竹叶椒对α-葡萄糖苷酶的抑制作用及机制研究
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摘要
采用体外抑制模型方法评价竹叶椒生物碱对α-葡萄糖苷酶(酵母菌来源、小鼠小肠来源)抑制作用,并采用Lineweaver-Burk双倒数法分析其抑制α-葡萄糖苷酶活性的机制。结果显示,竹叶椒脂溶性生物碱和水溶性生物碱都对α-葡萄糖苷酶有一定的抑制作用。竹叶椒脂溶性生物碱和水溶性生物碱对酵母来源α-葡萄糖苷酶IC50(半数抑制浓度)分别为(0.73±0.17) mg/mL、(2.74±0.28) mg/mL;脂溶性生物碱对小鼠小肠来源α-葡萄糖苷酶的IC_(50)为(1.94±0.13) mg/mL。动力学研究表明,竹叶椒生物碱提取物对α-葡萄糖苷酶的抑制作用类型为典型的非竞争性抑制。竹叶椒生物碱对α-葡萄糖苷酶有较好的抑制作用,为进一步的开发利用提供强有力的理论依据。
Study on the inhibition of alkaloids from Zanthoxylum armatum DC. on α-glucosidase and mechanism. The inhibitory activity of alkaloids from Zanthoxylum armatum againstα-glucosidase(from yeast and murine small intestine) were evaluated using vitro model,and the mechanism was analyzed using Lineweaver-Burk double-reciprocal analysis. Our results revealed that fat-soluble and dissoluble alkaloids both had significant inhibition on α-glucosidase,IC_(50) values for α-glucosidase from yeast were(0.73±0.17) mg/mL、(2.74±0.28) mg/mL,respectively. Ones forα-glucosidase from murine small intestine were(1.94±0.13) mg/mL. Moreover,the results of kinetic studies demonstrated inhibitive mechanism of alkaloids is noncompetition inhibition. The results suggested that alkaloids can effectively inhibit the α-glucosidase,and provide strong rationale for further exploitation and utilization.
Study on the inhibition of alkaloids from Zanthoxylum armatum DC. on α-glucosidase and mechanism. The inhibitory activity of alkaloids from Zanthoxylum armatum againstα-glucosidase(from yeast and murine small intestine) were evaluated using vitro model,and the mechanism was analyzed using Lineweaver-Burk double-reciprocal analysis. Our results revealed that fat-soluble and dissoluble alkaloids both had significant inhibition on α-glucosidase,IC_(50) values for α-glucosidase from yeast were(0.73±0.17) mg/mL、(2.74±0.28) mg/mL,respectively. Ones forα-glucosidase from murine small intestine were(1.94±0.13) mg/mL. Moreover,the results of kinetic studies demonstrated inhibitive mechanism of alkaloids is noncompetition inhibition. The results suggested that alkaloids can effectively inhibit the α-glucosidase,and provide strong rationale for further exploitation and utilization.
引文
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[2]LORDAN S,Smyth T J,SOLER V A,et al.The amylase and a-glucosidase inhibitory effects of Irish seaweed extracts[J].Food Chemistry,2013,141(3):2170-2176.
[3]GUO T,XIE H,XIA Y,et al.A new lignan and other constituents from Zanthoxylum armatum DC.[J].Natural Product Research,2012,26(9):859-864.
[4]GUO T,DENG Y X,XIE H,et al.Antinociceptive and anti-inflammatory activities of ethyl acetate fraction from Zanthoxylum armatum DC.in mice[J].Fitoterapia,2011,82(3):347-351.
[5]PACHON G,RASSOANAIVO H,AZQUETA A,et al.Anticancer efect of a new benzophenanthridine isolated from Zanthoxylum madagascariense(Rutaceline)[J].Vivo,2007,21(2):417-422.
[6]LI Hang,LI Peng.Studies on the chemical constituents of Zanthoxylum Armatum DC[J].China Pharmacy,2006,17(13):1035-1037.(in Chinese)
[7]EZZATS M,SALAMA M M.A new a-glucosidase inhibitor from Achillea fragrantissima(Forssk.)Sch.Bip.growing in Egypt[J].Natural Product Research,2014,28(11):812-818.
[8]SUN Min,WANG Xinrong,LONG Quan et al.Screening of SH-9766,an Inhibitor ofα-Glucosidase from Microorganisms and its Taxonomy[J].Journal of Food Science and Biotechnology,2005,24(3):48-51.(in Chinese)
[9]GERSHELL L.Type 2 diabetes market[J].Nature Reviews Drug Discovery,2005,4(5):367-368.
[10]YANG Fumei,SUN Qianyun.Study on microassay for screeningα-glucosidase inhibitors by orthogonal matrix method[J].Chinese Pharmacological Bulletin,2009,25(8):1113-1116.(in Chinese)
[11]GU Juefen,CHEN Zijuan.The studies and applications ofα-glucosidase inhibitors[J].Progress in Pharmaceutical Science,2009,33(2):62-67.(in Chinese)
[12]ZHANG Y,PENG Y H,ZENG D Q,et al.Insecticida l activity of essential oil from Zanthoxylum armatum fructiication against two mosquito species[J].Guihaia,2010,2:26-28.
[13]ZHU Wenjia,ZHU Limin,ZHOU Fengwei,et al.Study on the inhibitory activities of twelve species of edible traditional Chinese medicines toα-glucosidase[J].Journal of Dalian Dalian Polytechnic University,2011,30(5):325-328.(in Chinese)
[14]JI Fang,XIAO Guochun,DONG Li,et al.α-glucosidase inhibitor from medicinal herbs[J].China Jouranl of Chinese Materia Medica,2010,35(12):1633-1640.(in Chinese)
[15]GUO Tao,SUN Li,HUANG Yan,et al.Review research progress on pharmacological activities of past five years on Zanthoxylum armatum DC.[J].Modern Chinese Medicine,2013,15(2):109-111.(in Chinese)
[16]ZHANG Bingyun,SU Dan,GUO Tao,et al.Study on the inhibitory effect and inhibition mechanism onα-glycosidase of ethanol extract from Zanthoxylum armatum DC[J].Science and Technology of Food Industry,2015,6(21):345-348.(in Chinese)
[17]YU Z P,YIN Y G,ZHAO W Z,et al.Anti-diabetic activity peptides from albumin againstα-glucosidase andα-amylase[J].Food Chemistry,2012,135(3):2078-2085.
[18]KANG Wenyi,ZHANG Li.α-g lucosidase inhitory of extracts of five genera of Gesneriacceae[J].Nat Prod Res Dev,2010,22:122-125.
[19]WIKUL A,DAMSUD T,KATAOKA K,et al(+)-Pinoresinol is a putative hypoglycemic agent in defatted sesame(Sesamum indicum)seeds though inhibiting a-g lucosidase[J].Bioorganic&Medicinal Chemistry Letters,2012,22(16):5215-5217.
[20]LI Luan,LU Juan,LI Yongji,et al.Screening of the components with hypoglycemic activity from mulberry leaves and its pharmacological study[J].Information on Traditional Chinese Medicine,2012,29(5):10-14.(in Chinese)
[21]ZHONG Wei,XIA Wenshui,CUI Baoliang,et al.Screening of lagerstroemia specious leaves constituents hypoglycemic activity[J].Journal of Food Science and Biotechnology,2005,25(3):67-71.(in Chinese)