Phenolic Compounds from Carissa spinarum Are Characterized by Their Antioxidant, Anti-Inflammatory and Hepatoprotective Activities

Abstract

Carissa spinarum has been traditionally used for the treatment of various diseases due to its different pharmacological activities. However, the active compounds responsible for its potentially specific activities have rarely been explored. To this end, the ethyl acetate (EA) fraction was screened out and selected for further phytochemical isolation because of its promising activities in preliminary 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP) and COX-2 inhibition assays. As a result, 10 compounds (1−10), including a new one (5), were isolated, with eight of these being identified as phenolic compounds, as expected. Compound 9 possessed an IC50 value of 16.5 ± 1.2 µM, which was lower than that of positive control (vitamin C, 25.5 ± 0.3 µM) in the DPPH assay, and compounds 2, 6, 7 and 9 showed better total antioxidant capacity than vitamin C in the FRAP assay. Meanwhile, compounds 1−6 and 9 also had IC50 values of less than 1.0 µM, which was even better than the positive control indomethacin in the COX-2 inhibition assay. In this context, compounds 2 and 9 were further evaluated to exhibit clear hepatoprotective activities by improving the L02 cell viability and reducing ROS production using a H2O2-induced L02 cell injury model. This study provides initial evidence revealing the most potent phenolic compounds from the root bark of C. spinarum responsible for its antioxidant, anti-inflammatory and hepatoprotective activities.

Lignans as Pharmacological Agents in Disorders Related to Oxidative Stress and Inflammation: Chemical Synthesis Approaches and Biological Activities

“…exerted protective effects against oxidative stress-induced apoptosis in human umbilical vein endothelial cells (HUVECs) via a mechanism involving the upregulation of phosphatidylinositol 3-kinase (PI3K) and phosphorylated Akt, which lead to upregulated levels of phosphorylated Bcl-2-associated agonist of cell death (p-Bad) [ 31 ]. (+)-Isolariciresinol-3a-O-β-D-glucopyranoside extracted from Carissa spinarum exhibited moderate DPPH radical scavenging activity and high ferric reducing capacity (stronger than vitamin C), exerted significant hepatoprotective effects against H 2 O 2 -induced L02 cell injury by reducing ROS production, and also possessed a much better COX-2 inhibition activity compared with indomethacin [ 30 ]. (–)-Isolariciresinol-5-methoxy-9-β-D-xylopyranosyl showed the ability to scavenge DPPH radicals that were 1.5 times weaker than well-known antioxidant quercetin [ 29 ].…”

Recent development on COX-2 inhibitors as promising anti-inflammatory agents: The past 10 years

“…Liu et al. 73 recently discovered two novel anti-inflammatory compounds 102 and 103 from Carissa spinarum . Compounds 102 and 103 were identified and showed good COX-2 inhibition by the COX-2 inhibition screening method (EIA) and the activity of compound 102 (IC 50 value = 0.3 μmol/L) was comparable to indomethacin (IC 50 = 1.1 μmol/L).…”

Flavonoids from Selaginella doederleinii Hieron and Their Antioxidant and Antiproliferative Activities

“…The DPPH assay of S. doederleinii ethanol extract and four fractions was assessed as described in [35,36], with some minor modifications. Firstly, the DPPH solution was prepared with methanol at a concentration of 0.1 mM.…”