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  3. Strictosamide

Strictosamide 是一种可以从 Nauclea officinalis 中分离得到的化合物。Strictosamide 具有抗炎、镇痛、抗疟原虫、抗真菌和促伤口愈合等多种活性。

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Strictosamide

Strictosamide Chemical Structure

CAS No. : 23141-25-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Strictosamide is a compound that can be isolated from Nauclea officinalis. Strictosamide has various activities such as anti-inflammatory, analgesic, anti-Plasmodium, antifungal, and promoting wound healing[1][2][3][4][5].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 80 μM
Compound: 21
Cytotoxicity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
[PMID: 31804070]
HepG2 IC50
> 80 μM
Compound: 21
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
[PMID: 31804070]
MCF7 IC50
> 80 μM
Compound: 21
Cytotoxicity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
[PMID: 31804070]
体外研究
(In Vitro)

Strictosamide (0-200 μM; 24 h) 在 LPS (HY-D1056) 处理的 RAW 264.7 中能抑制 NO、TNF-α 和 IL-1β 的产生以及 iNOS 表达。机制涉及对 NF-κB 和 MAPK 通路的抑制[1]
Strictosamide (0.25-2 mg/mL) 可抑制离体肾脏中 Mg2+-ATPase 活性[2]

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

Western Blot Analysis[1]

Cell Line: LPS (HY-D1056)-treated RAW 264.7 cells
Concentration: 0, 25, 50, 100 and 200 µM
Incubation Time: 24 h
Result: Markedly decreased the expressions of p-p65, p-IκBα and p-IKKα in NF-κB signaling pathways.
Significantly decreased the phosphorylation of p38, ERK and JNK in MAPK signaling pathways.
体内研究
(In Vivo)

Strictosamide (50-200 mg/kg; 腹腔注射; 单剂量) 可增加小鼠脑 Na+, K+-ATPase 活性,抑制肾脏 Mg2+-ATPase 活性[2]
Strictosamide (10-40 mg/kg; 静脉注射; 每天 2 次; 3 天) 在多种小鼠模型中具有抗炎和镇痛的作用[3]
Strictosamide (0.5-1.5 mg/kg; 涂抹;每天 2 次; 8 天) 在大鼠伤口模型中具有促进伤口愈合的作用。机制涉及对 PI3K/AKT 信号通路的激活[4]

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

Animal Model: ICR mice, weighing 18-22 g[3]
Dosage: 10, 20 and 40 mg/kg
Administration: Intravenous injection; twice a day; 3 days
Result: Obviously decreased the 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mice ear edema (24.7 and 28.1% inhibition, respectively) at 20 and 40 mg/kg.
Significantly inhibited acetic acid (HY-Y0319)-stimulated peritoneal vascular permeability in mice (23.3 and 33.4% inhibition, respectively) at 20 and 40 mg/kg.
Significantly decreased the leukocytes in the mice peritoneal cavity induced by CMC–Na at all the tested doses (46.0, 49.1, and 58.7% inhibition, respectively).
Markedly prolonged the pain latency at 20 and 40 mg/kg and decreased the writhing counts at 40 mg/kg (49.7% inhibition) in acetic acid (HY-Y0319)-induced writhing test in mice. However, it did not obviously improve the pain threshold of mice in hot-plate test.
Animal Model: Male Sprague Dawley (SD) rats (200-220 g) with skin wound model[4]
Dosage: 0.5 and 1.5 mg/kg
Administration: Topical application; twice a day; 8 days
Result: Promoted wound healing.
Reduced inflammatory infiltration.
Enhanced collagen deposition.
Upregulated the expression of CD31 and PCNA
分子量

498.53

Formula

C26H30N2O8

CAS 号
性状

固体

颜色

Off-white to yellow

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 (200.59 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 2.0059 mL 10.0295 mL 20.0590 mL
5 mM 0.4012 mL 2.0059 mL 4.0118 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 (5.01 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.01 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。
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
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 2.0059 mL 10.0295 mL 20.0590 mL 50.1474 mL
5 mM 0.4012 mL 2.0059 mL 4.0118 mL 10.0295 mL
10 mM 0.2006 mL 1.0029 mL 2.0059 mL 5.0147 mL
15 mM 0.1337 mL 0.6686 mL 1.3373 mL 3.3432 mL
20 mM 0.1003 mL 0.5015 mL 1.0029 mL 2.5074 mL
25 mM 0.0802 mL 0.4012 mL 0.8024 mL 2.0059 mL
30 mM 0.0669 mL 0.3343 mL 0.6686 mL 1.6716 mL
40 mM 0.0501 mL 0.2507 mL 0.5015 mL 1.2537 mL
50 mM 0.0401 mL 0.2006 mL 0.4012 mL 1.0029 mL
60 mM 0.0334 mL 0.1672 mL 0.3343 mL 0.8358 mL
80 mM 0.0251 mL 0.1254 mL 0.2507 mL 0.6268 mL
100 mM 0.0201 mL 0.1003 mL 0.2006 mL 0.5015 mL
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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Strictosamide
目录号:
HY-N1198
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