• 盤點青蒿素背后的植物類神藥

    發布時間: 2015-10-08 02:10:47 來源: 本站 點擊次數

    文北卡醫藥 2015.10.07(部分資料來自網絡)


    一個遲到的諾貝爾醫學獎引爆了國慶節,屠呦呦教授成為了中國科學界的領袖,來自于植物的青蒿素再一次家喻戶曉。那么,除了青蒿素,還有哪些劃時代的來源于植物特別是中草藥的神奇藥物呢?今天就重點介紹從植物中得到的四種可持續開發的藥物(及其衍生物)——喜樹堿,紫杉醇,天麻素和黃連素。


    1. 喜樹堿,衍生消化系統癌癥的克星
    喜樹的喜樹果是一味經典的抗癌中藥材,其主要成分和功效如下:
    【中藥名】喜樹果xishuguo【別名】喜果、千丈樹、水栗子、天梓樹、水桐樹。【英文名】FructusCamptothecae【來源】珙桐科植物旱蓮木CamptothecaacuminataDecne.的果實。【主要成分】含喜樹堿、羥基喜樹堿、去氧喜樹堿、喜樹次堿,尚含樺皮酸及喜果苷。從喜樹果中還分離得11-羥基喜樹堿、10-甲氧基喜樹堿、脫落酸、丁香脂素和β-谷甾醇。喜樹的根、莖干、皮、葉和果實一樣均含喜樹堿,均有抗癌作用。(此為近代研究發現,不屬于醫書記載,后同)【功效與作用】抗癌,散結,破血化瘀。屬活血化瘀藥下分類的破血消癥藥。千丈樹(喜樹)
    喜樹堿(Camptothecin,CPT),是1966年由M.E.Wall和M.C. Wani通過有系統的篩選天然物質,進而發現的抗癌藥物。它是一種細胞毒性喹啉類生物堿,能抑制DNA拓撲異構酶(TOPO I)。
    喜樹堿是從產于中國的喜樹(喜樹,幸福樹)漿果和枝葉,樹皮等中分離出來的,早期喜樹果用于傳統中醫療法治療癌癥。喜樹堿在初步臨床試驗中發現有顯著的抗癌特性、但同時也有溶解度低以及含有高度的藥物不良反應的特性。藥物化學家進而利用這些特性開發出了多樣的合成喜樹堿和各種衍生品,以增加良好的效果并減少不良反應。現今喜樹堿衍生物已經是消化系統癌癥的重要一二線藥物。已經上市藥物中,除了喜樹堿之外,還有10-羥基喜樹堿(主要用于胃癌的治療),鹽酸拓撲替康和鹽酸伊立替康。本文中我們將著重介紹鹽酸伊立替康。


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