Amphotericin B|1397-89-3|癌症|Medlife|陌孚医药

中文名称 ：Amphotericin B.

中文别名：两性霉素B;二性霉素B;两性霉素;两性霉素乙;可溶性两性霉素 B;两性霉属B;庐山霉素;多烯抗生素;两性多烯;可溶性两性霉素;两性酶素b;两性霉素B EP标准品;两性霉素B USP标准品;两性霉素B 标准品;两性霉素B,BR;两性霉素B-13C6;两性霉素B峰鉴别 EP标准品;两性霉素B口服粉;两性霉素B微生物鉴定 EP标准品;两性霉素B（冷藏运输）;芦山霉素;两性霉素 B 来源于链霉菌 属;两性霉素 B;异性霉素

英文名称：Amphotericin B

英文别名：Amphotericin B;33-[(3-amino-3,6-dideoxy-beta-d-mannopyranosyl)oxy]-1,3,5,6,9,11,17,37-octahydroxy-15,16,18-trimethyl-13-oxo-14,39-dioxabicyclo[33.3.1]nonatriaconta-19,21,23,25,27,29,31-heptaene-36-carboxylic acid;ABELCET;AMBISOME;AMPHOTERCIN B;AMPHOTERICIN B SOLUBILIZED;AMPHOTERICIN B, SOLUBLE;AMPHOTERICIN B, STREPTOMYCES NODOSUS;AMPHOTERICIN B, STREPTOMYCES SPECIES;AMPHOZONE;FUNGIZONE;FUNGIZONE(R);Amphotericin B trihydrate;Abelecet;Amphocin;AMPHOTERICIN B, NON STERILE;fungilin;Halizon;LNS-AmB;ns718;Fungizone;33-[(3-Amino-3,6-dideoxy-beta-D-mannopyranosyl)oxy]-1,3,5,6,9,11,17,37-octahydroxy-15,16,18-trimethyl-13-oxo-14,39-Dioxabicyclo[33.3.1]nonatriaconta-19,21,23,25,27,29,31-heptaene-36-carboxylic acid;F;amphotericineb;amphotericinbstandardsolution;ampho-moronal;amphomoronal;33-((3-amino-3,6-dideoxy-beta-d-mannopyranosyl)oxy)-1,3,5,6,9,11,-xylicaci;14,39-dioxabicyclo(33.3.1)nonatriaconta-19,21,23,25,27,29,31-heptaene-36-carbo

Cas No.：1397-89-3

分子式：C47H73NO17

分子量：924.08

包装储存：4°C, protect from light

       *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

生物活性 ：Amphotericin B is a polyene antifungal agent against a wide variety of fungal pathogens. It binds irreversibly to ergosterol, resulting in disruption of membrane integrity and ultimately cell death.

性状：Solid

IC50 & Target[1][2]：Fungal

体外研究(In Vitro)：

Amphotericin B administration is limited by infusion-related toxicity, including fever and chills, an effect postulated to result from proinflammatory cytokine production by innate immune cells. Amphotericin B induces signal transduction and inflammatory cytokine release from cells expressing TLR2 and CD14. Amphotericin B interacts with cholesterol, the major sterol of mammal membranes, thus limiting the usefulness of Amphotericin B due to its relatively high toxicity. Amphotericin B is dispersed as a pre-micellar or as a highly aggregated state in the subphase. Amphotericin B only kills unicellular Leishmania promastigotes (LPs) when aqueous pores permeable to small cations and anions are formed. Amphotericin B (0.1 mM) induces a polarization potential, indicating K leakage in KCl-loaded liposomes suspended in an iso-osmotic sucrose solution. Amphotericin B (0.05 mM) exhibits a nearly total collapse of the negative membrane potential, indicating Na entry into the cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)：

Amphotericin B results in prolonging the incubation time and decreasing PrPSc accumulation in the hamster scrapie model. Amphotericin B markedly reduces PrPSc levels in mice with transmissible subacute spongiform encephalopathies (TSSE). Amphotericin B exerts a direct effect on Plasmodium falciparum and influences eryptosis of infected erythrocytes, parasitemia and hostsurvival in murine malaria. Amphotericin B tends to delay the increase of parasitemia and significantly delays host death plasmodium berghei-infected mice.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件：Room temperature or refrigerated transportation.

结构分类：Ketones, Aldehydes, Acids

来源：Streptomyces?nodosus

参考文献

[1]. Sau K, et al. The antifungal drug amphotericin B promotes inflammatory cytokine release by a Toll-like receptor- and CD14-dependent mechanism. J Biol Chem. 2003 Sep 26;278(39):37561-8. Epub 2003 Jul 14.  [Information]

[2]. Barwicz J, et al. The effect of aggregation state of amphotericin-B on its interactions with cholesterol- or ergosterol-containing phosphatidylcholine monolayers. Chem Phys Lipids. 1997 Feb 28;85(2):145-55.  [Information]

[3]. Ramos H, et al. Amphotericin B kills unicellular leishmanias by forming aqueous pores permeable to small cations and anions. J Membr Biol. 1996 Jul;152(1):65-75.  [Information]

[4]. Demaimay R, et al. Pharmacological studies of a new derivative of amphotericin B, MS-8209, in mouse and hamster scrapie. J Gen Virol. 1994 Sep;75 (Pt 9):2499-503.  [Information]

[5]. Adams ML, et al. Amphotericin B encapsulated in micelles based on poly(ethylene oxide)-block-poly(L-amino acid) derivatives exerts reduced 体外研究 hemolysis but maintains potent in vivo antifungal activity. Biomacromolecules. 2003 May-Jun;4(3):750-7.  [Information]

两亲多烯抗生素，Amphotericin B是针对多种真菌病原体的多烯抗真菌 (fungal) 剂。 它与麦角甾醇不可逆地结合，导致膜完整性破坏并最终导致细胞死亡。

一、抗真菌机制与疗效研究

两性霉素B作为一种多烯类大环内酯抗生素，其主要通过与真菌细胞膜上的固醇类（如麦角甾醇）结合，形成孔道，导致细胞内容物外漏，从而发挥抗真菌作用。研究方向包括深入探究其作用机制，以及评估其对各种真菌（如隐球菌、球孢子菌、念珠菌、毛霉菌、曲菌等）引起的全身感染的疗效。目标在于进一步明确两性霉素B的抗菌谱，优化其治疗方案，提高疗效。

二、降低毒性与副作用研究

两性霉素B虽然疗效显著，但由于其也能与人体细胞膜上的固醇结合，因此存在严重的副作用，包括寒战、高热、肾功能损害、低钾血症、血液系统毒性反应等。研究方向包括通过化学修饰、结构改造等方法降低其毒性，以及开发新型给药系统（如脂质体、纳米粒等）以减少副作用。目标在于提高两性霉素B的安全性和耐受性，使其更适用于临床应用。

三、新型抗真菌药物研发

基于两性霉素B的结构和作用机制，科学家们致力于研发新型多烯抗真菌药物。这些新型药物在保留两性霉素B抗菌活性的同时，显著降低其毒性。研究方向包括合成具有更高抗真菌活性、更低毒性的衍生物，以及探索其作用机制和疗效。目标在于为抗真菌治疗领域带来新的突破和发展，提高患者的生存率和生活质量。

四、质量控制与杂质研究

两性霉素B的质量控制对于确保其疗效和安全性至关重要。研究方向包括建立灵敏、准确的质量控制方法，如改良夹角余弦法结合近红外光谱法（NIR）进行多元组分药物的分析。同时，对两性霉素B中的杂质进行富集、分离和结构鉴定，评估杂质对疗效和毒性的影响。目标在于提高两性霉素B的质量稳定性和一致性，降低杂质带来的风险。

五、耐药性研究

随着抗真菌药物的广泛使用，真菌耐药性问题日益严重。研究方向包括探究两性霉素B的耐药机制，以及评估新型抗真菌药物对耐药菌株的敏感性。目标在于为制定有效的抗真菌治疗策略提供科学依据，延长药物的使用寿命。

综上所述，两性霉素B在科研领域的研究方向及目标涵盖了抗真菌机制与疗效、降低毒性与副作用、新型抗真菌药物研发、质量控制与杂质研究以及耐药性研究等多个方面。这些研究旨在提高两性霉素B的疗效和安全性，为抗真菌治疗领域带来新的突破和发展。