从水麻(Debregeasia orientalis C J Chen)地上部分的95%乙醇提取物中首次分离到18个化合物,应用波谱方法或与已知品对照的手段鉴定它们为棕榈酸(1)、正二十烷酸(2)、正二十烷酸甲酯(3)、β-谷甾醇(4)、Monogynol A(5)、白桦酸(6)、Hede...从水麻(Debregeasia orientalis C J Chen)地上部分的95%乙醇提取物中首次分离到18个化合物,应用波谱方法或与已知品对照的手段鉴定它们为棕榈酸(1)、正二十烷酸(2)、正二十烷酸甲酯(3)、β-谷甾醇(4)、Monogynol A(5)、白桦酸(6)、Heder agenin(7)、β-胡萝卜甙(8)、18αH-20(29)-烯-3-酮-乌苏烷(9)、3,4-开环-20(29)-烯-乌苏烷-3-酸(10)、Pomolic acid(11)、表儿茶素(12)、儿茶素(13)、槲皮素(14)、槲皮素-3-O-β-D-吡喃葡萄糖苷(15)、紫丁香苷(16)、紫丁香酚苷(17)和山萘酚-3-O-β-D-芦丁糖苷(18)。展开更多
Protein tyrosine phosphatase 1 B(PTP1 B) has led to an intense interest in developing its inhibitors as anti-diabetes, anti-obesity and anti-cancer agents. The fruits of Rubus chingii(Chinese raspberry) were used as a...Protein tyrosine phosphatase 1 B(PTP1 B) has led to an intense interest in developing its inhibitors as anti-diabetes, anti-obesity and anti-cancer agents. The fruits of Rubus chingii(Chinese raspberry) were used as a kind of dietary traditional Chinese medicine. The methanolic extract of R. chingii fruits exhibited significant PTP1 B inhibitory activity. Further bioactivity-guided fractionation resulted in the isolation of three PTP1 B inhibitory ursane-type triterpenes: ursolic acid(1), 2-oxopomolic acid(2), and 2α, 19α-dihydroxy-3-oxo-urs-12-en-28-oic acid(3). Kinetics analyses revealed that 1 was a non-competitive PTP1 B inhibitor, and 2 and 3 were mixed type PTP1 B inhibitors. Compounds 1-3 and structurally related triterpenes(4-8) were further analyzed the structure-activity relationship, and were evaluated the inhibitory selectivity against four homologous protein tyrosine phosphatases(TCPTP, VHR, SHP-1 and SHP-2). Molecular docking simulations were also carried out, and the result indicated that 1, 3-acetoxyurs-12-ene-28-oic acid(5), and pomolic acid-3β-acetate(6) bound at the allosteric site including α3, α6, and α7 helix of PTP1 B.展开更多
Seven new triterpenoid saponins,including five ursane-type saponins,ilexchinenosides R–V(1–5),and two oleananetype saponins,ilexchinenosides W–X(6–7),with four known triterpenoid saponins(8–11)were isolated from ...Seven new triterpenoid saponins,including five ursane-type saponins,ilexchinenosides R–V(1–5),and two oleananetype saponins,ilexchinenosides W–X(6–7),with four known triterpenoid saponins(8–11)were isolated from the leaves of Ilex chinensis.Their structures were elucidated by comprehensive spectroscopic 1 D and 2 D NMR and HR-ESI-MS data.Their sugar moieties were determined by HPLC analysis compared with standards after hydrolysis and derivatization.Compounds 1,2,4,9 and 10 exhibited potential hepatoprotective activity against N-acetyl-p-aminophenol(APAP)-induced Hep G2 cell injury in vitro.展开更多
采用乙醇提取,硅胶柱反复层析的方法,从白透骨消[Glechoma biondiana(Diels)C.Y.Wu et C.Chen]全草的乙酸乙酯部分分离了11个化合物,利用现代波谱技术(MS,1H-NMR,13C-NMR,DEPT)以及与文献对照的方法鉴定了这些化合物的结构,分别为2α-...采用乙醇提取,硅胶柱反复层析的方法,从白透骨消[Glechoma biondiana(Diels)C.Y.Wu et C.Chen]全草的乙酸乙酯部分分离了11个化合物,利用现代波谱技术(MS,1H-NMR,13C-NMR,DEPT)以及与文献对照的方法鉴定了这些化合物的结构,分别为2α-羟基乌苏酸(1)、2α,3α-二羟基乌苏-12-烯-28-酸(2)、乌苏酸(3)、2α,3α,23-三羟基乌苏-12-烯-28-酸(4)、3β,24-二羟基乌苏-12-烯-28-酸(5)、3α-羟基乌苏-12-烯-28-酸(6)、豆甾烷-3,6-二酮(7)、7β-羟基谷甾醇(8)、豆甾醇(9)、β-胡萝卜苷(10)、棕榈酸(11)。除化合物(3)和(10)外,其余均为首次从该植物中分离得到。展开更多
The flower buds of Lonicera macranthoides(Shan Yin-Hua), represent an important traditional Chinese medicine and food ingredient. A phytochemical investigation of the 70% EtOH extract of the flower buds of L. macranth...The flower buds of Lonicera macranthoides(Shan Yin-Hua), represent an important traditional Chinese medicine and food ingredient. A phytochemical investigation of the 70% EtOH extract of the flower buds of L. macranthoides resulted in the isolation of 12 triterpenoids(1-12), including two new ursane-type nortriterpenes, 2α, 24-dihydroxy-23-nor-ursolic acid(1) and 2α, 4α-dihydroxy-23-nor-ursolic acid(2). Their structures were established by multiple spectroscopic methods and comparison with literature data. All isolated compounds were evaluated for their anti-inflammatory effects in LPS-activated RAW264.7 cells. Compounds 1 and 2 exhibited inhibitory effects on iNOS at the concentration of 30 μmol·L^(-1).展开更多
文摘从水麻(Debregeasia orientalis C J Chen)地上部分的95%乙醇提取物中首次分离到18个化合物,应用波谱方法或与已知品对照的手段鉴定它们为棕榈酸(1)、正二十烷酸(2)、正二十烷酸甲酯(3)、β-谷甾醇(4)、Monogynol A(5)、白桦酸(6)、Heder agenin(7)、β-胡萝卜甙(8)、18αH-20(29)-烯-3-酮-乌苏烷(9)、3,4-开环-20(29)-烯-乌苏烷-3-酸(10)、Pomolic acid(11)、表儿茶素(12)、儿茶素(13)、槲皮素(14)、槲皮素-3-O-β-D-吡喃葡萄糖苷(15)、紫丁香苷(16)、紫丁香酚苷(17)和山萘酚-3-O-β-D-芦丁糖苷(18)。
基金supported by the National Natural Science Foundation of China(No.81628012)
文摘Protein tyrosine phosphatase 1 B(PTP1 B) has led to an intense interest in developing its inhibitors as anti-diabetes, anti-obesity and anti-cancer agents. The fruits of Rubus chingii(Chinese raspberry) were used as a kind of dietary traditional Chinese medicine. The methanolic extract of R. chingii fruits exhibited significant PTP1 B inhibitory activity. Further bioactivity-guided fractionation resulted in the isolation of three PTP1 B inhibitory ursane-type triterpenes: ursolic acid(1), 2-oxopomolic acid(2), and 2α, 19α-dihydroxy-3-oxo-urs-12-en-28-oic acid(3). Kinetics analyses revealed that 1 was a non-competitive PTP1 B inhibitor, and 2 and 3 were mixed type PTP1 B inhibitors. Compounds 1-3 and structurally related triterpenes(4-8) were further analyzed the structure-activity relationship, and were evaluated the inhibitory selectivity against four homologous protein tyrosine phosphatases(TCPTP, VHR, SHP-1 and SHP-2). Molecular docking simulations were also carried out, and the result indicated that 1, 3-acetoxyurs-12-ene-28-oic acid(5), and pomolic acid-3β-acetate(6) bound at the allosteric site including α3, α6, and α7 helix of PTP1 B.
基金CAMS Innovation Fund for Medicial Sciences(CIFMS-2019-I2M-1-005)。
文摘Seven new triterpenoid saponins,including five ursane-type saponins,ilexchinenosides R–V(1–5),and two oleananetype saponins,ilexchinenosides W–X(6–7),with four known triterpenoid saponins(8–11)were isolated from the leaves of Ilex chinensis.Their structures were elucidated by comprehensive spectroscopic 1 D and 2 D NMR and HR-ESI-MS data.Their sugar moieties were determined by HPLC analysis compared with standards after hydrolysis and derivatization.Compounds 1,2,4,9 and 10 exhibited potential hepatoprotective activity against N-acetyl-p-aminophenol(APAP)-induced Hep G2 cell injury in vitro.
文摘采用乙醇提取,硅胶柱反复层析的方法,从白透骨消[Glechoma biondiana(Diels)C.Y.Wu et C.Chen]全草的乙酸乙酯部分分离了11个化合物,利用现代波谱技术(MS,1H-NMR,13C-NMR,DEPT)以及与文献对照的方法鉴定了这些化合物的结构,分别为2α-羟基乌苏酸(1)、2α,3α-二羟基乌苏-12-烯-28-酸(2)、乌苏酸(3)、2α,3α,23-三羟基乌苏-12-烯-28-酸(4)、3β,24-二羟基乌苏-12-烯-28-酸(5)、3α-羟基乌苏-12-烯-28-酸(6)、豆甾烷-3,6-二酮(7)、7β-羟基谷甾醇(8)、豆甾醇(9)、β-胡萝卜苷(10)、棕榈酸(11)。除化合物(3)和(10)外,其余均为首次从该植物中分离得到。
基金supported by the National Natural Science Foundation of China(Nos.81602984 and 81630097)Science and Technology Planning Project of Guangdong Province(No.2015B030301005)
文摘The flower buds of Lonicera macranthoides(Shan Yin-Hua), represent an important traditional Chinese medicine and food ingredient. A phytochemical investigation of the 70% EtOH extract of the flower buds of L. macranthoides resulted in the isolation of 12 triterpenoids(1-12), including two new ursane-type nortriterpenes, 2α, 24-dihydroxy-23-nor-ursolic acid(1) and 2α, 4α-dihydroxy-23-nor-ursolic acid(2). Their structures were established by multiple spectroscopic methods and comparison with literature data. All isolated compounds were evaluated for their anti-inflammatory effects in LPS-activated RAW264.7 cells. Compounds 1 and 2 exhibited inhibitory effects on iNOS at the concentration of 30 μmol·L^(-1).