首页分享 Calenduloside E

Calenduloside E

来源：花匠小妙招时间：2025-01-21 03:02

生物活性

Calenduloside E is a pentacyclic triterpenoid saponin that can be extracted from the bark and roots of Aralia ovata, and has anti-inflammatory and anti-apoptotic activities. Calenduloside E alleviates atherosclerosis by regulating macrophage polarization, improves mitochondrial function by regulating the AMPK-SIRT3 pathway, and alleviates acute liver injury. In addition, Calenduloside E promotes the interaction between L-type calcium channels and Bcl-2 related apoptosis genes, inhibits calcium overload, and alleviates myocardial ischemia/reperfusion injury. Calenduloside E also improves non-alcoholic fatty liver disease by regulating heat shock-dependent pathways, and inhibits ROS mediated JAK1-STAT3 pathways to reduce cellular inflammatory responses[1][2][3][4][5][6].

细胞效力
(Cellular Effect)

HCT-116MCF7MOLT-4NCI-H460SK-BR-3

Cell Line Type Value Description References HCT-116 IC50

18 μM

Compound: OAG

Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay

10.1039/C5MD00502G MCF7 IC50

11.33 μM

Compound: OAG

Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay

10.1039/C5MD00502G MOLT-4 IC50

13.34 μM

Compound: OAG

Cytotoxicity against human MOLT4 cells assessed as reduction in cell viability after 72 hrs by MTT assay

10.1039/C5MD00502G NCI-H460 IC50

6 μM

Compound: 18

Cytotoxicity against human NCI-H460 cells incubated for 72 hrs by cell-titer 96 aqueous non-radioactive cell proliferation assay

[PMID: 26287548] SK-BR-3 IC50

11.88 μM

Compound: OAG

Cytotoxicity against human SKBR3 cells assessed as reduction in cell viability after 72 hrs by MTT assay

10.1039/C5MD00502G 体外研究
(In Vitro)

Calenduloside E (1.25 μg/mL; 24 h) 抑制糖酵解介导的 M1 巨噬细胞极化[2]。
Calenduloside E (1 μM; 2 h) 可缓解 LPS (HY-D1056)/D-galn 诱导的 AML12 和 LX2 细胞损伤和 AMPK-SIRT3 信号通路蛋白表达[3]。
Calenduloside E (0-16 μM; 24 h) 抑制脂质混合物刺激 AML-12 细胞中炎性小体激活和 AML-12 细胞的焦亡 (Pyroptosis)[5]。

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

Western Blot Analysis[2]

Cell Line: ox-LDL-induced M1 macrophages Concentration: 1.25 μg/mL Incubation Time: 24 h Result: Reduced the levels of IL-1 β, IL-6, PFKFB3, GLUT1 and LDHA.

Western Blot Analysis[3]

Cell Line: LPS/ d-galn-induced AML12 and LX2 cells Concentration: 1 μM Incubation Time: 2 h Result: Reduced ROS and JC-1 levels, as well as cell apoptosis.

Immunofluorescence[5]

Cell Line: AML-12 cells stimulated with lipid mixture Concentration: 2, 4, 8 and 16 μM Incubation Time: 24 h Result: Inhibited the increased expression of NLRP3, Caspase-1 p20, and IL-1β. 体内研究
(In Vivo)

Calenduloside E (11 mg/kg; i.g.; 每天 1 次连续 16 周) 减小 ApoE-/- 小鼠动脉粥样硬化斑块大小，增强斑块稳定性，并减少炎症反应[2]。
Calenduloside E (15 和 30 mg/kg; i.g.; 每天 1 次连续 7 天) 抑制 LPS (HY-D1056) 和 D-GalN 诱导的急性肝损伤小鼠肝细胞凋亡，降低小鼠氧化应激和免疫炎症[3]。
Calenduloside E (7.5-30 mg/kg; i.g.; 每天 1 次连续 3 天) 恢复了成年大鼠心室肌细胞 (ARVMs) 的肌节收缩和钙瞬态[4]。
Calenduloside E (5 和 10 mg/kg; i.g.; 每天 1 次连续 4 周) 改善了非酒精性脂肪肝模型小鼠的肝损伤、脂质积累和促纤维化表型并抑制小鼠肝脏炎性体活化和焦亡 (pyroptosis)[5]。

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

Animal Model: HFD-fed ApoE-/- mice[2] Dosage: 11 mg/kg Administration: i.g.；Once a day for 16 weeks Result: Reduced the levels of IL-1β, IL-6, TNF-α, and monocyte chemoattractant protein-1 (MCP-1) in the serum of ApoE-/- mice. Animal Model: LPS (HY-D1056)/dGalN-induced acute liver injury in mice[3] Dosage: 15 and 30 mg/kg Administration: i.g.; 1 time per day for 7 consecutive days Result: Improved hepatocyte infiltration and reduced hepatocyte necrosis and shrinkage.
Reduced hepatocyte ROS levels and serum MDA levels, and increased GSH-Px and SOD levels. Animal Model: Rat Model of MI/R Injury[4] Dosage: 7.5, 15 and 30 mg/kg Administration: i.g.; 1 time per day for 3 consecutive days Result: Myocardial infarction area/risk area decreased to 53%, 38% and 43% respectively.
Restored the expression of calcium-regulating proteins, including calcium transporters (SERCA, a1C, RyR2, and NCX) to normal levels. Animal Model: Establishment of NAFLD model in apoE-/- mice by western diet[5] Dosage: 5 and 10 mg/kg Administration: i.g.; 1 time per day for 4 weeks Result: Reduced the expression of TNF-α, MCP-1, CCL2, Ly6c and cd68 in the liver.
Reversed the upregulation of lipogenic genes FASN, Srebpf, ACC and PPARγ and lipid uptake gene cd36.
Reduced the expression of NLRP3, pNLRC4, NLRC4, cleaved GSDMD, cleaved Caspase1 and IL-1β. 分子量

632.82

Formula

C36H56O9

CAS 号

26020-14-4

性状

固体

颜色

White to off-white

结构分类 Terpenoids Triterpenes 初始来源植物五加科辽东楤木植物其他科内源性代谢物运输条件

Room temperature in continental US; may vary elsewhere.

储存方式 Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (158.02 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 1.5802 mL 7.9011 mL 15.8023 mL 5 mM 0.3160 mL 1.5802 mL 3.1605 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。-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)

体积 (start)

浓度 (final)

体积 (final)

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 (3.95 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。

以 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 (3.95 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。

以 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

每只动物的给药体积

μL

动物数量

只

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 +

2">

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）。

100.0">

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: 99.07%

选择批次：

Data Sheet (659 KB) SDS (251 KB)

COA (291 KB) HNMR (286 KB) LCMS (87 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Tian Y, et al. The clickable activity-based probe of anti-apoptotic calenduloside E. Pharm Biol. 2019 Dec;57(1):133-139. [Content Brief]

[2]. Lanfang Li, et al. "Calenduloside e modulates macrophage polarization via KLF2-regulated glycolysis, contributing to attenuates atherosclerosis." International Immunopharmacology 117 (2023): 109730. [Content Brief]

[3]. Pengli Guo, et al. "Isolation of Calenduloside E from achyranthes bidentata blume and its effects on LPS/D-GalN-induced acute liver injury in mice by regulating the AMPK-SIRT3 signaling pathway." Phytomedicine 125 (2024): 155353. [Content Brief]

[4]. Ruiying Wang, et al. "Calenduloside E suppresses calcium overload by promoting the interaction between L-type calcium channels and Bcl2-associated athanogene 3 to alleviate myocardial ischemia/reperfusion injury." Journal of Advanced Research 34 (2021): 173-186. [Content Brief]

[5]. Yifei Le, et al. "Calenduloside E ameliorates non-alcoholic fatty liver disease via modulating a pyroptosis-dependent pathway." Journal of Ethnopharmacology 319 (2024): 117239. [Content Brief]

[6]. Min Wang, et al. "Calenduloside E ameliorates myocardial ischemia‐reperfusion injury through regulation of AMPK and mitochondrial OPA1." Oxidative Medicine and Cellular Longevity 2020.1 (2020): 2415269. [Content Brief]