秋水仙素
维基百科，自由的百科全书
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Image:Colchicine.png |
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| N-((7S)-5,6,7,9-tetrahydro- 1,2,3,10-tetramethoxy-9- oxobenzo(a)heptalen-7-yl)- acetamide |
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| CAS number 64-86-8 |
ATC code M04AC01 |
| 化学式 | C22H25NO6 |
| 相对分子质量 | 399.44 |
| Bioavailability | ? |
| Metabolism | ? |
| Elimination half-life | ? |
| Excretion | ? |
| Pregnancy category | ? |
| Legal status | ? |
| Routes of administration | Oral tablets |
秋水仙素 是一种剧毒的生物碱, 最初萃取于秋水仙 。最先用于治癒风湿病和痛風，但其具瀉藥及促進嘔吐的功能也成為醫師開處方的原因之一。現今主要用於治療痛風上。
目录 |
[编辑] 历史
秋水仙的的萃取物可用於痛風治療上的記載最先出現於Padanius Dioscorides於第一世紀的CE時所著的De Materia Medica。
秋水仙素最先由两位法国化学家PS·波列特与J·卡文顿於1820年提取出来(Pelletier PS, Caventon J. Ann. Chim. Phys. 1820;14:69).
此物質之後經研究，為三環類的生物鹼，而它在痛風治療上的止痛及消炎效果則與其跟微管蛋白結合的能力有關。
[编辑] 药理学
[编辑] 生物功能
Colchicine inhibits microtubule polymerization by binding to tubulin, one of the main constituents of microtubules. Apart from inhibiting mitosis, a process heavily dependent on cytoskeletal changes, it also inhibits neutrophil motility and activity, leading to a net anti-inflammatory effect.
[编辑] Colchicine as medicine
Colchicine is FDA-approved for the treatment of gout and also for familial Mediterranean fever, secondary amyloidosis(AA), and scleroderma. Side-effects include gastro-intestinal upset and neutropenia. Starting the drug early during an attack of gout can exacerbate the symptoms. High doses can also damage bone marrow and lead to anemia. It is not used in the treatment of cancer, as the dose required would lead to intolerable side-effects.
[编辑] 毒性
中毒症状与砷中毒类似：中毒后2至5小时出现症状，包括口渴和喉咙有烧灼感，发热，呕吐，腹泻，腹疼和肾衰竭。随后伴有呼吸衰竭并引起死亡。现阶段还没有能够应用于临床的解毒剂。
[编辑] 植物学应用
Since chromosome segregation is driven by microtubules, colchicine is also used for inducing polyploidy in plant cells during cellular division by inhibiting chromosome segregation during meiosis; half the resulting gametes therefore contain no chromosomes, while the other half contain double the usual number of chromosomes (i.e., diploid instead of haploid as gametes usually are), and lead to embryos with double the usual number of chromosomes (i.e. tetraploid instead of diploid). While this would be fatal in animal cells, in plant cells it is not only usually well tolerated, but in fact frequently results in plants which are larger, hardier, faster growing, and in general more desirable than the normally diploid parents; for this reason, this type of genetic manipulation is frequent in breeding plants commercially. In addition, when such a tetraploid plant is crossed with a diploid plant, the triploid offspring will be sterile (which may be commercially useful in itself by requiring growers to buy seed from the supplier) but can often be induced to create a "seedless" fruit if pollinated (usually the triploid will also not produce pollen, therefore a diploid parent is needed to provide the pollen). This is the method used to create seedless watermelons, for instance.
[编辑] 外部链接
- Feature on colchicine
- Pharmacology of colchicine
