Inhibitory effects against α-glucosidase and α-amylase of the flavonoids-rich extract from Scutellaria baicalensis shoots and interpretation of structure-activity relationship of its eight flavonoids by a refined assign-score method.

Q1 Chemistry Chemistry Central Journal Pub Date : 2018-07-12 DOI:10.1186/s13065-018-0445-y
Ke Li, Fan Yao, Qiang Xue, Hang Fan, Lingguang Yang, Xiang Li, Liwei Sun, Yujun Liu
{"title":"Inhibitory effects against α-glucosidase and α-amylase of the flavonoids-rich extract from Scutellaria baicalensis shoots and interpretation of structure-activity relationship of its eight flavonoids by a refined assign-score method.","authors":"Ke Li,&nbsp;Fan Yao,&nbsp;Qiang Xue,&nbsp;Hang Fan,&nbsp;Lingguang Yang,&nbsp;Xiang Li,&nbsp;Liwei Sun,&nbsp;Yujun Liu","doi":"10.1186/s13065-018-0445-y","DOIUrl":null,"url":null,"abstract":"<p><p>A flavonoids-rich extract of Scutellaria baicalensis shoots and its eight high content flavonoids were investigated for their inhibitory effects against α-glucosidase and α-amylase. Results show that abilities of the extract in inhibiting the two enzymes were obviously higher than those of acarbose. Moreover, inhibitory abilities of all the eight individual flavonoids against the two enzymes show exactly a same order (i.e., apigenin > baicalein > scutellarin > chrysin > apigenin-7-O-glucuronide > baicalin > chrysin-7-O-glucuronide > isocarthamidin-7-O-glucuronide), and their structure-activity relationship could be well-interpretated by the refined assign-score method. Furthermore, based on the inhibitory abilities and their contents in the extract, it was found that the eight flavonoids made predominant contributions, among which baicalein and scutellarin played roles as preliminary contributors, to overall inhibitory effects of the extract against the two enzymes. Beyond these, contributions of the eight flavonoids to the overall enzyme inhibitory activity were compared with those to the overall antioxidant activity characterized in our recent study, and it could be inferred that within the basic flavonoid structure the hydroxyl on C-4' of ring B was more effective than that on C-6 of ring A in enzyme inhibitory activities while they behaved inversely in antioxidant activities; scutellarin and apigenin contributed more to the overall enzyme inhibitory activity, and baicalin and scutellarin, to the overall antioxidant activity of the extract; and flavonoids of the extract, apart from directly inhibiting enzymes, might also be conducive to curing type 2 diabetes via scavenging various free radicals caused by increased oxidative stresses.</p>","PeriodicalId":9842,"journal":{"name":"Chemistry Central Journal","volume":"12 1","pages":"82"},"PeriodicalIF":0.0000,"publicationDate":"2018-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1186/s13065-018-0445-y","citationCount":"84","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Chemistry Central Journal","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1186/s13065-018-0445-y","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"Chemistry","Score":null,"Total":0}
引用次数: 84

Abstract

A flavonoids-rich extract of Scutellaria baicalensis shoots and its eight high content flavonoids were investigated for their inhibitory effects against α-glucosidase and α-amylase. Results show that abilities of the extract in inhibiting the two enzymes were obviously higher than those of acarbose. Moreover, inhibitory abilities of all the eight individual flavonoids against the two enzymes show exactly a same order (i.e., apigenin > baicalein > scutellarin > chrysin > apigenin-7-O-glucuronide > baicalin > chrysin-7-O-glucuronide > isocarthamidin-7-O-glucuronide), and their structure-activity relationship could be well-interpretated by the refined assign-score method. Furthermore, based on the inhibitory abilities and their contents in the extract, it was found that the eight flavonoids made predominant contributions, among which baicalein and scutellarin played roles as preliminary contributors, to overall inhibitory effects of the extract against the two enzymes. Beyond these, contributions of the eight flavonoids to the overall enzyme inhibitory activity were compared with those to the overall antioxidant activity characterized in our recent study, and it could be inferred that within the basic flavonoid structure the hydroxyl on C-4' of ring B was more effective than that on C-6 of ring A in enzyme inhibitory activities while they behaved inversely in antioxidant activities; scutellarin and apigenin contributed more to the overall enzyme inhibitory activity, and baicalin and scutellarin, to the overall antioxidant activity of the extract; and flavonoids of the extract, apart from directly inhibiting enzymes, might also be conducive to curing type 2 diabetes via scavenging various free radicals caused by increased oxidative stresses.

Abstract Image

Abstract Image

Abstract Image

查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
黄芩芽富含黄酮类化合物提取物对α-葡萄糖苷酶和α-淀粉酶的抑制作用及其8种黄酮类化合物构效关系的精细分配评分法解释
研究了黄芩芽富含黄酮类化合物的提取物及其8种高含量黄酮类化合物对α-葡萄糖苷酶和α-淀粉酶的抑制作用。结果表明,该提取物对这两种酶的抑制能力明显高于阿卡波糖。8种黄酮类化合物对这两种酶的抑制能力顺序为:芹菜素>黄芩素>黄芩素>菊花素>芹菜素-7- o -葡萄糖醛酸苷>黄芩苷>菊花素-7- o -葡萄糖醛酸苷>异胡萝卜素-7- o -葡萄糖醛酸苷),其构效关系可以用精细分配评分法很好地解释。此外,根据提取物对两种酶的抑制能力及其含量,发现8种黄酮类化合物对提取物对两种酶的总体抑制作用起主导作用,其中黄芩苷和黄芩苷起初步作用。此外,我们还比较了8种黄酮类化合物对总酶抑制活性的贡献与我们最近研究的总抗氧化活性的贡献,可以推断,在黄酮类化合物的基本结构中,B环C-4′上的羟基比A环C-6′上的羟基对酶抑制活性更有效,而抗氧化活性则相反;黄芩苷和黄芩苷对总酶抑制活性的贡献更大,黄芩苷和黄芩苷对总抗氧化活性的贡献更大;提取物中的黄酮类化合物,除了直接抑制酶外,还可能通过清除氧化应激增加引起的各种自由基,有助于治疗2型糖尿病。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 去求助
来源期刊
Chemistry Central Journal
Chemistry Central Journal 化学-化学综合
CiteScore
4.40
自引率
0.00%
发文量
0
审稿时长
3.5 months
期刊介绍: BMC Chemistry is an open access, peer reviewed journal that considers all articles in the broad field of chemistry, including research on fundamental concepts, new developments and the application of chemical sciences to broad range of research fields, industry, and other disciplines. It provides an inclusive platform for the dissemination and discussion of chemistry to aid the advancement of all areas of research. Sections: -Analytical Chemistry -Organic Chemistry -Environmental and Energy Chemistry -Agricultural and Food Chemistry -Inorganic Chemistry -Medicinal Chemistry -Physical Chemistry -Materials and Macromolecular Chemistry -Green and Sustainable Chemistry
期刊最新文献
Design, synthesis and biological potential of heterocyclic benzoxazole scaffolds as promising antimicrobial and anticancer agents. Regio and stereoselective synthesis of anticancer spirooxindolopyrrolidine embedded piperidone heterocyclic hybrids derived from one-pot cascade protocol. Augmentation of hepatoprotective potential of Aegle marmelos in combination with piperine in carbon tetrachloride model in wistar rats. Polyaniline/palladium nanohybrids for moisture and hydrogen detection. Benzoxazole derivatives: design, synthesis and biological evaluation.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1