In recent years,preclinical research on diabetic kidney disease (DKD) has surged to the forefront of scientific and clinical attention.DKD has become a pervasive complication of type 2 diabetes.Given the complexity of...In recent years,preclinical research on diabetic kidney disease (DKD) has surged to the forefront of scientific and clinical attention.DKD has become a pervasive complication of type 2 diabetes.Given the complexity of its etiology and pathological mechanisms,current interventions,including drugs,dietary modifications,exercise,hypoglycemic treatments and lipid-lowering methods,often fall short in achieving desired therapeutic outcomes.Iridoids,primarily derived from the potent components of traditional herbs,have been the subject of long-standing research.Preclinical data suggest that iridoids possess notable renal protective properties;however,there has been no summary of the research on their efficacy in the management and treatment of DKD.This article consolidates findings from in vivo and in vitro research on iridoids in the context of DKD and highlights their shared anti-inflammatory activities in treating this condition.Additionally,it explores how certain iridoid components modify their chemical structures through the regulation of intestinal flora,potentially bolstering their therapeutic effects.This review provides a focused examination of the mechanisms through which iridoids may prevent or treat DKD,offering valuable insights for future research endeavors.展开更多
In order to determine the chemical constituents of Cistanche deserticola cultured in Tarim desert,a systematically phytochemical investigation was carried out.The constituents were isolated by silica gel,Sephadex LH-2...In order to determine the chemical constituents of Cistanche deserticola cultured in Tarim desert,a systematically phytochemical investigation was carried out.The constituents were isolated by silica gel,Sephadex LH-20,MCI gel,ODS column chromatography,and semi-preparative HPLC.Their structures were determined on the basis of MS and NMR spectroscopic analyses,by chemical methods,and/or comparison with literature data.The anti-inflammatory activities of the isolates were evaluated for their inhibitory effects on the lipopolysaccharide(LPS)-induced nitric oxide(NO)production in BV-2 mouse microglial cells.Nine iridoids were isolated and identified as cistadesertoside A(1),cistanin(2),cistachlorin(3),6-deoxycatalpol(4),gluroside(5),kankanoside A(6),ajugol(7),bartsioside(8),and 8-epi-loganic acid(9).Compound 9 exhibited potent inhibition on the NO production with an IC_(50) value being 5.2 μmol·L^(-1),comparable to the positive control quercetin(4.3 μmol·L^(-1)).Compound 1 was a new iridoid,and compounds 5,6,and 8 were isolated from this species for the first time.展开更多
Gardeniae Fructus(GF)and Semen Sojae Praeparatum(SSP)are both medicine food homologies and widely used in Chinese clinical prescriptions together.The research investigated the pharmacokinetics of four iridoids in norm...Gardeniae Fructus(GF)and Semen Sojae Praeparatum(SSP)are both medicine food homologies and widely used in Chinese clinical prescriptions together.The research investigated the pharmacokinetics of four iridoids in normal rats and isolfavones-fed rats,which were administered with isolfavones from SSP for 7,14,21 and 28 consecutive days.A validated LC-MS/MS method was developed for determining shanzhiside,genipin-1-gentiobioside,geniposide and their metabolite genipin in rat plasma.Plasma samples were pretreated by solid-phase extraction using paeoniflorin as the internal standard.The chromatographic separation was performed on a Waters Atlantis T3(4.6 mm×150 mm,3 mm)column using a gradient mobile phase consisting of acetonitril and water(containing 0.06%acetic acid).The mass detection was under the multiple reaction monitoring(MRM)mode via polarity switching between negative and positive ionization modes.The calibration curves exhibited good linearity(r>0.997)for all components.The lower limit of quantitation was in the range of 1 e10 ng/m L.The intra-day and inter-day precisions(RSD)at three different levels were both less than 12.2%and the accuracies(RE)ranged fromà10.1%to 16.4%.The extraction recovery of them ranged from 53.8%to 99.7%.Pharmacokinetic results indicated the bioavailability of three iridoid glycosides and the metabolite,genipin in normal rats was higher than that in rats exposed to isoflavones.With the longer time of administration of isoflavones,plasma concentrations of iridoids decreased,while genipin sulfate,the phase II metabolite of genposide and genipin-1-gentiobioside,appeared the rising exposure.The pharmacokinetic profiles of main iridoids from GF were altered by isoflavones.展开更多
Two new iridoids (1 and 2) were isolated from the roots of Patrinia rupestris (Pail.) Juss. Their structures were elucidated by spectroscopic methods. Compounds 1 and 2 exhibited strong antibacterial activities ag...Two new iridoids (1 and 2) were isolated from the roots of Patrinia rupestris (Pail.) Juss. Their structures were elucidated by spectroscopic methods. Compounds 1 and 2 exhibited strong antibacterial activities against Eschecichia coli and Staphylococcus aureus, respectively.展开更多
The investigation of Morinda officinalis led to the isolation of twelve compounds(1-12),including three new iridoid glycosides morindallns A-C(1-3)and nine known compounds(4-12).Their structural identifications were c...The investigation of Morinda officinalis led to the isolation of twelve compounds(1-12),including three new iridoid glycosides morindallns A-C(1-3)and nine known compounds(4-12).Their structural identifications were conducted using HRMS,1D and 2D NMR,and electronic circular dichroism(ECD)spectra as well as quantum chemical computations.Compound 6 displayed the most significantly agonistic activity against farnesoid X receptor(FXR)with an EC_(50) value of 7.18 μM,and its agonistic effect was verified through the investigation of FXR downstream target genes including small heterodimer partner 1(SHP1),bile salt export pump(BSEP),and organic solute transporter subunit alpha and beta(OSTα and OSTβ).The potential interaction of compound 6 with FXR was analyzed by molecular docking and molecular dynamics stimulation,revealing that amino acid residues Leu287;Thr288,and Ser332 played a crucial role in the activation of compound 6 towards FXR.These findings suggested that compound 6 could be regarded as a potential candidate for the development of FXR agonists.展开更多
The whole plant with root ofHedyotis diffusa Willd. (AE) has been demonstrated to have anti-inflammatory, antioxidant, and anti-bacterial activities. In our study, we aim to examine the anti-tumor effect of alcoholi...The whole plant with root ofHedyotis diffusa Willd. (AE) has been demonstrated to have anti-inflammatory, antioxidant, and anti-bacterial activities. In our study, we aim to examine the anti-tumor effect of alcoholic extract of AE in mice implanted with sarcoma S180 cells (SBT mice). We also compared the immune system function and the life span of SBT mice with that of control mice. We found that AE displayed a significant inhibitory effect on solid tumor growth, as well as increased the life span. At the dose of 10 mg/kg body weight, both tumor weight and volume were decreased significantly. We also measured several immune fimction markers, inlcuding spleen index (SI), thymus index (TI) and parameters of hematological. We observed no reduce in these markers, indicatine that AE could inhibit tumor ~rowth without affectino immune function in SBT ,nice.展开更多
A new glycoside named 6β-O-β-D-glucosylpaederosidic acid(1) was isolated from Paederia scandens and its structure was elucidated on the basis of spectroscopic and chemical evidence,together with four known iridoids,...A new glycoside named 6β-O-β-D-glucosylpaederosidic acid(1) was isolated from Paederia scandens and its structure was elucidated on the basis of spectroscopic and chemical evidence,together with four known iridoids,paederoside(2),paederosidic acid(3),paederosidic acid methyl ester(4),and deacetyl asperulosidic acid methyl ester(5).Compound 5 was isolated from this plant for the first time.展开更多
In order to observe the effects of the ground and intact Zhi Zi (Fructus Gardeniae) and different combinations of the ingredients and refined single Chinese drug granules in Yin Chen Hao Decoction compound prescriptio...In order to observe the effects of the ground and intact Zhi Zi (Fructus Gardeniae) and different combinations of the ingredients and refined single Chinese drug granules in Yin Chen Hao Decoction compound prescription on the contents of gardenoside (an effective component of the prescription), the contents of gardenoside were determined with reversed phase high performance liquid chromatography (HPLC), with acetonitrile-water (15:85) as mobile phase, at wave length 238nm. The results indicated that the gardenoside-decocted-out rates in the decoctions prepared by different combinations of the ingredients with the ground Zhi Zi (Fructus Gardeniae) all were higher significantly than those in the decoction with intact Zhi Zi (Fructus Gardeniae), and generally, different combinations of the ingredients in the decoction had only little effect on the gardenoside-decocted-out rate.展开更多
A new ceramide, (2S,3S,4R, 10E)-2-[(2'R)-2'-hydroxytetracosanoyl amino]-10-octadecene-1, 3,4-triol (1), together with twelve known compounds, cerebroside A, cerebroside B, cerebroside D, cytochalasin D, epoxyc...A new ceramide, (2S,3S,4R, 10E)-2-[(2'R)-2'-hydroxytetracosanoyl amino]-10-octadecene-1, 3,4-triol (1), together with twelve known compounds, cerebroside A, cerebroside B, cerebroside D, cytochalasin D, epoxycytochalasin D, cytochalasin C, loganin, cerevisterol, ergosta-7,22-dien-3beta, 5alpha, 6alpha-triol, ergosta-4,6,8(14),22-tetraen-3-one, ergosterol peroxide and ergosta-5,7,22-trien-3-ol, was isolated from ethyl acetate fraction of Engleromyces goetzei P. Henn. The structure of new ceramide (1) was elucidated by spectral data and chemical method, especially by 2D-NMR techniques. All of the compounds except cytochalasin D were first obtained from this fungus.展开更多
A new iridoid was isolated from the 80% ethanol extract of the whole plant of Incarvillea delavayi. Its structure was defined, and named incarvillic acid, on the basis of spectral evidences.
A new iridoid glycoside, 6'-O-sinapoylgeniposide, was isolated from Gardeniajasminoides Ellis and its structure was elucidated on the basis of 1D and 2D NMR, HR-ESI-MS techniques.
Chemical study on the roots of Gentiana crassicaulis Duthie ex Burk(Gentianaceae)afforded 15 compounds,including two new iridoid glycosides,qinjiaosides B(1)and C(2).Their structures were elucidated by spectroscopic m...Chemical study on the roots of Gentiana crassicaulis Duthie ex Burk(Gentianaceae)afforded 15 compounds,including two new iridoid glycosides,qinjiaosides B(1)and C(2).Their structures were elucidated by spectroscopic methods and chemical evidence.The isolated iridoid glycosides 1,4-6 and 8-11 were tested for their anti-inflammatory activity by the inhibitory effects on LPS-induced NO and TNF-αproduction in macrophage RAW264.7 cells.All of them showed inhibitory effects on inflammatory mediators NO at a concentration of 15μM,while 5 and 9 displayed the most potential inhibitory effects on TNF-awith IC50 of 0.06 and 0.05μM,respectively.The structure-activity relationships(SARs)of these iridoid derivatives were discussed.展开更多
Two new epimeric pairs of iridoid scyphiphin A1 (la), A2 (lb) and scyphiphin B 1 (2a), B2 (2b) were isolated from Scyphiphora hydrophyllacea Gaertn. F. Their structures were elucidated by spectroscopic methods...Two new epimeric pairs of iridoid scyphiphin A1 (la), A2 (lb) and scyphiphin B 1 (2a), B2 (2b) were isolated from Scyphiphora hydrophyllacea Gaertn. F. Their structures were elucidated by spectroscopic methods. The mixture of scyphiphin B 1 and scyphiphin B2 showed moderate cytotoxicity against human hepatoma SMMC-7721 cell line in vitro by MTT method.展开更多
Tau oligomers are the etiologic molecules of Alzheimer disease(AD), and correlate strongly with neuronal loss and exhibit neurotoxicity. Recent evidence indicates that small tau oligomers are the most relevant toxic a...Tau oligomers are the etiologic molecules of Alzheimer disease(AD), and correlate strongly with neuronal loss and exhibit neurotoxicity. Recent evidence indicates that small tau oligomers are the most relevant toxic aggregate species. The aim of the present study was to investigate the mechanisms of cornel iridoid glycoside(CIG) on tau oligomers and cognitive functions. We injected wortmannin and GF-109203 X(WM/GFX, 200 μmol·L-1 each) into the lateral ventricles to induce tau oligomer and memory impairment in rats. When oral y administered with CIG at 60 and 120 mg·kg-1 per day for 14 d, CIG decreased the escape latency in Morris water maze test. We also found that CIG restored the expression of presynaptic p-synapsin, synaptophysin, and postsynaptic density-95(PSD-95) decreased by WM/GFX in rat cortex. CIG reduced the accumulation of tau oligomers in the brain of WM/GFX rats and in cells transfected with wild type glycogen synthase kinase-3β(wt GSK-3β). In addition, CIG up-regulated the levels of ATG7, ATG12, Beclin-1, and LC3 II in vivo and in vitro, suggesting the restoration of autophagy function. These results suggest that CIG could ameliorate memory deficits and regulate memory-associated synaptic proteins through the clearance of tau oligomers accumulation. Moreover, CIG clears tau oligomers by restoring autophagy function.展开更多
A new iridoid glycoside 1 and a new iridoid 2 were isolated from the whole plant of Pedicularis kansuensis f. albiflora. Their structures were elucidated by spectroscopie methods.
Aim To study the chemical constituents of Buddleja lindeyana. Methods The constituents were separated and purified by different methods of chromatography, and their structures were elucidated by IR, MS and NMR. Result...Aim To study the chemical constituents of Buddleja lindeyana. Methods The constituents were separated and purified by different methods of chromatography, and their structures were elucidated by IR, MS and NMR. Results Three iridoid glycosides and two other compounds were isolated from Buddleja lindeyana. Their structures were elucidated to be 6-O-feruloylajugol ( 1 ), erythro-6-oxo-4′-( 3-methoxyl-4-hydroxyphenylglycol-8')-feruloylaj-ugol ( 2 ), threo-6-oxo-4′-(3-methoxyl-4-hydroxyphenylglycol-8')-feruloylajugol ( 3 ), tetra-cosanoic acid 2,3-dihydroxypropyl ester (4), and galactitol (5). Conclusion All the compounds have been isolated from this plant for the first time. Compounds 1, 2 and 3 have protective effect agains MPP+ -induced apoptosis.展开更多
A rapid and validated UPLC-MS method was developed for investigating the absorbed components of Paederia scandens(Lour.) Merrill(P.scandens) in rat plasma.The bioactive constituents in plasma samples from rats adminis...A rapid and validated UPLC-MS method was developed for investigating the absorbed components of Paederia scandens(Lour.) Merrill(P.scandens) in rat plasma.The bioactive constituents in plasma samples from rats administrated orally with P.scandens extract were analyzed by Ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS).Four prototype compounds were identified in rat serum as potential bioactive components of P.scandens by comparing their retention times and mass spectrometry data or by mass spectrometry analysis and retrieving the reference literatures.Glucuronidation after deglycosylation was the major metabolic pathway for the iridoid glycosides in P.scandens.These results showed that the methods had high sensitivity and resolution and were suitable for identifying the bioactive constituents in plasma after oral administration of P.scandens.providing helpful chemical information for further pharmacological and mechanistic researched on the P.scandens.展开更多
rTg4510 mice are transgenic mice expressing P301L mutant tau and have been developed as an animal model of tauopathies including Alzheimer’s disease(AD).Besides cognitive impairments,rTg4510 mice also show abnormal h...rTg4510 mice are transgenic mice expressing P301L mutant tau and have been developed as an animal model of tauopathies including Alzheimer’s disease(AD).Besides cognitive impairments,rTg4510 mice also show abnormal hyperactivity behavior.Cornel iridoid glycoside(CIG)is an active ingredient extracted from Cornus officinalis,a traditional Chinese herb.The purpose of the present study was to investigate the effects of CIG on the emotional disorders such as hyperactivity,and related mechanisms.The emotional hyperactivity was detected by locomotor activity test and Y maze test.Immunofluorescent and immunohistochemical analyses were conducted to measure neuron loss and phosphorylated tau.Western blotting was used to detect the expression of related proteins.The results showed that intragastric administration of CIG for 3 months decreased the hyperactivity phenotype,prevented neuronal loss,reduced tau hyperphosphorylation and aggregation in the amygdala of rTg4510 mice.Meanwhile,CIG alleviated the synaptic dysfunction by increasing the expression of N-methyl-D-aspartate receptors(NMDARs)subunits GluN1 and GluN2A andαamino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptor(AMPAR)subunits GluA1 and GluA2,and increased the level of phosphorylated Ca2+/calmodulin dependent protein kinase IIα(p-CaMK IIα)in the brain of rTg4510 mice.In conclusion,CIG may have potential to treat the emotional disorders in tauopathies such as AD through reducing tau pathology and improving synaptic dysfunction.展开更多
Two new iridoid glucosides, serratoside A and serratoside B, were isolated from the aerial parts of Clerodendrum serratum var. amplexifolium Moldenke. Their structures were elucidated by spectral and chemical methods.
AIM: To study the gastroprotective effect and in vivo antioxidant potential of a standardized iridoid fraction from B. prionitis leaves(BPE) against different gastric ulcer models in rats. METHOD: The standardized iri...AIM: To study the gastroprotective effect and in vivo antioxidant potential of a standardized iridoid fraction from B. prionitis leaves(BPE) against different gastric ulcer models in rats. METHOD: The standardized iridoid fraction from BPE at 50, 100, and 200 mg/kg body weight was administered orally, twice daily for 5 days for prevention from aspirin, ethanol, cold-restraint stress(CRS), and pylorus ligation(PL)-induced ulcers. Estimation of the antioxidant enzyme activity was carried out in a CRS-induced ulcer model, and various gastric secretion parameters including volume of gastric juice, acid output, and pH value were estimated in the PL-induced ulcer model. RESULTS: BPE showed a dose-dependent ulcer protective effect in PL(18.67%–66.26% protection), aspirin(24.65%–63.25% protection), CRS(20.77%–59.42% protection), and EtOH(16.93%–77.04% protection)-induced ulcers. BPE treatment in PL-rats showed a decrease in acid-pepsin secretion, and enhanced mucin and mucosal glycoproteins. However, BPE reduced the ulcer index with significant decrease in LPO(P < 0.01–0.001), SOD(P < 0.01–0.001), and an increase in CAT(P < 0.01–0.001), activity in the CRS-induced model. CONCLUSION: The data shows that the iridoid fraction from BPE possesses anti-ulcerogenic and antioxidant potential.展开更多
基金supported by grants from the National Natural Science Foundation of China (No.82074400)key projects supported by the National Natural Science Foundation of China and Joint Fund for Regional Innovation and Development (No.U21A20411)。
文摘In recent years,preclinical research on diabetic kidney disease (DKD) has surged to the forefront of scientific and clinical attention.DKD has become a pervasive complication of type 2 diabetes.Given the complexity of its etiology and pathological mechanisms,current interventions,including drugs,dietary modifications,exercise,hypoglycemic treatments and lipid-lowering methods,often fall short in achieving desired therapeutic outcomes.Iridoids,primarily derived from the potent components of traditional herbs,have been the subject of long-standing research.Preclinical data suggest that iridoids possess notable renal protective properties;however,there has been no summary of the research on their efficacy in the management and treatment of DKD.This article consolidates findings from in vivo and in vitro research on iridoids in the context of DKD and highlights their shared anti-inflammatory activities in treating this condition.Additionally,it explores how certain iridoid components modify their chemical structures through the regulation of intestinal flora,potentially bolstering their therapeutic effects.This review provides a focused examination of the mechanisms through which iridoids may prevent or treat DKD,offering valuable insights for future research endeavors.
基金financially supported by National Natural Sciences Foundation of China(No.81222051)Scientific Research Project of Traditional Chinese Medicine(No.201307002)National Key Technology R&D Program “New Drug Innovation”of China(Nos.2012ZX09301002-002-002,2012ZX09304-005)
文摘In order to determine the chemical constituents of Cistanche deserticola cultured in Tarim desert,a systematically phytochemical investigation was carried out.The constituents were isolated by silica gel,Sephadex LH-20,MCI gel,ODS column chromatography,and semi-preparative HPLC.Their structures were determined on the basis of MS and NMR spectroscopic analyses,by chemical methods,and/or comparison with literature data.The anti-inflammatory activities of the isolates were evaluated for their inhibitory effects on the lipopolysaccharide(LPS)-induced nitric oxide(NO)production in BV-2 mouse microglial cells.Nine iridoids were isolated and identified as cistadesertoside A(1),cistanin(2),cistachlorin(3),6-deoxycatalpol(4),gluroside(5),kankanoside A(6),ajugol(7),bartsioside(8),and 8-epi-loganic acid(9).Compound 9 exhibited potent inhibition on the NO production with an IC_(50) value being 5.2 μmol·L^(-1),comparable to the positive control quercetin(4.3 μmol·L^(-1)).Compound 1 was a new iridoid,and compounds 5,6,and 8 were isolated from this species for the first time.
基金the National Natural Science Foundation of China(grant numbers 81573584,81773862)。
文摘Gardeniae Fructus(GF)and Semen Sojae Praeparatum(SSP)are both medicine food homologies and widely used in Chinese clinical prescriptions together.The research investigated the pharmacokinetics of four iridoids in normal rats and isolfavones-fed rats,which were administered with isolfavones from SSP for 7,14,21 and 28 consecutive days.A validated LC-MS/MS method was developed for determining shanzhiside,genipin-1-gentiobioside,geniposide and their metabolite genipin in rat plasma.Plasma samples were pretreated by solid-phase extraction using paeoniflorin as the internal standard.The chromatographic separation was performed on a Waters Atlantis T3(4.6 mm×150 mm,3 mm)column using a gradient mobile phase consisting of acetonitril and water(containing 0.06%acetic acid).The mass detection was under the multiple reaction monitoring(MRM)mode via polarity switching between negative and positive ionization modes.The calibration curves exhibited good linearity(r>0.997)for all components.The lower limit of quantitation was in the range of 1 e10 ng/m L.The intra-day and inter-day precisions(RSD)at three different levels were both less than 12.2%and the accuracies(RE)ranged fromà10.1%to 16.4%.The extraction recovery of them ranged from 53.8%to 99.7%.Pharmacokinetic results indicated the bioavailability of three iridoid glycosides and the metabolite,genipin in normal rats was higher than that in rats exposed to isoflavones.With the longer time of administration of isoflavones,plasma concentrations of iridoids decreased,while genipin sulfate,the phase II metabolite of genposide and genipin-1-gentiobioside,appeared the rising exposure.The pharmacokinetic profiles of main iridoids from GF were altered by isoflavones.
文摘Two new iridoids (1 and 2) were isolated from the roots of Patrinia rupestris (Pail.) Juss. Their structures were elucidated by spectroscopic methods. Compounds 1 and 2 exhibited strong antibacterial activities against Eschecichia coli and Staphylococcus aureus, respectively.
基金the National Natural Science Foundation of China(No.81703679)the Liaoning Provincial Key Research and Development Program(No.2019JH2/10300022)+1 种基金the Natural Science Foundation of Liaoning Province(No.2020-MS-256)the Dalian Young Star of Science and Tech nology(Nos.2019RQ123 and 2019RQ116).
文摘The investigation of Morinda officinalis led to the isolation of twelve compounds(1-12),including three new iridoid glycosides morindallns A-C(1-3)and nine known compounds(4-12).Their structural identifications were conducted using HRMS,1D and 2D NMR,and electronic circular dichroism(ECD)spectra as well as quantum chemical computations.Compound 6 displayed the most significantly agonistic activity against farnesoid X receptor(FXR)with an EC_(50) value of 7.18 μM,and its agonistic effect was verified through the investigation of FXR downstream target genes including small heterodimer partner 1(SHP1),bile salt export pump(BSEP),and organic solute transporter subunit alpha and beta(OSTα and OSTβ).The potential interaction of compound 6 with FXR was analyzed by molecular docking and molecular dynamics stimulation,revealing that amino acid residues Leu287;Thr288,and Ser332 played a crucial role in the activation of compound 6 towards FXR.These findings suggested that compound 6 could be regarded as a potential candidate for the development of FXR agonists.
文摘The whole plant with root ofHedyotis diffusa Willd. (AE) has been demonstrated to have anti-inflammatory, antioxidant, and anti-bacterial activities. In our study, we aim to examine the anti-tumor effect of alcoholic extract of AE in mice implanted with sarcoma S180 cells (SBT mice). We also compared the immune system function and the life span of SBT mice with that of control mice. We found that AE displayed a significant inhibitory effect on solid tumor growth, as well as increased the life span. At the dose of 10 mg/kg body weight, both tumor weight and volume were decreased significantly. We also measured several immune fimction markers, inlcuding spleen index (SI), thymus index (TI) and parameters of hematological. We observed no reduce in these markers, indicatine that AE could inhibit tumor ~rowth without affectino immune function in SBT ,nice.
基金supported by the National Natural Sciences Foundation of China(No.20876126)Southwest University for Nationalities Foundation for doctors(No.26701001)
文摘A new glycoside named 6β-O-β-D-glucosylpaederosidic acid(1) was isolated from Paederia scandens and its structure was elucidated on the basis of spectroscopic and chemical evidence,together with four known iridoids,paederoside(2),paederosidic acid(3),paederosidic acid methyl ester(4),and deacetyl asperulosidic acid methyl ester(5).Compound 5 was isolated from this plant for the first time.
文摘In order to observe the effects of the ground and intact Zhi Zi (Fructus Gardeniae) and different combinations of the ingredients and refined single Chinese drug granules in Yin Chen Hao Decoction compound prescription on the contents of gardenoside (an effective component of the prescription), the contents of gardenoside were determined with reversed phase high performance liquid chromatography (HPLC), with acetonitrile-water (15:85) as mobile phase, at wave length 238nm. The results indicated that the gardenoside-decocted-out rates in the decoctions prepared by different combinations of the ingredients with the ground Zhi Zi (Fructus Gardeniae) all were higher significantly than those in the decoction with intact Zhi Zi (Fructus Gardeniae), and generally, different combinations of the ingredients in the decoction had only little effect on the gardenoside-decocted-out rate.
文摘A new ceramide, (2S,3S,4R, 10E)-2-[(2'R)-2'-hydroxytetracosanoyl amino]-10-octadecene-1, 3,4-triol (1), together with twelve known compounds, cerebroside A, cerebroside B, cerebroside D, cytochalasin D, epoxycytochalasin D, cytochalasin C, loganin, cerevisterol, ergosta-7,22-dien-3beta, 5alpha, 6alpha-triol, ergosta-4,6,8(14),22-tetraen-3-one, ergosterol peroxide and ergosta-5,7,22-trien-3-ol, was isolated from ethyl acetate fraction of Engleromyces goetzei P. Henn. The structure of new ceramide (1) was elucidated by spectral data and chemical method, especially by 2D-NMR techniques. All of the compounds except cytochalasin D were first obtained from this fungus.
文摘A new iridoid was isolated from the 80% ethanol extract of the whole plant of Incarvillea delavayi. Its structure was defined, and named incarvillic acid, on the basis of spectral evidences.
基金supported by the National Natural Science Foundation of China(No.30600805)supported by Program for New Century Excellent Talents in University(No.NCET-06-0497).
文摘A new iridoid glycoside, 6'-O-sinapoylgeniposide, was isolated from Gardeniajasminoides Ellis and its structure was elucidated on the basis of 1D and 2D NMR, HR-ESI-MS techniques.
基金This work was supported by the Science&Technology Planning Project of Yunnan Province(2010CD106)the 973 Program of Ministry of Science&Technology of China(2011CB915503)+2 种基金the State Key Laboratory of Phytochemistry and Plant Resources in West China,Chinese Academy of Sciences(CAS)(P2010-ZZ03)the Fourteenth Candidates of the Young Academic Leaders of Yunnan Province(Min XU,2011CI044)the West Light program of CAS.
文摘Chemical study on the roots of Gentiana crassicaulis Duthie ex Burk(Gentianaceae)afforded 15 compounds,including two new iridoid glycosides,qinjiaosides B(1)and C(2).Their structures were elucidated by spectroscopic methods and chemical evidence.The isolated iridoid glycosides 1,4-6 and 8-11 were tested for their anti-inflammatory activity by the inhibitory effects on LPS-induced NO and TNF-αproduction in macrophage RAW264.7 cells.All of them showed inhibitory effects on inflammatory mediators NO at a concentration of 15μM,while 5 and 9 displayed the most potential inhibitory effects on TNF-awith IC50 of 0.06 and 0.05μM,respectively.The structure-activity relationships(SARs)of these iridoid derivatives were discussed.
文摘Two new epimeric pairs of iridoid scyphiphin A1 (la), A2 (lb) and scyphiphin B 1 (2a), B2 (2b) were isolated from Scyphiphora hydrophyllacea Gaertn. F. Their structures were elucidated by spectroscopic methods. The mixture of scyphiphin B 1 and scyphiphin B2 showed moderate cytotoxicity against human hepatoma SMMC-7721 cell line in vitro by MTT method.
文摘Tau oligomers are the etiologic molecules of Alzheimer disease(AD), and correlate strongly with neuronal loss and exhibit neurotoxicity. Recent evidence indicates that small tau oligomers are the most relevant toxic aggregate species. The aim of the present study was to investigate the mechanisms of cornel iridoid glycoside(CIG) on tau oligomers and cognitive functions. We injected wortmannin and GF-109203 X(WM/GFX, 200 μmol·L-1 each) into the lateral ventricles to induce tau oligomer and memory impairment in rats. When oral y administered with CIG at 60 and 120 mg·kg-1 per day for 14 d, CIG decreased the escape latency in Morris water maze test. We also found that CIG restored the expression of presynaptic p-synapsin, synaptophysin, and postsynaptic density-95(PSD-95) decreased by WM/GFX in rat cortex. CIG reduced the accumulation of tau oligomers in the brain of WM/GFX rats and in cells transfected with wild type glycogen synthase kinase-3β(wt GSK-3β). In addition, CIG up-regulated the levels of ATG7, ATG12, Beclin-1, and LC3 II in vivo and in vitro, suggesting the restoration of autophagy function. These results suggest that CIG could ameliorate memory deficits and regulate memory-associated synaptic proteins through the clearance of tau oligomers accumulation. Moreover, CIG clears tau oligomers by restoring autophagy function.
文摘A new iridoid glycoside 1 and a new iridoid 2 were isolated from the whole plant of Pedicularis kansuensis f. albiflora. Their structures were elucidated by spectroscopie methods.
文摘Aim To study the chemical constituents of Buddleja lindeyana. Methods The constituents were separated and purified by different methods of chromatography, and their structures were elucidated by IR, MS and NMR. Results Three iridoid glycosides and two other compounds were isolated from Buddleja lindeyana. Their structures were elucidated to be 6-O-feruloylajugol ( 1 ), erythro-6-oxo-4′-( 3-methoxyl-4-hydroxyphenylglycol-8')-feruloylaj-ugol ( 2 ), threo-6-oxo-4′-(3-methoxyl-4-hydroxyphenylglycol-8')-feruloylajugol ( 3 ), tetra-cosanoic acid 2,3-dihydroxypropyl ester (4), and galactitol (5). Conclusion All the compounds have been isolated from this plant for the first time. Compounds 1, 2 and 3 have protective effect agains MPP+ -induced apoptosis.
基金supported by the National Natural Science Foundation(Nos.81274013 and 81473315)the National Natural foundationof the major program of China(No.81130069)+1 种基金the Chinese National S&T Special Project on Major New Drug Innovation(No.2011ZX09307-002-01)the program for Changjiang Scholars and Innovative Research Team in University of Ministry of Education of China(No.IRT1140)
文摘A rapid and validated UPLC-MS method was developed for investigating the absorbed components of Paederia scandens(Lour.) Merrill(P.scandens) in rat plasma.The bioactive constituents in plasma samples from rats administrated orally with P.scandens extract were analyzed by Ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS).Four prototype compounds were identified in rat serum as potential bioactive components of P.scandens by comparing their retention times and mass spectrometry data or by mass spectrometry analysis and retrieving the reference literatures.Glucuronidation after deglycosylation was the major metabolic pathway for the iridoid glycosides in P.scandens.These results showed that the methods had high sensitivity and resolution and were suitable for identifying the bioactive constituents in plasma after oral administration of P.scandens.providing helpful chemical information for further pharmacological and mechanistic researched on the P.scandens.
基金This research was supported by National Natural Science Foundation of China(Nos.81473373,81874351,81673406)Capital Science and Technology Leading Talent Training Project(No.Z 191100006119017)+1 种基金Beijing Hospitals Authority Ascent Plan(No.DFL20190803)Cultivation Fund of Capital Medical University(No.PYZ19134).
文摘rTg4510 mice are transgenic mice expressing P301L mutant tau and have been developed as an animal model of tauopathies including Alzheimer’s disease(AD).Besides cognitive impairments,rTg4510 mice also show abnormal hyperactivity behavior.Cornel iridoid glycoside(CIG)is an active ingredient extracted from Cornus officinalis,a traditional Chinese herb.The purpose of the present study was to investigate the effects of CIG on the emotional disorders such as hyperactivity,and related mechanisms.The emotional hyperactivity was detected by locomotor activity test and Y maze test.Immunofluorescent and immunohistochemical analyses were conducted to measure neuron loss and phosphorylated tau.Western blotting was used to detect the expression of related proteins.The results showed that intragastric administration of CIG for 3 months decreased the hyperactivity phenotype,prevented neuronal loss,reduced tau hyperphosphorylation and aggregation in the amygdala of rTg4510 mice.Meanwhile,CIG alleviated the synaptic dysfunction by increasing the expression of N-methyl-D-aspartate receptors(NMDARs)subunits GluN1 and GluN2A andαamino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptor(AMPAR)subunits GluA1 and GluA2,and increased the level of phosphorylated Ca2+/calmodulin dependent protein kinase IIα(p-CaMK IIα)in the brain of rTg4510 mice.In conclusion,CIG may have potential to treat the emotional disorders in tauopathies such as AD through reducing tau pathology and improving synaptic dysfunction.
基金the National Natural Science Foundation of China ! 29772039
文摘Two new iridoid glucosides, serratoside A and serratoside B, were isolated from the aerial parts of Clerodendrum serratum var. amplexifolium Moldenke. Their structures were elucidated by spectral and chemical methods.
文摘AIM: To study the gastroprotective effect and in vivo antioxidant potential of a standardized iridoid fraction from B. prionitis leaves(BPE) against different gastric ulcer models in rats. METHOD: The standardized iridoid fraction from BPE at 50, 100, and 200 mg/kg body weight was administered orally, twice daily for 5 days for prevention from aspirin, ethanol, cold-restraint stress(CRS), and pylorus ligation(PL)-induced ulcers. Estimation of the antioxidant enzyme activity was carried out in a CRS-induced ulcer model, and various gastric secretion parameters including volume of gastric juice, acid output, and pH value were estimated in the PL-induced ulcer model. RESULTS: BPE showed a dose-dependent ulcer protective effect in PL(18.67%–66.26% protection), aspirin(24.65%–63.25% protection), CRS(20.77%–59.42% protection), and EtOH(16.93%–77.04% protection)-induced ulcers. BPE treatment in PL-rats showed a decrease in acid-pepsin secretion, and enhanced mucin and mucosal glycoproteins. However, BPE reduced the ulcer index with significant decrease in LPO(P < 0.01–0.001), SOD(P < 0.01–0.001), and an increase in CAT(P < 0.01–0.001), activity in the CRS-induced model. CONCLUSION: The data shows that the iridoid fraction from BPE possesses anti-ulcerogenic and antioxidant potential.