Yunnan University of Chinese Medicine

Coumaronochromones, characterized by a distinctive benzofuro[2,3- b ]chromenone core, constitute a rare subclass of isoflavonoids. Biosynthetically, they are proposed to originate from carbohydrate metabolism and the phenylpropanoid pathway like other isoflavones. To date, 92 natural coumaronochromones have been isolated and characterized from nearly 28 species across 24 genera within 7 families (including one fungal source). These compounds are predominantly distributed in the Fabaceae family, which accounts for over half (64%) of all known derivatives. Notably, approximately 20% of coumaronochromones are derived from the genus Euchresta (Fabaceae). The unique scaffold of coumaronochromones confers a broad spectrum of notable pharmacological activities, including anti-inflammatory, antibacterial, insecticidal, cytotoxic, and immunomodulatory effects, highlighting their potential as valuable natural leads for pharmaceutical and agrochemical development. This review comprehensively summarizes recent advances in the chemistry and biology of coumaronochromones, providing a detailed account of their natural occurrence, documented biological activities, and chemical syntheses. Graphical Abstract

New dearomatized isoprenylated acylphloroglucinols hyperprzewones A ( 1 ) and B ( 2 ) were isolated and characterized from the dried aerial parts of Hypericum przewalskii . The structures of these compounds were confirmed by extensive spectroscopic experiments. A facile synthetic route to 1 and 2 was developed via Friedel-Crafts acylation, alkylation, dearomatization, and oxidative [4 + 2] cyclization, giving a 17% overall yield. Moreover, the synthetic derivative 8 exhibited moderate inhibition on T-type calcium channels Ca v 3.2. Graphical Abstract

Ulcerative colitis (UC) is a kind of hard to cure chronic inflammatory disease. In present work, a series of new costunolide derivatives bearing indole/indoline have been prepared, and anti-inflammatory activities and mechanism have been tested. The results indicated that costunolide derivatives displayed good inhibition of NO generation. The in vivo studies showed that 4c exerted good protective effects in DSS-induced UC mice model by inhibiting the expression of IL-17 A and IL-17F, reducing the infiltration of immune cells, and inhibiting the phosphorylation of JAK2-STAT3 tyrosine residues. Therefore, new costunolide derivatives could be considered as potential JAK2/STAT3 pathway modulator for treatment of UC.