Inhibition of human neutrophil elastase by labdane diterpenes from the fruiting bodies of Ramaria formosa

• Published in: Bioscience, biotechnology, and biochemistry Vol. 79; no. 12; pp. 1921 - 1925
• Main Authors: Lee, Ik-Soo, Kim, Kwan-Chul, Yoo, Ick-Dong, Ha, Byung-Jo
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 02.12.2015
• Subjects: Basidiomycota - chemistry; Diterpenes - chemistry; Diterpenes - isolation & purification; Diterpenes - pharmacology; Fruiting Bodies, Fungal - chemistry; Gomphaceae; human neutrophil elastase; Humans; labdane diterpene; Leukocyte Elastase - antagonists & inhibitors; Protease Inhibitors - chemistry; Protease Inhibitors - isolation & purification; Protease Inhibitors - pharmacology; Ramaria formosa; labdane diterpene; Gomphaceae; Ramaria formosa; human neutrophil elastase
• ISSN: 0916-8451; 1347-6947
• DOI: 10.1080/09168451.2015.1065168

Two new labdane diterpenes (1 and 2) were isolated from the fruiting bodies of Ramaria formosa. The structures of these compounds were established by extensive spectroscopic studies and chemical evidence. The inhibitory activity of compounds 1 and 2 against human neutrophil elastase (HNE) was evaluated in vitro. Compounds 1 and 2 inhibited HNE activity moderately. The IC 50 values for compounds 1 and 2 were 36.4 ± 1.2 and 40.8 ± 1.5 μM, respectively; the IC 50 value for the positive control, EGCG, was 12.5 ± 0.8 μM. In addition, the mechanism by which 2 inhibited HNE was a mixed-type noncompetitive inhibition, with a K i of 41.5 ± 1.8 μM.