问题：求紫杉醇物化性质，稳定性数据。
类型：求助 (悬赏分:3分)
提问：zhangpacer
等级：▲
版块：药物化学(jaywoo,合成小象,)
信誉：100%
回复：4
阅读：2459
时间：2005-07-07 22:56:28 编辑加入/取消收藏订制/取消短消息举报该贴

谢谢

回复人：dingding,▲▲▲▲ (书到用时方恨少) 时间：2005-07-08 01:21:33 编辑

1楼

概况：
　　紫杉醇是从红豆杉树中提取的一种天然抗癌原料药，为白色结晶粉末、不溶于水，易溶于氯仿、丙酮等有机溶剂。紫杉醇是一种高效、低毒、广谱、作用机制独特的抗癌天然药物，能够治疗卵巢癌、乳腺癌，对铂类等已有抗药性的顽固性卵巢癌亦有效，也可用于治疗肺癌、头颈部癌、食管癌、生殖细胞肿瘤、子宫内膜癌、淋巴瘤、膀胱癌等。现已经证实在诸多有抗癌活性的紫杉烷类化合物中，紫杉醇的抗癌活性最强。美国FDA于1992年批准紫杉醇注射液上市，用于治疗卵巢癌，乳腺癌及非小细胞肺癌。紫杉醇对类风湿和老年综合症都有较好的疗效。
技术特点：
　　国内多采用硅胶正相层析法，国外多采用大孔吸附树脂或反相层析法，前者因负载纯化量小，纯化步骤多而使生产效率难以提高，后者介质价格昂贵，且耗费大量溶剂。本技术利用特殊的色层分离介质，提高了回收率，并使得部分非紫杉醇结构的物质转化为紫杉醇。在分离的同时将部分非目标物质转化为目标产物。提高了生产效率和经济效益。
市场分析：
　　紫杉醇被国际上公认为首选的抗癌药物，美国年需求量300公斤以上，国际市场售价为每克2000美元。市场上供不应求。美国在我国临床试用产品时，每克费用可达9万元。在2000年世界上最畅销的抗癌药物和生物药物中，紫杉醇被列为第一，其年销售额将超过10亿美元。

Paclitaxel is a white to off-white crystalline powder with the empirical formula C47H51NO14 and a molecular weight of 853.9. It is highly lipophilic, insoluble in water, and melts at around 216-217°C.

http://www.rxlist.com/cgi/generic/paclitaxel.htm

珍惜红豆杉资源，发了财可要记得回报论坛呀。

回复人：chhchem,▲ () 时间：2005-07-08 14:37:48 编辑

2楼

Monograph Number: 7052
Title: Paclitaxel
CAS Registry Number: 33069-62-4
CAS Name: [2aR-[2aa,4b,4ab,6b,9a(aR*,bS*),11a,12a,12aa,12ba]]-b-(Benzoylamino)-a-hydroxybenzenepropanoic acid 6,12b-bis(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b]oxet-9-yl ester
Additional Names: 5b,20-epoxy-1,2a,4,7b,10b,13a-hexahydroxytax-11-en-9-one 4,10-diacetate 2-benzoate 13-ester with (2R,3S)-N-benzoyl-3-phenylisoserine; taxol A
Manufacturers' Codes: NSC-125973
Trademarks: Anzatax (Faulding); Paxene (Baker Norton); Taxol (Bristol-Myers Squibb)
Molecular Formula: C47H51NO14
Molecular Weight: 853.90.
Percent Composition: C 66.11%, H 6.02%, N 1.64%, O 26.23%
Literature References: Antileukemic and antitumor agent first isolated, as the l-form, from the bark of the Pacific yew tree, Taxus brevifolia, Taxaceae; promotes the assembly of microtubules and inhibits the tubulin disassembly process. Isoln and structure: M. C. Wani et al., J. Am. Chem. Soc. 93, 2325 (1971). In vitro promotion of microtubule assembly: P. B. Schiff et al., Nature 277, 665 (1979). Isoln from Taxus baccala L. and in vitro inhibition of depolymerization of microtubules into tubulin: G. Chauviere et al., C.R. Acad. Sci. Paris Ser. II 293, 501 (1981). Total synthesis of taxusin, which contains the entire ring skeleton: R. A. Holton et al., J. Am. Chem. Soc. 110, 6558 (1988). Total stereosynthesis: R. A. Holton et al., ibid. 116, 1597, 1599 (1994); K. C. Nicolaou et al., Nature 367, 630 (1994). Synthesis and anticancer activity of derivs: D. G. I. Kingston et al., Studies in Organic Chemistry vol. 26, entitled "New Trends in Natural Products Chemistry 1986", Atta-ur-Rahman, P. W. Le Quesne, Eds. (Elsevier, Amsterdam, 1986) pp 219-235. Production by Taxomyces andreanae, an endophytic fungus associated with T. brevifolia: A. Stierle et al., Science 260, 214 (1993). Use in study of structure and function of microtubules: S. B. Horwitz et al., Cold Spring Harbor Symp. Quant. Biol. 46, 219 (1982). Clinical evaluation in Kaposi's sarcoma: M. W. Saville et al., Lancet 346, 26 (1995). Review of mechanism of action: J. J. Manfredi, S. B. Horwitz, Pharmacol. Ther. 25, 83-125 (1984); S. B. Horwitz et al., Ann. N.Y. Acad. Sci. 466, 733-744 (1986); S. B. Horwitz, Trends Pharmacol. Sci. 13, 134-136 (1992). Symposium on clinical toxicology, pharmacology and efficacy: Sem. Oncol. 20, Suppl. 3, 1-60 (1993). Review in ovarian cancer: C. D. Runowicz et al., Cancer 71, 1591-1596 (1993). Book: Taxol? Science and Applications, M. Suffness, Ed. (CRC Press, Boca Raton, 1995) 426 pp.
Properties: Needles from aq methanol, mp 213-216?(dec). [a]D20 -49?(methanol). uv max (methanol): 227, 273 nm (e 29800, 1700).
Melting point: mp 213-216?(dec)
Optical Rotation: [a]D20 -49?(methanol)
Absorption maximum: uv max (methanol): 227, 273 nm (e 29800, 1700)
Use: Tool in study of structure and function of microtubules.
Therap-Cat: Antineoplastic.

回复人：soslito,▲ () 时间：2005-07-08 16:26:21 编辑	3楼
接受答案了。

回复人：zhangpacer,▲ (创业中，欢迎化学化工生物医药等领域的大侠交流和合作。) 时间：2005-07-09 17:27:08 编辑	4楼
我是在配制紫杉醇溶液时，发现在二氯甲烷溶液中，紫杉醇的高效液相分析结果与计算结果相差比较大，好象大部分紫杉醇有了降解的现象，我不知道是紫杉醇在二氯甲烷溶液不稳定，还是我的分析方法有问题？

得分人：dingding-2,chhchem-2,

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