Structure of Farrerol
CAS No.: 24211-30-1
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Farrerol is a natural product isolated and purified from the leaves of Rhododendron dauricum L.
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CAS No. : | 24211-30-1 |
Formula : | C17H16O5 |
M.W : | 300.31 |
SMILES Code : | CC1=C2C(C(C[C@@H](C3=CC=C(C=C3)O)O2)=O)=C(C(C)=C1O)O |
MDL No. : | MFCD28347824 |
InChI Key : | DYHOLQACRGJEHX-UHFFFAOYSA-N |
Pubchem ID : | 91144 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
HEK 293FT cells | 0.1, 1, 5, 10 μM | 24 hours | Promotes SpCRISPR/Cas9-mediated gene targeting efficiency | PMC7380943 |
EA.hy926 cells | 40-160 μM | 24 or 48 hours | FA did not significantly affect the viability of EA.hy926 cells. | PMC8430798 |
Mouse mammary epithelial cells (mMECs) | 90, 110, 130 µM | 1 h pretreatment followed by LPS stimulation for 4 h | Inhibited inflammatory response and phosphorylation of AKT, NF-κB p65, p38, and ERK1/2 | PMC6032361 |
HepG2 cells | 5, 10, 20 μM | 1 hour | To evaluate the protective effect of Farrerol against H2O2-induced cytotoxicity, results showed that Farrerol pretreatment significantly suppressed cytotoxicity caused by H2O2 in a dose-dependent manner. | PMC6429022 |
RAW264.7 cells | 25, 50, 100 μM | 1 hour | Farrerol significantly reduced the production of inflammatory mediators (IL-1β, IL-6, TNF-α, COX-2, and iNOS) in LPS-induced RAW264.7 cells by suppressing AKT, ERK1/2, JNK1/2, and NF-κB p65 phosphorylation. | PMC6073308 |
Bone marrow-derived macrophages (BMDM) | 20 μM | 15 minutes | To investigate the inhibitory effect of FA on NLRP3 inflammasome activation in macrophages. Results showed that FA significantly reduced IL-1β release and caspase-1 activation. | PMC9043491 |
HepG2 cells | 5, 10, 20 μM | 18 hours | To evaluate the inhibitory effect of Farrerol on H2O2-induced ROS generation, results showed that Farrerol pretreatment significantly reduced H2O2-induced ROS generation in a dose-dependent manner. | PMC6429022 |
Human proximal tubule cells (HK-2) | 5, 10, 20 μM | 18 hours | Farrerol pretreatment significantly attenuated cisplatin-induced cytotoxicity, particularly at a concentration of 20 μM. | PMC6901966 |
Mouse tubular epithelial cells (MTECs) | 5, 10, 20 μM | 18 hours | Farrerol pretreatment significantly attenuated cisplatin-induced cytotoxicity, particularly at a concentration of 20 μM. | PMC6901966 |
Rat thoracic aorta vascular smooth muscle cells (VSMCs) | 0.3–10 μM | 2 h pretreatment followed by 48 h stimulation | Inhibited FBS-induced VSMC proliferation and DNA synthesis, associated with G1 cell cycle arrest, down-regulation of cell cycle proteins, and reduction in FBS-induced ERK1/2 phosphorylation | PMC4001983 |
HaCaT cells | 4.7 µM (IC50) | 20 hours | Evaluate inhibition of Farrerol on VEGF-induced wound healing, results showed IC50 of 4.7 µM | PMC11767819 |
HCA2-hTERT cells | 0.1 μM | 24 hours | Farrerol promoted the recruitment of RAD51 at DNA damage sites and accelerated γH2AX foci clearance via UCHL3 | PMC10070447 |
HEK293 cells | 20 μM | 24 hours | Confirmed UCHL3 as the direct target of Farrerol via CETSA assay, Farrerol increased the thermal stability of UCHL3 | PMC10070447 |
Mouse embryonic stem cells (ESCs) | 0.1, 1, 5, 10 μM | 24 hours | Significantly enhances SpCRISPR/Cas9-mediated gene targeting efficiency | PMC7380943 |
Fibroblasts | 20 μM | 24 hours | Farrerol significantly inhibited Ang II-induced fibroblast migration and proliferation and reduced the expression of Collagen III and α-SMA. | PMC9846078 |
Neonatal rat cardiomyocytes (NRCM) | 20 μM | 24 hours | Farrerol reduced the Ang II-induced increase in cardiomyocyte surface area and decreased mitochondrial ROS levels. | PMC9846078 |
Human renal tubular epithelial cells (HK-2) | 20 μM | 24 hours | To evaluate the effect of Farrerol on the expression of Nrf2 and PINK1 | PMC8631930 |
HepG2 cells | 20 μM | 24 hours | To investigate the effect of Farrerol on PAOA-induced lipid accumulation in HepG2 cells. Results showed that Farrerol reduced lipid accumulation by targeting PTPN1 and decreasing INSR dephosphorylation. | PMC11408267 |
Rat tenocytes | 1, 5, 10, 20 and 40 μ M | 24 hours | To evaluate the protective effect of Farrerol against RSL3-induced ferroptosis. Results showed that Farrerol at 10-40 μM concentrations was non-toxic and significantly inhibited RSL3-induced cell death and lipid peroxidation. | PMC9189353 |
RAW264.3 cells | 1 µM, 10 µM, 25 µM | 24 hours | Evaluate inhibition of Farrerol on VEGF-induced NF-κB activity, results showed dose-dependent suppression | PMC11767819 |
HaCaT cells | 1 µM, 10 µM, 25 µM, 50 µM, 100 µM | 24 hours | Evaluate cytotoxicity, results showed Farrerol did not induce significant apoptosis at concentrations up to 100 µM | PMC11767819 |
SKOV3 cells | 40-160 μM | 24 or 48 hours | FA decreased the viability of SKOV3 cells in a dose- and time-dependent manner, inducing G2/M cell cycle arrest and apoptosis. | PMC8430798 |
A549 cells | 0-64 µg/mL | 3 hours | Evaluate the effect of Farrerol on the survival of A549 cells infected with MRSA USA300. Results showed that Farrerol significantly reduced LDH release, indicating decreased cell damage. | PMC11963547 |
Rat liver microsomes | 50 μM | 60 minutes | To study the metabolites of Farrerol, 15 in vitro metabolites were identified | PMC6804004 |
3T3-L1 cells | 15 or 30 μM | 8 days | FA significantly increased adipocyte differentiation and intracellular lipid accumulation, and reversed TNF-α-mediated lipolysis. | PMC8430798 |
Neofusicoccum laricinum | 0.10 g/L, 0.25 g/L, 0.5 g/L, 1 g/L, 2 g/L | 8 days | Evaluate the inhibitory effect of Farrerol on Neofusicoccum laricinum. The results showed that the inhibitory effect increased with the concentration of Farrerol, with 2 g/L achieving nearly 100% inhibition rate. | PMC11547970 |
Rat aortic vascular smooth muscle cells (VSMCs) | 14.02 μM | To study the effect of Farrerol on L-type voltage-gated Ca2+ channels (LVGC) using whole-cell patch clamp, results showed Farrerol significantly inhibited Ca2+ influx current. | PMC4013652 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
B6 mice | APAP-induced hepatotoxicity model | Intraperitoneal injection | 40 mg/kg | Twice, at 12 h and 1 h intervals | To evaluate the protective effect of Farrerol against APAP-induced hepatotoxicity, results showed that Farrerol significantly reduced mortality, histopathological liver changes, and ALT and AST levels caused by APAP. | PMC6429022 |
C57BL/6 mice | Cisplatin-induced acute kidney injury model | Intraperitoneal injection | 20 mg/kg | Farrerol was administered 1 hour after cisplatin, and again at 24 and 48 hours, with sacrifice 24 hours after the last dose. | Farrerol significantly improved cisplatin-induced renal damage, including recovery of BUN, SCr, KIM-1, and NGAL levels, and alleviated pathological damage. | PMC6901966 |
Mice | Embryo model | Added to culture medium | 0.05, 0.1 μM | 24 hours | Improves SpCRISPR/Cas9-mediated gene targeting efficiency and supports efficient generation of gene-targeted mice | PMC7380943 |
C57BL/6 mice | TNBS-induced colitis model | Oral | 45 mg/kg | Once daily for 3 days | Farrerol significantly improved weight change, clinical scores, colon length, and intestinal epithelium barrier damage, and markedly decreased inflammatory cytokines production in TNBS-induced mice. | PMC6073308 |
C57BL/6J mice | Angiotensin II (Ang II)-induced cardiac remodeling model | Intraperitoneal injection | 10 mg/kg | Once daily for 2 weeks | Farrerol inhibited Ang II-induced cardiac hypertrophy, inflammation, fibrosis, and oxidative stress, and improved cardiac function. | PMC9846078 |
BALB/c mice | LPS-induced mastitis model | Intraperitoneal injection | 20, 30, 40 mg/kg | Second dose administered 12 h after LPS injection | Improved pathological injury of mammary gland, reduced MPO activity, inhibited pro-inflammatory mediators and phosphorylation of AKT, NF-κB p65, p38, and ERK1/2 | PMC6032361 |
C57BL/6J mice | Myocardial ischemia/reperfusion (I/R) injury model | Intraperitoneal injection | 10 mg/kg or 40 mg/kg | Once daily for 7 days | To investigate the protective effect of FA on myocardial I/R injury. Results showed that FA significantly alleviated myocardial tissue damage, reduced the secretion of myocardial injury factors (CK-MB, LDH, troponin-1, and NT-proBNP), and inhibited the release of inflammatory factors (IL-1β, IL-6, and TNF-α). | PMC9043491 |
C57BL/6 wild-type and Nrf2 knockout mice | Cisplatin-induced chronic kidney disease (CKD) model | Intraperitoneal injection | 10 mg/kg | Once daily until the day of harvest or 5 days after the second cisplatin injection | To evaluate the protective effect of Farrerol on cisplatin-induced CKD and its mechanism | PMC8631930 |
C57BL/6J mice | High-fat diet-induced MAFLD model | Intraperitoneal injection | 40 mg/kg | Once daily for 8 weeks | To investigate the effect of Farrerol on insulin resistance and hepatic steatosis in high-fat diet-induced MAFLD mice. Results showed that Farrerol improved insulin sensitivity, glucose tolerance, and alleviated hepatic steatosis and lipid accumulation. | PMC11408267 |
Sprague-Dawley rats | Collagenase-induced tendinopathy model | Local injection | 2 µg/100 μl | Once a week for 4 weeks | To evaluate the therapeutic effect of Farrerol on tendinopathy. Results showed that Farrerol significantly reduced inflammatory cell infiltration, promoted tenogenesis, and improved tendon mechanical properties. Additionally, Farrerol alleviated tendinopathy by inhibiting iron accumulation and ferroptosis. | PMC9189353 |
Rats | Oral administration model | Oral | 20 mg/kg | Single dose, sampling time from 0.083 to 24 hours | To study the in vivo metabolism of Farrerol, 42 in vivo metabolites were identified | PMC6804004 |
C57BL/6J mice | S. aureus-induced pneumonia model | Intraperitoneal injection | 50 mg/kg | Every 12 hours for 96 hours | Evaluate the protective effects of Farrerol combined with cefepime in mice with S. aureus-induced pneumonia. Results showed that the combination therapy significantly improved survival rates, reduced bacterial load in the lungs, and ameliorated tissue damage. | PMC11963547 |
Tags: Farrerol | Rhododendron | antioxidative | anti-inflammatory | anti-tumor | neuroprotective | hepatoprotective | 24211-30-1
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