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.
Highlights
Publisher’s Note: MDPI stays neutralHedyotis diffusa Willd. (Rubiaceae) is a plant commonly used as folk medicine and distributed in southern provinces of China [1]
Further chromatography purification resulted in the characterization of twenty-six anthraquinones (1–26), eight iridoids glycosides (27–34), two phenolics (35–36), two triterpenoids (37–38), two steroids (39–40), and one amide (41)
Seven anthraquinones, diffusaquinone A-H (1–7), were reported for the first time from natural sources, and their structures were established on the basis of 1D and 2D NMR and mass spectrometric analyses
Summary
Publisher’s Note: MDPI stays neutralHedyotis diffusa Willd. (Rubiaceae) is a plant commonly used as folk medicine and distributed in southern provinces of China [1]. The herb of H. diffusa has the effects of clearing heat and detoxifying, relieving pain and dispelling masses, diuresis, and dehumidification [2]. It is mainly used for treating lung heat, asthma and cough, gastroenteritis, appendicitis, urinary system infection, throat swelling and pain, intestinal carbuncle sore, dysentery, malignant tumors, etc. Previous studies indicated that H. diffusa exhibits various pharmacological activities, including antioxidant, antiangiogenic, antiinflammatory, hepatoprotective, apoptosis, and anticancer activities [3,8,9,10,11,12,13,14,15,16]. Methylanthraquinones from H. diffusa induced cell apoptosis by changing Fas and Fas
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