In Vitro Antiinflammatory Activity of Kalopanaxsaponin A Isolated from Kalopanax pictus in Murine Macrophage RAW 264.7 Cells.

Abstract

The stem bark of Kalopanax pictus NAKAI (Araliaceae), a deciduous tree growing in East Asian countries, 1) has been traditionally used for the treatment of rheumatoidal arthritis, neurotic pain and diabetes mellitus. The constituents such as hederagenin glycosides, syringin, liriodendrin and coniferylaldehyde glucosides have been isolated from this plant. 2,3)Our previous reports on anti-diabetic, 4) cytotoxic 5) and antifungal assays 6) have shown that the active components should be hederagenin monodesmosides. In addition, we also demonstrated that hederagenin bisdesmoside could be converted to its monodesmosides and its serial saponins by human intestinal bacteria and that these metabolites showed anti-diabetic activity. 7) Although several pharmacological effects of hederagenin monodesmosides as well as its serial saponins are reported, there have been very few reports on the effects of hederagenin monodesmosides on the antiinflammatory role. During inflammatory processes, large amounts of pro-inflammatory mediators, nitric oxide (NO) and prostaglandin E 2 (PGE 2 ) are generated by the inducible isoforms of NO synthase (iNOS) and cyclooxygenase (COX-2), respectively. 8) In mammailian cells, three isoforms of NOS, types I, II, and III, have been identified on the basis of physical and biochemical characteristics of the purified enzymes. Type I (neuronal NOS, nNOS) and type III (endothelial NOS, eNOS) have been classified as constitutive NOS (cNOS) because these are continuously present in the cells, whereas type II, an iNOS, is expressed only after exposure to specific stimulants such as cytokines, bacterial endotoxic lipopolysaccharide (LPS), and calcium ionophore in some cells.9-11) Cyclooxygenase (COX) is the enzyme which converts arachidonic acid to prostaglandins (PGs). Like NOS, COX has been found in two isoforms, and COX-2 is an inducible form responsible for the production of large amounts of proinflammatory PGs at the inflammatory site. 12)Our previous investigation concerning kalopanaxsaponin A demonstrated their anti-inflammatory syndromes in the rat induced by Freund's complete adjuvant reagent.13) Thus, as a prelude to reveal the underlying mechanisms for the anti-inflammatory effect of kalopanaxsaponin A, we evaluated and compared the effects of various hederagenin monodesmosides ( Fig. 1) isolated from stem bark of Kalopanax pictus NAKAI on LPS-induced NO, PGE 2 and tumor necrosis factora (TNF-a) release by the macrophage cell line RAW 264.7 in the present study. Moreover, we also examined if these hederagenin monodesmosides reduced iNOS and COX-2 enzyme expression. Wonju 220-702, Korea. Received October 30, 2001; accepted January 16, 2002 In the present study, effects of various hederagenin monodesmosides isolated from the stem bark of Kalopanax pictus NAKAI, such as hederagenin, d d-hederin, kalopanaxsaponin A, kalopanaxsaponin I, and sapindoside C, have been evaluated on lipopolysaccharide (LPS)-induced nitric oxide (NO), prostaglandin E 2 (PGE 2 ) and tumor necrosis factor-a a (TNF-a a...

Evaluation of anti-inflammatory and analgesic effects on the extracts of different parts of Excoecaria agallocha L.

“…The anti-inflammatory activity action of triterpenoids has been reported by many researchers (Vazquez et al, 1996;Suh et al, 1998';Huss et al, 2002). Saponnins has also been reported to have anti-inflammatory activities by inhibition of the enzymes iNos, Cox-2 and lipoxygenase (Bermejo Benito et al, 1998;Li and Chu, 1999;Kim et al, 2002). Therefore, it seems that analgesic and anti-inflmmatory profile of E. agallocha seed might be related to the triterpenoids and saponins present in seed.…”

Anti-Inflammatory and Antinociceptive Effects of <i>Mitragyna speciosa</i> Korth Methanolic Extract

“…Moreover, the suppression of inducible nitric oxide synthase and cyclo-oxygenase-2 enzymes has been shown for alkaloids and flavonoids [28,29] . Saponins have also been reported to have antiinflammatory activities by inhibition of the enzymes inducible nitric oxide synthase, cyclo-oxygenase-2 and lipoxygenase [30] . Therefore, it seems that the anti-inflammatory and antinociceptive effects of MSM could also be attributed to the presence of alkaloids, saponins, flavonoids, tannins and sterols in the leaves of M. speciosa.…”

Radical Scavenging Activities of Phellinus pini

“…Especially, the active polysaccharide, isolated from mycelial culture of P. linteus, stimulates humoral and cell-mediated immunity, and exhibits a wider range of immunostimulation and anti-tumor activity than other polysaccharides isolated from Basidiomycetes [21]. Their polysaccharide showed the hypoglycemic effect, which was investigated in streptozotocin-induced diabetic rats, and also decreased total cholesterol, triacylglycerol and aspartate aminotransferase activity [23]. Most of all mushrooms inclusive of the genus Phellius had abundant biological active compounds and the phenolic compound was representative.…”