivative possessing four identical amide substituents at C(2) and C(5) formed a strong intramolecular H-bonding network consisting of all the amide groups. This conformation yielded a cyclochiral structure with a handedness that depended on the directionality of the H-bonding network. The most stable compound was isolated and applied to the acylative kinetic resolution of secondary alcohol. The handedness of the H-bonding network was biased by the presence of chiral substituents, and the preferred direction could be switched under an external stimulus. A structural analysis using NMR, X-ray crystallography, and theoretical calculation techniques indicated that the conformation of the substituents was highly ordered and depended on the directionality of the H-bonding network
Chunhui Huang - One of the best experts on this subject based on the ideXlab platform.
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The synthesis and fluorescence of a methoxy-phenyl substituted C60-Pyrrolidine Derivative
Chinese Journal of Chemistry, 2010Co-Authors: Dejian Zhou, Liangbing Gan, Chuping Luo, Chunhui Huang, Guangqing YaoAbstract:A new 4-methoxyphenyl substituted C60-Pyrrolidine Derivative, C60(C10H13NO) (1), was prepared and its room-temperature fluorescence waa studied. Its fluorescence intensity is three times stronger than that of C60. Its singlet energy was estimated to be 25 kJ/mol lower than that of C60. The fluorescence lifetime was determined to be 2.1±0.3 ns by using the frequency domain method. The fluorescence quenching by concentration and aromatic electron donor: N, N-dimethyl aniline (DMA) wan investigated. Data show that its fluorescence could not be quenched by DMA.
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A new 4-acetalphenyl C60-Pyrrolidine Derivative and its Langmuir-Blodgett film study
Solid State Communications, 1997Co-Authors: Dejian Zhou, Liangbing Gan, Chuping Luo, Chunhui HuangAbstract:Abstract A new 4-acetalphenyl substituted C60-Pyrrolidine Derivative C60(C12H17NO2) (1) was prepared and characterized by 1H-NMR, 13C-NMR, FDMS, FTIR and UV-vis spectra. Its Langmuir film study indicates that it can form stable monolayer at the air/water interface, which can be transferred onto hydrophilic substrates to form LB films. The LB monolayer exhibits weak second harmonic generation (SHG). Its second-order susceptibility χpp(2) is evaluated to be 6 × 10−9 esu.
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synthesis langmuir blodgett deposition and optical characterization of a 4 acetalphenyl substituted c60 Pyrrolidine Derivative c60 c12h17no2
Journal of the Chemical Society Faraday Transactions, 1997Co-Authors: Dejian Zhou, Liangbing Gan, Chuping Luo, Geoffrey J Ashwell, Rakesh Rajan, Chunhui HuangAbstract:A new 4-acetalphenyl-substituted C 60 -Pyrrolidine Derivative, C 60 (C 12 H 17 NO 2 ) (1), has been prepared and its Langmuir films, with and without 22-tricosenoic acid [CH 2 CH–(CH 2 ) 20 CO 2 H (TA)], at the air/water interface have been investigated. Pure 1 forms monolayers more easily than the parent molecule, C 60 , and can be transferred onto solid substrates to form Langmuir–Blodgett (LB) films. The mixed Langmuir films of 1 and TA were transferred onto hydrophilically pretreated quartz, glass substrates and silicon wafers. Reflectometric measurement of a 63-layer 1:2 mixed film on a silicon wafer using an He–Ne laser (λ = 632.8 nm) provided a film thickness and refractive index of 171 nm and 1.73, respectively. Weak second harmonic generation (SHG) from LB monolayers of pure 1 and 1:2 and 1:4 mixed LB monolayer films of 1 and TA was observed. The second-order susceptibilities, χ pp (2) , were evaluated to be in the range (4–6)×10 −9 esu.
Yunxia Yuan - One of the best experts on this subject based on the ideXlab platform.
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using caffeoyl Pyrrolidine Derivative ly52 a potential inhibitor of matrix metalloproteinase 2 to suppress tumor invasion and metastasis
International Journal of Molecular Medicine, 2006Co-Authors: Yunxia Yuan, Minghui Chen, Shuxiang Cui, Masatoshi Makuuchi, Munehiro Nakata, Zhigang Tian, Qian Guo, Ruoyan Gai, Wei TangAbstract:LY52 is a caffeoyl Pyrrolidine Derivative designed to fit the S'1 active pocket of gelatinases that act in tumor invasion and metastasis. Herein, we examined the effects of LY52 on expression of matrix metalloproteinase (MMP)-2 expression in human breast cancer MDA-MB-231 cells and on in vitro invasion and in vivo metastasis. LY52 significantly blocked MMP-2 activity as evidenced by a decrease in the degradation of succinylated gelatin. Gelatin zymography analysis showed that LY52 (0.1-200 microg/ml) inhibited expression of active MMP-2 in concanavalin A-stimulated MDA-MB-231 cells. Inhibition of MMP-2 expression was also observed in tissue of tumor xenografts in mice that were orally administered LY52 (25 or 100 mg/kg). Furthermore, LY52 displayed an inhibitory effect on in vitro invasion of MDA-MB-231 cells and pulmonary metastasis of B16F10 murine melanoma cells in mice without significant toxic effects. These results suggest that LY52 is a potential MMP-2 inhibitor that may effectively suppress tumor invasion and metastasis.
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caffeoyl Pyrrolidine Derivative ly52 inhibits tumor invasion and metastasis via suppression of matrix metalloproteinase activity
Anticancer Research, 2006Co-Authors: Yunxia Yuan, Minghui Chen, Shuxiang Cui, Hong Meng, Masatoshi Makuuchi, Munehiro Nakata, Wei TangAbstract:Background: LY52 is a caffeoyl Pyrrolidine Derivative designed to fit and extend into the active pocket of matrix metalloproteinase (MMP). In this study, the effects of LY52 on MMP-2 and MMP-9 activities and tumor invasion and metastasis were examined. Materials and Methods: MMP expression in SKOV3 cells was analyzed by gelatin zymography. The anti-invasion and anti-metastasis abilities of LY52 were evaluated with penetration of SKOV3 cells through Matrigel- coated membrane in vitro and pulmonary metastasis of Lewis lung carcinoma in mice, respectively. Results: LY52 significantly blocked the proteolytic activity of gelatinase. Gelatin zymography revealed that MMP-2 and MMP-9 expressions in SKOV3 cells were reduced in the presence of LY52. LY52 also suppressed SKOV3 cell invasion in vitro. Furthermore, a significant inhibition of pulmonary metastasis of Lewis lung carcinoma cells was observed in LY52-administrated mice. Conclusion: LY52 might suppress invasion and metastasis of carcinoma cells via inhibition of MMP-2 and MMP-9 proteolytic activities. Matrix metalloproteinases (MMPs) play a crucial role in the development and metastatic spread of cancer. One of the earliest events in the metastatic spread of cancer is invasion through basement membrane and proteolytic degradation of extracellular matrix (ECM) proteins, such as collagens,
Kenji Mishiro - One of the best experts on this subject based on the ideXlab platform.
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a cyclochiral conformational motif constructed using a robust hydrogen bonding network
Journal of the American Chemical Society, 2013Co-Authors: Kenji Mishiro, Takumi Furuta, Takahiro Sasamori, Kazuhiro Hayashi, Norihiro Tokitoh, Shiroh Futaki, Takeo KawabataAbstract:A novel conformational motif constructed with a robust intramolecular hydrogen-bonding (H-bonding) network was discovered. A Pyrrolidine Derivative possessing four identical amide substituents at C(2) and C(5) formed a strong intramolecular H-bonding network consisting of all the amide groups. This conformation yielded a cyclochiral structure with a handedness that depended on the directionality of the H-bonding network. The most stable compound was isolated and applied to the acylative kinetic resolution of secondary alcohol. The handedness of the H-bonding network was biased by the presence of chiral substituents, and the preferred direction could be switched under an external stimulus. A structural analysis using NMR, X-ray crystallography, and theoretical calculation techniques indicated that the conformation of the substituents was highly ordered and depended on the directionality of the H-bonding network.
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A Cyclochiral Conformational Motif Constructed Using a Robust Hydrogen-Bonding Network
2013Co-Authors: Kenji Mishiro, Takumi Furuta, Takahiro Sasamori, Kazuhiro Hayashi, Norihiro Tokitoh, Shiroh Futaki, Takeo KawabataAbstract:A novel conformational motif constructed with a robust intramolecular hydrogen-bonding (H-bonding) network was discovered. A Pyrrolidine Derivative possessing four identical amide substituents at C(2) and C(5) formed a strong intramolecular H-bonding network consisting of all the amide groups. This conformation yielded a cyclochiral structure with a handedness that depended on the directionality of the H-bonding network. The most stable compound was isolated and applied to the acylative kinetic resolution of secondary alcohol. The handedness of the H-bonding network was biased by the presence of chiral substituents, and the preferred direction could be switched under an external stimulus. A structural analysis using NMR, X-ray crystallography, and theoretical calculation techniques indicated that the conformation of the substituents was highly ordered and depended on the directionality of the H-bonding network
