Arjunolic acid

Arjunolic acid is an orally active, multifunctional bioactive compound. Arjunolic acid exhibits free radical scavenging activity, as well as fungal and bacterial activities. Arjunolic acid induces apoptosis (Apoptosis) in various cancer cells. Arjunolic acid protects hepatocytes against induced oxidative stress and apoptosis by reducing reactive oxygen species and inhibiting NF-κB activation. Arjunolic acid regulates pancreatic dysfunction in type 2 diabetic rats by blocking the activation of the TLR-4/MyD88 and canonical Wnt pathways. Arjunolic acid inhibits neuroinflammation and ameliorates depressive behaviors via the SIRT1/AMPK/Notch1 signaling pathway in microglia. Arjunolic acid improves Crohn's disease-like colitis by restoring gut microbiota composition and inhibiting TLR4 signaling. Arjunolic acid suppresses osteosarcoma progression by inhibiting Wnt3a-mediated M2 polarization of macrophages. Arjunolic acid ameliorates diabetic retinopathy via the autophagy pathway regulated by AMPK/mTOR/HO-1. Arjunolic acid is applicable to research related to type 2 diabetes, organ toxicity, depression, Crohn's disease, osteosarcoma, diabetic retinopathy, and testicular dysfunction^{[1][2][3][4][5][6][7]}. In Vitro:Arjunolic acid acts as a free radical scavenger in cell-free systems by scavenging superoxide radicals, hydroxyl radicals, hydrogen peroxide, and nitric oxide radicals^[2].
Arjunolic acid (0.5-30 μg/spot) inhibits the growth of *Bacillus subtilis*, *Escherichia coli* and *Shigella sonnei* in an in vitro spot assay^[2].
Arjunolic acid (20 μg/mL) inhibits the growth of *Cryptococcus neoformans* with an IC₅₀ of 20 μg/mL in in vitro antifungal assays^[2].
Arjunolic acid induces 66% cell death in Dalton cells and 70% cell death in Ehrlich cells via membrane damage^[2].
Arjunolic acid inhibits 12-O-tetradecanoylphorbol-13-acetate-induced Epstein-Barr virus-EA activation in Raji cells^[2].
Arjunolic acid (200 μM) protects mouse hepatocytes against cadmium-induced oxidative stress and apoptotic death by reducing reactive oxygen species, inhibiting NF-κB activation, and blocking both endogenous and exogenous apoptotic signaling pathways; it also prevents sodium fluoride-induced oxidative stress and necrotic death in mouse hepatocytes^[2].
Arjunolic acid (5-20 μM; 1 h) promotes the polarization of LPS (HY-D1056)-stimulated BV2 cells from the pro-inflammatory M1 phenotype to the anti-inflammatory M2 phenotype, upregulates the expression and activity of SIRT1 in cells, activates AMPK and inhibits the expression of Notch1^[3].
Arjunolic acid (20-200 μM; 2-24 h) directly binds to and stabilizes the SIRT1 protein in BV2 mouse microglial cell lysates^[3].
Arjunolic acid (5-40 μM; 48 h) protects LPS-induced colonic organoids from wild-type mice by reducing epithelial cell apoptosis and enhancing organoid viability^[4].
Arjunolic acid (1-100 μg/mL; 24 h) reduces the viability of Saos-2 and U-2OS osteosarcoma cells in a concentration-dependent manner^[5].
M2/M0 macrophages pretreated with arjunolic acid (50 μg/mL; 24 h pre-treatment of M2/M0 macrophages) inhibit the proliferation, migration and invasion of Saos-2 and U-2OS osteosarcoma cells, induce G1-phase cell cycle arrest, and promote apoptosis of these cells^[5].
Arjunolic acid (50 μg/mL) promotes the polarization of M0 macrophages toward the pro-inflammatory M1 phenotype^[5].
Arjunolic acid (50 μg/mL; 24 h) inhibits osteosarcoma cell-induced polarization of M0 macrophages toward the M2 phenotype and promotes their polarization toward the M1 phenotype^[5].
Arjunolic acid (50 μg/mL; 24 h) inhibits Wnt3a-mediated polarization of M0 macrophages toward the M2 phenotype and promotes their polarization toward the M1 phenotype^[5].
Arjunolic acid (5-10 μM; 24 h, co-treated with H₂O₂) significantly enhances the viability of ARPE-19 cells damaged by H₂O₂^[6].
Arjunolic acid (5-10 μM; 24 h, co-treated with H₂O₂) dose-dependently reduces H₂O₂-induced early and total apoptosis levels in ARPE-19 cells, and restores the expression of apoptosis-related proteins to normal levels^[6].
Arjunolic acid (5-10 μM; 24 h, co-treated with H₂O₂) alleviates oxidative stress in ARPE-19 cells by reducing reactive oxygen species (ROS) and malondialdehyde (MDA) levels, increasing superoxide dismutase (SOD) levels, and upregulating heme oxygenase-1 (HO-1) at the dose of 10 μM^[6].
Arjunolic acid (5-10 μM; 24 h, co-treated with H₂O₂) inhibits H₂O₂-induced autophagy in ARPE-19 cells via activation of the AMPK/mTOR pathway^[6]. In Vivo:Arjunolic acid (25-50 mg/kg; p.o.; daily; 28 days) improves pancreatic tissue structure in type 2 diabetic rats induced by Streptozotocin (HY-13753)-Nicotinamide (HY-B0150), downregulates the inflammatory (TLR-4/MyD88/NF-κB) pathway and the canonical Wnt/β-catenin signaling pathway, and restores insulin signaling markers^[1].
Arjunolic acid (80 mg/kg; p.o.; single dose) provides complete pre-treatment protection against Acetaminophen (HY-66005)-induced hepatic necrosis, and also offers significant post-treatment protection even when administered 8 h later^[2].
Arjunolic acid (50 mg/kg; two doses) exerts a protective effect against Acetaminophen-induced renal injury by maintaining antioxidant defense capacity, reducing the production of inflammatory mediators, and blocking the caspase-dependent cell death pathway^[2].
Arjunolic acid (25 mg/kg; once every 2 days; 3 doses) protects against Doxorubicin (HY-15142A)-induced cardiomyocyte apoptosis by scavenging reactive oxygen species and inhibiting the MAPK-mediated pro-apoptotic signaling pathway^[2].
Arjunolic acid antagonizes isoproterenol-induced myocardial necrosis, corrects abnormalities in cardiac biomarkers and electrocardiograms, and inhibits platelet aggregation and coagulation function^[2].
Arjunolic acid (20 mg/kg; daily; 4 days) inhibits sodium arsenite-induced hepatic oxidative damage and necrotic liver injury by maintaining the antioxidant defense system^[2].
Arjunolic acid exerts a protective effect against Streptozotocin-induced diabetic cardiomyopathy by reducing hyperglycemia and hyperlipidemia, alleviating vascular inflammation, inhibiting pro-apoptotic signaling pathways, and preserving myocardial mitochondrial function^[2].
Arjunolic acid (10-100 mg/kg; single dose) exerts dose-dependent anti-inflammatory activity. At a dose of 100 mg/kg, it inhibits carrageenan-induced paw edema in rats by 80.8% (accompanied by gastrointestinal toxicity), while at 10 mg/kg, the inhibition rate is 37.6% (no toxicity)^[2].
Arjunolic acid (10 mg/kg; single dose) exhibits antinociceptive activity and reduces acetic acid-induced abdominal constriction in mice by 30.3%^[2].
Arjunolic acid inhibits arachidonic acid (HY-109590)-induced ear edema in mice with an inhibition rate of 55.5%, indicating that it possesses activity targeting cyclooxygenase-mediated arachidonic acid metabolism^[2].
Arjunolic acid (50-100 mg/kg; single dose) exerts dose-dependent mast cell-stabilizing activity, reducing compound 48/80-induced rat mast cell degranulation to 42% at a dose of 50 mg/kg and to 33% at 100 mg/kg^[2].
Arjunolic acid (50-100 mg/kg; single dose) exhibits dose-dependent anti-asthmatic activity. At the dose of 100 mg/kg, it protects guinea pigs against histamine-induced bronchospasm with a maximum protection rate of 64%, and against acetylcholine-induced bronchospasm with a maximum protection rate of 51%^[2].
Arjunolic acid (1% topical ointment) promotes skin wound healing in rats and achieves complete epithelialization on day 20^[2].
Arjunolic acid (10-40 mg/kg; i.g.; daily; 7 days) significantly ameliorates LPS-induced depressive-like behaviors in male C57BL/6 mice by promoting M2 polarization of microglia, increasing BDNF and 5-HT levels in the hippocampus, and activating the SIRT1/AMPK/Notch1 signaling pathway^[3].
Arjunolic acid (15-60 mg/kg; p.o.; daily; 28 days) alleviates spontaneous Crohn's disease-like colitis in Il-10^-/- mice by improving intestinal barrier function, inhibiting intestinal epithelial cell apoptosis (via downregulating the TLR4/MyD88 pathway), and restoring the composition of beneficial intestinal flora and the production of short-chain fatty acids^[4].
Arjunolic acid (100 mg/kg; p.o.; once daily; 21 days) inhibits the progression and metastasis of osteosarcoma in nude mice by downregulating Wnt3a, reducing tumor proliferation, promoting tumor cell apoptosis, and shifting the polarization of tumor-associated macrophages from the pro-tumor M2 phenotype to the anti-tumor M1 phenotype^[5].
Oral administration of arjunolic acid (10-30 mg/kg; p.o.; once daily for 10 weeks) improves Streptozotocin (HY-13753)-induced diabetic retinopathy in rats by reducing fasting blood glucose, increasing body weight, preserving retinal structure, inhibiting retinal cell apoptosis and inflammatory responses, upregulating HO-1, and activating the AMPK/mTOR-regulated autophagy pathway^[6].
Arjunolic acid (1.0-2.0 mg/kg; p.o.; daily; 4 weeks) reverses Fluoxetine (HY-B0102)-induced testicular dysfunction in male Wistar rats by inhibiting oxidative inflammatory stress and apoptosis, with the anti-inflammatory efficacy of the 2.0 mg/kg oral dose being superior to that of the 1.0 mg/kg dose^[7].