tyropeptin A | 402830-01-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: tyropeptin A
• 英文别名: isovaleryl-L-tyrosyl-L-valyl-DL-tyrosinal；(2S)-2-[[(2S)-3-(4-hydroxyphenyl)-2-(3-methylbutanoylamino)propanoyl]amino]-N-[1-(4-hydroxyphenyl)-3-oxopropan-2-yl]-3-methylbutanamide
• CAS: 402830-01-7
• 化学式: C₂₈H₃₇N₃O₆
• 分子量: 511.618
• InChiKey: OSMJFYFZOAVCNP-KLZDYHPHSA-N

物化性质

• 沸点：
  850.5±65.0 °C(Predicted)
• 密度：
  1.195±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  37
• 可旋转键数：
  13
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  145
• 氢给体数：
  5
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  tyropeptin A 在 盐酸 、 sodium tetrahydroborate 作用下， 以 甲醇 为溶剂， 反应 20.0h， 生成 D-酪氨醇
  参考文献：
  名称：

  酪蛋白A和B，Kitasatospora sp。生产的新型蛋白酶体抑制剂。MK993-dF2。二。结构确定与综合。

  摘要：

  酪蛋白A和B的结构，Kitasatospora sp。生产的新型蛋白酶体抑制剂。通过分析各种NMR实验确定MK993-dF2。酪蛋白的1 H和13 C NMR由于醛基的存在而变得复杂。因此，酪蛋白被硼氢化钠转化为它们的醇。这些醇衍生物给出可分配的NMR光谱。通过分析来自酪肽的酸水解产物来确定酪肽的立体化学，并通过总合成进一步证实。发现酪蛋白A和B的结构分别是异戊酰基-L-酪氨酰基-L-戊酰基-DL-酪氨酸和正丁酰基-L-酪氨酰基-L-亮氨酰-DL-酪氨酸。

  DOI：

  10.7164/antibiotics.54.1004
• 作为产物：
  描述：

  L-酪氨醇盐酸盐 在 palladium on activated charcoal sodium hydroxide 、 pyridine-SO3 complex 、 氢气 、 sodium hydride 、 1-羟基苯并三唑一水物 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 、 三氟乙酸 作用下， 以 1,4-二氧六环 、 二氯甲烷 、 二甲基亚砜 、 N,N-二甲基甲酰胺 为溶剂， 反应 84.17h， 生成 tyropeptin A
  参考文献：
  名称：

  酪蛋白A和B，Kitasatospora sp。生产的新型蛋白酶体抑制剂。MK993-dF2。二。结构确定与综合。

  摘要：

  酪蛋白A和B的结构，Kitasatospora sp。生产的新型蛋白酶体抑制剂。通过分析各种NMR实验确定MK993-dF2。酪蛋白的1 H和13 C NMR由于醛基的存在而变得复杂。因此，酪蛋白被硼氢化钠转化为它们的醇。这些醇衍生物给出可分配的NMR光谱。通过分析来自酪肽的酸水解产物来确定酪肽的立体化学，并通过总合成进一步证实。发现酪蛋白A和B的结构分别是异戊酰基-L-酪氨酰基-L-戊酰基-DL-酪氨酸和正丁酰基-L-酪氨酰基-L-亮氨酰-DL-酪氨酸。

  DOI：

  10.7164/antibiotics.54.1004

文献信息

• Flaxseed lignan complex, methods of using and compositions thereof
  申请人：Christofidou-Solomidou Melpo

  公开号：US10449224B2

  公开（公告）日：2019-10-22

  This invention relates to methods and compositions for treating pathological lung conditions using whole-grain flaxseed or flaxseed lignans (isolated in form of the lignan precursor Secoisolariciresinol diglucoside (SDG) directly from whole-grain flaxseed or chemically synthesized directly into the mammalian, readily metabolizable forms, Enterodiol (ED) or Enterolactone (EL). Such pathological condition result from oxidative lung injury such as ischemia-reperfusion injury (related to lung transplantation), radiation fibrosis and cancer. Specifically, the invention is directed to the use of flaxseed lignans in the treatment of acute and chronic lung injury as well as cancer.

  本发明涉及使用全粒亚麻籽或亚麻籽木脂素（直接从全粒亚麻籽中分离出木脂素前体 Secoisolariciresinol diglucoside (SDG)，或直接化学合成哺乳动物易代谢形式 Enterodiol (ED) 或 Enterolactone (EL)）治疗病理性肺部疾病的方法和组合物。 这种病理状态源于氧化性肺损伤，如缺血再灌注损伤（与肺移植有关）、放射性纤维化和癌症。 具体而言，本发明涉及亚麻籽木酚素在治疗急性和慢性肺损伤以及癌症中的应用。
• Reducing axon degeneration with proteasome inhibitors
  申请人：He Zhigang

  公开号：US20060074028A1

  公开（公告）日：2006-04-06

  Reduced degeneration of an axon predetermined to be subject to degenerative neuropathy in a term patient is effected by contacting the axon in situ with an effective amount of a ubiquitin-proteasome system (UPS) inhibitor sufficient to reduce degeneration of the axon; and detecting a resultant reduction in the degeneration of the axon in situ.

  通过使轴突在原位与有效量的泛素-蛋白酶体系统（UPS）抑制剂接触，足以减少轴突的变性，并检测轴突在原位变性的减少情况，从而减少预定患有神经退行性病变的轴突的变性。
• RADIOIMAGING MOIETIES COUPLED TO PEPTIDEASE-BINDING MOIETIES FOR IMAGING TISSUES AND ORGANS THAT EXPRESS PEPTIDASES
  申请人：Babich J. W.

  公开号：US20080213172A1

  公开（公告）日：2008-09-04

  Conjugates, methods and kits are described for imaging tissues and organs that express one or more peptidases. In a preferred embodiment of the invention, a series of di-(2-pyridylmethyl)amine (D) ligands, which can bind M(CO) 3 + [M=Tc or Re], were coupled to lisinopril (L). Aliphatic tethers with varying number of methylene groups (3, 4, 5, and 7; D(C 4 )L, D(C 5 )L, D(C 6 )L, and D(C 8 )L, respectively) were utilized, with in vitro inhibitory activity increasing with increasing number of methylene groups. The D(C 8 )L conjugate was observed to be significantly more potent than D(C 4 )L. In vivo specificity for ACE was studied in both tissue distribution and gamma imaging studies, demonstrating localization in tissues with high ACE content. Localization was blocked by pretreatment with lisinopril.
• FLAXSEED LIGNAN COMPLEX, METHODS OF USING AMD COMPOSITIONS THEREOF
  申请人：Christofidou-Solomidou Melpo

  公开号：US20100239696A1

  公开（公告）日：2010-09-23

  This invention relates to methods and compositions for treating pathological lung conditions using whole-grain flaxseed or flaxseed lignans (isolated in form of the lignan precursor Secoisolariciresinol diglucoside (SDG) directly from whole-grain flaxseed or chemically synthesized directly into the mammalian, readily metabolizable forms, Enterodiol (ED) or Enterolactone (EL). Such pathological condition result from oxidative lung injury such as ischemia-reperfusion injury (related to lung transplantation), radiation fibrosis and cancer. Specifically, the invention is directed to the use of flaxseed lignans in the treatment of acute and chronic lung injury as well as cancer.
• FLAXSEED LIGNAN COMPLEX AND ITS USE THEREOF
  申请人：CHRISTOFIDOU-SOLOMIDOU Melpo

  公开号：US20110300247A1

  公开（公告）日：2011-12-08

  The invention relates compositions and methods for treating pathological lung conditions using whole-grain flaxseed or flaxseed lignans. Specifically, the invention relates to the dietary use of flaxseed lignans.