Garcinol
(Synonyms: 山竹子素) 目录号 : GC13474Garcinol是组蛋白乙酰转移酶p300和PCAF的非特异性抑制剂，IC50分别为7μM和5μM。
Cas No.:78824-30-3
Sample solution is provided at 25 µL, 10mM.
Garcinol is an nonspecificity inhibitor of the histone acetyltransferases (HATs) p300 and PCAF, IC50 values are 7μM and 5μM respectively[1-3]. It is also an nonspecificity inhibitor of potent histone deacetylase 11(HDAC11), IC50 value is 5μM[4].
Garcinol Suppresses CAL-27 cells (10μM, 24h) Proliferation and Colony Formation, inhibits Cell Cycle G1 Phase[5]. And Garcinol induces SCC-15 cells (20μM, 24h) Apoptosis[5]. Garcinol(100μM, 2h) could inhibit the elevated ROS level in H2O2 stimulation-induced Mouse Bone Marrow Mesenchymal Stem Cells(BMSCs) as well[6].
Garcinol(20mg/kg/d for 3days dissolved in 0.1% DMSO by intraperitoneal injection) could decrease inflammation and oxidative stress in cerebral ischemia-reperfusion (I/R) rats, and decreased cerebral injury of I/R rats and improved its neurological function[7]. Garcinol(20mg/kg for 5min dissolved in 0.1% DMSO and intraperitoneally injected)exhibits antithrombotic activity without impacting bleeding time under an efficacious dosage in a model of adenosine diphosphate(ADP)-induced acute pulmonary thromboembolism in mice[8].
Garcinol can prevent ischemia-reperfusion brain injury by inhibiting the TLR4/NF-ĸB signaling pathway to reduce inflammation and oxidative stress and improve nerve function[7].
References:
[1] KOPYTKO P, PIOTROWSKA K, JANISIAK J, et al. Garcinol-A Natural Histone Acetyltransferase Inhibitor and New Anti-Cancer Epigenetic Drug [J]. Int J Mol Sci, 2021, 22(6):
[2] BALASUBRAMANYAM K, ALTAF M, VARIER R A, et al. Polyisoprenylated benzophenone, garcinol, a natural histone acetyltransferase inhibitor, represses chromatin transcription and alters global gene expression [J]. J Biol Chem, 2004, 279(32): 33716-26.
[3] CAO H, AL MAMUN BHUYAN A, UMBACH A T, et al. Garcinol A Novel Inhibitor of Platelet Activation and Apoptosis [J]. Toxins, 2019, 11(7):
[4] SON S I, SU D, HO T T, et al. Garcinol Is an HDAC11 Inhibitor [J]. ACS Chem Biol, 2020, 15(11): 2866-71.
[5] ZHANG G, FU J, SU Y, et al. Opposite Effects of Garcinol on Tumor Energy Metabolism in Oral Squamous Cell Carcinoma Cells [J]. Nutrition and Cancer, 2019, 71(8): 1403-11.
[6] ZOU J, CHEN H, FAN X, et al. Garcinol prevents oxidative stress-induced bone loss and dysfunction of BMSCs through NRF2-antioxidant signaling [J]. Cell Death Discov, 2024, 10(1): 82.
[7] KANG Y, SUN Y, LI T, et al. Garcinol protects against cerebral ischemia-reperfusion injury in vivo and in vitro by inhibiting inflammation and oxidative stress [J]. Mol Cell Probes, 2020, 54(101672.
[8] HSIA C W, HUANG W C, JAYAKUMAR T, et al. Garcinol acts as a novel integrin alpha(IIb)beta(3) inhibitor in human platelets [J]. Life Sci, 2023, 326(121791.
Garcinol是组蛋白乙酰转移酶p300和PCAF的非特异性抑制剂，IC50分别为7μM和5μM[1-3]。它也是强效的组蛋白脱乙酰酶11（HDAC11）的非特异性抑制剂（IC50为5μM）[4]。
Garcinol抑制CAL-27细胞（10μM，24小时）的增殖与克隆形成，使细胞周期停留在G1期[5]。Garcinol还诱导SCC-15细胞（20μM，24小时）凋亡[5]。Garcinol（100μM，2小时）能够抑制由H2O2刺激引起的骨髓间充质干细胞（BMSCs）中升高的活性氧水平[6]。
Garcinol（20mg/kg，三天，0.1% DMSO溶解腹腔注射）能减少脑缺血再灌注大鼠的炎症与氧化应激，并减轻脑缺血再灌注大鼠的脑损伤，改善其神经功能[7]。Garcinol（20mg/kg，5分钟，0.1% DMSO溶解腹腔注射）在二磷酸腺苷诱导的小鼠急性肺栓塞模型中，在有效剂量下表现出抗血栓活性而不影响出血时间[8]。
Garcinol可以通过抑制TLR4/NF-ĸB信号通路减轻炎症和氧化应激以及改善神经功能来预防缺血再灌注脑损伤[7]。
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Cell experiment [1]: |
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Cell lines |
Mouse Bone Marrow Mesenchymal Stem Cells (BMSCs) |
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Preparation method |
The BMSCs cultured at 37°C in a humidified atmosphere with 95% air and 5% CO2. BMSCs were treated with H2O2 at 100μM for 2h to induce the intracellular oxidative stress, followed by treatment with Garcinol of Concentration gradient. |
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Reaction Conditions |
2.5μM, 5μM, 7.5μM, 10μM for 48h. |
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Applications |
Garcinol prevented oxidative stress-related BMSC damage and bone loss. |
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Animal experiment[2]: |
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Animal models |
LPS-induced male mouse calvarial osteolysis model |
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Preparation method |
Mice were injected 5mg/kg LPS and different concentration of garcinol(low‐dose:1mg/kg,high-dose:5mg/kg). Garcinol was dissolved in 5% DMSO in PBS. The mice received a subcutaneous injection over the sagittal midline suture of the calvarium under light inhalation anesthesia. |
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Dosage form |
1mg/kg, 5mg/kg: alternating days over 7‐day; subcutaneous injection. |
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Applications |
Garcinol was evidenced by marked inhibition of lipopolysaccharide‐induced bone resorption. |
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References: [1] ZOU J, CHEN H, FAN X, et al. Garcinol prevents oxidative stress-induced bone loss and dysfunction of BMSCs through NRF2-antioxidant signaling [J]. Cell Death Discov, 2024, 10(1): 82. [2] JIA Y, JIANG J, LU X, et al. Garcinol suppresses RANKL-induced osteoclastogenesis and its underlying mechanism [J]. J Cell Physiol, 2019, 234(5): 7498-509. |
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| Cas No. | 78824-30-3 | SDF | |
| 别名 | 山竹子素 | ||
| 化学名 | (1R,5R,7R)-3-(3,4-dihydroxybenzoyl)-4-hydroxy-8,8-dimethyl-5-((S)-5-methyl-2-(prop-1-en-2-yl)hex-4-en-1-yl)-1,7-bis(3-methylbut-2-en-1-yl)bicyclo[3.3.1]non-3-ene-2,9-dione | ||
| Canonical SMILES | O=C1[C@](C(O)=C2C(C3=CC(O)=C(O)C=C3)=O)(C[C@H](C/C=C(C)/C)C(C)=C)C[C@@H](C/C=C(C)/C)C(C)(C)[C@@]1(C/C=C(C)/C)C2=O | ||
| 分子式 | C38H50O6 | 分子量 | 602.8 |
| 溶解度 | 20mg/mL in ethanol, 25mg/mL in DMSO, 25mg/mL in DMF | 储存条件 | Store at -20°C,protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
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