Aureobasidin A
(Synonyms: 巴西芬净,Basifungin) 目录号 : GC62854
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。
Cas No.:127785-64-2
Sample solution is provided at 25 µL, 10mM.
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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]。
| 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: | |
| Cas No. | 127785-64-2 | SDF | |
| 别名 | 巴西芬净,Basifungin | ||
| 分子式 | C60H92N8O11 | 分子量 | 1101.42 |
| 溶解度 | DMSO : 100 mg/mL (90.79 mM; Need ultrasonic) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.9079 mL | 4.5396 mL | 9.0792 mL |
| 5 mM | 0.1816 mL | 0.9079 mL | 1.8158 mL |
| 10 mM | 0.0908 mL | 0.454 mL | 0.9079 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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