CN103655552B - Manzamenone O在治疗胰腺癌药物中的应用 - Google Patents
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- MQOSGVWARDSXKJ-PDOPHQTESA-N methyl (3S,3aR,4R,6S,7R)-3-[(3aR,5S,6aS)-5-hexadecyl-5-hydroxy-2-oxo-6,6a-dihydro-3H-furo[3,2-b]furan-3a-yl]-4-heptadecanoyl-6-hydroxy-6-methyl-2-oxo-7-pentadecyl-3a,4,5,7-tetrahydro-3H-indene-1-carboxylate Chemical compound CCCCCCCCCCCCCCCCC(=O)[C@@H]1C[C@](C)(O)[C@H](CCCCCCCCCCCCCCC)C2=C(C(=O)OC)C(=O)[C@H]([C@@]34[C@@H](OC(=O)C3)C[C@](O)(CCCCCCCCCCCCCCCC)O4)[C@@H]12 MQOSGVWARDSXKJ-PDOPHQTESA-N 0.000 title claims abstract description 58
- 206010061902 Pancreatic neoplasm Diseases 0.000 title claims abstract description 23
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 title claims abstract description 23
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- 229940079593 drug Drugs 0.000 title abstract description 10
- 201000002528 pancreatic cancer Diseases 0.000 claims abstract description 22
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Abstract
本发明公开了Manzamenone O在治疗胰腺癌药物中的应用，属于药物新用途技术领域。本发明通过体外MTT抗肿瘤活性评价发现，Manzamenone O对人胰腺癌细胞株PANC-1和BXPC-3的生长也具有显著的抑制作用。因此，Manzamenone O能用于制备抗胰腺癌药物，具有良好的开发应用前景。对于本发明涉及的Manzamenone O在制备治疗胰腺癌药物中的用途属于首次公开，而且其对于胰腺癌细胞的抑制活性强，具有显著的进步。
Description
技术领域
本发明涉及化合物Manzamenone O的新用途，尤其涉及Manzamenone O在制备治疗胰腺癌药物中的应用。
背景技术
癌症是对人类生命健康危害最大的疾病之一，每年都有大量的人死于癌症。抗癌药物的研发一直是药学研究的热点。抗肿瘤药物中有74%是天然产物或其衍生物，如紫杉醇及其衍生物就是目前临床上应用效果比较好的抗肿瘤药物。因此，从天然产物中寻找抗癌化合物或先导化合物具有重要的意义。
本发明涉及的化合物Manzamenone O是一个2013年发表（Naonobu Tanaka，et al.,Manzamenone O,New Trimeric Fatty Acid Derivative from a Marine Sponge Plakortissp.Organic Letters，2013,15(10):2518–2521.）的新化合物，该化合物拥有全新的骨架类型，目前的用途发现其抗微生物（Naonobu Tanaka，et al.,Manzamenone O,New TrimericFatty Acid Derivative from a Marine Sponge Plakortis sp.Organic Letters，2013,15(10):2518–2521.），本发明涉及的Manzamenone O在制备治疗胰腺癌药物中的用途属于首次公开。
发明内容
本发明的目的在于根据现有Manzamenone O研究中未发现其具有抗胰腺癌活性的报道的现状，提供了Manzamenone O在制备抗胰腺癌药物中的应用。
所述化合物Manzamenone O结构如式（Ⅰ）所示：
本发明通过体外MTT抗肿瘤活性评价发现，Manzamenone O对人胰腺癌细胞株PANC-1和BXPC-3的生长也具有显著的抑制作用，抑制这2株细胞生长的IC50值分别为1.84±0.68μM和1.36±0.28μM。因此，Manzamenone O能用于制备抗胰腺癌药物，具有良好的开发应用前景。
对于本发明涉及的Manzamenone O在制备治疗胰腺癌药物中的用途属于首次公开，由于骨架类型属于全新的骨架类型，而且其对于胰腺癌细胞的抑制活性强，具备突出的实质性特点，同时用于胰腺癌的防治显然具有显著的进步。
具体实施方式
以下通过实施例对本发明作进一步详细的说明，但本发明的保护范围不受具体实施例的任何限制，而是由权利要求加以限定。
本发明所涉及化合物Manzamenone O的制备方法参见文献（Naonobu Tanaka，et al.,Manzamenone O,New Trimeric Fatty Acid Derivative from a Marine Sponge Plakortissp.Organic Letters，2013,15(10):2518–2521.），按照上述方法制备化合物ManzamenoneO。
实施例1：本发明所涉及化合物Manzamenone O片剂的制备：
取5克化合物Manzamenone O，加入糊精195克，混匀，常规压片制成1000片。
实施例2：本发明所涉及化合物Manzamenone O胶囊剂的制备：
取5克化合物Manzamenone O，加入淀粉195克，混匀，装胶囊制成1000粒。
下面通过药效学实验来进一步说明其药物活性。
实验例：采用MTT法评价化合物Manzamenone O对人胰腺癌细胞株的生长抑制作用
1.方法：处于生长对数期的细胞：人胰腺癌细胞株PANC-1和BXPC-3（购买自中国科学院细胞库）以1.5×104浓度种于96孔板中。细胞培养24h贴壁后吸去原来的培养基。试验分为空白对照组、药物处理组。空白组更换含10%胎牛血清的1640培养基；药物处理组更换含浓度为100μM，50μM，10μM，1μM，0.1μM，0.01μM和0.001μM的Manzamenone O的培养基。培养48h后，加入浓度5mg/mL的MTT，继续放于CO2培养箱培养4h，然后沿着培养液上部吸去100μL上清，加入100μL DMSO，暗处放置10min，利用酶标仪（Sunrise公司产品）测定吸光值(波长570nm)，并根据吸光值计算细胞存活情况，每个处理设6个重复孔。细胞存活率(%)=ΔOD药物处理/ΔOD空白对照×100。
2.结果：Manzamenone O对人胰腺癌细胞株PANC-1和BXPC-3的生长具有显著的抑制作用。该化合物抑制人胰腺癌细胞株PANC-1和BXPC-3生长的IC50值分别为1.84±0.68μM和1.36±0.28μM。
由上述实施例表明，本发明的Manzamenone O对人胰腺癌细胞株PANC-1和BXPC-3的生长具有很好的抑制作用。由此证明，本发明的Manzamenone O具有抗胰腺癌活性，能用于制备抗胰腺癌药物。
Claims (1)
1.Manzamenone O在制备治疗胰腺癌药物中的应用，所述化合物Manzamenone O结构如式(Ⅰ)所示：
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT201700078586A1 (it) * | 2017-07-13 | 2019-01-13 | Univ Della Calabria | Derivati 6,6a-diidrofuro[3,2-b]furan-2-(5H)onici, loro preparazione e uso nel trattamento dei tumori |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102861050A (zh) * | 2012-10-27 | 2013-01-09 | 吴俊华 | Houttuynoid A在治疗胰腺癌药物中的应用 |
| CN102885809A (zh) * | 2012-10-25 | 2013-01-23 | 南京大学 | Aphanamixoid A在治疗胰腺癌药物中的应用 |
| CN103251638A (zh) * | 2013-06-03 | 2013-08-21 | 南京正亮医药科技有限公司 | Polyflavanostilbene A在制备治疗胰腺癌药物中的应用 |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102885809A (zh) * | 2012-10-25 | 2013-01-23 | 南京大学 | Aphanamixoid A在治疗胰腺癌药物中的应用 |
| CN102861050A (zh) * | 2012-10-27 | 2013-01-09 | 吴俊华 | Houttuynoid A在治疗胰腺癌药物中的应用 |
| CN103251638A (zh) * | 2013-06-03 | 2013-08-21 | 南京正亮医药科技有限公司 | Polyflavanostilbene A在制备治疗胰腺癌药物中的应用 |
Non-Patent Citations (1)
| Title |
|---|
| Manzamenone O, New Trimeric Fatty Acid Derivative from a Marine Sponge Plakortis sp.;Naonobu Tanaka等;《Organic Letters》;20130507;第15卷(第10期);第2518-2521页 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT201700078586A1 (it) * | 2017-07-13 | 2019-01-13 | Univ Della Calabria | Derivati 6,6a-diidrofuro[3,2-b]furan-2-(5H)onici, loro preparazione e uso nel trattamento dei tumori |
| EP3428169A1 (en) * | 2017-07-13 | 2019-01-16 | Universita' Della Calabria | 6,6a-dihydro furo[3,2-b]furan-2-(5h)one derivatives, their preparation and use for treating tumors |
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