Multifunctional drug delivery systems(DDSs)have shown great prospects in overcoming the heterogeneous barrier of delivery drugs to the complex tumor microenvironment(TME).In this study,multifunctional AS/Ge-pNAB micro...Multifunctional drug delivery systems(DDSs)have shown great prospects in overcoming the heterogeneous barrier of delivery drugs to the complex tumor microenvironment(TME).In this study,multifunctional AS/Ge-pNAB microgels with dual-active targeting,triple environment responsiveness,and fluorescence imaging capability were prepared through a straightforward procedure.This was aimed to improve the antitumor therapeutic application of gambogic acid(GA)based on the biological characteristics of TME.The microgels have a uniform double-layer structure with aptamer in the outer layer which helps in recognizing receptors on the tumor cells.The GA loaded nano-herb exhibited environment-responsive drug release profiles under acidic pH,reductant and high temperature.The nano-herb significantly improved the accumulation of GA in tumor sites through the synergistic combination of the enhanced permeability and retention effect and dual-ligand mediated internalization.Then,it accelerated intracellular drug release and killed tumor cells.Therefore,the nano-herb had specific therapeutic effects on the tumor in vitro and in vivo as they remarkably inhibited tumor growth while depicting optimal biosafety and lower levels of off-target toxicity.Overall,these findings demonstrate the great potential of the multifunctional AS/Ge-pNAB microgels for precisely targeted GA delivery and open a new avenue for the facile preparation of multifunctional DDSs.展开更多
Stimulated Brillouin scattering(SBS)-induced mode distortion(MD)in high power narrow linewidth fiber amplifiers has been implemented,and the origin has been investigated from the aspect of the evolution of the optical...Stimulated Brillouin scattering(SBS)-induced mode distortion(MD)in high power narrow linewidth fiber amplifiers has been implemented,and the origin has been investigated from the aspect of the evolution of the optical spectrum,spatial beam profiles,and temporal-frequency domain characteristics.展开更多
A series of(R)-2-phenyl-4,5-dihydrothiazole-4-carboxamide derivatives containing a sulfur ether moiety were synthesized and characterized on the basis of NMR and elemental analysis(EA). The crystal structure of(R)-N-(...A series of(R)-2-phenyl-4,5-dihydrothiazole-4-carboxamide derivatives containing a sulfur ether moiety were synthesized and characterized on the basis of NMR and elemental analysis(EA). The crystal structure of(R)-N-(2-methyl-1-(methylthio)propan-2-yl)-2-(4-nitrophenyl)-4,5-dihydrothiazole-4-carboxamide(13 d) was determined to show R configuration. The bioasssy results indicated that most title compounds displayed good and broad spectrum antifungal activities against several phytopathogenic fungi. The structure activity relationships were discussed. Based on the antifungal activity of title compounds against Phytophthora capsici, a CoMSIA calculation was performed to establish a 3 D-QSAR model, which revealed that electrostatic and hydrophobic fields were the two most significant factors for antifungal activity. According to the established 3D-QSAR model, structure optimization was carried out to find(R)-N-((R)-1-(methylthio)propan-2-yl)-2-(p-tolyl)-4,5-dihydrothiazole-4-carboxamide(15 h)with excellent activity against Phytophthora capsici, thus emerging as a new lead compound for novel antiphytopathogenic fungus agent development.展开更多
The experimental investigation of mode distortion induced by stimulated Raman scattering(SRS)in a high-power fiber amplifier,which includes the evolutions of optical spectra,spatial beam profiles,and time-frequency ch...The experimental investigation of mode distortion induced by stimulated Raman scattering(SRS)in a high-power fiber amplifier,which includes the evolutions of optical spectra,spatial beam profiles,and time-frequency characteristics,has been carried out in detail.Temporal-frequency characteristics have been studied for the first time,to the best of our knowledge,by using a low-speed camera and high-speed photodiode traces,which revealed that temporal-frequency characteristics of SRS-induced mode distortion are different from traditional dynamic mode instability(MI).The experimental results show that the output beam profile remains stable before the mode distortion occurs and fluctuates obviously after the onset of SRS-induced MI but on a time scale of seconds,which is much lower than that of Yb-gain-induced MI featuring millisecond-level beam profile fluctuation.It also shows that the mode distortion became measurable in company with the onset of inter-mode four-wave mixing(IM-FWM)when the ratio of Raman light reaches 3%;further,the beam quality factor M2degrades gradually from 1.4 to 2.1 as the ratio of Raman light increases.The mode distortion is accompanied by an obvious temperature increase of the output passive fiber,which further confirms that the mode distortion originates from SRS.The cause of the mode distortion induced by SRS has been explained in the context of core-pumped SRS effect,and the investigation on the accompanying IM-FWM effect indicates that the main content of the SRSinduced high-order mode is the LP21 mode.展开更多
基金financially supported by the National Natural Science Foundation of China(Nos.21907076 and 31901908)Natural Science Foundation of Tianjin(No.22JCQNJC01570)Scientific Project of Tianjin Municipal Education Commission(No.2022KJ026).
文摘Multifunctional drug delivery systems(DDSs)have shown great prospects in overcoming the heterogeneous barrier of delivery drugs to the complex tumor microenvironment(TME).In this study,multifunctional AS/Ge-pNAB microgels with dual-active targeting,triple environment responsiveness,and fluorescence imaging capability were prepared through a straightforward procedure.This was aimed to improve the antitumor therapeutic application of gambogic acid(GA)based on the biological characteristics of TME.The microgels have a uniform double-layer structure with aptamer in the outer layer which helps in recognizing receptors on the tumor cells.The GA loaded nano-herb exhibited environment-responsive drug release profiles under acidic pH,reductant and high temperature.The nano-herb significantly improved the accumulation of GA in tumor sites through the synergistic combination of the enhanced permeability and retention effect and dual-ligand mediated internalization.Then,it accelerated intracellular drug release and killed tumor cells.Therefore,the nano-herb had specific therapeutic effects on the tumor in vitro and in vivo as they remarkably inhibited tumor growth while depicting optimal biosafety and lower levels of off-target toxicity.Overall,these findings demonstrate the great potential of the multifunctional AS/Ge-pNAB microgels for precisely targeted GA delivery and open a new avenue for the facile preparation of multifunctional DDSs.
基金National Natural Science Foundation of China(62205317).
文摘Stimulated Brillouin scattering(SBS)-induced mode distortion(MD)in high power narrow linewidth fiber amplifiers has been implemented,and the origin has been investigated from the aspect of the evolution of the optical spectrum,spatial beam profiles,and temporal-frequency domain characteristics.
基金financially supported by the Scientific Project of Tianjin Municipal Education Commission(No. 2018KJ008)Tianjin Natural Science Foundation(No. 16JCYBJC29400)
文摘A series of(R)-2-phenyl-4,5-dihydrothiazole-4-carboxamide derivatives containing a sulfur ether moiety were synthesized and characterized on the basis of NMR and elemental analysis(EA). The crystal structure of(R)-N-(2-methyl-1-(methylthio)propan-2-yl)-2-(4-nitrophenyl)-4,5-dihydrothiazole-4-carboxamide(13 d) was determined to show R configuration. The bioasssy results indicated that most title compounds displayed good and broad spectrum antifungal activities against several phytopathogenic fungi. The structure activity relationships were discussed. Based on the antifungal activity of title compounds against Phytophthora capsici, a CoMSIA calculation was performed to establish a 3 D-QSAR model, which revealed that electrostatic and hydrophobic fields were the two most significant factors for antifungal activity. According to the established 3D-QSAR model, structure optimization was carried out to find(R)-N-((R)-1-(methylthio)propan-2-yl)-2-(p-tolyl)-4,5-dihydrothiazole-4-carboxamide(15 h)with excellent activity against Phytophthora capsici, thus emerging as a new lead compound for novel antiphytopathogenic fungus agent development.
基金National Natural Science Foundation of China(61905226)National Key Research and Development Program of China(2017YFB1104401)。
文摘The experimental investigation of mode distortion induced by stimulated Raman scattering(SRS)in a high-power fiber amplifier,which includes the evolutions of optical spectra,spatial beam profiles,and time-frequency characteristics,has been carried out in detail.Temporal-frequency characteristics have been studied for the first time,to the best of our knowledge,by using a low-speed camera and high-speed photodiode traces,which revealed that temporal-frequency characteristics of SRS-induced mode distortion are different from traditional dynamic mode instability(MI).The experimental results show that the output beam profile remains stable before the mode distortion occurs and fluctuates obviously after the onset of SRS-induced MI but on a time scale of seconds,which is much lower than that of Yb-gain-induced MI featuring millisecond-level beam profile fluctuation.It also shows that the mode distortion became measurable in company with the onset of inter-mode four-wave mixing(IM-FWM)when the ratio of Raman light reaches 3%;further,the beam quality factor M2degrades gradually from 1.4 to 2.1 as the ratio of Raman light increases.The mode distortion is accompanied by an obvious temperature increase of the output passive fiber,which further confirms that the mode distortion originates from SRS.The cause of the mode distortion induced by SRS has been explained in the context of core-pumped SRS effect,and the investigation on the accompanying IM-FWM effect indicates that the main content of the SRSinduced high-order mode is the LP21 mode.
