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Optimization of hydrolysis process of linarin using response surface
methodology and research about ARI activity of glycosylation-acacetin
WANG Jiao， XU Jun， ZHANG Tie-jun
(1.Tianjin Medical University， Tianjin 300070， China；
2. Tianjin Institute of Pharmaceutical Research， Tianjin Engineering Laboratory of Quality Control Technology of
Traditional Chinese Medicine， National Local United Engineering Laboratory of Modern Preparation and
Quality Control Technology of Traditional Chinese Medicine (Tianjin)， State Key Laboratory of Drug Delivery
Technology and Pharmacokinetics， Tianjin 300193， China)
[Abstract] Objective： To optimize the hydrolysis process of linarin by response surface methodology， and to use the model of aldose reductase to study the acacetin′s activity of aldose reductase inhibitory. Method： The model of acacetin enzyme in vitro was established by the determination of fluorescence absorption of NADPH， the inhibition rate of acacetin aldose reductase was calculated， and then the IC50 of hydrolysis was obtained. The hydrolysis process of linarin hydrolysis condition was optimized by using response surface method. Result： The results indicated that the IC50of acacetin (2.74 mg·L-1) was less than the IC50of linarin (3.53 mg·L-1). Hydrolyzation time of 7.4 h， sulphuric acid concentration of 0.54 mol·L-1 and the ratio of material to liquid of 3∶1 were the optimum conditions. Conclusion： Hydrolyzate acacetin has preferable inhibitory activity of aldose reductase. The optimized hydrolysis condition of linarin is convenient to use with good predictability.
[Key words] linarin； response surface methodology； acacetin； aldose reductase inhibitor
doi：10.4268/cjcmm20141123
[责任编辑 马超一], http://www.100md.com(王娇 许浚 张铁军)
Optimization of hydrolysis process of linarin using response surface
methodology and research about ARI activity of glycosylation-acacetin
WANG Jiao， XU Jun， ZHANG Tie-jun
(1.Tianjin Medical University， Tianjin 300070， China；
2. Tianjin Institute of Pharmaceutical Research， Tianjin Engineering Laboratory of Quality Control Technology of
Traditional Chinese Medicine， National Local United Engineering Laboratory of Modern Preparation and
Quality Control Technology of Traditional Chinese Medicine (Tianjin)， State Key Laboratory of Drug Delivery
Technology and Pharmacokinetics， Tianjin 300193， China)
[Abstract] Objective： To optimize the hydrolysis process of linarin by response surface methodology， and to use the model of aldose reductase to study the acacetin′s activity of aldose reductase inhibitory. Method： The model of acacetin enzyme in vitro was established by the determination of fluorescence absorption of NADPH， the inhibition rate of acacetin aldose reductase was calculated， and then the IC50 of hydrolysis was obtained. The hydrolysis process of linarin hydrolysis condition was optimized by using response surface method. Result： The results indicated that the IC50of acacetin (2.74 mg·L-1) was less than the IC50of linarin (3.53 mg·L-1). Hydrolyzation time of 7.4 h， sulphuric acid concentration of 0.54 mol·L-1 and the ratio of material to liquid of 3∶1 were the optimum conditions. Conclusion： Hydrolyzate acacetin has preferable inhibitory activity of aldose reductase. The optimized hydrolysis condition of linarin is convenient to use with good predictability.
[Key words] linarin； response surface methodology； acacetin； aldose reductase inhibitor
doi：10.4268/cjcmm20141123
[责任编辑 马超一], http://www.100md.com(王娇 许浚 张铁军)