利用MCI gel CHP-20、ODS、Sephadex LH-20、硅胶及半制备高效液相等多种色谱技术,从皂角刺乙酸乙酯部位分离得到7个木脂素类化合物,并根据波谱数据分析鉴定其结构,分别为(7R,8S,7'E,7''S,8''R)-buddlenol P(1)、(...利用MCI gel CHP-20、ODS、Sephadex LH-20、硅胶及半制备高效液相等多种色谱技术,从皂角刺乙酸乙酯部位分离得到7个木脂素类化合物,并根据波谱数据分析鉴定其结构,分别为(7R,8S,7'E,7''S,8''R)-buddlenol P(1)、(+)-丁香脂素(2)、(+)-异落叶松脂素(3)、(7S,8R)-cedrusin(4)、(7S,8R)-4,9,9'-三羟基-3,3'-二甲氧基-7,8-二氢苯骈呋喃-1'-丙基新木脂素(5)、3',4-O-dimethylcedrusin(6)和蛇菰宁(7)。其中化合物1为新化合物,命名为(7R,8S,7'E,7''S,8''R)-buddlenol P,化合物2~7为首次从皂荚属中分离得到。采用MTT法探究化合物2~7对脂多糖(LPS)诱导的大鼠肾小管上皮细胞损伤的干预作用,化合物2、3和7对LPS诱导的NRK-52e细胞损伤具有保护作用。展开更多
Patrinia scabiosaefolia,is used as wild vegetable in China for more than 2000 years,with a variety of pharmacological activities,including anti-inflammatory,anti-tumor and hypoglycemic.Based on our ongoing research on...Patrinia scabiosaefolia,is used as wild vegetable in China for more than 2000 years,with a variety of pharmacological activities,including anti-inflammatory,anti-tumor and hypoglycemic.Based on our ongoing research on chemical constituents and hypoglycemic activity of P.scabiosaefolia,4 lignan compounds,(+)-isolariciresinol(1),7R,7’R,8S,8’S-(+)-neo-olivil-4-O-β-D-glucopyranoside(2),4-O-methylcedrusin(3)and patrinian A(4),were isolated and identifi ed.The hypoglycemic activity showed that compounds 2 and 3 could extremely signifi cantly improve insulin resistance at 100(P<0.001),50(P<0.001)and 25μmol/L(P<0.01)in IR 3T3-L1 cells.While compound 4 only promoted glucose uptake by IR 3T3-L1 cells at 100μmol/L(P<0.01).Western blotting experiments showed that compounds 2 and 4 up-regulated the protein expressions of p-IRS,PI-3K,p-AKT and glucose transporter 4(GLUT4),and promoted the transcription of GLUT4 mRNA.Therefore,the mechanisms of compounds 2 and 4 were presumed to improve IR by activating PI-3K/AKT signaling pathway.展开更多
Two new ar-bisabol sequiterpenes,(+)-(7S,10S)-10-epi-7,10-epoxy-3-hydroxy-ar-bisabol-11-ol(1)and(+)-(7R,8R,10S)-10-epi-7,10-epoxy-8-hydroxy-ar-bisabol-11-ol(2),have been isolated by a combination of various column chr...Two new ar-bisabol sequiterpenes,(+)-(7S,10S)-10-epi-7,10-epoxy-3-hydroxy-ar-bisabol-11-ol(1)and(+)-(7R,8R,10S)-10-epi-7,10-epoxy-8-hydroxy-ar-bisabol-11-ol(2),have been isolated by a combination of various column chromatographic techniques including reversed-phase semipreparative HPLC from an ethanol extract of the stem bark of Fraxinus sielboldiana.Their structures were determined by spectroscopic methods including IR,MS,and 1D and 2D NMR experiments.This is the first report of sequiterpenes in the genus Fraxinus.展开更多
Vascular endothelial growth factor receptor 2(VEGFR-2)and neuropilin-1(NRP-1)are two prominent antiangiogenic targets.They are highly expressed on vascular endothelial cells and some tumor cells.Therefore,targeting VE...Vascular endothelial growth factor receptor 2(VEGFR-2)and neuropilin-1(NRP-1)are two prominent antiangiogenic targets.They are highly expressed on vascular endothelial cells and some tumor cells.Therefore,targeting VEGFR-2 and NRP-1 may be a potential antiangiogenic and antitumor strategy.A7R,a peptide with sequence of Ala-Thr-Trp-Leu-Pro-Pro-Arg that was found by phage display of peptide libraries,can preferentially target VEGFR-2 and NRP-1 and destroy the binding between vascular endothelial growth factor 165(VEGF165)and VEGFR-2 or NRP-1.This peptide is a new potent inhibitor of tumor angiogenesis and a targeting ligand for cancer therapy.This review describes the discovery,function and mechanism of the action of A7R,and further introduces the applications of A7R in antitumor angiogenic treatments,tumor angiogenesis imaging and targeted drug delivery systems.In this review,strategies to deliver different drugs by A7R-modified liposomes and nanoparticles are highlighted.A7R,a new dual targeting ligand of VEGFR-2 and NRP-1,is expected to have efficient therapeutic or targeting roles in tumor drug delivery.展开更多
The first enantioselective total synthesis of 5-acetoxygoniothalamin 1 and 5-acetoxyisogoniothalamin oxide 2 was achieved through the Sharpless kinetic resolution of racemic secondary 2- furylmethanol 5 and the Mitsun...The first enantioselective total synthesis of 5-acetoxygoniothalamin 1 and 5-acetoxyisogoniothalamin oxide 2 was achieved through the Sharpless kinetic resolution of racemic secondary 2- furylmethanol 5 and the Mitsunobu reaction. At the same time we developed a short synthetic route for 6R-(+)-goniothalamin 3 and (6R, 7R, 8R)-(+)-goniothalamin oxide 4. And according to this route the configuration of 5-acetoxygoniothalamin 1 was confirmed as (5S, 6S).展开更多
Objective:To study the antipyretic and anti-inflammatory constituents from the active fraction of Reduning(RDN)Injection.Methods:In this study,the active fraction of RDN Injection was screened by the LPS-induced mouse...Objective:To study the antipyretic and anti-inflammatory constituents from the active fraction of Reduning(RDN)Injection.Methods:In this study,the active fraction of RDN Injection was screened by the LPS-induced mouse endotoxin shock model.The chemical constituents were isolated by chromatography on HP-20 macroporous adsorptive resins,silica gel,ODS columns and reverse phase MPLC and HPLC repeatedly,and their structures were elucidated based on spectroscopic analysis(HR-ESI-MS,NMR,ECD)and chemical methods.Meanwhile,we evaluated the anti-inflammatory activities of the isolates by measuring their inhibitory effects on TNF-αproduction in LPS stimulated RAW 264.7 macrophages.Results:The 95%ethanol eluate of RDN Injection by the macroporous adsorption resin column was proved to be the antipyretic and anti-inflammatory active fraction of this injection.A novel iridoid,named jasminoide A(1),and a new guaiane sesquiterpenoid,named(1 R,7 R,8 S,10 R)-7,8,11-trihydroxy-4-guaien-3-one(2),were isolated from Reduning injection,and compound 2 can inhibit TNF-αproduction with IC50 values of 72.24μmol/L.Conclusion:In this study,two new terpenoids were isolated from Reduning Injection,and compound 2 showed inhibitory activity against LPS-activated TNF-αproduction in RAW 264.7 cells in vitro.展开更多
基金funded by National Key R&D Program of China(2022YFF1100300)National Natural Science Foundation of China(31900292)+1 种基金Science and Technology Development Program of Henan Province(212102110469,222102520035)Research on Precision Nutrition and Health Food,Department of Science and Technology of Henan Province(CXJD2021006).
文摘Patrinia scabiosaefolia,is used as wild vegetable in China for more than 2000 years,with a variety of pharmacological activities,including anti-inflammatory,anti-tumor and hypoglycemic.Based on our ongoing research on chemical constituents and hypoglycemic activity of P.scabiosaefolia,4 lignan compounds,(+)-isolariciresinol(1),7R,7’R,8S,8’S-(+)-neo-olivil-4-O-β-D-glucopyranoside(2),4-O-methylcedrusin(3)and patrinian A(4),were isolated and identifi ed.The hypoglycemic activity showed that compounds 2 and 3 could extremely signifi cantly improve insulin resistance at 100(P<0.001),50(P<0.001)and 25μmol/L(P<0.01)in IR 3T3-L1 cells.While compound 4 only promoted glucose uptake by IR 3T3-L1 cells at 100μmol/L(P<0.01).Western blotting experiments showed that compounds 2 and 4 up-regulated the protein expressions of p-IRS,PI-3K,p-AKT and glucose transporter 4(GLUT4),and promoted the transcription of GLUT4 mRNA.Therefore,the mechanisms of compounds 2 and 4 were presumed to improve IR by activating PI-3K/AKT signaling pathway.
基金Financial support from the National Natural Sciences Foundation of China(NNSFC,Grant nos.30825044 and 20932007)the National Science and Technology Project of China(Nos.2009ZX09311-004 and 2009ZX09301-003-4-1)is acknowledged.
文摘Two new ar-bisabol sequiterpenes,(+)-(7S,10S)-10-epi-7,10-epoxy-3-hydroxy-ar-bisabol-11-ol(1)and(+)-(7R,8R,10S)-10-epi-7,10-epoxy-8-hydroxy-ar-bisabol-11-ol(2),have been isolated by a combination of various column chromatographic techniques including reversed-phase semipreparative HPLC from an ethanol extract of the stem bark of Fraxinus sielboldiana.Their structures were determined by spectroscopic methods including IR,MS,and 1D and 2D NMR experiments.This is the first report of sequiterpenes in the genus Fraxinus.
基金funded by National Natural Science Foundation of China(No.81302686)Primary Research&Developement Plan of Shandong Province(No.2016GSF201083)
文摘Vascular endothelial growth factor receptor 2(VEGFR-2)and neuropilin-1(NRP-1)are two prominent antiangiogenic targets.They are highly expressed on vascular endothelial cells and some tumor cells.Therefore,targeting VEGFR-2 and NRP-1 may be a potential antiangiogenic and antitumor strategy.A7R,a peptide with sequence of Ala-Thr-Trp-Leu-Pro-Pro-Arg that was found by phage display of peptide libraries,can preferentially target VEGFR-2 and NRP-1 and destroy the binding between vascular endothelial growth factor 165(VEGF165)and VEGFR-2 or NRP-1.This peptide is a new potent inhibitor of tumor angiogenesis and a targeting ligand for cancer therapy.This review describes the discovery,function and mechanism of the action of A7R,and further introduces the applications of A7R in antitumor angiogenic treatments,tumor angiogenesis imaging and targeted drug delivery systems.In this review,strategies to deliver different drugs by A7R-modified liposomes and nanoparticles are highlighted.A7R,a new dual targeting ligand of VEGFR-2 and NRP-1,is expected to have efficient therapeutic or targeting roles in tumor drug delivery.
基金We are grateful to the National Natural Science Foundation of China(No.2017223)for financial support
文摘The first enantioselective total synthesis of 5-acetoxygoniothalamin 1 and 5-acetoxyisogoniothalamin oxide 2 was achieved through the Sharpless kinetic resolution of racemic secondary 2- furylmethanol 5 and the Mitsunobu reaction. At the same time we developed a short synthetic route for 6R-(+)-goniothalamin 3 and (6R, 7R, 8R)-(+)-goniothalamin oxide 4. And according to this route the configuration of 5-acetoxygoniothalamin 1 was confirmed as (5S, 6S).
基金supported by the National Standard Research of Traditional Chinese Medicine for Reduning Injection(ZYBZHC-JS-31)National Standard Research of Traditional Chinese Medicine for Guzhi Fuling Capsule(ZYBZH-C-JS-28)grant from the National Natural Science Foundation of China(No.81602984)。
文摘Objective:To study the antipyretic and anti-inflammatory constituents from the active fraction of Reduning(RDN)Injection.Methods:In this study,the active fraction of RDN Injection was screened by the LPS-induced mouse endotoxin shock model.The chemical constituents were isolated by chromatography on HP-20 macroporous adsorptive resins,silica gel,ODS columns and reverse phase MPLC and HPLC repeatedly,and their structures were elucidated based on spectroscopic analysis(HR-ESI-MS,NMR,ECD)and chemical methods.Meanwhile,we evaluated the anti-inflammatory activities of the isolates by measuring their inhibitory effects on TNF-αproduction in LPS stimulated RAW 264.7 macrophages.Results:The 95%ethanol eluate of RDN Injection by the macroporous adsorption resin column was proved to be the antipyretic and anti-inflammatory active fraction of this injection.A novel iridoid,named jasminoide A(1),and a new guaiane sesquiterpenoid,named(1 R,7 R,8 S,10 R)-7,8,11-trihydroxy-4-guaien-3-one(2),were isolated from Reduning injection,and compound 2 can inhibit TNF-αproduction with IC50 values of 72.24μmol/L.Conclusion:In this study,two new terpenoids were isolated from Reduning Injection,and compound 2 showed inhibitory activity against LPS-activated TNF-αproduction in RAW 264.7 cells in vitro.
