Alkaloids from Tetrastigma hemsleyanum and Their Anti-Inflammatory Effects on LPS-Induced RAW264.7 Cells

Abstract

Alkaloids 1–10 were isolated from the aerial parts of Tetrastigma hemsleyanum (APTH) and obtained from species of the genus Tetrastigma for the first time. The chemical structures of the isolated compounds were identified by NMR, UV, and MS analyses. Their anti-inflammatory activities were investigated by measuring nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW264.7 macrophages. Among all the isolates, compounds 6, 7 and 10 showed potent inhibitory activity against LPS-stimulated NO production in RAW264.7 cells (IC50: 31.9, 25.2 and 6.3 μM, respectively). Furthermore, APTH and S-(−)-trolline (10) inhibited induction of inflammatory cytokines or mediators such as interleukin-1β (IL-1β) and inducible nitric oxide synthase (iNOS) via suppression of nuclear factor κB (NF-κB) translocation into the nucleus. In addition, 10 suppressed extracellular signal-regulated protein kinase 1/2 (ERK1/2) mitogen-activated protein kinase (MAPK) phosphorylation in a dose-dependent manner. These results conclusively demonstrated that compound 10 displays anti-inflammatory activity via suppression of NF-κB activation and the ERK-MAPK signaling pathway in LPS-stimulated RAW264.7 cells.

Antimycobacterial and Nitric Oxide Production Inhibitory Activities of Triterpenes and Alkaloids from Psychotria nuda (Cham. & Schltdl.) Wawra

“…Plants or their extracts belonging to the genus Psychotria have been used in folk medicine in the treatment of inflammation [45]. Indole alkaloids, the main chemosystematic markers of the genus Psychotria [13], also exhibited anti-inflammatory activities in vitro [46] and in vivo [47]. These data suggest that both extracts of these species and indole alkaloids could serve as models for the development of new anti-inflammatory drugs.…”

The Phytochemistry, Pharmacology, and Quality Control of Tetrastigma hemsleyanum Diels & Gilg in China: A Review

“…Separation of the EtOAc-soluble fraction of the methanolic extract of the aerial parts of TDG result in the isolation of ten alkaloids. Then, Wang et al. (2018a) also discover that with the spectral data in the current literature, and the alkaloids are identified as indole (100), indole-3-carboxylic acid (101), indole-3-propanoic acid (102), 5-hydroxy-indole-3-carboxaldehyde (103), 5-hydroxy-indole-3-carboxylic acid (104), 6-hydroxy-3,4-dihydro-1-oxo-β-carboline (105), hippophamide (106), 4-hydroxycinnamide (107), pyrrole-3-propanoic acid (108) and S-(-)-trolline (109).…”

“…(2017) discover that the aerial part of TDG has antipyretic, analgesic, and anti-inflammatory effects, and the efficacy increases with the increase of drug dosage, but the molecular mechanism by which this activity happens should be further studied. Wang et al. (2018a) isolate alkaloids from the aerial part of TDG for the first time, three of which have good anti-inflammatory activity.…”

A comprehensive review on traditional uses, chemical compositions, pharmacology properties and toxicology of Tetrastigma hemsleyanum

“…Numerous reports have demonstrated that the biological activities of T. hemsleyanum are attributed to its many chemical components ( Fu et al, 2019 ). Wang has reported isolated alkaloids from the aerial parts of T. hemsleyanum ( Wang et al, 2018 ). Ru extracted a novel polysaccharide TDGP-3 from T. hemsleyanum with a molecular weight of 3.31 × 10 5 Da by enzymolysis-ultrasonic assisted extraction method ( Ru et al, 2019a , Ru et al, 2019b ).…”