1. Metabolic Enzyme/Protease
  2. MMP Endogenous Metabolite
  3. Stigmasterol

Stigmasterol  (Synonyms: 豆甾醇)

目录号: HY-N0131 纯度: 98.48%
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Stigmasterol 是一种口服有效、能够穿过血脑屏障、具有抗炎和神经保护作用的免疫调节剂。Stigmasterol 激活 AMPK,进而抑制 NF-κBNLRP3 信号通路,减轻小胶质细胞介导的神经炎症,缓解认知障碍和阿尔茨海默病。Stigmasterol 通过 TLR4/NF-κB 通路调节小胶质细胞 M1/M2 极化,从而减轻神经性疼痛。Stigmasterol 可用于神经退行性疾病、炎症性疾病以及疼痛管理等。

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Stigmasterol Chemical Structure

Stigmasterol Chemical Structure

CAS No. : 83-48-7

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Other Forms of Stigmasterol:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Stigmasterol is an orally acitve, immunomodulatory agent with anti-inflammatory and neuroprotective effect, as well as able to cross the blood-brain barrier. Stigmasterol activates AMPK, which in turn inhibits NF-κB and NLRP3 signaling pathways, reduces microglia-mediated neuroinflammation, and alleviates cognitive impairment and Alzheimer's disease. Stigmasterol regulates M1/M2 polarization of microglia through the TLR4/ NF-κB pathway, thereby reducing neuropathic pain. Stigmasterol can be used for neurodegenerative diseases, inflammatory diseases, and pain management, among others[1][2][3][4][5].

IC50 & Target

Human Endogenous Metabolite

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
10.36 μM
Compound: SS
Cytotoxicity against human A549 cells assessed as decrease in cell viability after 24 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as decrease in cell viability after 24 hrs by MTT assay
10.1039/C6MD00178E
A549 IC50
98.2 μM
Compound: 4, stigmasterol
Cytotoxicity against human A549 cells after 1 hr by MTT assay
Cytotoxicity against human A549 cells after 1 hr by MTT assay
[PMID: 18343122]
Calu-1 IC50
> 100 μM
Compound: 7
Inhibition of human Calu1 cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
Inhibition of human Calu1 cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
[PMID: 11374975]
DU-145 IC50
22.73 μM
Compound: 3
Cytotoxicity against human DU145 cells after 24 hrs by MTT assay
Cytotoxicity against human DU145 cells after 24 hrs by MTT assay
[PMID: 22687747]
HeLa IC50
> 100 μM
Compound: 7
Inhibition of human HeLa cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
Inhibition of human HeLa cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
[PMID: 11374975]
HeLa IC50
> 50 μM
Compound: 3
Cytotoxicity against human HeLa cells by MTT assay
Cytotoxicity against human HeLa cells by MTT assay
[PMID: 19388709]
HeLa IC50
12.21 μM
Compound: SS
Cytotoxicity against human HeLa cells assessed as decrease in cell viability after 24 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as decrease in cell viability after 24 hrs by MTT assay
10.1039/C6MD00178E
J774 IC50
> 242.3 μM
Compound: 12
Cytotoxicity against mouse J774 cells by alamar blue assay
Cytotoxicity against mouse J774 cells by alamar blue assay
[PMID: 17637068]
K562 IC50
> 100 μM
Compound: 7
Inhibition of human K562 cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
Inhibition of human K562 cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
[PMID: 11374975]
K562 IC50
11.14 μM
Compound: 3
Cytotoxicity against human K562 cells after 24 hrs by MTT assay
Cytotoxicity against human K562 cells after 24 hrs by MTT assay
[PMID: 22687747]
KB ED50
> 4 μg/mL
Compound: stigmasterol
Cytotoxicity against human KB cells after 72 hrs
Cytotoxicity against human KB cells after 72 hrs
[PMID: 9644061]
MCF7 IC50
21.43 μM
Compound: 3
Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay
[PMID: 22687747]
MDA-MB-231 IC50
564 μM
Compound: 8
Cytotoxicity against human MDA-MB-231 cells after 3 days by Celltiter-Glo assay
Cytotoxicity against human MDA-MB-231 cells after 3 days by Celltiter-Glo assay
[PMID: 28945373]
P388D1 IC50
> 50 μM
Compound: 3
Cytotoxicity against mouse P388D1 cells by MTT assay
Cytotoxicity against mouse P388D1 cells by MTT assay
[PMID: 19388709]
PC-3 IC50
18.28 μM
Compound: 3
Cytotoxicity against human PC3 cells after 24 hrs by MTT assay
Cytotoxicity against human PC3 cells after 24 hrs by MTT assay
[PMID: 22687747]
Raji IC50
> 100 μM
Compound: 7
Inhibition of human Raji cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
Inhibition of human Raji cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
[PMID: 11374975]
Vero IC50
> 100 μM
Compound: 7
Inhibition of african green monkey Vero cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
Inhibition of african green monkey Vero cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
[PMID: 11374975]
WISH IC50
> 100 μM
Compound: 7
Inhibition of human WISH cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
Inhibition of human WISH cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
[PMID: 11374975]
体外研究
(In Vitro)

Stigmasterol 与 IL-1beta 处理的细胞预孵育显示人和小鼠中的 MMP-3 mRNA、小鼠中的 MMP-3 蛋白、小鼠和人中的 MMP-13 mRNA、人中的 ADAMTS-4 mRNA、人中的 PGE2 蛋白显著减少和鼠标。Stigmasterol 还能够抵消 IL-1beta 诱导的 NF-κB 通路[1]

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

Cell Viability Assay[2]

Cell Line: GMI-R1 cells
Concentration: 1 μM, 5 μM, 10 μM, 15 μM, 20 μM, 30 μM, 40 μM, 50 μM
Incubation Time: 24 h
Result: Showed that 1-50 μM stigmasterol did not affect the viability of GMI-R1 cells.

Western Blot Analysis[1]

Cell Line: BV2 cells
Concentration: 10 μM, 20 μM
Incubation Time: 4 h (after 24 h pretreatment with Aβ42 oligomers)
Result: Rescued the reduction of p-AMPK(T 172) in Aβ42 oligomers treated BV2 cells.
Suppressed the increase of p-IκBα and the decrease of IκBα induced by Aβ42 oligomers, reduced the nuclear translocation of NF-κB p65, and inhibited the increase of NLRP3 and Caspase-1 at 20 μM, which are components of the NLPR3 inflammasome.
体内研究
(In Vivo)

Stigmasterol (50 mg/kg;灌胃;每天一次;一个月) 可减轻小鼠认知缺陷,降低大脑皮层和海马体中 Aβ42 的浓度,通过降低促炎细胞因子水平和小胶质细胞活化来抑制神经炎症[1]
Stigmasterol (40 mg/kg;灌胃;每天两次;21 天) 在慢性压迫损伤 (CCI) 的大鼠中,可降低热痛觉过敏和机械痛觉过敏,降低血清 IL-1β 和 IL-8 水平,增加血清 IL-4TGF-β 水平。Stigmasterol 还能降低右侧坐骨神经中 IL-1β、COX-2 和 TLR4 的表达以及脊髓中 IL-1β 的表达,并促进脊髓中 M1 小胶质细胞向 M2 小胶质细胞的转化[2]
Stigmasterol (50-100 mg/kg;腹腔注射;在 LPS 处理前注射,单剂量) 在 LPS 诱导处理的大鼠和小鼠中,可降低大鼠 LPS 诱导的总发热反应,抑制小鼠血液和腹腔液中的中性粒细胞增殖,控制肺和肝损伤,并抑制 LPS 的致死作用[3]
Stigmasterol (20-80 mg/kg;腹腔注射;缺血 2 小时后注射,单剂量) 在大鼠的大脑缺血再灌注损伤模型中,能有效减少神经功能缺损和梗死损伤,改善组织病理学变化,恢复内源性抗氧化防御系统的水平,降低 beclin1 的表达水平和LC3 I 向 LC3 II 的转化,促进 mTOR 的磷酸化,并抑制 24 小时再灌注诱导的 AMPKJNK 的磷酸化以及 JNK 的表达[4]
Stigmasterol (10 mg/kg;口服;单剂量) 在东莨菪碱诱导小鼠记忆损伤的模型中,可显著减轻被动回避和 Morris 水迷宫任务中由东莨菪碱诱导的记忆损伤,并增加海马体中 ERK 和 CREB 的磷酸化水平。这种改善作用可被 Dizocilpine (HY-15084B) 和 Tamoxifen (HY-13757A) 阻断[5]

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

Animal Model: Alzheimer's disease mouse model (APPswe/PS1dE9 male mice (male; 8-month-old))[1]
Dosage: 50 mg/kg (dissolved in medium chain triglycerides (MCT))
Administration: Gavage, once per day, one month
Result: Significantly increased the stigmasterol concentration in the brain, liver and serum.
In the Morris water maze test, it reduced the escape latency in the navigation trails and increased the time spent in the target quadrant and the number of crossovers in the probe test.
ELISA results showed that it significantly reduced the Aβ42 concentration in the cortex and hippocampus, but had no significant effect on Aβ42 concentration.
TMT-based quantitative proteomic analysis and subsequent experiments showed that it suppressed the elevation of pro-inflammatory cytokines TNFα and IL-1β in the cortex, hippocampus and serum, decreased the activation of microglia and astrocytes, and inhibited the activated NF-κB signaling and NLRP3 inflammasome in the brain.
Animal Model: Chronic constriction injury (CCI) model (male Sprague-Dawley rats ;male; 180-220 g; 7-8 weeks old)[2]
Dosage: 40 mg/kg
Administration: Gavage, twice per day, 21 days
Result: In behavioral evaluations, stigmasterol treatment relieved thermal and mechanical hyperalgesia from the 7th day to the 21st day.
ELISA results showed that it decreased the levels of pro-inflammatory cytokines (IL-1β and IL-8) and increased the levels of anti-inflammatory cytokines (IL-4 and TGF-β in the serum.
H&E staining and immunohistochemical analysis showed that it decreased the number of inflammatory cells in the injured sciatic nerve, partially restored the tissue structure, and improved neuroinflammation in the spinal cord by reducing the expression levels of IL-1β and COX-2 and increasing the expression level of IL-10.
Immunofluorescence results showed that it reduced the expression of M1 markers (such as CD32) and increased the expression of M2 markers (such as CD206) in the spinal cord. Western blotting analysis showed that it decreased the expression of Iba-1, TLR4, MyD88, pNF-κB, pP38 MAPK, pJNK, and pERK in the spinal cord.
Animal Model: LPS-induced pyrexia model (Wistar rats; 180-220 g)[3]
Dosage: 10 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Intraperitoneal injection, once, 30 min before LPS challenge
Result: Pretreatment with stigmasterol at 10, 50 and 100 mg/kg significantly reduced the peak increase in basal rectal temperature and the total pyrexia response (Thermal Index) compared to the control group. The inhibition rates of LPS-induced pyrexia were 39.93%, 53.05% and 77.27% respectively.
分子量

412.69

Formula

C29H48O

CAS 号
性状

固体

颜色

White to off-white

中文名称

豆甾醇

结构分类
初始来源
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 2 years
-20°C 1 year
溶解性数据
细胞实验: 

Acetone 中的溶解度 : 2 mg/mL (4.85 mM; 超声助溶 (<60°C))

DMF 中的溶解度 : 1 mg/mL (2.42 mM; 超声助溶 (<60°C))

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

1M NaOH 中的溶解度 : < 1 mg/mL (insoluble)

Ethanol 中的溶解度 : < 1 mg/mL (insoluble)

DMSO 中的溶解度 : < 1 mg/mL (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4231 mL 12.1156 mL 24.2313 mL
5 mM --- --- ---
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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: Corn Oil

    Solubility: 3.12 mg/mL (7.56 mM); 澄清溶液; 超声助溶 (<50°C)

  • 方案 二

    请依序添加每种溶剂: 15% Cremophor EL    85% Saline

    Solubility: 10 mg/mL (24.23 mM); 悬浊液; 超声助溶

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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 98.48%

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMF / Acetone 1 mM 2.4231 mL 12.1156 mL 24.2313 mL 60.5782 mL
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  • 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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产品名称:
Stigmasterol
目录号:
HY-N0131
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