Garcinol 是一种从印度藤黄提取的聚异戊二烯基二苯甲酮，对乙酰胆碱酯酶 (AChE) 和丁酰胆碱酯酶 (BChE) 具有抗胆碱酯酶的特性，IC50分别为 0.66 μM 和 7.39 μM。Garcinol 还抑制组蛋白乙酰转移酶 (HATs,IC50=7 μM) 和 p300/CPB 相关因子 (PCAF,IC50=5 μM)。Garcinol 具有抗炎和抗癌活性。
| 生物活性 | Garcinol, a polyisoprenylated benzophenone harvested fromGarcinia indica, exerts anti-cholinesterase properties towardsacetylcholinesterase(AChE)andbutyrylcholinesterase (BChE)withIC50s of 0.66 μM and 7.39 μM, respectively[1]. Garcinol also inhibitshistone acetyltransferases(HATs,IC50= 7 μM) andp300/CPB-associated factor(PCAF,IC50= 5 μM). Garcinol has anti-inflammatory and anti-cancer activity[2]. |
| IC50& Target | AChE | BChE | GCN5/PCAF | Human Endogenous Metabolite |
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体外研究
(In Vitro) | Garcinol (10-50 μM; 24-72 hours) can inhibit the proliferation of two HNSCC cell lines tested (CAL27 and UMSCC1) in a time- and dose-dependent manner[3].
Garcinol (10-50 μM; 24-72 hours) induces apoptosis in HNSCC cells[3].
Garcinol (50 μM; 1-6 hours) suppresses phosphorylation and degradation of the constitutive IκBα in a time-dependent manner[3].
Cell Proliferation Assay[3] | Cell Line: | CAL27 and UMSCC1 cells | | Concentration: | 10, 25, 50 μM | | Incubation Time: | 24, 48, and 72 hours | | Result: | Inhibited the proliferation of two HNSCC cell lines in a time- and dose-dependent manner. |
Apoptosis Analysis[3] | Cell Line: | CAL27 and UMSCC1 cells | | Concentration: | 10, 25, 50 μM | | Incubation Time: | 24, 48, and 72 hours | | Result: | Induced apoptosis in HNSCC cells. |
Western Blot Analysis[3] | Cell Line: | CAL27 cells | | Concentration: | 50 μM | | Incubation Time: | 1, 2, 4, 6 hours | | Result: | Suppressed phosphorylation and degradation of the constitutive IκBα in a time-dependent manner. |
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体内研究
(In Vivo) | Garcinol (i.p.; 1 and 2 mg/kg; five times/week for 4 consecutive weeks) induces significant inhibition of tumor growth[3].
| Animal Model: | Five-week-old athymic nu/nu male mice bearing subcutaneous CAL27 tumors[3] | | Dosage: | 1 and 2 mg/kg | | Administration: | I.p.; five times/week for 4 consecutive weeks | | Result: | Induced significant inhibition of tumor growth. |
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| 来源 | - Plants
- Guttiferae
- Garcinia indica
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(82.95 mM;Need ultrasonic) Ethanol : 20 mg/mL(33.18 mM;Need ultrasonic and warming) 配制储备液 | 1 mM | 1.6589 mL | 8.2946 mL | 16.5893 mL | | 5 mM | 0.3318 mL | 1.6589 mL | 3.3179 mL | | 10 mM | 0.1659 mL | 0.8295 mL | 1.6589 mL |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-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 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (4.15 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (4.15 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 25.0 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。 |
