This study was conducted to extract pachyman to the greatest degree with ultrasonic technology, and to determine the content of pachyman by the phe-nol-sulfuric acid method, so as to choose the optimal technique of ul...This study was conducted to extract pachyman to the greatest degree with ultrasonic technology, and to determine the content of pachyman by the phe-nol-sulfuric acid method, so as to choose the optimal technique of ultrasonic extrac-tion of pachyman. Firstly, the ultrasonic power, extraction time and solid-to-liquid ra-tio were investigated by ultrasonic extraction method. Then, on this basis, a respon-sible surface experiment was designed, to select the optimal process conditions ac-cording to the index of pachyman yield. The optimized ultrasonic water extraction conditions were as fol ow： ultrasonic power of 100 W, extraction time of 30 min, and solid-to-liquid ratio at 1：40. The Oxford cup method was used to study the an-timicrobial activity of pachyman. lt was found that pachyman could significantly in-hibit Bacilus subtilis_and Staphylococcus aureus.展开更多
High purity polysaccharide of pachyman was isolated from the powder of Poria cocos sclerotium with an yield of 77.8%. The intrinsic viscosity of polysaccharide was found to be 78.95 mL/g in DMSO solution at 25℃. The ...High purity polysaccharide of pachyman was isolated from the powder of Poria cocos sclerotium with an yield of 77.8%. The intrinsic viscosity of polysaccharide was found to be 78.95 mL/g in DMSO solution at 25℃. The isolated polysaccharide was reacted with chlorosulfonic acid to obtain pachyman sulfate using the improved Wolfrom method. The results of the orthogonality experiment on the sulfation reaction identified that the effectiveness of the reaction conditions on the degree of sulfation and the value of intrinsic viscosity is in the following order： molar ratio of chlorosulfonic acid to glucoside （3-5） 〉 reaction temperature （60-80℃） 〉 reaction time （1 2 h）, The kinetic studies of the pachyman sulfation indicated that the hydrolysis is accompanied with the sulfation process. The decrease in intrinsic viscosity of the sulfated pachyman is proportional to the increase in the degree of sulfation under the mild reaction conditions of 〈 80℃, chlorosulfonic acid/glucoside mole ratio 〈 5, and reaction time 〈 2 h. Beyond the above reaction conditions, excessive loss of --OH group occurs during hydrolysis. The NMR results indicated a complete sulfation on C-6 and a partial sulfation on the C-2 and C-4 of glucoside.展开更多
Objective To examine the effects of pachyman in combination with vinorelbine and cisplatin on tumor growth and the expression of epidermal growth factor receptor(EGFR)and K-ras in a mouse model of lung cancer induced ...Objective To examine the effects of pachyman in combination with vinorelbine and cisplatin on tumor growth and the expression of epidermal growth factor receptor(EGFR)and K-ras in a mouse model of lung cancer induced using the human lung cancer cell line A549,and to investigate the molecular mechanisms underlying the antitumor effects of pachyman.Methods We recorded the size of the tumor xenografts in mice after treatment with pachyman monotherapy or pachymanin combination with vinorelbine and cisplatin.We performed immunohistochemical analysis to determine the levels of expression and distribution of EGFR and K-ras in lung cancer tissues.Real-time fluorescence quantitative PCR was used to determine the relative mRNA expression levels of EGFR and K-ras in lung cancer tissues.Results Vinorelbine and cisplatin significantly decreased the rate of growth of A549 xenografts,and pachyman increased the efficacy of vinorelbine and cisplatin.EGFR and K-ras were widely expressed in A549 xenografts.Vinorelbine and cisplatin could significantly decrease the expression,distribution and mRNA expression levels of EGFR and K-ras in tumor tissues.Pachyman monotherapy significantly decreased the distribution and the mRNA expression levels of EGFR in lung cancer tissues.In addition,pachyman in combination with vinorelbine and cisplatin markedly decreased the distribution and expression levels of EGFR in lung cancer tissues.However,pachyman monotherapy or combination therapy did not significantly decrease the mRNA expression levels of K-ras.Conclusion Thus,pachyman in combination with vinorelbine can significantly inhibit the growth of A549 xenografts,and pachyman can regulate the expression of the EGFR gene to increase the efficacy of vinorelbine and cisplatin in lung cancer and decrease the side effects associated with chemotherapy.展开更多
Pachyman based nanoparticles loading salicylic acid as model drug （SA-PNPs） were prepared by an inverse microemulsion crosslinking approach using epichlorohydrin （ECH） as crosslinker. The effects of crosslinking r...Pachyman based nanoparticles loading salicylic acid as model drug （SA-PNPs） were prepared by an inverse microemulsion crosslinking approach using epichlorohydrin （ECH） as crosslinker. The effects of crosslinking reaction time, initial volume ratio of oil to aqueous phase and dosage of crosslinker on the particle size of SA-PNPs were optimized by orthogonal experimental design. SA-PNPs prepared under the optimal conditions had the average size of 230 nm and high encapsulation efficiency of 90%. The in vitro drug release was also investigated and the release data were analyzed using zero order, first order and Higuchi＇s kinetics model. According to the determined coefficients, release data fitted to Higuchi＇s model, which suggested that the release of SA from SA-PNPs in phosphate buffer （pH 7.4） was diffusion controlled release. The experimental results indicated that pachyman possesses a promising potential to be applied as nanocarriers for controlled drug release.展开更多
基金Supported by Natural Science Foundation of Hubei Province(2013CFB472)~~
文摘This study was conducted to extract pachyman to the greatest degree with ultrasonic technology, and to determine the content of pachyman by the phe-nol-sulfuric acid method, so as to choose the optimal technique of ultrasonic extrac-tion of pachyman. Firstly, the ultrasonic power, extraction time and solid-to-liquid ra-tio were investigated by ultrasonic extraction method. Then, on this basis, a respon-sible surface experiment was designed, to select the optimal process conditions ac-cording to the index of pachyman yield. The optimized ultrasonic water extraction conditions were as fol ow： ultrasonic power of 100 W, extraction time of 30 min, and solid-to-liquid ratio at 1：40. The Oxford cup method was used to study the an-timicrobial activity of pachyman. lt was found that pachyman could significantly in-hibit Bacilus subtilis_and Staphylococcus aureus.
文摘High purity polysaccharide of pachyman was isolated from the powder of Poria cocos sclerotium with an yield of 77.8%. The intrinsic viscosity of polysaccharide was found to be 78.95 mL/g in DMSO solution at 25℃. The isolated polysaccharide was reacted with chlorosulfonic acid to obtain pachyman sulfate using the improved Wolfrom method. The results of the orthogonality experiment on the sulfation reaction identified that the effectiveness of the reaction conditions on the degree of sulfation and the value of intrinsic viscosity is in the following order： molar ratio of chlorosulfonic acid to glucoside （3-5） 〉 reaction temperature （60-80℃） 〉 reaction time （1 2 h）, The kinetic studies of the pachyman sulfation indicated that the hydrolysis is accompanied with the sulfation process. The decrease in intrinsic viscosity of the sulfated pachyman is proportional to the increase in the degree of sulfation under the mild reaction conditions of 〈 80℃, chlorosulfonic acid/glucoside mole ratio 〈 5, and reaction time 〈 2 h. Beyond the above reaction conditions, excessive loss of --OH group occurs during hydrolysis. The NMR results indicated a complete sulfation on C-6 and a partial sulfation on the C-2 and C-4 of glucoside.
基金support from the National Natural Science Foundation of China(No.81774126,No.81503445 and No.81703919)China Postdoctoral Science Foundation(No.2017M622587)+5 种基金Hunan Provincial Natural Science Foundation(No.2016JJ2095 and No.2017JJ3232)Hunan Provincial Traditional Chinese Medicine Key Research Project(No.201701)Hunan Education Department Scientific Research Project(16C1203 and 16C1216)Hunan Health Department Scientific Research Project(C2015-16,C2016049 and B2016093)Busky Pharmaceutical Collaborative Research Fund,Hunan Provincial Higher Educational Institutions Research Team "Traditional Chinese Medicine prevention and treatment research on infectious diseases" Funding program(No.15)Hunan Province Teaching and Science "Thirteenth Five-Year Plan" Project(No.XJK17BGD057)
文摘Objective To examine the effects of pachyman in combination with vinorelbine and cisplatin on tumor growth and the expression of epidermal growth factor receptor(EGFR)and K-ras in a mouse model of lung cancer induced using the human lung cancer cell line A549,and to investigate the molecular mechanisms underlying the antitumor effects of pachyman.Methods We recorded the size of the tumor xenografts in mice after treatment with pachyman monotherapy or pachymanin combination with vinorelbine and cisplatin.We performed immunohistochemical analysis to determine the levels of expression and distribution of EGFR and K-ras in lung cancer tissues.Real-time fluorescence quantitative PCR was used to determine the relative mRNA expression levels of EGFR and K-ras in lung cancer tissues.Results Vinorelbine and cisplatin significantly decreased the rate of growth of A549 xenografts,and pachyman increased the efficacy of vinorelbine and cisplatin.EGFR and K-ras were widely expressed in A549 xenografts.Vinorelbine and cisplatin could significantly decrease the expression,distribution and mRNA expression levels of EGFR and K-ras in tumor tissues.Pachyman monotherapy significantly decreased the distribution and the mRNA expression levels of EGFR in lung cancer tissues.In addition,pachyman in combination with vinorelbine and cisplatin markedly decreased the distribution and expression levels of EGFR in lung cancer tissues.However,pachyman monotherapy or combination therapy did not significantly decrease the mRNA expression levels of K-ras.Conclusion Thus,pachyman in combination with vinorelbine can significantly inhibit the growth of A549 xenografts,and pachyman can regulate the expression of the EGFR gene to increase the efficacy of vinorelbine and cisplatin in lung cancer and decrease the side effects associated with chemotherapy.
基金Funded by the Chen Guang Foundation of Scientif ic and Technologic Council of Wuhan (20055003059-21)the Fundamental Research Funds for the Central Universities (3082014)
文摘Pachyman based nanoparticles loading salicylic acid as model drug （SA-PNPs） were prepared by an inverse microemulsion crosslinking approach using epichlorohydrin （ECH） as crosslinker. The effects of crosslinking reaction time, initial volume ratio of oil to aqueous phase and dosage of crosslinker on the particle size of SA-PNPs were optimized by orthogonal experimental design. SA-PNPs prepared under the optimal conditions had the average size of 230 nm and high encapsulation efficiency of 90%. The in vitro drug release was also investigated and the release data were analyzed using zero order, first order and Higuchi＇s kinetics model. According to the determined coefficients, release data fitted to Higuchi＇s model, which suggested that the release of SA from SA-PNPs in phosphate buffer （pH 7.4） was diffusion controlled release. The experimental results indicated that pachyman possesses a promising potential to be applied as nanocarriers for controlled drug release.
