Bioassay-guided separation of the proinflammatory constituents from the roots of Euphorbia kansui.
In view of the toxic inflammatory reaction induced by Euphorbia kansui roots, a traditional Chinese medicine used for the treatment of edema, ascites, and asthma, the 95% ethanol extract was found to have a significant stimulating effect on inflammatory cells. Bioassay-guided separation of the 95% ethanol extract from the roots of E. kansui led to the isolation of five diterpenoids whose structures were identified by (1)H, (13)C NMR spectroscopy and HR-ESI-MS as kansuinine B (1), kansuinine A (2), kansuiphorin C (3), 3-O-benzoyl-20-deoxyingenol (4), and 3-O-(2'E,4'Z-decadienoyl)-20-O-acetylingenol (5). The proinflammatory effect of compounds 1-5 was evaluated in vitro in models of inflammation using exoteric mice splenic lymphocytes (SPL) and rat peritoneal macrophages (PMphi). Compounds 1, 2, and 5 markedly promoted SPL proliferation and NO production by PMphi at concentrations from 0.78 to 12.50 microg/mL. Hence the three compounds are believed to be important proinflammatory components of the roots of E. kansui.
Jiangsu Key Laboratory for TCM Formulae Research, Nanjing University of Chinese Medicine, Nanjing, China.
Xiaoyun
X
Shu
Li
L
Yu
Yuping
Y
Tang
Li
L
Zhang
Anwei
A
Ding
Dan
D
Luo
Jin-ao
JA
Duan
Xiangchun
X
Shen
D000818:Animals; D001681:Biological Assay / Q000379:methods; D049109:Cell Proliferation / Q000187:drug effects; D004224:Diterpenes / Q000008:administration & dosage / Q000302:isolation & purification / Q000633:toxicity*; D004305:Dose-Response Relationship, Drug; D028481:Euphorbia / Q000737:chemistry*; D007249:Inflammation / Q000139:chemically induced*; D008214:Lymphocytes / Q000187:drug effects / Q000378:metabolism; D017737:Macrophages, Peritoneal / Q000187:drug effects / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D008297:Male; D008516:Medicine, Chinese Traditional; D051379:Mice; D008813:Mice, Inbred ICR; D009569:Nitric Oxide / Q000378:metabolism; D010936:Plant Extracts / Q000008:administration & dosage / Q000633:toxicity*; D018517:Plant Roots; D051381:Rats; D017207:Rats, Sprague-Dawley; D021241:Spectrometry, Mass, Electrospray Ionization; D013154:Spleen / Q000166:cytology / Q000378:metabolism
D004224:Diterpenes; D010936:Plant Extracts; D009569:Nitric Oxide