2. Neuronal Signaling Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis Anti-infection
  3. Cholinesterase (ChE) Lipase Reactive Oxygen Species (ROS) Apoptosis Bacterial
  4. Aspulvinone H

Aspulvinone H 是一种具有口服活性的 AChE、胰脂肪酶 (Lipase)、谷草转氨酶 1、α-葡萄糖苷酶抑制剂，其 IC50 值分别为 25.95 μM、47.06 μM、5.91/6.91 μM 和 4.6 μM，针对 GOT1 的 Ka 为 2.14 μM，针对 α-葡萄糖苷酶的 Ki 为 6.58 μM。Aspulvinone H 可抑制癌细胞增殖，干扰谷氨酰胺代谢，升高 ROS 水平，诱导细胞凋亡 (apoptosis) 及 S 期阻滞。Aspulvinone H 对金黄色葡萄球菌具有抗菌活性。Aspulvinone H 抑制胰腺导管腺癌异种移植瘤的生长。Aspulvinone H 降低小鼠餐后血糖。Aspulvinone H 可用于胰腺导管腺癌、糖尿病和金黄色葡萄球菌感染的相关研究。

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Aspulvinone H

Aspulvinone H Chemical Structure

CAS No. : 57744-69-1

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Aspulvinone H 相关抗体

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  • 生物活性

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  • 参考文献

生物活性

Aspulvinone H is an orally active inhibitor of AChE, pancreatic lipase, glutamic-oxaloacetic transaminase 1, and α-glucosidase, with IC50 values of 25.95 μM, 47.06 μM, 5.91/6.91 μM, and 4.6 μM, respectively. It has a Ka of 2.14 μM against GOT1 and a Ki of 6.58 μM against α-glucosidase. Aspulvinone H inhibits cancer cell proliferation, interferes with glutamine metabolism, elevates ROS levels, and induces cell apoptosis and S-phase arrest. Aspulvinone H exhibits antibacterial activity against Staphylococcus aureus. Aspulvinone H inhibits the growth of pancreatic ductal adenocarcinoma xenografts. Aspulvinone H reduces postprandial blood glucose in mice. Aspulvinone H can be used in research related to pancreatic ductal adenocarcinoma, diabetes, and Staphylococcus aureus infection[1][2][3][4].

体外研究
(In Vitro)

Aspulvinone H (Compound 4) 可在体外中度抑制乙酰胆碱酯酶、胰脂肪酶，IC50 分别为 25.95、47.06 μM[1]。
Aspulvinone H (Compound 6) 可抑制重组人 GOT1 酶活性，其 IC50 分别为 5.91 μM 和 6.91 μM，还能直接与 GOT1 结合，Kd 为 2.14 μM[2]。
Aspulvinone H (0.1-100 μM; 48 h) 可选择性抑制 SW1990、PANC-1 和 AsPC-1 胰腺导管腺癌细胞的增殖 (IC50 6.32-10.47 μM)，而对非恶性 HPDE6C7 细胞的毒性极低 (处理 48 h 后 IC50 >100 μM)[2]。
Aspulvinone H (10-40 μM) 可干扰谷氨酰胺代谢，降低 SW1990 胰腺导管腺癌细胞内的 NADPH/NADP+比值，并升高其 ROS 水平[2]。
Aspulvinone H (10-40 μM; 48 h) 可在 SW1990 胰腺导管腺癌细胞中诱导剂量依赖性凋亡及 S 期细胞周期阻滞，抑制细胞的增殖，并以剂量和时间依赖性方式抑制其迁移[2]。
Aspulvinone H (Compound 4) (0.1 μM-10 mM; 10 min enzyme incubation, 15 min substrate incubation) 可通过混合型抑制机制强效抑制酿酒酵母来源的 α-葡萄糖苷酶，其 IC50 为 4.6 μM，且对游离酶的亲和力高于酶-底物复合物[3]。
Aspulvinone H (40 μg/disc; 24 h) 对金黄色葡萄球菌具有抗菌活性，在 38 °C 条件下孵育 24 h 后可产生 11 mm 的抑菌圈[4]。

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

Aspulvinone H 相关抗体:

Cell Viability Assay[2]

Cell Line: Pancreatic ductal adenocarcinoma cell lines SW1990, PANC-1, AsPC-1; nonmalignant human pancreatic duct epithelial cell line HPDE6C7
Concentration: 0.1-100 μM
Incubation Time: 48 h
Result: Inhibited growth of PDAC cell lines with IC50 values of 6.32 μM (SW1990), 10.47 μM (PANC-1), and a value between these for AsPC-1.
Exhibited minimal cytotoxicity to nonmalignant HPDE6C7 cells, with an IC50 value over 100 μM.

Apoptosis Analysis[2]

Cell Line: SW1990 PDAC cells
Concentration: 10-40 μM
Incubation Time: 48 h
Result: Induced apoptosis in a dose-dependent manner, with apoptosis rates of 9.5% (10 μM), 28.3% (20 μM), and 80.2% (40 μM).
Induced S-phase cell cycle arrest, increasing S-phase cell proportion to 32.5% (10 μM), 38.6% (20 μM), and 43.9% (40 μM), while decreasing G0/G1 phase proportion to 59.4% (10 μM), 48.6% (20 μM), and 43.5% (40 μM).
体内研究
(In Vivo)

Aspulvinone H (2.5-5 mg/kg；腹腔注射；每日一次；连续 14 天) 可显著抑制胰腺导管腺癌异种移植瘤的生长，调控肿瘤谷氨酰胺代谢，且无显著的体内毒性[2]。
Aspulvinone H (25 mg/kg；灌胃；单次给药) 可使口服蔗糖、麦芽糖耐量试验的雌性 C57BL/6J 小鼠餐后血糖的 AUC0-t 降低 ，并抑制其血糖升高[3]。

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

Animal Model: CB-17/SCID (male, 8 weeks old, subcutaneous injection of 3×106 SW1990 cells)[2]
Dosage: 2.5 mg/kg; 5 mg/kg
Administration: i.p.; daily; 14 days
Result: Reduced tumor volumes significantly compared to control.
Decreased oxaloacetate (OAA) and malate levels in tumor tissue.
Increased aspartate (Asp) and glutamine (Gln) levels in tumor tissue.
Decreased NADPH/NADP+ ratio in tumor tissue.
Caused no significant changes in mouse body weight or histomorphology.
Animal Model: C57BL/6J (female, 6 weeks old, 16-20 g)[3]
Dosage: 25 mg/kg
Administration: i.g.; single dose
Result: Significantly suppressed the rise in blood glucose levels at 30 and 60 minutes after sucrose loading compared to the negative control group.
Reduced the area under the blood glucose concentration-time curve (AUC) over 0-120 minutes by 13.2%.\nSignificantly reduced the postprandial blood glucose peak compared to the negative control group.
Reduced the AUC of postprandial blood glucose over 0-120 minutes by 19.7%.
分子量

432.51

Formula

C27H28O5
CAS 号
结构分类
初始来源

Aspergillus terreus ASM-1
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

Aspulvinone H 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Aspulvinone H57744-69-1Cholinesterase (ChE)LipaseReactive Oxygen Species (ROS)ApoptosisBacterialPancreatic Lipase/Acetylcholinesterase/Glutamic-oxaloacetic Transaminase 1/Alpha-glucosidase InhibitorapoptosisCB-17/SCID miceC57BL/6J miceInhibitorinhibitorinhibit

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