In the present study,we carried out a phytochemical investigation of the ethanol extract of the aerial parts of Baeckea frutescens,which resulted in the isolation of two new flavonoid glycosides,myricetin 3-O-(5'-...In the present study,we carried out a phytochemical investigation of the ethanol extract of the aerial parts of Baeckea frutescens,which resulted in the isolation of two new flavonoid glycosides,myricetin 3-O-(5'-O-galloyl)-α-L-arabinofuranoside(1),6-methylquercetin 7-O-β-D-glucopyranoside(2),one new methylchromone glycoside,7-O-(4',6'-digalloyl)-β-D-glucopyranosyl-5-hydroxy-2-methylchromone(3),together with three known compounds(4-6).The structures of these isolated compounds were established on the basis of 1 D and 2 D NMR techniques and chemical methods.The anti-inflammatory activities of the compounds 1-6 were evaluated for their inhibitory effects against cyclooxygenases-1 and-2 in vitro.Compounds 1-6 showed potent COX-1 and COX-2 inhibiting activities in vitro with IC50 values ranging from 1.95 to 5.54 μmol·L^(-1) and ranging from 1.01 to 2.27 μmol·L^(-1),respectively.展开更多
The fruits of Eucalyptus globulus Labill.are known to have a plenty of medicinal properties,such as anti-tumor,anti-inflammatory,and immunosuppressive activity.Our previous study found that the phloroglucinol-sesquite...The fruits of Eucalyptus globulus Labill.are known to have a plenty of medicinal properties,such as anti-tumor,anti-inflammatory,and immunosuppressive activity.Our previous study found that the phloroglucinol-sesquiterpene adducts in the fruits of E.globulus were immunosuppressive active constituents,especially Eucalyptin C(EuC).Phosphoinositide 3-kinases-γ(PI3Kγ)plays a pivotal role in T cell mediated excessive immune responses.In this study,EuC was first discovered to be a novel selective PI3Kγinhibitor with an IC50 value of 0.9μmol·L^(−1) and selectivity over 40-fold towards the other PI3K isoforms.Molecular docking,molecular dynamics simulation,and cellular thermal shift assay showed that EuC bound to PI3Kγ.Furthermore,EuC suppressed the downstream of PI3Kγto induce the apoptosis and inhibit the activation of primary spleen cells derived from allergic contact dermatitis mice.This work highlights the role of the fruits of E.globulus as a source of bioactive plant with immunosuppressive activity.展开更多
基金supported by the National Natural Science Foundation of China(No.81573309)
文摘In the present study,we carried out a phytochemical investigation of the ethanol extract of the aerial parts of Baeckea frutescens,which resulted in the isolation of two new flavonoid glycosides,myricetin 3-O-(5'-O-galloyl)-α-L-arabinofuranoside(1),6-methylquercetin 7-O-β-D-glucopyranoside(2),one new methylchromone glycoside,7-O-(4',6'-digalloyl)-β-D-glucopyranosyl-5-hydroxy-2-methylchromone(3),together with three known compounds(4-6).The structures of these isolated compounds were established on the basis of 1 D and 2 D NMR techniques and chemical methods.The anti-inflammatory activities of the compounds 1-6 were evaluated for their inhibitory effects against cyclooxygenases-1 and-2 in vitro.Compounds 1-6 showed potent COX-1 and COX-2 inhibiting activities in vitro with IC50 values ranging from 1.95 to 5.54 μmol·L^(-1) and ranging from 1.01 to 2.27 μmol·L^(-1),respectively.
基金This work was supported by China Postdoctoral Science Foundation(Nos.2019M662006 and 2019TQ0357)the National Natural Science Foundation of China(Nos.81973206,81803392 and 81573309)+5 种基金the Major National Science and Technology Projects of the Chinese Thirteen Five-Year Plan(No.2017ZX09309024)the Funding of Double First-rate Discipline Innovation Team(Nos.CPU2018PZQ17,CPU2018PZQ18,and CPU2018GF05)the Local Innovative and Research Teams Project of Guangdong Pearl River Talents Program(No.2017BT01Y036)the Research and Innovation Project for College Graduates of Jiangsu Province 2017(No.KYCX170694)the National College Student Innovation Project for the R&D of Novel Drugs(No.201710316100)Jiangsu Province Graduate Student Training Innovation Project(No.KYLX16_1208).
文摘The fruits of Eucalyptus globulus Labill.are known to have a plenty of medicinal properties,such as anti-tumor,anti-inflammatory,and immunosuppressive activity.Our previous study found that the phloroglucinol-sesquiterpene adducts in the fruits of E.globulus were immunosuppressive active constituents,especially Eucalyptin C(EuC).Phosphoinositide 3-kinases-γ(PI3Kγ)plays a pivotal role in T cell mediated excessive immune responses.In this study,EuC was first discovered to be a novel selective PI3Kγinhibitor with an IC50 value of 0.9μmol·L^(−1) and selectivity over 40-fold towards the other PI3K isoforms.Molecular docking,molecular dynamics simulation,and cellular thermal shift assay showed that EuC bound to PI3Kγ.Furthermore,EuC suppressed the downstream of PI3Kγto induce the apoptosis and inhibit the activation of primary spleen cells derived from allergic contact dermatitis mice.This work highlights the role of the fruits of E.globulus as a source of bioactive plant with immunosuppressive activity.
