Inhibition of 15-hydroxyprostaglandin dehydrogenase activity in rabbit gastric antral mucosa by panaxynol isolated from oriental medicines.
Panaxynol is a polyacetylene compound with anti-inflammatory and anti-platelet-aggregatory effects isolated from commonly used oriental medicines. The effects of panaxynol on the activity of prostaglandin-synthesizing and catabolizing enzymes in the rabbit gastric antral mucosa have been examined. At concentrations ranging from 25 to 200 microM panaxynol had no effect on the synthesis of prostaglandins E2, F2alpha and D2 from exogenous arachidonic acid in the microsomal fraction of the gastric mucosa whereas at 25-200 microM it dose-dependently inhibited the activity of 15-hydroxyprostaglandin dehydrogenase (PGDH), which catalyses the initial step of prostaglandin catabolism, in the cytosolic fraction. The concentration required for 50% inhibition (IC50) was approximately 25 microM. Inhibition of PGDH by panaxynol was non-competitive with regard to NAD+ and prostaglandin E2. These results suggest that panaxynol has the potential to inhibit PGDH activity in gastric mucosa, possibly as a result of pharmacological activity.
Fujimoto
Y
Y
Department of Hygienic Chemistry, Osaka University of Pharmaceutical Sciences, Takatsuki, Japan.
Sakuma
S
S
Komatsu
S
S
Sato
D
D
Nishida
H
H
Xiao
Y Q
YQ
Baba
K
K
Fujita
T
T
D000480:Alkynes; D000818:Animals; D053280:Diynes; D004365:Drugs, Chinese Herbal / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology; D005233:Fatty Alcohols / Q000302:isolation & purification / Q000494:pharmacology*; D005753:Gastric Mucosa / Q000187:drug effects* / Q000378:metabolism; D006911:Hydroxyprostaglandin Dehydrogenases / Q000037:antagonists & inhibitors*; D008297:Male; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology*; D011453:Prostaglandins / Q000096:biosynthesis*; D011706:Pyloric Antrum / Q000187:drug effects / Q000378:metabolism; D011817:Rabbits
D000480:Alkynes; D053280:Diynes; D004365:Drugs, Chinese Herbal; D004791:Enzyme Inhibitors; D005233:Fatty Alcohols; D010936:Plant Extracts; D011453:Prostaglandins; C018541:falcarinol; D006911:Hydroxyprostaglandin Dehydrogenases; C035859:15-hydroxyprostaglandin dehydrogenase