1. Cell Cycle/DNA Damage Apoptosis Epigenetics Anti-infection
  2. Topoisomerase Caspase PARP Fungal
  3. Echinoside A

Echinoside A 是一种皂苷。Echinoside A 可从海参中分离得到。Echinoside A 抑制 Top2α 的催化活性,降低 Top2α 与 DNA 的非共价结合作用。Echinoside A 激活 Caspase-3 并诱导 PARP 裂解。Echinoside A 诱导细胞凋亡 (Apoptosis)。Echinoside A 对前列腺癌、肝细胞癌和 S-180 肉瘤具有抗癌活性。Echinoside A 对多种真菌表现出抗真菌 (antifungal) 活性,其最低生长抑制浓度范围为 3.12-50.0 μg/mL,包括对 AspergillusPenicillium 属真菌的强效活性。

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Echinoside A

Echinoside A Chemical Structure

CAS No. : 75410-53-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Echinoside A is a saponin. Echinoside A can be isolated from sea cucumber. Echinoside A inhibits the catalytic activity of Top2α, reduces the noncovalent binding of Top2α to DNA. Echinoside A activates Caspase-3 and induces PARP cleavage. Echinoside A induces Apoptosis. Echinoside A has anticancer activity against prostate cancer, hepatocellular carcinoma, and S-180 sarcoma. Echinoside A exhibits antifungal activity against a variety of fungi, with a minimum growth inhibitory concentration range of 3.12 to 50.0 μg/mL, including potent activity against Aspergillus and Penicillium species[1][2][3].

IC50 & Target[1]

topoisomerase II alpha

 

Caspase-3

 

体外研究
(In Vitro)

Echinoside A (0.80-3.98 μM; 6-24 h) 可剂量依赖性地强效抑制 HepG2 细胞增殖,在 2.70 μM 作用 12 h 时可使细胞活力降低 54.7%[1]
Echinoside A (1.35-2.70 μM; 12 h) 可在体外以剂量依赖方式诱导 HepG2 细胞发生凋亡[1]
Echinoside A (1.35-2.70 μM; 12 h) 可调控 HepG2 细胞中细胞周期相关基因的表达,上调 p16、p21 的表达,下调 cyclin D1 的表达,但对 p27 无影响[1]
Echinoside A (1.35-2.70 μM; 12 h) 对 HepG2 细胞中 NF-κB p65 蛋白的表达无显著影响[1]
Echinoside A (0.25-2 μM;对于 DNA 片段化,3 h) 可在人白血病细胞 HL-60 中诱导浓度依赖性凋亡、 DNA 片段化[2]
Echinoside A 对多种真菌具有抗真菌活性,其最低生长抑制浓度范围为 3.12 至 50.0 μg/mL,包括对曲霉属和青霉属物种的强效活性[3]

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

Apoptosis Analysis[1]

Cell Line: human hepatocellular liver carcinoma HepG2 cells
Concentration: 1.35, 2.70 μM
Incubation Time: 12 h
Result: Showed slightly increased percentages of early and late apoptotic cells compared to control cells.
Induced visible perinuclear chromatin condensation as bright green patches or fragments in cells treated with 2.70 μM.\nResulted in 18.1% total apoptotic cells (13.2% early apoptotic, 4.9% late apoptotic) at 1.35 μM for 12 h.
Resulted in 62.2% total apoptotic cells at 2.70 μM for 12 h.
Induced apoptosis in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: human hepatocellular liver carcinoma HepG2 cells
Concentration: 1.35, 2.70 μM
Incubation Time: 12 h
Result: Increased the population of HepG2 cells in the G0/G1 phase from 67.9% to 75.2% at 2.70 μM for 12 h.
Increased the sub-G0/G1 cell population (indicative of apoptosis) from 1.83% to 21.21% at 2.70 μM for 12 h.

Western Blot Analysis[1]

Cell Line: human hepatocellular liver carcinoma HepG2 cells
Concentration: 1.35, 2.70 μM
Incubation Time: 12 h
Result: Activated caspase-3 and induced PARP cleavage.\nHad no significant inhibitory effect on NF-κB p65 protein expression.
体内研究
(In Vivo)

Echinoside A (0.5-2.5 mg/kg;腹腔注射;每日一次;10 天) 可在 BALB/c 小鼠中以剂量依赖方式抑制肝细胞癌肿瘤生长[1]
Echinoside A (1.5-3.0 mg/kg;静脉注射;每日一次;7 天) 抑制 KM 小鼠的 S-180 肉瘤生长[2]
Echinoside A (2.6-5.2 mg/kg;静脉注射;每周一次;持续 4 周) 可抑制裸鼠体内 PC-3 前列腺癌异种移植物的生长,对应的 T/C % 值分别为 53.7% 和 45.1%[2]

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

Animal Model: BALB/c (male, 17-22g, subcutaneous implantation of H22 hepatocarcinoma cells)[1]
Dosage: 0.5 mg/kg; 2.5 mg/kg
Administration: i.p.; daily; 10 days
Result: Reduced mean tumour weight to 1.53 ± 0.36 g, corresponding to a 33.8% tumour growth inhibition rate (P < 0.01).
Reduced mean tumour weight to 1.16 ± 0.22 g, corresponding to a 49.8% tumour growth inhibition rate (P < 0.01).
Animal Model: KM mice (female, 7 weeks old, 18-22 g, specific pathogen-free, S-180 sarcoma model via s.c. inoculation)[2]
Dosage: 1.5 mg/kg/day; 3.0 mg/kg/day
Administration: i.v.; daily; 7 days
Result: Achieved a tumor growth inhibition rate of 52.0% at 1.5 mg/kg.
Achieved a tumor growth inhibition rate of 80.0% at 3 mg/kg.
分子量

1207.31

Formula

C54H87NaO26S

CAS 号
结构分类
初始来源

Echinoside A was isolated from sea cucumber

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
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Echinoside A
目录号:
HY-N17442
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