1. Apoptosis
  2. Apoptosis
  3. Helichrysetin

Helichrysetin  (Synonyms: 蜡菊亭)

目录号: HY-N4058 纯度: 99.92%
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Helichrysetin 可从 Helichrysum odoratissimum 的花朵中分离得到。Helichrysetin 是一种 ID2 (DNA 结合抑制剂 2) 抑制剂。 Helichrysetin 能诱导细胞凋亡 (apoptosis)。Helichrysetin 有抗肿瘤和抗氧化活性。

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Helichrysetin

Helichrysetin Chemical Structure

CAS No. : 62014-87-3

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Other Forms of Helichrysetin:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Helichrysetin is isolated from the flower Helichrysum odoratissimum. Helichrysetin is an ID2 (DNA binding inhibitor 2) inhibitor. Helichrysetin induces apoptosis. Helichrysetin has anti-tumor and antioxidant activity[1][2][3].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 50 μM
Compound: 11a
Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
[PMID: 25629304]
HeLa IC50
48.1 μM
Compound: 11a
Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
[PMID: 25629304]
HeLa IC50
5.2 μM
Compound: 12, Helichrysetin
Cytotoxicity against human HeLa cells by MTT assay
Cytotoxicity against human HeLa cells by MTT assay
[PMID: 18343123]
HepG2 IC50
40.2 μM
Compound: 11a
Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
[PMID: 25629304]
HT-1080 ED50
40.1 μM
Compound: 9
Antiproliferative activity against human HT1080 cells by MTT assay
Antiproliferative activity against human HT1080 cells by MTT assay
[PMID: 11277741]
Macrophage IC50
21.7 μM
Compound: 28
Toxicity against BALB/c mouse macrophage by MTT assay
Toxicity against BALB/c mouse macrophage by MTT assay
[PMID: 19962891]
体外研究
(In Vitro)

Helichrysetin (0-100 μM, 48 h) 通过靶向 DNA 抑制剂 2 (ID2) 抑制导管原位癌(DCIS) 的发展[1]
Helichrysetin (5-20 μg/mL) 在 A549 人肺癌细胞中可阻断细胞周期, 诱导细胞凋亡[2]
Helichrysetin (10-40 μM, 48 h) 通过靶向 mTOR/p70S6K/c-Myc/pdhk1 介导的癌细胞能量代谢重编程来抑制胃癌细胞的生长[3]

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

Cell Viability Assay[1]

Cell Line: HT-29, A549, MCF-7, and Ca Ski
Concentration: 1.56, 3.13, 6.25, 12.5, 25, 50, 100 μg/mL
Incubation Time: 72 h
Result: Inhibited cell growth in a dose-dependent manner.
IC50 for A549, Ca Ski, HT29, MCF-7 was 50.72 ± 1.26 μM (14.52 ± 0.36 μg/mL), 31.02 ± 0.45 μM (8.88 ± 0.13 μg/mL), 102.94 ± 2.20 μM (29.47 ± 0.63 μg/mL) and 97.35 ± 1.71 μM (27.87 ± 0.49 μg/mL).

Apoptosis Analysis[2]

Cell Line: A549
Concentration: 5, 15, 20 μg/mL
Incubation Time: 24-72 h
Result: The population of early apoptotic cells increased from 2.65 ± 0.31% (control) to 2.78 ± 0.21%, 14.98 ± 0.79%, and 28.55 ±1.19%.
Caused accumulation of cells in S phase, occurring simultaneously with the significant reduction of cell percentage in G0/G1 phase with 15 and 20 μg/mL.

Western Blot Analysis[3]

Cell Line: MGC803
Concentration: 10, 20 40 μM
Incubation Time: 24 h
Result: Increased the protein expression of cleaved caspase 3 (20 and 40 μM) and reduced protein expression of Bcl-2 (40 μM), but had no significant effect on the protein expression of Bax.

RT-PCR[3]

Cell Line: MGC803
Concentration: 10, 20 40 μM
Incubation Time: 24 h
Result: Reduced the mRNA and protein expression of PDHK1 and LDHA but only decreased the mRNA level of LDHB.
Decreased the protein expression of pyruvate dehydrogenase phosphatase (PDP) 2 and the ratio of p-PDHA1/PDHA1.
Increased the expression levels of Nrf2, HO-1, and NQO-1 and reduced Keap1.
Inhibited the phosphorylation of PI3K, Akt, mTOR, and P70S6K.
体内研究
(In Vivo)

Helichrysetin (10 mg/kg, 腹腔注射) 在小鼠中可抑制 DCIS 生长,且无明显副作用[1]
Helichrysetin (3, 10, 30 mg/kg, 腹腔注射) 在胃癌细胞移植小鼠模型中可抑制肿瘤生长[3]

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

Animal Model: MGC803 cell-xenografted mouse model[3]
Dosage: 3, 10, 30 mg/kg
Administration: i.p.
Result: Decreased the tumor size and weight without an obvious effect on body weight in nude mice.
Reduced the expression of Ki67 and increased the number of apoptotic cells in tumor tissues.
分子量

286.28

Formula

C16H14O5

CAS 号
性状

固体

颜色

White to yellow

中文名称

蜡菊亭

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°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 : 50 mg/mL (174.65 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 3.4931 mL 17.4654 mL 34.9308 mL
5 mM 0.6986 mL 3.4931 mL 6.9862 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: ≥ 2.08 mg/mL (7.27 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (7.27 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 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

纯度: 99.92%

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 3.4931 mL 17.4654 mL 34.9308 mL 87.3271 mL
5 mM 0.6986 mL 3.4931 mL 6.9862 mL 17.4654 mL
10 mM 0.3493 mL 1.7465 mL 3.4931 mL 8.7327 mL
15 mM 0.2329 mL 1.1644 mL 2.3287 mL 5.8218 mL
20 mM 0.1747 mL 0.8733 mL 1.7465 mL 4.3664 mL
25 mM 0.1397 mL 0.6986 mL 1.3972 mL 3.4931 mL
30 mM 0.1164 mL 0.5822 mL 1.1644 mL 2.9109 mL
40 mM 0.0873 mL 0.4366 mL 0.8733 mL 2.1832 mL
50 mM 0.0699 mL 0.3493 mL 0.6986 mL 1.7465 mL
60 mM 0.0582 mL 0.2911 mL 0.5822 mL 1.4555 mL
80 mM 0.0437 mL 0.2183 mL 0.4366 mL 1.0916 mL
100 mM 0.0349 mL 0.1747 mL 0.3493 mL 0.8733 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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