wilfordine | 37239-51-3

• 物质功能分类: 生物化工 - 提取物
• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 英文名称: wilfordine
• 英文别名: ent-(1¹¹S,7Ξ)-1¹β,1⁶α,1⁸β,1⁹β,1¹⁴-pentaacetoxy-1²β-benzoyloxy-1^5,11-epoxy-1⁴,7-dihydroxy-7-methyl-(1³βH,1⁷βH)-2,9-dioxa-1(12,3)-eudesmana-4(3,2)-pyridina-cyclononaphane-3,8-dione；8α-acetoxy-O²-benzoyl-26-hydroxy-O²-deacetyl-8-deoxo-evonimine；Wilfordin；[(1S,3R,18S,19R,20R,21R,22S,23R,24R,25R,26S)-20,22,23,25-tetraacetyloxy-21-(acetyloxymethyl)-15,26-dihydroxy-3,15,26-trimethyl-6,16-dioxo-2,5,17-trioxa-11-azapentacyclo[16.7.1.01,21.03,24.07,12]hexacosa-7(12),8,10-trien-19-yl] benzoate
• CAS: 37239-51-3
• 化学式: C₄₃H₄₉NO₁₉
• 分子量: 883.857
• InChiKey: XQDBHSNYTFRCNJ-OURLNJDISA-N

物化性质

• 熔点：
  175-6°C
• 沸点：
  895.5±65.0 °C(Predicted)
• 密度：
  1.44±0.1 g/cm3(Predicted)
• 溶解度：
  溶于氯仿、二氯甲烷、乙酸乙酯、DMSO、丙酮等。

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  63
• 可旋转键数：
  14
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  273
• 氢给体数：
  2
• 氢受体数：
  20

制备方法与用途

概述

雷公藤中主要的有效活性成分包括雷公藤生物碱、二萜以及三萜类化合物。其中，最早从雷公藤根里分离出来的几种代表性生物碱是雷公藤吉碱（wilforgine）、雷公藤次碱（wilforine）、雷公藤定碱（wilfordine）和雷公藤春碱（wilfortrine）。

用途

雷公藤是一种传统的中国中药，其中的活性成分——雷公藤定碱具有治疗免疫疾病、抗炎以及抗生育等多种功效。

反应信息

• 作为产物：
  描述：

  乙酸酐 、 alatamine 生成 wilfordine
  参考文献：
  名称：

  大叶黄杨（Euonymus alatus forma striatus（thunb。）makino）的一种新生物碱阿拉特明和一种杀虫性生物碱小花ford碱的分离和结构。

  摘要：

  一种新的生物碱alatamine 5和杀虫生物碱雷公藤6用evonine一起分离2，新evonine 3，和euonymine 4从卫矛备考叶蝉（藤）牧野（家庭卫矛科）。通过化学和光谱方法完全建立了阿拉米特5和维甲酸6的结构。进行了阿拉坦胺5向野生素6的转化。

  DOI：

  10.1016/0040-4020(78)80097-0

文献信息

• Tripterygium wilfordii Hook F root preparation for birth control
  申请人：THE BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM

  公开号：EP1645281A1

  公开（公告）日：2006-04-12

  The present invention provides for the use of Tripterygium Wilfordii Hook F extracts and purified components thereof in the treatment of inflammation or an immune disorder with concomitant lack of steroidal effect. Extracts of this plant (T2) bound to the glucocorticoid receptor and competitively inhibited glucocorticoid mediated cellular processes, such as dexamethasone binding to the glucocorticoid receptor, glucocorticoid mediated activation of target genes, dexamethasone dependent cellular growth, with concomitant inhibition of cyclooxygenase-2 induction and inflammatory processes such as the production of prostaglandin E2. The T2 extract components triptolide and tripdiolide were effective inhibitors. The particular advantage provided by the methods herein is the treatment or prevention of inflammation and the concomitant lack of steroidal agonist effects and NSAID side effects. Conditions treatable by the present methods include inflammation and immune disorders including autoimmune disease.

  本发明提供了Tripterygium Wilfordii Hook F提取物及其纯化成分在治疗炎症或免疫紊乱中的应用，同时缺乏类固醇作用。这种植物的提取物（T2）与糖皮质激素受体结合，竞争性抑制糖皮质激素介导的细胞过程，如地塞米松与糖皮质激素受体结合、糖皮质激素介导的靶基因激活、地塞米松依赖的细胞生长，同时抑制环氧化酶-2的诱导和炎症过程，如前列腺素E2的产生。T2 提取物成分曲普内酯（triptolide）和曲普地内酯（tripdiolide）是有效的抑制剂。本方法的特别优势在于治疗或预防炎症，同时没有类固醇激动剂的作用和非甾体抗炎药的副作用。本方法可治疗的疾病包括炎症和免疫紊乱，包括自身免疫性疾病。
• 8-ARM POLYETHYLENE GLYCOL DERIVATIVE, MANUFACTURING METHOD AND MODIFIED BIO-RELATED SUBSTANCE THEREBY
  申请人：Xiamen Sinopeg Biotech Co., Ltd.

  公开号：EP3315531A1

  公开（公告）日：2018-05-02

  Disclosed are an 8-arm polyethylene glycol (PEG) derivative (formula 1), manufacturing method and modified bio-related substance thereby, wherein a tetravalent group U and four trivalent groups Ec form a highly symmetric octavalent central structure CORE0 together, Lc connects the octavalent center to eight PEG arms having polydiversity or monodiversity and having n1-n8 as the degrees of polymerization thereof. The terminal of one PEG chain is connected to at least one functional group F (k ≥ 1), and said PEG chain and F can be directly connected (g = 0) or connected with a divalent linking group L0 connected with a terminal branched group G (g = 1) therebetween. The latter provides more reacting sites to combine more pharmaceutical molecules, thereby increasing the drug loading capacity. The near-center symmetric structure of the derivative allows more precise control over the molecular weight during large-scale production, thereby facilitating acquisition of a product having a narrower molecular weight distribution. A bio-related substance modified thereby has a more uniform and controllable performance.

  本发明公开了一种 8 臂聚乙二醇（PEG）衍生物（式 1）、其制造方法和改性生物相关物质，其中一个四价基团 U 和四个三价基团 Ec 共同形成一个高度对称的八价中心结构 CORE0，Lc 将八价中心连接到八个 PEG 臂上，这些 PEG 臂具有多元性或单元性，其聚合度为 n1-n8。一条 PEG 链的末端与至少一个官能团 F（k ≥ 1）相连，所述 PEG 链和 F 可以直接相连（g = 0），也可以通过二价连接基 L0 与中间的末端支化基 G（g = 1）相连。后者提供了更多的反应位点，可以结合更多的药物分子，从而提高药物负载能力。衍生物的近中心对称结构可以在大规模生产过程中更精确地控制分子量，从而有利于获得分子量分布更窄的产品。由此改性的生物相关物质具有更均匀、更可控的性能。
• Eight-arm polyethylene glycol derivative, production method therefor, and modified bio-related substance thereof
  申请人：XIAMEN SINOPEG BIOTECH CO., LTD.

  公开号：US10434182B2

  公开（公告）日：2019-10-08

  Disclosed are an eight-arm polyethylene glycol (PEG) derivative (formula I), production method therefor and modified bio-related substance thereby. Wherein, one tetravalent group U together with four trivalent groups Ec form a highly symmetrical octavalent group CORE0; Lc connects the octavalent group to eight PEG chains having polydispersity or monodispersity and having n1 to n8 as the degree of polymerization thereof; the terminal of one PEG chain is connected to at least one functional group F (k≥1); said PEG chain and F therebetween can be directly connected (g=0) or be indirectly connected via a linking group L0 to a terminal end-branching group G (g=1); the latter provides more reactive sites for binding more drug molecules and increases the drug loading. The eight-arm polyethylene glycol derivative has a centrosymmetric or approximately centrosymmetric structure, and leads to more precise control of the molecular weight in large-scale production and much narrower distribution of molecular weight for products. The modified bio-related substance thereby has a more uniform and controllable performance.

  本发明公开了一种八臂聚乙二醇（PEG）衍生物（式 I）、其生产方法及其改性生物相关物质。其中，一个四价基团 U 与四个三价基团 Ec 形成一个高度对称的八价基团 CORE0；Lc 将八价基团连接到八条具有多分散性或单分散性且聚合度为 n1 至 n8 的 PEG 链上；一条 PEG 链的末端与至少一个官能团 F 连接（k≥1）；所述 PEG 链和 F 之间可以直接连接（g=0），也可以通过连接基团 L0 与末端支化基团 G 间接连接（g=1）；后者提供了更多的反应位点，可以结合更多的药物分子，增加药物负载量。八臂聚乙二醇衍生物具有中心对称或近似中心对称结构，因此在大规模生产中可以更精确地控制分子量，产品的分子量分布也更窄。因此，改性生物相关物质的性能更均匀、更可控。
• Therapeutic composition of herbal extracts and the uses thereof
  申请人：Advanced Herbal Therapeutics, Inc.

  公开号：US20030008024A1

  公开（公告）日：2003-01-09

  A novel therapeutic composition comprises three novel herbal extracts: Herba epimedium Extract, Rhizoma Drynaria fortunei (kze.) J. Sm Extract and Radix Tripterygium hypoglaucum (L'evl.) Hutch Extract, which are prepared through standardized manufacturing processes, respectively. A new formulation AHT-323 contains these three herbal extracts. The novel therapeutic composition described in the present application can be used for treating autoimmune diseases such as rheumatoid arthritis, inflammatory disorders and pain.

  一种新型治疗组合物由三种新型草药提取物组成： 附子草提取物 提取物 旱金莲 (kze.) J. Sm 提取物和 Radix Tripterygium hypoglaucum (L'evl.) Hutch 提取物，它们分别通过标准化生产工艺制备而成。新制剂 AHT-323 包含这三种草药提取物。本申请所述的新型治疗组合物可用于治疗自身免疫性疾病，如类风湿性关节炎、炎症性疾病和疼痛。
• Foam with germproof and mildew-proof effects
  申请人：Kuo Peng-Yi

  公开号：US20060147506A1

  公开（公告）日：2006-07-06

  The present invention relates to foam with the germproof and mildew-proof effects. To produce such foam, Chinese herbaceous extracts are prepared by extracting from angelica - laxiflora, ranunculacese - clematis chinensis, tripterygium wilfordli hook, Atractylodes lancea (Thunb)DC, talc powder, alunite, Cnidium monnieri (L.)Cuss and hydnocarpus anthelmintica P. These extracts are then blended with plastic or rubber material and brought to a foaming treatment. Accordingly, plastic or rubber products with germproof and mildew-proof effects are manufactured, and the effects can be lasted.

  本发明涉及具有防菌防霉效果的泡沫。为了生产这种泡沫，中草药提取物的制备方法是从 当归 - 当归 - 白术（Thunb）DC、滑石粉、白云石、芒硝、芒硝粉、芒硝粉、芒硝粉、芒硝粉、芒硝粉、芒硝粉。 (Thunb)DC、滑石粉、矾土、 蛇床子 (L.)Cuss和 hydnocarpus anthelmintica P.然后将这些提取物与塑料或橡胶材料混合并进行发泡处理。这样，就能制造出具有防菌防霉效果的塑料或橡胶制品，而且效果可以持续。