N,N’-diphenylurea reacted with phosphorus trichloride and phenyl dicklorophospbane giving theheterocyclic compounds 1 and 2 with a direct phosphorus-phosphorus bond (P-P bond ), respectively. The newcompounds were ch...N,N’-diphenylurea reacted with phosphorus trichloride and phenyl dicklorophospbane giving theheterocyclic compounds 1 and 2 with a direct phosphorus-phosphorus bond (P-P bond ), respectively. The newcompounds were characterized by elementary analysis, NMR and IR spectra. The results or preliminary bioassay showed that these heterocycles possess selective herbicidal activity at 1.5 kg/hm2.展开更多
The immunomodulation of several charged synthetic polymers containing phosphorus in the backbone was studied in vitro through examining their inhibition or promotion effect on the proliferation of both T and B lymphoc...The immunomodulation of several charged synthetic polymers containing phosphorus in the backbone was studied in vitro through examining their inhibition or promotion effect on the proliferation of both T and B lymphocytes. It is found that polymers based on long chain alkyl ester of tyrosine exhibit immunomodulative activity. Negatively charged polymers show stimulative activiactivity on LPS-induced B lymphocytes proliferation. Positively charged polymers exhibit inhibitory activity on both Con A-induced T lymphocytes and LPS-induced B lymphocytes proliferation.展开更多
Based on specific host-guest interactions between amine-modified ?-cyclodextrin(CD-TAEA) and functional adamantane(AD) derivatives, a module-template strategy has been proposed for the construction of low-molecular-we...Based on specific host-guest interactions between amine-modified ?-cyclodextrin(CD-TAEA) and functional adamantane(AD) derivatives, a module-template strategy has been proposed for the construction of low-molecular-weight cationic assemblies for gene transport. This strategy offers great flexibility in terms of the introduction of mono- or multi-functionality by the inclusion of one or more adamantane-based modules with the desired functionalities. As proof of concept, phenylboronic acid(PB) containing adamantane(PB-AD) was used as a model module in the hope of offering enhanced cytosolic delivery in consideration of the special affinity of PB groups with cell membranes. The physicochemical properties of the complexes formed with plasmid DNA, such as particle size, zeta potential and morphology were investigated. Confocal laser scanning microscopy and flow cytometry experiments demonstrated the important contribution of the functional PB-AD module to the considerably enhanced intracellular internalization and uptake by cellular nuclei. Compared to the parent CD-TAEA, PB-AD/CDTAEA assemblies mediated higher transfection rates, which were even comparable to that of PEI25K. In addition, PB-AD/CDTAEA displayed much lower cytotoxicity than PEI25K in both 293T and HeLa cell lines. The encouraging results suggest that CD-TAEA can be developed as a powerful template capable of readily accommodating various AD-based modules giving versatile functionalities for improved transfection.展开更多
A novel camptothecin(CPT) prodrug was successfully synthesized by conjugating CPT to adamantanecarboxylic acid(AD) via a cleavable disulfide linkage. The resulting CPT-ss-AD prodrug could act as a low molecular weight...A novel camptothecin(CPT) prodrug was successfully synthesized by conjugating CPT to adamantanecarboxylic acid(AD) via a cleavable disulfide linkage. The resulting CPT-ss-AD prodrug could act as a low molecular weight gelator to form molecular gels in water/water-miscible organic solvent mixture. Meanwhile, biodegradable amphiphilic block copolymer m PEG-b-P(MAC-co-DTC)(PPMD) was also employed as an organic framework together with CPT-ss-AD to form gel structure. CPT-ss-AD/PPMD gel exhibited less compact molecular arrangement but much more stability than CPT-ss-AD gel. The two kinds of gels could effectively release the original CPT under reductive condition at a near-constant rate without any initial burst. As compared to CPT-ss-AD single-component gel, the two-component gel, CPT-ss-AD/PPMD, had a significantly higher release rate of CPT, while 3-[4,5-dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide(MTT) assays also indicated highly potent cytotoxic activity against He La cells.展开更多
文摘N,N’-diphenylurea reacted with phosphorus trichloride and phenyl dicklorophospbane giving theheterocyclic compounds 1 and 2 with a direct phosphorus-phosphorus bond (P-P bond ), respectively. The newcompounds were characterized by elementary analysis, NMR and IR spectra. The results or preliminary bioassay showed that these heterocycles possess selective herbicidal activity at 1.5 kg/hm2.
文摘The immunomodulation of several charged synthetic polymers containing phosphorus in the backbone was studied in vitro through examining their inhibition or promotion effect on the proliferation of both T and B lymphocytes. It is found that polymers based on long chain alkyl ester of tyrosine exhibit immunomodulative activity. Negatively charged polymers show stimulative activiactivity on LPS-induced B lymphocytes proliferation. Positively charged polymers exhibit inhibitory activity on both Con A-induced T lymphocytes and LPS-induced B lymphocytes proliferation.
基金supported by the National Basic Research Program of China(2011CB606202)the National Natural Science Foundation of China(21174110)+1 种基金the Ministry of Education of China(20120141130003)the Fundamental Research Funds for the Central Universities(2012203020210)
文摘Based on specific host-guest interactions between amine-modified ?-cyclodextrin(CD-TAEA) and functional adamantane(AD) derivatives, a module-template strategy has been proposed for the construction of low-molecular-weight cationic assemblies for gene transport. This strategy offers great flexibility in terms of the introduction of mono- or multi-functionality by the inclusion of one or more adamantane-based modules with the desired functionalities. As proof of concept, phenylboronic acid(PB) containing adamantane(PB-AD) was used as a model module in the hope of offering enhanced cytosolic delivery in consideration of the special affinity of PB groups with cell membranes. The physicochemical properties of the complexes formed with plasmid DNA, such as particle size, zeta potential and morphology were investigated. Confocal laser scanning microscopy and flow cytometry experiments demonstrated the important contribution of the functional PB-AD module to the considerably enhanced intracellular internalization and uptake by cellular nuclei. Compared to the parent CD-TAEA, PB-AD/CDTAEA assemblies mediated higher transfection rates, which were even comparable to that of PEI25K. In addition, PB-AD/CDTAEA displayed much lower cytotoxicity than PEI25K in both 293T and HeLa cell lines. The encouraging results suggest that CD-TAEA can be developed as a powerful template capable of readily accommodating various AD-based modules giving versatile functionalities for improved transfection.
基金Supported by the Natural Science Foundation of Hubei Province of China(2014CFB696)the Opening Project of Key Laboratory of Biomedical Polymers of Ministry of Education at Wuhan University(20150102)the National Natural Science Foundation of China(21074098)
文摘A novel camptothecin(CPT) prodrug was successfully synthesized by conjugating CPT to adamantanecarboxylic acid(AD) via a cleavable disulfide linkage. The resulting CPT-ss-AD prodrug could act as a low molecular weight gelator to form molecular gels in water/water-miscible organic solvent mixture. Meanwhile, biodegradable amphiphilic block copolymer m PEG-b-P(MAC-co-DTC)(PPMD) was also employed as an organic framework together with CPT-ss-AD to form gel structure. CPT-ss-AD/PPMD gel exhibited less compact molecular arrangement but much more stability than CPT-ss-AD gel. The two kinds of gels could effectively release the original CPT under reductive condition at a near-constant rate without any initial burst. As compared to CPT-ss-AD single-component gel, the two-component gel, CPT-ss-AD/PPMD, had a significantly higher release rate of CPT, while 3-[4,5-dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide(MTT) assays also indicated highly potent cytotoxic activity against He La cells.
