Objective To investigate the antidepressant effects of Yuanzhi(Polygalae Radix;PR)aqueous extract on chronic unpredictable mild stress(CUMS)-induced depression rat models and the underlying mechanisms.Methods A total ...Objective To investigate the antidepressant effects of Yuanzhi(Polygalae Radix;PR)aqueous extract on chronic unpredictable mild stress(CUMS)-induced depression rat models and the underlying mechanisms.Methods A total of 40 male Sprague Dawley(SD)rats were randomly divided into control;model;low dose of PR(PR-L;0.5 g/kg);high dose of PR(PR-H;1 g/kg);and fluoxetine(10 mg/kg)groups;with 8 rats in each group.Except for the rats in control group;those in the other four groups underwent CUMS-induced depression modeling.PR and fluoxetine were administered intragastrically once daily;30 min prior to the CUMS procedure;for 14 consecu-tive days until the behavioral tests were performed.After CUMS modeling;the sucrose prefer-ence test(SPT);open field test(OFT);novelty-suppressed feeding test(NSFT);forced swim test(FST);and tail suspension test(TST)were employed to assess the pharmacological ef-fects of PR on the mitigation of depressive-like behaviors in rat models.Additionally;the en-zyme-linked immunosorbent assay(ELISA)was utilized to quantify the serum levels of tumor necrosis factor(TNF)-α;interleukin(IL)-6;and IL-1βin the rats.Western blot analysis was al-so conducted to evaluate the protein expression levels of nuclear factor kappa-B(NF-κB);in-ducible nitric oxide synthase(iNOS);cyclooxygenase-2(COX-2);nucleotide-binding oligomerization domain(NOD)-like receptor family pyrin domain containing 3(NLRP3);apoptosis-associated speck-like protein containing caspase recruitment domain(ASC);and caspase-1 in the hippocampal tissues of the rats.Immunofluorescence staining was per-formed to observe the morphological changes in ionized calcium-binding adapter molecule 1 positive(Iba-1+)cells in the dentate gyrus(DG)of rats with CUMS-induced depression.Results(i)Treatment with PR-H and fluoxetine resulted in significant enhancements in both the total distance and time the rats moved during tests(P<0.01 and P<0.05;respectively).Post-administration of PR-H and fluoxetine also led to statistically significant increase in su-crose preference among rats(P<0.05).Besides;PR-L;PR-H;and fluoxetine treatment markedly decreased the latency of ingestion(P<0.05;P<0.05;and P<0.01;respectively).As observed from the FST;PR-L;PR-H;and fluoxetine presented antidepressant effects on rats with CUMS-induced depression;leading to the reduction in time of their immobility(P<0.05;P<0.01;and P<0.01;respectively).The results of TST indicated reduced immobility time in rats receiving PR-H and fluoxetine treatment as well(P<0.01).(ii)Rats in model group showed an increase in the levels of Iba-1+microglia in their left and right brains in compari-son with control group(P<0.01).However;such increase was negated post PR treatment(P<0.01).Treatment with PR-L;PR-H;and fluoxetine considerably reduced the levels of inflam-matory factors(TNF-α;IL-1β;and IL-6;P<0.01).In addition;treatment of PR-L and PR-H ef-fectively counteracted the elevated levels of NLRP3;ASC;and caspase-1;and markedly down-regulated the expression levels of phosphorylated p65(p-p65);COX-2;and iNOS in rats’hip-pocampus(P<0.01).Conclusion Collectively;these findings indicate that PR exerts an antidepressant effect on rats with CUMS-induced depression partially through the modulation of the NLRP3 and NF-κB signaling pathways.展开更多
Polygala tenuifolia,commonly known as Yuanzhi(YZ)in Chinese,has been shown to possess antiinsomnia properties.However,the material basis and the mechanism underlying its sedative-hypnotic effects remain unclear.Herein...Polygala tenuifolia,commonly known as Yuanzhi(YZ)in Chinese,has been shown to possess antiinsomnia properties.However,the material basis and the mechanism underlying its sedative-hypnotic effects remain unclear.Herein,we investigated the active components and neurochemical mechanism of YZ extracts using liquid chromatography tandem mass spectrometry(LC-MS/MS)-based pharmacometabolomics and mass spectrometry imaging(MSI)-based spatial resolved metabolomics.According to the results,17 prototypes out of 101 ingredients in the YZ extract were detected in both the plasma and brain,which might be the major components contributing to the sedative-hypnotic effects.Network pharmacology analysis revealed that these prototypes may exert their effects through neuroactive ligand-receptor interaction,serotonergic synapse,dopaminergic synapse,and dopaminergic synapse,among other pathways.LC-MS/MS-based targeted metabolomics and Western blot(WB)revealed that tryptophan-serotonin-melatonin(Trp-5-HT-Mel)and tyrosine-norepinephrine-adrenaline(Tyr-Ne-Ad)are the key regulated pathways.Dopa decarboxylase(DDC)upregulation and phenylethanolamine Nmethyltransferase(PNMT)downregulation further confirmed these pathways.Furthermore,MSI-based spatially resolved metabolomics revealed notable alterations in 5-HT in the pineal gland(PG),and Ad in the brainstem,including the middle brain(MB),pons(PN),and hypothalamus(HY).In summary,this study illustrates the efficacy of an integrated multidimensional metabolomics approach in unraveling the sedative-hypnotic effects and neurochemical mechanisms of a Chinese herbal medicine,YZ.展开更多
[Objectives]To explore the effects of Polygona fallax Hemsl water extract on gastrointestinal motility in normal mice and gastric motility disorder model mice and approximate mechanism.[Methods]Using normal mice and m...[Objectives]To explore the effects of Polygona fallax Hemsl water extract on gastrointestinal motility in normal mice and gastric motility disorder model mice and approximate mechanism.[Methods]Using normal mice and mice with gastric motility disorders(modeled with atropine),the effects of different mass concentration groups of P.fallax Hemsl water extract(0.125,0.250,0.500 g/mL)and domperidone groups on gastric residual rate,small intestine propulsion rate,serum motilin(MLT),vasoactive intestinal peptide(VIP),and tissue morphology were studied.[Results]There was a highly significant difference(P<0.01)in the small intestine propulsion rate of liquid in normal mice among the different concentration groups of P.fallax Hemsl water extract compared to the blank group.The small intestine propulsion rate and gastric residue rate of semi-solid paste were statistically significant compared to the blank group(P<0.05).Among them,there was a highly significant difference between the high concentration group(67.75%±7.65%,46.5%±10.62%)and the medium concentration group(60.90%±5.87%,59.27%±7.82%)(P<0.01).There was statistical significance in normal mouse serum MLT content in the high concentration group(P<0.05).There was no effect on serum VIP levels in normal mice;no effect on the morphology of stomach and intestinal tissues of normal mice.The small intestine propulsion rate and gastric residue rate of liquid and semi-solid paste in mice with gastric motility disorders were statistically significant compared to the atropine group,with extremely significant differences(P<0.01).[Conclusions]P.fallax Hemsl water extract has a promoting effect on gastrointestinal motility.One of the specific mechanisms by which P.fallax Hemsl promotes gastrointestinal motility in normal mice may be related to the content of MLT in mouse serum.The mechanism of action in atropine induced gastric paresis mice may be related to the reactivation of M receptors,and the action mechanism of P.fallax Hemsl does not change the original histological basis.It can be inferred that P.fallax Hemsl water extract has a synergistic effect on promoting gastrointestinal motility through other mechanisms,but it is not fully understood and further in-depth research is needed.展开更多
The aim of this study was to isolate the chemical constituents of the aerial parts of Polygala tenuifolia Willd. and to determine their antioxidant activities. Ten flavonoids were isolated and purified by silica gel, ...The aim of this study was to isolate the chemical constituents of the aerial parts of Polygala tenuifolia Willd. and to determine their antioxidant activities. Ten flavonoids were isolated and purified by silica gel, Sephadex LH-20, and ODS column chromatography, and semi-preparative HPLC. Their structures were elucidated by spectroscopic analysis and identified as isorhamnetin-3-O-13-D-glucopyranoside （1）, isorhamnetin-3-O-13-D-galactopyranoside （2）, quercetin-3-O-13-o-glucopyranosyl （1--＊2）-I^-D-galactopyranoside （3）, quercetin-3-O-13-O-glucopyranosyl （1---~2）-13-D-glucopyranoside （4）, linarin （5）, quercetin-3-O- 13-D-glucopyranoside （6）, 5,7-dihydroxy-8-methxoyflavone-7-O-13-o-glucuronoside （7）, isorhamnetin （8）, kaempferol （9） and quercetin （10）. All these compounds were isolated from this plant for the first time, and compounds 1-5 and 7 were isolated from the genus of Polygala for the first time. The antioxidant activities of the isolated compounds were evaluated by DPPH free radical scavenging assay, and compounds 3, 4, 6, 8, 9 and 10 showed potent antioxidant activities.展开更多
Abstract： To investigate the chemical constituents of the roots of Polygala wattersii Hance, the separation and purification were performed by solvent extraction and repeated column chromatography （CC） on silica ge...Abstract： To investigate the chemical constituents of the roots of Polygala wattersii Hance, the separation and purification were performed by solvent extraction and repeated column chromatography （CC） on silica gel, Sephadex LH-20 and macroporous resin D101, preparative TLC and semi-preparative HPLC. The structures were identified by spectroscopic analysis and comparison of their 1H and 13C NMR data with those reported in literatures. Twenty-three known compounds, including eleven xanthones （1-11）, nine sugar esters （12-20）, two triterpenoid saponins （21 and 22） and one phenylpropanoid （23） were isolated and their structures were identified as 1,3-dihydroxyxanthone （1）, 1-hydroxy-3-methoxyxanthone （2）, 1,3-dihydroxy-2-methoxyxanthone （3）, 1,3,7-trihydroxy-2- methoxyxanthone （4）, 1,3,6-trihydroxy-2,7-dimethoxyxanthone （5）, 1,6,7-trihydroxy-2,3-dimethoxyxanthone （6）, 1,7-dihydroxy- 2,3-methylenedioxyxanthone （7）, 1,7-dimethoxyxanthone （8）, 1,2,3-trimethoxyxanthone （9）, 1-methoxy-2,3-methylenedioxyxanthone （10）, 6-hydroxy-0-methoxy-2,3-methylenedioxyxanthone （11）, 3＇-O-feruloyl-6-O-acetyl sucrose （12）, arillatose B （13）, sibricose A5 （14）, sibricose A6 （15）, 3＇,6-di-O-sinapoyl sucrose （16）, tenufoliside A （17）, 3＇-O-3,4,5-trimethoxycinnamoyl-6-O-p-methoxybenzoyl sucrose （18）, glomeratose A （19）, 1-O-p-coumaroyl-D-glucopyranose （20）, bayogenin-3-O-glucoside （21）, tenufolin （22）, and sinapic acid （23）. Among them, compounds 2 and 12 were obtained from genus Polygala for the first time, and except compound 16, all others were isolated from this species for the first time.展开更多
To investigate the chemical constituents of the roots ofPolygala sibirica L. The separation and purification were performed by solvent extraction and repeated chromatography with silica gel, Sephadex LH-20, ODS column...To investigate the chemical constituents of the roots ofPolygala sibirica L. The separation and purification were performed by solvent extraction and repeated chromatography with silica gel, Sephadex LH-20, ODS columns, and semiprep. HPLC. The structures were elucidated by spectral analysis. Twelve known compounds were isolated and identified as tenuifoliside A （1）, tenuifoliside B （2）, glomeratose A （3）, 3＇,6-disinapoyl sucrose （4）, sibiricose A5 （5）, sibiricose A6 （6）, sibiricose A1 （7）, sibiricose A2 （8）, polygalatenoside E （9）, 1-O-L-arabinopyranosyl-O-（6→1）-β-D-glucopyranosyl-salicylate （10）, canthoside A （11）, and methyl- 3,4,5-trimethoxycinnamate （12）. Compound 11 was obtained from genus Polygala for the first time, and compounds 2, 9, 10 and 12 were isolated from this plant for the first time.展开更多
A simple,low-cost and effective reverse flow-high performance capillary electrophoresis（RF-HPCE）method was developed for the separation and determination of tenuifolin in Polygalae Radix.Through optimization of sepa...A simple,low-cost and effective reverse flow-high performance capillary electrophoresis（RF-HPCE）method was developed for the separation and determination of tenuifolin in Polygalae Radix.Through optimization of separation conditions, a buffer of 50 mmol/L borax containing methanol（65：35,v/v）was selected for the separation of analytes.Regression equation revealed good linear relationship between peak area and concentration of the analyte in the range of 0.0563-0.9000 mg/mL （r=0.9988）.The recoveries ranged from 99.50%-104.7%.The results indicated that this method is simple,rapid and accurate. It can be used for the quality control of Polygalae Radix.展开更多
AIM:To investigate the chemical constituents of the roots of Polygala sibirica L.(Polygalaceae) METHOD:The isolation was performed by solvent extraction and various chromatographic techniques,including silica gel,Seph...AIM:To investigate the chemical constituents of the roots of Polygala sibirica L.(Polygalaceae) METHOD:The isolation was performed by solvent extraction and various chromatographic techniques,including silica gel,Sephadex LH-20,ODS,semi-preparative HPLC,and preparative TLC.The chemical structures were elucidated based on extensive spectroscopic analysis,including HR-ESI-MS and 1D- and 2D-NMR spectroscopic data.RESULTS:A total of sixteen compounds,including five xanthones(5,7–10),five saccharide esters(1,3,4,12,13),two flavonoids(14,16),two triterpenoids(11,15),one phenylpropanoid(6),and one benzophenone glycoside(2) were isolated.Their structures were determined as sibiricose A7(1),sibiriphenone A(2),polygalatenoside A(3),polygalatenoside C(4),lancerin(5),3,4,5-trimethoxycinnamic acid(6),6-hydroxy-1,2,3,7-tetramethoxyxanthone(7),1,3,7-trihydroxy-2-methoxyxanthone(8),onjixanthone II(9),1,2,3,6,7-pentamethoxyxanthone(10),presenegenin(11),3'-O-3,4,5-trimethoxycinnamoyl-6-O-4-methoxy benzoyl sucrose(12),tenuifoliside C(13),5,3'-dihydroxy-7,4'-dimethoxyflavonol-3-O-β-D-glucopyranoside(14),tenuifolin(15),and rhamnetin 3-O-β-D-glucopyranoside(16).CONCLUSION:Compounds 1 and 2 are two new compounds from P.sibirica.展开更多
Two new xanthone glycosides, polygalaxanthone IV and V were isolated from the roots of Polygala tenuifolia Willd. Their structures were established as 6-O-[a-L-rhamnopyranosyl- (12)-b-D-glucopyranosyl]-1-hydroxy-3, 7...Two new xanthone glycosides, polygalaxanthone IV and V were isolated from the roots of Polygala tenuifolia Willd. Their structures were established as 6-O-[a-L-rhamnopyranosyl- (12)-b-D-glucopyranosyl]-1-hydroxy-3, 7-dimethoxyxanthone (polygalaxanthone IV), and 6-O- [a-L-rhamnopyranosyl-(12)-b-D-glucopyranosyl]-1, 3-dihydroxy-7-methoxyxanthone (polyga- laxanthone V), respectively, on the basis of chemical and spectral evidence.展开更多
A new tdterpenoid glycoside, 3-β-O-β-D-glucopyranosyl presenegenin 28-O-α-L-arabipyranosyl（1 → 3）-6-β- xylopyranosyl（1 → 4）-[β-D-apiofuranosyl（1 → 3）]-Ct-L-rhamnopyranosyl（1 → 2）-[α-L-rhamnopyranosyl...A new tdterpenoid glycoside, 3-β-O-β-D-glucopyranosyl presenegenin 28-O-α-L-arabipyranosyl（1 → 3）-6-β- xylopyranosyl（1 → 4）-[β-D-apiofuranosyl（1 → 3）]-Ct-L-rhamnopyranosyl（1 → 2）-[α-L-rhamnopyranosyl（1 → 3）]-β-D-fucopyranosyl ester （1） was isolated from the Polygala tenuifolia Willd., together with two known saponins, including polygalasaponinXXIV （2） and polygalasaponinXXVIII （3）. The structure of new compound was elucidated by spectroscopic methods.展开更多
Two new dioxyxanthones, polyhongkongenoxanthones A and B（1 and 2） were isolated from the herbs of Polygala hongkongensis, together with six known xanthones. Their structures were elucidated on the basis of chemical ...Two new dioxyxanthones, polyhongkongenoxanthones A and B（1 and 2） were isolated from the herbs of Polygala hongkongensis, together with six known xanthones. Their structures were elucidated on the basis of chemical and spectroscopic evidence. The isolates were tested for their cytotoxicity against three tumor cell lines（HepG2, GLC-82 and MCF-7, HepG2=human hepatocellular carcinoma cells; GLC-82=human lung carcinoma cells; MCF-7= human breast carcinoma cells） by MTT assay, among which polyhongkongenoxanthone B（2）, 1,7-dihydroxy-2,3- methylenedioxyxanthone（3） and 1,7-dihydroxy-3,4,8-trimethoxyxanthone（6） are potential antitumor candidate due to their significant cytotoxic effects on the three cell lines..展开更多
Introduction Xanthones are secondary metabolites commonly occurring in a few higher plant families, fungi and lichen. Their high taxonomic value in such families and their pharmacological properties, including in vitr...Introduction Xanthones are secondary metabolites commonly occurring in a few higher plant families, fungi and lichen. Their high taxonomic value in such families and their pharmacological properties, including in vitro cytotoxicity, in vivo antitumour activity, antifungal, antibacterial, antiinflammatory properties and aldose reductase inhibitory activity have provoked great interest. The discovery of the antidiabetic activity of some axnthones＇ from Swertiaceae has prompted us to undertake a more broadly search for novel xanthones from plants of Polygalaceae. The phytochemical investigation has not been performed on this plant up to now. Herein we report the isolation and structure elucidation of two new xanthones （ compounds 1 and 2 ） and three known xanthones （compound 3, 4 and 5 ）.展开更多
The aim of the present study is to analyze sperm membrane changes and the spermicidal effect in treatment with the crude extract from Polygala tenuifo/ia Willd （PTW） in vitro. The root of PTW was extracted in distil...The aim of the present study is to analyze sperm membrane changes and the spermicidal effect in treatment with the crude extract from Polygala tenuifo/ia Willd （PTW） in vitro. The root of PTW was extracted in distilled water. Normal human spermatozoa were used to assess the spermicidal activity （Sander-Cramer assay） of the extract from the PTW root. The hypo-osmotic swelling （HOS） test and the eosin Y （EY） staining were used to detect the integrity of sperm membrane and vitality. The sperm chromatin dispersion （SCD） test was performed to determine sperm DNA integrity. N-9 was used as a reference standard and semen added to physiological saline was used as the control. Semen samples were donated by 42 healthy fertile men. The crude extract from the root of PTW could immobilize and kill 100% spermatozoa within 20 s in vitro at the concentrations of 20.0 and 10.0 mg/ml; at the concentration of 5.0 mg/ml, spermatozoa were immobilized in （39.5±3.2） s. In the groups of the crude extract from the root of PTW and N-9 solution the rate of the normal HOS （tails swollen） and the white head （unstained） was 0%, and the rate of the abnormal HOS （tails unswollen） and red head （stained） was 100%. Sperm DNA fragmentation showed no change in exposure to the crude extract from the root of PTW and N-9 solution. The sperm revival test did not show any spermatozoa that recovered their motilities. The rapid spermicidal activity of the crude extract from the root of PTW in vitro may occur by the disruption of the sperm membrane integrity.展开更多
Three new xanthones, 3, 6-dihydroxy-1, 2, 7-trimethoxyxanthone 1, 1, 3, 6-trihydroxy-2, 7, 8-trimethoxyxanthone 2, and 3, 6-dihydroxy-1, 2, 7, 8-tetramethoxyxanthone 3, were isolated from the roots of Polygala crotala...Three new xanthones, 3, 6-dihydroxy-1, 2, 7-trimethoxyxanthone 1, 1, 3, 6-trihydroxy-2, 7, 8-trimethoxyxanthone 2, and 3, 6-dihydroxy-1, 2, 7, 8-tetramethoxyxanthone 3, were isolated from the roots of Polygala crotalarioides. Their structures were elucidated by spectral and chemical methods.展开更多
OBJECTIVE:To analyze the constituents of volatile oils extracted from Yuan Zhi(Radix Polygalae),Shi Chang Pu(Acorus Tatarinowii),and a mixture of the two herbs.METHODS:The volatile oils were extracted using supercriti...OBJECTIVE:To analyze the constituents of volatile oils extracted from Yuan Zhi(Radix Polygalae),Shi Chang Pu(Acorus Tatarinowii),and a mixture of the two herbs.METHODS:The volatile oils were extracted using supercritical fluid extraction(SFE) with CO 2,and the constituents of the volatile oil extracts were analyzed by gas chromatography-mass spectrometry(GC-MS).The relative content of each component was calculated using peak area normalization.RESULTS:The optimized SFE conditions were 45 MPa at 35℃ for 2 h.Twenty-four compounds were identified in the extract from the Yuan Zhi(Radix Polygalae) and Shi Chang Pu(Acorus Tatarinowii) mixture,and six of these had relative contents >1.These compounds were 1,2-dimethoxy-4-(2-propenyl)-benzene;1,2,3-trimethoxy-5-(2-propenyl)-benzene;β-asarone;(Z,Z) 9,12-octadecadienoic acid;(Z) 6-octadecenoic acid;and ethyl oleate.Combination of the herbs increased the number of pharmacologically active substances in the extract and decreased the number of compounds with one benzene ring compared with the extracts from the individual herbs.CONCLUSION:These results indicate there is a synergistic relationship among the compounds in these herbs.展开更多
Two new oleanane-type saponins,crotalarioside A（1） and crotalarioside B（2）,were isolated from the roots of Polygala crotalarioides.Their structures were elucidated on the basis of spectroscopic and chemical evidence.
Objective:To investigate the chemical constituents of Polygala japonica Houtt.. Methods:The constituents were separated and purified by column chromatographies with silical gel, RP-silical gel and Sephadex LH-20. Thei...Objective:To investigate the chemical constituents of Polygala japonica Houtt.. Methods:The constituents were separated and purified by column chromatographies with silical gel, RP-silical gel and Sephadex LH-20. Their structures were elucidated on the basis of spectral data (IR, MS, 1H-NMR, 13C-NMR, HMQC and HMBC). Results: Totally 15 compounds were obtained from Polygala japonica Houtt. And their structures were identified as castaprenol-12 (Ⅰ), β-sitosterol (Ⅱ), stigmasterol (Ⅲ),stigmasta-7,22-di-ene-3-one (Ⅳ), n-dotriacontanol ( Ⅴ ), n-hexadecanol ( Ⅵ ), arachidic acid (Ⅶ), erogosterol (Ⅷ), kaempferol (Ⅸ), quercetin (Ⅹ), daucosterol (Ⅺ), p-hydroxybenzoic acid (Ⅻ),coumaric acid (ⅩⅢ), rhamnocitrin 3-O-β-D-galactopyranoside (ⅪⅤ), quercetin 3-O-β-D-glucopyranoside (ⅩⅤ). Conclusion: Compounds Ⅰ , Ⅲ , Ⅳ, Ⅴ , Ⅵ, Ⅶ, Ⅷ, Ⅻ , ⅩⅢ and ⅩⅣ were obtained from this plant for the first time.展开更多
A new benzophenone C-glucoside,3’-C-[4-O-(5-hydroxyferuloyl)-β-D-glucopyranosyl]-2′,4′,6′-trihydroxy-3,4-dimethoxy-benzophenone, named telephenone D,was isolated from the whole plants of Polygala telephioides,and...A new benzophenone C-glucoside,3’-C-[4-O-(5-hydroxyferuloyl)-β-D-glucopyranosyl]-2′,4′,6′-trihydroxy-3,4-dimethoxy-benzophenone, named telephenone D,was isolated from the whole plants of Polygala telephioides,and its structure was determined by analysis of spectroscopic data.展开更多
基金International Cooperative Project of Traditional Chinese Medicine(GZYYG2020023)CAMS Innovation Fund for Medical Sciences(CIFMS)Grant(2021-I2M-1-034)Key Research Project of Hunan Province(222SK2018).
文摘Objective To investigate the antidepressant effects of Yuanzhi(Polygalae Radix;PR)aqueous extract on chronic unpredictable mild stress(CUMS)-induced depression rat models and the underlying mechanisms.Methods A total of 40 male Sprague Dawley(SD)rats were randomly divided into control;model;low dose of PR(PR-L;0.5 g/kg);high dose of PR(PR-H;1 g/kg);and fluoxetine(10 mg/kg)groups;with 8 rats in each group.Except for the rats in control group;those in the other four groups underwent CUMS-induced depression modeling.PR and fluoxetine were administered intragastrically once daily;30 min prior to the CUMS procedure;for 14 consecu-tive days until the behavioral tests were performed.After CUMS modeling;the sucrose prefer-ence test(SPT);open field test(OFT);novelty-suppressed feeding test(NSFT);forced swim test(FST);and tail suspension test(TST)were employed to assess the pharmacological ef-fects of PR on the mitigation of depressive-like behaviors in rat models.Additionally;the en-zyme-linked immunosorbent assay(ELISA)was utilized to quantify the serum levels of tumor necrosis factor(TNF)-α;interleukin(IL)-6;and IL-1βin the rats.Western blot analysis was al-so conducted to evaluate the protein expression levels of nuclear factor kappa-B(NF-κB);in-ducible nitric oxide synthase(iNOS);cyclooxygenase-2(COX-2);nucleotide-binding oligomerization domain(NOD)-like receptor family pyrin domain containing 3(NLRP3);apoptosis-associated speck-like protein containing caspase recruitment domain(ASC);and caspase-1 in the hippocampal tissues of the rats.Immunofluorescence staining was per-formed to observe the morphological changes in ionized calcium-binding adapter molecule 1 positive(Iba-1+)cells in the dentate gyrus(DG)of rats with CUMS-induced depression.Results(i)Treatment with PR-H and fluoxetine resulted in significant enhancements in both the total distance and time the rats moved during tests(P<0.01 and P<0.05;respectively).Post-administration of PR-H and fluoxetine also led to statistically significant increase in su-crose preference among rats(P<0.05).Besides;PR-L;PR-H;and fluoxetine treatment markedly decreased the latency of ingestion(P<0.05;P<0.05;and P<0.01;respectively).As observed from the FST;PR-L;PR-H;and fluoxetine presented antidepressant effects on rats with CUMS-induced depression;leading to the reduction in time of their immobility(P<0.05;P<0.01;and P<0.01;respectively).The results of TST indicated reduced immobility time in rats receiving PR-H and fluoxetine treatment as well(P<0.01).(ii)Rats in model group showed an increase in the levels of Iba-1+microglia in their left and right brains in compari-son with control group(P<0.01).However;such increase was negated post PR treatment(P<0.01).Treatment with PR-L;PR-H;and fluoxetine considerably reduced the levels of inflam-matory factors(TNF-α;IL-1β;and IL-6;P<0.01).In addition;treatment of PR-L and PR-H ef-fectively counteracted the elevated levels of NLRP3;ASC;and caspase-1;and markedly down-regulated the expression levels of phosphorylated p65(p-p65);COX-2;and iNOS in rats’hip-pocampus(P<0.01).Conclusion Collectively;these findings indicate that PR exerts an antidepressant effect on rats with CUMS-induced depression partially through the modulation of the NLRP3 and NF-κB signaling pathways.
基金support from the National Key R&D Program of China(Grant No:2022YFC3401003)the National Natural Science Foundation of China(Grant No:21927808)+2 种基金the National Natural Science Foundation of China(Grant No:22104160)the National Key Research and Development Program of China(Grant No:2017YFC1704006)the Innovation Team of Ethnomedicine of National Ethnic Affairs Commission,China.We thank all the research staff who contributed to the study.
文摘Polygala tenuifolia,commonly known as Yuanzhi(YZ)in Chinese,has been shown to possess antiinsomnia properties.However,the material basis and the mechanism underlying its sedative-hypnotic effects remain unclear.Herein,we investigated the active components and neurochemical mechanism of YZ extracts using liquid chromatography tandem mass spectrometry(LC-MS/MS)-based pharmacometabolomics and mass spectrometry imaging(MSI)-based spatial resolved metabolomics.According to the results,17 prototypes out of 101 ingredients in the YZ extract were detected in both the plasma and brain,which might be the major components contributing to the sedative-hypnotic effects.Network pharmacology analysis revealed that these prototypes may exert their effects through neuroactive ligand-receptor interaction,serotonergic synapse,dopaminergic synapse,and dopaminergic synapse,among other pathways.LC-MS/MS-based targeted metabolomics and Western blot(WB)revealed that tryptophan-serotonin-melatonin(Trp-5-HT-Mel)and tyrosine-norepinephrine-adrenaline(Tyr-Ne-Ad)are the key regulated pathways.Dopa decarboxylase(DDC)upregulation and phenylethanolamine Nmethyltransferase(PNMT)downregulation further confirmed these pathways.Furthermore,MSI-based spatially resolved metabolomics revealed notable alterations in 5-HT in the pineal gland(PG),and Ad in the brainstem,including the middle brain(MB),pons(PN),and hypothalamus(HY).In summary,this study illustrates the efficacy of an integrated multidimensional metabolomics approach in unraveling the sedative-hypnotic effects and neurochemical mechanisms of a Chinese herbal medicine,YZ.
基金2022 National College Student Innovation and Entrepreneurship Training Program(202210599004).
文摘[Objectives]To explore the effects of Polygona fallax Hemsl water extract on gastrointestinal motility in normal mice and gastric motility disorder model mice and approximate mechanism.[Methods]Using normal mice and mice with gastric motility disorders(modeled with atropine),the effects of different mass concentration groups of P.fallax Hemsl water extract(0.125,0.250,0.500 g/mL)and domperidone groups on gastric residual rate,small intestine propulsion rate,serum motilin(MLT),vasoactive intestinal peptide(VIP),and tissue morphology were studied.[Results]There was a highly significant difference(P<0.01)in the small intestine propulsion rate of liquid in normal mice among the different concentration groups of P.fallax Hemsl water extract compared to the blank group.The small intestine propulsion rate and gastric residue rate of semi-solid paste were statistically significant compared to the blank group(P<0.05).Among them,there was a highly significant difference between the high concentration group(67.75%±7.65%,46.5%±10.62%)and the medium concentration group(60.90%±5.87%,59.27%±7.82%)(P<0.01).There was statistical significance in normal mouse serum MLT content in the high concentration group(P<0.05).There was no effect on serum VIP levels in normal mice;no effect on the morphology of stomach and intestinal tissues of normal mice.The small intestine propulsion rate and gastric residue rate of liquid and semi-solid paste in mice with gastric motility disorders were statistically significant compared to the atropine group,with extremely significant differences(P<0.01).[Conclusions]P.fallax Hemsl water extract has a promoting effect on gastrointestinal motility.One of the specific mechanisms by which P.fallax Hemsl promotes gastrointestinal motility in normal mice may be related to the content of MLT in mouse serum.The mechanism of action in atropine induced gastric paresis mice may be related to the reactivation of M receptors,and the action mechanism of P.fallax Hemsl does not change the original histological basis.It can be inferred that P.fallax Hemsl water extract has a synergistic effect on promoting gastrointestinal motility through other mechanisms,but it is not fully understood and further in-depth research is needed.
基金New-Century Talent Program, Ministry of Education of China (Grant No.985-2-102-113)National Science Fund for Excellent Young Scholars (Grant No. 81222051)National Key Technology R&D Program "New Drug Innovation" of China (Grant No. 2012ZX09304-005, 2012ZX09301002-002)
文摘The aim of this study was to isolate the chemical constituents of the aerial parts of Polygala tenuifolia Willd. and to determine their antioxidant activities. Ten flavonoids were isolated and purified by silica gel, Sephadex LH-20, and ODS column chromatography, and semi-preparative HPLC. Their structures were elucidated by spectroscopic analysis and identified as isorhamnetin-3-O-13-D-glucopyranoside （1）, isorhamnetin-3-O-13-D-galactopyranoside （2）, quercetin-3-O-13-o-glucopyranosyl （1--＊2）-I^-D-galactopyranoside （3）, quercetin-3-O-13-O-glucopyranosyl （1---~2）-13-D-glucopyranoside （4）, linarin （5）, quercetin-3-O- 13-D-glucopyranoside （6）, 5,7-dihydroxy-8-methxoyflavone-7-O-13-o-glucuronoside （7）, isorhamnetin （8）, kaempferol （9） and quercetin （10）. All these compounds were isolated from this plant for the first time, and compounds 1-5 and 7 were isolated from the genus of Polygala for the first time. The antioxidant activities of the isolated compounds were evaluated by DPPH free radical scavenging assay, and compounds 3, 4, 6, 8, 9 and 10 showed potent antioxidant activities.
基金The National Key Technology R&D Program"New Drug Innovation"of China(Grant No.2012ZX09301002-002-002,2012ZX09304-005)special funds for scientific research on traditional Chinese medicine(Grant No.201307002)National Science Fund for Excellent Young Scholars(Grant No.81222051)
文摘Abstract： To investigate the chemical constituents of the roots of Polygala wattersii Hance, the separation and purification were performed by solvent extraction and repeated column chromatography （CC） on silica gel, Sephadex LH-20 and macroporous resin D101, preparative TLC and semi-preparative HPLC. The structures were identified by spectroscopic analysis and comparison of their 1H and 13C NMR data with those reported in literatures. Twenty-three known compounds, including eleven xanthones （1-11）, nine sugar esters （12-20）, two triterpenoid saponins （21 and 22） and one phenylpropanoid （23） were isolated and their structures were identified as 1,3-dihydroxyxanthone （1）, 1-hydroxy-3-methoxyxanthone （2）, 1,3-dihydroxy-2-methoxyxanthone （3）, 1,3,7-trihydroxy-2- methoxyxanthone （4）, 1,3,6-trihydroxy-2,7-dimethoxyxanthone （5）, 1,6,7-trihydroxy-2,3-dimethoxyxanthone （6）, 1,7-dihydroxy- 2,3-methylenedioxyxanthone （7）, 1,7-dimethoxyxanthone （8）, 1,2,3-trimethoxyxanthone （9）, 1-methoxy-2,3-methylenedioxyxanthone （10）, 6-hydroxy-0-methoxy-2,3-methylenedioxyxanthone （11）, 3＇-O-feruloyl-6-O-acetyl sucrose （12）, arillatose B （13）, sibricose A5 （14）, sibricose A6 （15）, 3＇,6-di-O-sinapoyl sucrose （16）, tenufoliside A （17）, 3＇-O-3,4,5-trimethoxycinnamoyl-6-O-p-methoxybenzoyl sucrose （18）, glomeratose A （19）, 1-O-p-coumaroyl-D-glucopyranose （20）, bayogenin-3-O-glucoside （21）, tenufolin （22）, and sinapic acid （23）. Among them, compounds 2 and 12 were obtained from genus Polygala for the first time, and except compound 16, all others were isolated from this species for the first time.
基金Program for Changjiang Scholar and Innovative Team in University(Grant No.985-2-063-112)Program for New Century Excellent Talents in University(Grant No.985-2-102-113).
文摘To investigate the chemical constituents of the roots ofPolygala sibirica L. The separation and purification were performed by solvent extraction and repeated chromatography with silica gel, Sephadex LH-20, ODS columns, and semiprep. HPLC. The structures were elucidated by spectral analysis. Twelve known compounds were isolated and identified as tenuifoliside A （1）, tenuifoliside B （2）, glomeratose A （3）, 3＇,6-disinapoyl sucrose （4）, sibiricose A5 （5）, sibiricose A6 （6）, sibiricose A1 （7）, sibiricose A2 （8）, polygalatenoside E （9）, 1-O-L-arabinopyranosyl-O-（6→1）-β-D-glucopyranosyl-salicylate （10）, canthoside A （11）, and methyl- 3,4,5-trimethoxycinnamate （12）. Compound 11 was obtained from genus Polygala for the first time, and compounds 2, 9, 10 and 12 were isolated from this plant for the first time.
基金Natural Science Foundation of Shanxi Province (Grant No.200801107-1)
文摘A simple,low-cost and effective reverse flow-high performance capillary electrophoresis（RF-HPCE）method was developed for the separation and determination of tenuifolin in Polygalae Radix.Through optimization of separation conditions, a buffer of 50 mmol/L borax containing methanol（65：35,v/v）was selected for the separation of analytes.Regression equation revealed good linear relationship between peak area and concentration of the analyte in the range of 0.0563-0.9000 mg/mL （r=0.9988）.The recoveries ranged from 99.50%-104.7%.The results indicated that this method is simple,rapid and accurate. It can be used for the quality control of Polygalae Radix.
基金financially supported by the National Key Technology R&D Program"New Drug Innovation"of China(Nos.2012ZX09301002-002-002,2012ZX09304-005)special funds for scientific research on traditional Chinese medicine(No.201307002)National Science Fund for Excellent Young Scholars(No.81222051)
文摘AIM:To investigate the chemical constituents of the roots of Polygala sibirica L.(Polygalaceae) METHOD:The isolation was performed by solvent extraction and various chromatographic techniques,including silica gel,Sephadex LH-20,ODS,semi-preparative HPLC,and preparative TLC.The chemical structures were elucidated based on extensive spectroscopic analysis,including HR-ESI-MS and 1D- and 2D-NMR spectroscopic data.RESULTS:A total of sixteen compounds,including five xanthones(5,7–10),five saccharide esters(1,3,4,12,13),two flavonoids(14,16),two triterpenoids(11,15),one phenylpropanoid(6),and one benzophenone glycoside(2) were isolated.Their structures were determined as sibiricose A7(1),sibiriphenone A(2),polygalatenoside A(3),polygalatenoside C(4),lancerin(5),3,4,5-trimethoxycinnamic acid(6),6-hydroxy-1,2,3,7-tetramethoxyxanthone(7),1,3,7-trihydroxy-2-methoxyxanthone(8),onjixanthone II(9),1,2,3,6,7-pentamethoxyxanthone(10),presenegenin(11),3'-O-3,4,5-trimethoxycinnamoyl-6-O-4-methoxy benzoyl sucrose(12),tenuifoliside C(13),5,3'-dihydroxy-7,4'-dimethoxyflavonol-3-O-β-D-glucopyranoside(14),tenuifolin(15),and rhamnetin 3-O-β-D-glucopyranoside(16).CONCLUSION:Compounds 1 and 2 are two new compounds from P.sibirica.
文摘Two new xanthone glycosides, polygalaxanthone IV and V were isolated from the roots of Polygala tenuifolia Willd. Their structures were established as 6-O-[a-L-rhamnopyranosyl- (12)-b-D-glucopyranosyl]-1-hydroxy-3, 7-dimethoxyxanthone (polygalaxanthone IV), and 6-O- [a-L-rhamnopyranosyl-(12)-b-D-glucopyranosyl]-1, 3-dihydroxy-7-methoxyxanthone (polyga- laxanthone V), respectively, on the basis of chemical and spectral evidence.
基金the National Nature Science Foundation of China (No.30772890)the Collaborative Education,Research and Development Project of Beijing Municipal Commission of Education and the Key Project of Chinese Ministry of Education (No.108132).
文摘A new tdterpenoid glycoside, 3-β-O-β-D-glucopyranosyl presenegenin 28-O-α-L-arabipyranosyl（1 → 3）-6-β- xylopyranosyl（1 → 4）-[β-D-apiofuranosyl（1 → 3）]-Ct-L-rhamnopyranosyl（1 → 2）-[α-L-rhamnopyranosyl（1 → 3）]-β-D-fucopyranosyl ester （1） was isolated from the Polygala tenuifolia Willd., together with two known saponins, including polygalasaponinXXIV （2） and polygalasaponinXXVIII （3）. The structure of new compound was elucidated by spectroscopic methods.
基金Supported by the Natural Science Foundation of Guangdong Province, China(No.9151064201000042)
文摘Two new dioxyxanthones, polyhongkongenoxanthones A and B（1 and 2） were isolated from the herbs of Polygala hongkongensis, together with six known xanthones. Their structures were elucidated on the basis of chemical and spectroscopic evidence. The isolates were tested for their cytotoxicity against three tumor cell lines（HepG2, GLC-82 and MCF-7, HepG2=human hepatocellular carcinoma cells; GLC-82=human lung carcinoma cells; MCF-7= human breast carcinoma cells） by MTT assay, among which polyhongkongenoxanthone B（2）, 1,7-dihydroxy-2,3- methylenedioxyxanthone（3） and 1,7-dihydroxy-3,4,8-trimethoxyxanthone（6） are potential antitumor candidate due to their significant cytotoxic effects on the three cell lines..
文摘Introduction Xanthones are secondary metabolites commonly occurring in a few higher plant families, fungi and lichen. Their high taxonomic value in such families and their pharmacological properties, including in vitro cytotoxicity, in vivo antitumour activity, antifungal, antibacterial, antiinflammatory properties and aldose reductase inhibitory activity have provoked great interest. The discovery of the antidiabetic activity of some axnthones＇ from Swertiaceae has prompted us to undertake a more broadly search for novel xanthones from plants of Polygalaceae. The phytochemical investigation has not been performed on this plant up to now. Herein we report the isolation and structure elucidation of two new xanthones （ compounds 1 and 2 ） and three known xanthones （compound 3, 4 and 5 ）.
基金Project (No.2008-01) supported by the Foundation of Shandong Provincial Committee Family Planning Development,China
文摘The aim of the present study is to analyze sperm membrane changes and the spermicidal effect in treatment with the crude extract from Polygala tenuifo/ia Willd （PTW） in vitro. The root of PTW was extracted in distilled water. Normal human spermatozoa were used to assess the spermicidal activity （Sander-Cramer assay） of the extract from the PTW root. The hypo-osmotic swelling （HOS） test and the eosin Y （EY） staining were used to detect the integrity of sperm membrane and vitality. The sperm chromatin dispersion （SCD） test was performed to determine sperm DNA integrity. N-9 was used as a reference standard and semen added to physiological saline was used as the control. Semen samples were donated by 42 healthy fertile men. The crude extract from the root of PTW could immobilize and kill 100% spermatozoa within 20 s in vitro at the concentrations of 20.0 and 10.0 mg/ml; at the concentration of 5.0 mg/ml, spermatozoa were immobilized in （39.5±3.2） s. In the groups of the crude extract from the root of PTW and N-9 solution the rate of the normal HOS （tails swollen） and the white head （unstained） was 0%, and the rate of the abnormal HOS （tails unswollen） and red head （stained） was 100%. Sperm DNA fragmentation showed no change in exposure to the crude extract from the root of PTW and N-9 solution. The sperm revival test did not show any spermatozoa that recovered their motilities. The rapid spermicidal activity of the crude extract from the root of PTW in vitro may occur by the disruption of the sperm membrane integrity.
文摘Three new xanthones, 3, 6-dihydroxy-1, 2, 7-trimethoxyxanthone 1, 1, 3, 6-trihydroxy-2, 7, 8-trimethoxyxanthone 2, and 3, 6-dihydroxy-1, 2, 7, 8-tetramethoxyxanthone 3, were isolated from the roots of Polygala crotalarioides. Their structures were elucidated by spectral and chemical methods.
基金Supported by Shanxi Science and Technology Tackling Fund(No.20100311090)Shanxi Provincial Health Department Science and Technology Tackling Fund (No.2008034)
文摘OBJECTIVE:To analyze the constituents of volatile oils extracted from Yuan Zhi(Radix Polygalae),Shi Chang Pu(Acorus Tatarinowii),and a mixture of the two herbs.METHODS:The volatile oils were extracted using supercritical fluid extraction(SFE) with CO 2,and the constituents of the volatile oil extracts were analyzed by gas chromatography-mass spectrometry(GC-MS).The relative content of each component was calculated using peak area normalization.RESULTS:The optimized SFE conditions were 45 MPa at 35℃ for 2 h.Twenty-four compounds were identified in the extract from the Yuan Zhi(Radix Polygalae) and Shi Chang Pu(Acorus Tatarinowii) mixture,and six of these had relative contents >1.These compounds were 1,2-dimethoxy-4-(2-propenyl)-benzene;1,2,3-trimethoxy-5-(2-propenyl)-benzene;β-asarone;(Z,Z) 9,12-octadecadienoic acid;(Z) 6-octadecenoic acid;and ethyl oleate.Combination of the herbs increased the number of pharmacologically active substances in the extract and decreased the number of compounds with one benzene ring compared with the extracts from the individual herbs.CONCLUSION:These results indicate there is a synergistic relationship among the compounds in these herbs.
文摘Two new oleanane-type saponins,crotalarioside A（1） and crotalarioside B（2）,were isolated from the roots of Polygala crotalarioides.Their structures were elucidated on the basis of spectroscopic and chemical evidence.
基金Supported by the 863 Foundation of China ( No.2003AA2Z3507 ) the Scientific Foundation of Shanghai,China (No. 03QMH1414, 04DZ19843, 04DZ19856 and 04DZ19857)
文摘Objective:To investigate the chemical constituents of Polygala japonica Houtt.. Methods:The constituents were separated and purified by column chromatographies with silical gel, RP-silical gel and Sephadex LH-20. Their structures were elucidated on the basis of spectral data (IR, MS, 1H-NMR, 13C-NMR, HMQC and HMBC). Results: Totally 15 compounds were obtained from Polygala japonica Houtt. And their structures were identified as castaprenol-12 (Ⅰ), β-sitosterol (Ⅱ), stigmasterol (Ⅲ),stigmasta-7,22-di-ene-3-one (Ⅳ), n-dotriacontanol ( Ⅴ ), n-hexadecanol ( Ⅵ ), arachidic acid (Ⅶ), erogosterol (Ⅷ), kaempferol (Ⅸ), quercetin (Ⅹ), daucosterol (Ⅺ), p-hydroxybenzoic acid (Ⅻ),coumaric acid (ⅩⅢ), rhamnocitrin 3-O-β-D-galactopyranoside (ⅪⅤ), quercetin 3-O-β-D-glucopyranoside (ⅩⅤ). Conclusion: Compounds Ⅰ , Ⅲ , Ⅳ, Ⅴ , Ⅵ, Ⅶ, Ⅷ, Ⅻ , ⅩⅢ and ⅩⅣ were obtained from this plant for the first time.
基金supported by the Beijing Nova Program(No.2007B030)the program for Agricultural products processing technology and storage engineering in Beijing key construction disciplines(No.PXM2009-014207- 078172).
文摘A new benzophenone C-glucoside,3’-C-[4-O-(5-hydroxyferuloyl)-β-D-glucopyranosyl]-2′,4′,6′-trihydroxy-3,4-dimethoxy-benzophenone, named telephenone D,was isolated from the whole plants of Polygala telephioides,and its structure was determined by analysis of spectroscopic data.
