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Hypericin/金丝桃素 {[allProObj[0].p_purity_real_show]}

货号:A703737 同义名: 金丝桃蒽酮 / NSC 407313; NSC 622946

Hypericin是从贯叶连翘中提取的天然产物,是多种酶(如 PKC、MAO、CYP450)的抑制剂,具有抗肿瘤、抗病毒和抗抑郁活性,可诱导细胞凋亡和免疫激活。

Hypericin/金丝桃素 化学结构 CAS号:548-04-9
Hypericin/金丝桃素 化学结构
CAS号:548-04-9
Hypericin/金丝桃素 3D分子结构
CAS号:548-04-9
Hypericin/金丝桃素 化学结构 CAS号:548-04-9
Hypericin/金丝桃素 3D分子结构 CAS号:548-04-9
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Hypericin/金丝桃素 纯度/质量文件 产品仅供科研

货号:A703737 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PKC PKCα PKCβ PKCγ PKCδ PKCε PKCζ PKCη PKCθ 其他靶点 纯度
Daphnetin +

PKC, IC50: 25.01 μM

PKA,EGFR 95%
Dequalinium Chloride 99%+
Quercetin Sirtuin,Src 95%
Myricetrin 96%
Go 6983 +++

PKCα, IC50: 7 nM

+++

PKCβ, IC50: 7 nM

+++

PKCγ, IC50: 6 nM

+++

PKCδ, IC50: 10 nM

++

PKCζ, IC50: 60 nM

99%+
Go6976 +++

PKC, IC50: 7.9 nM

++++

PKCα, IC50: 2.3 nM

+++

PKCβ1, IC50: 6.2 nM

FLT3 99%+
Bisindolylmaleimide I +++

PKCα, IC50: 20 nM

+++

PKCβ2, IC50: 16 nM

PKCβ1, IC50: 17 nM

+++

PKCγ, IC50: 20 nM

99%+
Lawsone methyl ether 99%
Sotrastaurin ++++

PKCα, Ki: 0.95 nM

++++

PKCβ1, Ki: 0.64 nM

++++

PKCδ, Ki: 2.1 nM

++++

PKCε, Ki: 3.2 nM

++++

PKCη, Ki: 1.8 nM

++++

PKCθ, Ki: 0.22 nM

99%+
Enzastaurin ++

PKCα, IC50: 39 nM

+++

PKCβ, IC50: 6 nM

+

PKCγ, IC50: 83 nM

+

PKCε, IC50: 110 nM

98%
Midostaurin ++

PKCα, IC50: 22 nM

++

PKCβ2, IC50: 31 nM

PKCβ1, IC50: 30 nM

++

PKCγ, IC50: 24 nM

+

PKCδ, IC50: 330 nM

+

PKCε, IC50: 1.25 μM

+

PKCη, IC50: 160 nM

99%
Ro 31-8220 mesylate ++++

PKCα, IC50: 5 nM

+++

PKCβ2, IC50: 14 nM

PKCβ1, IC50: 24 nM

++

PKCγ, IC50: 27 nM

++

PKCε, IC50: 24 nM

99%+
Staurosporine ++++

PKCα, IC50: 2 nM

++++

PKCγ, IC50: 5 nM

+++

PKCδ, IC50: 20 nM

++

PKCε, IC50: 73 nM

++++

PKCη, IC50: 4 nM

99%+
Ruboxistaurin HCl +

PKCα, IC50: 0.36 μM

++++

PKCβ2, IC50: 5.9 nM

PKCβ1, IC50: 4.7 nM

+

PKCγ, IC50: 0.3 μM

+

PKCδ, IC50: 0.25 μM

++

PKCη, IC50: 0.052 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 ALK1 ALK2 ALK3 ALK4 ALK6 Smad3 TGF-β TGFβRI/ALK5 TGFβRII 其他靶点 纯度
LDN193189 ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

99%+
LDN-212854 ++++

ALK1, IC50: 2.4 nM

++++

ALK2, IC50: 1.3 nM

+

ALK3, IC50: 85.8 nM

+

ALK4, IC50: 2133 nM

+

ALK5, IC50: 9276 nM

99%+
ML347 ++

ALK1, IC50: 46 nM

++

ALK2, IC50: 32 nM

98%
K02288 ++++

ALK1, IC50: 1.8 nM

++++

ALK2, IC50: 1.1 nM

++

ALK3, IC50: 34.4 nM

+++

ALK6, IC50: 6.4 nM

99%+
LDN-193189 2HCl ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

99%
LDN-214117 ++

ALK2, IC50: 24 nM

98%
DMH-1 +

ALK2, IC50: 107.9 nM

99%+
SB-505124 +

ALK4, IC50: 129 nM

++

ALK5, IC50: 47 nM

99%+
Vactosertib +++

ALK4, IC50: 13 nM

+++

ALK5, IC50: 11 nM

99%+
Alantolactone 98%
(E/Z)-SIS3 free base 97%
Pirfenidone 98%
Hesperetin 97%
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

98%
GW788388 +++

ALK5, IC50: 18 nM

98%
LY364947 ++

TGFβRI, IC50: 59 nM

+

TGFβRII, IC50: 0.4 μM

98%
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

99%
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

99%+
LY2109761 ++

TβRI, Ki: 38 nM

+

TβRII, Ki: 300 nM

99%+
Galunisertib ++

TβRI, IC50: 56 nM

98%
SB 431542 +

ALK5, IC50: 94 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Telomerase 其他靶点 纯度
4',7-Dimethoxyisoflavone 97%
BIBR 1532 +++

Telomerase, IC50: 100 nM

99%+
Costunolide ++

Telomerase (MCF-7), IC50: 90 μM

Telomerase (MDA-MB-231), IC50: 65 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 MAO MAO-A MAO-B 其他靶点 纯度
Sennoside A ++

MAO, IC50: 17 μM

98%+
Glycyrrhizic acid ++++

MAO, IC50: 0.16 μM

80% HPLC
Rasagiline ++++

MAO-A, IC50: 412 nM

++++

MAO-B, IC50: 4.43 nM

97%
Isatin ++

MAO, IC50: 15 μM

+

MAO-A, IC50: 58 μM

++

MAO-B, IC50: 14 μM

98%
Paeonol +

MAO-A, IC50: 54.6 μM

+

MAO-B, IC50: 42.5 μM

98%
Tranylcypromine HCl +++

MAO-A, IC50: 11.5 μM

+++

MAO-B, IC50: 7 μM

97%
Moclobemide +++

MAO-A (5-HT), IC50: 6.1 μM

99%+
Pargyline HCl ++

MAO-A, Ki: 13 μM

+++

MAO-B, Ki: 0.5 μM

99%+
Safinamide ++++

MAO-B, IC50: 98 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Hypericin/金丝桃素 生物活性

描述 Hypericin, a powerful naturally occurring photosensitizer, is found in Hypericum perforatum plants, commonly known as St. John's wort. Hypericin can induce both apoptosis and necrosis in a concentration and light dose-dependent fashion[3]. Among its antidepressant and light-dependent antiviral actions, hypericin is a powerful natural photosensitizer that is applicable in the photodynamic therapy (PDT) of various oncological diseases. In addition, light-activated hypericin acts as a strong pro-oxidant agent with antineoplastic and antiangiogenic properties, since it effectively induces the apoptosis, necrosis or autophagy of cancer cells. Moreover, a strong affinity of hypericin for necrotic tissue was discovered[4]. Hypericin significantly decreased the minimum inhibitory concentrations of β-lactam antibiotics (e.g., oxacillin, cefazolin and nafcillin), biofilm formation and fibronectin binding in MRSA strain JE2[5]. In vivo, prophylactic or therapeutic use of hypericin inhibited islet β-cell apoptosis and enhanced the anti-oxidative ability of pancreatic tissue in high-fat/high-sucrose (HFHS)-fed mice, thus alleviating β-cell loss and maintaining or improving β-cell mass and islet size. More importantly, hypericin treatment decreased fasting blood glucose, improved glucose intolerance and insulin intolerance, and alleviated HFHS-fed mice[6].

Hypericin/金丝桃素 细胞实验

Cell Line
Concentration Treated Time Description References
Methicillin-resistant Staphylococcus aureus (MRSA) strain JE2 64 mg/L 24 hours To investigate the effect of hypericin on the minimum inhibitory concentrations (MICs) of β-lactam antibiotics (e.g., oxacillin, cefazolin, and nafcillin), showing that hypericin significantly decreased the MICs of these antibiotics. Acta Pharm Sin B. 2019 Nov;9(6):1174-1182
Vero E6 cells 3, 30, 300 nM 15 minutes under light or dark conditions To evaluate the antiviral efficacy of Hypericin against SARS-CoV-2. Results showed that under light conditions, 30 and 300 nM Hypericin significantly reduced viral titer (TCID50/mL from 105.5 to <101); under dark conditions, 300 nM Hypericin also significantly reduced viral titer (from 105.5 to 102.5). ACS Appl Mater Interfaces. 2022 Mar 30;14(12):14025-14032
INS-1 cells 20 nM, 200 nM, 2000 nM 72 hours To investigate the protective effect of Hypericin on INS-1 cell viability under high-glucose conditions. Results showed that Hypericin significantly improved INS-1 cell viability under high-glucose conditions, inhibited high-glucose-induced apoptosis and NO production. Int J Biol Sci. 2019 Jun 2;15(7):1472-1487
HepG2 cells 50-500 nM 2 hours To evaluate the transfection efficiency of photochemical internalization (PCI) technology in HepG2 cells. Results showed that transfection efficiency was significantly enhanced at 600 mJ/cm² radiant exposure, with a 60-75 fold increase compared to nonirradiated cells. ACS Appl Mater Interfaces. 2024 Aug 21;16(33):43416-43429

Hypericin/金丝桃素 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Alcoholic liver injury model Gavage 168.50 mg/g Once daily for 8 weeks Hyperoside prevents alcoholic liver injury through antioxidation, with effects equivalent to silymarin Antioxidants (Basel). 2019 Oct 31;8(11):524
CD1 male mice MRSA bacteremia model Intravenous (hypericin), Intramuscular (oxacillin) 5 mg/kg Once daily (hypericin), Three times a day (oxacillin), for 3 days To evaluate the therapeutic effect of hypericin in combination with oxacillin in the MRSA bacteremia model, showing that the combination significantly reduced MRSA densities in target tissues. Acta Pharm Sin B. 2019 Nov;9(6):1174-1182
C57BL/6J mice HFHS-induced type II diabetes model Intraperitoneal injection 0.5 mg/kg, 1 mg/kg, 2 mg/kg Administered every other day for four months (prevention group) or 30 days (treatment group) To investigate the preventive and therapeutic effects of Hypericin on HFHS-induced type II diabetes in mice. Results showed that Hypericin significantly reduced fasting blood glucose levels, improved glucose intolerance and insulin intolerance, decreased islet β-cell apoptosis, and enhanced the anti-oxidative ability of pancreatic tissue. Int J Biol Sci. 2019 Jun 2;15(7):1472-1487

Hypericin/金丝桃素 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01726764 Type 2 Diabetes ... 展开 >> Depression 收起 << Phase 1 Completed - Denmark ... 展开 >> Department of Clinical Pharmacology, Institute of Public Health, University of Southern Denmark Odense, Denmark, DK-5000 收起 <<
NCT02862236 Subclinical Anxious Adults ... 展开 >> Nootropic Potential of Hypericum and Alprazolam Healthy Adults 收起 << Phase 4 Completed - Israel ... 展开 >> Technion, Israel Institute of Technology Haifa, Israel 收起 <<
NCT00000792 HIV Infections Phase 1 Completed - United States, Maryland ... 展开 >> Johns Hopkins Adult AIDS CRS Baltimore, Maryland, United States, 21287 United States, Massachusetts Beth Israel Deaconess - East Campus A0102 CRS Boston, Massachusetts, United States, 02215 United States, New York NY Univ. HIV/AIDS CRS New York, New York, United States, 10016 收起 <<

Hypericin/金丝桃素 参考文献

[1]Agostinis P, Vantieghem, et al. Hypericin in cancer treatment: more light on the way. Int J Biochem Cell Biol. 2002 Mar;34(3):221-41.

[2]Lenard J, Rabson A, Vanderoef R. Photodynamic inactivation of infectivity of human immunodeficiency virus and other enveloped viruses using hypericin and rose bengal: inhibition of fusion and syncytia formation. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):158-62.

[3]Agostinis P, Vantieghem A, Merlevede W, de Witte PA. Hypericin in cancer treatment: more light on the way. Int J Biochem Cell Biol. 2002 Mar;34(3):221-41

[4]Jendželovská Z, Jendželovský R, Kuchárová B, Fedoročko P. Hypericin in the Light and in the Dark: Two Sides of the Same Coin. Front Plant Sci. 2016 May 6;7:560

[5]Wang G, Li L, Wang X, Li X, Zhang Y, Yu J, Jiang J, You X, Xiong YQ. Hypericin enhances β-lactam antibiotics activity by inhibiting sarA expression in methicillin-resistant Staphylococcus aureus. Acta Pharm Sin B. 2019 Nov;9(6):1174-1182

[6]Liang C, Hao F, Yao X, Qiu Y, Liu L, Wang S, Yu C, Song Z, Bao Y, Yi J, Huang Y, Wu Y, Zheng L, Sun Y, Wang G, Yang X, Yang S, Sun L, Li Y. Hypericin maintians PDX1 expression via the Erk pathway and protects islet β-cells against glucotoxicity and lipotoxicity. Int J Biol Sci. 2019 Jun 2;15(7):1472-1487

Hypericin/金丝桃素 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.91mL

1.98mL

0.99mL

19.82mL

3.96mL

1.98mL

Hypericin/金丝桃素 技术信息

CAS号548-04-9
分子式C30H16O8
分子量 504.44
SMILES Code O=C1C2=C(O)C=C(O)C3=C2C4=C(C5=C6C(O)=CC(C)=C5C7=C4C1=C(O)C=C7C)C8=C3C(O)=CC(O)=C8C6=O
MDL No. MFCD00016683
别名 金丝桃蒽酮 ;NSC 407313; NSC 622946; SGX301
运输蓝冰
InChI Key YDOIFHVUBCIUHF-UHFFFAOYSA-N
Pubchem ID 3663
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

溶解方案

DMSO: 250 mg/mL(495.6 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 二
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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
方案 二
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