1. Autophagy Anti-infection Metabolic Enzyme/Protease Apoptosis
  2. Autophagy SARS-CoV Cytochrome P450 Apoptosis Parasite
  3. Cepharanthine

Cepharanthine  (Synonyms: 千金藤碱)

目录号: HY-N6972 纯度: 99.91%
COA 产品使用指南

Cepharanthine 是一种可以从植物 Stephania cephalantha  Hayata中分离出来的天然产物。Cepharanthine 具有抗SARS-CoV-2 的活性。Cepharanthine 对病毒增殖有良好的抑制作用 (半数最大 (50%) 抑制浓度 (IC50) 和 90% 抑制浓度 (IC90) 值为 1.90 和 4.46 µM。Cepharanthine 还能有效逆转 K562 细胞中 P-gp 介导的多重耐药性,并增强异种移植小鼠模型中抗癌药物的敏感性。Cepharanthine 对人肝细胞色素 P450 酶 CYP3A4,CYP2E1 和 CYP2C9具有抑制作用。Cepharanthine 具有抗肿瘤、抗炎和镇痛效果。

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Cepharanthine Chemical Structure

Cepharanthine Chemical Structure

CAS No. : 481-49-2

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Other Forms of Cepharanthine:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM[1]. Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model[2][3]. Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects[4][5][6][7][8].

IC50 & Target[4]

CYP3A4

16.29 μM (IC50)

CYP2E1

25.62 μM (IC50)

CYP2C9

24.57 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-431 ED50
2.1 μg/mL
Compound: 11
Cytotoxicity against human A431 cells after 3 days by sulforhodamine B assay
Cytotoxicity against human A431 cells after 3 days by sulforhodamine B assay
[PMID: 8450319]
A549 IC50
5 μM
Compound: 7
Cytotoxicity against human A549 cells after 48 hrs by MTS assay
Cytotoxicity against human A549 cells after 48 hrs by MTS assay
[PMID: 23621840]
A673 GI50
4.5 μM
Compound: Cepheranthine
Antiproliferative activity against human A673 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human A673 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
ECa-109 cell line IC50
> 10 μM
Compound: 7
Cytotoxicity against human ECA109 cells after 48 hrs by MTT assay
Cytotoxicity against human ECA109 cells after 48 hrs by MTT assay
[PMID: 23621840]
ECa-109 cell line IC50
436.7 nM
Compound: CEP
Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
[PMID: 36892076]
HCC1806 GI50
7.2 μM
Compound: Cepheranthine
Antiproliferative activity against human HCC1806 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human HCC1806 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
HCC1937 GI50
6 μM
Compound: Cepheranthine
Antiproliferative activity against human HCC1937 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human HCC1937 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
HCC70 GI50
5.8 μM
Compound: Cepheranthine
Antiproliferative activity against human HCC70 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human HCC70 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
HEK-293T CC50
2.1 μM
Compound: 3; cep
Cytotoxicity against HEK293T cells assessed as reduction in cell viability by CellTiter-Glo assay
Cytotoxicity against HEK293T cells assessed as reduction in cell viability by CellTiter-Glo assay
[PMID: 37043739]
HeLa IC50
1.53 μM
Compound: Cepharanthine
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
[PMID: 29624387]
HL-60 IC50
9.2 μM
Compound: 7
Cytotoxicity against human HL60 cells after 48 hrs by MTS assay
Cytotoxicity against human HL60 cells after 48 hrs by MTS assay
[PMID: 23621840]
HT-1080 ED50
6.1 μg/mL
Compound: 11
Cytotoxicity against human HT1080 cells after 3 days by sulforhodamine B assay
Cytotoxicity against human HT1080 cells after 3 days by sulforhodamine B assay
[PMID: 8450319]
KB ED50
5.9 μg/mL
Compound: 11
Cytotoxicity against human KB cells after 3 days by sulforhodamine B assay
Cytotoxicity against human KB cells after 3 days by sulforhodamine B assay
[PMID: 8450319]
KB ED50
9700 nM
Compound: 12
Cytotoxicity against human KB cells after 72 hrs by SRB assay
Cytotoxicity against human KB cells after 72 hrs by SRB assay
[PMID: 9917283]
KB-V1 ED50
0.9 μg/mL
Compound: 11
Cytotoxicity against human KBV1 cells after 3 days by sulforhodamine B assay
Cytotoxicity against human KBV1 cells after 3 days by sulforhodamine B assay
[PMID: 8450319]
LNCaP ED50
5.6 μg/mL
Compound: 11
Cytotoxicity against human LNCAP cells after 3 days by sulforhodamine B assay
Cytotoxicity against human LNCAP cells after 3 days by sulforhodamine B assay
[PMID: 8450319]
MCF7 IC50
2.9 μM
Compound: 7
Cytotoxicity against human MCF7 cells after 48 hrs by MTS assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTS assay
[PMID: 23621840]
MDA-MB-231 GI50
5.3 μM
Compound: Cepheranthine
Antiproliferative activity against human MDA-MB-231 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
MDA-MB-453 GI50
5.5 μM
Compound: Cepheranthine
Antiproliferative activity against human MDA-MB-453 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human MDA-MB-453 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
MOLT-4 CC50
10 μg/mL
Compound: CEP, Cepharanthine
Cytotoxicity against human MOLT4 cells assessed as cell growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human MOLT4 cells assessed as cell growth inhibition after 24 hrs by MTT assay
[PMID: 24704028]
P388 ED50
0.3 μg/mL
Compound: 11
Cytotoxicity against mouse P388 cells after 2 days by sulforhodamine B assay
Cytotoxicity against mouse P388 cells after 2 days by sulforhodamine B assay
[PMID: 8450319]
SJRH30 GI50
3.8 μM
Compound: Cepheranthine
Antiproliferative activity against human SJRH30 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human SJRH30 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
SK-MEL-2 ED50
14.5 μg/mL
Compound: 11
Cytotoxicity against human SK-MEL-2 cells after 3 days by sulforhodamine B assay
Cytotoxicity against human SK-MEL-2 cells after 3 days by sulforhodamine B assay
[PMID: 8450319]
SMMC-7721 IC50
9.9 μM
Compound: 7
Cytotoxicity against human SMMC7721 cells after 48 hrs by MTS assay
Cytotoxicity against human SMMC7721 cells after 48 hrs by MTS assay
[PMID: 23621840]
SW480 IC50
4.7 μM
Compound: 7
Cytotoxicity against human SW480 cells after 48 hrs by MTS assay
Cytotoxicity against human SW480 cells after 48 hrs by MTS assay
[PMID: 23621840]
U-937 IC50
> 50 μM
Compound: 8, NSC 623442
Cytotoxicity against human U937 cells after 24 hrs by alamar blue assay
Cytotoxicity against human U937 cells after 24 hrs by alamar blue assay
[PMID: 22766217]
Vero CC50
> 50 μM
Compound: Cepharanthine
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
10.1101/2020.03.20.999730
Vero IC50
4.47 μM
Compound: Cepharanthine
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
10.1101/2020.03.20.999730
ZR-75-1 ED50
1.2 μg/mL
Compound: 11
Cytotoxicity against human ZR-75-1 cells after 3 days by sulforhodamine B assay
Cytotoxicity against human ZR-75-1 cells after 3 days by sulforhodamine B assay
[PMID: 8450319]
体外研究
(In Vitro)

Cepharanthine (CEP) (2 μM,48 小时) 抑制细胞活力和集落形成,并通过线粒体途径诱导人 TNBC 细胞凋亡[2]
Cepharanthine (2 μM,48 小时) 会损害 MDA-MB-231 细胞中线粒体的功能,导致线粒体分裂和凋亡[2]
Cepharanthine (5 μM,24 小时) 可增强 K562 细胞 对抗癌剂 Doxorubicin (HY-15142A) 和 Vincristine (HY-N0488) 的敏感性,并可增强抗癌剂诱导下的凋亡[2]
Cepharanthine (10-50 μM,0.5-1 h) 通过抑制细胞质细胞器的酸化改变了 K562 细胞中 Doxorubicin (HY-15142A) 从细胞质液泡到核质的分布[3]
Cepharanthine (0-50 μM,30 min) 在体外显示出对人肝细胞色素 P450 酶 CYP3A4,CYP2E1 和 CYP2C9的抑制作用[4]
Cepharanthine (0-4 μM,48 小时) 阻止恶性疟原虫在环状阶段的发育,对 FCM29,W2,3D7 和 K1 的IC50 分别为 3.059,0.927,2.276 和 1.803 μM[5]

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

Apoptosis Analysis[2]

Cell Line: MDAMB-231 and BT549 cells
Concentration: 2 μM
Incubation Time: 48 h
Result: Cepharanthine alone minimally increased apoptosis (~5% to ~10%), whereas combinated with Epirubicin (HY-13624) markedly increased apoptosis (~50%).

Western Blot Analysis[2]

Cell Line: MDAMB-231 cells
Concentration: 2 μM
Incubation Time: 48 h
Result: Combinated with Epirubicin (HY-13624) markedly resulted in oxidation of the actin-remodeling protein cofilin, which promoted formation of an intramolecular disulfide bridge between Cys39, Cys80 and Ser3 dephosphorylation, leading to mitochondria translocation of cofilin.
Combinated with Epirubicin (HY-13624) induced mitochondrial fission in MDA-MB-231 cells.

Immunofluorescence[3]

Cell Line: K562 cells or MIA-PaCa-2 cells
Concentration: 10,20,25,50 μM
Incubation Time: 0.5 h or 1 h
Result: Made the intracellular localization of Doxorubicin (HY-15142A) in cytoplasmic vesicles shifted to the nucleoplasm.
Decreased red AO (weakly basic fluorescence probe) fluorescence by dose-dependent mannar in K562 cells.

Cell Viability Assay[5]

Cell Line: P. falciparum cultivated in type A+ human erythrocytes
Concentration: 2 μM
Incubation Time: 48 h
Result: Blocked P. falciparum development in ring stage with IC50s of 3.059, 0.927, 2.276, and 1.803 μM for FCM29, W2, 3D7 and K1, respectively.
体内研究
(In Vivo)

Cepharanthine (CEP) (12 mg/kg,腹腔注射,每日 1 次,持续 36 天) 增强 Epirubicin (HY-13624) 在 MDA-MB-231 细胞异种移植物中的治疗效果[2]
Cepharanthine (10 mg/kg,腹腔注射,单次给药) 通过抑制白细胞活化来预防 LPS 诱导的大鼠肺血管损伤[6]
Cepharanthine (10 mg/kg,腹腔注射,单次给药) 通过 NF-kB 抑制 LPS 诱导的大鼠全身炎症模型发挥抗炎作用[7]
Cepharanthine (20-180 mg/kg,腹腔注射) 在小鼠疼痛模型可产生剂量依赖性镇痛作用,ED50 值为 24.5 mg/kg [8]

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

Animal Model: MDA-MB-231 cell xenografts in mice[1]
Dosage: 12 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 36 days
Result: Combinated with Epirubicin (HY-13624) greatly enhanced the therapeutic efficacy compared with administration of either drug alone.
Animal Model: LPS-induced pulmonary vascular injury in male Wistar rats[6]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Decreased LPS-induced pulmonary vascular injury.
Significantly inhibited the increases in plasma tumor necrosis factor-a (TNF-a) concentrations.
Animal Model: LPS-induced Wistar rat model of systemic inflammation[7]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Significantly inhibited the increase in LPS-induced IL-6, TNF-α and nitrate/nitrite levels.
Reduced interstitial edema and inflammatory cell compared with the control group.
Reduced pathologic abnormalities, such as vacuolization, dot necrosis, striped necrosis, and bridging necrosis appeared, and inflammatory cells compared with the control group.
group compared with the LPS group.
Animal Model: Mice pain models in Kunming (KM) strain male and female mice [8]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Resulted in a dose-dependent antinociceptive effect with an ED50 value of 24.5 mg/kg in mice pain models.
Significantly decreased the intestinal propulsion with maximal inhibition at 33.6%.
Clinical Trial
分子量

606.71

Formula

C37H38N2O6

CAS 号
性状

固体

颜色

White to yellow

中文名称

千金藤碱;千金藤素

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 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (82.41 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 1.6482 mL 8.2412 mL 16.4823 mL
5 mM 0.3296 mL 1.6482 mL 3.2965 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)

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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.12 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.43 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。

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: 50% PEG300    50% Saline

    Solubility: 6.02 mg/mL (9.92 mM); 悬浊液; 超声助溶

  • 方案 二

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

    Solubility: 6.02 mg/mL (9.92 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
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)。
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: 99.91%

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。-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 1.6482 mL 8.2412 mL 16.4823 mL 41.2058 mL
5 mM 0.3296 mL 1.6482 mL 3.2965 mL 8.2412 mL
10 mM 0.1648 mL 0.8241 mL 1.6482 mL 4.1206 mL
15 mM 0.1099 mL 0.5494 mL 1.0988 mL 2.7471 mL
20 mM 0.0824 mL 0.4121 mL 0.8241 mL 2.0603 mL
25 mM 0.0659 mL 0.3296 mL 0.6593 mL 1.6482 mL
30 mM 0.0549 mL 0.2747 mL 0.5494 mL 1.3735 mL
40 mM 0.0412 mL 0.2060 mL 0.4121 mL 1.0301 mL
50 mM 0.0330 mL 0.1648 mL 0.3296 mL 0.8241 mL
60 mM 0.0275 mL 0.1374 mL 0.2747 mL 0.6868 mL
80 mM 0.0206 mL 0.1030 mL 0.2060 mL 0.5151 mL
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