SCI TRANSL MED:MMV390048的抗疟疗效如何?

2017-04-30 xing.T MedSci原创

由此可见,MMV390048能够阻止疟原虫的所有生命周期阶段的能力表明,该化合物应该得到进一步的发展,作为单剂量联合治疗的一部分,可能有助于控制和根除疟疾。

疟疾仍然是一个严重的公共卫生问题,特别对撒哈拉以南非洲而言。世界卫生组织发布的《2016年世界疟疾报告》显示,2015年全世界有2.12亿疟疾新病例和42.9万例死亡。作为根除疟疾全球努力的一部分,整个细胞表型筛选发现了2-氨基吡啶类的小分子可以作为开发新的抗疟药物一个很好的起点。

近日,Science Translational Medicine杂志发表了一篇研究文章,研究人员从2-氨基吡啶类化合物中发现一个衍生物,MMV390048,与现有的用于治疗疟疾的药物不存在交叉耐药性。该化合物可以有效地对疟原虫所有的生命周期阶段进行抑制,除了肝脏中的晚期休眠子外。

在人源化的恶性疟原虫小鼠模型中实验效果显示,在伯氏疟原虫小鼠模型中可以中度减少小鼠与小鼠之间疟原虫的传播。在猴子体内的实验结果显示,MMV390048具有用于完整的化疗保护作用的能力。虽然MMV390048无法消除肝脏中的晚期休眠子,但可以推迟食蟹猴疟原虫猴子模型动物的复发。基因组学和化学蛋白组学的研究均确定了疟原虫的一种激酶-磷脂酰肌醇4-激酶,其作为MMV390048的分子靶标。

由此可见,MMV390048能够阻止疟原虫的所有生命周期阶段的能力表明,该化合物应该得到进一步的发展,作为单剂量联合治疗的一部分,可能有助于控制和根除疟疾。

原始出处:

Tanya Paquet,et al. Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase.Science Translational Medicine. http://stm.sciencemag.org/content/9/387/eaad9735

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channel=null, level=null, likeNumber=26, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/mStl88fu4Nd44v3xHnnictn9UpctwtH62EPQ59TMdI9lnqHMgQ16nH7GmGCfpzicsHgjibYVk6vwSpXrC86gMibRkoaIzf5HwSz7/0, createdBy=78cc1691107, createdName=龙胆草, createdTime=Mon May 01 06:42:13 CST 2017, time=2017-05-01, status=1, ipAttribution=)]
    2017-05-01 cqykthl

    抗疟疾药物的研发

    0

  5. 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channel=null, level=null, likeNumber=26, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/mStl88fu4Nd44v3xHnnictn9UpctwtH62EPQ59TMdI9lnqHMgQ16nH7GmGCfpzicsHgjibYVk6vwSpXrC86gMibRkoaIzf5HwSz7/0, createdBy=78cc1691107, createdName=龙胆草, createdTime=Mon May 01 06:42:13 CST 2017, time=2017-05-01, status=1, ipAttribution=)]
    2017-05-01 dhzzm

    学习了分享了,很好

    0

  6. 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channel=null, level=null, likeNumber=26, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/mStl88fu4Nd44v3xHnnictn9UpctwtH62EPQ59TMdI9lnqHMgQ16nH7GmGCfpzicsHgjibYVk6vwSpXrC86gMibRkoaIzf5HwSz7/0, createdBy=78cc1691107, createdName=龙胆草, createdTime=Mon May 01 06:42:13 CST 2017, time=2017-05-01, status=1, ipAttribution=)]
    2017-05-01 shaosai

    好好学习,涨知识

    0

  7. 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topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/jW482SpianMayicTRbRZ5RzaiabIFicf63hKvVMjL6aJlx4yX4UcXmzX9DyibCRcicq0QtCRWMaQKh8MYjE1D3EKUBopgiaGWYuqbeR/0, createdBy=0c2b1999806, createdName=三生有幸9135, createdTime=Mon May 01 07:25:18 CST 2017, time=2017-05-01, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=192390, encodeId=4e8b1923905d, content=很好的人的啊, beContent=null, objectType=article, channel=null, level=null, likeNumber=22, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/PiajxSqBRaEIkNwCMvcaJiclcUnbibMY8aNMrNCO1ZwiaS6Na5waERicZaIP2UbGVwHvdnTVHwOetJuQoy1zFYyCGqw/0, createdBy=d8891630715, createdName=成恩, createdTime=Mon May 01 07:14:03 CST 2017, time=2017-05-01, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=192354, encodeId=be591923542f, content=学习了,谢谢分享, beContent=null, objectType=article, channel=null, level=null, likeNumber=26, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/mStl88fu4Nd44v3xHnnictn9UpctwtH62EPQ59TMdI9lnqHMgQ16nH7GmGCfpzicsHgjibYVk6vwSpXrC86gMibRkoaIzf5HwSz7/0, createdBy=78cc1691107, createdName=龙胆草, createdTime=Mon May 01 06:42:13 CST 2017, time=2017-05-01, status=1, ipAttribution=)]
    2017-05-01 lovetcm

    就是不知道它的毒性如何,如果毒性比较小的话未来应用前景是比较大的

    0

  8. 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topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/jW482SpianMayicTRbRZ5RzaiabIFicf63hKvVMjL6aJlx4yX4UcXmzX9DyibCRcicq0QtCRWMaQKh8MYjE1D3EKUBopgiaGWYuqbeR/0, createdBy=0c2b1999806, createdName=三生有幸9135, createdTime=Mon May 01 07:25:18 CST 2017, time=2017-05-01, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=192390, encodeId=4e8b1923905d, content=很好的人的啊, beContent=null, objectType=article, channel=null, level=null, likeNumber=22, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/PiajxSqBRaEIkNwCMvcaJiclcUnbibMY8aNMrNCO1ZwiaS6Na5waERicZaIP2UbGVwHvdnTVHwOetJuQoy1zFYyCGqw/0, createdBy=d8891630715, createdName=成恩, createdTime=Mon May 01 07:14:03 CST 2017, time=2017-05-01, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=192354, encodeId=be591923542f, content=学习了,谢谢分享, beContent=null, objectType=article, channel=null, level=null, likeNumber=26, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/mStl88fu4Nd44v3xHnnictn9UpctwtH62EPQ59TMdI9lnqHMgQ16nH7GmGCfpzicsHgjibYVk6vwSpXrC86gMibRkoaIzf5HwSz7/0, createdBy=78cc1691107, createdName=龙胆草, createdTime=Mon May 01 06:42:13 CST 2017, time=2017-05-01, status=1, ipAttribution=)]
    2017-05-01 三生有幸9135

    学习一下谢谢分享

    0

  9. 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topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/jW482SpianMayicTRbRZ5RzaiabIFicf63hKvVMjL6aJlx4yX4UcXmzX9DyibCRcicq0QtCRWMaQKh8MYjE1D3EKUBopgiaGWYuqbeR/0, createdBy=0c2b1999806, createdName=三生有幸9135, createdTime=Mon May 01 07:25:18 CST 2017, time=2017-05-01, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=192390, encodeId=4e8b1923905d, content=很好的人的啊, beContent=null, objectType=article, channel=null, level=null, likeNumber=22, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/PiajxSqBRaEIkNwCMvcaJiclcUnbibMY8aNMrNCO1ZwiaS6Na5waERicZaIP2UbGVwHvdnTVHwOetJuQoy1zFYyCGqw/0, createdBy=d8891630715, createdName=成恩, createdTime=Mon May 01 07:14:03 CST 2017, time=2017-05-01, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=192354, encodeId=be591923542f, content=学习了,谢谢分享, beContent=null, objectType=article, channel=null, level=null, likeNumber=26, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/mStl88fu4Nd44v3xHnnictn9UpctwtH62EPQ59TMdI9lnqHMgQ16nH7GmGCfpzicsHgjibYVk6vwSpXrC86gMibRkoaIzf5HwSz7/0, createdBy=78cc1691107, createdName=龙胆草, createdTime=Mon May 01 06:42:13 CST 2017, time=2017-05-01, status=1, ipAttribution=)]
    2017-05-01 成恩

    很好的人的啊

    0

  10. 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channel=null, level=null, likeNumber=26, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/mStl88fu4Nd44v3xHnnictn9UpctwtH62EPQ59TMdI9lnqHMgQ16nH7GmGCfpzicsHgjibYVk6vwSpXrC86gMibRkoaIzf5HwSz7/0, createdBy=78cc1691107, createdName=龙胆草, createdTime=Mon May 01 06:42:13 CST 2017, time=2017-05-01, status=1, ipAttribution=)]
    2017-05-01 龙胆草

    学习了,谢谢分享

    0