Chemical Constituents of Hedyotis diffusa and Their Anti-Inflammatory Bioactivities

Abstract

Seven new anthraquinones with rare 2-isopropyldihydrofuran (1–3) and 2,2-dimethylpyrano (4–7) moieties together with thirty-four known compounds were isolated from the extracts of whole Hedyotis diffusa plants. Their structures were elucidated and established by various spectroscopic and spectrometric analytical methods. Among these isolates, selected compounds were examined for their anti-inflammatory activity. The results showed that rare substituted anthraquinones displayed potent inhibitory activity with IC50 values ranging from 0.15 ± 0.01 to 5.52 ± 1.59 µM on the N-formyl-methionyl-leucyl-phenylalanine/cytochalasin B (fMLP/CB)-induced superoxide anion generation and elastase release cellular models. Meanwhile, the proposed drug target of the active anthraquinone was studied by computer modeling. The binding affinity between the anti-inflammatory anthraquinone and elastase was evaluated by molecular docking. These results provided the scientific insight into the medicinal values of Hedyotis diffusa and vision of development as lead compounds.

Lupus Recipe inhibits cGVHD‐induced lupus nephritis in mice and promote renal LC3‐associated autophagy

“…H. diffusa Willd has the function of heat-clearing and detoxifying, diuresis and dehumidification, and antiinflammation. 20,21 Recent evidence showed that extraction solution from H. diffusa Willd had suppressive effects on inflammation and the proliferation of T lymphocytes by regulating the STAT3 signaling pathway, thus ameliorating renal injury in MRL/lpr mice. 22 Another study proved that H. diffusa Willd containing a Chinese Herbal compound could suppress the activation of peritoneal macrophages via modulating the IRAK1-NF-κB signaling pathway in MRL/lpr mice.…”

“…S. miltiorrhiza Bunge and leonurus japonicus Houtt serve as the associates and have the effect of activating blood circulation and removing stasis. H. diffusa Willd has the function of heat‐clearing and detoxifying, diuresis and dehumidification, and anti‐inflammation 20,21 . Recent evidence showed that extraction solution from H. diffusa Willd had suppressive effects on inflammation and the proliferation of T lymphocytes by regulating the STAT3 signaling pathway, thus ameliorating renal injury in MRL/lpr mice 22 .…”

Targeting formyl peptide receptor 1 with anteiso‐C13‐surfactin for neutrophil‐dominant acute respiratory distress syndrome

“…Extracellular generation of superoxide anion from neutrophils was evaluated using the ferricytochrome c reduction method, described previously (Hung et al, 2022). Neutrophils were preincubated with ferricytochrome c and treated with IA-1 or DMSO (control) for 5 min, followed by stimulation with chemoattractants, with or without cytochalasin B. Absorbance change was monitored at 550 nm using a spectrophotometer at 37 C.…”

Total flavonoids of Oldenlandia diffusa (Willd.) Roxb. suppresses the growth of hepatocellular carcinoma through endoplasmic reticulum stress-mediated autophagy and apoptosis

“…Oldenlandia diffusa (Willd.) Roxb is a plant commonly used in Chinese Tradition medicine and is widely distributed in the southern provinces of China ( Hung et al, 2022 ). Hedyotis diffusa Willd is a kind of Chinese herbal medicine commonly used in clinic, which has anti-inflammatory, antioxidant and anti-proliferation effects ( Luo et al, 2011 ; Li et al, 2020a ; Hung et al, 2022 ).…”

“…Roxb is a plant commonly used in Chinese Tradition medicine and is widely distributed in the southern provinces of China ( Hung et al, 2022 ). Hedyotis diffusa Willd is a kind of Chinese herbal medicine commonly used in clinic, which has anti-inflammatory, antioxidant and anti-proliferation effects ( Luo et al, 2011 ; Li et al, 2020a ; Hung et al, 2022 ). At present, more than 180 compounds have been found from Hedyotis diffusa Willd , including iridoid terpenes, flavonoids, anthraquinones, phenols and other substances ( Chen et al, 2016a ).…”