Yong-Lin Wang

Guiyang Medical University, Kuei-yang, Guizhou Sheng, China

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Publications (35)29.19 Total impact

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    ABSTRACT: Polygonum capitatum (P. capitatum) is a well-known Miao medicinal plant that has been used for many years for its unique therapeutic effects on various urological disorders, including urinary calculus and urinary tract infections.
    Journal of Ethnopharmacology. 10/2014;
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    ABSTRACT: A UPLC method has been developed in the current investigation for simultaneous determination of nine chemical markers of Bletilla striata, 4-hydroxymethylphenyl beta-D-glucoside, blestroside, dactylorhin A, militarine, dihydrophenanthrene 5, gymnoside V, dihydrophenanthrene 1, benzylphenanthrene 3 and gymnosides IX. Separation was performed at 45 degrees C on an ACQUITY UPLC BEH C18 column (2.1 mm x 150 mm, 1.7 microm) with a gradient solvent system of acetonitrile-water as the mobile phase. The flow rate was 0.3 mL x min(-1), the detection wavelength was 280 nm. The results showed that the nine chemical markers could be well resolved and that in the selected linear range, all calibration curves of the nine chemical markers showed good linearity (r > or = 0.999 3). The recoveries (n = 6) were in the range of 98.15% - 102.2% and RSDs were between 2.1% - 3.6%. The data suggested that the developed UPLC-UV method had good reproducibility, robustness, and accuracy, which was suitable for the quality control of Bletilla striata. Applications of the method showed that the nine chemical markers had higher contents in the wild B. striata than in the cultivated ones.
    06/2014; 39(11):2051-5.
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    ABSTRACT: Tablets of oleanolic acid (OA) have been approved by SFDA in China as an adjuvant therapy for acute and chronic hepatitis. Co-occurring substances present in the tablets of OA and their hepatocytotoxicity have not yet been reported. In the current investigation, the crude OA drug was separated by repeated column chromatography. The structures of the isolated compounds were characterized by spectral analysis and the cytotoxicity of each compound was evaluated in vitro against the human normal liver cell L02 at concentrations from 0.125 to 1000 μmol/L using the MTT method. As a result, OA and its 11 co-occurring trace compounds including one new triterpenoid, 3-O- (4-oxo-pentanoyl)-olean-12- en-28-oic acid, were isolated and structurally characterized. Cytotoxicity tests indicated that these compounds were all non-toxic at concentrations up to 50μmol/L. Clear structure-activity relationship (SAR) was also observed. The results suggested that OA tablets of similar origin might not cause obvious cytotoxicity to the normal liver cell. The work may facilitate further SAR studies of OA-type triterpenoids.
    Pakistan journal of pharmaceutical sciences 05/2014; 27(3):601-5. · 0.95 Impact Factor
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    ABSTRACT: The in vivo effects of traditional herbal medicines are generally mediated by multiple bioactive components. The main constituents of Polygonum orientale L. are flavonoids such as orientin, vitexin, cynaroside, and quercitrin. The aim of this study was to develop and validate a method for characterizing these flavonoids, in order to better understand the pharmacokinetics and pharmacodynamics of P. orientale L. We used ultra-performance liquid chromatography-electrospray ionization-tandem mass spectrometry (UPLC-ESI-MS/MS) to analyze the flavonoids. After precipitation of the proteins with methanol, the flavonoids were separated on a BEH C18 column (50mm×2.1mm, i.d., 1.7μm) by using an elution gradient of acetonitrile. Flavonoid content was determined using the multiple reaction monitoring (MRM) mode at m/z 449.2→329.2 for orientin, m/z 433.2→313.0 for vitexin, m/z 449.2→287.1 for cynaroside, m/z 449.2→303.4 for quercitrin, and m/z 417.0→267.0 for the internal standard, puerarin. Pharmacokinetics was assessed after intravenous administration of P. orientale L. extracts (POE) in Beagle dogs at a dose of 22, 44, or 88mg/kg. Analysis of the standard curves by linear regression revealed high linearity over a 243-fold dynamic range for the four flavonoids (the lower limit of quantitation values were 4-21ng/mL). The relative standard deviations of intra- and inter-day measurements were less than 15.1%, and the method was accurate to within -8.7% to 7.2%; the extraction recoveries from dog plasma were 70.6-89.3%, 69.8-88.7%, 72.5-85.7%, and 71.0-79.1% for orientin, vitexin, cynaroside, and quercitrin, respectively. Our results suggest non-linear pharmacokinetic characteristics with rapid clearance of the flavonoids. In conclusion, UPLC-ESI-MS/MS is a rapid and sensitive method for simultaneous quantification of multiple flavonoids from POE in dog plasma and is suitable for pharmacokinetic studies of herbal medicines.
    Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 03/2014; 957C:96-104. · 2.78 Impact Factor
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    ABSTRACT: Isomeric polyphenolic glycosides that possess regioisomeric O-acylated saccharide residues can be found in many medicinal plants and their preparations as well as some synthetic intermediates. The need for a pure and sufficient quantity of compounds for nuclear magnetic resonance measurements calls for a microanalytical method for their rapid differ entiation. In the current investigation, an electrospray ionization–tandem mass spectrometric method was developed for rapid differentiation of two pairs of regioisomeric acylated monosaccharides, quercetin-3-O-(3″-O-galloyl)-α-L-rhamnopyranoside and quercetin-3-O-(2″-O-galloyl)-α-L-rhamnopyranoside as well as quercetin-3-O-(3″-O-galloyl)-β-D-glucopyranoside and quercetin-3-O-(2″-O-galloyl)-β-D-glucopyranoside; the mechanisms governing their similar or differential fragmentations are also discussed. The work may facilitate the structural determination of these regioisomers and their analogs in pure form or in complex matrix.
    Spectroscopy Letters 01/2014; 47(1):19-23. · 0.67 Impact Factor
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    ABSTRACT: A series of mono l-amino acid ester, mono non-steroid anti-inflammation drug (NSAID), carboxylic ester derivatives of acyclonucleoside phosphonates were prepared by using a “one pot synthesis” method and their in vitro anti-HBV activity were evaluated in HepG 2.2.15 cells. Compound 9a exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with IC50 and selective index (SI) values of 0.48 μmol/L and 763.72, respectively.
    Chinese Chemical Letters 01/2014; 25(1):115–118. · 1.18 Impact Factor
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    ABSTRACT: This in vitro investigation was designed to examine potential neuroprotection by dicaffeoylquinic acids (diCQAs) extracted from a traditional Chinese medicinal herb herba erigerontis and their effects against the toxicity induced by β-amyloid peptide (Aβ25-35 ). The neuroblastoma SH-SY5Y cell line was treated with Aβ or 3, 4-diCQA, 3, 5-diCQA or 4, 5-diCQA. 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) reduction was assayed by spectrophotometrical method, lipid peroxidation (malondialdehyde) on the basis of the level of thiobarbituric acid-reactive substance, the activity of superoxide dismutase by the xanthine oxidase procedure, the frequency of apoptosis by flow cytometry, and the levels of α3 and α7 nicotinic acetylcholine receptor (nAChR) subunit proteins by Western blotting. When the cells were exposed to Aβ25-35 , MTT reduction declined, oxidative stress and apoptosis were enhanced, and the expression of α3 and α7 nAChR subunit proteins was lowered. Expression of the α7 nAChR subunit protein was increased by all three diCQAs, and the level of α3 was increased by 3, 5-diCQA and 4, 5-diCQA. Significantly, pretreatment with diCQAs attenuated the neurotoxic effects of Aβ25-35 , a neuroprotective effect in which the upregulation of α7 and α3 nAChR may be involved. The diCQAs exert a protective effect on Aβ-induced neurotoxicity in SH-SY5Y cells and a potential underlying mechanism involving stimulation of nAChRs.
    The Journal of pharmacy and pharmacology. 12/2013; 65(12):1736-44.
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    ABSTRACT: Polygonum capitatum is a well-known Chinese medicinal plant widely used by the Miao people for the treatment of various urologic disorders. Previous investigations have shown the presence of various types of phenolics. Our ultrahigh-performance liquid chromatography with photodiode array detection and mass spectrometry (UPLC-PDA-MS) analysis indicated that flavonoid glycosides and polyphenolic glycosides were its major constituents and quite a number of phenolic compounds have not yet been identified. Identification or characterisation of the major compounds of this plant will contribute to the scientific understanding of the medicinal plant and the authentication of the plant material and its pharmaceutical preparations. To develop an efficient method for the identification and structural characterisation of the major compounds present in P. capitatum. Elution of the 70% ethanol extract of P. capitatum by 80% ethanol on a D101 macroporous resin column afforded a phenolics-enriched fraction, separation of which by Sephadex LH-20 column chromatography eluted with absolute ethanol gave a tannin-free phenolic fraction (TFPF). Compounds present in TFPF were identified and structurally characterised by UPLC-PDA-ESI-MS/MS. An amino acid and 40 phenolics including a number of flavonoid glycosides and polyphenolic glycosides were identified or structurally characterised in TFPF. Among these compounds, four were new and 19 were described in the plant for the first time. The study showed that TFPF of P. capitatum contained flavonoid glycosides and polyphenolic glycosides as its major principles. Polyphenolic glycosides were perhaps the most typical chemical markers of P. capitatum. Copyright © 2013 John Wiley & Sons, Ltd.
    Phytochemical Analysis 11/2013; 24(6):556-68. · 2.48 Impact Factor
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    ABSTRACT: A simple and selective ultra performance liquid chromatography–electrospray ionization tandem mass spectrometry (UPLC–ESI-MS/MS) assay was developed for the determination of the human plasma protein binding of four bioactive flavonoids (such as orientin and vitexin) in Polygonum orientale. Protein precipitation was used for sample preparation. Equilibrium dialysis technique was applied to determine the plasma protein binding under physiological conditions. The separation was achieved through a Waters C18 column with a mobile phase composed of 0.1% formic acid in acetonitrile and 0.1% aqueous formic acid using step gradient elution at a flow rate of 0.35 mL/min. A Waters ACQUITY™ TQD system was operated under the multiple reaction monitoring (MRM) mode of positive electrospray ionization. All of the recovery, precision, accuracy and stability of the method met the requirements. Good correlations (r>0.99) of the four compounds were found, which suggested that these compounds can be simultaneously determined with acceptable accuracy. Results showed that the plasma protein bindings of the four bioactive flavonoids were in the range of 74–89% over the six concentrations studied. The binding parameters containing protein binding affinity, protein binding dissociation constant, and protein binding site were studied. The maximum ability to bind with protein was also determined in the assay in order to understand the drug-protein binding of each compound better.
    Journal of Pharmaceutical Analysis. 10/2013; 3(5):376–381.
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    ABSTRACT: A series of carbamate prodrugs of scutellarin methyl ester (4a–4e) were prepared in the presence of bis(trichloromethyl) carbonate (BTC) with scutellarin methyl esters and l-amino acid tert-butyl ester hydrochloride as starting materials. In vitro stability and aqueous solubility of target compounds were evaluated. The results indicated that compounds 4d and 4e have higher solubility and in vitro stability than scutellarin respectively.
    Chinese Chemical Letters 04/2013; 24(4):338–340. · 1.18 Impact Factor
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    ABSTRACT: ETHNOPHARMACOLOGICAL RELEVANCE: Except for as a well-known tonic Chinese herbal medicine for the treatment of splenic asthenia, anorexia, lassitude and weakness, the roots of Pseudostellaria heterophylla was also used in Chinese medicines for the treatment of palpitation. AIM OF THE STUDY: The study was designed to determine whether fractions from P. heterophylla could provide cardioprotection on hypoxic cardiomyocytes, what structural types of compounds were responsible for the observed effects, and which is the possible mechanism of action. MATERIALS AND METHODS: The roots of P. heterophylla were extracted successively with 70% aqueous ethanol and water to give a 70% ethanol extract and a water extract. The latter was first precipitated by 80% ethanol and then protein-removed by the Sevage method to give a fraction enriched in polysaccarides (PHP). The former was separated by column chromatography into a fraction enriched in small-molecule sugars and amino acids (PHSSAC), saponins (PHS), cyclopeptides (PHCP), and sapogenins (PHSG). UV spectral or chemical methods were used to confirm the five fractions. The cardioprotective effects of the fractions were evaluated by measuring the viability and the leakage of lactate dehydrogenase (LDH) of the fraction-pretreated cardiomyocyte H9c2 after exposure to CoCl2-induced hypoxia. The mechanism of action was studied by investigating the nature of cell death inhibition (by Annexin V/PI flow cytometric analysis) and their effects on the levels of malonaldehyde (MDA), superoxide dismutase (SOD) and intracellular reactive oxygen species (ROS). RESULTS: Fractions PHS and PHP could attenuate CoCl2-induced hypoxic damage to an extent higher than or comparable to the effect of the positive control N-Acetyl-L-Cysteine (NAC). Pretreatment of the cells with 800μg/mL of PHS or 10mg/mL of PHP markedly decreased the level of MDA, reduced intracellular ROS, increased the activity of SOD, and reduced leakage of LDH to the levels close to or better than that with 326μg/mL of NAC. Reduction of apoptosis was also observed for both fractions. CONCLUSIONS: The overall results suggested that the traditional use of this plant for the treatment of palpitation may be attributed to the presence of cardioprotective agents in P. heterophylla. PHP and PHS were the two active fractions responsible for its cardioprotective effect. The mechanism might involve protections of the cell membrane from hypoxic damage and of the cells from oxidative injury via preventing increased oxidative stress. Protection of the cells via inhibition of cellular apoptosis may also be involved.
    Journal of ethnopharmacology 03/2013; · 2.32 Impact Factor
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    ABSTRACT: Acylated monosaccharide residues are structural subunits of natural products or synthetic intermediates that have received much attention in past years. Determination of the acylation sites of these residues still relies heavily on the comparison of their characteristic NMR signals with those of known standards and synthesized acylated glycosides. It is important to develop a rapid analytical method for determining the acylation sites for these compounds, and this is described in this study. Six known polyphenolic glycosides were used for the electrospray ionization and collision-induced dissociation tandem mass spectrometry (ESI-CID-MS/MS) discrimination of the acylated monosaccharide residues with different acylation sites. A combination of ESI-CID-MS/MS, using a triple quadrupole mass spectrometer, with ultra-performance liquid chromatography (UPLC) and photo-diode array (PDA) detection (UPLC-PDA) has been applied to the identification or characterization of polyphenolic glycosides in Polygonum capitatum that possess an acylated monosaccharide residue. An ESI-MS and CID-MS/MS method has been developed for the determination of the acylation sites of polyphenolic glycosides that possess an acylated monosaccharide residue. Twelve polyphenolic glycosides including four new ones have been identified or characterized in P. capitatum. Eight (including the new ones) of the twelve glycosides were reported for the first time from this plant. The developed ESI-MS and CID-MS/MS method provided a very useful strategy for the determination of the sites of polyphenolic glycosides that possess an acylated monosaccharide residue. The acylation site could be determined by the characteristic product ion spectra of the in-source CID-generated O-acyl monosaccharide ion [B(1) ](+) . The presented work may facilitate the structural characterization of these types of compounds. Copyright © 2012 John Wiley & Sons, Ltd.
    Rapid Communications in Mass Spectrometry 11/2012; 26(21):2483-92. · 2.51 Impact Factor
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    ABSTRACT: To study the protective effect of flowers, branch with leaves and main stem of Polygonum orientale on H9c2 myocardial cells oxidative injury induced by H202 and discuss its efficacious substance foundation of anti-myocardial ischemia. UPLC fingerprint was established for flowers, branch with leaves and main stem of P. orientale, and the chromatographic peak was identified. Meanwhile, the protective effect of composites of flowers, branch with leaves and main stem of P. orientale in different proportions on myocardial cells oxidative injury was observed (with MTT method as indicators of concentration screening and cell livability) and MDA were detected. The correlation analysis was made between activity information of composites and chemical information of UPLC fingerprint to infer efficacious substance foundation. Branch with leaves and flowers from Polygonum orientale showed a protective effect on H9c2 myocardial cells oxidative injury. According to the study on spectrum-activity relationship, peak 3-5, 11-14, 18-19, 21-25 showed a positive correlation with their antioxidant activities. This study determined activity of Polygonum orientale on anti-oxidative injury, laying an experimental foundation for in-depth study and development of P. orientale herbs.
    Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 09/2012; 37(17):2585-8.
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    ABSTRACT: To investigate the chemical constituents of the active fraction of Polygonum capitatum. Various preparative chromatographic techniques were used for the isolation and purification of the compounds in the flavonoid-enriched fraction and their structures were determined by comparison of their physicochemical and chromatographic data with those of the authentic samples and spectral analysis. Fourteen compounds were obtained and identified as 1-O-P-D-(6'-O-galloyl)-glucopyranosyl-3-methoxy-5-hydroxybenzene (1) ,5,7-dihydroxy-4H-chromen-4-one (2), ellagic acid (3), myricetrin (4), hirsutine (5), rutin (6), quercetin-3-O-(2"-O-galloyl)-beta-D-glucopyranoside (7) , quercetin-3-O-( 3"-O-galloyl) -/3-D-glucopyranoside (8), quercitrin (9) , kaempferol-3-O-alpha-L-rhamnopyranoside (10), quercetin-3-O-(2"-O-galloyl) -alpha-L-rhamnopyranoside (11), quercetin-3-O-(3"-O-galloyl) -alpha-L-rhamnopyranoside (12), quercetin (13), kaempferol (14). The flavonoid-enriched fraction contains flavonols and their glycosides as its major components,which might be responsible for the biological effects of Polygonum capitatum. Compounds 1, 8 and 12 are isolated from the genus Polygonum for the first time; Compound 3 is isolated from Polygonum capitatum for the first time.
    Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials 09/2012; 35(9):1425-8.
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    ABSTRACT: This study was designed to investigate the processes underlying the neurotoxicity induced by β-amyloid peptide (Aβ) in the rat brain, as well as to examine whether scutellarin (Scu) can prevent this neurotoxicity. Thirty Wistar rats were randomly divided into 3 groups, i.e., untreated (control), treated with Aβ and treated with both Aβ and Scu. The treated rats were subjected to bilateral intracerebroventricular injection of Aβ(25-35) with or without subsequent dietary exposure to Scu. Learning and memory were assessed with the Morris water maze test; the activities of superoxide dismutase (SOD) and monoamine oxidase (MAO) were assayed biochemically; expression of the interleukin-1β (IL-1β), interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) proteins was determined by immunohistochemistry; and neuronal apoptosis was detected with Annexin staining followed by flow cytometry. The animals treated with Aβ exhibited impaired learning and memory; reduced SOD and elevated MAO activity, elevated protein levels of IL-1β, IL-6 and TNF-α; and a higher percentage of apoptotic neurons in the brain. Interestingly, all of these effects were ameliorated by administration of Scu. These findings indicate that the deficits in learning and memory demonstrated by the rats receiving Aβ are due to elevated oxidative stress and inflammation, which result in apoptosis and that Scu may prevent these deleterious effects.
    Experimental and toxicologic pathology: official journal of the Gesellschaft fur Toxikologische Pathologie 06/2012; · 1.43 Impact Factor
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    ABSTRACT: INTRODUCTION: A flavonoid-enriched extract (FEE) of Polygonum orientale was reported to show cardioprotective effect but only very few compounds were reported to contribute to the effect. Identification of compounds interacting with the target cardiac cell is important for the understanding of active compounds. OBJECTIVE: To develop an efficient method for the screening of potential active compounds directly acting on the target cardiac cell in FEE and to structurally characterise these compounds. METHODOLOGY: Flavonoid-enriched extract was prepared by extraction of the plant with water, addition of ethanol to the solution to remove polysaccharides and proteins, and removal of tannins by a polyamide column chromatography. Cell extraction was conducted on a cardiac h9c2 cell and the solution containing compounds released from the cell were desalted by solid phase extraction. Compounds present in the cell extract were detected by ultra-performance liquid chromatography (UPLC) and targeted multi-reaction monitoring (MRM), while their structures were characterised by UPLC-photodiodide array (PDA)-electrospray ion source (ESI)-MS/MS investigations of the FEE. RESULTS: Twenty-three potentially active phenolics including ten flavonoid C-glycosides and six flavonoid O-glycosides have been identified from the 40 compounds screened in the cell extract. Among these compounds, three were new and nine were identified from this plant for the first time. Strategies for the structural characterisation of flavonoid glycosides were also discussed. CONCLUSION: The study has shown that FEE contains the flavonoid as its major principles and the coupling of UPLC-PDA-ESI-MS/MS and targeted UPLC-MRM with target cell extraction is an efficient method for the screening and structural characterisation of potential active compounds. Copyright © 2012 John Wiley & Sons, Ltd.
    Phytochemical Analysis 06/2012; · 2.48 Impact Factor
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    ABSTRACT: AimTo investigate antitumor compounds from Vernonia bockiana.Methods The compounds were isolated by column chromatography and preparative HPLC. Their structures were elucidated by 1H and 13C NMR spectroscopic methods and MS experiments. The antitumor activity was evaluated by testing their cytotoxicity against the human promyelomonocyte leukemic cell line HL-60 by the MTT method.ResultsSix sesquiterpene lactones, 8α-(4-hydroxymethacryloyloxy)-10α-hydroxy-13-methoxyhirsutinolide (1), 8α-methacryloyloxy-10α-hydroxy-13-O-methylhirsutinolide (2), piptocarphin A (3), 8α-[4-hydroxymethacryloyloxy]-10α-hydroxyhisutinolide-13-O-acetate (4), piptocarphin F (5), and 8α-acetoxy-10α-hydroxy-13-O-methylhirsutinolide (6), and one known inone glycoside, saussureosides B (7), were isolated from the whole plant of V. bockiana. The six sesquiterpene lactones showed cytotoxic activity (IC50 3.87–12.5 μmol·L−1) against the human leukemic cell line HL-60 while the inone glycoside 7 was inactive in the test.Conclusion Compounds 1, 2, 6, and 7 were obtained for the first time from this plant; The sesquiterpene lactones present in V. bockiana were active as antitumor agents against the human leukemic cell line HL-60.
    Chinese Journal of Natural Medicines 05/2012; 10(3):230–233.
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    ABSTRACT: A series of phosphonate ester prodrugs of adefovir incorporating l-amino (thio)acid and non-steroidal anti-inflammatory drug (NSAID) moieties were synthesized and their anti-HBV activity and renal cell toxicity were evaluated in HepG2 2.2.15 and HK-2 cells respectively. Bioactivity evaluation results revealed that this kind of adefovir prodrug have lower renal cell toxicity than adefovir dipivoxil. Compounds 8a and 8b, incorporating the NSAID ketoprofen and the l-amino acid (Val or Ile) structural fragments, exhibited more potent anti-HBV activity than adefovir dipivoxil with IC(50) = 0.51 and 0.73 μM, SI = 1697.64 and 881.92 respectively. In vitro stability studies showed that the synthesized prodrugs have higher chemical and plasma stability than the positive control adefovir dipivoxil.
    European Journal of Medicinal Chemistry 03/2012; 49:211-8. · 3.43 Impact Factor
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    Li-li Guo, Zhi-zhong Guan, Yong-lin Wang
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    ABSTRACT: To examine the protective effects of scutellarin (Scu) on rats with learning and memory deficit induced by β-amyloid peptide (Aβ). Fifty male Wistar rats were randomly divided into 5 groups: control, sham operation, Aβ, Aβ+Scu, and Aβ+piracetam groups. Aβ(25-35) was injected into the lateral ventricle (10 μg each side). Scu (10 mg/2 mL) or piracetam (10 mg/2 mL was intragastrically administered per day for 20 consecutive days following Aβ treatment. Learning and memory was assessed with Morris water maze test. The protein and mRNA levels of nicotinic acetylcholine receptor (nAChR) α4, α7, and β2 subunits in the brain were examined using Western blotting and real-time PCR, respectively. The activities of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) in the brain and plasma were measured using Ellman's colorimetric method. In Aβ group, the escape latency period and first platform cross was significantly increased, and the total number of platform crossings was significantly decreased, as compared with the control and the sham operation groups. Both Scu and piracetam treatment significantly reduced the escape latency period and time to cross platform, and increased the number of platform crosses, but there were no significant differences between Aβ+Scu and Aβ+piracetam groups. In Aβ group, the protein levels of nAChR α4 and α7 subunits in the cerebral cortex were significantly decreased by 42%-47% and 58%-61%, respectively, as compared to the control and the sham operation groups. Scu treatment caused upregulation of α4 and α7 subunit proteins by around 24% and 30%, respectively, as compared to Aβ group, but there were no significant differences between Aβ+Scu and Aβ+piracetam groups. The protein level of nAChR β2 subunit had no significant difference among different groups. The mRNA levels of nAChR α4, α7, and β2 subunits were not significantly changed. In Aβ group, the activities of AChE and BuChE in the brain were significantly increased, but were significantly decreased in the plasma, as compared to the control and the sham operation groups. Scu or piracetam treatment restored the activities in brain and plasma nearly to the levels in the control group. The results suggest that Scu may rescue some of the deleterious effects of Aβ, possibly by stimulating nAChR protein translation and regulating cholinesterase activity.
    Acta Pharmacologica Sinica 12/2011; 32(12):1446-53. · 2.35 Impact Factor
  • Li-li Guo, Yong-lin Wang, Yong Huang
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    ABSTRACT: To observe the effect of Scutellarin (Scu) on expressions of nicotinic acetylcholine receptor (nAChR) subunit protein and mRNA in dementia rats, and to study its possible mechanism on dementia. Forty-two Wistar rats were randomly divided into 5 groups, i.e., the normal control group (n=6), the sham-operative group (n=6), the memory deficit model group, the Scu treatment group (n=10), and the positive drug (piracetam) control group (n=10). The dementia rat model was established by bilateral ventricle injection with beta-amyloid peptide (Abeta)(25-35) and abdominal cavity injection with D-galactose. Rats in the Scu treatment group or the piracetam control group were treated with Scu or piracetam by gastrogavage. The learning and memory ability of rats were detected by Morris water maze test, nAChR alpha4, alpha7, and beta2 subunits at protein and mRNA levels were detected by Western blot and Real-time PCR respectively. Compared with the normal control group and the sham-operative group, the learning and memory ability decreased in rats of the model group (P<0.05). nAChR alpha4 and alpha7 subunit protein expressions were obviously lowered (P<0.05), but changes of beta2 were not obvious. No obvious change of mRNA expressions in all three nAChR subunits was seen (P>0.05). After treatment of Scu, the learning and memory ability was greatly improved, nAChRs alpha4 and alpha7 subunit protein expressions increased in rats with dementia (all P<0.05). No obvious change of mRNA expressions in all three nAChR subunits was seen (P>0.05). No obvious difference of each index was shown between the Scu treatment group and the positive drug (piracetam) control group. Scutellarin could improve the learning and memory ability of dementia rats. Its mechanism might be associated with its up-regulation of nAChR expressions.
    Zhongguo Zhong xi yi jie he za zhi Zhongguo Zhongxiyi jiehe zazhi = Chinese journal of integrated traditional and Western medicine / Zhongguo Zhong xi yi jie he xue hui, Zhongguo Zhong yi yan jiu yuan zhu ban 06/2011; 31(6):789-93.