Ingol-type diterpenes from Euphorbia antiquorum with mouse 11β-hydroxysteroid dehydrogenase type 1 inhibition activity.
Eighteen new ingol-type diterpenes, euphorantins A-R (1-18), along with four known analogues (19-22), were isolated from the aerial parts of Euphorbia antiquorum. Compounds 1-3 are the first examples of C-17-oxygenated ingol-type diterpenes, and compounds 16-18 represent a rare class of 2,3-di-epimers of ingols. Diterpenes 1, 14, and 22 exhibited inhibitory activities against mouse 11β-HSD1 with IC50 values of 12.0, 6.4, and 0.41 μM, respectively.
State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University , Lanzhou 730000, People's Republic of China.
Wei-Yan
WY
Qi
Wei-Yi
WY
Zhang
Yu
Y
Shen
Ying
Y
Leng
Kun
K
Gao
Jian-Min
JM
Yue
D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors*; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D004224:Diterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D028481:Euphorbia / Q000737:chemistry*; D018922:HL-60 Cells; D006801:Humans; D007941:Leukemia P388; D051379:Mice; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular
D000972:Antineoplastic Agents, Phytogenic; D004224:Diterpenes; D004365:Drugs, Chinese Herbal; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1