Kaurane diterpenoids from Isodon excisus inhibit LPS-induced NF-kappaB activation and NO production in macrophage RAW264.7 cells.
As part of an ongoing search for plant-derived compounds that inhibit the activation of NF-kappaB, the methanol extract of the aerial parts of Isodon excisus was found to have significant inhibitory effects on the activation of NF-kappaB in murine macrophage RAW264.7 cells. Bioactivity-guided isolation of the extract yielded five new diterpenoids, excisusin A-E (1-5), along with seven known compounds, inflexarabdonin I (6), inflexarabdonin G (7), inflexin (8), inflexanin A (9), inflexanin B (10), inflexinol (11), and inflexarabdonin A (12). The structures were determined by analysis of the spectroscopic data including 2D NMR. All of the isolates were evaluated for their inhibitory effects on LPS-induced NF-kappaB activation and nitric oxide production in RAW264.7 cells.
Hong
Seong Su
SS
College of Pharmacy, Chungbuk National University, Cheongju, Chungbuk 361-763, Korea, Korea Research Institute of Bioscience and Biotechnology, P.O. Box 115, Yuseong, Daejeon 305-600, Korea.
Lee
Seon A
SA
Han
Xiang Hua
XH
Jin
Hui Zi
HZ
Lee
Jeong Hyung
JH
Lee
Dongho
D
Lee
Jung Joon
JJ
Hong
Jin Tae
JT
Kim
Youngsoo
Y
Ro
Jai Seup
JS
Hwang
Bang Yeon
BY
D000818:Animals; D045786:Diterpenes, Kaurane / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D037602:Isodon / Q000737:chemistry*; D007723:Korea; D008070:Lipopolysaccharides / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects*; D051379:Mice; D008968:Molecular Conformation; D015394:Molecular Structure; D016328:NF-kappa B / Q000037:antagonists & inhibitors*; D009569:Nitric Oxide / Q000037:antagonists & inhibitors*; D010946:Plants, Medicinal / Q000737:chemistry*
D045786:Diterpenes, Kaurane; D008070:Lipopolysaccharides; D016328:NF-kappa B; C583089:inflexanin B; D009569:Nitric Oxide