ENZYME AND MICROBIAL TECHNOLOGY
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2019
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IF 3.553
Yuping Shen,Man Wang,Jinwei Zhou,Yufei Chen,Lili Xu,Mengru Wu,Guohua Xia,James P. Tam,Jiangnan Yu,Xiying Teng,Huan Yang,Xiaobin Jia
Baohuoside I, a rare secondary glycoside from Epimedii Folium, has anti-osteoporosis and other pharmacological effects. In addition, it exhibits improved bioactivities compared with its original glycoside icariin. Conventional methods for the production of baohuoside I, such as acid hydrolysis, exhibit very low efficiency with serious pollution and substantial byproducts. The aim of this study was to develop an eco-efficient biphasic enzymatic hydrolysis system for the green production of rare baohuoside I. β -glucanase was selected to hydrolyze icariin and showed better performance than β -glucosidase. The biphasic system was constructed using HAc-NaAc buffer (pH 4.5) containing β -glucanase/icariin (C icariin = 100 mg/mL; 1:1, w/w ) and propyl acetate (1:2, v/v ), and the hydrolysis was performed at 60℃ for 6 h. The hydrolysis capacity of icariin in the system was largely increased from 0.5 mg/mL to 100 mg/mL. The conversion ratio of icariin was greater than 99% in a 100-fold scale-up pilot test, demonstrating its strong potential for industrial applications. Furthermore, a process flow and production plant were designed to produce 1 ton of baohuoside I annually, and the profit would be approximately 4.5-fold its total cost. Biphasic enzymatic hydrolysis is an eco-efficient technology to produce baohuoside I and represents a promising method in the pharmaceutical industry.
研究领域:
药学
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生物技术
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植物化学
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产品关联
DOI
PubMed
高影响因子
Molecular Catalysis
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2025
·
IF 4.9
Haoyu Jia,Jinyue Hu,Le Zhao,Xiaoke Zheng,Weisheng Feng
Baohuoside I, a valuable flavonoid derivative of Herba Epimedii , exhibits superior bioactivities compared to its precursor, icariin. The conversion of icariin to baohuoside I using β-glucosidase (β-G) is an efficient approach for industrial production. Herein, β-G was successfully immobilized into a porous materials metal-organic frameworks (MOFs) via a simple one-pot coprecipitation method. The β-G@MOF biocomposite exhibited high encapsulation efficiency and excellent tolerance to extreme pH, high temperature, organic solvent and glucose. Remarkably, β-G@MOF retained its full initial activity even at 200 mM glucose. The β-G@MOF has a lower K m value compared with the free β-G, indicating enhanced substrate affinity. A conversion of 99.8 % was achieved in the hydrolysis of icariin to baohuoside I within 2 h. Additionally, β-G@MOF exhibited significantly reusability, maintaining 70.5 % yield after eight cycles at 60 °C. This study provides a simple, efficient, and sustainable approach for industrial production of baohuoside I and has potential for hydrolyzing other poorly soluble flavonoids.
研究领域:
生物化学
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材料科学
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药物生产
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产品关联
DOI
高影响因子
MOLECULES
·
2024
·Vol. 29
·期 22
·5280
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IF 4.2
Xiaoling Zhang,Yitong Wang,Tiantian Zhang,Ziqiao Yuan,Yongjun Wei
Epimedium Folium(EF) is a traditional Chinese herbal medicine, and its primary bioactive ingredients, such as icariin, are flavonoid glycosides. A rare EF flavonoid, baohuoside I, exhibits superior bioactivities and enhanced bioavailability compared to its metabolic precursor icariin. The biotransformation of icariin to baohuoside I can be effectively and specifically achieved by β-glucosidases. In this study, 33 candidate full-length β-glucosidase genes were screened from a previously built carbohydrate active enzyme (CAZyme) gene dataset derived from cow fecal microbiota. Thirteen of them exhibited β-glucosidase activity, with DCF-bgl-26 and DCF-bgl-27 showing relatively high expression levels and β-glucosidase activity. The maximum β-glucosidase activity of DCF-bgl-26 and DCF-bgl-27 was achieved at 45 °C and pH 6.0, with DCF-bgl-26 demonstrating better thermostability and pH tolerance compared to DCF-bgl-27. The activities of DCF-bgl-26 and DCF-bgl-27 were 123.2 U/mg protein and 157.9 U/mg protein, respectively, both of which are higher than those of many bacterial β-glucosidases. Structure analysis suggested that both β-glucosidases possess canonical (β/α)8-TIM barrel fold structure of GH1 family β-glucosidases. Thin-layer chromatography results showed that both enzymes could efficiently convert icariin to baohuoside I in 30 min, indicating they have potential application in the production of high value rare baohuoside I.
研究领域:
生物化学
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生物技术
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药理学
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微生物学
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产品关联
DOI
PubMed
高影响因子
DRUG DELIVERY
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2017
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IF 6.402
Hongmei Yan,Jie Song,Xiaobin Jia,Zhenhai Zhang
Baohuoside I is an effective but a poorly soluble antitumor drug. In this study, we prepared baohuoside I-loaded mixed micelles with didecyldimethylammonium bromide (DDAB) and d-a-tocopheryl polyethylene glycol succinate (TPGS) (DTBM) and active targeting mixed micelles (HDTBM) with hyaluronic acid (HA) as the targeting ligand on the surface of the mixed micelles. We performed a systematic comparative evaluation of the antiproliferative effect, cellular uptake, antitumor efficacy, and in vivo tumor targeting of these micelles using A549 cells. HDTBM showed improved cellular uptake and had a greater hypersensitizing effect on A549 cell lines than baohuoside I; half-maximal inhibitory concentration (IC50) was 8.86 versus 20.42 μg/mL, respectively. Results of the antitumor efficacy study and the imaging study for in vivo targeting showed that the mixed-micelle formulation had higher antitumor efficacy and achieved effective and targeted drug delivery. Therefore, our results indicate that HA/baohuoside I-M may be used as a potential antitumor formulation.
研究领域:
药剂学
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肿瘤学
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药物递送系统
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纳米技术
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）