Garcinol (Synonyms: Camboginol) |
Catalog No.GC13474
One-Click Copy Product Info
|
Garcinol은 비특이성 히스톤 아세틸트랜스퍼라제(HATs) p300과 PCAF의 저해제로 IC50 값이 각각 7μM과 5μM이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 78824-30-3
Sample solution is provided at 25 µL, 10mM.
Garcinol은 비특이성 히스톤 아세틸트랜스퍼라제(HATs) p300과 PCAF의 저해제로 IC50 값이 각각 7μM과 5μM이다. 게다가 강력한 히스톤 디아세틸라제 11(HDAC11)의 비특이성 저해제로 IC50 값이 5μM이다[4]. Garcinol은 CAL - 27 세포(10μM, 24시간)의 증식과 군락 형성을 억제하고 세포 주기 G1기에 저해작용을 한다[5].
Garcinol은 SCC - 15 세포(20μM, 24시간)의 사멸을 유도한다[5]. Garcinol(100μM, 2시간)은 H₂O₂ 자극 유도 쥐 골수 중간엽 줄기세포(BMSCs)에서 상승한 ROS 수준을 저해할 수도 있다[6].
Garcinol (20mg/kg/일, 3일간 0.1% DMSO에 녹여 복강 주사)은 뇌허혈 재관류(I/R)쥐에서 염증과 산화 스트레스를 줄일 수 있고 I/R쥐의 뇌 손상을 줄이고 그 신경 기능을 향상시킬 수 있다[7]. Garcinol (20mg/kg, 5분, 0.1% DMSO에 녹여 복강 주사)은 쥐의 아데노신 이인산(ADP) - 유도 급성 폐혈전 색전증 모델에서 효과적인 용량 하에서 출혈 시간에 영향을 미치지 않고 항혈전 활성을 나타낼 수 있다[8].
Garcinol은 TLR4 / NF - ĸB 신호 전달 경로를 저해하고 염증과 산화 스트레스를 줄이고 신경 기능을 향상시켜서 허혈 재관류 뇌 손상을 예방할 수 있다[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.
|
세포 실험 [1]: |
|
|
세포 라인 |
쥐 골수 중간엽 줄기세포(BMSCs) |
|
제조 방법 |
BMSCs는 37°C에서 95% 공기와 5% CO₂가 포함된 습윤한 분위기에서 배양했습니다. BMSCs는 세포 내 산화 스트레스를 유도하기 위해 100μM의 H₂O₂로 2시간 처리한 후 농도 경사에 따른 Garcinol 처리를 했습니다. |
|
반응 조건 |
2.5μM, 5μM, 7.5μM, 10μM , 48시간 동안. |
|
응용 분야 |
Garcinol은 산화 스트레스와 관련된 BMSC 손상과 골 손실을 예방했습니다. |
|
동물 실험[2]: |
|
|
동물 모델 |
LPS 유도 수컷 두개골 용해 모델 |
|
제조 방법 |
쥐는 5mg/kg LPS와 Garcinol의 다른 농도(저용량:1mg/kg, 고용량:5mg/kg)를 주사했습니다. Garcinol은 PBS에 5% DMSO가 포함된 것으로 희석했습니다. 쥐는 경증 흡입 마취하에 반구 뚜껑의 사경 중앙선 봉합부위에 피하 주사를 받았습니다. |
|
반응 조건 |
1mg/kg, 5mg/kg: 7일 이상 번갈아가는 일;피하 주사 |
|
응용 분야 |
Garcinol은 지질 다당류 유도 골 흡수를 유의하게 억제로 증명되었습니다. |
|
참고 문헌: [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. |
|
| Cas No. | 78824-30-3 | SDF | |
| Synonyms | Camboginol | ||
| Chemical Name | (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 | ||
| Formula | C38H50O6 | M.Wt | 602.8 |
| Solubility | 20mg/mL in ethanol, 25mg/mL in DMSO, 25mg/mL in DMF | Storage | Store at -20°C,protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6589 mL | 8.2946 mL | 16.5893 mL |
| 5 mM | 331.8 μL | 1.6589 mL | 3.3179 mL |
| 10 mM | 165.9 μL | 829.5 μL | 1.6589 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)