Hypericin 是一种天然存在于贯叶连翘中的物质。Hypericin 是PKC(蛋白激酶C)、MAO(单胺氧化酶)、多巴胺-beta-羟化酶、逆转录酶、端粒酶和CYP (cytochrome P450) 的抑制剂。Hypericin 具有抗肿瘤、抗病毒和抗抑郁的活性，可诱导细胞凋亡。
| 生物活性 | Hypericin is a naturally occurring substance found inHyperlcurn perforatumL.Hypericin is an inhibitor ofPKC(protein kinase C),MAO(monoaminoxidase),dopamine-beta-hydroxylase,reverse transcriptase,telomeraseand CYP (cytochrome P450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induceapoptosis[1][2][3]. |
体外研究
(In Vitro) | Hypericin (0.25-4 μM; 24 h) inhibits the growth of fibroblasts (Fb), melanocytes (Mc), and keratinocytes (Kc)[2].
Hypericin (3 μM; 24 h) treatment can induce cells apoptosis[2].
Cell Viability Assay[2] | Cell Line: | Fibroblasts (Fb), melanocytes (Mc), and keratinocytes (Kc) | | Concentration: | 0.25 μM; 0.5 μM; 1 μM; 2 μM; 3 μM; 4 μM | | Incubation Time: | 24 hours | | Result: | Showed the LD50for Fb and Mc at 1.75 μM and 3.5 μM, respectively, and for Kc at a greater dose than 4 μM. |
Apoptosis Analysis[2] | Cell Line: | Fibroblasts (Fb), melanocytes (Mc), and keratinocytes (Kc) | | Concentration: | 3 μM | | Incubation Time: | 24 hours | | Result: | Showed a significant (p<0.001) early apoptotic Fb population (64%), and a smaller, significant (p<0.05) early apoptotic Mc population (20%). |
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体内研究
(In Vivo) | Hypericin (Intravenous injection; 10 mg/kg; once) treatment delays tumor growth[3].
| Animal Model: | 18-20 week-old female BALB/c mice injected with CT26 carcinomas[3] | | Dosage: | 10 mg/kg | | Administration: | Intravenous injection; 10 mg/kg; once | | Result: | Showed a four times delayed tumor growth compared to the control groups. |
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| 来源 | - Plants
- Guttiferae
- Hyperlcurn perforatumL.
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(495.60 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 1.9824 mL | 9.9120 mL | 19.8240 mL | | 5 mM | 0.3965 mL | 1.9824 mL | 3.9648 mL | | 10 mM | 0.1982 mL | 0.9912 mL | 1.9824 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 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 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.08 mg/mL (4.12 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (4.12 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.08 mg/mL (4.12 mM); Clear solution; Need ultrasonic
此方案可获得 2.08 mg/mL (4.12 mM) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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