1. Metabolic Enzyme/Protease Apoptosis Autophagy NF-κB Immunology/Inflammation MAPK/ERK Pathway
  2. MMP Apoptosis Autophagy NF-κB TNF Receptor COX Toll-like Receptor (TLR) SOD ASK1 JNK
  3. Ecliptasaponin A

Ecliptasaponin A  (Synonyms: 旱莲苷A)

目录号: HY-N1508 纯度: 99.50%
COA 产品使用指南 技术支持

Ecliptasaponin A 是一种口服有效的五环三萜皂苷。Ecliptasaponin A 通过激活 ASK1/JNK 通路,诱导肺癌细胞凋亡 (apoptosis) 和自噬 (autophagy) 发挥抗肿瘤活性。Ecliptasaponin A 可抑制 HMGB1/TLR4/NF-κB 通路、COX-2MMP9 表达发挥抗炎/抗纤维化作用并保护心血管系统。 Ecliptasaponin A 能增强 SOD 活性、降低 MDA 水平,减轻氧化应激损伤。Ecliptasaponin A 通过抑制 MMP13 的表达、调节炎症因子发挥软骨保护作用。 Ecliptasaponin A 通过上调 ESR1 受体表达,改善卵巢功能,调节性激素。

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Ecliptasaponin A

Ecliptasaponin A Chemical Structure

CAS No. : 78285-90-2

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Customer Review

Other Forms of Ecliptasaponin A:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ecliptasaponin A is an orally active pentacyclic triterpenoid saponin. Ecliptasaponin A exerts anti-tumor activity by activating ASK1/JNK pathway, inducing apoptosis and autophagy in lung cancer cells. Ecliptasaponin A exerts anti-inflammatory/anti-fibrotic effects and protects the cardiovascular system by inhibiting the HMGB1/TLR4/NF-κB pathway, and the expression of COX-2 and MMP-9. Ecliptasaponin A can enhance SOD activity, reduce MDA levels, and alleviate oxidative stress damage. Ecliptasaponin A exerts chondroprotective effects by inhibiting the expression of MMP13 and regulating inflammatory factors. Ecliptasaponin A improves ovarian function and regulates sex hormones by upregulating the expression of ESR1 receptors[1][2][3][4][5][6][7].

IC50 & Target[2][7]

MMP-9

 

MMP-13

 

MMP-2

 

NF-κB

 

COX-2

 

TLR4

 

体外研究
(In Vitro)

Ecliptasaponin A (5-20 μM) 可抑制 HMGB1/TLR4/NF-κB 通路,对氧糖剥夺 (OGD) 的 H9C2 细胞发挥保护作用[3]
Ecliptasaponin A (0-120 μM, 24-48 h) 对 H460 和 H1975 细胞的活力及集落形成能力表现出剂量和时间依赖性抑制[4]
Ecliptasaponin A (0-30 μM, 24 h) 通过激活 ASK1/JNK 通路和自噬,在 H460 和 H1975 细胞中诱导凋亡[4]
Ecliptasaponin A (5-30 μM, 48 h) 抑制转化生长因子-β1 (TGFβ1) 诱导的人肾-2 (HK-2) 细胞中 ECM 和 MMP13 的表达[5]
Ecliptasaponin A (0-25 μM) 靶向 ESR1 蛋白,在环磷酰胺 (HY-17420) 诱导的 AW-CCH252 细胞损伤中提高细胞活力并减少凋亡[6]
Ecliptasaponin A (10-50 ng/mL, 25 h) 在 IL-1β 刺激的 SW1353 细胞中,所有骨关节炎相关分子的表达均降低[7]

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

Cell Viability Assay[4]

Cell Line: H460 and H1975 cells
Concentration: 0, 20, 40, 60, 80, 100 and 120 μM
Incubation Time: 24 and 48 h
Result: Significantly induced cell death in both dose-dependent and time-dependent ways.

Apoptosis Analysis[4]

Cell Line: H460 and H1975 cells
Concentration: 0, 10, 20 and 30 μM
Incubation Time: 24 h
Result: Dose-dependently increased the proportion of apoptotic cells, with early apoptosis (Annexin V+/PI-) being the predominant type.
Displayed typical apoptotic features: nuclear shrinkage, chromatin condensation, nuclear fragmentation, and the formation of apoptotic bodies.

Western Blot Analysis[4]

Cell Line: H460 and H1975 cells
Concentration: 0, 10, 20 and 30 μM
Incubation Time: 24 h
Result: Increased the Caspase-3/8/9 cleavage products and PARP cleavage.
Increased the LC3-II/I ratio, upregulated Beclin-1 expression, and accelerated the degradation of p62.
Increased the expression of p-ASK1 and p-JNK, and decreased the expression of p-ERK.

Western Blot Analysis[5]

Cell Line: HK-2 cells
Concentration: 20 nM
Incubation Time: 48 h
Result: Inhibited the protein expression of ECM proteins such as FN, Col-1, Col-3, and CTGF.
Specifically inhibited MMP13 rather than MMP10.
Inhibited Col-1, α-SMA, and CTGF.

RT-PCR[5]

Cell Line: HK-2 cells
Concentration: 5, 10, 15, 20, 25, 30 nM
Incubation Time: 48 h
Result: Decreased the expression of type I collagen in a concentration-dependent manner.
Inhibited the gene expression of ECM proteins such as FN, Col-1, Col-3, and CTGF.
Significantly inhibited the mRNA expression of MMP10 (not obvious) and MMP13.

RT-PCR[7]

Cell Line: SW1353 cells
Concentration: 10, 30, 50 ng/mL
Incubation Time: Pretreated at 1 h before IL-1β stimulation (24 h) for 25 h
Result: Decreased the mRNA expression of OA-related molecules (MMP13, TNF-α, IL-1β, COX1/2).

Western Blot Analysis[7]

Cell Line: SW1353 cells
Concentration: 10, 30, 50 ng/mL
Incubation Time: Pretreated at 1 h before IL-1β stimulation (24 h) for 25 h
Result: Decreased the protein expression of OA-related molecules (MMP13, Collagen type II, TNF-α, IL-1β, and COX-2).
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Rat 1000 mg/kg p.o. T1/2 3.34 h
Rat 16000 mg/kg p.o. AUC0-∞ 275.23 μg/L·h
Rat 8000 mg/kg p.o. T1/2 3.02 h
Rat 1000 mg/kg p.o. Tmax 0.28 h
Rat 16000 mg/kg p.o. AUC0-t 269.92 μg/L·h
Rat 8000 mg/kg p.o. Tmax 0.23 h
Rat 1000 mg/kg p.o. Cmax 35.15 μg/mL
Rat 16000 mg/kg p.o. Cmax 246.98 μg/L
Rat 8000 mg/kg p.o. Cmax 110.80 μg/L
Rat 1000 mg/kg p.o. AUC0-t 87.52 μg/L·h
Rat 16000 mg/kg p.o. Tmax 0.25 h
Rat 8000 mg/kg p.o. AUC0-t 124.99 μg/L·h
Rat 1000 mg/kg p.o. AUC0-∞ 129.88 μg/L·h
Rat 16000 mg/kg p.o. T1/2 2.94 h
Rat 8000 mg/kg p.o. AUC0-∞ 127.28 μg/L·h
体内研究
(In Vivo)

Ecliptasaponin A (1-18 g/kg, p.o., 单次给药) 分布于多种组织中,浓度顺序为:肝脏 > 脾脏 > 肺 > 肾脏 > 心脏[1]
Ecliptasaponin A (80 mg/kg, p.o., 每日一次共 28 天) 通过抑制 TGF-β1 的表达预防小鼠纤维化[2]
Ecliptasaponin A (0.5-2.5 mg/kg, 左心室心肌心肌内单次注射) 在小鼠急性心肌梗死 (AMI) 模型中具有心脏保护作用[3]
Ecliptasaponin A (25-50 mg/kg, i.p., 共 21 天) 在肺癌裸鼠中可显著抑制肿瘤生长[4]
Ecliptasaponin A (80 mg/kg, p.o., 每日一次共 10 天) 减少肾纤维化单侧输尿管梗阻 (UUO) 小鼠的肾胶原纤维沉积和肾细胞外基质 (ECM) 蛋白的表达[5]
Ecliptasaponin A (200 mg/mL, 和 Specnuezhenide (HY-N0665) 连用, p.o., 每日一次共 30 天) 在早发性卵巢功能不全 (POF) 小鼠中改善基础特征和性激素水平[6]

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

Animal Model: Pulmonary fibrosis model induced by Bleomycin (HY-108345) established in adult male ICR mice (6-7 weeks)[2]
Dosage: 80 mg/kg
Administration: Oral administration (p.o.), once daily for 28 days
Result: Blocked BLM-induced histological changes of lung tissue.
Decreased the high levels of TGF-β1 and α-SMA.
Animal Model: AMI model induced by underwent left anterior descending coronary artery (LAD) ligation established in male SPF C57/BL6 mice, aged 8-10 weeks and weighing 23-25 g[3]
Dosage: 0.5, 1.25, and 2.5 mg/kg
Administration: Intramyocardial injection of the left ventricular myocardium, single dose
Result: Significantly improved ejection fraction (EF%) and short-axis shortening rate (FS%).
Significantly reduced the area of myocardial infarction.
Reduced myocardial cell apoptosis and inflammatory cell infiltration.
Significantly reduced the expressions of HMGB1 and TLR4, as well as the phosphorylation of p-IkBα and p-P65, and the levels of inflammatory factors IL-1β, IL-6, and TNF-α.
Significantly enriched HMGB1/TLR4/NF-κB pathway.
Animal Model: H460 cells induced xenograft tumor model established in male BALB-c nude mice (4-week-old)[4]
Dosage: 25 and 50 mg/kg
Administration: Intraperitoneal injection (i.p.), for 21 days
Result: Decreased the tumor weight and volume.
No significant biological toxicity.
Animal Model: Renal fibrosis UUO model established in six-week-old C57BL/6 J mice[5]
Dosage: 80 mg/kg
Administration: Oral administration (p.o.), once daily for 10 days
Result: Ameliorated the obstructive kidney weight ratio.
Attenuated histological damage and collagen deposition in the kidneys.
Animal Model: POF model established in SPF-grade female C57 mice, 6-8 weeks[6]
Dosage: 200 mg/mL with Specnuezhenide
Administration: Oral administration (p.o.), once daily for 30 days
Result: Increased the ovarian index and serum estradiol (E2) levels.
Reduced the level of follicle-stimulating hormone (FSH).
Extended the emotional cycle.
Increased the number and diameter of follicles.
Promoted ovarian angiogenesis (increase the expression of CD31 and VEGFA).
分子量

634.84

Formula

C36H58O9

CAS 号
性状

固体

颜色

White to off-white

中文名称

早莲苷 A

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (157.52 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5752 mL 7.8760 mL 15.7520 mL
5 mM 0.3150 mL 1.5752 mL 3.1504 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (protect from light)。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (3.94 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.94 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.50%

参考文献

完整储备液配制表

* 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, 6 months; -20°C, 1 month (protect from light)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5752 mL 7.8760 mL 15.7520 mL 39.3800 mL
5 mM 0.3150 mL 1.5752 mL 3.1504 mL 7.8760 mL
10 mM 0.1575 mL 0.7876 mL 1.5752 mL 3.9380 mL
15 mM 0.1050 mL 0.5251 mL 1.0501 mL 2.6253 mL
20 mM 0.0788 mL 0.3938 mL 0.7876 mL 1.9690 mL
25 mM 0.0630 mL 0.3150 mL 0.6301 mL 1.5752 mL
30 mM 0.0525 mL 0.2625 mL 0.5251 mL 1.3127 mL
40 mM 0.0394 mL 0.1969 mL 0.3938 mL 0.9845 mL
50 mM 0.0315 mL 0.1575 mL 0.3150 mL 0.7876 mL
60 mM 0.0263 mL 0.1313 mL 0.2625 mL 0.6563 mL
80 mM 0.0197 mL 0.0984 mL 0.1969 mL 0.4922 mL
100 mM 0.0158 mL 0.0788 mL 0.1575 mL 0.3938 mL
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HY-N1508
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