The Experts below are selected from a list of 6357 Experts worldwide ranked by ideXlab platform
X. X. Zhu - One of the best experts on this subject based on the ideXlab platform.
-
bitter sweet polymeric micelles formed by block copolymers from glucosamine and Cholic Acid
Biomacromolecules, 2017Co-Authors: Kun Zhang, Yongguang Jia, Ihuang Tsai, Satu Strandman, Li Ren, Liangzhi Hong, Guangzhao Zhang, Ying Guan, Yongjun Zhang, X. X. ZhuAbstract:Natural compounds glucosamine and Cholic Acid have been used to make acrylic monomers which are subsequently used to prepare amphiphilic block copolymers by reversible addition–fragmentation chain transfer (RAFT) polymerization. Despite the striking difference in polarity and solubility, three diblock copolymers consisting of glucosamine and Cholic Acid pendants with different hydrophilic and hydrophobic chain lengths have been synthesized without the use of protecting groups. They are shown to self-assemble into polymeric micelles with a “bitter” bile Acid core and “sweet” sugar shell in aqueous solutions, as evidenced by dynamic light scattering and transmission electron microscopy. The critical micelle concentration varies with the hydrophobic/hydrophilic ratio, ranging from 0.62 to 1.31 mg/L. Longer chains of polymers induced the formation of larger micelles in range of 50–70 nm. These micelles can solubilize hydrophobic compounds such as Nile Red in aqueous solutions. Their loading capacity mainly de...
-
thermo and ph responsive copolymers bearing Cholic Acid and oligo ethylene glycol pendants self assembly and ph controlled release
ACS Applied Materials & Interfaces, 2015Co-Authors: Yongguang Jia, X. X. ZhuAbstract:A family of block and random copolymers of norbornene derivatives bearing Cholic Acid and oligo(ethylene glycol) pendants were prepared in the presence of Grubbs’ catalyst. The phase transition temperature of the copolymers in aqueous solutions may be tuned by the variation of comonomer ratios and pH values. Both types of copolymers formed micellar nanostructures with a hydrophilic poly(ethylene glycol) shell and a hydrophobic core containing Cholic Acid residues. The micellar size increased gradually with increasing pH due to the deprotonation of the carboxylic Acid groups. These micelles were capable of encapsulating hydrophobic compounds such as Nile Red (NR). A higher hydrophobicity/hydrophilicity ratio in both copolymers resulted in a higher loading capacity for NR. With similar molecular weights and monomer compositions, the block copolymers showed a higher loading capacity for NR than the random copolymers. The NR-loaded micelles exhibited a pH-triggered release behavior. At pH 7.4 within 96 h, the...
-
self healing supramolecular hydrogel made of polymers bearing Cholic Acid and β cyclodextrin pendants
Chemistry of Materials, 2015Co-Authors: Yongguang Jia, X. X. ZhuAbstract:Natural compounds Cholic Acid and β-cyclodextrin are attached separately as pendant groups in a copolymer with N,N′-dimethylacrylamides. The formation of supramolecular hydrogels is induced by inclusion complex formation between Cholic Acid and β-cyclodextrin moieties as evidenced by rheological analysis and 1H NMR spectroscopy. Storage modulus of the hydrogel shows a maximum value when the molar ratio of Cholic Acid to β-cyclodextrin units is adjusted to 1:1. The concentration of the hydrogel can be as low as 5.5 wt %. Both shear-thickening and shear-thinning have been observed when the shear rate gradually increases from 0.01 to 100 s–1. The inclusion complexation renders the gel–sol process reversible under heating and cooling cycles. The self-healing of such hydrogels is observed and confirmed by step-strain rheological measurements. The dynamically reversible host–guest complexation provides reasonably good mechanical properties of the cross-linked polymer network. The natural origin of the constitue...
-
thermoresponsiveness of copolymers bearing Cholic Acid pendants induced by complexation with β cyclodextrin
Langmuir, 2014Co-Authors: Yongguang Jia, X. X. ZhuAbstract:Copolymers of N-alkylacrylamides and methacrylate bearing Cholic Acid pendant groups were synthesized via radical polymerization. The Cholic Acid pendant groups of such copolymers can form complexes with β-cyclodextrin, and the effect of complexation on their thermoresponsive properties was studied. The phase transition temperatures (transition from hydrophilic to hydrophobic state) of the copolymers gradually increase with the addition of β-cyclodextrin, due to the complexation of the Cholic Acid guest with the β-cyclodextrin host. The increase of the phase transition temperature may be reversed by the addition of a competing guest molecule, potassium 1-adamantylcarboxylate. The host–guest complexation provides a straightforward way to vary the thermoresponsive properties of such copolymers.
-
Multishape Memory Effect of Norbornene-Based Copolymers with Cholic Acid Pendant Groups
Macromolecules, 2012Co-Authors: Yu Shao, Christine Lavigueur, X. X. ZhuAbstract:Multishape memory copolymers were prepared through copolymerization of two norbornene derivatives: one based on Cholic Acid and the other on triethylene glycol monomethyl ether. The glass transitio...
Jingkang Shen - One of the best experts on this subject based on the ideXlab platform.
-
Novel liver-specific Cholic Acid-cytarabine conjugates with potent antitumor activities: Synthesis and biological characterization.
Acta pharmacologica Sinica, 2011Co-Authors: Danqi Chen, Xin Wang, Lin Chen, Ze-hong Miao, Jingkang ShenAbstract:Novel liver-specific Cholic Acid-cytarabine conjugates with potent antitumor activities: Synthesis and biological characterization
-
novel liver specific Cholic Acid cytarabine conjugates with potent antitumor activities synthesis and biological characterization
Acta Pharmacologica Sinica, 2011Co-Authors: Danqi Chen, Xin Wang, Lin Chen, Ze-hong Miao, Jingkang ShenAbstract:Cytarabine is an efficient anticancer agent for acute myelogenous leukemia, but with short plasma half-life and rapid deamination to its inactive metabolite. The aim of this study was to design and synthesize novel Cholic Acid-cytarabine conjugates to improve its pharmacokinetic parameters. The in vitro stability of novel Cholic Acid-cytarabine conjugates was investigated in simulated gastric and intestinal fluid, mouse blood and liver homogenate using HPLC. The portacaval samples of the conjugates were examined in male Sprague-Dawley rats using LC/MS, and in vivo distribution was examined in male Kunming mice using LC/MS. Antitumor activities were tested in HL60 cells using MTT assay. Cholic Acid-cytarabine compounds with four different linkers were designed and synthesized. All the four Cholic Acid-cytarabine conjugates could release cytarabine when incubated with the simulated gastric and intestinal fluid, mouse blood and liver homogenate. The conjugates 6, 12, and 16 were present in the portacaval samples, whereas the conjugate 7 was not detected. The conjugates 6 and 16 showed high specificity in targeting the liver (liver target index 34.9 and 16.3, respectively) and good absorption in vivo, as compared with cytarabine. In cytarabine-sensitive HL60 cells, the conjugates 6, 12, and 16 retained potent antitumor activities. Three novel Cholic Acid-cytarabine conjugates with good liver-targeting properties and absorption were obtained. Further optimization of the conjugates is needed in the future.
Danqi Chen - One of the best experts on this subject based on the ideXlab platform.
-
Novel liver-specific Cholic Acid-cytarabine conjugates with potent antitumor activities: Synthesis and biological characterization.
Acta pharmacologica Sinica, 2011Co-Authors: Danqi Chen, Xin Wang, Lin Chen, Ze-hong Miao, Jingkang ShenAbstract:Novel liver-specific Cholic Acid-cytarabine conjugates with potent antitumor activities: Synthesis and biological characterization
-
novel liver specific Cholic Acid cytarabine conjugates with potent antitumor activities synthesis and biological characterization
Acta Pharmacologica Sinica, 2011Co-Authors: Danqi Chen, Xin Wang, Lin Chen, Ze-hong Miao, Jingkang ShenAbstract:Cytarabine is an efficient anticancer agent for acute myelogenous leukemia, but with short plasma half-life and rapid deamination to its inactive metabolite. The aim of this study was to design and synthesize novel Cholic Acid-cytarabine conjugates to improve its pharmacokinetic parameters. The in vitro stability of novel Cholic Acid-cytarabine conjugates was investigated in simulated gastric and intestinal fluid, mouse blood and liver homogenate using HPLC. The portacaval samples of the conjugates were examined in male Sprague-Dawley rats using LC/MS, and in vivo distribution was examined in male Kunming mice using LC/MS. Antitumor activities were tested in HL60 cells using MTT assay. Cholic Acid-cytarabine compounds with four different linkers were designed and synthesized. All the four Cholic Acid-cytarabine conjugates could release cytarabine when incubated with the simulated gastric and intestinal fluid, mouse blood and liver homogenate. The conjugates 6, 12, and 16 were present in the portacaval samples, whereas the conjugate 7 was not detected. The conjugates 6 and 16 showed high specificity in targeting the liver (liver target index 34.9 and 16.3, respectively) and good absorption in vivo, as compared with cytarabine. In cytarabine-sensitive HL60 cells, the conjugates 6, 12, and 16 retained potent antitumor activities. Three novel Cholic Acid-cytarabine conjugates with good liver-targeting properties and absorption were obtained. Further optimization of the conjugates is needed in the future.
Ze-hong Miao - One of the best experts on this subject based on the ideXlab platform.
-
Novel liver-specific Cholic Acid-cytarabine conjugates with potent antitumor activities: Synthesis and biological characterization.
Acta pharmacologica Sinica, 2011Co-Authors: Danqi Chen, Xin Wang, Lin Chen, Ze-hong Miao, Jingkang ShenAbstract:Novel liver-specific Cholic Acid-cytarabine conjugates with potent antitumor activities: Synthesis and biological characterization
-
novel liver specific Cholic Acid cytarabine conjugates with potent antitumor activities synthesis and biological characterization
Acta Pharmacologica Sinica, 2011Co-Authors: Danqi Chen, Xin Wang, Lin Chen, Ze-hong Miao, Jingkang ShenAbstract:Cytarabine is an efficient anticancer agent for acute myelogenous leukemia, but with short plasma half-life and rapid deamination to its inactive metabolite. The aim of this study was to design and synthesize novel Cholic Acid-cytarabine conjugates to improve its pharmacokinetic parameters. The in vitro stability of novel Cholic Acid-cytarabine conjugates was investigated in simulated gastric and intestinal fluid, mouse blood and liver homogenate using HPLC. The portacaval samples of the conjugates were examined in male Sprague-Dawley rats using LC/MS, and in vivo distribution was examined in male Kunming mice using LC/MS. Antitumor activities were tested in HL60 cells using MTT assay. Cholic Acid-cytarabine compounds with four different linkers were designed and synthesized. All the four Cholic Acid-cytarabine conjugates could release cytarabine when incubated with the simulated gastric and intestinal fluid, mouse blood and liver homogenate. The conjugates 6, 12, and 16 were present in the portacaval samples, whereas the conjugate 7 was not detected. The conjugates 6 and 16 showed high specificity in targeting the liver (liver target index 34.9 and 16.3, respectively) and good absorption in vivo, as compared with cytarabine. In cytarabine-sensitive HL60 cells, the conjugates 6, 12, and 16 retained potent antitumor activities. Three novel Cholic Acid-cytarabine conjugates with good liver-targeting properties and absorption were obtained. Further optimization of the conjugates is needed in the future.
Xin Wang - One of the best experts on this subject based on the ideXlab platform.
-
Novel liver-specific Cholic Acid-cytarabine conjugates with potent antitumor activities: Synthesis and biological characterization.
Acta pharmacologica Sinica, 2011Co-Authors: Danqi Chen, Xin Wang, Lin Chen, Ze-hong Miao, Jingkang ShenAbstract:Novel liver-specific Cholic Acid-cytarabine conjugates with potent antitumor activities: Synthesis and biological characterization
-
novel liver specific Cholic Acid cytarabine conjugates with potent antitumor activities synthesis and biological characterization
Acta Pharmacologica Sinica, 2011Co-Authors: Danqi Chen, Xin Wang, Lin Chen, Ze-hong Miao, Jingkang ShenAbstract:Cytarabine is an efficient anticancer agent for acute myelogenous leukemia, but with short plasma half-life and rapid deamination to its inactive metabolite. The aim of this study was to design and synthesize novel Cholic Acid-cytarabine conjugates to improve its pharmacokinetic parameters. The in vitro stability of novel Cholic Acid-cytarabine conjugates was investigated in simulated gastric and intestinal fluid, mouse blood and liver homogenate using HPLC. The portacaval samples of the conjugates were examined in male Sprague-Dawley rats using LC/MS, and in vivo distribution was examined in male Kunming mice using LC/MS. Antitumor activities were tested in HL60 cells using MTT assay. Cholic Acid-cytarabine compounds with four different linkers were designed and synthesized. All the four Cholic Acid-cytarabine conjugates could release cytarabine when incubated with the simulated gastric and intestinal fluid, mouse blood and liver homogenate. The conjugates 6, 12, and 16 were present in the portacaval samples, whereas the conjugate 7 was not detected. The conjugates 6 and 16 showed high specificity in targeting the liver (liver target index 34.9 and 16.3, respectively) and good absorption in vivo, as compared with cytarabine. In cytarabine-sensitive HL60 cells, the conjugates 6, 12, and 16 retained potent antitumor activities. Three novel Cholic Acid-cytarabine conjugates with good liver-targeting properties and absorption were obtained. Further optimization of the conjugates is needed in the future.