Taxine | 12607-93-1

• 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: Taxine
• 英文别名: [(2S,3E,5S,7S,8S,10R,13S)-2,13-diacetyloxy-7,10-dihydroxy-8,12,15,15-tetramethyl-9-oxo-5-tricyclo[9.3.1.14,8]hexadeca-3,11-dienyl] (2R,3S)-3-(dimethylamino)-2-hydroxy-3-phenylpropanoate
• CAS: 12607-93-1
• 化学式: C₃₅H₄₇NO₁₀
• 分子量: 641.7
• InChiKey: KOTXAHKUCAQPQA-AAUVPWARSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  46
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  160
• 氢给体数：
  3
• 氢受体数：
  11

ADMET

毒理性

• 解毒与急救

在人因故意摄入导致中毒的情况下，治疗方法包括诱导呕吐或洗胃，然后进行一般的排毒措施。各种临床措施，如使用循环刺激剂、人工呼吸和心脏起搏器，都未能防止紫杉中毒导致的死亡。/紫杉中毒/

In cases of human poisoning, resulting from deliberate ingestion, treatment has involved induction of emesis or gastric lavage, followed by general detoxification measures. A variety of clinical measures such as the administration of circulatory stimulants, artificial respiration, and cardiac pacemakers have not been able to prevent death from yew intoxication. /Yew intoxication/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

症状和体征：在人类故意摄入紫杉的情况下，出现的症状和体征与动物报告的类似。人类食用紫杉会导致眩晕、瞳孔扩大、恶心、呕吐、弥漫性腹痛、心动过速（初期）、肌肉无力以及抽搐。这些症状可能导致心动过缓、呼吸缓慢、舒张期心搏停止或死亡。/紫杉中毒/

/SIGNS AND SYMPTOMS/ In cases of deliberate yew poisoning in humans, signs and symptoms are similar to those reported in animals. Human ingestion of yew causes dizziness, pupil dilation, nausea, vomiting, diffuse abdominal pain, tachycardia (initially), muscle weakness, and convulsions. These symptoms can proceed to bradycardia, bradypnea, diastolic cardiac standstill, or death. /Yew poisoning/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

体征和症状：摄入可能导致低血压、心动过缓、心肌收缩力下降和类似于洋地黄中毒的传导延迟。

/SIGNS AND SYMPTOMS/ Ingestion may result in hypotension, bradycardia, depressed myocardial contractility, and conduciton delay similar to digitalis poisoning.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

病例报告：一名成年女性企图自杀，摄入紫杉叶导致罕见且致命的中毒病例被呈现。临床表现为：头晕（摄入后1小时发作），恶心，弥漫性腹痛，意识丧失，呼吸微弱，心动过速，短暂室性扑动后出现缓慢脉搏，最终因呼吸停止和舒张期心脏停搏而死亡。心电图显示非典型束支阻滞，QRS波群最大持续时间为0.24秒。与高钾血症的心电图相似，P波消失。急性高钾血症可能是叶子心脏毒性的部分原因。

/CASE REPORTS/ A CASE OF A RARE LETHAL INTOXICATION WITH YEW LEAVES IN AN ADULT FEMALE ATTEMPTING SUICIDE /IS PRESENTED/. THE CLINICAL SIGNS WERE: DIZZINESS (ONSET 1 HR AFTER INGESTION), NAUSEA, DIFFUSE ABDOMINAL PAIN, UNCONSCIOUSNESS, WEAK BREATHING, TACHYCARDIA, BRIEF VENTRICULAR FLUTTER AFTERWARDS SLOW PULSE, & FINALLY DEATH BY RESPIRATORY ARREST & DIASTOLIC CARDIAC STANDSTILL. THE ECG SHOWED AN ATYPICAL BUNDLE BRANCH BLOCK WITH MAX QRS-DURATION OF 0.24 SEC. STRIKING RESEMBLENCE TO THE ECG IN THE CASE OF HYPERKALEMIA IS SEEN IN THAT P-WAVES WERE ABSENT. AN ACUTE HYPERKALEMIA POSSIBLY COULD BE PARTLY RESPONSIBLE FOR THE CARDIOTOXIC EFFECT OF THE LEAF.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

病例报告：一名年轻大学生因食用红豆杉叶导致致命的紫杉碱中毒的案例报道。讨论了该植物的毒性，并回顾了有限的医学文献。

/CASE REPORTS/ A case of fatal taxine poisoning from the ingestion of yew leaves by a young college man is reported. The toxicity of the plant is discussed, and the limited medical literature is reviewed.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

一种用于检测欧洲红豆杉（紫杉）伪生物碱的半定量LC-MS方法已从人体液体和组织样本中开发出来。这种方法被用来检查一名43岁男子死亡的原因，他在喝下紫杉叶煎剂几小时后死亡。尸检和组织学检查显示早期心肌缺氧的迹象。由于对胃内容物的调查没有提供摄入紫杉的证据，因此通过LC-MS测定了死者的血液、胃内容物和组织样本中的紫杉生物碱。样品通过RP-18柱的固相萃取进行制备。通过HPLC在RP-8柱上进行色谱分离，并与离子阱质谱仪（Finnigan LCQ）耦合。进行了大气压电喷雾离子化。记录了生物碱的光谱，分别在单MS模式和MS-MS模式下，并与从紫杉叶提取物获得的参考光谱进行比较。在死者的胃内容物、肾脏、肝脏和心血样本中，确定了欧洲红豆杉的生物碱，主要是taxine B和iso-taxine B。对心血的半定量评估显示taxine的浓度为11微克taxine/克。

A semi-quantitative LC-MS method was developed for the detection of the pseudo alkaloids of Taxus baccata (yew) from human body fluids and tissue samples. This method was used to examine the cause of death of a 43-year-old man who died several hours after he drank a decoction of taxus leaves. Autopsy and histology demonstrated early signs of myocardial hypoxia. Since investigation of the stomach content did not yield evidence of taxus ingestion, the taxus alkaloids were determined in blood, stomach content and tissue samples of the deceased by LC-MS. The samples were prepared by solid phase extraction on RP-18 columns. Chromatographic separation was achieved by HPLC on a RP-8 column, coupled to an ion trap mass spectrometer (Finnigan LCQ). An atmospheric pressure electrospray ionisation was performed. Spectra of the alkaloids were recorded in the single MS mode and in the MS-MS mode and compared with reference spectra obtained from an extract of yew leaves. In the stomach content, the kidneys, the liver and a heart blood sample of the deceased, alkaloids of Taxus baccata, predominantly taxine B and iso-taxine B, were identified. The semi-quantitative evaluation of the heart blood revealed a taxine concentration of 11 micro g taxine/g.

来源:Hazardous Substances Data Bank (HSDB)

文献信息

• Orthomolecular vitamin E derivatives
  申请人：——

  公开号：US20030007961A1

  公开（公告）日：2003-01-09

  Orthomolecular Vitamin E derivative compounds, compositions, and their uses for effecting aging and longevity, nerve activity, hematopoiesis and maintenance of blood cells, hepatic activity, nephritic activity, heart and cardiovascular function, pulmonary function, muscular function, cartilage, bone, and joint health, gastrointestinal function, reproductive system function, vision, immune function, cell membrane integrity, and pain and inflammation; preventing or treating diseases or conditions; treating cancers or obesity; and reducing the risk of Sudden Infant Death Syndrome in an animal. The compounds of the present invention are of formula I: 1 or a pharmaceutically acceptable salt, ester, or solvate, thereof, wherein: A, B, C, D, and R are as defined herein.

  正分子维生素 E 衍生物化合物、组合物及其在以下方面的用途：衰老和长寿、神经活动、造血和血细胞维护、肝活动、肾活动、心脏和心血管功能、肺功能、肌肉功能、软骨、骨骼和关节健康、肠胃功能、生殖系统功能、视力、免疫功能、细胞膜完整性以及疼痛和炎症；预防或治疗疾病或病症；治疗癌症或肥胖症；降低动物患婴儿猝死综合征的风险。本发明的化合物如式 I 所示： 1 或其药学上可接受的盐、酯或溶液，其中： A、B、C、D 和 R 如本文所定义。
• Orthomolecular sulpho-adenosylmethionine derivatives with antioxidant properties
  申请人：——

  公开号：US20030078231A1

  公开（公告）日：2003-04-24

  Orthomolecular Sulpho-Adenosylmethionine derivative compounds, compositions, and their uses for effecting a biological activity in an animal, such as neurochemical activity; liver biology activity; heart and artery function; cartilage, bone and joint health; stomach and/or intestinal lining resistance to ulceration; immune function; cell membrane integrity; and pain and inflammation. The compounds of the present invention are further useful for preventing or treating diseases or conditions; treating viral infections, infectious diseases, leukemia, and obesity; and reducing the risk of Sudden Infant Death Syndrome in an animal. The compounds of the present invention are of formula I: 1 A is 0 or N; and X is a reaction product as defined herein.

  本发明的正分子磺基腺苷蛋氨酸衍生物化合物、组合物及其用途可影响动物的生物活性，如神经化学活性；肝脏生物活性；心脏和动脉功能；软骨、骨骼和关节健康；胃和/或肠壁抗溃疡能力；免疫功能；细胞膜完整性；以及疼痛和炎症。本发明的化合物还可用于预防或治疗疾病或病症；治疗病毒感染、传染病、白血病和肥胖症；降低动物患婴儿猝死综合症的风险。本发明的化合物如式 I 所示： 1 A 是 0 或 N；以及 X 是本文定义的反应产物。
• DFMO AND TAXOL FOR THE TREATMENT OR PREVENTION OF BREAST CANCER
  申请人：Ilex Oncology, Inc.

  公开号：EP0871441B1

  公开（公告）日：2003-08-13
• EP0882231A4
  申请人：——

  公开号：EP0882231A4

  公开（公告）日：1999-03-03
• RECOVERY OF TAXANES FROM CONIFERS
  申请人：THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

  公开号：EP0882231A1

  公开（公告）日：1998-12-09