[16-Hydroxytriptolide, a new active diterpene isolated from Tripterygium wilford II].
A new diterpene triepoxide, 16-hydroxytriptolide was isolated from the root and leaves of Tripterygium wilfordii Hook.f. 16-Hydroxytriptolide was obtained as white cluster crystal, mp 232-233.5 degrees C. Its molecular formula is C20H24O7. The structure and stereochemistry of 16-hydroxytriptolide was established as L2 on the basis of spectral data (IR, MS, UV, 1H-NMR, 13C-NMR, 2d-NMR, NOE) and X-ray crystallographic analysis. In the pharmacologic screening, 16-hydroxytriptolide showed definite antiinflammatory actions and strong immunosuppressive and antifertile activities. In antiinflammatory action, its half effective dose (ED50) was 0.12 mg/kg with the model of croton oil induced ear swelling of mice. In immunosuppressive action, its ED50 was 0.05 mg/kg with the model of the formation of haemolysinantibody of mice. Its lowest effective dose (po) was 0.027mg/kg x 33d in antifertile action.
Ma
P C
PC
Institute of Dermatology, Chinese Academy of Medical Sciences, Nanjing.
Lu
X Y
XY
Yang
J J
JJ
Zheng
Q T
QT
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D003272:Contraceptive Agents, Male / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D004224:Diterpenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D004365:Drugs, Chinese Herbal / Q000737:chemistry*; D007166:Immunosuppressive Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D008297:Male; D051379:Mice; D008968:Molecular Conformation; D015394:Molecular Structure; D029757:Tripterygium
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003272:Contraceptive Agents, Male; D004224:Diterpenes; D004365:Drugs, Chinese Herbal; D007166:Immunosuppressive Agents; C076300:16-hydroxytriptolide