Showing papers in "Chinese Traditional and Herbal Drugs in 2008"

Preparation of floating rutin-alginate-chitosan microcapsule

Abstract: Objective Using rutin as the model drug to prepare floating alginate-chitosan microcapsule and investigate the feasibility of this pulsatile drug delivery system applied in Chinese materia medicaMethods By means of complex coacervation to prepare alginate-chitosan microcapsule and foaming agent to turn the microcapsule into gastric floating system and to investigate the release profile of the microcapsule in vitro and the influence of gas forming agent to the lag-time of the microcapsuleResults In vitro release,the microcapsule responded to the change of pH value and the release profile showed "S" profile,the lag-time increased from 3 h to 6 h as the quantity of gas forming agent with the dosage of foamer increasedConclusion Floating alginate-chitosan microcapsule is suitable to be applied in pulsatile drug delivery system of Chinese materia medica with the desirable entrapment efficiency

Chemical constituents from brown alga Sargassum fusiforme

Abstract: Objective To study the chemical constituents of brown alga Sargassum fusiformeMethods The compounds were isolated by silica gel chromatography,ODS chromatography,and preparative HPLC,and their structures were elucidated on the basis of chemical and spectroscopic methods,including HR EI-MS,1D and 2D NMR spectral techniquesResults Six sterols and two glycolipids were isolated from the n-hexane soluble part of ethanol extract of Sfusiforme and their structures were identified as fucosterol(Ⅰ),24R,28R-and 24S,28S-epoxy-24-ethylcholesterol(Ⅱ),24-hydroperoxy-24-vinylcholesterol(Ⅲ),29-hydroperoxystigmasta-5,24(28)-dien-3β-ol(Ⅳ),(24S)-5,28-stigmastadien-3β,24-diol(Ⅴ),(24R)-5,28-stigmastadien-3β,24-diol(Ⅵ),1-O-myristoyl-3-O-(6′-sulfo-αD-quinovopyranosyl) glycerol(Ⅶ),and 1-O-palmitoyl3-O-(6′-sulfo-α-D-quinovopyranosyl) glycerol(Ⅷ)Conclusion This is the first report for the isolation of Ⅳ,Ⅶ,and Ⅷ from alga of Sargassum(Turn) Ag,and compounds Ⅱ and Ⅲ from this algaThe isomers of saringosterols 24S(Ⅴ) and 24R(Ⅵ) from this alga are obtained by preparative normal-phase HPLC for the first time

Isolation and structure identification of steroidal saponin from Dioscorea zingiberensis

Abstract: Objective To study the chemical constituents of Dioscorea zingiberensis.Methods The fresh rhizome of D.zingiberensis was extracted three times,3 h once with EtOH-H2O at 80 ℃.The EtOH was evaporated under reduced pressure to give a residue which was suspended in water and then was exacted with petroleum ether,ethyl acetate,and n-butanol fraction.The water fraction was isolated by the reversed-phase ODS column chromatography.The chemical structures were elucidated by means of 1H-NMR,13C-NMR,135DEPT,HMQC,and HMBC spectroscopic analyses.Results Three steroidal saponins were isolated from the fresh rhizome of D.zingiberensis.The compounds were identified as:diosgenin-3-O-β-D-glucopyranosyl(1→3)-β-D-glucopyranosyl(1→4)-[α-L-rhamnopyranosyl(1→2)]-β-D-glucopyranoside(Ⅰ),(25R)-26-O-β-D-glucopyranosyl-furost-5-en-3β,22ζ-diol-3-O-β-D-glucopyranosyl(1→3)-β-D-glucopyranosyl(1→4)-[α-L-rhamnopyranosyl(1→2)]-β-D-glucopyranoside(Ⅱ),and(25R)-26-O-β-D-glucopyranosyl-furost-5-en-3β,22ζ-diol-7-carbonyl-3-O-β-D-glucopyranosyl(1→3)-β-D-glucopyranosyl(1→4)-[α-L-rhamnopyranosyl(1→2)]-β-D-glucopyranoside(Ⅲ).Conclusion Compound Ⅲ is a novel compound named as zingiberenin H.

Secoiridoid glycosides from Flos Lonicerae

Abstract: Objective To study the constituents in water-extracts from Flos Lonicerae. Methods Compounds were isolated and purified by using various column chromatography such as D101, Sephadex LH-20, and silica gel, etc. Their structures were identified on the basis of physical and spectral data. Results Seven secoiridoid glycosides were obtained and identified as vogeloside (Ⅰ), 7-epi-vogeloside (Ⅱ), secologanic acid (Ⅲ), sweroside (Ⅳ), secoxyloganin (Ⅴ), secologanoside (Ⅵ), (E)-aldosecologanin (Ⅶ). Conclusion Among them, compounds Ⅲ and Ⅵ are firstly obtained from the plants in Lonicera L. The structure of compound Ⅶ is rare in nature so far.

Chemical constituents of Eclipta prostrata

Abstract: Objective To study their chemical components of Eclipta prostrata and identify their chemical structures. Methods The compounds were isolated by chromatography, purified by Sephadex LH-20 gel, identified by spectral analyses, and compared with the published data. Results Ten compounds were isolated and identified as 2, 2', 5″, 2″-terthiophene-5-carboxylic acid (Ⅰ), β-sitosterol (Ⅱ), apigenin (Ⅲ), quercetin (Ⅳ), luteolin (Ⅴ), wedelolactone (Ⅵ), demethyl wedelolactone (Ⅶ), ecliptasaponin C (Ⅷ), luteoloside (Ⅸ), and linarin (Ⅹ). Conclusion Compound Ⅰ is a new compound from nature and compound Ⅹ is obtained from E. prostrata for the first time.

Pharmacokinetic study on baicalin and wogonoside in diabetic rats in vivo after oral administrating Huanglian-Jiedu Decoction

Abstract: Objective To investigate the pharmacokinetic profiles of baicalin and wogonoside in diabe-tic rats in vivo,which are two major constituents in Huanglian-Jiedu Decoction(HJD).Methods The diabetic rats were induced by ip administration of streptozotocin(STZ).After the establishment of the method and the set-up of diabetic rats,the pharmacokinetic profiles of baicalin and wogonoside were investigated.Diabetic and normal rats were ig HJD extract,and then the blood samples were collected at the given time points.Contents of baicalin and wogonoside in diabetic and normal rat plasma were assayed by HPLC-UV method.The pharmacokinetic parameters(except Cmax and tmax) were analyzed by noncompartmental method.The area under the serum concentration-time curve(AUC0-t) was calculated using trapezoidal rule to the last point.Moreover,the presystemic metabolism of baicalin was investigated and compared to explore the pharmacokinetic difference by fermentation of baicalin in feces suspensions of normal and diabetic rats,respectively.Results The pharmacokinetic parameters of baicalin in normal and diabe-tic rats were:(4.50±1.92) and(7.5±1.0) h for tmax 2;(2.83±0.25) and(9.54±2.87) μg/mL for Cmax1,(2.56±0.63) and(6.58±1.15) μg/mL for Cmax2;(37.58±7.57) and(92.75±24.62) μg·h/mL for AUC(0～24),(6.6±2.4) and(12.64±3.35) h for t1/2,respectively.And the pharmacokinetic parameters of wogonoside in normal and diabetic rats were:(5.5±1.0) and(8.00±1.63) h for tmax 2;(1.36±0.17) and(6.16±1.40) μg/mL for Cmax1;(1.58±0.17) and(4.11±0.76) μg/mL for Cmax2;(27.02±3.72) and(58.16±16.43) μg·h/mL for AUC(0～24);(9.72±2.24) and(7.89±1.63) h for t1/2,respectively.The results indicated that Cmax1,Cmax2,AUC(0～24) of baicalin and wogonoside were significantly enhanced and t1/2 of baicalin was remarkably extended when compared with the normal rats.And the results also revealed that baicalin contained in HJD hydrolyzed more rapidly when incubated in the feces suspension of diabetic rats than in that of normal rats.Conclusion The results indicate that the pharmacokinetic difference of baicalin between diabetic and normal rats may result from the presystemic metabolism of baicalin.

Effects of fungal elicitors on growth of Dendrobium candidum protocorms

Abstract: Objective To study the effects of two fungal elicitors on the growth of Dendrobium candidum protocorms cultured on the solid mediumMethods The medium for propagation of protocorms was selected and the growth curve on that medium was obtainedAccording to the curve,the two fungal elicitors were added at the different growth stages of protocormsThe fresh weight(FW) and dry weight(DW) of protocorms were measuredResults The medium for propagation of protocorms was 1/2MS+20% potato extract+3% sucrose+08% agarCompared with the control MF23 elicitor added at weeks 11 and 13 could significantly increase the FW by 164%(P001) and 234%(P001),respectively,and the DW by 67%(P005) and 179%(P001),respectively,and MF23 added into the medium for the whole culture could significantly decrease the DW by 99%(P001)Compared with the control,MF24 elicitor added at weeks 11 and 13 could significantly increase the FW by 177%(P001) and 120%(P005),respectively,added at week 11 could significantly increase the DW by 92%(P005),and MF24 added into the medium for the whole culture could significantly decrease the DW by 139%(P001)Conclusion The growth of protocorms can be inhibited when the fungal elicitor is added at the early stage of culture and be improved when the fungal elicitor is added at the later stage of the culture

Effects of borneol on distribution of sodium ferulate in plasma and in brain regions of mice

Abstract: Objective To explore the pharmaeokinetics of dosage factor and borneol on sodium ferulic (SF)in plasma and in brain regions of mice.Methods Mice were treated with SF(ig)alone or accompa- nied by borneol in different doses,the sample from plasma and different brain regions were obtained at dif- ferent time points(2.5,5,7.5,10,15,and 30 min),respectively after application of SF.HPLC was em- ployed to determine the concentrations of SF in plasma and in brain regions of mice.Pharmaeokinetie pa- rameters were assayed by using PCNONLIN software.Results AUC_(0-30),t_(max)and C_(max)of single low dose SF(0.2 g/kg)in plasma were 853.9μg/(mL·min),5.0 min,and 44.1μg/mL,respectively and that in hippocampus were 11.8μg/(g·min),5.0min,and 1.4μg/g,respectively;Single high dose SF(2 g/kg, ig)could only increase 2.5 times in plasma and 1.9 times in eerebellar region compared to single low dose SF(0.2 g/kg,ig).No changes was found in hippocampus.Borneol(50 mg/kg)not only accelerated the distribution of SF in hippoeampus(t_(max)in advance 2.5min),but also increased the concentration of that in plasma.Compared to single low dose SF(0.2 g/kg)group,the C_(max)and AUC_(0-30)are increased to 1.2 times and 1.7 times,respectively in hippoeampus in single low dose SF(0.2 g/kg)plus borneol(50 mg/ kg)group.Conclusion Increasing the close of SF alone dose not increase the concentration of SF appro- priately in brain.The concentration of SF in plasma and that in brain regions are increased by borneol.To- tally,these results suggest that the application of SF combined with borneol for CNS diseases,such as brain isehemia,might be more effective in clinic.

Studies on chemical constituents of flavonoids and glycosides in Ranunculus ternatus

Abstract: Objective To study the chemical constituents of Ranunculus ternatus.Methods The constituents were isolated and purified by column chromatographic methods.Their structures were elucidated by physicochemical properties and spectral analyses.Results Nine compounds were obtained and identified as robustaflavone-4′-methyl ether(Ⅰ),kayaflavone(Ⅱ),podocarpusflavone A (Ⅲ),bilobetin(Ⅳ),isoginkgetin(Ⅴ),amentoflavone(Ⅵ),4-oxo-5-(O-β-D-glucopyranosyl)-pentanoic acid-1O-butyl ester(Ⅶ),4-oxo-5-(O-β-D-glucopyranosyl)-pentansaeure-methyl ester(Ⅷ),benzyl alcohol O-β-D-glucopyranoside(Ⅸ).Conclusion Compounds Ⅰ-Ⅵ are obtained from the plants of Ranunculus Linn.for the first time,compound Ⅷ is a new natural product and compound Ⅸ is obtained from this plant for the first time.

Isolation and identification of steroidal saponins from fresh rhizome of Dioscorea zingiberensis

Abstract: Objective To study the steroidal saponins from the fresh rhizome of Dioscorea zingiberensis and search for new bioactive compounds.Methods The steroidal saponins were isolated by normal phase silica gel and RP-C_(18)column chromatography.Their chemical structures were elucidated by IR,MS,and NMR methods.Results Three steroidal saponins were isolated from EtOH extract of the fresh rhizome of D.zingiberensis and identified as gracillin(Ⅰ),zingiberenin A(Ⅱ),and 26-O-β-D-glucopyranosyl-3β, 26-diol-25(R)-furosta-5,20(22)-dien-3-O-{α-L-rhamnopyranosyl-(1→4)-[β-D-glucopyranosyl-(1→3)-β- D-glucopyranosyl-(1→2)]}-β-glucopyranoside,Ⅲ).Conclusion CompoundⅢis a new compound named as zingiberenin G.

Chemical constituents in aerial parts of Pulsatilla chinensis

Abstract: Objective To study the chemical constituents in the aerial parts of Pulsatilla chinensis.Methods The compounds were isolated and purified by silica gel and ODS column chromatographies.Their structures were identified by physical and chemical properties as well as spectral data.Results Nine compounds were isolated from the 95% ethanol extract in the aerial parts of this plant.Their structures were elucidated as L-chicoric acid(Ⅰ),tiliroside(Ⅱ), apigenin 7-O-(3″-p-coumaryl)-glucoside(Ⅲ),4,6,7-trimethoxy-5-methyl coumarin(Ⅳ),4,7-dimethoxy-5-methyl coumarin(Ⅴ),myo-inositol(Ⅵ),shikimic acid(Ⅶ),1,4-amber acid(Ⅷ),and 5-hydroxy-4-oxo-pentanoic acid(Ⅸ),respectively.Conclusion Compound Ⅰ is a new natural product.All compounds are isolated from this plant for the first time.

Chemical constituents from Elsholtzia rugulosa

Abstract: Objective To study the chemical constituents from Elsholtzia rugulosa.Methods The compounds were isolated by column chromatography on silica gel,Sephadex LH-20,and MCI-gel CHP-20P.The structures were identified by means of NMR and MS analyses.Results Twelve compounds were isolated and their structures were identified as 4′,5-dihydroxy-7-methoxyflavone(Ⅰ),5-hydroxy-4′,6,7-trimethoxyflavone(Ⅱ),5,6-dihydroxy-3′,4′,7,8-tetramethoxyflavone(Ⅲ),apigenin(Ⅳ),kaempferol(Ⅴ),quercetin(Ⅵ),1H-indole-3-carboxylic acid(Ⅶ),ursolic acid(Ⅷ),oleanolic acid(Ⅸ),ergosta-7-en-3β-ol(Ⅹ),β-sitosterol(Ⅺ),and β-daucosterol(ⅩⅡ).Conclusion Compounds Ⅰ-Ⅹ are obtained from the Plants of Elsholtzia Willd.for the first time.

Speculating about scientific investigation on nature of Chinese materia medica

Abstract: The scientific investigation on the nature of Chinese materia medica(CMM)has stepped into a critical moment.In this paper,the objectivity of the CMM nature and some other relevant existing problems are discussed based on retrospective and prospective analyses.It could be concluded that there is a duality about the objective connotation of the CMM nature.In order to get a significant breakthrough in near future in the scientific investigation on the CMM nature,the goal,strategy,and methodology should be reconsidered and adjusted.Cold and heat,the most radical and important elements of the CMM nature should be treated as the most principal task in the field.The key scientific issues can be refined to establish a set of objective and scientific evaluating system for the CMM nature,and to elucidate its objective conno- tation.In view of restoration to integration as well as thermodynamic expression,a set of new ideas and methods for the investigation on the CMM nature has been put forward in this paper.

Blood lipid regulation of ethyl acetate extracting fraction and stilbene glycoside from tuber of Polygonum multiflorum

Abstract: Objective To investigate the blood lipid regulation of ethyl acetate extracting fraction from the tube of Polygonum multiflorum (EAEF-PM) and stilbene glycoside from the tuber of P. multiflorum. Methods The effects of EAEF-PM and stilbene glycoside on blood lipid and liver index were studied in normal mice. Acute hyperlipidemic model mice induced by ip Triton as markers were used to observe the effects of EAEF-PM and stilbene glycoside on the blood lipid level. The investigation was also employed in the hyperlipidemic model rats induced by feeding with the high-lipid diet accompanied by ig EAEF-PM and stilbene glycoside for 28 d, respectively. The effects of EAEF-PM and stilbene glycoside were studied by measuring the concentrations of lipids, malondialdehyde (MDA), nitric oxide (NO), and the activity of superoxide dismutase (SOD) in serum of the hyperlipidemic rats. The levels of total cholesterol (TC) and triglyeride (TG) in liver as well as liver index were also simultaneously determined. Results In the normal mice, EAEF-PM and stilbene glycoside not only increased the level of serum high density lipoprotein cholesterol (HDL-C), also decreased the level of serum low density lipoprotein cholesterol (LDL-C). EAEF-PM and stilbene glycoside lowered serum TC, TG and LDL-C, and increased serum HDL-C in the hyperlipidemic mice. Administration of EAEF-PM (60 mg/kg) could signi-ficantly reduce the liver index in hyperlipidemic rats. Administration of EAEF-PM (30 and 60 mg/kg) could remarkably decrease the levels of serum TC, TG, LDL-C as well as the ratio of TC/HDL-C, also remarkably increase serum HDL-C, NO, and SOD. Compared with EAEF-PM, stilbene glycoside had the somewhat lower effect but no significant difference. Conclusion EAEF-PM and stilbene glycoside possess the obvious effects of blood lipid-regulation, antioxidation and protecting vascular endothelium. The potential constituent is stilbene glycoside which can be used to prevent and/or treat hyperlipidemia.

Rare constituents with anti-cancer activity from hydrolytic products in saponins of Panax quinquefolium stems and leaves

Abstract: Objective To study the chemical constituents of the acid hydrolytic products from the stems and leaves of Panax quinquefolium. Methods The stems and leaves of P. quinquefolium were hydrolyzed with acid;Isolation and purification were carried out by various chromatographic techniques,such as silica gel and so on. Compounds were identified and elucidated by spectral and chemical methods. Results Eight compounds were obtained from the acid hydrolytic products in the stems and leaves of P. quinquefolium and identified as 20 (S)-panaxadiol (Ⅰ),20 (S)-protopanaxadiol (Ⅱ),20 (R)-protopanaxadiol (Ⅲ),20 (S)-panaxatriol (Ⅳ),24 (R)-ocotillol (Ⅴ),20 (R)-protopanaxatriol (Ⅵ),20 (R)-dammarane-3β,12β,20,25-tetrol (Ⅶ),and 20 (R)-dammarane-3β,6α,12β,20,25-pentol (Ⅷ). Conclusion Compounds Ⅰ-Ⅷ are the derivates of the aglycones of ginsenosides,isolated from the acid hydrolytic products from the stems and leaves of P. quinquefolium for the first time. Among these compounds,Ⅳ,Ⅶ,and Ⅷ are discoverd from the roots,stems,leaves,fruits,and buds of P. quinquefolium for the first time. Compound Ⅶ is discovered and reported that it is the derivate of the aglycone of protopanoxadiol ginsenoside,with the conspicuous anticancer activity from the fruits of P. ginseng for the first time.

Chemical constituents of Selaginella sinensis

Abstract: Objective To study the chemical constituents from Selaginella sinensis.Methods The compounds were isolated with Diaion HP-20,Toyopearl HW-40,silica gel column chromatography.The structures of these compounds were identified by physicochemical properties and spectral analyses.Results Eleven compounds were isolated from the 70% acetone-extracts and their structures were identified as β-sitosterol(Ⅰ),vanillic acid(Ⅱ),(7S,8R)-4,9,9′-trihydroxy-3,3′-dimethoxy-7,8-dihydrobenzofuran-1′-propylneolignan(Ⅲ),syringaresinol(Ⅳ),(-)-pinoresinol(Ⅴ),pinoresinol-4-Oβ-D-glucopyranoside(Ⅵ),syringaresinol-4,4′-O-di-β-D-glucopyranoside(Ⅶ),β-methylD-xylopyranoside(Ⅷ),β-methyl-D-arabinopyranoside(Ⅸ),hinokiflavone(Ⅹ),and amentoflavone(Ⅺ).Conclusion Compounds Ⅱ-Ⅸ are isolated from this plant for the first time.

Antitumor effects of neogambogic acid both in vivo and in vitro

Abstract: Objective To investigate the antitumor effects of neogambogic acid both in vivo and in vitro.Methods Cancer cell lines were incubated with various concentrations of neogambogic acid for 24,48,and 72 h,antiproliferative activities against cancer cells were measured by MTT assay;The BALB/c-nude mice were transplanted with cancer cells,then iv by 4,8,16,and 32 mg/kg neogambogic acid,the size and weight of the tumor were measured.Results Neogambogic acid could inhibit the proliferation of cancer cell lines(human colon carcinoma HCT-8 cell,human hepatoma Bel-7402 cell,human gastric carcinoma BGC-823 cell,human non-small cell lung cancer A549 cell,and human ovarian cancer A2780 cell).The 50% inhibiting concentration(IC50) of neogambogic acid of 72 h was from 1.75 to 3 μmol/L.It also showed the inhibition on the growth of A549 in nude mice at the doses of 8,16,and 32 mg/kg of neogambogic acid intravenously(P0.05).However neogambogic acid did not show the obvious inhibition on the growth of tumor Bel-7402 at the dose from 4 to 16 mg/kg.Conclusion It suggests that neogambogic acid has the inhibitory effects on the proliferation of human cancer cell lines in vitro and on the tumor growth of nude mice transplanted with A549 cell in vivo.

HPLC Fingerprint of flavonoids from Lycium barbarum

Abstract: Objective To establish chromatographic fingerprint of flavonoids from Lycium barbarum by HPLC and distinguish the Fructus Lycii from different habitats. Methods The mutual mode was established depending on ten Fructus Lycii samples from different growing areas in Ningxia. The solftware "Similarity Evaluation System for Chromatographic Fingerprint of Chinese Materia Medica" was applied to analyzing 15 Fructus Lycii samples from different habitats. Results The established chromatographic fingerprint method had good repeatability; 16 peaks are characteristic of HPLC fingerprints of flavonoids and flavonoids of Fructus Lycii from different habitats were quite different in content and constituent. Conclusion This chromatographic fingerprint spectrum of flavonoids could be used to distinguish Fructus Lycii from different habitats.

Chemical constituents of Balanophora involucrata

Abstract: Objective To study the chemical constituents of Balanophora involucrata.Methods Silica gel column chromatography and HPLC were used to isolate and purify the compounds and NMR,ESI-MS,EI-MS,and circular dichroism spectrum was applied to elucidate their structures.Results Ten compounds,including an isocumarin,two phenylacrylic acid glucosides,and seven flavonoids were isolated from the ethyl acetate extract of B.involucrata.They were(2R)-eriodictyol-5-O-β-D-glucopyranoside(Ⅰ),(2S)-eriodictyol-5-O-β-D-glucopyranoside(Ⅱ),phloridzin(Ⅲ),3-hydroxy-phloridzin(Ⅳ),trilobatin(Ⅴ),(E)-3,4,2',4',6'-pentahydroxychalcone-2'-O-β-D-glucopyranoside(Ⅵ),aureusidin-4-O-β-D-glucopyranoside(Ⅶ),(E)-1-O-p-coumaroyl-β-D-glucopyranoside(Ⅷ),(E)-1-O-caffeoyl-β-D-glucopyranoside(Ⅸ),and methyl brevifolincarboxylate(Ⅹ).Conclusion All the compounds are isolated from this plant for the first time and compound Ⅰ is a new flavanone glucoside named as balaninvolin.

Apoptosis induced by Capparis spionosa polysaccharide in human HepG2

Abstract: Objective To investigate the apoptosis of Capparis spionosa polysaccharide(CSPS)on human HepG2.Methods MTT was adopted to determine if CSPS had cytotoxic effect to HepG2.The alteration of HepG2's morphology was observed by invert microscope.Morphology of HepG2 changed with dosage of CSPS was detected by AO/EB and laser confocal scanning microscope.Flow cytometry(FCM)was used to detect the apoptosis index with PI labeling method.Results The result of MTT showed that CSPS could inhibit the growth of HepG2,IC50 was 471.53 mg/L;The morphology of cell was observed by invert microscope and laser confocal scanning microscope in cell collapsed,break to pieces,even appearance of apoptosis body.The apoptosis rate in high dose group was 74.926%,detected by FCM.Conclusion This consequence indicates that CSPS could induce human HepG2 apoptosis.