Bioactive chemical constituents from the root bark of Morus australis

• Published in: Bioorganic & medicinal chemistry letters 2017-01, Vol.27 (2), p.309-313
• Main Authors: Liao, Yu-Ren, Kuo, Ping-Chung, Tsai, Wei-Jern, Huang, Guan-Jhong, Lee, Kuo-Hsiung, Wu, Tian-Shung
• Format: Article
• Language: English
• Subjects: Adenosine Diphosphate - pharmacology; Animals; Anti-platelet aggregation; Arachidonic Acid - antagonists & inhibitors; Arachidonic Acid - pharmacology; Dose-Response Relationship, Drug; Flavonoids - chemistry; Flavonoids - isolation & purification; Flavonoids - pharmacology; Mice; Molecular Structure; Morus - chemistry; Morus australis; Nitric Oxide - antagonists & inhibitors; Nitric Oxide - biosynthesis; NO inhibitory activity; Plant Roots - chemistry; Platelet Activating Factor - antagonists & inhibitors; Platelet Activating Factor - pharmacology; Platelet Aggregation - drug effects; Pyranoflavonoid; Rabbits; RAW 264.7 Cells; Structure-Activity Relationship
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2016.11.046

[Display omitted] Two new pyranoflavonoids, morustralins A (1) and B (2), a new natural benzene derivative, one benzenoid (Z)-1-hydroxy-4-(2-nitroethenyl)benzene (3), and thirty known compounds were isolated and characterized from the root bark of Morus australis. The structures of the new compounds were established from spectroscopic and spectrometric analyses. Ten isolates (1–10) were examined for inhibitory effects on adenosine diphosphate (ADP)-, arachidonic acid (AA)-, and platelet-aggregating factor (PAF)-induced platelet aggregation. Among the tested compounds, compound 3 displayed the most significant inhibition of ADP- and AA-induced platelet aggregation with IC50 values of 9.76±5.54 and 9.81±2.7μM, respectively. In addition, eight purified compounds (3–10) were examined for inhibition of nitric oxide (NO) production in RAW 264.7 cells and six compounds (3–8) displayed significant inhibitory effects with IC50 values ranging from 2.1±0.3 to 6.3±0.6μM.