title: Antinociceptive and antiinflammatory effects of Niga-ichigoside F1 and 23-hydroxytormentic acid obtained from Rubus coreanus.
abstract: As an attempt to search for bioactive natural constituents exerting antinociceptive and antiinflammatory activities, we examined the potency of the extract of Rubus coreanus fruits by the activity-guided fractionation. The EtOAc- and BuOH fraction and those alkaline hydrolysates showed significant antinociceptive effects as assessed by writhing-, hot plate- and tail flicks tests in mice and rats as well as antiinflammatory effect in rats with carrageenan-induced edema. BuOH extract was subjected to column chromatography to obtain a large amount of niga-ichigoside F(1) (1,23-hydroxytormentic acid 28-O-glc), which was again hydrolyzed in NaOH solution to yield an aglycone 23-hydroxytormentic acid (1a). The aglycone, 23-hydroxytormentic acid, was much more potent in both antinociceptive and antiinflammatory tests than the glycoside, niga-ichigoside F(1). The antiinflammatory effects of these compounds were further supported by the reduction of carrageenan-induced lipid peroxidation and hydroxyl radical in serum. These results suggested that 23-hydroxytormentic acid might be an active moiety of niga-ichigoside F(1) present in R. coreanus.
authors.affiliation: College of Pharmacy, Daeyeon-Dong, Kyungsung University, Japan.
authors.forename: Jongwon
authors.initials: J
authors.lastname: Choi
authors.forename: Kyung-Tae
authors.initials: KT
authors.lastname: Lee
authors.forename: Joohun
authors.initials: J
authors.lastname: Ha
authors.forename: Sei-Young
authors.initials: SY
authors.lastname: Yun
authors.forename: Chang-Duk
authors.initials: CD
authors.lastname: Ko
authors.forename: Hyun-Ju
authors.initials: HJ
authors.lastname: Jung
authors.forename: Hee-Juhn
authors.initials: HJ
authors.lastname: Park
mesh_terms: D000700:Analgesics / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D005638:Fruit; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D010147:Pain Measurement / Q000187:drug effects / Q000379:methods; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D012503:Saponins / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D014315:Triterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D004365:Drugs, Chinese Herbal; D010936:Plant Extracts; D012503:Saponins; D014315:Triterpenes; C007695:euscaphic acid; C090725:niga-ichigoside F1