Effect of saikosaponin‐A, a triterpenoid glycoside, isolated from Bupleurum falcatum on experimental allergic asthma

Abstract

The separation and isolation of an extract of Bupleurum falcatum were performed based on antiallergic activities in preliminary studies with higher plants. The final active compound was identified as saikosaponin-A (SSA), a triterpenoid glycoside. SSA at more than 1 mg/kg (i.v.) significantly inhibited the passive cutaneous anaphylaxis reaction in rats in a dose-dependent manner, attaining a maximum inhibition of approximately 60% with 10 mg/kg. SSA at 3 and 10 mg/kg also suppressed asthmatic bronchoconstriction in sensitized guinea-pigs. SSA possesses a weak inhibitory activity on histamine-induced tracheal contraction in guinea-pigs and on histamine release induced by A-23187 in rat mast cells. These results indicate that SSA has an inhibitory activity against allergic asthma. This activity seems to derive from both antagonism of the histamine action and inhibition of allergic mediators. Additional mechanisms may also be involved.

Genus Bupleurum: a review of its phytochemistry, pharmacology and modes of action

“…It is usually difficult to separate the inflammatory process from the immune response; drugs with immunomodulatory [75,76] Alcoholic extract (-) Helicobacter pylori activity [77] Saikosaponin C (-) Hepatitis B replication [75] B. falcatum Acidic polysaccharide fraction (-) Gastric lesions [78] Saikosaponin mixture (-) Acute and chronic inflammation [79] Bupleuran 2IIc (-) Gastric lesions [80][81][82] (+) Gastric mucosa regeneration Saikosaponin A (+) B cells [83][84][85][86][87][88] (-) T cells (-) PGE2 (-) sGOT and sGPT levels (-) Lipid peroxidation (-) Asthmatic bronchoconstriction Saikosaponin D (+) Macrophage phagocytosis [75,[84][85][86][87][92][93][94] (-) T cells (+) Acid phosphatase (+) IL-2/IL-4 production (-) NF-kB (-) IL-6, TNF-a, IFN-g (+) PGE2 production (-) sGOT, sGPT and TGF-b1 levels (-) Lipid peroxidation Cytotoxic against HepG2 cell line (-) Measles and herpes viruses Saikosaponin B1…”

Isolation of Saponins with the Inhibitory Effect on Nitric Oxide, Prostaglandin E2 and Tumor Necrosis Factor-.ALPHA. Production from Pleurospermum kamtschaticum

“…saponin in P. kamtschaticum and thus that its inhibitory effect on NO, PGE 2 and TNF-a formation might be associated with its putative anti-inflammatory effect. Although numerous reports on the biological activities of saikosaponins and saikogenins, i.e., anti-inflammatory, 12) anti-allergic, 13) and anti-angiogenesis 14) and an elevation in intracellular calcium ion concentration, 15) this is the first report on the inhibitory effects of the saponins isolated in the present research on NO, PGE 2 and TNF-a production.…”

“…Acid hydrolysis of compound 1 produced D-fucose and D-glucose as the sugar moiety and saikogenin A (3) and -H (4) as the artifact of the sapogenin. Sugar moieties were identified on TLC and the structure of the triterpene produced was established by physicochemical (mp, [a] D ) and spectroscopic data ( 1 H-, 13 C-NMR, MS). Our physical and spectroscopic data was in accordance with the literature data on buddlejasaponin IV.…”

Induction of Cardiovascular Anaphylaxis and Basic Pharmacological Analysis of Involved Mediators in Pithed Rats

“…The skin and superficial muscles around the ventral cervix were removed to expose trachea. The trachea was dissected out at a length of 4-5 cartilage rings, and longitudinally cut open along the fibrous attachment (Park et al, 2002). The open ring was suspended in a 20-ml organ bath containing 95%-O 2 /5%-CO 2 -saturated Krebs-Henseleit solution (pH 7.4).…”