Lupane-Type Saponins from Leaves of Acanthopanax sessiliflorus and Their Inhibitory Activity on Pancreatic Lipase

Abstract

Three known saponins, chiisanoside, 11-deoxyisochiisanoside, and isochiisanoside, and one novel saponin, 3,4-seco-4(23),20(29)-lupadiene-3,28-dioic acid 28-O-alpha-l-rhamnopyranosyl (1-->4)-beta-d-glucopyranosyl (1-->6)-beta-d-glucopyranoside, referred to as sessiloside, were isolated from a hot water extract of Acanthopanax sessiliflorus leaves. All of these saponins were lupane-type triterpene triglycosides, and their concentrations were 4.1, 1.0, 0.5, and 0.4% (w/w) of the total extract, respectively. Sessiloside and chiisanoside inhibited pancreatic lipase activity in vitro, and addition of the saponin-rich fraction to a high-fat diet suppressed the body weight gain of mice. The possibility of application of the lupane-type saponins from A. sessiliflorus leaves to the treatment of obesity is discussed.

The role of lipid and carbohydrate digestive enzyme inhibitors in the management of obesity: a review of current and emerging therapeutic agents

“…In vitro studies have shown that both sessiloside and chiisanoside inhibit HPL activity in a dosedependent manner, with IC 50 values of 0.36 and 0.75 mg/mL, respectively. 53 In mice, simultaneous administration of oil and chiisanoside (100 and 300 mg/kg) decreased plasma TG levels and increased the amount of undigested TG in the intestinal lumen. 66 No clinical data are available on A. sessiliflorus.…”

“…51 Certain saponins such as oleanane, lupine and dammarane-type can inhibit pancreatic lipase activity and therefore have potential as treatments that could prove effective for obesity and related disorders. [52][53][54] However, the clinical potential of saponins remains difficult to judge with such limited clinical data available.…”

Chiisanoside Is Not Absorbed but Inhibits Oil Absorption in the Small Intestine of Rodents

“…1) Chiisanoside, 1-hydroxy-3, 4-seco-4 (23), 20 (29)-lupadien-3, 11-olid-28-oic acid 28-O--L-rhamnopyranosyl (1!4)--D-glucopyranosyl (1!6)--D-glucopyranoside, is the main component of A. sessiliflorus leaves. In our previous study, 2) we have reported that chiisanoside inhibited pancreatic lipase activity in a dose-dependent manner in vitro. Furthermore, the addition of the saponin-rich fraction (SF) of A. sessiliflorus containing chiisanoside at 42.6% (w/w) was shown to suppress the increase of body weight gain in mice when added to a high-fat diet for 4 weeks of feeding.…”

Effect of Acanthopanax sessiliflorus Extracts on Stress Response and Aging in Caenorhabditis elegans

“…Triterpenoids extracted from the fruits of A. sessiliflorus reduced nitric oxide production in macrophages . The water extracts of A. sessiliflorus inhibited pancreatic lipase activity and suppressed body weight gain in high-fat diet mice (Yoshizumi et al, 2006).…”

“…Triterpenoids extracted from the fruits of A. sessiliflorus reduced nitric oxide production in macrophages . The water extracts of A. sessiliflorus inhibited pancreatic lipase activity and suppressed body weight gain in high-fat diet mice (Yoshizumi et al, 2006).Recent studies also reports anti-oxidant and anti-aging activity of Acanthopanax species. The extracts from A. sessiliflorus leaves significantly decreased DNA and cell damage induced by oxidative stress (Ryu et al, 2012).…”