puerarin | 76436-63-0

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 异黄酮类化合物
• 英文名称: puerarin
• 英文别名: genistein 8-C-glucoside；5,7-dihydroxy-3-(4-hydroxyphenyl)-8-[(3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxychromen-4-one
• CAS: 76436-63-0
• 化学式: C₂₁H₂₀O₁₁
• 分子量: 448.383
• InChiKey: RXUWDKBZZLIASQ-VZDZYFQOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  32
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  186
• 氢给体数：
  7
• 氢受体数：
  11

反应信息

• 作为产物：
  描述：

  genistein 8-C-apiosyl(1-6) glucoside 在 盐酸 作用下， 以 甲醇 为溶剂， 反应 2.0h， 生成 methyl D-apiofuranoside 、 puerarin
  参考文献：
  名称：

  Kinjo, Jun-Ei; Furusawa, Jun-Ichi; Baba, Junko, Chemical and pharmaceutical bulletin, 1987, vol. 35, # 12, p. 4846 - 4850

  摘要：

  DOI：

文献信息

• NEW C-GLYCOSYLPOLYPHENOL ANTIDIABETIC AGENTS, EFFECT ON GLUCOSE TOLERANCE AND INTERACTION WITH BETA-AMYLOID. THERAPEUTIC APPLICATIONS OF THE SYNTHESIZED AGENT(S) AND OF GENISTA TENERA ETHYL ACETATE EXTRACTS CONTAINING SOME OF THOSE AGENTS
  申请人：UNIVERSIDADE DE LISBOA

  公开号：US20150031639A1

  公开（公告）日：2015-01-29

  The present invention concerns the antidiabetic-activity of compounds type A, namely of 8-β-D-glucosylgenistein, which is not toxic to eukaryotic cells and has demonstrated to produce complete normalization of fasting hyperglycaemia, to reduce excessive postprandial glucose excursion, to increase glucose-induced insulin secretion and insulin sensitivity. An alternative synthesis for this molecular entity and its binding ability to β-amyloid oligomers is also included in the present invention, which also comprises Genista tenera ethyl acetate extract for use as antihyperglycaemic, agent i.e. for lowering blood glucose levels in mammals that are pre-diabetic or have type 2 or type 1 diabetes. The inhibitory activity of α-glucosidase by Genista tenera ethyl acetate and butanol extracts and that of glucose-6-phosphatase by these two extracts and the diethyl ether plant extract is also part of the present invention.

  本发明涉及A型化合物的抗糖尿病活性，即8-β-D-葡萄糖基异黄酮的抗糖尿病活性。该化合物对真核细胞无毒，并已证明能完全正常化空腹高血糖，减少过度餐后血糖波动，增加葡萄糖诱导的胰岛素分泌和胰岛素敏感性。本发明还包括该分子实体的另一种合成方法以及其与β-淀粉样寡聚体的结合能力，同时还包括Genista tenera乙酸乙酯提取物用作抗高血糖剂，即用于降低处于糖尿病前期或已患2型或1型糖尿病的哺乳动物的血糖水平。本发明还包括Genista tenera乙酸乙酯和丁醇提取物的α-葡萄糖苷酶抑制活性以及这两种提取物和乙醚植物提取物的葡萄糖-6-磷酸酶抑制活性。
• US9775856B2
  申请人：——

  公开号：US9775856B2

  公开（公告）日：2017-10-03
• [EN] THERAPEUTIC RELEASE AGENTS<br/>[FR] AGENTS DE LIBÉRATION THÉRAPEUTIQUES
  申请人：ORGANON NV

  公开号：WO2008100977A2

  公开（公告）日：2008-08-21

  [EN] Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. Esters of alkylcarbamic acids are disclosed that are inhibitors of FAAH activity. Compounds disclosed herein inhibit FAAH activity. Described herein are processes for the preparation of esters of alkylcarbamic acid compounds, compositions that include them, and methods of use thereof.
  [FR] L'inhibition pharmacologique de l'activité de l'amide hydrolase d'acides gras (FAAH) entraîne une augmentation des taux d'amides d'acides gras. L'invention concerne des esters d'acides alkylcarbamiques qui constituent des inhibiteurs de l'activité de la FAAH. Les composés décrits inhibent l'activité de la FAAH. L'invention concerne aussi des procédés de préparation d'esters de composés d'acides alkylcarbamiques, des compositions renfermant ceux-ci et des procédés d'utilisation de celles-ci.
• [EN] NEW C-GLYCOSYLPOLYPHENOL ANTIDIABETIC AGENTS, EFFECT ON GLUCOSE TOLERANCE AND INTERACTION WITH BETA-AMYLOID. THERAPEUTIC APPLICATIONS OF THE SYNTHESIZED AGENT(S) AND OF GENISTA TENERA ETHYL ACETATE EXTRACTS CONTAINING SOME OF THOSE AGENTS<br/>[FR] NOUVEAUX AGENTS ANTIDIABÉTIQUES DE TYPE C-GLYCOSYLPOLYPHÉNOL, EFFET SUR LA TOLÉRANCE AU GLUCOSE ET INTERACTION AVEC LES BÊTA-AMYLOÏDES. APPLICATIONS THÉRAPEUTIQUES DU/DES AGENT(S) SYNTHÉTISÉ(S) ET DES EXTRAITS À BASE D'ACÉTATE D'ÉTHYLE DE GENISTA TENERA CONTENANT CERTAINS DE CES AGENTS
  申请人：UNIV LISBOA

  公开号：WO2013132470A2

  公开（公告）日：2013-09-12

  The present invention concerns the antidiabetic activity of compounds type A, namely of 8-β-D-glucosylgenistein, which is not toxic to eukaryotic cells and has demonstrated to produce complete normalization of fasting hyperglycaemia, to reduce excessive postprandial glucose excursion, to increase glucose-induced insulin secretion and insulin sensitivity. An alternative synthesis for this molecular entity and its binding ability to β-amyloid oligomers is also included in the present invention, which also comprises Genista tenera ethyl acetate extract for use as antihyperglycaemic agent i.e. for lowering blood glucose levels in mammals that are pre- diabetic or have type 2 or type 1 diabetes. The inhibitory activity of α-glucosidase by Genista tenera ethyl acetate and butanol extracts and that of glucose-6- phosphatase by these two extracts and the diethyl ether plant extract is also part of the present invention.