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肺癌的治疗

ID #1007

紫杉醇是什么?

  【产品名称】 紫杉醇
  【英文名称】 Paclitaxel
  【产品别名】 泰素,紫素,特素
  【化学名称】 5β,20-环氧-1,2α,4,7β,10β,13α-六羟基紫杉烷-11-烯-9-酮-4,10-二乙酸酯-2-苯甲酸酯-13[(2’R,3’S)-N-苯甲酰-3-苯基异丝氨酸酯]
  【分 子 式】 C47H51NO14
  【分 子 量】 853.92
  【CA S NO】 33069-62-4
  【产品来源】 为红豆杉科植物红豆杉的干燥根、枝叶以及树皮。
  红豆杉【规格含量】 99.5%(和霖生物)
  【物理性质】 白色结晶体粉末。无臭,无味。不溶于水,易溶于氯仿、丙酮等有机溶剂。
  【药理作用】 紫杉醇是红豆杉属植物中的一种复杂的次生代谢产物, 也是目前所了解的惟一一种可以促进微管聚合和稳定已聚合微管的药物。同位素示踪表明, 紫杉醇只结合到聚合的微管上, 不与未聚合的微管蛋白二聚体反应。细胞接触紫杉醇后会在细胞内积累大量的微管,这些微管的积累干扰了细胞的各种功能,特别是使细胞分裂停止于有丝分裂期,阻断了细胞的正常分裂。 通过Ⅱ-Ⅲ临床研究,紫杉醇主要适用于卵巢癌和乳腺癌,对肺癌、大肠癌、黑色素瘤、头颈部癌、淋巴瘤、脑瘤也都有一定疗效。
  紫杉醇是红豆杉属植物中的一种复杂的次生代谢产物, 也是目前所了解的惟一一种可以促进微管聚合和稳定已聚合微管的药物。同位素示踪表明, 紫杉醇只结合到聚合的微管上, 不与未聚合的微管蛋白二聚体反应。细胞接触紫杉醇后会在细胞内积累大量的微管,这些微管的积累干扰了细胞的各种功能,特别是使细胞分裂停止于有丝分裂期,阻断了细胞的正常分裂。
  【发现历史】
  1963年美国化学家瓦尼(M.C. Wani)和沃尔(Monre E. Wall)首次从一种生长在美国西部大森林中称谓太平洋杉(Pacific Yew)树皮和木材中分离到了紫杉醇的粗提物。在筛选实验中,Wani和 Wall发现紫杉醇粗提物对离体培养的鼠肿瘤细胞有很高活性,并开始分离这种活性成份。由于该活性成份在植物中含量极低,直到1971年,他们才同杜克(Duke)大学的化学教授姆克法尔(Andre T. McPhail)合作,通过x-射线分析确定了该活性成份的化学结构——一种四环二萜化合物,并把它命名为紫杉醇(taxol)。

==== 翻译 ====

【Product Name】 paclitaxel
Alias】 【product Taxol, purple elements, special elements
【Chemical name】 5β, 20 - epoxy -1,2 α, 4,7 β, 10β, 13α-6-hydroxy taxane -11 - ene--9 - one -4,10 - diacetate -2 - benzyl Ester -13 [(2'R, 3'S)-N-benzoyl -3 - phenylisoserine ester]
【Molecular Formula】 C47H51NO14
【Molecular Weight】 853.92
【CA S NO】 33069-62-4
Origin of the products】 【yew Taxus plants of the dry roots, leaves and bark.
Content of Taxus 【Specification】 99.5% (and Lin biological)
【】 White crystals physical properties of powder. Odorless, tasteless. Insoluble in water, soluble in chloroform, acetone and other organic solvents.
】 【Pharmacological effects of Taxol in Taxus species is a complex secondary metabolites, is currently the only kind of understanding can promote microtubule polymerization and stability of microtubules have been aggregated drug. Isotope tracer showed that only the combination of paclitaxel to the polymerization of microtubules, do not and are not aggregated tubulin dimer reaction. Cells in the cell after contact with Taxol accumulated a large number of microtubules, which interfere with microtubule accumulation of cells in various functions, in particular to enable cell division to stop at the mitotic phase, blocked the normal cell division. Through Ⅱ - Ⅲ clinical studies, paclitaxel is mainly suitable for ovarian cancer and breast cancer, lung cancer, colorectal cancer, melanoma, head and neck cancer, lymphoma, brain tumors also have some effects.
Taxol is a Taxus species in a complex secondary metabolites, is currently the only kind of understanding can promote microtubule polymerization and stability of microtubules have been aggregated drug. Isotope tracer showed that only the combination of paclitaxel to the polymerization of microtubules, do not and are not aggregated tubulin dimer reaction. Cells in the cell after contact with Taxol accumulated a large number of microtubules, which interfere with microtubule accumulation of cells in various functions, in particular to enable cell division to stop at the mitotic phase, blocked the normal cell division.
History】 【found
Vanni 1963, the U.S. chemist (MC Wani) and Wall (Monre E. Wall) for the first time from one grows in the forests of the western United States the title Pacific Grand Fir (Pacific Yew) isolated bark and wood to crude Taxol material. In screening experiments, Wani and Wall found that crude extracts of taxol in vitro culture of mouse tumor cells have high activity, and begin to separate the active ingredients. Because the active ingredients in plants were very low until 1971 that they did with the Duke (Duke) professor of chemistry at the University of Lemke Jaafar (Andre T. McPhail), and through x-ray analysis identified the active ingredient in chemical structure - a tetracyclic diterpenoid compounds, and it named paclitaxel (taxol).

Tags: 紫杉醇

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更新日期: 2009-10-26 08:31
作者: : mcyclub
修订: 1.1

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