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PNAS:改良型万古霉素可打破细菌耐药性

2017-06-10 秋海 来宝网

最新研究发现,一种改良后的万古霉素可使其抗生作用更加强大,并且可有力地打破耐药性。

最新研究发现,一种改良后的万古霉素可使其抗生作用更加强大,并且可有力地打破耐药性。

来自加利福尼亚州拉荷亚斯克里普斯研究所化学部的Okanoa博士,与他的同事重新设计了万古霉素的化学结构,增加了三个修饰,由此显着的增加了万古霉素的趋向性,降低了抵抗性。该研究结果已在线发表于5月30日Proceedings of the National Academy of Sciences期刊上。

综合起来,这些修饰使其活性增加了1000倍,这就意味着临床医生在治疗感染时可使用更少量的抗生素

在这之前,有报道过这三种修饰中的两种。其中之一,是通过改变与细胞壁的结合口袋,直接克服万古霉素抵抗性的分子位点。第二个修饰周围的,在类似物上增加一个新的化学结构来干扰细菌的细胞壁,从而提高药物对细菌的敏感性和抵抗性,包括金黄色葡萄球菌对甲氧西林抵抗性,以及肠球菌对万古霉素的抵抗性。

在当前的研究报告中,Okanoa博士与他的同事阐述了第三种周围的修饰,该修饰也能干扰细菌的细胞壁,但是通过另外一种机制。

“我们所做的这些改变反映了侵袭细菌的三种不同的机制,使细菌耐药性的出现更加困难,”首席研究人Dale Boger博士说道,他也是斯克里普斯研究所化学部的联合主席。

到目前为止,这些被修饰后的抗生素对细菌的抵抗性已经在实验室试验了,在实验室里至少观察到其活性强于25000倍肠球菌对万古霉素的抵抗性以及金黄色葡萄球菌对甲氧西林抵抗性,作者写道。此外,经改良的抗生素作用50次测试后,任何一种菌株都没有耐药性。

这时,该合成抗生素分子的开发是一个需要30步的过程,这就让商业生产更加困难。在Medscape Medical News采访中,Boger博士如是说道。“我们目前重点在于简化该过程,使得其更加简单,成本更低,在那之后我们再开始临床前测试其有效性与安全性。我们的希望和目标是在5年内将该药应用于临床。”

尽管万古霉素是该药物开发项目的主要研究目标,因为万古霉素使用时间长,且在近期才出现耐药性,但是相同的研究亦可应用于其他抗生素。“我们希望我们的工作能够激发其他研究人员将该方法应用于其他抗生素,因为当前抗生素失败率在逐渐增加,”Boger博士说道。

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    2018-01-08 drwjr
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    2017-06-19 医鸣惊人

    学习了

    0

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    2017-06-19 jacob9231

    学习了谢谢分享

    0

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time=2017-06-12, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=209388, encodeId=c2d020938860, content=药物合成新产品,会有新的临床药理研究。学习了。, beContent=null, objectType=article, channel=null, level=null, likeNumber=74, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/xkvRjYnJzzRJ2R0y7VhicibvkjPWHjIMmu4ZpKnE9cWAu4lVicS3uDUCfF4M4JWvrkrYfpb2KehPV0Ee29tPqyPEebBUibiaKhnvD/0, createdBy=f8412001184, createdName=惠映实验室, createdTime=Sun Jun 11 11:52:29 CST 2017, time=2017-06-11, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=209363, encodeId=e33a20936364, content=非常好的文章,学习了,很受益, beContent=null, objectType=article, channel=null, level=null, likeNumber=35, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/NUyjXTCJjo7LIiaRZTzJ3SEfiauCzTMPW7YvPPYLNJBXG9oh6Al1icq2VQQkIHWxqXehcicTS62YKJVBhxeth3wggw/0, createdBy=7ce01621306, createdName=天涯183, createdTime=Sun Jun 11 11:03:17 CST 2017, time=2017-06-11, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=209238, encodeId=206a2092383a, content=以后不知道怎么用药了, 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/oLAjfB7s1ib3IzoRn621JdKCFUI4XvNELcibocrAVU6aUzEVDSaf3rYH08PUYUiagGqxAEhj8g9WqqNvD1CupIpCrmnR2OrqHZh/0, createdBy=7f181365728, createdName=飛歌, createdTime=Sun Jun 11 07:34:33 CST 2017, time=2017-06-11, status=1, ipAttribution=)]
    2017-06-12 明天会更好!

    感谢分享!继续关注!

    0

  7. 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    2017-06-12 龙胆草

    学习谢谢分享

    0

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    2017-06-11 惠映实验室

    药物合成新产品,会有新的临床药理研究。学习了。

    0

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time=2017-06-12, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=209388, encodeId=c2d020938860, content=药物合成新产品,会有新的临床药理研究。学习了。, beContent=null, objectType=article, channel=null, level=null, likeNumber=74, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/xkvRjYnJzzRJ2R0y7VhicibvkjPWHjIMmu4ZpKnE9cWAu4lVicS3uDUCfF4M4JWvrkrYfpb2KehPV0Ee29tPqyPEebBUibiaKhnvD/0, createdBy=f8412001184, createdName=惠映实验室, createdTime=Sun Jun 11 11:52:29 CST 2017, time=2017-06-11, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=209363, encodeId=e33a20936364, content=非常好的文章,学习了,很受益, beContent=null, objectType=article, channel=null, level=null, likeNumber=35, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/NUyjXTCJjo7LIiaRZTzJ3SEfiauCzTMPW7YvPPYLNJBXG9oh6Al1icq2VQQkIHWxqXehcicTS62YKJVBhxeth3wggw/0, createdBy=7ce01621306, createdName=天涯183, createdTime=Sun Jun 11 11:03:17 CST 2017, time=2017-06-11, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=209238, encodeId=206a2092383a, content=以后不知道怎么用药了, 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/oLAjfB7s1ib3IzoRn621JdKCFUI4XvNELcibocrAVU6aUzEVDSaf3rYH08PUYUiagGqxAEhj8g9WqqNvD1CupIpCrmnR2OrqHZh/0, createdBy=7f181365728, createdName=飛歌, createdTime=Sun Jun 11 07:34:33 CST 2017, time=2017-06-11, status=1, ipAttribution=)]
    2017-06-11 天涯183

    非常好的文章,学习了,很受益

    0

  10. 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    2017-06-11 飛歌

    以后不知道怎么用药了

    0

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