ウベニメクス 化学特性,用途語,生産方法
外観
白色~ほとんど白色, 結晶性粉末~粉末
溶解性
水、メタノールにはよく溶けやすく、エタノールにはほとんど溶けない。
用途
病理研究用
効能
抗悪性腫瘍薬, 免疫調節薬
商品名
ベスタチン (日本化薬)
説明
Bestatin is an aminopeptidase inhibitor originally isolated from
S. olivoreticuli. It inhibits aminopeptidase B (IC
50 = 0.05 μg/ml), aminopeptidase N (IC
50 = 16.9 μM), leucine aminopeptidase (IC
50 = 0.01 μg/ml), and the aminopeptidase activity of leukotriene A
4 (LTA
4) hydrolase (K
app = 172 nM). It is selective for these aminopeptidases over aminopeptidase A, trypsin, chymotrypsin, elastase, papain, pepsin, and thermolysin. Bestatin inhibits the production of LTB
4 in erythrocytes when used at a concentration of 70 μM. It increases the expression of Akt, inhibits proliferation, migration, and invasion, and induces autophagy and apoptosis in 5637 bladder cancer cells. Bestatin (5 and 15 mg/kg) decreases serum levels of LTB
4 and reduces tumor growth in a patient-derived xenograft (PDX) mouse model of colorectal cancer.
化学的特性
white powder, soluble in methanol, ethanol, DMSO and other organic solvents, from Streptomyces olivoreticuli.
使用
Ubenimex (also known as bestatin) is a competitive aminopeptidase B inhibitor with an IC50 of 100 mg/ml for K562 cells. Proliferation of all the cell lines except KG1 was inhibited by bestatin. P39/TSU, HL60 and U937 were highly sensitive, with 50% growth inhibitory concentration. It is useful in the treatment of non-lymphocytic leukemia. In other types of cancers ubenimex added to radiotherapy or chemotherapy following surgery significantly inmases survival time through immunopotentiation. It is being studied for use in the treatment of acute myelocytic leukemia.
一般的な説明
Bestatin was found in the culture broth of Streptomyces olivoreticuli in 1976by Umezawa et al. in the course of screening specific enzyme inhibitors of microbial origin. It shows inhibitory activity against specific exopeptidases, e.g., aminopeptidase B and leucine aminopeptidase. However, it does not act against aminopeptidase A, carboxypeptidases A and B, or endopeptidases. Bestatin acts as a bioresponse modifier and shows antitumor activity via stimulation of immuno response in the host. In combination with cytotoxic anticancer drugs, it is now under clinical evaluation for use in cancer therapy.
生物活性
Aminopeptidase inhibitor (K i = 0.001-90 mM); inhibits enkephalin metabolism and leukotriene A 4 hydrolase. Inhibits tumor cell proliferation.
安全性プロファイル
Poison by intraperitoneal route.Moderately toxic by subcutaneous route. Experimentalreproductive effects. When heated to decomposition itemits toxic fumes of NOx.
概要
Streptomyces 属の産生するプロテアーゼ阻害剤.アミノペプチダーゼBおよびロイシンアミノペプチダーゼを阻害
ウベニメクス 上流と下流の製品情報
原材料
準備製品