头孢色菌素 | 25908-26-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 萘并吡喃类
• 中文名称: 头孢色菌素
• 英文名称: chephalochromin
• 英文别名: cephalochromin；5,6,8-trihydroxy-2-methyl-9-(5,6,8-trihydroxy-2-methyl-4-oxo-2,3-dihydrobenzo[g]chromen-9-yl)-2,3-dihydrobenzo[g]chromen-4-one
• CAS: 25908-26-3
• 化学式: C₂₈H₂₂O₁₀
• 分子量: 518.477
• InChiKey: JGQBYBXYRUCBQY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  38
• 可旋转键数：
  1
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  174
• 氢给体数：
  6
• 氢受体数：
  10

反应信息

• 作为反应物：
  描述：

  重氮甲烷 、 头孢色菌素 以 乙醚 为溶剂， 反应 4.0h， 生成 cephalochromin 5,5'-dimethyl ether 、 cephalochromin 5-methyl ether
  参考文献：
  名称：

  Inhibitory Effects of Fungal Bis(naphtho-.GAMMA.-pyrone) Derivatives on Nitric Oxide Production by a Murine Macrophage-Like Cell Line, RAW 264.7, Activated by Lipopolysaccharide and Interferon-.GAMMA.

  摘要：

  研究了六种真菌双（萘并-γ-吡喃酮）衍生物对由脂多糖和干扰素-γ 激活的鼠巨噬细胞样细胞系 RAW 264.7 产生一氧化氮（NO）的抑制作用。这些衍生物中，毛色素 (4) (IC50: 0.8 μM)、头孢色素 (1) (IC50 1.5 μM) 和二氢异乌芪苷 A (6) (IC50 2.8) μM)表现出很强的抑制活性。双(萘并-γ-吡喃酮)衍生物不影响诱导型一氧化氮合酶(iNOS)的酶活性。然而，这些衍生物显着降低了 iNOS 蛋白的诱导和 iNOS mRNA 的表达。这些结果表明双(萘并-γ-吡喃酮)衍生物具有抑制活化巨噬细胞产生NO的药理能力。

  DOI：

  10.1248/bpb.28.786

文献信息

• NOVEL METHODS FOR RAPID DRUG SUSCEPTIBILITY TESTING AND DRUG SCREENS FOR GROWING AND NON-GROWING CELLS OF PROKARYOTIC AND EUKARYOTIC ORIGIN
  申请人：Zhang, Ying

  公开号：EP3321371A1

  公开（公告）日：2018-05-16

  The presently disclosed subject matter provides methods, compositions, and kits for extremely rapid assessment of drug susceptibility of growing as well as non-growing cells of prokaryotic and also eukaryotic origins, without the need for organism growth, which is in contrast to the current growth-dependent methods.This growth-independent new methodology achieves extremely rapid drug susceptibility testing results previously not possible. Methods for rapidly identifying compounds with inhibitory activity against both growing and non-growing cells in real-time continuous manner with previously unachievable efficiency in drug screens using the novel methodology are also provided. Cell cultures are incubated with a drug or test agent and with a staining mixture containing a first fluorescent dye indicative the emission of which is indicative of live cells (e.g. SYBR Green I) and a second fluorescent dye indicative emitting a different color, the emission of which is indicative of dead cells (e.g. Propidium iodide). The ratio of the intensities of the emitted fluorescence of the dyes is indicative of the percentage live and dead cells in the culture.

  与目前依赖生长的方法相比，本公开的主题提供了无需生物体生长即可对原核和真核的生长和非生长细胞的药物敏感性进行极快速评估的方法、组合物和试剂盒，这种不依赖生长的新方法实现了以前无法实现的极快速药物敏感性测试结果。此外，还提供了实时连续地快速鉴定对生长细胞和非生长细胞具有抑制活性的化合物的方法，这种方法在使用新方法进行药物筛选时具有以前无法实现的效率。细胞培养物与药物或测试剂以及染色混合物一起孵育，染色混合物含有第一种荧光染料指示剂，其发射的荧光指示剂可指示活细胞（如 SYBR 绿 I）和第二种发出不同颜色的荧光染料指示剂，其发射的荧光指示剂可指示死细胞（如碘化丙啶）。染料发射荧光强度的比值表示培养液中活细胞和死细胞的百分比。
• METHODS AND COMPOSITIONS FOR THE TREATMENT OR PREVENTION OF PATHOLOGICAL CARDIAC REMODELING AND HEART FAILURE
  申请人：University Of Rochester

  公开号：EP2279009A2

  公开（公告）日：2011-02-02
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  公开号：EP3897602A1

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