| 名稱 | Bestatin |
| 描述 | Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity. |
| 細胞實驗 | Growing cells (1×106 to 2×106 cells/mL) are diluted to 1.0×103 cells/mL and transferred (3 mL) into a well in a 12-well multiwell plate (2.5-cm diameter/well). Cells are treated with 0, 10, 50, 100, 300, or 600 μM Bestatin and allowed to grow at 21°C shaking at 180 rpm for 48 h. A hemocytometer is used to measure cell density after 0, 24, and 48 h. |
| 激酶實驗 | Cells are harvested, washed, and lysed in NP-40 lysis buffer (50 mM Tris-HCl [pH 7.5], 150 mM NaCl, 0.5% NP-40). Total cell protein is quantified using the Bradford assay and 1-mg/mL protein aliquots are made. Ten microliters of total cell protein is mixed with 290 μL of substrate solution (0.1 mg/mL dithiothreitol [DTT], 0.1 mg/mL albumin, and 1 mM alanine-β-naphthylamide). Fluorometric measurements (340 nm excitation, 400 nm emission) are made after 15 and 30 min. The slope of the line between the 15- and 30-min measurements is used to represent aminopeptidase activity. Total cell protein is preincubated with bestatin, amastatin, puromycin, EDTA, and/or ZnCl2 for 20 min before the fluorometric aminopeptidase assay. |
| 體外活性 | 在B16-BL6黑色素瘤細胞荷瘤的小鼠背部側(cè)中,Bestatin使既定原發(fā)性腫瘤塊血管的數(shù)量下降.在小鼠背部氣囊測定中,Bestatin顯著抑制黑色素瘤細胞誘導的血管生成. 在EGDA大鼠中,Bestatin可降低EAC的發(fā)病率（57.7％降至26.1％）.在EGDA大鼠的食管組織中,Bestatin對白三烯B4生物合成的抑制具有明顯的統(tǒng)計學意義. |
| 體內(nèi)活性 | Bestatin對SN12M細胞侵入重組基底膜（基質(zhì)膠）具有濃度依賴性的抑制作用。在非腫瘤條件培養(yǎng)基中,其還可濃度依賴性抑制腫瘤細胞IV型膠原退化。在U937細胞中,烏苯美司可使caspase-3的活性增強并誘導DNA梯和DNA片段化。在SN12M Bestatin抑制氨基肽酶底物的水解活性。Bestatin對人臍靜脈內(nèi)皮細胞中的管狀形成具有抑制作用。通過固定在細胞表面的亮氨酸氨肽酶,Bestatin直接刺激淋巴細胞（和單核細胞）,而間接刺激則是通過氨基肽酶乙抑制吞噬作用激素的分解代謝發(fā)揮。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | 1eq. NaOH : 15.4 mg/mL (50 mM)
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| 關(guān)鍵字 | Aminopeptidase | Bacterial | Inhibitor | Antibiotic | Bestatin | inhibit |
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