Studies on the antitumor-promoting activity of naturally occurring substances. II. Inhibition of tumor-promoter-enhanced phospholipid metabolism by umbelliferous materials.
Ninety-five extracts prepared from 14 kinds of Umbelliferous materials were studied to determine their effects on tumor-promoter-induced phenomena in vitro. Of the materials, 5 Chinese crude drugs, two Bai-Hua Qian-Hu classified as Q-I and Q-II types, the root of Peucedanum praeruptorum Dunn., Zi-Hua Qian-Hu, the root of P. decursivum Maxim., Tang-Bai-Zhi, the root of Angelica dahurica Benth, et Hook. var. pai-chi Kimura, Hata et Yen., Dang-Gui, the root of A. acutiloba Kitagawa and 2 Umbelliferous plants, ashita-ba. A. keiskei Koidz., and ama-nyuu, A. edulis Miyabe, showed potent inhibitory effects on 12-O-tetradecanoylphorbol-13-acetate (TPA)-stimulated 32Pi incorporation into phospholipids of cultured cells. From the active fraction of the crude drug "Tang-Bai-Zhi," imperation (1), isoimperatoin (2), oxypeucedanin (3), pabulenol (4), neobyakangelicol (5) and byakangelicin (6) were identified as active or inactive principles. Compound 4 had not previously been isolated from Tang-Bai-Zhi, A. dahurica var. pai-chi. We also discuss the structure-activity relationship among the above 6 kinds of linear-type furanocoumarins, together with 3 kinds of antitumor-promoter coumarins having the same skeleton, psoralen (7), bergapten (8) and xanthotoxin (9), obtained from "ashita-ba" (eaten as a vegetable in Japan). Among the compounds in the present experiment, compounds 1 and 2 showed potent inhibitory activity at the concentration of 50 micrograms/ml and 3-9 were found to have less or no activity.
Okuyama
T
T
Department of Pharmacognosy and Phytochemistry, Meiji College of Pharmacy, Tokyo, Japan.
Takata
M
M
Nishino
H
H
Nishino
A
A
Takayasu
J
J
Iwashima
A
A
D000818:Animals; D002273:Carcinogens; D002478:Cells, Cultured; D004336:Drug Antagonism; D010743:Phospholipids / Q000378:metabolism*; D010936:Plant Extracts / Q000032:analysis / Q000494:pharmacology; D014468:Umbelliferones / Q000494:pharmacology*
D002273:Carcinogens; D010743:Phospholipids; D010936:Plant Extracts; D014468:Umbelliferones