腾毒素 | 28540-82-1

• 物质功能分类: 分析化学 - 标准品 - 食品和化妆品标准品
• 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
• 中文名称: 腾毒素
• 英文名称: tentoxin
• 英文别名: (3S,6S,12Z)-12-benzylidene-1,6,7-trimethyl-3-(2-methylpropyl)-1,4,7,10-tetrazacyclododecane-2,5,8,11-tetrone
• CAS: 28540-82-1；64070-01-5；65452-16-6
• 化学式: C₂₂H₃₀N₄O₄
• 分子量: 414.505
• InChiKey: SIIRBDOFKDACOK-LFXZBHHUSA-N

物化性质

• 熔点：
  >174°C (dec.)
• 溶解度：
  氯仿（微溶）、DMSO（微溶）、甲醇（微溶、超声处理）
• 碰撞截面：
  202 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine]

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  30
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  98.8
• 氢给体数：
  2
• 氢受体数：
  4

安全信息

• 危险品标志：
  Xi
• WGK Germany：
  3
• 海关编码：
  29337900

制备方法与用途

生物活性方面，tentoxin 是一种从细交链孢菌中提取的环状四肽。作为一种除草剂，它能够抑制循环光合磷酸化和能量传递，从而导致幼苗枯黄。

反应信息

• 作为反应物：
  描述：

  腾毒素 以 甲醇 为溶剂， 反应 2.5h， 生成 tentoxin
  参考文献：
  名称：

  Isotentoxin, a conversion product of the phytotoxin tentoxin

  摘要：

  Isotentoxin, the E-isomer of the phytotoxin tentoxin, can be produced from tentoxin by UV irradiation. A clean separation of both cyclopeptides is possible using adsorption chromatography on Sephadex G-15. Since artificial daylight causes an inter-conversion of both compounds, special care should be taken in consideration for the interpretation of the chlorosis bioassays. Indeed, isotentoxin seems to have no chlorosis activity, but has stronger wilting effects than tentoxin against the problem weed Galium aparine L.

  DOI：

  10.1016/0031-9422(96)00194-x
• 作为产物：
  描述：

  在 N,N′-二叔丁基碳二亚胺 、 1-羟基苯并三唑 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 1.5h， 生成 腾毒素
  参考文献：
  名称：

  Tentoxin as a Scaffold for Drug Discovery. Total Solid-Phase Synthesis of Tentoxin and a Library of Analogues

  摘要：

  [GRAPHICS]A solid-phase method for the synthesis of tentoxin has been developed. Two key steps-dehydration and Malkylation-are carried out while the peptide is anchored to the resin. The method, which has been validated by the preparation of a library of tentoxin analogues, should be applicable to the generation of further libraries that have the tentoxin scaffold structure, as well as other structures containing N-alkylated didehydroamino acids.

  DOI：

  10.1021/ol0345273

文献信息

• MUCOUS LAYER-ADHESIVE POLY-r-GLUTAMIC ACID NANOMICELLES AND DRUG DELIVERY SYSTEM USING SAME
  申请人：BIOLEADERS CORPORATION

  公开号：US20160193348A1

  公开（公告）日：2016-07-07

  The present invention relates to nanomicelles composed of a complex of a lipophilic compound and a poly-gamma-glutamic acid wherein a portion of carboxyl groups are substituted with an amine group, and more particularly, to nanomicelles composed of a complex of a lipophilic compound and a poly-gamma-glutamic acid wherein a portion of carboxyl groups are substituted with an amine group, a preparation method thereof, and a drug delivery system employing the mucous membrane-adhesive property of the nanomicelles. According to the present invention, the nanomicelle drug delivery system based on poly-gamma-glutamic acid that is a natural biopolymer can be used for the delivery of a drug to mucous membranes to thereby increase the in vivo stability and effectiveness of the drug.

  本发明涉及由脂溶性化合物和聚γ-谷氨酸复合物组成的纳米胶束，其中部分羧基被胺基取代，更具体地，涉及由脂溶性化合物和聚γ-谷氨酸复合物组成的纳米胶束，其中部分羧基被胺基取代，以及其制备方法和利用纳米胶束的粘膜粘附性质的药物传递系统。根据本发明，基于天然生物聚合物聚γ-谷氨酸的纳米胶束药物传递系统可用于将药物传递至粘膜，从而增加药物在体内的稳定性和有效性。
• New synthesis of the cyclic tetrapeptide tentoxin employing an azlactone as key intermediate
  作者：Florine Cavelier、Jean Verducci

  DOI：10.1016/0040-4039(95)00762-2

  日期：1995.6

  An improved preparation of the cyclic tetrapeptide Tentoxin is reported employing an azlactone as key intermediate. This new synthetic route offers the advantage over existing methodologies that the dehydro amino acid would easily be varied, thus allowing the simple preparation of analogues.

  据报道，使用a内酯作为关键中间体，改进了环状四肽肌腱毒素的制备。这种新的合成路线提供了优于现有方法的优点，即脱氢氨基酸很容易被改变，从而允许类似物的简单制备。
• Präparat zur Wirkstoffapplikation in Kleinsttröpfchenform
  申请人：Cevc, Gregor, Prof. Dr.

  公开号：EP0475160A1

  公开（公告）日：1992-03-18

  Die Erfindung betrifft ein Präparat zur Applikation von Wirkstoffen in Form kleinster, insbesondere mit einer membranartigen Hülle aus einer oder wenigen Lagen amphiphiler Moleküle bzw. mit einer amphiphilen Trägersubstanz versehenen Flüssigkeitströpfchen, insbesondere zum Transport des Wirkstoffes in und durch natürliche Barrieren und Konstriktionen wie Häute und dergleichen. Das Präparat weist einen Gehalt einer randaktiven Substanz auf, der bis zu 99 Mol.-% des Gehaltes dieser Substanz entspricht, durch den der Solubilisierungspunkt der Tröpfchen erreicht wird. Das Präparat eignet sich zur nichtinvasiven Verabreichung von Antidiabetica, insbesondere von Insulin. Die Erfindung betrifft außerdem ein Verfahren zur Herstellung solcher Präparate.

  本发明涉及一种以微小液滴形式施用活性物质的制剂，特别是具有一层或几层两亲性分子或两亲性载体物质的膜状包膜，尤其是用于将活性物质输送到或通过皮肤等天然屏障和收缩物。制剂中边缘活性物质的含量最高可达 99 摩尔%，从而达到液滴的溶解点。该制剂适用于非侵入性给药抗糖尿病药物，特别是胰岛素。本发明还涉及生产这种制剂的工艺。
• BIOLOGICAL CONTROL OF WEEDS USING THE METABOLITES OF ALTERNARIA ALTERNATA
  申请人：Nanjing Agricultural University

  公开号：EP1849361A1

  公开（公告）日：2007-10-31

  This invention teaches a method of controlling weeds using the metabolites tenuazonic acid, iso-tenuazonic acid and their salts isolated from the cultures of Alternaria alternata (Fr.) Keissler. Spraying of any of these compounds at a concentration of 5 to 800 µg/g can cause main broad leaf, grassy and sedge weeds to hurt, wilt, and dry to death. Tenuazonic acid, iso-tenuazonic acid, and their salts exhibit herbicidal activity with broad spectrum, quick killing, and high efficiency. The addition of adjuvants improves the herbicidal activity of these compounds.

  本发明传授了一种使用从 Alternaria alternata (Fr.) Keissler 的培养物中分离出的代谢物tenuazonic 酸、异tenuazonic 酸及其盐类来控制杂草的方法。喷洒浓度为 5 至 800 µg/g 的这些化合物，可使主要阔叶杂草、禾本科杂草和莎草受伤、枯萎和干枯死亡。噻努唑啉酸、异噻努唑啉酸及其盐类具有广谱、速效、高效的除草活性。添加佐剂可提高这些化合物的除草活性。
• Method for improving the crop of laticiferous plants
  申请人：Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V.

  公开号：EP2055782A1

  公开（公告）日：2009-05-06

  The present invention broadly relates to the field of agronomy. In particular, the present invention is directed to methods specifically designed to improve the crop of laticiferous plants or parts thereof. According to one basic principle of the invention, it was found that a major component of the latex protein of the laticiferous Taraxacum species is represented by a polyphenoloxidase (PPO) and that latex polymerisation depends predominantly on polyphenoloxidase (PPO) activity. Indeed, a comparison of latex flow and the presence of a PPO revealed that latex exhibiting strong PPO activity polymerises rapidly, whereas reduced PPO activity results in a sequential reduction or delay of latex polymerisation. On the basis of these findings, genetically modified dandelion plants were established that showed down-regulation of the PPO activity via RNA interference resulting in a strong delay in latex polymerisation. Thus and in accordance with the present invention, there is provided a method for improving the crop of latex from laticiferous plants or parts thereof, wherein the improvement consists in using laticiferous plants or parts thereof in which the latex-specific polyphenoloxidase activity, as compared to the respective wild-type or untreated plant or part thereof, is significantly reduced or eliminated. Furthermore, there are provided genetically modified laticiferous plants and parts thereof showing reduced or eliminated latex-specific polyphenoloxidase activity.

  本发明广泛涉及农学领域。特别是，本发明涉及专门用于改良石蒜科植物或其部分作物的方法。 根据本发明的一个基本原理，研究人员发现，多叶植物 Taraxacum 种类的乳胶蛋白的主要成分是多酚氧化酶 (PPO)，而乳胶的聚合主要取决于多酚氧化酶 (PPO) 的活性。事实上，通过比较乳胶的流动性和 PPO 的存在，可以发现 PPO 活性强的乳胶聚合速度快，而 PPO 活性弱的乳胶聚合速度会逐渐减慢或延迟。根据这些研究结果，建立了转基因蒲公英植物，该植物通过 RNA 干扰下调 PPO 活性，导致胶乳聚合的强烈延迟。 因此，根据本发明，提供了一种用于改善有叶植物或其部分的胶乳作物的方法，其中的改进包括使用有叶植物或其部分，与相应的野生型或未经处理的植物或其部分相比，其中的胶乳特异性多酚氧化酶活性显著降低或消失。 此外，还提供了转基因叶菜类植物及其部分，它们显示出乳胶特异性多酚氧化酶活性降低或消失。