Myrtillin is a cationic anthocyanin compound that inhibits epidermal growth factor receptor (EGFR) with an IC50 value of 2.37µM[1]. Myrtillin exhibits oxygen radical absorbance capacity (ORAC), scavenging power of ABTS (EC50=20.66µM), and DPPH-free radical (EC50=60.37µM) and inhibitory activity of α-glucosidase (IC50=239.7µM)[2]. Myrtillin combines with the bacterial protein FtsZ, NAD+-dependent DNA ligase, and amidase through hydrogen bonds and hydrophobic interactions, interfering with bacterial metabolism, inhibiting the production of ROS, and alleviating the oxidative damage caused by bacterial pathogens to Caenorhabditis elegans[3]. Myrtillin has been widely used in tumor research to inhibit the proliferation of colorectal cancer cells and leukemia cells[4].
In vitro, Myrtillin treatment for 24 hours markedly reduced the viability of HCT 116 and HT-29 cells, with IC50 values of 395.9µg/ml and 329.1µg/ml, respectively[5]. The combination treatment of 50µM Myrtillin and 1.25µg/ml lipopolysaccharide (LPS) for 24 hours induced the proliferation of mesenchymal stem cells (MSCs), promoting the increase of IL-10 and TGF-β levels and the decrease of NF-κB expression[6]. Treatment with 200µM Myrtillin for 72h suppressed MDA-MB-231 migration by disrupting actin[7].
In vivo, Myrtillin administration via intraperitoneal injection at a dose of 20mg/kg/day for 3 days reduced neuronal damage and cerebral infarction, and restored regional cerebral blood flow in a neonatal mouse model of hypoxic-ischemic encephalopathy (HIE)[8]. Oral administration of Myrtillin at a dose of 20mg/kg/day for 12 weeks alleviated aortic lesions, oxidative stress, and inflammatory responses in a high-fat diet-induced rabbit model of atherosclerosis[9].
References:
[1] Mazewski C, Liang K, de Mejia E G. Comparison of the effect of chemical composition of anthocyanin-rich plant extracts on colon cancer cell proliferation and their potential mechanism of action using in vitro, in silico, and biochemical assays[J]. Food Chemistry, 2018, 242: 378-388.
[2] Zhu C, Lü H, Du L, et al. Five blueberry anthocyanins and their antioxidant, hypoglycemic, and hypolipidemic effects in vitro[J]. Frontiers in nutrition, 2023, 10: 1172982.
[3] Nas J S B. Myrtillin prolongs lifespan and enhances tolerance against pathogenic infections in Caenorhabditis elegans[J]. Journal of Preventive, Diagnostic and Treatment Strategies in Medicine, 2023, 2(3): 154-163.
[4] Iqbal S, Omara T, Kahwa I, et al. Anticancer potential of delphinidin and its derivatives: Therapeutic and mechanistic insights[J]. Medicinal Chemistry Research, 2024, 33(10): 1769-1786.
[5] Mazewski C, Kim M S, Gonzalez de Mejia E. Anthocyanins, delphinidin-3-O-glucoside and cyanidin-3-O-glucoside, inhibit immune checkpoints in human colorectal cancer cells in vitro and in silico[J]. Scientific reports, 2019, 9(1): 11560.
[6] Neves B R O, de Freitas S, Borelli P, et al. Delphinidin-3-O-glucoside in vitro suppresses NF-κB and changes the secretome of mesenchymal stem cells affecting macrophage activation[J]. Nutrition, 2023, 105: 111853.
[7] Viegas O, Faria M A, Sousa J B, et al. Delphinidin-3-O-glucoside inhibits angiogenesis via VEGFR2 downregulation and migration through actin disruption[J]. Journal of Functional Foods, 2019, 54: 393-402.
[8] Xu J, Hao P, Chen J, et al. Delphinidin-3-O-glucoside attenuates neonatal hypoxic-ischemic encephalopathy in a neonatal mouse model by reprogramming microglial polarization[J]. Frontiers in Pharmacology, 2026, 17: 1797078.
[9] Sun B, Li F, Zhang X, et al. Delphinidin-3-O-glucoside, an active compound of Hibiscus sabdariffa calyces, inhibits oxidative stress and inflammation in rabbits with atherosclerosis[J]. Pharmaceutical biology, 2022, 60(1): 247-254.