{"id":11881,"date":"2016-11-09T08:24:14","date_gmt":"2016-11-09T00:24:14","guid":{"rendered":"\/\/www.gsbet888.com\/?p=11881"},"modified":"2019-08-02T18:53:51","modified_gmt":"2019-08-02T10:53:51","slug":"%e5%a7%9c%e9%bb%84%e7%b4%a0-curcumin%ef%bc%88%e5%92%96%e5%96%b1%e4%b8%ad%e7%9a%84%e6%8a%97%e7%99%8c%e6%88%90%e5%88%86%ef%bc%89","status":"publish","type":"post","link":"\/\/www.gsbet888.com\/molecule\/2016\/11\/%e5%a7%9c%e9%bb%84%e7%b4%a0-curcumin%ef%bc%88%e5%92%96%e5%96%b1%e4%b8%ad%e7%9a%84%e6%8a%97%e7%99%8c%e6%88%90%e5%88%86%ef%bc%89.html","title":{"rendered":"\u59dc\u9ec4\u7d20 curcumin\uff08\u5496\u55b1\u4e2d\u7684\u6297\u764c\u6210\u5206\uff09"},"content":{"rendered":"

$\"crucumin-1\"$ <\/p>\n

\u59dc\u9ec4\u7d20(curcumin)<\/strong>\u662f\u4e00\u79cd\u4ece\u59dc\u9ec4\uff08Curcuma longa<\/em>\uff09\u6839\u830e\u4e2d\u63d0\u53d6\u5f97\u5230\u7684\u9ec4\u8272\u8272\u7d20\uff0c\u4ece\u7ed3\u6784\u6765\u770b\u662f\u4e00\u79cd\u591a\u915a\u7c7b\u5316\u5408\u7269\u3002<\/p>\n

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\u5386\u53f2\u30fb\u7528\u9014<\/strong><\/li>\n<\/ul>\n
\u6709\u6570\u636e\u8868\u660e\uff0c\u5370\u5ea6\u4eba\u7531\u4e8e\u5e38\u5e74\u5403\u5496\u55b1\uff0c\u60a3\u764c\u51e0\u7387\u6bd4\u4e0d\u5403\u5496\u55b1\u7684\u8981\u4f4e\uff0c\u800c\u5496\u55b1\u7684\u9ec4\u8272\u5c31\u662f\u7531\u6765\u4e8e\u59dc\u9ec4\u7d20\u3002\u59dc\u9ec4\u7d20\u5177\u6709\u6297\u6c27\u5316\u3001\u6297\u764c\u4f5c\u7528\u3002\u65e9\u57281988\u5e74\u5f00\u59cb\uff0c\u7f8e\u56fd\u56fd\u7acb\u764c\u75c7\u7814\u7a76\u6240\u5c31\u5f00\u59cb\u4e86\u5bf9\u59dc\u9ec4\u7d20\u7684\u6297\u764c\u7814\u7a76\u3002\u8fd1\u5e74\u6765\uff0c\u968f\u7740\u8367\u5149\u6807\u8bb0\u6280\u672f\u7684\u53d1\u5c55\uff0c\u901a\u8fc7\u5408\u6210\u59dc\u9ec4\u7d20\u7684\u5206\u5b50\u63a2\u9488\uff08GO-Y086<\/strong>\uff09\u53d1\u73b0\u4e86\u59dc\u9ec4\u7d20\u7684\u6297\u764c\u53d7\u4f53\u86cb\u767dFUBP<\/strong>\uff0c\u4e3a\u5176\u6297\u764c\u673a\u5236\u63d0\u4f9b\u4e86\u4f9d\u636e^{(1)<\/sup>
\n<\/p>\n}
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\u5173\u8054\u6587\u732e<\/strong><\/li>\n<\/ul>\n
(1) \u201cKSRP\/FUBP2 Is a Binding Protein of GO-Y086, a Cytotoxic Curcumin Analogue\u201d<\/p>\n
Yamakoshi, H.; Kanoh, N.; Kudo, C.; Sato, A.; Ueda, K.; Muroi, M.; Kon, S.; Satake, M.; Ohori, H.; Ishioka, C. ACS Med. Chem. Lett.\u00a0<\/i>2010<\/b>, 1<\/i>, 273-276. DOI:?10.1021\/ml1000454<\/a><\/p>\n
Bis(arylmethylidene)acetone derivatives are an important class of curcumin analogues that exhibit various biological and pharmacological activities. We herein report that GO-Y086, a biotinylated bis(arylmethylidene)acetone, inhibits cancer cell growth. We also show that GO-Y086 specifically interacts with the nuclear protein KSRP\/FUBP2 by covalent modification. GO-Y086 markedly suppresses the expression of the c-Myc protein, which plays an important role in cellular proliferation and whose expression is regulated by KSRP\/FUBP2.<\/p><\/blockquote>\n
(2) \u201cStructure\u2013activity relationship of C5-curcuminoids and synthesis of their molecular probes thereof\u201d<\/p>\n
Yamakoshi, H.; Ohori, H.; Kudo, C.; Sato, A.; Kanoh, N.; Ishioka, C.; Shibata, H.; Iwabuchi, Y. Bioorg. Med. Chem.<\/i> 2010<\/b>, 18<\/i>, 1083-1092. DOI:10.1016\/j.bmc.2009.12.045<\/a><\/p>\n
$\"1-s2-0-s0968089609011377-fx1\"$ <\/p>\n
A series of novel analogues of 1,5-bis(4-hydroxy-3-methoxyphenyl)-penta-(1E<\/em>,4E<\/em>)-1,4-dien-3-one (C_{5<\/sub>-curcumin), which is a natural analogue of curcumin isolated from the rhizomes of\u00a0Curcuma domestica<\/em>\u00a0Val. (Zingiberacea), were synthesized and evaluated for their cytotoxicities against human colon cancer cell line HCT-116 to conclude the SAR of C_{5<\/sub>-curcuminoids for further development of their use in cancer chemotherapy: (1) Bis(arylmethylidene)acetone serves as a promising skeleton for eliciting cytotoxicity. (2) The 3-oxo-1,4-pentadiene structure is essential for eliciting cytotoxicity. (3) As for the extent of the aromatic substituents, hexasubstituted compounds exhibit strong activities, in which 3,4,5-hexasubstitution results in the highest potency. (5) The symmetry between two aryl rings is not an essential requirement for bis(arylmethylidene)acetones to elicit cytotoxicity. (6)\u00a0para<\/em>-Positions allows the installation of additional functional groups for use as molecular probes. By taking advantage of the SAR diagram, we have elaborated several advanced derivatives having GI_{50<\/sub>\u00a0of single-digit micromolar potencies that will function as molecular probes to target and\/or report key biomolecules interacting with curcumin and C_{5<\/sub>-curcumin.<\/p><\/blockquote>\n}}}}
\u672c\u6587\u7248\u6743\u5c5e\u4e8e\u00a0Chem-Station\u5316\u5b66\u7a7a\u95f4<\/a>\uff0c \u6b22\u8fce\u70b9\u51fb\u6309\u94ae\u5206\u4eab\uff0c\u672a\u7ecf\u8bb8\u53ef\uff0c\u8c22\u7edd\u8f6c\u8f7d\uff01<\/strong> <\/p>\n","protected":false},"excerpt":{"rendered":"\u59dc\u9ec4\u7d20(curcumin)\u662f\u4e00\u79cd\u4ece\u59dc\u9ec4\uff08Curcuma longa\uff09\u6839\u830e\u4e2d\u63d0\u53d6\u5f97\u5230\u7684\u9ec4\u8272\u8272\u7d20\uff0c\u4ece\u7ed3\u6784\u6765\u770b\u662f\u4e00\u79cd\u591a\u915a\u7c7b\u5316\u5408\u7269\u3002 \u5386\u53f2\u30fb\u7528\u9014 \u6709\u6570\u636e\u8868\u660e\uff0c\u5370\u5ea6\u4eba\u7531\u4e8e\u5e38\u5e74\u5403\u5496\u55b1\uff0c\u60a3\u764c\u51e0\u7387\u6bd4\u4e0d\u5403\u5496\u55b1\u7684\u8981\u4f4e\uff0c\u800c\u5496\u55b1\u7684\u9ec4\u8272\u5c31\u662f\u7531\u6765\u4e8e\u59dc\u9ec4\u7d20\u3002\u59dc\u9ec4\u7d20\u5177\u6709\u6297\u6c27\u5316\u3001\u6297\u764c\u4f5c\u7528\u3002\u65e9\u57281988\u5e74\u5f00\u59cb\uff0c\u7f8e\u56fd\u56fd\u7acb\u764c\u75c7\u7814\u7a76\u6240\u5c31\u5f00\u59cb\u4e86\u5bf9\u59dc\u9ec4\u7d20\u7684\u6297\u764c\u7814\u7a76\u3002\u8fd1\u5e74\u6765\uff0c\u968f\u7740\u8367\u5149\u6807\u8bb0\u6280\u672f\u7684\u53d1\u5c55\uff0c\u901a\u8fc7\u5408\u6210\u59dc\u9ec4\u7d20\u7684\u5206\u5b50\u63a2\u9488\uff08GO-Y086\uff09\u53d1\u73b0\u4e86\u59dc\u9ec4\u7d20\u7684\u6297\u764c\u53d7\u4f53\u86cb\u767dFUBP\uff0c\u4e3a\u5176\u6297\u764c\u673a\u5236\u63d0\u4f9b\u4e86\u4f9d\u636e(1) \u540c\u65f6\uff0c\u4e0d\u4ec5\u4ec5\u662f\u6297\u764c\u6d3b\u6027\uff0c\u6700\u8fd1\u53c8\u53d1\u73b0\u8be5\u7269\u8d28\u663e\u793a\u51fa\u6297\u963f\u5c14\u8328\u6d77\u9ed8\u7684\u6548\u679c\u3002 \u7531\u4e8e\u59dc\u9ec4\u7d20\u542b\u6709\u591a\u79cd\u6709\u76ca\u6d3b\u6027\uff0c\u56e0\u6b64\u542b\u6709\u59dc\u9ec4\u7d20\u7684\u591a\u79cd\u5065\u5eb7\u98df\u54c1\u5982\u96e8\u540e\u6625\u7b0b\u3002\u6bd4\u5982\u8bf4\u59dc\u9ec4\u7d20\u7684\u89e3\u9152\u996e\u6599\uff0c\u8fd9\u662f\u56e0\u4e3a\u59dc\u9ec4\u7d20\u53ef\u4ee5\u6d3b\u5316\u80c6\u6c41\u7684\u5206\u6ccc\uff0c\u7ef4\u6301\u809d\u810f\u6574\u4f53\u7684\u826f\u597d\u7684\u529f\u80fd\u3002 \u5173\u8054\u6587\u732e (1) \u201cKSRP\/FUBP2 Is a Binding Protein of GO-Y086, a Cytotoxic Curcumin Analogue\u201d Yamakoshi, H.; Kanoh, N.; Kudo, C.; Sato, A.; Ueda, K.; Muroi, M.; Kon, S.; Satake, M.; Ohori, H.; Ishioka, C. ACS Med. Chem. Lett.\u00a02010, 1, 273-276. DOI:?10.1021\/ml1000454 Bis(arylmethylidene)acetone derivatives are an important class of curcumin analogues that exhibit various biological and pharmacological activities. We herein report that GO-Y086, a biotinylated bis(arylmethylidene)acetone, inhibits cancer cell growth. We also show that GO-Y086 specifically interacts with the nuclear protein KSRP\/FUBP2 by covalent modification. GO-Y086 markedly suppresses the expression of the c-Myc protein, which plays an important role in cellular proliferation and whose […]","protected":false},"author":5,"featured_media":11885,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"jetpack_post_was_ever_published":false,"_jetpack_newsletter_access":"","_jetpack_dont_email_post_to_subs":false,"_jetpack_newsletter_tier_id":0,"_jetpack_memberships_contains_paywalled_content":false,"_jetpack_memberships_contains_paid_content":false,"footnotes":"","jetpack_publicize_message":"","jetpack_publicize_feature_enabled":true,"jetpack_social_post_already_shared":true,"jetpack_social_options":{"image_generator_settings":{"template":"highway","enabled":false},"version":2}},"categories":[869],"tags":[1574,826],"jetpack_publicize_connections":[],"jetpack_featured_media_url":"https:\/\/assets.www.gsbet888.com\/uploads\/2016\/10\/curcumine.png","jetpack_shortlink":"https:\/\/wp.me\/p96op1-35D","jetpack_sharing_enabled":true,"_links":{"self":[{"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/posts\/11881"}],"collection":[{"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/users\/5"}],"replies":[{"embeddable":true,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/comments?post=11881"}],"version-history":[{"count":2,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/posts\/11881\/revisions"}],"predecessor-version":[{"id":27569,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/posts\/11881\/revisions\/27569"}],"wp:featuredmedia":[{"embeddable":true,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/media\/11885"}],"wp:attachment":[{"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/media?parent=11881"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/categories?post=11881"},{"taxonomy":"post_tag","embeddable":true,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/tags?post=11881"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}