A kind of triterpene glycosides echinoside A(EA)was extracted from sea cucumber Pearsonothuria graeffei,and its yield was about 0.78%.The purity of EA was 99.0%,and its molecular weight was 1206 Da.EA was a linear tet...A kind of triterpene glycosides echinoside A(EA)was extracted from sea cucumber Pearsonothuria graeffei,and its yield was about 0.78%.The purity of EA was 99.0%,and its molecular weight was 1206 Da.EA was a linear tetrasaccharide attached to a pentacyclic triterpene aglycon.It inhibited the growth of MDA-MB-231 cells in vitro.The antitumor effect was related to elevate ROS level,decrease mitochondrial membrane potential,enhance caspase-3 expression,induce cells apoptosis and arrest cell cycle at G2/M phase.EA also dose-dependently suppressed the expressions of phophorylation proteins p-PI3K,p-Akt,and p-mTOR as analyzed by western blotting.These results suggested that EA caused MDA-MB-231 cells apoptosis via intrinsic mitochondrial and PI3K/Akt/mTOR pathway.EA can be a potential anti-breast cancer agent to enhance the clinical efficacy.展开更多
Sea cucumber saponins have attracted more attention in recent years due to biological activities.It is a popular practice to soak sea cucumber in Baijiu at home and being applied to industrial manufacturing in China.H...Sea cucumber saponins have attracted more attention in recent years due to biological activities.It is a popular practice to soak sea cucumber in Baijiu at home and being applied to industrial manufacturing in China.However,knowledge of the effect of alcohol on the absorption and metabolism of sea cucumber saponins is limited.The effects of alcohol on digestion,absorption and metabolism of sea cucumber saponins in BALB/c mice were investigated after gavage and tail intravenous injection.The results showed that the content of saponins in serum and liver was significantly higher under the influence of alcohol than that in the control group after oral administration.Alcohol promoted the absorption of sea cucumber saponins prototype as well as inhibited the process of saponins being transformed into deglycositic metabolites in the small intestine.Moreover,sea cucumber saponins remained in circulation for a long time and alcohol slowed down the clearance of sea cucumber saponins under the influence of alcohol after intravenous injection.This confirmed the feasibility of marinating sea cucumber in Baijiu to improve the efficacy of saponins and provides an important theoretical basis for the utilization of sea cucumber and the development of sea cucumber liquor.展开更多
Echinoside A is a triterpene saponin isolated from the sea cucumberActinopyga echinites （JAEGER）, which displays potent antitumor activities in vitro and in vivo. Here, we report the synthesis of the ABC-fused ring ...Echinoside A is a triterpene saponin isolated from the sea cucumberActinopyga echinites （JAEGER）, which displays potent antitumor activities in vitro and in vivo. Here, we report the synthesis of the ABC-fused ring skeleton of the aglycon of Echinoside A, with the enantiomerically pure （＋）-Wieland-Miescher ketone being used as starting material and a Robinson annulation as the key reaction.展开更多
基金supported by the National Key R&D Program of China(No.2018YFC0311206)the China Postdoctoral Science Foundation(No.2018M642706)the Postdoctoral Innovation Program of Shandong Province.
文摘A kind of triterpene glycosides echinoside A(EA)was extracted from sea cucumber Pearsonothuria graeffei,and its yield was about 0.78%.The purity of EA was 99.0%,and its molecular weight was 1206 Da.EA was a linear tetrasaccharide attached to a pentacyclic triterpene aglycon.It inhibited the growth of MDA-MB-231 cells in vitro.The antitumor effect was related to elevate ROS level,decrease mitochondrial membrane potential,enhance caspase-3 expression,induce cells apoptosis and arrest cell cycle at G2/M phase.EA also dose-dependently suppressed the expressions of phophorylation proteins p-PI3K,p-Akt,and p-mTOR as analyzed by western blotting.These results suggested that EA caused MDA-MB-231 cells apoptosis via intrinsic mitochondrial and PI3K/Akt/mTOR pathway.EA can be a potential anti-breast cancer agent to enhance the clinical efficacy.
文摘Sea cucumber saponins have attracted more attention in recent years due to biological activities.It is a popular practice to soak sea cucumber in Baijiu at home and being applied to industrial manufacturing in China.However,knowledge of the effect of alcohol on the absorption and metabolism of sea cucumber saponins is limited.The effects of alcohol on digestion,absorption and metabolism of sea cucumber saponins in BALB/c mice were investigated after gavage and tail intravenous injection.The results showed that the content of saponins in serum and liver was significantly higher under the influence of alcohol than that in the control group after oral administration.Alcohol promoted the absorption of sea cucumber saponins prototype as well as inhibited the process of saponins being transformed into deglycositic metabolites in the small intestine.Moreover,sea cucumber saponins remained in circulation for a long time and alcohol slowed down the clearance of sea cucumber saponins under the influence of alcohol after intravenous injection.This confirmed the feasibility of marinating sea cucumber in Baijiu to improve the efficacy of saponins and provides an important theoretical basis for the utilization of sea cucumber and the development of sea cucumber liquor.
基金financially supported by the Ministry of Science and Technology of China(No.2013AA092903)
文摘Echinoside A is a triterpene saponin isolated from the sea cucumberActinopyga echinites （JAEGER）, which displays potent antitumor activities in vitro and in vivo. Here, we report the synthesis of the ABC-fused ring skeleton of the aglycon of Echinoside A, with the enantiomerically pure （＋）-Wieland-Miescher ketone being used as starting material and a Robinson annulation as the key reaction.
