Article(id=1236369014256103713, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1236369013111050820, articleNumber=null, orderNo=null, doi=null, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=null, receivedDateStr=null, revisedDate=null, revisedDateStr=null, acceptedDate=1667404800000, acceptedDateStr=2022-11-03, onlineDate=1772702943624, onlineDateStr=2026-03-05, pubDate=1694707200000, pubDateStr=2023-09-15, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1772702943624, onlineIssueDateStr=2026-03-05, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1772702943624, creator=13701087609, updateTime=1772702943624, updator=13701087609, issue=Issue{id=1236369013111050820, tenantId=1146029695717560320, journalId=1235980733773295621, year='2023', volume='32', issue='17', pageStart='1697', pageEnd='1800', issueExtLink='null', onlineDate='null', pubDate='null', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1772702943351, creator=13701087609, updateTime=1772703317941, updator=13701087609, preIssue=null, nextIssue=null, ext={EN=IssueExt(id=1236370584322495028, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1236369013111050820, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1236370584326689333, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1236369013111050820, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null}, startPage=1768, endPage=1773, ext={EN=ArticleExt(id=1236369014490984758, articleId=1236369014256103713, tenantId=1146029695717560320, journalId=1235980733773295621, language=EN, title=Synthesis of resveratrol analogues and evaluation of their anti-diabetic activity, columnId=null, journalTitle=Chinese Journal of New Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=
Objective:

To synthesize resveratrol analogues and investigate their anti-diabetic activity and related mechanism.

Methods:

Using different substituted anilines and different substituted benzaldehydes as raw materials, resveratrol analogs were synthesized under ethanol reflux, and their protective effects on pancreatic β cells were tested under the stimulation of palmitic acid (PA). The anti-diabetic mechanism of the dominant compounds was explored.

Results:

Most of the compounds have protective effects on pancreatic β cells, and the compounds JA10 and JA12 have significant cytoprotective effects. Molecular mechanism studies showed that the compounds JA10 and JA12 reduced the generation of reactive oxygen, and inhibited the gene expression of inflammatory factors IL-1β and IL-6.

Conclusion:

The resveratrol analogs JA10 and JA12 are potential antidiabetic new chemical entities.

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目的:

合成白藜芦醇类似物,考察其抗糖尿病活性及作用机制。

方法:

以不同取代的苯胺和不同取代的苯甲醛为原料,在乙醇回流下合成了白藜芦醇类似物,并测试其在棕榈酸(palmitic acid, PA)刺激下对胰岛β细胞的保护作用,同时探究优势化合物抗糖尿病的作用机制。

结果:

大部分化合物在PA刺激下对胰岛β细胞有保护作用,化合物JA10和JA12具有明显的细胞保护作用。分子机制研究显示,化合物JA10和JA12可以减少PA刺激下细胞内活性氧的生成,同时可以抑制炎症因子IL-1β和IL-6的基因表达。

结论:

白藜芦醇类似物JA10和JA12是潜在的抗糖尿病新化学实体。

, correspAuthors=null, authorNote=null, correspAuthorsNote=
李伟泽,男,教授,研究方向:新药研究与开发。联系电话:(029)86177039,E-mail:
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关丽,女,副教授,研究方向:新药设计合成与筛选。联系电话:(029)86177539,E-mail:

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关丽,女,副教授,研究方向:新药设计合成与筛选。联系电话:(029)86177539,E-mail:

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白藜芦醇类似物的合成及抗糖尿病活性
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关丽 1 , 李小宁 2 , 李爱云 3 , 苏琬真 3 , 银瑞佳 1 , 高璐 1 , 李伟泽 1
中国新药杂志 | 实验研究 2023,32(17): 1768-1773
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中国新药杂志 | 实验研究 2023, 32(17): 1768-1773
白藜芦醇类似物的合成及抗糖尿病活性
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关丽1 , 李小宁2, 李爱云3, 苏琬真3, 银瑞佳1, 高璐1, 李伟泽1
作者信息
  • 1西安医学院药学院,西安 710021
  • 2陕西省药品和疫苗检查中心,西安 710065
  • 3山西医科大学生理学系/细胞生理学教育部重点实验室,太原 030001
  • 关丽,女,副教授,研究方向:新药设计合成与筛选。联系电话:(029)86177539,E-mail:

通讯作者:

李伟泽,男,教授,研究方向:新药研究与开发。联系电话:(029)86177039,E-mail:
Synthesis of resveratrol analogues and evaluation of their anti-diabetic activity
Li GUAN1 , Xiao-ning LI2, Ai-yun LI3, Wan-zhen SU3, Rui-jia YIN1, Lu GAO1, Wei-ze LI1
Affiliations
  • 1College of Pharmacy, Xi'an Medical University, Xi'an 710021, China
  • 2Shaanxi Pharmaceutical and Vaccine Inspection Center, Xi'an 710065, China
  • 3Key Laboratory of Cellular Physiology, Ministry of Education/Department of Physiology, Shanxi Medical University, Taiyuan 030001, China
出版时间: 2023-09-15
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目的:

合成白藜芦醇类似物,考察其抗糖尿病活性及作用机制。

方法:

以不同取代的苯胺和不同取代的苯甲醛为原料,在乙醇回流下合成了白藜芦醇类似物,并测试其在棕榈酸(palmitic acid, PA)刺激下对胰岛β细胞的保护作用,同时探究优势化合物抗糖尿病的作用机制。

结果:

大部分化合物在PA刺激下对胰岛β细胞有保护作用,化合物JA10和JA12具有明显的细胞保护作用。分子机制研究显示,化合物JA10和JA12可以减少PA刺激下细胞内活性氧的生成,同时可以抑制炎症因子IL-1β和IL-6的基因表达。

结论:

白藜芦醇类似物JA10和JA12是潜在的抗糖尿病新化学实体。

糖尿病  /  白藜芦醇类似物  /  胰岛β细胞保护作用  /  作用机制
Objective:

To synthesize resveratrol analogues and investigate their anti-diabetic activity and related mechanism.

Methods:

Using different substituted anilines and different substituted benzaldehydes as raw materials, resveratrol analogs were synthesized under ethanol reflux, and their protective effects on pancreatic β cells were tested under the stimulation of palmitic acid (PA). The anti-diabetic mechanism of the dominant compounds was explored.

Results:

Most of the compounds have protective effects on pancreatic β cells, and the compounds JA10 and JA12 have significant cytoprotective effects. Molecular mechanism studies showed that the compounds JA10 and JA12 reduced the generation of reactive oxygen, and inhibited the gene expression of inflammatory factors IL-1β and IL-6.

Conclusion:

The resveratrol analogs JA10 and JA12 are potential antidiabetic new chemical entities.

diabetes  /  resveratrol analogues  /  pancreatic β-cells protection  /  molecular mechanism
关丽, 李小宁, 李爱云, 苏琬真, 银瑞佳, 高璐, 李伟泽. 白藜芦醇类似物的合成及抗糖尿病活性. 中国新药杂志, 2023 , 32 (17) : 1768 -1773 .
Li GUAN, Xiao-ning LI, Ai-yun LI, Wan-zhen SU, Rui-jia YIN, Lu GAO, Wei-ze LI. Synthesis of resveratrol analogues and evaluation of their anti-diabetic activity[J]. Chinese Journal of New Drugs, 2023 , 32 (17) : 1768 -1773 .
  • 国家自然科学基金资助项目(82004075)
  • 陕西高校青年创新团队建设资助项目(陕教[2019]90号)
  • 西安医学院科技创新团队配套(2021TDPT04)
  • 药学省级重点学科建设项目重点资助项目(2016YXXK01; 2016YXXK07)
  • 西安医学院大学生创新创业训练项目(121521073)
  • 陕西省科技厅资助项目(2013-JC-QN-0827)
2023年第32卷第17期
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  • 首发时间:2026-03-05
  • 出版时间:2023-09-15
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  • 录用日期:2022-11-03
基金
国家自然科学基金资助项目(82004075)
陕西高校青年创新团队建设资助项目(陕教[2019]90号)
西安医学院科技创新团队配套(2021TDPT04)
药学省级重点学科建设项目重点资助项目(2016YXXK01; 2016YXXK07)
西安医学院大学生创新创业训练项目(121521073)
陕西省科技厅资助项目(2013-JC-QN-0827)
作者信息
    1西安医学院药学院,西安 710021
    2陕西省药品和疫苗检查中心,西安 710065
    3山西医科大学生理学系/细胞生理学教育部重点实验室,太原 030001

通讯作者:

李伟泽,男,教授,研究方向:新药研究与开发。联系电话:(029)86177039,E-mail:
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2种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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