Abstract
Acanthopanax sessiliflorus (Araliaceae) have been reported to exhibit many pharmacological activities. Our preliminary study suggested that A. sessiliflorus fruits include many bioactive 3,4-seco-triterpenoids. A. sessiliflorus fruits were extracted in aqueous EtOH and fractionated into EtOAc, n-BuOH, and H2O fractions. Repeated column chromatographies for the organic fractions led to the isolation of 3,4-seco-triterpenoid glycosides, including new compounds. Ultra-high-performance liquid chromatography (UPLC) mass spectrometry (MS) systems were used for quantitation and quantification. BV2 and RAW264.7 cells were induced by LPS, and the levels of pro-inflammatory cytokines and mediators and their underlying mechanisms were measured by ELISA and Western blotting. NMR, IR, and HR-MS analyses revealed the chemical structures of the nine noble 3,4-seco-triterpenoid glycosides, acanthosessilioside G–O, and two known ones. The amounts of the compounds were 0.01–2.806 mg/g, respectively. Acanthosessilioside K, L, and M were the most effective in inhibiting NO, PGE2, TNF-α, IL-1β, and IL-6 production and reducing iNOS and COX-2 expression. In addition, it had inhibitory effects on the LPS-induced p38 and ERK MAPK phosphorylation in both BV2 and RAW264.7 cells. Nine noble 3,4-seco-triterpenoid glycosides were isolated from A. sessiliflorus fruits, and acanthosessilioside K, L, and M showed high anti-inflammatory and anti-neuroinflammatory effects.
Highlights
Oxidative stress in the human body is caused by excess reactive oxygen or nitrogen species (ROS or RNS), including superoxide (O2 − ), hydrogen peroxide (H2 O2 ), and nitric oxide (NO), and it triggers certain types of apoptotic cell death, such as neuronal cell death and macrophage immune injury
If the microglia overwhelmed by stimulation such as lipopolysaccharide (LPS), interferon-gamma (IFN-α), or tumor necrosis factoralpha (TNF-α), NO, excessive cytokines, and ROS are secreted, causing neurotoxicity and destroying brain tissue, causing degenerative brain diseases such as Alzheimer’s, Parkinson’s disease, and Croyfeldt–Jakob disease [4,5,6]
A 70% ethanolic extract of dried A. sessiliflorus fruits was suspended in H2 O and extracted successively with EtOAc and n-BuOH
Summary
Oxidative stress in the human body is caused by excess reactive oxygen or nitrogen species (ROS or RNS), including superoxide (O2 − ), hydrogen peroxide (H2 O2 ), and nitric oxide (NO), and it triggers certain types of apoptotic cell death, such as neuronal cell death and macrophage immune injury. If ROS or RNS are not appropriately removed, oxidative stress can cause the lipid peroxidation of the cellular membrane, leading to inordinate cell death [1]. The investigation of the cause and drug development for degenerative brain disease is rapidly progressing. The microglia in the central nerve system (CNS) plays an important role in the immunity, degeneration, and inflammation of the CNS, so it can prevent degenerative brain diseases by regulating the inflammatory. Antioxidants 2021, 10, 1334 response that occurs in microglials [3]. To prevent brain damage caused by ROS, RNS (NO), and excessive cytokines, it is useful to take anti-inflammatory and anti-neuroinflammatory supplements. There is a need to develop alternative natural anti-inflammatory drugs without side effects
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