ビンブラスチン硫酸塩 化学特性,用途語,生産方法
外観
白色～わずかにうすい黄色、結晶～粉末
溶解性
水にやや溶けやすく、メタノールにやや溶けにくく、エタノール(99.5)にほとんど溶けない。
用途
紡錘体の形成及び微小管の脱
重合を阻害することにより細胞分裂阻害作用
を示します。
効能
抗悪性腫瘍薬, 微小管重合阻害薬
商品名
エクザール (日本化薬)
説明
Vinblastine sulfate is the salt of an alkaloid extracted from Vinca rosea Linn., a common flowering herb known as the periwinkle (more properly known as Catharanthus roseus G. Don). Previously, the generic name was vincaleukoblastine, abbreviated VLB. It is a stathmokinetic oncolytic agent. When treated in vitro with this preparation, growing cells are arrested in metaphase. Chemical and physical evidence indicate that vinblastine sulfate is a dimeric alkaloid containing both indole and dihydroindole moieties.
化学的特性
Vinblastine sulfate is a white to off-white crystalline powder that is freely soluble in water, soluble in methane, and slightly soluble in ethanol. Its empiric formula is C46H58N4O9.H2SO4 , and it has a molecular weight of 909.07.
使用
Anticancer agent; microtubule disrupter; Induces apoptosis.Vinblastine sulfate is therapeutically used as an antineoplastic. It is also used in the treatment of Hodgkin disease, choriocarcinoma, acute and chronic leukemias.
一般的な説明
Vinblastine Sulfate is the sulfate salt of vinblastine, a natural alkaloid isolated from the plant Catharanthus roseus (Madagascar periwinkle) with antineoplastic properties. Vinblastine disrupts microtubule formation and function during mitosis and interferes with glutamic acid metabolism. (NCI04)
空気と水の反応
Water soluble..Rapidly hydrolyzes.
反応プロフィール
Vinblastine sulfate is sensitive to light, hydrolysis, oxidation, and heat. Vinblastine sulfate is very hygroscopic. .
健康ハザード
SYMPTOMS: Symptoms of exposure to Vinblastine sulfate include temporary mental depression, paresthesias, loss of deep-tendon reflexes, headache, convulsions, psychoses; dysfunction of the autonomic nervous system, with marked constipation, paralytic ileus, urinary retention, bilateral pain and tenderness of the parotid glands associated with dryness of the mouth, sinus tachycardia; nausea, vomiting, anorexia, diarrhea; loss of hair, vesicular mucositis of the mouth, and dermatitis.
生物活性
Anticancer agent; microtubule disrupter. Induces apoptosis in cultured hepatocytes and human lymphoma cells.
安全性プロファイル
Poison by ingestion,
intraperitoneal, and intravenous routes. An
experimental teratogen. Human systemic
effects by intravenous route: blood
leukopenia and hair changes. Experimental
reproductive effects. Questionable
carcinogen. Human mutation data reported. When heated to decomposition it emits very
toxic fumes of NOx and SOx. See also
VINCALEUKOBLASTINE and
SULFATES.
純化方法
Crystallise the sulfate from MeOH or EtOH and dry it in vacuo over conc H2SO4. The free base crystallises from EtOH or MeOH m 211-216o (+ 2MeOH .1 H2O) and forms a stable etherate from Et2O with m 201-211o, and [] D +42o (CHCl3), and UV max at 214 and 259nm (log 4.73 and 4.21). The dihydrochloride has m 244-246o(dec)(MeOH). It is a monoamine oxidase B inhibitor and induces microtubule aggregation. It is an antineoplastic drug for Hodgkin’s lymphoma. [Neuss et al. J Am Chem Soc 81 4754 1959, Jong-KeunSon et al. J Med Chem 33 1845 1990, Warfield & Bouck Science 186 1219 1974, Beilstein 26 III/IV 3167.]
ビンブラスチン硫酸塩 上流と下流の製品情報
原材料
準備製品