Moracin O is a hypoxia-inducible factor (HIF-1) inhibitor isolated from Morus alba Linn., exhibiting significant anti-inflammatory and antioxidant activities[1,2]. Moracin O reduces reactive oxygen species (ROS) generation induced by oxygen-glucose deprivation (OGD)[3] and is commonly used in studies of neuroprotection, oxidative stress, and the regulation of related signaling pathways[4,5].
In vitro, treatment of 4T1-NF-κB reporter cells with Moracin O (3, 10, 100nM) for 24h dose-dependently inhibited NF-κB activity. Pretreatment of HaCaT human keratinocytes with Moracin O (10μM) for 1h, followed by co-incubation with tumor necrosis factor-related apoptosis-inducing ligand (TRAIL, 20ng/mL) for 24h, significantly attenuated TRAIL-induced cell damage and improved cell viability[6]. Pretreatment of SK-N-SH human neuroblastoma cells with Moracin O (10μM) for 4h, followed by exposure to 30mM glutamate for 4h, significantly inhibited glutamate-induced cell death[7].
In vivo, Institute of Cancer Research (ICR) mice were pretreated with Moracin O (80mg/kg, i.p.) 30min prior to the injection of 0.7% acetic acid to induce a pain model. Moracin O significantly inhibited acetic acid-induced writhing responses, reducing the mean number of writhes from 17 ± 6 in the control group to 0 ± 1, with an inhibition rate of 98%[7].
References:
[1] NAIK R, HARMALKAR D S, XU X, et al. Bioactive benzofuran derivatives: Moracins A-Z in medicinal chemistry[J]. European Journal of Medicinal Chemistry, 2015, 90: 379-393.
[2] DAT N T, JIN X, LEE K, et al. Hypoxia-inducible factor-1 inhibitory benzofurans and chalcone-derived Diels–Alder adducts from Morus species[J]. Journal of Natural Products, 2009, 72(1): 39-43.
[3] LEE H J, LYU D H, KOO U, et al. Inhibitory effect of 2-arylbenzofurans from the Mori Cortex Radicis (Moraceae) on oxygen glucose deprivation (OGD)-induced cell death of SH-SY5Y cells[J]. Archives of Pharmacal Research, 2011, 34(8): 1373-1380.
[4] LEE J H, KO H J, WOO E R, et al. Moracin M inhibits airway inflammation by interrupting the JNK/c-Jun and NF-κB pathways in vitro and in vivo[J]. European Journal of Pharmacology, 2016, 783: 64-72.
[5] ZOOFISHAN Z, KÚSZ N, CSORBA A, et al. Antispasmodic activity of prenylated phenolic compounds from the root bark of Morus nigra[J]. Molecules, 2019, 24(13): 2497.
[6] HARDIANTI B, UMEYAMA L, LI F, et al. Anti-inflammatory compounds moracin O and P from Morus alba Linn. (Sohakuhi) target the NF-κB pathway[J]. Molecular Medicine Reports, 2020, 22(6): 5385-5391.
[7] WANG Y N, LIU M F, HOU W Z, et al. Bioactive benzofuran derivatives from Cortex Mori Radicis, and their neuroprotective and analgesic activities mediated by mGluR1[J]. Molecules, 2017, 22(2): 236.