The inclusion-complex of CD-MCP （β-cyclodextrin （β-CD） including 1-methylcyclopropene （1-MCP）） was prepared and characterized. Basing on programmed-heating procedure and weight-temperature analysis, as well as...The inclusion-complex of CD-MCP （β-cyclodextrin （β-CD） including 1-methylcyclopropene （1-MCP）） was prepared and characterized. Basing on programmed-heating procedure and weight-temperature analysis, as well as the application of Satava-Sestak＇s, Ozawa＇s and Kissinger＇s methods, the mechanism and kinetics of thermal dissociation of this inclusion complex were studied. An additional mass loss is found at 170-180℃. The mechanism of thermal dissociation of CD-MCP is dominated by a one-dimensional random nucleation and subsequent growth process （A2/3）. The activation energy Es and the pre-exponential factor AS for the process are 102.14 kJ/mol and 3.63×10^10s^-1, respectively. This ES value shows that there is no strong chemical intere, ctions between β-CD and 1-MC;P,展开更多
Heptakis(2, 3, 6-tri-O-octyl)-β-cyclodextrin was coated onto the fused silica capillary by sol-gel technology. Column efficiency and column selectivity were studied. The results indicated that high ability of separat...Heptakis(2, 3, 6-tri-O-octyl)-β-cyclodextrin was coated onto the fused silica capillary by sol-gel technology. Column efficiency and column selectivity were studied. The results indicated that high ability of separation was acquired . Positional isomers of aromatic compounds were well separated.展开更多
Here we have synthesized cancer targeting drug delivery system that contains β-cyclodextrin as a drug carrier and folic acid as a targeting ligand. Folic acid was selected as a cancer targeting ligand because folic a...Here we have synthesized cancer targeting drug delivery system that contains β-cyclodextrin as a drug carrier and folic acid as a targeting ligand. Folic acid was selected as a cancer targeting ligand because folic acid receptors are highly expressed in a variety of tumor types. β-cyclodextrin and folic acid were connected through a linker [1,10-phenanthroline or 5-(hydroxymethyl) furfural]. β-cyclodextrin and folic acid were attached to the linker by formation of Schiffbase and ester, respectively. Our targeted synthetic products were confirmed by NMR, Mass and IR spectroscopy. We anticipate that our synthetic products can confer cancer cell-specific drug delivery as well as desired properties such as nanoparticle formation.展开更多
An efficient and green method has been developed for the synthesis of 2H-indazolo[2,1-b]phthalazinetriones derivatives by employing 15 mol%β-cyclodextrinvia a one-pot multicomponent reaction of aldehyde,dimedone,hydr...An efficient and green method has been developed for the synthesis of 2H-indazolo[2,1-b]phthalazinetriones derivatives by employing 15 mol%β-cyclodextrinvia a one-pot multicomponent reaction of aldehyde,dimedone,hydrazine hydrate with succinic anhydride/phthalic anhydride in water at 80 ℃ for first time.The catalyst could be recovered and reused for four consecutive cycles without appreciable loss in catalytic activity and evaluated for in vitro antimicrobial activity against different Gram-positive and Gram-negative bacterial strains.The outcome of the screening study showed that compound 6d,6f and7 n exhibited excellent activity against E.coil.Whereas,compound 6f and 6h exhibited excellent activity against P.aeurginosa,and compound 6c,and 6e displayed again excellent activity against Staphylococcus aureus whereas compound 7o shows excellent activity against S.aureus and B.subtilis when compared with Ampicillin（standard control）.The results indicated that maximum compounds are moderately effective against bacterial growth and their effectiveness is highest against standard drugs.展开更多
Cholesterol is biosynthesized by all animal cells. Beyond its metabolic role in steroidogenesis, it is enriched in the plasma membrane where it has key structural and regulatory functions. Cholesterol is thus presumab...Cholesterol is biosynthesized by all animal cells. Beyond its metabolic role in steroidogenesis, it is enriched in the plasma membrane where it has key structural and regulatory functions. Cholesterol is thus presumably important for post-injury axon regrowth, and this notion is supported by studies showing that impairment of local cholesterol reutilization impeded regeneration. However, several studies have also shown that statins, inhibitors of 3-hydroxy-3-methylglutaryl-Co A reductase, are enhancers of axon regeneration, presumably acting through an attenuation of the mevalonate isoprenoid pathway and consequent reduction in protein prenylation. Several recent reports have now shown that cholesterol depletion, as well as inhibition of cholesterol synthesis per se, enhances axon regeneration. Here, I discussed these findings and propose some possible underlying mechanisms. The latter would include possible disruptions to axon growth inhibitor signaling by lipid raft-localized receptors, as well as other yet unclear neuronal survival signaling process enhanced by cholesterol lowering or depletion.展开更多
Apurinic/apyrimidinic endonuclease 1（APE1） plays an important role in protecting the fidelity of genetic material and is also a promising biomarker of cancers. Herein, a simple and sensitive fluorescent method for A...Apurinic/apyrimidinic endonuclease 1（APE1） plays an important role in protecting the fidelity of genetic material and is also a promising biomarker of cancers. Herein, a simple and sensitive fluorescent method for APE1 activity detection was designed based on host-guest interaction between β-cyclodextrin polymer（β-CDP） and pyrene. In this method, pyrene-labelled DNA probes（AP-S1 S2） and β-CDP functioned as fluorescent signal producer and enhancer, respectively. When APE1 was absent, pyrene on the AP-S1 S2 could not enter the cavity of β-CDP because of steric hindrance, leading to a weak fluorescence intensity/anisotropy. When APE1 was present, it would recognize and cleave AP site in APS1 S2, thus producing a dissociated pyrene-labelled oligonucleotide segment. Pyrene labelled at the 50 end of oligonucleotide segment could be easily trapped into the cavity of β-CDP via host-guest interaction, leading to a significant enhancement of fluorescence intensity/anisotropy. This assay offered a dynamic range of 0.05 U/m L–5 U/m L and an estimated detection limit of 0.05 U/m L. Furthermore,assessment of APE1 activity in He La cell extracts was successfully implemented, which hold the potential for APE1-related cancer diagnosis and biological researches.展开更多
A supramolecular complex between β-cyclodextrin and cholesterol was synthesized and characterized via proton 1H NMR spectroscopy. In the supramolecular complex,the stoichiometric proportion of β-cyclodextrin to chol...A supramolecular complex between β-cyclodextrin and cholesterol was synthesized and characterized via proton 1H NMR spectroscopy. In the supramolecular complex,the stoichiometric proportion of β-cyclodextrin to cholesterol is 1：2. The possible conformation of the supramolecular complex was depicted according to the chemical shift variance of proton 1H NMR of the host and guest molecules inside the inclusion complex. Removal efficiency of cholesterol complexed by β-cyclodextrin in our work is increased to a remarkable extent. This result can be applied in the field of drug development to reduce cholesterol in blood and other human organs.展开更多
We construct MUC1 vaccines usingβ-cyclodextrin grafted chitosan(CS-g-CD)as carrier via host-guest interaction.These vaccines based on non-covalent assembling can provoke robust immune responses,including high level o...We construct MUC1 vaccines usingβ-cyclodextrin grafted chitosan(CS-g-CD)as carrier via host-guest interaction.These vaccines based on non-covalent assembling can provoke robust immune responses,including high level of specific antibodies and cytokines.The induced antibodies can specifically recognize tumor cells and mediate cytotoxicity against tumor cells.These results indicate that CS-g-CD with strong immunostimulatory activities can be a straightforward platform for peptide-based vaccine construction.展开更多
The complexation of triprolidine hydrochloride （TRP） and β-cyclodextrin （β-CD） in deuterium oxide was investigated by 400 MHz 1^H NMR spectroscopy. The 800 MHz 2D ROESY data revealed that two 1 ：1 and one 2 ：...The complexation of triprolidine hydrochloride （TRP） and β-cyclodextrin （β-CD） in deuterium oxide was investigated by 400 MHz 1^H NMR spectroscopy. The 800 MHz 2D ROESY data revealed that two 1 ：1 and one 2 ： 1 β-CD-TRP inclusion complexes were formed. Both aromatic moieties （p-tolyl and pyridyl ring） has entered into the β-CD cavity, confirming the existence of two different equilibria for 1 ： 1 inclusion complexes in which p-tolyl ring of the guest is more tightly held by the host cavity. The ROE intermolecular interactions provided the plausible structures of these 1 ： 1 and 2 ： 1 stoichiometric inclusion complexes of β-CD-triprolidine hydrochloride in solu- tion.展开更多
Cholesterol plays a significant role in the organization of lipids and modulation of membrane dynamics in mammalian cells. However, the effect of cholesterol depletion on the eukaryotic cell membranes seems controvers...Cholesterol plays a significant role in the organization of lipids and modulation of membrane dynamics in mammalian cells. However, the effect of cholesterol depletion on the eukaryotic cell membranes seems controversial. In this study, the effects of cholesterol on the topography and mechanical behaviors of CHO-K1 cells with manipulated membrane cholesterol contents were investigated by atomic force microscopy (AFM) technique. Here, we found that the depletion of cholesterol in cell membranes could increase the membrane stiffness, reduce the cell height as well as promote cell retraction and detachment from the surface, whereas the cholesterol restoration could reverse the effect of cholesterol depletion on the membrane stiffness. Increased methyl-β-cyclodextrin levels and incubation time could significantly increase Young’s modulus and degree of stiffing on cell membrane and cytoskeleton. This research demonstratede importance of cholesterol in regulating the dynamics of cytoskeleton-mediated processes. AFM technique offers excellent advantages in the dynamic monitoring of the change in membranes mechanical properties and behaviors during the imaging process. This promising technology can be utilized in studying the membrane properties and elucidating the underlying mechanism of distinct cells in the near-native environment.展开更多
文摘The inclusion-complex of CD-MCP （β-cyclodextrin （β-CD） including 1-methylcyclopropene （1-MCP）） was prepared and characterized. Basing on programmed-heating procedure and weight-temperature analysis, as well as the application of Satava-Sestak＇s, Ozawa＇s and Kissinger＇s methods, the mechanism and kinetics of thermal dissociation of this inclusion complex were studied. An additional mass loss is found at 170-180℃. The mechanism of thermal dissociation of CD-MCP is dominated by a one-dimensional random nucleation and subsequent growth process （A2/3）. The activation energy Es and the pre-exponential factor AS for the process are 102.14 kJ/mol and 3.63×10^10s^-1, respectively. This ES value shows that there is no strong chemical intere, ctions between β-CD and 1-MC;P,
文摘Heptakis(2, 3, 6-tri-O-octyl)-β-cyclodextrin was coated onto the fused silica capillary by sol-gel technology. Column efficiency and column selectivity were studied. The results indicated that high ability of separation was acquired . Positional isomers of aromatic compounds were well separated.
文摘Here we have synthesized cancer targeting drug delivery system that contains β-cyclodextrin as a drug carrier and folic acid as a targeting ligand. Folic acid was selected as a cancer targeting ligand because folic acid receptors are highly expressed in a variety of tumor types. β-cyclodextrin and folic acid were connected through a linker [1,10-phenanthroline or 5-(hydroxymethyl) furfural]. β-cyclodextrin and folic acid were attached to the linker by formation of Schiffbase and ester, respectively. Our targeted synthetic products were confirmed by NMR, Mass and IR spectroscopy. We anticipate that our synthetic products can confer cancer cell-specific drug delivery as well as desired properties such as nanoparticle formation.
基金supported by Special Assistance Programme SAP,University Grants Commission,New Delhi,India
文摘An efficient and green method has been developed for the synthesis of 2H-indazolo[2,1-b]phthalazinetriones derivatives by employing 15 mol%β-cyclodextrinvia a one-pot multicomponent reaction of aldehyde,dimedone,hydrazine hydrate with succinic anhydride/phthalic anhydride in water at 80 ℃ for first time.The catalyst could be recovered and reused for four consecutive cycles without appreciable loss in catalytic activity and evaluated for in vitro antimicrobial activity against different Gram-positive and Gram-negative bacterial strains.The outcome of the screening study showed that compound 6d,6f and7 n exhibited excellent activity against E.coil.Whereas,compound 6f and 6h exhibited excellent activity against P.aeurginosa,and compound 6c,and 6e displayed again excellent activity against Staphylococcus aureus whereas compound 7o shows excellent activity against S.aureus and B.subtilis when compared with Ampicillin（standard control）.The results indicated that maximum compounds are moderately effective against bacterial growth and their effectiveness is highest against standard drugs.
文摘Cholesterol is biosynthesized by all animal cells. Beyond its metabolic role in steroidogenesis, it is enriched in the plasma membrane where it has key structural and regulatory functions. Cholesterol is thus presumably important for post-injury axon regrowth, and this notion is supported by studies showing that impairment of local cholesterol reutilization impeded regeneration. However, several studies have also shown that statins, inhibitors of 3-hydroxy-3-methylglutaryl-Co A reductase, are enhancers of axon regeneration, presumably acting through an attenuation of the mevalonate isoprenoid pathway and consequent reduction in protein prenylation. Several recent reports have now shown that cholesterol depletion, as well as inhibition of cholesterol synthesis per se, enhances axon regeneration. Here, I discussed these findings and propose some possible underlying mechanisms. The latter would include possible disruptions to axon growth inhibitor signaling by lipid raft-localized receptors, as well as other yet unclear neuronal survival signaling process enhanced by cholesterol lowering or depletion.
基金supported by the National Natural Science Foundation of China (Nos. 21675047, 21375034, 21190040)the Foundation for Innovative Research Groups of National Natural Science Foundation of China (No. 21521063)
文摘Apurinic/apyrimidinic endonuclease 1（APE1） plays an important role in protecting the fidelity of genetic material and is also a promising biomarker of cancers. Herein, a simple and sensitive fluorescent method for APE1 activity detection was designed based on host-guest interaction between β-cyclodextrin polymer（β-CDP） and pyrene. In this method, pyrene-labelled DNA probes（AP-S1 S2） and β-CDP functioned as fluorescent signal producer and enhancer, respectively. When APE1 was absent, pyrene on the AP-S1 S2 could not enter the cavity of β-CDP because of steric hindrance, leading to a weak fluorescence intensity/anisotropy. When APE1 was present, it would recognize and cleave AP site in APS1 S2, thus producing a dissociated pyrene-labelled oligonucleotide segment. Pyrene labelled at the 50 end of oligonucleotide segment could be easily trapped into the cavity of β-CDP via host-guest interaction, leading to a significant enhancement of fluorescence intensity/anisotropy. This assay offered a dynamic range of 0.05 U/m L–5 U/m L and an estimated detection limit of 0.05 U/m L. Furthermore,assessment of APE1 activity in He La cell extracts was successfully implemented, which hold the potential for APE1-related cancer diagnosis and biological researches.
基金Supported by Autonomous Research Foundation (DC10040106)Central University Special Research Foundation
文摘A supramolecular complex between β-cyclodextrin and cholesterol was synthesized and characterized via proton 1H NMR spectroscopy. In the supramolecular complex,the stoichiometric proportion of β-cyclodextrin to cholesterol is 1：2. The possible conformation of the supramolecular complex was depicted according to the chemical shift variance of proton 1H NMR of the host and guest molecules inside the inclusion complex. Removal efficiency of cholesterol complexed by β-cyclodextrin in our work is increased to a remarkable extent. This result can be applied in the field of drug development to reduce cholesterol in blood and other human organs.
基金supported by the National Natural Science Foundation of China(Nos.21907038 and 32000904)Natural Science Foundation of Jiangsu Province(No.BK20200601)+5 种基金National Postdoctoral Program for Innovative Talents of China(No.BX20200153)China Postdoctoral Science Foundation(Nos.2018M632227 and2021M691293)the Social Development Key Project of Jiangsu Province(No.BE2019632)the Health and Family Planning Commission of Wuxi,China(No.Z202005)Suzhou People’s Livelihood Science and Technology Project,China(No.SYS2018100)supported by the 111 Project(No.111-2-06)。
文摘We construct MUC1 vaccines usingβ-cyclodextrin grafted chitosan(CS-g-CD)as carrier via host-guest interaction.These vaccines based on non-covalent assembling can provoke robust immune responses,including high level of specific antibodies and cytokines.The induced antibodies can specifically recognize tumor cells and mediate cytotoxicity against tumor cells.These results indicate that CS-g-CD with strong immunostimulatory activities can be a straightforward platform for peptide-based vaccine construction.
文摘The complexation of triprolidine hydrochloride （TRP） and β-cyclodextrin （β-CD） in deuterium oxide was investigated by 400 MHz 1^H NMR spectroscopy. The 800 MHz 2D ROESY data revealed that two 1 ：1 and one 2 ： 1 β-CD-TRP inclusion complexes were formed. Both aromatic moieties （p-tolyl and pyridyl ring） has entered into the β-CD cavity, confirming the existence of two different equilibria for 1 ： 1 inclusion complexes in which p-tolyl ring of the guest is more tightly held by the host cavity. The ROE intermolecular interactions provided the plausible structures of these 1 ： 1 and 2 ： 1 stoichiometric inclusion complexes of β-CD-triprolidine hydrochloride in solu- tion.
文摘Cholesterol plays a significant role in the organization of lipids and modulation of membrane dynamics in mammalian cells. However, the effect of cholesterol depletion on the eukaryotic cell membranes seems controversial. In this study, the effects of cholesterol on the topography and mechanical behaviors of CHO-K1 cells with manipulated membrane cholesterol contents were investigated by atomic force microscopy (AFM) technique. Here, we found that the depletion of cholesterol in cell membranes could increase the membrane stiffness, reduce the cell height as well as promote cell retraction and detachment from the surface, whereas the cholesterol restoration could reverse the effect of cholesterol depletion on the membrane stiffness. Increased methyl-β-cyclodextrin levels and incubation time could significantly increase Young’s modulus and degree of stiffing on cell membrane and cytoskeleton. This research demonstratede importance of cholesterol in regulating the dynamics of cytoskeleton-mediated processes. AFM technique offers excellent advantages in the dynamic monitoring of the change in membranes mechanical properties and behaviors during the imaging process. This promising technology can be utilized in studying the membrane properties and elucidating the underlying mechanism of distinct cells in the near-native environment.
