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Compounds inhibiting COX-2 and iNOS promoter activities

机译:抑制COX-2和iNOS启动子活性的化合物

摘要

A new chemical compound for treating human inflammatory diseases, tissue damage, stroke, septic shock and cancer. This chemical compound is produced from a process including the following steps: (a) washing human foreskin fibroblasts with a fresh DMEM medium then incubated in a fresh medium containing 2.5%-10% fetal bovine serum for at least 8 hours to form a proliferating phase medium (PPM); (b) subjecting the proliferating phase medium to a 10-kDa ultrafiltration membrane to separate the proliferating phase medium into a 10 kDa fraction, which passes through the 10-kDa ultrafiltration membrane, and a 10 kDa fraction, which is retained by the 10-kDa ultrafiltration membrane; (c) Chromatographing the 10 kDa fraction on a Superdex 30 column by FPLC to separate the 10 kDa fraction into five post-FPLC fractions; (d) Injecting the second post-FPLC fraction into a C18 column in a HPLC system with a gradient elute from 10% to 50% acetonitrile and water containing 0.1% trifluoroacetic acid, to separate the second post-FPLC fraction into five post-HPLC fractions; and (e) collecting the fourth post-FPLC fraction for further purification. Fluorescence spectroscopy shows that this product is a derivative of trypophan or trypophan-like, and mass spectrometry indicates that it has a molecular weight of about 604 daltons with a minor peak having a molecular weight of about 779 daltons.
机译:一种用于治疗人类炎症性疾病,组织损伤,中风,败血性休克和癌症的新型化合物。该化合物是通过以下步骤生产的:(a)用新鲜的DMEM培养基洗涤人包皮成纤维细胞,然后在含有2.5%-10%胎牛血清的新鲜培养基中孵育至少8小时以形成增殖相中(PPM); (b)将增殖相培养基置于10 kDa的超滤膜中,以将增殖相培养基分离成<10 kDa的馏分(通过10 kDa的超滤膜)和> 10 kDa的馏分,保留在10 kDa超滤膜(c)通过FPLC在Superdex 30色谱柱上层析<10 kDa馏分,将<10 kDa馏分分离为五个FPLC后馏分; (d)在HPLC系统中,将FPLC后的第二馏分注入C 18 色谱柱中,用10%至5​​0%乙腈和含0.1%三氟乙酸的水梯度洗脱,以分离第二步-FPLC馏分分为五个HPLC后馏分; (e)收集FPLC后的第四部分以进一步纯化。荧光光谱法表明该产物是锥虫或类锥虫的衍生物,质谱表明其分子量为约604道尔顿,次要峰的分子量为约779道尔顿。

著录项

  • 公开/公告号US2002015739A1

    专利类型

  • 公开/公告日2002-02-07

    原文格式PDF

  • 申请/专利权人 WU KENNETH K.;

    申请/专利号US20010920121

  • 发明设计人 KENNETH K. WU;

    申请日2001-07-31

  • 分类号A61K35/12;

  • 国家 US

  • 入库时间 2022-08-22 00:47:53

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