Cafestol |
| Catalog No.GC40352 |
Cafestol, one of the major components of coffee, is a coffee-specific diterpene form and an inhibitor of ERK2.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 469-83-0
Sample solution is provided at 25 µL, 10mM.
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Cafestol, one of the major components of coffee, is a coffee-specific diterpene form and an inhibitor of ERK2[1]. Cafestol has elevated blood lipids[2], anti-inflammatory[1], anti-angiogenic[3] and anti-diabetic[4] activities. In addition, Cafestol induces tumor cell apoptosis and autophagy, which can be used in the study of cancer[5].
In vitro, Cafestol (0–100μM; 1–24h) dose-dependently suppressed PGE₂ production and reduced COX-2 mRNA levels in LPS-stimulated RAW 264.7 cells, while concurrently inhibiting AP-1 activation and ERK2 activity after 1h treatment[1]. Cafestol (30μM, 24h) significantly potentiated ABT-737-induced apoptosis in Mcl-1-overexpressed human renal carcinoma Caki cells, human glioma U251MG cells, and human breast carcinoma MDA-MB231 cells by downregulating Mcl-1 protein expression (via promoting protein degradation) and upregulating Bim expression, while showing no cytotoxicity in normal human skin fibroblasts[6].
In vivo, Cafestol (40–80mg/kg; i.g.; 20 days) markedly reduced tumor growth in a colon cancer xenograft mouse model[5]. Oral administration of Cafestol (5mg/kg/day for 14 days) in Wistar albino rats significantly protected against doxorubicin-induced cardiotoxicity by attenuating oxidative stress (downregulate MDA, upregulate GSH/SOD/CAT/Gpx-1), activating the Nrf2/HO-1/NQO-1 pathway (downregulate Keap1/NF-κB), suppressing inflammation (downregulate TNF-α/IL-1β), and inhibiting apoptosis (downregulate Bax/Casp3, downregulate TUNEL-positive cells), while improving cardiac biomarkers (CK-MB/LDH/ALP/ALT) and histopathology[7].
References:
[1] Shen, T., Lee, J., Lee, E., Kim, S. H., Kim, T. W., & Cho, J. Y. (2010). Cafestol, a coffee-specific diterpene, is a novel extracellular signal-regulated kinase inhibitor with AP-1-targeted inhibition of prostaglandin E2 production in lipopolysaccharide-activated macrophages. Biological & pharmaceutical bulletin, 33(1), 128–132.
[2] Urgert, R., Schulz, A. G., & Katan, M. B. (1995). Effects of cafestol and kahweol from coffee grounds on serum lipids and serum liver enzymes in humans. The American journal of clinical nutrition, 61(1), 149–154.
[3] Wang, S., Yoon, Y. C., Sung, M. J., Hur, H. J., & Park, J. H. (2012). Antiangiogenic properties of cafestol, a coffee diterpene, in human umbilical vein endothelial cells. Biochemical and biophysical research communications, 421(3), 567–571.
[4] Mellbye, F. B., Jeppesen, P. B., Shokouh, P., Laustsen, C., Hermansen, K., & Gregersen, S. (2017). Cafestol, a Bioactive Substance in Coffee, Has Antidiabetic Properties in KKAy Mice. Journal of natural products, 80(8), 2353–2359.
[5] Feng, Y., Yang, J., Wang, Y., Wang, X., Ma, Q., Li, Y., Zhang, X., Wang, S., Zhang, Q., Mi, F., Wang, Y., Zhong, D., & Yin, J. (2024). Cafestol inhibits colon cancer cell proliferation and tumor growth in xenograft mice by activating LKB1/AMPK/ULK1-dependent autophagy. The Journal of nutritional biochemistry, 129, 109623.
[6] Woo, S. M., Min, K. J., Seo, B. R., Nam, J. O., Choi, K. S., Yoo, Y. H., & Kwon, T. K. (2014). Cafestol overcomes ABT-737 resistance in Mcl-1-overexpressed renal carcinoma Caki cells through downregulation of Mcl-1 expression and upregulation of Bim expression. Cell death & disease, 5(11), e1514.
[7] Al-Kenany, S. A., & Al-Shawi, N. N. (2023). Protective effect of cafestol against doxorubicin-induced cardiotoxicity in rats by activating the Nrf2 pathway. Frontiers in pharmacology, 14, 1206782.
| Cell experiment [1]: | |
Cell lines | Human renal carcinoma cells (Caki), human breast carcinoma cells (MDA-MB231), human glioma cells (U251MG), human colon carcinoma cells (HCT116), human leukemia cells (U937), and human prostate carcinoma (PC3) cells |
Preparation Method | Human renal carcinoma cells (Caki), human breast carcinoma cells (MDA-MB231), human glioma cells (U251MG), human colon carcinoma cells (HCT116), human leukemia cells (U937), and human prostate carcinoma (PC3) cells were obtained from the American Type Culture Collection. All cells were cultured in Dulbecco’s Modified Eagle’s Medium containing 10% fetal bovine serum, 20mM HEPES buffer, 100U/ml penicillin, 100μg/ml streptomycin, and 100μg/ml gentamicin. A cell death detection ELISA plus kit was used for assessing apoptotic activity by detecting fragmented DNA within the nucleus in ABT-737-, cafestol-, and combination of ABT-737 and cafestol-treated cells. Briefly, cells were treated with different concentrations of cafestol(20 or 30μM) and ABT-737 alone or in combination. After 24h, each culture plate was centrifuged for 10min at 200×g, the supernatant was removed, and the pellet was lysed for 30min. After centrifuging the plate again at 200×g for 10min, the supernatant that contained the cytoplasmic histoneassociated DNA fragments was collected and incubated with an immobilized anti-histone antibody. The reaction products were incubated with a peroxidase substrate for 5min and measured by spectrophotometry at 405 and 490nm (reference wavelength) with a microplate reader. The signals in the wells containing the substrate alone were subtracted as the background. |
Reaction Conditions | 20 or 30μM; 24h |
Applications | Cafestol significantly potentiated ABT-737-induced apoptosis. |
| Animal experiment [2]: | |
Animal models | Wistar albino experimental rats |
Preparation Method | A total of 32 Wistar albino experimental rats of both sexes aged 6 weeks with an average weight of 150g were used in this study; animals were acquired and kept under controlled conditions of a light/dark cycle (12h) at a temperature of 23°C±2°C and humidity of 50% ± 5%. Experimental animals were randomly assigned into four groups (n = 8) as follows: Group I: each rat was given vehicle only (5% Tween in DDW) orally via oral gavage for 14 consecutive days. Then, a single dose of NaCl (0.9%), 10mL/kg, was injected intraperitoneally 1h after the last vehicle administration on day 14. This group served as the normal (negative control) group. Group II: each rat was orally given cafestol (5mg/kg/day) for 14 consecutive days. Group III: each rat was given vehicle only (5% Tween in DDW) via oral gavage for 14 consecutive days. Then, a single dose of doxorubicin (15mg/kg) was injected intraperitoneally 1h after the last vehicle administration on day 14 to serve as the positive control group. Group IV: each rat received cafestol (5mg/kg/day) orally for 14 consecutive days, and then, a single dose of doxorubicin (15mg/kg) was injected intraperitoneally 1h after the last cafestol treatment on day 14. 24 hours after doxorubicin dose administration (i.e., day 15), the animals were anaesthetized and samples were collected for further analysis. |
Dosage form | 5mg/kg/day for 14 days; p.o. |
Applications | Cafestol significantly protected against doxorubicin-induced cardiotoxicity by attenuating oxidative stress, activating the Nrf2/HO-1/NQO-1 pathway, suppressing inflammation, and improving cardiac biomarkers and histopathology. |
References: | |
| Cas No. | 469-83-0 | SDF | |
| Canonical SMILES | O[C@]1(CO)C[C@]23[C@](CC[C@]1([H])C3)([H])[C@@](CCC4=C5C=CO4)(C)[C@]5([H])CC2 | ||
| Formula | C20H28O3 | M.Wt | 316.4 |
| Solubility | DMF: 12 mg/ml,DMF:PBS (pH 7.2) (1:50): 0.02 mg/ml,DMSO: 5 mg/ml,Ethanol: 5 mg/ml | Storage | 4°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 | 3.1606 mL | 15.8028 mL | 31.6056 mL |
| 5 mM | 632.1 μL | 3.1606 mL | 6.3211 mL |
| 10 mM | 316.1 μL | 1.5803 mL | 3.1606 mL |
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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 ddH2O, 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
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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