Винбластин сульфат химические свойства, назначение, производство
Описание
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.
Химические свойства
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.
Использование
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.
Общее описание
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)
Реакции воздуха и воды
Water soluble..Rapidly hydrolyzes.
Профиль реактивности
Vinblastine sulfate is sensitive to light, hydrolysis, oxidation, and heat. Vinblastine sulfate is very hygroscopic. .
Угроза здоровью
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.
Биологическая активность
Anticancer agent; microtubule disrupter. Induces apoptosis in cultured hepatocytes and human lymphoma cells.
Профиль безопасности
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.
Методы очистки
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.]
Винбластин сульфат препаратная продукция и сырье
сырьё
препарат