2. Anti-infection Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. Antibiotic Bacterial Apoptosis Reactive Oxygen Species (ROS) Bcl-2 Family NO Synthase COX TNF Receptor Interleukin Related
  4. Asperlin

Asperlin 是一种有口服活性的海洋衍生物抗生素，具有抗真菌、抗癌、抗炎和抗动脉粥样硬化活性。Asperlin 可诱导细胞凋亡 (apoptosis)。Asperlin 可增加活性氧 (ROS) 和 DNA 损伤相关的 G2/M 期停滞和 ATM 磷酸化。Asperlin 在体内可有效预防 HFD 诱发的肥胖并调节肠道菌群。

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Asperlin Chemical Structure

Asperlin Chemical Structure

CAS No. : 30387-51-0

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Asperlin 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Asperlin is an orally active marine-derived antibiotic with antifungal, anticancer, anti-inflammatory and anti-atherosclerotic activities. Asperlin induces apoptosis. Asperlin increases reactive oxygen species (ROS)- and DNA damage-associated G2/M phase arrest and ATM phosphorylation. Asperlin is effective in preventing HFD-induced obesity and modulating gut microbiota[1][2][3][4][5].

体外研究
(In Vitro)

Asperlin (6-25 μM，24-48 小时) 以剂量依赖性方式抑制细胞生长，诱导 caspase-3 和 PARP 裂解，降低 Bcl-2，并诱导细胞凋亡。NAC 可以阻断 Asperlin 在 HeLa 细胞中的所有凋亡作用[1]。
Aaperlin (6-25 μM，24 小时) 增加 ROS 和 DNA 损伤相关的 G2/M 期停滞和 ATM 磷酸化，并且可以通过 NAC 或 ATM 抑制剂 KU-55933 预处理显著阻断[1]。
Aaperlin (5-40 μM, 12 小时) 在巨噬细胞中具有抗炎作用，抑制 LPS 诱导的 iNOS 和 COX-2 表达，以剂量依赖性方式降低小鼠腹膜巨噬细胞和 RAW264.7 巨噬细胞中的 TNF-α 和 IL-1β 产生[3]。
Asperlin (500 μg/ml，1 天) 可有效控制番茄晚疫病和小麦叶锈病的发展，病害防治值为95%[4]。

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

Asperlin 相关抗体:

Cell Viability Assay[1]

Cell Line: HeLa
Concentration: 6, 12.5, 25 μM
Incubation Time: 24, 48 h
Result: Increased ROS generation while little increase could be seen in the presence of NAC.
Cell growth was inhibited in dose dependent manner, but was restored in the presence of NAC.

Cell Cycle Analysis[1]

Cell Line: HeLa
Concentration: 6, 12, 25 μM
Incubation Time: 24 h
Result: Significantly increased G2/M phase cells.
Pretreatment with either NAC or KU-55933 significantly abrogated the G2/M arresting effect.
Phosphorylation of Chk2, cdc2 and cyclinB1 was found to be reduced by pretreatment of NAC and KU-99533

Apoptosis Analysis[1]

Cell Line: HeLa
Concentration: 25 μM
Incubation Time: 24, 48 h
Result: Induced caspase-3 activation and PARP cleavage as well as Bcl2 reduction, and the effect were completely blocked by NAC pretreatment to the cells.

Western Blot Analysis[1]

Cell Line: HeLa
Concentration: 6, 12, 25 μM
Incubation Time: 24 h
Result: Expression of cyclin A2 and cyclin B1 was increased.
Phosphorylation of Bcl-2 and of cdc2 which is inactive when phosphorylated at residues Thr-14 and Tyr-15, was increased. and cdc25C expression was reduced.
Induced the phosphorylation of both ATM and Chk2 in the cells without having any effect on p21.
体内研究
(In Vivo)

Asperlin (40-80 mg/kg；口服；每天一次，持续 12 周) 可有效预防高脂饮食 (HFD) 小鼠的肥胖发展，刺激能量消耗并调节肠道微生物群[2]。
Asperlin (80 mg/kg；口服；每天一次，持续 12 周) 在高脂饮食 (HFD) 喂养的 ApoE-/- 小鼠中显著抑制主动脉粥样硬化斑块的形成，表现为主动脉扩张减少，动脉粥样硬化病变面积减少[5]。

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

Animal Model: C57BL/6J mice (8-weeks old, weighing 20-25g) were fed with a high-fat diet (HFD) to induce obesity[2]
Dosage: 40, 80 mg/kg
Administration: Oral gavage (p.o.), once daily for 12 weeks
Result: Showed lower body weight, and food intake was not varied.
Reduced the blood levels of total cholesterol (TC), triglycerides (TG) and low-density lipoprotein (LDL-c). Liver TC, TG contents and fat vacuoles were also substantially reversed.
Increased energy expenditure and enhanced thermogenic gene (PGC1α, UCP1, CIDEA, CPT1B, FATP1, CYTO-C) expression in adipose tissue.
Increased the diversity of the gut microbes. Significantly shifted the structure of the gut microbiota.
Animal Model: Male C57BL/6 J and C57BL/6 J ApoE-/- mice (6-8 weeks, weighting 20-25 g)[5]
Dosage: 80 mg/kg
Administration: Oral gavage (p.o.), once daily for 12 weeks
Result: Remarkably suppressed atherosclerotic plaque formation in aorta, reduced the white atherosclerotic lesions, effectively inhibited aortic dilatation in ApoE-/- mice.
分子量

212.20

Formula

C10H12O5
CAS 号
结构分类
初始来源

Aspergillus caespitosus
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Asperlin 相关分类

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Keywords:

Asperlin30387-51-0AntibioticBacterialApoptosisReactive Oxygen Species (ROS)Bcl-2 FamilyNO SynthaseCOXTNF ReceptorInterleukin RelatedNitric oxide synthasesNOSCyclooxygenaseTumor Necrosis Factor ReceptorTNFRILgut microbiotaobesityG2/MATMDNA-damageantibioticROSanti-inflammatoryantifungalanti-atherosclerotic activitiesanticancerInhibitorinhibitorinhibit

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