首页|淫羊藿苷仿生酶解过程的多因素考察

淫羊藿苷仿生酶解过程的多因素考察

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本实验对影响淫羊藿苷仿生酶解成宝藿苷Ⅰ的多种因素进行考察,并选择最佳反应条件,为构建新型的淫羊藿苷仿生酶解给药系统提供研究基础.以酶解温度为37℃、缓冲溶液为人工肠液和人工胃液模拟体内环境,并以宝藿苷Ⅰ转化率为指标,考察酶的种类、酶活力、水解底物浓度、反应时间、人工肠液中胰酶及表面活性剂对宝藿苷Ⅰ生成的影响.结果表明:在人工胃液中纤维素酶、β-葡萄糖苷酶和蜗牛酶均失活,基本没有宝藿苷Ⅰ生成;人工肠液中胰酶对β-葡萄糖苷酶、蜗牛酶酶解反应没有明显影响(P>0.05),但显著降低纤维素酶的活性(P<0.05).人工肠液中β-葡萄糖苷酶酶解淫羊藿苷得到的宝藿苷Ⅰ最多,最佳反应条件为酶活力10 U·mL-1、底物浓度1 mg·mL-1和3 g·L-1鼠李糖脂,反应时间3h,此条件下宝藿苷Ⅰ转化率达99.8%.
Study on different factors affecting the bionic enzymatic hydrolysis of icariin
This study aims to observe different factors which affected the bionic enzymatic hydrolysis of icariin into baohuoside Ⅰ and to optimize the reaction conditions in order to provide research foundation for building a novel bionic enzymolysis drug delivery system.To simulate the environment in vivo,37 ℃ was set as the temperature and artificial intestinal juice and gastric juice were selected as the buffer solutions.Taking the conversion of baohuoside Ⅰ as index,the effects of the kinds of enzyme,enzyme activity,substrate concentration,reaction time,pancreatin in artificial intestinal juice and surfactant on the conversion of baohuoside Ⅰ were investigated.The results showed that cellulase,β-glucosidase and snailase were all inactive in artificial gastric juice and no baohuoside Ⅰ generated.Pancreatin in artificial intestinal juice couldn't significantly influence the activity of β-glucosidase or snailase (P > 0.05),but noticeably decrease the activity of cellulase (P < 0.05).In artificial intestinal juice,the conversion of baohuoside Ⅰ was highest by using β-glucosidase,and the optimum reaction conditions were determined as follows:enzyme activity 10 U·mL-1,substrate concentration 1 mg·mL-1,3 g·L-1 rhamnolipid and reaction time 3 h.Under this condition,the conversion of baohuoside Ⅰ was 99.8%.

icariinbaohuoside Ⅰbionic enzymolysisβ-glucosidasesurfactant

高霞、陈彦、王莹、孙文杰、贾晓斌

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南京中医药大学附属中西医结合医院,江苏南京210046

江苏省中医药研究院,国家中医药管理局中药释药系统重点研究室,江苏南京210028

淫羊藿苷 宝藿苷Ⅰ 仿生酶解 β-葡萄糖苷酶 表面活性剂

国家自然科学基金江苏省中医药领军人才项目江苏省"333人才培养工程"项目

81173557LJ200913BRA2011219

2013

药学学报
中国药学会 中国医学科学院药物研究所

药学学报

CSTPCDCSCD北大核心
影响因子:1.274
ISSN:0513-4870
年,卷(期):2013.48(11)
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