HIRAI Yasuaki School of Pharmaceutical Sciences, Showa University, Associate Professor, 薬学部, 助教授 (50175551)
新宮 一司 昭和大学, 薬学部, 助手 (70258086)
梶本 哲也 昭和大学, 薬学部, 助教授 (80185777)
|Budget Amount *help
¥3,300,000 (Direct Cost : ¥3,300,000)
Fiscal Year 1999 : ¥800,000 (Direct Cost : ¥800,000)
Fiscal Year 1998 : ¥2,500,000 (Direct Cost : ¥2,500,000)
The dried root of Achyranthes fauriei Leveille et Vniot (Amaranthaceae) is one of the source plants of Achyranthes Root (Goshitsu in Japanese). Six novel triterpene glycosides, achymnthosides A-F, were isolated as methyl esters from the root of Actylanthes fauriei. These structures were characterized as oleanolic acid glucuronides having unique substituents at the C-3 posidon of glucuronic acid.
Many mimetics of sialyl Lewis X (sLeィイD1xィエD1), which can inhibit the excess interaction between neutrophiles and E-selectin much more potently than sLex itself, have been researched for some years as candidates for use as antiinflammatory agents for clinical tests. Achyranthes root has been utilized in East Asia from ancient times to cure arthritis caused by rhcumatism. Therefore, Achyranthosides are potential components which can inhibit the excess recruiting of neutrophiles to injured tissues.
The effect of the fraction composed from Achyranthosides E and F on carragenin-induced edema and myel
operoxidase (MPO) activity were examined. The fraction composed from Achyranthosides E and F (200 mg/kg, ip) significantly suppressed carragenin-induced edema and MPO activity.
Furthermore, effect of the fractions composed from Achyranthosides E and F, and ecdysteroids on the adhesion of polymorphonuclear leukocytes (PMNs) to human umbilical cells (HUVECs) was examined. Both samples showed the adhesion activity, particularly the measured IC50 value of the fraction composed from Achyranthosides E and F was 50 μg/ml, which is 100 times more potent than sLex..
As mendoned above, achyrnathoside E and F from A. fauriei, which were characterized as novel glucuronide saponins having unique substituents at the GluA C-3 position, potently inhibited the interaction between PMNs and E-selectin.
To determine the individual activity of saponins and ecdysteroids, we have reinvestigated the crude saponin fraction and the crude ecdysteroid fraction from the methanolic extract of Achyranthes fauriei roots except methylation. Consequently, three glycosides of oleanolic acid and six ecdysteroids include three new compounds.
The antiinflammatory activity of the compounds is under investigation. Less