Sci Rep:CE-004.8可减弱脂肪生成并预防饮食诱导的肥胖

2018-11-07 MedSci MedSci原创

在过去几年中,内源性大麻素系统(ECs)已经成为调节食物摄入和能量代谢的重要参与者,其药理学操作或是代谢疾病管理的新策略。研究发现VCE-004.8,一种双重PPARγ和CB2受体激动剂,也抑制脯氨酰-羟化酶(PHD)并激活HIF通路,为研究其在脂肪生成体外模型和代谢综合征小鼠模型中的作用提供了理论基础,所有过程都受到VCE-004.8靶标的严格监管。根据其与PPARγ的不同结合模式,与罗格列酮(

在过去几年中,内源性大麻素系统(ECs)已经成为调节食物摄入和能量代谢的重要参与者,其药理学操作或是代谢疾病管理的新策略。研究发现VCE-004.8,一种双重PPARγ和CB2受体激动剂,也抑制脯氨酰-羟化酶(PHD)并激活HIF通路,为研究其在脂肪生成体外模型和代谢综合征小鼠模型中的作用提供了理论基础,所有过程都受到VCE-004.8靶标的严格监管。

根据其与PPARγ的不同结合模式,与罗格列酮(RGZ)相比,VCE-004.8既不诱导脂肪形成分化,也不影响成骨细胞生成。每天给HFD小鼠施用VCE-004.8(20mg/kg)3周,可诱导小鼠体重增加,总脂肪量,脂肪细胞体积和血浆甘油三酯水平显著降低。VCE-004.8还可以显着改善葡萄糖耐量,降低瘦素水平(肥胖的标志物)并增加脂联素和肠促胰岛素(GLP-1和GIP)水平。

值得注意的是,VCE-004.8增加了白色和棕色脂肪以及BAT细胞系中FGF21 mRNA的表达,使大麻氨基醌类成为一类治疗肥胖及其常见代谢性合并症的新型治疗候选药物。

原始出处:

Belen Palomares, Francisco Ruiz-Pino, et al., VCE-004.8, A Multitarget Cannabinoquinone, Attenuates Adipogenesis and Prevents Diet-Induced Obesity. Sci Rep. 2018; 8: 16092.


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  2. [GetPortalCommentsPageByObjectIdResponse(id=1821101, encodeId=aa9b182110151, content=<a href='/topic/show?id=95cb101256be' target=_blank style='color:#2F92EE;'>#饮食诱导#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=35, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=101256, encryptionId=95cb101256be, topicName=饮食诱导)], attachment=null, authenticateStatus=null, createdAvatar=https://thirdqq.qlogo.cn/qqapp/1103841572/17F844FBE270B8196CB4C53EC9493C57/100, createdBy=9d712500079, createdName=ms5906905816781247, createdTime=Mon Jul 29 21:58:00 CST 2019, time=2019-07-29, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=351914, encodeId=d7bc35191425, content=了解一下谢谢, beContent=null, objectType=article, channel=null, level=null, likeNumber=44, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=http://thirdwx.qlogo.cn/mmopen/vi_32/Q0j4TwGTfTLbTp9nZtjwVrSZNxAXbAicnKQWnic2eBdJUQYhxO36XdkstSicr7FVF8p5ReH4omtmsbnLdvZLiaJJ1A/132, createdBy=8bff2327056, createdName=kafei, createdTime=Thu Nov 08 08:27:26 CST 2018, time=2018-11-08, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=351877, encodeId=750c3518e70a, content=了解一下,谢谢分享!, beContent=null, objectType=article, channel=null, level=null, likeNumber=46, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=http://cdnapi.center.medsci.cn/medsci/head/2019/12/23/2f51002e1349ccda5be11c1eea1e1e60.jpg, createdBy=a22097948, createdName=天地飞扬, createdTime=Wed Nov 07 21:24:02 CST 2018, time=2018-11-07, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=351873, encodeId=94ae3518e3f3, content=好, beContent=null, objectType=article, channel=null, level=null, likeNumber=45, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=0aa31415219, createdName=orangesking, createdTime=Wed Nov 07 21:17:59 CST 2018, time=2018-11-07, status=1, ipAttribution=)]
    2018-11-08 kafei

    了解一下谢谢

    0

  3. [GetPortalCommentsPageByObjectIdResponse(id=1821101, encodeId=aa9b182110151, content=<a href='/topic/show?id=95cb101256be' target=_blank style='color:#2F92EE;'>#饮食诱导#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=35, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=101256, encryptionId=95cb101256be, topicName=饮食诱导)], attachment=null, authenticateStatus=null, createdAvatar=https://thirdqq.qlogo.cn/qqapp/1103841572/17F844FBE270B8196CB4C53EC9493C57/100, createdBy=9d712500079, createdName=ms5906905816781247, createdTime=Mon Jul 29 21:58:00 CST 2019, time=2019-07-29, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=351914, encodeId=d7bc35191425, content=了解一下谢谢, beContent=null, objectType=article, channel=null, level=null, likeNumber=44, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=http://thirdwx.qlogo.cn/mmopen/vi_32/Q0j4TwGTfTLbTp9nZtjwVrSZNxAXbAicnKQWnic2eBdJUQYhxO36XdkstSicr7FVF8p5ReH4omtmsbnLdvZLiaJJ1A/132, createdBy=8bff2327056, createdName=kafei, createdTime=Thu Nov 08 08:27:26 CST 2018, time=2018-11-08, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=351877, encodeId=750c3518e70a, content=了解一下,谢谢分享!, beContent=null, objectType=article, channel=null, level=null, likeNumber=46, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=http://cdnapi.center.medsci.cn/medsci/head/2019/12/23/2f51002e1349ccda5be11c1eea1e1e60.jpg, createdBy=a22097948, createdName=天地飞扬, createdTime=Wed Nov 07 21:24:02 CST 2018, time=2018-11-07, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=351873, encodeId=94ae3518e3f3, content=好, beContent=null, objectType=article, channel=null, level=null, likeNumber=45, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=0aa31415219, createdName=orangesking, createdTime=Wed Nov 07 21:17:59 CST 2018, time=2018-11-07, status=1, ipAttribution=)]
    2018-11-07 天地飞扬

    了解一下,谢谢分享!

    0

  4. [GetPortalCommentsPageByObjectIdResponse(id=1821101, encodeId=aa9b182110151, content=<a href='/topic/show?id=95cb101256be' target=_blank style='color:#2F92EE;'>#饮食诱导#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=35, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=101256, encryptionId=95cb101256be, topicName=饮食诱导)], attachment=null, authenticateStatus=null, createdAvatar=https://thirdqq.qlogo.cn/qqapp/1103841572/17F844FBE270B8196CB4C53EC9493C57/100, createdBy=9d712500079, createdName=ms5906905816781247, createdTime=Mon Jul 29 21:58:00 CST 2019, time=2019-07-29, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=351914, encodeId=d7bc35191425, content=了解一下谢谢, beContent=null, objectType=article, channel=null, level=null, likeNumber=44, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=http://thirdwx.qlogo.cn/mmopen/vi_32/Q0j4TwGTfTLbTp9nZtjwVrSZNxAXbAicnKQWnic2eBdJUQYhxO36XdkstSicr7FVF8p5ReH4omtmsbnLdvZLiaJJ1A/132, createdBy=8bff2327056, createdName=kafei, createdTime=Thu Nov 08 08:27:26 CST 2018, time=2018-11-08, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=351877, encodeId=750c3518e70a, content=了解一下,谢谢分享!, beContent=null, objectType=article, channel=null, level=null, likeNumber=46, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=http://cdnapi.center.medsci.cn/medsci/head/2019/12/23/2f51002e1349ccda5be11c1eea1e1e60.jpg, createdBy=a22097948, createdName=天地飞扬, createdTime=Wed Nov 07 21:24:02 CST 2018, time=2018-11-07, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=351873, encodeId=94ae3518e3f3, content=好, beContent=null, objectType=article, channel=null, level=null, likeNumber=45, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=0aa31415219, createdName=orangesking, createdTime=Wed Nov 07 21:17:59 CST 2018, time=2018-11-07, status=1, ipAttribution=)]
    2018-11-07 orangesking

    0