8,8-Dimethyldihydroberberine with improved bioavailability and oral efficacy on obese and diabetic mouse models
文献类型：期刊论文
| 作者 | Cheng, Zhe2; Chen, An-Feng1; Wu, Fang2; Sheng, Li2; Zhang, Han-Kun1; Gu, Min2 ; Li, Yuan-Yuan2; Zhang, Li-Na2; Hu, Li-Hong1; Li, Jing-Ya2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2010-08-15 |
| 卷号 | 18期号:16页码:5915-5924 |
| 关键词 | Berberine Dihydroberberine Di-Me AMPK Diet-induced obese mice db/db mice |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2010.06.085 |
| 文献子类 | Article |
| 英文摘要 | The clinical use of the natural alkaloid berberine (BBR) as an antidiabetic reagent is limited by its poor bioavailability. Our previous work demonstrated that dihydroberberine (dhBBR) has enhanced bioavailability and in vivo efficacy compared with berberine. Here we synthesized the 8,8-dimethyldihydroberberine (Di-Me) with improved stability, and bioavailability over dhBBR. Similar to BBR and dhBBR, Di-Me inhibited mitochondria respiration, increased AMP:ATP ratio, activated AMPK and stimulated glucose uptake in L6 myotubes. In diet-induced obese (DIO) mice, Di-Me counteracted the increased adiposity, tissue triglyceride accumulation and insulin resistance, and improved glucose tolerance at a dosage of 15 mg/kg. Administered to db/db mice with a dosage of 50 mg/kg, Di-Me effectively reduced random fed and fasting blood glucose, improved glucose tolerance, alleviated insulin resistance and reduced plasma triglycerides, with better efficacy than dhBBR at the same dosage. Our work highlights the importance of dihydroberberine analogs as potential therapeutic reagents for type 2 diabetes treatment. (C) 2010 Elsevier Ltd. All rights reserved. |
| WOS关键词 | ACTIVATED PROTEIN-KINASE ; BERBERINE DERIVATIVES ; GLUCOSE-METABOLISM ; INSULIN-RESISTANCE ; MECHANISM DISTINCT ; RATS ; DIET ; DYSLIPIDEMIA ; MITOCHONDRIA ; INHIBITION |
| 资助项目 | Chinese National Science Technology[2009ZX09301-001] ; Chinese National Science Technology[2009ZX09102-022] ; National Natural Science Foundation of China[30925040] ; National Natural Science Foundation of China[90713046] ; National Natural Science Foundation of China[30772638] ; National Natural Science Foundation of China[] ; National Natural Science Foundation of China[U0633008] ; CAS Foundation[KSCX2-YW-R-168] ; CAS Foundation[KSCX2-YW-R-179] ; Shanghai Commission of Science and Technology[08DZ2291300] ; Shanghai Commission of Science and Technology[09DZ2291200] ; Shanghai Commission of Science and Technology[09431902100] ; National Hi-Tech Research and Development Program Grant of China[2007AA09Z402] ; National Hi-Tech Research and Development Program Grant of China[2007AA02Z147] ; National Hi-Tech Research and Development Program Grant of China[2008AA02Z105] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000280664100014 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278797]  |
| 专题 | 上海中药现代化研究中心 国家新药筛选中心 |
| 通讯作者 | Hu, Li-Hong |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Cheng, Zhe,Chen, An-Feng,Wu, Fang,et al. 8,8-Dimethyldihydroberberine with improved bioavailability and oral efficacy on obese and diabetic mouse models[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2010,18(16):5915-5924. |
| APA | Cheng, Zhe.,Chen, An-Feng.,Wu, Fang.,Sheng, Li.,Zhang, Han-Kun.,...&Li, Jia.(2010).8,8-Dimethyldihydroberberine with improved bioavailability and oral efficacy on obese and diabetic mouse models.BIOORGANIC & MEDICINAL CHEMISTRY,18(16),5915-5924. |
| MLA | Cheng, Zhe,et al."8,8-Dimethyldihydroberberine with improved bioavailability and oral efficacy on obese and diabetic mouse models".BIOORGANIC & MEDICINAL CHEMISTRY 18.16(2010):5915-5924. |
入库方式： OAI收割
来源：上海药物研究所
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