8-O-cinnamoylneoline, a new alkaloid from the flower buds of Aconitum carmichaeli and its toxic and analgesic activities.
From flower buds of Aconitum carmichaeli Debx., a new alkaloid, 8- O-cinnamoylneoline, was isolated. The structure of the new alkaloid was determined by spectral analysis, and the alkaloid was examined for its toxic and analgesic activities. Its LD50 value was 11.89 mg/kg (s.c.) in mice: the toxicity was 1/30 times that of mesaconitine and 20 times that of benzoylmesaconine. Its ED50 value was 0.86 mg/kg (s.c.) in mice using the tail pressure method: its analgesic effect was 1/40 times that of mesaconitine and 45 times that of benzoylmesaconine. Its safety margin (= LD50/ED50) was higher than that of benzoylmesaconine but lower than that of mesaconitine.
Taki
Masanori
M
Tsumura Research Institute, Tsumura & Co., 3586 Yoshiwara, Ami-machi, Inashiki-gun, Ibaraki 300-1192, Japan. taki_masanori@mail.tsumura.co.jp
Niitu
Kazuaki
K
Omiya
Yuji
Y
Noguchi
Masamichi
M
Fukuchi
Mikio
M
Aburada
Masaki
M
Okada
Minoru
M
D031841:Aconitum; D000470:Alkaloids / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D000700:Analgesics / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D000818:Animals; D002934:Cinnamates / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D035264:Flowers; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D010146:Pain / Q000517:prevention & control*; D010147:Pain Measurement / Q000187:drug effects; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity
C480881:8-O-cinnamoylneoline; D000470:Alkaloids; D000700:Analgesics; D002934:Cinnamates; D010936:Plant Extracts