To improve the encapsulation efficiency and minimize particle agglomeration of liposomes, rapid expansion from supercritical to surfactant solution（RESSS） was applied to self-assembly of liposomes entrapping hinesol...To improve the encapsulation efficiency and minimize particle agglomeration of liposomes, rapid expansion from supercritical to surfactant solution（RESSS） was applied to self-assembly of liposomes entrapping hinesol in supercritical carbon dioxide（SC-CO2） medium. In the process, the solution of liposomal materials and hinesol dissolved in the mixture of SC-CO2/ethanol was sprayed into a surfactant solution. The surfactant provided stabilization for liposomes by preventing bubbles overflowing and liposomes agglomeration during the spraying process. The encapsulating performance and particle size distribution of liposomes could be controlled by changing expansion processing conditions. When the solution was sprayed into a 5.0% Poloxamer 188 solution at a flow rate of 2 L/min, the entrapment efficiency and average particle size of liposomes were found to be 88.26% and 124 nm, respectively, which came to the standards of Chinese pharmacopoeia. The results show RESSS process provides an innovative method for formation of liposomes incorporating valid compositions extracted from the Chinese traditional medicines in SC-CO2 medium.展开更多
Stereoselective total synthesis of (±)hinesol 1 was achieved from readily available stafting materials and thorough mild reaction conditions. The structure of synthetic hinesol was confirmed by chemical transform...Stereoselective total synthesis of (±)hinesol 1 was achieved from readily available stafting materials and thorough mild reaction conditions. The structure of synthetic hinesol was confirmed by chemical transformation.展开更多
A mild base-catalyzed retro-benzilic acid rearrangement of a proto-[2+2]photocycloadduct, formed in highly steroselective photoaddition of methyl 2,4-dioxo-pentanoate to 1,5-dimethyl-6-methylenecyclohexene, afforded ...A mild base-catalyzed retro-benzilic acid rearrangement of a proto-[2+2]photocycloadduct, formed in highly steroselective photoaddition of methyl 2,4-dioxo-pentanoate to 1,5-dimethyl-6-methylenecyclohexene, afforded a spiro[4, 5] decenedione from which hinesol and agarospirol were synthesized by means of reductive elimination of α-diketone and C1-homologation.展开更多
OBJECTIVE Liver cancer is one of the most common causes of cancer related deaths worldwide,specially,in China.Hinesol,extracted from Atractylodeslance a(Thunb.) DC.has been proved that has anti-cancer effect in leukem...OBJECTIVE Liver cancer is one of the most common causes of cancer related deaths worldwide,specially,in China.Hinesol,extracted from Atractylodeslance a(Thunb.) DC.has been proved that has anti-cancer effect in leukemia in vitro and in vivo.However,it has been not well under.stood in liver cancer cells.METHODS Cell proliferation,apoptosis,cell cycle and invasion were performed to investigate the anti-liver cancer effect of hinesol in SMMC-7721 and LM3 by MTT assay,flow cytometry and scratch assay.Western blot was used to research the potential mechanism.RESULTS We revealed that hinesol suppresses cell proliferation and invasion,prompts population of G1 phase,induces apop.tosis in dose-dependent manner in SMMC-7721 and LM3 cells.Western blot data showed that hinesol could inhibits the expression of cyclin-D1,Bcl-2 and Bax,and inhibited phosphorylation of MEK and ERK,down-regulated the expressions of NF-κB p65 and phosphor-p65 in nucleus.The results indicated that hinesol reduces cell proliferation via arresting cell cycle at G1 phase and induces apoptosis.Further.more,western blot showed that hinesol inhibited phosphorylation of MEK and ERK,down-regulated the expressions of NF-κB p65 and phosphor-p65 in nucleus.CONCLUSION Our results demonstrate that hinesolreduces cell proliferation via arresting cell cycle at G1 phase and induces apoptosis,it has potent anti-cancer effect against liver cancer cells via down-regulation of MEK/ERK and NF-κB pathway,and indicate that hinesol is a potential liver cancer drug for further research.展开更多
基金Supported by the National Natural Science Foundation of China(No.20606013)the Produce-learn-research Project of Shenzhen Scinence and Technology Program(No.2008342)the Fundamental Research Project of Shenzhen Science and Technology, China(No.JC200903120089A)
文摘To improve the encapsulation efficiency and minimize particle agglomeration of liposomes, rapid expansion from supercritical to surfactant solution（RESSS） was applied to self-assembly of liposomes entrapping hinesol in supercritical carbon dioxide（SC-CO2） medium. In the process, the solution of liposomal materials and hinesol dissolved in the mixture of SC-CO2/ethanol was sprayed into a surfactant solution. The surfactant provided stabilization for liposomes by preventing bubbles overflowing and liposomes agglomeration during the spraying process. The encapsulating performance and particle size distribution of liposomes could be controlled by changing expansion processing conditions. When the solution was sprayed into a 5.0% Poloxamer 188 solution at a flow rate of 2 L/min, the entrapment efficiency and average particle size of liposomes were found to be 88.26% and 124 nm, respectively, which came to the standards of Chinese pharmacopoeia. The results show RESSS process provides an innovative method for formation of liposomes incorporating valid compositions extracted from the Chinese traditional medicines in SC-CO2 medium.
文摘Stereoselective total synthesis of (±)hinesol 1 was achieved from readily available stafting materials and thorough mild reaction conditions. The structure of synthetic hinesol was confirmed by chemical transformation.
文摘A mild base-catalyzed retro-benzilic acid rearrangement of a proto-[2+2]photocycloadduct, formed in highly steroselective photoaddition of methyl 2,4-dioxo-pentanoate to 1,5-dimethyl-6-methylenecyclohexene, afforded a spiro[4, 5] decenedione from which hinesol and agarospirol were synthesized by means of reductive elimination of α-diketone and C1-homologation.
文摘OBJECTIVE Liver cancer is one of the most common causes of cancer related deaths worldwide,specially,in China.Hinesol,extracted from Atractylodeslance a(Thunb.) DC.has been proved that has anti-cancer effect in leukemia in vitro and in vivo.However,it has been not well under.stood in liver cancer cells.METHODS Cell proliferation,apoptosis,cell cycle and invasion were performed to investigate the anti-liver cancer effect of hinesol in SMMC-7721 and LM3 by MTT assay,flow cytometry and scratch assay.Western blot was used to research the potential mechanism.RESULTS We revealed that hinesol suppresses cell proliferation and invasion,prompts population of G1 phase,induces apop.tosis in dose-dependent manner in SMMC-7721 and LM3 cells.Western blot data showed that hinesol could inhibits the expression of cyclin-D1,Bcl-2 and Bax,and inhibited phosphorylation of MEK and ERK,down-regulated the expressions of NF-κB p65 and phosphor-p65 in nucleus.The results indicated that hinesol reduces cell proliferation via arresting cell cycle at G1 phase and induces apoptosis.Further.more,western blot showed that hinesol inhibited phosphorylation of MEK and ERK,down-regulated the expressions of NF-κB p65 and phosphor-p65 in nucleus.CONCLUSION Our results demonstrate that hinesolreduces cell proliferation via arresting cell cycle at G1 phase and induces apoptosis,it has potent anti-cancer effect against liver cancer cells via down-regulation of MEK/ERK and NF-κB pathway,and indicate that hinesol is a potential liver cancer drug for further research.
