GlpBio

Aureobasidin A

目录号: GC62854纯度: >99.00%同义词: 巴西芬净,Basifungin,金担子素

Aureobasidin A是一种具有口服活性的环状肽抗生素。Aureobasidin A是肌醇磷酸化神经酰胺合成酶 AUR1的抑制剂。

Aureobasidin A
Cas No.: 127785-64-2
规格价格库存数量操作
1 mg¥1,350.00现货
1
5 mg¥3,510.00现货
1
10 mg¥5,220.00现货
1
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产品描述 Description

Aureobasidin A is an orally active cyclic peptide antibiotic[1]. Aureobasidin A is an inhibitor of inositol phosphorylating ceramide synthase AUR1[2]. Aureobasidin A has antifungal and antiparasitic activities[3, 4].

In vitro, Aureobasidin A (20ng/mL) treatment of Candida albicans SC5314 for 24h completely inhibited the growth of the strain[5]. Aureobasidin A (5, 10μg/mL) treated with Toxoplasma gondii tachyzoites for 24h significantly inhibited the proliferation of Toxoplasma gondii tachyzoites[6].

In vivo, Aureobasidin A (20, 40mg/kg) was used orally and subcutaneously to treat mice with systemic Candida infection, producing good therapeutic effects, which were superior to fluconazole and amphotericin B[7].

References:
[1] Teymuri M, Shams-Ghahfarokhi M, Razzaghi-Abyaneh M. Inhibitory effects and mechanism of antifungal action of the natural cyclic depsipeptide, aureobasidin A against Cryptococcus neoformans[J]. Bioorganic & Medicinal Chemistry Letters, 2021, 41: 128013.
[2] Katsuki Y, Yamaguchi Y, Tani M. Overexpression of PDR16 confers resistance to complex sphingolipid biosynthesis inhibitor aureobasidin A in yeast Saccharomyces cerevisiae[J]. FEMS microbiology letters, 2018, 365(3): fnx255.
[3] Alimehr S, Shams-Ghahfarokhi M, Razzaghi Abyaneh M. Antifungal activity of Aureobasidin a in combination with Fluconazole against fluconazole-resistant Candida albicans[J]. Infection Epidemiology and Microbiology, 2020, 6(4): 285-291.
[4] Tanaka A K, Valero V B, Takahashi H K, et al. Inhibition of Leishmania (Leishmania) amazonensis growth and infectivity by aureobasidin A[J]. Journal of Antimicrobial Chemotherapy, 2007, 59(3): 487-492.
[5] Zheng L, Xu Y, Dong Y, et al. Chromosome 1 trisomy confers resistance to aureobasidin A in Candida albicans[J]. Frontiers in Microbiology, 2023, 14: 1128160.
[6] Alqaisi A Q I, Mbekeani A J, Llorens M B, et al. The antifungal Aureobasidin A and an analogue are active against the protozoan parasite Toxoplasma gondii but do not inhibit sphingolipid biosynthesis[J]. Parasitology, 2018, 145(2): 148-155.
[7] TAKESAKO K, KURODA H, INOUE T, et al. Biological properties of aureobasidin A, a cyclic depsipeptide antifungal antibiotic[J]. The Journal of antibiotics, 1993, 46(9): 1414-1420.

Aureobasidin A是一种具有口服活性的环状肽抗生素[1]。Aureobasidin A是肌醇磷酸化神经酰胺合成酶 AUR1的抑制剂[2]。Aureobasidin A有抗真菌和抗寄生虫活性[3, 4]。

在体外，Aureobasidin A（20ng/mL）处理白色念珠菌SC5314 24h，完全抑制了菌株的生长[5]。Aureobasidin A（5, 10μg/mL）处理弓形虫速殖子24h，显著抑制了弓形虫速殖子的增殖[6]。

在体内，Aureobasidin A（20, 40mg/kg）通过口服和皮下治疗全身念珠菌感染的小鼠，产生了良好的治疗效果，作用优于氟康唑和两性霉素B[7]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

C. albicans lab strain SC5314

Preparation Method

C. albicans lab strain SC5314 was grown in YPD broth or on YPD plates supplemented with 0-20ng/mL Aureobasidin A. Optical density at 595nm was measured every 15min for 24h at 37°C using a Tecan plate reader. 3μL of 10-fold serial dilutions were spotted on YPD plates. The plates were incubated at 37°C for 48h then photographed.

Reaction Conditions

0-20ng/mL; 24h、48h

Applications

In the liquid medium, growth in the presence of 5ng/mL or 10ng/mL of Aureobasidin A did not significantly inhibit growth. 20ng/mL of Aureobasidin A completely inhibited growth. On the plates, growth was also inhibited by 20ng/ml of Aureobasidin A.
Animal experiment [2]:

Animal models

ICR mice

Preparation Method

Groups of mice were treated with Aureobasidin A, Fluconazole or Amphotericin B. Aureobasidin A or Fuconazole was administered orally once daily from day-0 to -6 at the dose of 20mg/kg and from day-3 to -9 at the dose of 40mg/kg. Amphotericin B was given subcutaneously once daily from day-3 to -9 at the dose of 5mg/kg. On day-0 and -4, -7, -10, -14, and -21 after infection, some mice in each group were sacrificed and their kidneys were removed aseptically. The removed kidneys were sectioned through the middle and the exposed surface was stamped on SD agar plates for inoculation. All of the plates were incubated at 30°C for 2 days and the number of visibly growing colonies of C. albicans were Whenfive counted.

Dosage form

20、40mg/kg; p.o.

Applications

Aureobasidin A shows low toxicity and good efficacy against murine candidiasis. Aureobasidin A also prolongs survival days of infected mice by oral treatment, even when the treatment was started after completion of infection.

References:
[1]Zheng L, Xu Y, Dong Y, et al. Chromosome 1 trisomy confers resistance to aureobasidin A in Candida albicans[J]. Frontiers in Microbiology, 2023, 14: 1128160.
[2]TAKESAKO K, KURODA H, INOUE T, et al. Biological properties of aureobasidin A, a cyclic depsipeptide antifungal antibiotic[J]. The Journal of antibiotics, 1993, 46(9): 1414-1420.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
127785-64-2
同义词
巴西芬净,Basifungin,金担子素
分子式
C60H92N8O11
分子量
1101.42 g/mol
溶解性
DMSO : 100 mg/mL (90.79 mM; Need ultrasonic)
保存条件
Store at -20°C, protect from light
General tips
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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol