Arbutin is a competitive inhibitor of tyrosinase in melanocytes, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents[3]. Arbutin inhibited the tyrosinase activity of cultured human melanocytes at noncytotoxic concentrations. It did not affect the expression of tyrosinase mRNA[4]. Arbutin (0.3-5.4 mM; 24 hours, 48 hours, 72 hours; B16 murine melanoma cells) inhibites the viability of B16 murine melanoma cells in a time-and dose-dependent manner. Arbutin (1.4-5.4 mM; 24 hours) increases the apoptosis rate of B16 murine melanoma cell of treatment at a dose of 5.4 mM[5]. Arbutin inhibits OS (osteosarcoma) cell proliferation, migration and invasion via miR-338-3p/MTHFD1L and by inactivating the AKT(phosphorylated-protein kinase B)/mTOR (phosphorylated-mammalian target of rapamycin) pathway[6].
Arbutin/熊果苷 细胞实验
Cell Line
Concentration
Treated Time
Description
References
IEC-6 cells
500 µM
12 hours
To evaluate the effect of Arbutin on LPS-induced apoptosis in IEC-6 cells, results showed that Arbutin significantly inhibited LPS-induced apoptosis.
Front Pharmacol. 2021 Sep 14;12:683818.
3T3-L1 cells
75 µM
24 hours
Arbutin reduced intracellular TG levels in 3T3-L1 cells without affecting cell viability.
Redox Biol. 2023 Dec;68:102963.
HepG2 cells
75 µM
24 hours
Arbutin reduced intracellular lipid deposition in HepG2 cells, decreased intracellular TG and TC levels, and reduced lipid droplet accumulation. Additionally, Arbutin inhibited the expression of lipid synthesis genes and promoted the expression of genes involved in lipid catabolism and transport.
Redox Biol. 2023 Dec;68:102963.
L-02 cells
25, 50, 100, 200 µM
24 hours
To evaluate the cytotoxicity of arbutin on hepatocytes, results showed that arbutin at concentrations of 0–200μM for 24 hours had no significant proliferative inhibition on L-02 cells.
Front Cell Dev Biol. 2021 Dec 2;9:758632.
IEC-6 cells
10-800 µM
24 hours
To evaluate the effect of Arbutin on cell viability, results showed that Arbutin had no significant effect on IEC-6 cell viability at concentrations ranging from 10-800 μM.
Front Pharmacol. 2021 Sep 14;12:683818.
PDPCs cells
0.2 mM
72 hours
Evaluate the protective effect of Arbutin on PDPCs cells under oxidative stress, results showed Arbutin restored cell viability and promoted the expression of differentiation markers
Antioxidants (Basel). 2020 Jul 2;9(7):579.
Saos-2 cells
0.2 mM
72 hours
Evaluate the protective effect of Arbutin on Saos-2 cells under oxidative stress, results showed Arbutin restored cell viability
Antioxidants (Basel). 2020 Jul 2;9(7):579.
C57BL/6 mice chondrocytes
0.5 mg/mL
GM-Lipo@ARB effectively reduced the inflammatory response in IL-1β-treated arthritic chondrocytes and regulated cartilage ECM homeostasis by inhibiting NF-κB signaling and activating the Nrf2 pathway.
Mater Today Bio. 2022 Jul 19;16:100370.
Arbutin/熊果苷 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
Normal mice and antibiotic-treated mice
Oral
0.1, 0.2, 0.4, 1 mg/ml
3 weeks
To investigate the effects of Arbutin on gut development and serum lipids, results showed that Arbutin promoted gut development (e.g., villus length, villus areas) and reduced serum lipids (e.g., total cholesterol, high-density lipoprotein).
Front Nutr. 2022 Sep 9;9:948573
C57BL/6 mice
High-fat diet-induced obesity model
Oral
1 g/kg
Continued for 10 weeks
Arbutin significantly alleviated high-fat diet-induced obesity and hepatic lipid deposition in mice, reduced liver TG and TC levels, and improved glucose metabolism and insulin sensitivity. Additionally, Arbutin reduced oxidative stress and iron overload, and inhibited ferroptosis.
Redox Biol. 2023 Dec;68:102963.
C57BL/6 mice
ANIT-induced cholestatic liver injury model
Intraperitoneal injection
10, 20, 40 mg/kg
Once daily for one week
To evaluate the protective effect of arbutin on ANIT-induced cholestatic liver injury, results showed that arbutin significantly reduced serum levels of ALT, AST, TBIL, γ-GT, TBA, and ALP, and improved liver pathological changes.
Front Cell Dev Biol. 2021 Dec 2;9:758632.
Lewis rats
Lewis rats
Oral
200 mg/kg
Daily administration for 14 or 28 days
To evaluate the effects of strawberry tree water leaf extract (STE) and arbutin on biochemical markers and DNA integrity in the brain tissue of Lewis rats. Results indicated high biocompatibility of both substances with rat brain tissue, with no significant harmful disturbances in oxidative/antioxidative status or DNA integrity.
Toxics. 2024 Aug 16;12(8):595
C57BL/6 mice
Destabilization of the medial meniscus (DMM)-induced osteoarthritis model
Intra-articular injection
25 mg/kg
Once every two weeks for eight weeks
Intra-articular use of GM-Lipo@ARB can effectively reduce inflammation and oxidative stress in the articular cartilage and thus, attenuating OA progression in a Mice model.
Mater Today Bio. 2022 Jul 19;16:100370.
Rats
Lead acetate-induced testicular injury model
Oral
250 mg/kg
Once daily for 10 days
Arbutin ameliorates Pb-evoked testicular damage by stimulating testicular antioxidants and the PK2/PKR2 pathway and inhibiting the JAK2/STAT3 and NLRP3/caspase-1 pro-inflammatory pathways. Intraperitoneal arbutin at a lower dose prompted a more pronounced mitigation of Pb-induced testicular dysfunction compared to oral administration.
Pharmaceuticals (Basel). 2024 Jul 8;17(7):909
C57BL/6 mice
DSS-induced colitis model
Gavage
50 and 100 mg/kg
Once daily for 7 consecutive days
To evaluate the effect of Arbutin on DSS-induced colitis symptoms, results showed that Arbutin significantly alleviated colitis symptoms, including body weight loss, increased disease activity index, and increased colon weight/length ratio.
Front Pharmacol. 2021 Sep 14;12:683818.
Swiss albino mice
MPTP-induced Parkinson’s disease model
Intraperitoneal injection
50 and 100 mg/kg
Once daily for 7 days
Arbutin significantly reduced lipid peroxidation, total nitrite levels, and inflammation in the substantia nigra and striatum of PD Mice models. In addition, arbutin decreased the activity of endogenous antioxidants, reduced the levels of dopamine, 3,4-dihydroxyphenylacetic acid, homovanillic acid, and γ-aminobutyric acid, and minimized neurodegeneration in the striatum. Arbutin also improved the abnormal performance of PD Mice models in the open field test, bar test, pole test, and rotarod test.
Neural Regen Res. 2021 Oct;16(10):2030-2040
BALB/c mice
DSS-induced ulcerative colitis model
Intragastric administration
50 mg/kg and 100 mg/kg
Once daily for 7 days
Arbutin ameliorated DSS-induced ulcerative colitis by eliciting anti-inflammatory effects and maintaining normal intestinal mucosal barrier function, the action mechanism of which could be associated with MAPK/ELK1 pathway.
Bioengineered. 2021 Dec;12(2):11707-11715
Rats
Lead acetate-induced testicular injury model
Intraperitoneal injection
75 mg/kg
Once daily for 10 days
Arbutin ameliorates Pb-evoked testicular damage by stimulating testicular antioxidants and the PK2/PKR2 pathway and inhibiting the JAK2/STAT3 and NLRP3/caspase-1 pro-inflammatory pathways. Intraperitoneal arbutin at a lower dose prompted a more pronounced mitigation of Pb-induced testicular dysfunction compared to oral administration.
Pharmaceuticals (Basel). 2024 Jul 8;17(7):909
HRM-2 hairless mice
UV-B-induced skin hyperpigmentation model
Topical application
0.5%
Twice daily for 25 days
To evaluate the ameliorative effect of BI2B on UV-B-induced skin hyperpigmentation
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