1. Apoptosis PI3K/Akt/mTOR Epigenetics Cell Cycle/DNA Damage NF-κB Stem Cell/Wnt Immunology/Inflammation
  2. Apoptosis AMPK Akt PERK Keap1-Nrf2 Caspase PARP GSK-3 NO Synthase Interleukin Related
  3. Gomisin N

Gomisin N  (Synonyms: 戈米辛N)

目录号: HY-N6866 纯度: 99.94%
COA 产品使用指南 技术支持

Gomisin N 是一种口服活性的木脂素化合物。Gomisin N 可从 Schisandra chinensis 中分离得到。Gomisin N 在多种细胞中诱导凋亡 (Apoptosis)。Gomisin N 激活 AMPKAktMAPK/ERKNrf2caspase-3PARP-1。Gomisin N 抑制 GSK3β、一氧化氮 (NO) 和促炎细胞因子 (IL-1βIL-6TNF-α)。Gomisin N 具有抗炎、抗氧化、抗肥胖、抗糖尿病、抑制黑色素生成活性。Gomisin N 对宫颈癌和肝癌具有抗肿瘤活性。Gomisin N 改善阿尔兹海默症。

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Gomisin N

Gomisin N Chemical Structure

CAS No. : 69176-52-9

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Gomisin N is an orally active lignan compound. Gomisin N can be isolated from Schisandra chinensis. Gomisin N induces Apoptosis in a variety of cells. Gomisin N activates AMPK, Akt, MAPK/ERK, Nrf2, caspase-3 and PARP-1. Gomisin N inhibits GSK3β, nitric oxide (NO), and proinflammatory cytokines (IL-1β, IL-6, TNF-α). Gomisin N has anti-inflammatory, antioxidant, anti-obesity, anti-diabetic, and anti-melanogenesis activities. Gomisin N has anti-tumor activity against cervical cancer and liver cancer. Gomisin N improves Alzheimer's disease[1][2][3][4][5][6][7][8][9][10].

IC50 & Target[1][2][3][4][5][6][7][8][9][10]

GSK-3β

 

PARP-1

 

Caspase-3

 

IL-1β

 

IL-6

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
21.1 μM
Compound: Gomisin N
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
[PMID: 18063366]
A549 IC50
87.8 μM
Compound: Wuweizisu B
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
[PMID: 18063366]
BV-2 IC50
> 100 μM
Compound: 15
Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reaction based assay
Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reaction based assay
[PMID: 27919656]
HCT-15 IC50
14.1 μM
Compound: Gomisin N
Antiproliferative activity against human HCT15 cells after 72 hrs by SRB assay
Antiproliferative activity against human HCT15 cells after 72 hrs by SRB assay
[PMID: 18063366]
HCT-15 IC50
88.1 μM
Compound: Wuweizisu B
Antiproliferative activity against human HCT15 cells after 72 hrs by SRB assay
Antiproliferative activity against human HCT15 cells after 72 hrs by SRB assay
[PMID: 18063366]
HL-60 IC50
52.4 μM
Compound: 9
Cytotoxicity against human HL60 cells by XTT assay
Cytotoxicity against human HL60 cells by XTT assay
[PMID: 16562834]
K562 IC50
22 μM
Compound: Gomisin N
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
[PMID: 18063366]
K562 IC50
62.6 μM
Compound: Wuweizisu B
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
[PMID: 18063366]
MDA-MB-231 IC50
> 100 μM
Compound: Wuweizisu B
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
[PMID: 18063366]
MDA-MB-231 IC50
> 100 μM
Compound: Gomisin N
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
[PMID: 18063366]
SK-HEP1 IC50
> 100 μM
Compound: Wuweizisu B
Antiproliferative activity against human SK-HEP1 cells after 72 hrs by SRB assay
Antiproliferative activity against human SK-HEP1 cells after 72 hrs by SRB assay
[PMID: 18063366]
SK-HEP1 IC50
> 100 μM
Compound: Gomisin N
Antiproliferative activity against human SK-HEP1 cells after 72 hrs by SRB assay
Antiproliferative activity against human SK-HEP1 cells after 72 hrs by SRB assay
[PMID: 18063366]
SNU-638 IC50
> 100 μM
Compound: Wuweizisu B
Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay
Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay
[PMID: 18063366]
SNU-638 IC50
23.1 μM
Compound: Gomisin N
Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay
Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay
[PMID: 18063366]
T47D IC50
> 100 μM
Compound: Wuweizisu B
Antiproliferative activity against human T47D cells after 72 hrs by SRB assay
Antiproliferative activity against human T47D cells after 72 hrs by SRB assay
[PMID: 18063366]
T47D IC50
19.2 μM
Compound: Gomisin N
Antiproliferative activity against human T47D cells after 72 hrs by SRB assay
Antiproliferative activity against human T47D cells after 72 hrs by SRB assay
[PMID: 18063366]
体外研究
(In Vitro)

Gomisin N (100 μM,30 min) 可增强 TRAIL 诱导的 Hela 细胞凋亡[1]
Gomisin N (10-100 μM;30 min-6 h) 可激活 C2C12 肌管中 AMPKAkt 信号传导,并刺激葡萄糖摄取[2]
Gomisin N (2.5-20 μM;1 h) 在 LPS 刺激的 Raw 264.7 细胞中表现出抗炎作用,可减少一氧化氮 (NO) 的产生和促炎细胞因子 (IL-1β、IL-6、TNF-α) 的表达[3]
Gomisin N (25-100 μM;48 h) 可降低 HepG2 和 HCCLM3 细胞的活力[5]
Gomisin N (40-320 μM; 24 h) 显著诱导 HepG2 细胞的抗增殖和促凋亡作用[6]
Gomisin N (10-100 μM; 16 h) 显示出对 HepG2 细胞中内质网应激诱导的肝脂肪变性的保护作用[8]
Gomisin N (1-10 μM; 72 h) 通过激活 Melan-A 细胞中的 PI3K/Akt 和 MAPK/ERK 信号通路来抑制黑素生成[9]
Gomisin N (50 μM;24 h) 通过抑制 GSK3β,激活 Nrf2 信号通路在 H2O2 处理的 SH-SY5Y/APP695swe 细胞中发挥抗氧化作用[10]

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

Apoptosis Analysis[1]

Cell Line: Hela cells treated with TRAIL
Concentration: 100 μM
Incubation Time: 30 min
Result: Significantly enhanced the cleavage of caspase-3 and PARP-1.
Enhanced TRAIL-induced apoptosis.

Real Time qPCR[8]

Cell Line: HepG2
Concentration: 10 μM, 50 μM, 100 μM
Incubation Time: Pre-incubation for 16 h
Result: Inhibited the expression of ER stress markers GRP78, CHOP, and XBP-1.
Inhibited the expression of inflammatory genes IL-6, TNF-α, and MCP-1 and lipogenic genes FAS, ACC1, and GPAT.
体内研究
(In Vivo)

Gomisin N (20 mg/kg;口服;每日一次;疗程 6 周) 可降低高脂饮食 (HFD) 诱导的肥胖 C57BL/6 小鼠的高血糖症并改善葡萄糖耐量[2]
Gomisin N (2-10 mg/kg;口服;每周 3 次;疗程 8 周) 可预防 HFD 诱导的肥胖并改善 C57BL/6 小鼠的肝脏脂肪变性[4]
Gomisin N (1-30 mg/kg;口服;4 天) 可缓解 Tunicamycin (HY-A0098) 诱导的肝脏内质网应激和甘油三酯蓄积,并改善 C57BL/6 小鼠的肝损伤[8]
Gomisin N (10-20 mg/kg;灌胃;2 个月) 可以改善 Aβ25-35 诱导的 AD 大鼠的学习记忆能力,减少海马和皮质区 Aβ 斑块面积,增加神经元数量,改善氧化应激状态[10]

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

Animal Model: C57BL/6 mice (male, 6-week-old) + high-fat diet (HFD)-induced obese model[2]
Dosage: 20 mg/kg
Administration: Oral gavage (p.o.), once a day for 6 weeks
Result: Reduced HFD-induced fasting glucose and insulin levels.
Lowered blood glucose levels at 30-120 min after glucose loading.
Increased the phosphorylation of AMPK and Akt.
Increased the ratio of plasma membrane GLUT4 to cytoplasmic GLUT4.
Stimulated the expression of mitochondria biogenesis genes in the skeletal muscle.
Animal Model: C57BL/6 mice (male and female, 8-week-old), Tunicamycin-induced hepatic steatosis model[8]
Dosage: 1 mg/kg, 30 mg/kg
Administration: Oral gavage (p.o.), 4 days
Result: Inhibited the increase in liver TG levels and the expression of ER stress markers.
Decreased serum GOT and GPT levels.
分子量

400.46

Formula

C23H28O6

CAS 号
性状

固体

颜色

White to off-white

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 (249.71 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 2.4971 mL 12.4856 mL 24.9713 mL
5 mM 0.4994 mL 2.4971 mL 4.9943 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.24 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 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

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

    Solubility: ≥ 2.5 mg/mL (6.24 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: 99.94%

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 2.4971 mL 12.4856 mL 24.9713 mL 62.4282 mL
5 mM 0.4994 mL 2.4971 mL 4.9943 mL 12.4856 mL
10 mM 0.2497 mL 1.2486 mL 2.4971 mL 6.2428 mL
15 mM 0.1665 mL 0.8324 mL 1.6648 mL 4.1619 mL
20 mM 0.1249 mL 0.6243 mL 1.2486 mL 3.1214 mL
25 mM 0.0999 mL 0.4994 mL 0.9989 mL 2.4971 mL
30 mM 0.0832 mL 0.4162 mL 0.8324 mL 2.0809 mL
40 mM 0.0624 mL 0.3121 mL 0.6243 mL 1.5607 mL
50 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2486 mL
60 mM 0.0416 mL 0.2081 mL 0.4162 mL 1.0405 mL
80 mM 0.0312 mL 0.1561 mL 0.3121 mL 0.7804 mL
100 mM 0.0250 mL 0.1249 mL 0.2497 mL 0.6243 mL
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    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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