两性霉素B作用机制 - Medchemexpress - MCE中国

1、Product Data SheetAmphotericin BCat. No.: HY-B0221CAS No.: 1397-89-3分式: CHNO分量: 924.08作靶点: Fungal作通路: Anti-infection储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性数据体外实验 DMSO : 100 mg/mL (108.22 mM)H2O : 0.1 mg/mL (insoluble)* means soluble, but satura

2、tion unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 1.0822 mL 5.4108 mL 10.8216 mL5 mM 0.2164 mL 1.0822 mL 2.1643 mL10 mM 0.1082 mL 0.5411 mL 1.0822 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 储存时，请在 6 个内使，-20C

3、储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 10 mg/mL (10.82 mM); Suspended solution; Ne

4、ed ultrasonic and warming此案可获得 10 mg/mL (10.82 mM) 的均匀悬浊液，悬浊液可于服和腹腔注射。以 1 mL 作液为例，取 100 L 100.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 10 mg/mL (10.82 mM); Suspended solution; Need ultrasoni

5、c and warming此案可获得 10 mg/mL (10.82 mM) 的均匀悬浊液，悬浊液可于服和腹腔注射。Page 1 of 2 www.MedChemE以 1 mL 作液为例，取 100 L 100.0 mg/mL 的澄合均匀。DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混BIOLOGICAL ACTIVITY物活性 Amphotericin B针对多种真 病原体的多烯抗真 (fungal) 剂。 它与麦甾醇不可逆地结合，导致膜完整性破坏并最终导致细胞死亡。IC & Target Fungal1体外研究 Amphotericin B administra

6、tion is limited by infusion-related toxicity, including fever and chills, an effect postulated toresult from proinflammatory cytokine production by innate immune cells. Amphotericin B induces signal transductionand inflammatory cytokine release from cells expressing TLR2 and CD141. Amphotericin B in

7、teracts with cholesterol,the major sterol of mammal membranes, thus limiting the usefulness of Amphotericin B due to its relatively hightoxicity. Amphotericin B is dispersed as a pre-micellar or as a highly aggregated state in the subphase2.Amphotericin B only kills unicellular Leishmania promastigo

8、tes (LPs) when aqueous pores permeable to small cationsand anions are formed. Amphotericin B (0.1 mM) induces a polarization potential, indicating K+ leakage in KCl-loadedliposomes suspended in an iso-osmotic sucrose solution. Amphotericin B (0.05 mM) exhibits a nearly total collapse ofthe negative

9、membrane potential, indicating Na+ entry into the cells3.体内研究 Amphotericin B results in prolonging the incubation time and decreasing PrPSc accumulation in the hamster scrapiemodel. Amphotericin B markedly reduces PrPSc levels in mice with transmissible subacute spongiformencephalopathies (TSSE)4. A

10、mphotericin B exerts a direct effect on Plasmodium falciparum and influences eryptosisof infected erythrocytes, parasitemia and hostsurvival in murine malaria. Amphotericin B tends to delay the increaseof parasitemia and significantly delays host death plasmodium berghei-infected mice5.PROTOCOLKinas

11、e Assay 1 THP-1 and HEK293 cells are transiently transfected using DEAE-dextran and Polyfect reagent, respectively. Plasmidstransfected contain genes coding for the NF-B-dependent pELAM-luc luciferase reporter, TLR2, TLR4, CD14, andMD2. Cells (5105 THP-1 or 1105 HEK293) are added to 12-well plates,

12、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 Promegaluciferase substrate and a Monolight 3010 luminometer.MCE has not independently confirmed the accuracy of these methods. They are for referenc

13、e only.Cell Assay 3 The kinetics of cell death induced by AmB against Leishmania promastigotes is followed by using fluorometry withthe DNA-binding compound ethidium bromide (EB). Fluorescence measurements are performed on a SPEX FluorologII spectrophotometer at 365-580 nm excitation-emission wavele

14、ngths. Promastigotes at a final concentration of25106 cells/mL are incubated for 5 min with gentle stirring in the fluorescence cuvette with 2 mL of differentbuffered solutions but always containing 10 mM glucose and EB (50 mM). After signal stabilization is achieved, AmBis added and dissolved in di

15、methylsulfoxide. Maximal EB incorporation is always obtained by adding digitonin (50mg/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

16、adjustedto 3905 mOsm using an advanced instrument SW2 osmometer.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.MedChemE户使本产品发表的科研献 Neuropharmacology. 2019 Apr 4;151:33-44. Am J Physiol Cell Physiol. 2019 Aug 1;317(2):C277-C286. Molecule

17、s. 2020 Apr 23;25(8). pii: E1980. Evid Based Complement Alternat Med. 2015;2015:639412.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Sau K, et al. The antifungal drug amphotericin B promotes inflammatory cytokine release by a Toll-like receptor- and CD14-dependent

18、mechanism. J BiolChem. 2003 Sep 26;278(39):37561-8. Epub 2003 Jul 14.2. Barwicz J, et al. The effect of aggregation state of amphotericin-B on its interactions with cholesterol- or ergosterol-containing phosphatidylcholinemonolayers. Chem Phys Lipids. 1997 Feb 28;85(2):145-55.3. Ramos H, et al. Amphotericin B kills unicellular leishmanias by forming aqueous pores permeable to small cations and anions. J Membr Biol. 1996Jul;152(1):65-75.4. Demaimay R, et al. Pharmacol