两性霉素B T1067

Product Introduction
Bioactivity


英文名: Amphotericin B

描述: Amphotericin B (NSC-527017) 是一种多烯类抗真菌剂，对许多真菌物种具有广谱活性。Amphotericin B 不可逆地结合麦角甾醇，破坏细胞膜完整性，从而起到抗真菌活性。

细胞实验: Amphotericin B is dissolved in DMSO. The kinetics of cell death induced by AmB against Leishmania promastigotes is followed by using fluorometry with the DNA-binding compound ethidium bromide (EB). Fluorescence measurements are performed on a SPEX Fluorolog II spectrophotometer at 365-580 nm excitation-emission wavelengths. Promastigotes at a final concentration of 25×106 cells/mL are incubated for 5 min with gentle stirring in the fluorescence cuvette with 2 mL of different buffered solutions but always containing 10 mM glucose and EB (50 mM). After signal stabilization is achieved, AmB is added and dissolved in dimethylsulfoxide. Maximal EB incorporation is always obtained by adding digitonin (50 mg/mL). All solutions used are buffered with 75 mM TRIS (pH 4 7.6) and contain 150 mM NaCl (BNa+), 150 mM KCl (BK+), 150 mM choline chloride, and 100 mM sucrose, 100 mM NaCl. The osmolarity of all solutions is always adjusted to 390±5 mOsm using an advanced instrument SW2 osmometer.

激酶实验: THP-1 and HEK293 cells are transiently transfected using DEAE-dextran and Polyfect reagent, respectively. Plasmids transfected contain genes coding for the NF-κB-dependent pELAM-luc luciferase reporter, TLR2, TLR4, CD14, and MD2. Cells (5×105 THP-1 or 1×105 HEK293) are added to 12-well plates, washed after 18 h, and stimulated for 5 h. Cells are then lysed with reporter lysis buffer as directed, and lysates are analyzed for luminescence using Promega luciferase substrate and a Monolight 3010 luminometer.

体外活性: 方法：人正常结肠上皮细胞 CCD 841 CoTr 和人结直肠癌细胞 HT-29 用含 Amphotericin B (0.05-25 µg/mL) 处理 24 h，使用 Neutral Red method 检测细胞活力。结果：较高浓度的 Amphotericin B 对 CCD 841 CoTr 和 HT-29 细胞有毒，IC50 值分别为 8.7 µg/mL 和 21.2 µg/mL。[1]方法：Candida albicans 用 Amphotericin B (100 µM) 处理 4-16 min，使用 FLIM technique 进行成像。结果：Amphotericin B 优先与细胞壁结合，而不会有效地穿过覆盖细胞膜的屏障。Amphotericin B 在出芽阶段可以更容易地通过年轻细胞的细胞壁屏障。[2]

体内活性: 方法：为检测体内抗真菌活性，将 Amphotericin B (0.25-4 mg/kg) 单次腹腔注射给 C. albicans K-1 感染的 ICR/Swiss 小鼠。结果：与治疗开始时的菌落数相比，只有最高单次剂量的 Amphotericin B 治疗才能显著减少菌落数。[3]

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: 5% DMSO+95% Saline : 1.05 mg/mL (1.14 mM, suspension)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (54.11 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: Fungal | NSC527017 | NSC-527017 | Inhibitor | Antibiotic | Amphotericin B | inhibit

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途