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src="/system/resource/js/news/newscontent.js"></script><script type="text/javascript">NewsvoteDWR.getNewsLinkUrl(6265,'1375031859','vsb',newsSkip);function newsSkip(data){if(data != ""){window.location.href = data;}}</script><script language="javascript" src="/system/resource/js/ajax.js"></script><form name="_newscontent_fromname"><script language="javascript" src="/system/resource/js/jquery/jquery-latest.min.js"></script> <div class="TrainRightConTit"> <p> 药学院张勇慧教授团队在二倍半萜研½I‰™¢†åŸŸå–å¾—æ–°˜q›å±•</p> <span> 来源åQšè¯å­¦é™¢ 2019-07-03 11:40:53 点击敎ͼš<script>_showDynClicks("wbnews", 1375031859, 6265)</script> ¾~–辑åQšå¼ åœ?/span> </div> <div class="TrainViewCon" id="vsb_content"><p style="text-indent: 32px; text-align: justify; line-height: 2em;"><span style="font-size: 16px; font-family: 宋体;">6æœ?9日,药学院张勇慧教授团队在国际化学顶¾U§åˆŠç‰©ã€Šå¯d国应用化学》上发表了关于二倍半萜研½I¶çš„最新成æž? Bipolarolides A–G, Ophiobolin-Derived Sesterterpenes Representing Three New Carbon Skeletons from <em>Bipolaris</em> sp. TJ403-B1. (Angew. Chem. Int. Ed., doi: 10.1002/anie.201905966)。张勇慧教授和药学院青年教师胡正喜äؓ本论文的通讯作者,药学院兼创新型研½I‰™™¢18¾U§åšå£«ç”Ÿåˆ˜æ¢¦å©·å’Œå­™ä¼Ÿå…‰åšå£«åŽä¸ºå…±åŒç¬¬ä¸€ä½œè€…ã€?/span></p> <p style="text-indent: 32px; text-align: justify; line-height: 2em;"><span style="font-size: 16px;"><span style="font-size: 16px; font-family: 宋体;">萜类化合物因å…ähœ‰¾l“构复杂多变åQŒç”Ÿç‰©æ´»æ€§æ˜¾è‘—的特点åQŒä¸€ç›´ä»¥æ¥æ˜¯å¤©ç„¶è¯ç‰©åŒ–学领域的研½I¶çƒ­ç‚V€‚许多著名的药物分子如ç‚÷杉醇、青蒿素、穿心莲内酯½{‰å‡ä¸ø™œ¾cÕdŒ–合物。近òq´æ¥åQŒè¯å­¦é™¢å¼ å‹‡æ…§æ•™æŽˆå›¢é˜Ÿå›´¾l•èœ¾cÕdŒ–合物的研½IӞ¼Œå–得了一¾pÕdˆ—½Hç ´æ€§çš„工作 (Angew. Chem. Int. Ed. 2016, 55, 4069; Chem. Sci. 2016, 7, 6563</span><span style="font-size: 16px; font-family: "ms mincho";">âˆ?/span><span lang="EN-US" style="font-size: 16px; font-family: 宋体;">6572; Org. Lett. 2018, 20, 5198</span><span style="font-size: 16px; font-family: "ms mincho";">âˆ?/span><span lang="EN-US" style="font-size: 16px; font-family: 宋体;">5202)ã€?/span></span></p> <p style="text-indent: 32px; text-align: justify; line-height: 2em;"><span style="font-family: 宋体; font-size: 16px;">æ ÒŽ®åŒ–合物分子结构中C<sub>5</sub>异戊二烯单元数目的不同,可将萜类分äؓ半萜、倍半萜、二萜、二倍半萜、三萜等。二倍半萜由5个C<sub>5</sub>单元¾l„装而成åQŒç›¸å¯¹äºŽC<sub>15</sub>倍半萜、C<sub>20</sub>倍二萜、C<sub>30</sub>倍三萜等其他萜类化合物较为稀ž®‘。张勇慧教授研究团队从离蠕孢属真菌TJ403-B1中发çŽîCº†ä¸ƒä¸ªè›‡å­¢èŒç´ æ¥æºçš„二倍半萜衍生物 (Bipolarolides A–G)åQŒéš¶å±žäºŽä¸‰ç§ä¸åŒçš„新骨架¾cÕdž‹ã€‚化合物<strong>1</strong>å’?strong>2</strong>含有独特的多环笼状氧杂五çŽ?span lang="EN-US" style="font-size: 16px; font-family: 宋体; color: windowtext;">[9.3.0.0<sup>1,6</sup>.0<sup>5,9</sup>.1<sup>8,12</sup>]</span>十五烷体¾p»ï¼›åŒ–合ç‰?strong>3</strong>å’?strong>4</strong>含有前所未有çš?/5/5/5骈合环系的核心碳骨架åQŒå…¶ä¸?strong>3</strong>中C-3–C-14氧桥形成了笼状结构;化合ç‰?strong>5</strong>â€?strong>7</strong>是一¾cÕd…¨æ–°çš„含有杂氧螺环[4.4]壬烷的二倍半萜生物碱杂合体。计½Ž—机虚拟½{›é€‰å’Œä½“外‹zÀL€§éªŒè¯è¡¨æ˜ŽåŒ–合物<strong>1</strong>是一个潜在的HMG-CoA˜q˜åŽŸé…¶æŠ‘制剂(IC<sub>50</sub> = 2.46 ûu 0.07µM)åQŒå‘ˆå‰‚量依赖性地抑制HepG2¾l†èƒžOA诱导的脂质积累,显著降低HepG2¾l†èƒžä¸­æ€»èƒ†å›ºé†‡å’Œç”˜æ²¹ä¸‰é…¯æ°´òqŸë€‚另外在对六株耐药菌(MRSAåQŒç²ªè‚ çƒèŒï¼Œé²æ›¼ä¸åŠ¨æ†èŒåQŒäñ”ESBL的大肠埃希菌åQŒé“œ¾l¿å‡å•èƒžèŒå’Œäº§NDM-1的肺炎克雷伯氏菌åQ‰å’Œä¸€æ ªçœŸèŒï¼ˆç™½è‰²é“„¡ƒèŒï¼‰çš„抗菌活性筛选中åQŒåŒ–合物<strong>6</strong>对白色链球菌å…ähœ‰è¾ƒå¼ºçš„抗菌活性,MIC = 4 μg/mL。该研究极大的扩展蛇孢菌素来源二倍半萜的骨架¾cÕdž‹åQŒä¹Ÿä¸ºåŒ–学合成以及生物合成机制研½I¶æä¾›äº†æœ‰è¶£çš„目标分子ã€?/span></p> <p><br></p> <p style="text-align: justify; line-height: 2em;"><span style="font-family: 宋体; font-size: 16px;">论文链接åQ?/span></p> <p style="text-align: justify; line-height: 2em;"><span style="font-size: 16px; font-family: 宋体;">https://onlinelibrary.wiley.com/doi/10.1002/anie.201905966åQˆAngew. 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