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2.
Article in English | WPRIM | ID: wpr-285264

ABSTRACT

SRT1720, a new discovered drug, was reported to activate silent information regulator 1 (SIRT1) and inhibit the chondrocyte apoptosis. However, the underlying mechanism remains elusive. In the present study, the chondrocytes were extracted from the cartilage tissues of New Zealand white rabbits, cultured in the presence of sodium nitroprusside (SNP) (2.5 mmol/L) and divided into five groups: 1, 5, 10, and 20 μmol/L SRT1720 groups and blank control group (0 μmol/L SRT1720). MTT assay was used to detect the chondrocyte viability and proliferation, and DAPI staining and flow cytometry to measure the chondrocyte apoptosis. The expression levels of SIRT1, p53, NF-κB/p65, Bax, and peroxisome proliferator-activated receptor gamma coactivator 1-α (PGC-1α) were detected by Western blotting and the expression levels of SIRT1, type II collagen, and aggrecan mRNA by RT-PCR. The results showed that in the SRT1720-treated groups, the nuclei of chondrocytes were morphologically intact and had uniform chromatin. In the blank control group, nuclear rupture into debris was observed in chondrocytes. With the SRT1720 concentration increasing, the chondrocyte viability increased, the apoptosis rate decreased, the protein expression levels of SIRT1 and PGC-1α and the mRNA expression levels of type II collagen and aggrecan increased ({ptP}<0.05), and the expression levels of p53, NF-κB and bax decreased (P<0.05). It was suggested that SRT1720 inhibits chondrocyte apoptosis by activating the expression of SIRT1 via p53/bax and NF-κB/PGC-1α pathways.


Subject(s)
Aggrecans , Genetics , Metabolism , Animals , Apoptosis , Cartilage, Articular , Cell Biology , Metabolism , Cell Proliferation , Cell Survival , Chondrocytes , Cell Biology , Metabolism , Chromatin , Chemistry , Metabolism , Collagen Type II , Genetics , Metabolism , Gene Expression Regulation , Heterocyclic Compounds, 4 or More Rings , Pharmacology , Nitroprusside , Toxicity , Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha , Genetics , Metabolism , Primary Cell Culture , Rabbits , Signal Transduction , Genetics , Sirtuin 1 , Genetics , Metabolism , Transcription Factor RelA , Genetics , Metabolism , Tumor Suppressor Protein p53 , Genetics , Metabolism , bcl-2-Associated X Protein , Genetics , Metabolism
3.
Article in English | WPRIM | ID: wpr-812134

ABSTRACT

The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (INa.L), transient sodium current (INa.T), HERG current (IHERG), and Kv1.5 current (IKv1.5). The values of INa.L, INa.T, IHERG and IKv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited INa.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol · L(-1), which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol · L(-1) for the INa.T. The inhibitory effect of GFA on INa,L was not affected by 200 μmol · L(-1) H2O2. It inhibited IHERG with an IC50 of (273 ± 34) μmol · L(-1) and has slight blocking effect on IKv1.5, decreasing IKv1.5 by only 20.6% at 200 μmol · L(-1). In summary, GFA inhibited INa.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders.


Subject(s)
Analysis of Variance , Animals , Anti-Arrhythmia Agents , Pharmacology , Dose-Response Relationship, Drug , Female , Guinea Pigs , HEK293 Cells , Heart Ventricles , Heterocyclic Compounds, 4 or More Rings , Pharmacology , Humans , Inhibitory Concentration 50 , Male , Membrane Potentials , Myocytes, Cardiac , Metabolism , Patch-Clamp Techniques , Sodium Channel Blockers , Pharmacology , Sodium Channels
4.
Article in English | WPRIM | ID: wpr-242818

ABSTRACT

<p><b>OBJECTIVE</b>To evaluate whether ursolic acid can inhibit breast cancer resistance protein (BCRP)-mediated transport of rosuvastatin in vivo and in vitro.</p><p><b>METHODS</b>Firstly, we explored the pharmacokinetics of 5-fluorouracil (5-FU, a substrate of BCRP) in rats in the presence or absence of ursolic acid. Secondly, we studied the pharmacokinetics of rosuvastatin in rats in the presence or absence of ursolic acid or Ko143 (inhibitor of BCRP). Finially, the concentration-dependent transport of rosuvastatin and the inhibitory effects of ursolic acid and Ko143 were examined in Madin-Darby Canine Kidney (MDCK) 2-BCRP421CC (wild type) cells and MDCK2-BCRP421AA (mutant type) cells.</p><p><b>RESULTS</b>As a result, significant changes in pharmacokinetics parameters of 5-FU were observed in rats following pretreatment with ursolic acid. Both ursolic acid and Ko143 could significantly affect the pharmacokinetics of rosuvastatin. The rosuvastatin transport in the BCRP overexpressing system was increased in a concentration-dependent manner. However, there was no statistical difference in BCRP-mediated transport of rosuvastatin betweent the wild type cells and mutant cells. The same as Ko143, ursolic acid inhibited BCRP-mediated transport of rosuvastatin in vitro.</p><p><b>CONCLUSION</b>Ursolic acid appears to be a potent modulator of BCRP that affects the pharmacokinetic of rosuvastatin in vivo and inhibits the transport of rosuvastatin in vitro.</p>


Subject(s)
ATP Binding Cassette Transporter, Subfamily G, Member 2 , ATP-Binding Cassette Transporters , Physiology , Adenosine , Pharmacology , Animals , Biological Transport , Diketopiperazines , Heterocyclic Compounds, 4 or More Rings , Hydroxymethylglutaryl-CoA Reductase Inhibitors , Pharmacokinetics , Rats , Rats, Sprague-Dawley , Rosuvastatin Calcium , Pharmacokinetics , Triterpenes , Pharmacology
5.
Article in English | WPRIM | ID: wpr-258874

ABSTRACT

Recently, a wide range of food-derived phytochemical compounds and their synthetic derivatives have been proposed for cancer treatment. Unfortunately, data available in related literature focus on the anti-cancer properties of compounds derived from edible plants, while very little is known about those derived from non-edible plants. And thus, the underlying mechanisms of their anti-cancer effects are yet to be elucidated. This review collates the available data on the anti-cancer activities of six phytochemical-derived compounds from edible and non-edible plants, i.e. rottlerin, berbamine, sparstolonin B, sulforaphane, plumbagin and 6-shogaol. These compounds are used as bioactive markers for cytotoxicity against tumors. As such, understanding their mode of action will provide the rationale for the combination strategies of these compounds with other drugs in the battle against cancer.


Subject(s)
Acetophenones , Pharmacology , Therapeutic Uses , Antineoplastic Agents, Phytogenic , Pharmacology , Therapeutic Uses , Benzopyrans , Pharmacology , Therapeutic Uses , Benzylisoquinolines , Pharmacology , Therapeutic Uses , Catechols , Pharmacology , Therapeutic Uses , Heterocyclic Compounds, 4 or More Rings , Pharmacology , Therapeutic Uses , Humans , Isothiocyanates , Pharmacology , Therapeutic Uses , Naphthoquinones , Pharmacology , Therapeutic Uses , Neoplasms , Drug Therapy , Phytotherapy , Plant Extracts , Pharmacology , Therapeutic Uses , Signal Transduction
6.
Article in English | WPRIM | ID: wpr-321374

ABSTRACT

A new hasubanan alkaloid, hernsubanine E (1), as well as two known compounds p-hydroxybenzaldehyde (2) and (-)-syringaresinol (3) have been isolated from the whole plants of Stephania hernandifolia by various column chromatographic methods. Their structures were identified by physicochemical properties and spectral analyses. Compounds 2 and 3 were isolated from the genus of Stephania for the first time.


Subject(s)
Alkaloids , Chemistry , Heterocyclic Compounds, 4 or More Rings , Chemistry , Stephania , Chemistry
7.
Article in Chinese | WPRIM | ID: wpr-291334

ABSTRACT

Five compounds were obtained from the stems and leaves of Sophora flavescens Ait. and ten compounds were obtained from the roots of S. flavescens by various chromatography methods including silica gel column chromatography and preparative HPLC. Their structures were identified on the basis of spectroscopic methods including 1H-NMR, 13C-NMR and ESI-MS, as corchionoside C (1), syringing (2), 2'-deoxythymidin (3), coniferin (4), benzyl O-beta-D-glucopyranoside (5), piscidic acid (6), trifolirhizin (7), kurarinone (8), trifolirhizin-6'-monoacetate (9), sophoraflavanone G (10), isoxanthohumol (11), noranhydroicaritin (12), 4'-methoxyisoflavone-7-O-beta-D-apiofuranosyl-(1 --> 6)-beta-D-glucopyranoside (13), kushenol O (14) and 6"-beta-D-xylopyranosylgenistin (15). Compounds 1-6 were isolated from the Sophora genus for the first time.


Subject(s)
Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Chemistry , Flavanones , Chemistry , Flavonoids , Chemistry , Glucosides , Chemistry , Heterocyclic Compounds, 4 or More Rings , Chemistry , Mass Spectrometry , Molecular Structure , Plant Roots , Chemistry , Sophora , Chemistry
8.
Acta Pharmaceutica Sinica ; (12): 1253-1258, 2013.
Article in Chinese | WPRIM | ID: wpr-259486

ABSTRACT

The present study was designed to observe the protection of Grateloupia filicina polysaccharide (GFP) against hepatotoxicity induced by Dioscorea bulbifera L in mice and its underlying mechanism. GFP was intragastrically (ig) given to mice at various doses. After 6 days, the mice were treated with ethyl acetate extract of Dioscorea bulbifera L (EF, ig). Serum levels of alanine/aspartate aminotransferase (ALT/AST), alkaline phosphatase (ALP), total bilirubin (TB) were measured, and liver histological evaluation was conducted. Furthermore, reductions of liver glutathione (GSH) amount and glutamate cysteine ligase (GCL) activity were tested. The expressions of GCL-c, GCL-m, and HO-1 (heme oxygenase-1) in liver were observed by Western-blot. The results showed that GFP (600 mg x kg(-1)) decreased EF-induced the increase of serum ALT, AST and TB, and GFP (400, 600 mg x kg(-1)) inhibited EF-induced the increase of serum ALP. Liver histological evaluation showed that the liver injury induced by EF was relieved after treated with GFP. GFP further increased liver GSH amount and reversed EF-induced the decrease of GCL activity. The Western-blot result showed that GFP augmented EF-induced the increase of HO-1, and reversed EF-induced the decrease of GCL-c. In conclusion, GFP can act against the oxidative stress liver injury induced by Dioscorea bulbifera L in mice.


Subject(s)
Alanine Transaminase , Blood , Alkaline Phosphatase , Blood , Animals , Aspartate Aminotransferases , Blood , Bilirubin , Blood , Chemical and Drug Induced Liver Injury , Blood , Metabolism , Dioscorea , Toxicity , Glutamate-Cysteine Ligase , Metabolism , Glutathione , Metabolism , Heme Oxygenase-1 , Metabolism , Heterocyclic Compounds, 4 or More Rings , Toxicity , Liver , Metabolism , Pathology , Male , Mice , Mice, Inbred ICR , Oxidative Stress , Plants, Medicinal , Chemistry , Polysaccharides , Pharmacology , Random Allocation , Rhodophyta , Chemistry
9.
Article in Korean | WPRIM | ID: wpr-38428

ABSTRACT

Neuronal differentiation is a complex biological process accompanying cytoskeletal reorganization, including neurite outgrowth and growth cone formation. Therefore, neuronal differentiation is critically regulated by actin-related signaling proteins, such as small Rho GTPases, guanine nucleotide exchange factors (GEFs), and myosins. This study will demonstrate the change in activity of three small Rho GTPases, Rac, Cdc42, and Rho A, by treatment with blebbistatin (BBS), a specific inhibitor for myosin, during bFGF-induced neurite outgrowth in PC12 cells. Treatment with BBS induced morphological changes in growth cones and neurites during differentiation. A marked increase in protrusion and filopodia structures in growth cones, the shaft of neuritis, and cell membranes was observed in the cells treated with BBS. Activity of Rho GTPases showed the alterations in response to BBS. Activities of both Rac and Rho A were inhibited by BBS in a time-dependent manner. By contrast, Cdc42 activity was not changed by BBS. These results suggest that inactivation of myosin II by BBS induced morphological changes in neurites and growth cones and distinct regulation of three Rho GTPases during differentiation of PC12 cells.


Subject(s)
Animals , Biological Phenomena , Cell Membrane , Growth Cones , Guanine Nucleotide Exchange Factors , Heterocyclic Compounds, 4 or More Rings , Myosin Type II , Myosins , Neurites , Neuritis , Neurons , PC12 Cells , Proteins , Pseudopodia , rho GTP-Binding Proteins
10.
Article in English | WPRIM | ID: wpr-17603

ABSTRACT

OBJECTIVE: We have carried out a bibliometric study on the scientific publications in relation to atypical or second-generation antipsychotic drugs (SGAs) in South Korea. METHODS: With the EMBASE and MEDLINE databases, we selected those publications made in South Korea whose title included the descriptors atypic* (atypical*) antipsychotic*, second-generation antipsychotic*, clozapine, risperidone, olanzapine, ziprasidone, quetiapine, sertindole, aripiprazole, paliperidone, amisulpride, zotepine, asenapine, iloperidone, lurasidone, perospirone and blonanserin. We applied some bibliometric indicators of paper production and dispersion with Price's law and Bradford's law, respectively. We also calculated the participation index (PI) of the different countries, and correlated the bibliometric data with some social and health data from Korea (such as total per capita expenditure on health and gross domestic expenditure on research and development). RESULTS: We collected 326 original papers published between 1993 and 2011. Our results state fulfilment of fulfilled Price's law, with scientific production on SGAs showing exponential growth (correlation coefficient r=0.8978, as against an r=0.8149 after linear adjustment). The most widely studied drugs were risperidone (91 papers), aripiprazole (77), olanzapine (53), and clozapine (43). Division into Bradford zones yielded a nucleus occupied by the Progress in Neuro-Psychopharmacology and Biological Psychiatry (36 articles). A total of 86 different journals were published, with 4 of the first 10 used journals having an impact factor being greater than 4. CONCLUSION: The publications on SGAs in South Korea have undergone exponential growth over the studied period, without evidence of reaching a saturation point.


Subject(s)
Antipsychotic Agents , Benzodiazepines , Biological Psychiatry , Bipolar Disorder , Clozapine , Complement Factor B , Dibenzothiazepines , Dibenzothiepins , Health Expenditures , Heterocyclic Compounds, 4 or More Rings , Imidazoles , Indoles , Isoindoles , Isoxazoles , Jurisprudence , Korea , Piperazines , Piperidines , Pyrimidines , Quinolones , Republic of Korea , Risperidone , Schizophrenia , Subject Headings , Sulpiride , Thiazoles , Quetiapine Fumarate , Aripiprazole , Lurasidone Hydrochloride
11.
Chinese Journal of Cancer ; (12): 150-158, 2012.
Article in English | WPRIM | ID: wpr-294426

ABSTRACT

S1-M1-80 cells, derived from human colon carcinoma S1 cells, are mitoxantrone-selected ABCG2-overexpressing cells and are widely used in in vitro studies of multidrug resistance(MDR). In this study, S1-M1-80 cell xenografts were established to investigate whether the MDR phenotype and cell biological properties were maintained in vivo. Our results showed that the proliferation, cell cycle, and ABCG2 expression level in S1-M1-80 cells were similar to those in cells isolated from S1-M1-80 cell xenografts (named xS1-M1-80 cells). Consistently, xS1-M1-80 cells exhibited high levels of resistance to ABCG2 substrates such as mitoxantrone and topotecan, but remained sensitive to the non-ABCG2 substrate cisplatin. Furthermore, the specific ABCG2 inhibitor Ko143 potently sensitized xS1-M1-80 cells to mitoxantrone and topotecan. These results suggest that S1-M1-80 cell xenografts in nude mice retain their original cytological characteristics at 9 weeks. Thus, this model could serve as a good system for further investigation of ABCG2-mediated MDR.


Subject(s)
ATP Binding Cassette Transporter, Subfamily G, Member 2 , ATP-Binding Cassette Transporters , Metabolism , Adenosine , Pharmacology , Animals , Antineoplastic Agents , Pharmacology , Cell Cycle , Cell Line, Tumor , Cell Proliferation , Cell Survival , Cisplatin , Pharmacology , Colonic Neoplasms , Metabolism , Pathology , Diketopiperazines , Doxorubicin , Metabolism , Drug Resistance, Multiple , Drug Resistance, Neoplasm , Female , Heterocyclic Compounds, 4 or More Rings , Humans , Inhibitory Concentration 50 , KB Cells , Male , Mice , Mice, Inbred BALB C , Mice, Nude , Mitoxantrone , Pharmacology , Neoplasm Proteins , Metabolism , Neoplasm Transplantation , Rhodamine 123 , Metabolism , Topotecan , Pharmacology
13.
Journal of Experimental Hematology ; (6): 1450-1455, 2011.
Article in Chinese | WPRIM | ID: wpr-331056

ABSTRACT

The membrane proximal α helix of integrin β subunit cytoplasmic tails plays an important functional role by interacting with various intracellular proteins, namely talin, α-actinin or skelemin. This study was designed to investigate the functional role of 5 highly conserved charged amino acids (R(724), K(725), E(726), E(731), E(733)) within this α helix by site-directed mutagenesis. The result showed that CHO cells expressing the αIIbβ3E726Q mutant had the most prominent phenotype and characterized by defective cell spreading on immobilized fibrinogen. In addition, this E726Q mutation induced membrane blebbing in cells adherent on fibrinogen, and this blebbing could be inhibited by the myosin light chain ATPase inhibitor blebbistatin. It is concluded that the membrane proximal α-helix of integrin β3 subunit is important in linking the phospholipid membrane to the submembraneous actin cortex.


Subject(s)
Animals , CHO Cells , Cell Surface Extensions , Cricetinae , Cricetulus , Heterocyclic Compounds, 4 or More Rings , Chemistry , Integrin beta3 , Genetics , Mutagenesis, Site-Directed , Mutation , Protein Structure, Tertiary
14.
Article in Korean | WPRIM | ID: wpr-81496

ABSTRACT

Psychopharmacology has developed over approximately the past five decades. The remarkable proliferation of information in this area has made it difficult for clinicians to understand the characteristics of various psychotropic agents. Atypical antipsychotics including amisulpride, asenapine, aripiprazole, blonanserin, clozapine, iloperidone, lurasidone, olanzapine, paliperidone, quetiapine, risperidone, ziprasidone, and zotepine cause fewer extrapyramidal problems and have many clinical applications, but they can cause metabolic disturbances. Mood stabilizers and lamotrigine are widely used for bipolar disorder. Other novel anticonvulsants such as topiramate, oxcarbazepine, gabapentin, tiagabine, pregabalin, vigabatrin, levetiracetam, and riulzole have also been tested with diverging or inconclusive results. Antidepressants are commonly used in the clinical treatment of depression and anxiety disorder. However, the mechanism of action of medications used in the treatment of psychiatric disorders remains unclear. Understanding the mechanisms of action and clarifying the diagnosis may enhance the treatment outcome in psychiatry. In this review, we analyzed clinical pharmacology data for each drug within a class and discussed clinical strategies for administering currently available antipsychotics, mood stabilizer/anticonvulsants, and antidepressants widely used for various psychiatric indications.


Subject(s)
Aripiprazole , Amines , Anticonvulsants , Antidepressive Agents , Antipsychotic Agents , Anxiety Disorders , Benzodiazepines , Bipolar Disorder , Carbamazepine , Clozapine , Cyclohexanecarboxylic Acids , Depression , Dibenzothiazepines , Dibenzothiepins , Fructose , gamma-Aminobutyric Acid , Heterocyclic Compounds, 4 or More Rings , Lurasidone Hydrochloride , Isoindoles , Isoxazoles , Nipecotic Acids , Quetiapine Fumarate , Pharmacology, Clinical , Pregabalin , Piperazines , Piperidines , Piracetam , Psychopharmacology , Pyrimidines , Quinolones , Risperidone , Sulpiride , Thiazoles , Treatment Outcome , Triazines , Vigabatrin
15.
Acta Pharmaceutica Sinica ; (12): 39-44, 2011.
Article in Chinese | WPRIM | ID: wpr-353332

ABSTRACT

Metabolic profile of bile acids was used to evaluate hepatotoxicity of mice caused by ethanol extraction of Dioscorea bulbifera L. (ethanol extraction, ET) and diosbulbin B (DB), separately. Ultra-performance liquid chromatography coupled with quadrupole mass spectrometry (UPLC-MS) was applied to determine the contents of all kinds of endogenous bile acids including free bile acids, taurine conjugates and glycine conjugates. Obvious liver injuries could be observed in mice after administrated with ET and DB. Based on the analysis using principle components analysis (PCA), toxic groups could be distinguished from their control groups, which suggested that the variance of the contents of bile acids could evaluate hepatotoxicity caused by ET and DB. Meanwhile, ET and DB toxic groups were classified in the same trends comparing to control groups in the loading plot, and difference between the two toxic groups could also be observed. DB proved to be one of the toxic components in Dioscorea bulbifera L. Bile acids of tauroursodeoxycholic acid (TUDCA), taurochenodeoxycholic acid (TCDCA), taurocholic acid (TCA), taurodeoxycholic acid (TDCA), cholic acid (CA) and others proved to be important corresponds to ET and DB induced liver injury according to analysis of partial least square-discriminant analysis (PLS-DA) and the statistical analysis showed that there were significant differences between the control groups and toxic groups (P < 0.01). Furthermore, good correlation could be revealed between the foregoing bile acids and ALT, AST. It indicated that taurine conjugated bile acids as TUDCA, TCDCA, TCA and TDCA along with CA could be considered as sensitive biomarkers of ET and DB induced liver injury. This work can provide the base for the further research on the evaluation and mechanism of hepatotoxicity caused by Dioscorea bulbifera L.


Subject(s)
Animals , Bile Acids and Salts , Metabolism , Chemical and Drug Induced Liver Injury , Metabolism , Cholic Acid , Metabolism , Chromatography, High Pressure Liquid , Methods , Dioscorea , Toxicity , Drugs, Chinese Herbal , Toxicity , Heterocyclic Compounds, 4 or More Rings , Toxicity , Least-Squares Analysis , Male , Mice , Mice, Inbred ICR , Plants, Medicinal , Toxicity , Principal Component Analysis , Rhizome , Toxicity , Tandem Mass Spectrometry , Methods , Taurochenodeoxycholic Acid , Metabolism , Taurocholic Acid , Metabolism , Taurodeoxycholic Acid , Metabolism
16.
Pakistan Journal of Pharmaceutical Sciences. 2010; 23 (2): 182-187
in English | IMEMR | ID: emr-98352

ABSTRACT

Preliminary pharmacological study was conducted for the pterocarpans macckian [Mac] and trifolirhizin [Trif]. The two compounds isolated from Ononis vaginalis were tested for their hepatoprotective effects against CCU[4] induced hepatotoxicity in rats. Activity was accessed by measuring liver enzymes and NP-SH groups. Estrogenic activity was expressed as increase in uterine weight of young female rats. Rat paw edema as a model of acute inflammation induced in Wistar rats using carragenan was used to evaluate the anti-inflammatory activity. Percentage inhibition of the aggregation induced by adenosine diphosphate [ADP] to platelets-rich plasma [PRP] obtained from rats was used as measure for antiplatelet aggregation effect. The aglycone Mac was only more active than the glycoside Trif in the anti-inflammatory assay. It resulted in 65.7% reduction in carregeenan induced rat paw edema compares with 79.8% reduction by indomethacin at the same molar concentration. The activity of Trif was about half of that of silymarin in reducing the elevated levels of liver enzymes at the same molar concentration. About 10 fold molar concentration of Trif produced about half fold increase in uterine weight produced by 17 beta estradiol


Subject(s)
Animals , Male , Female , Plant Roots/chemistry , Plant Extracts/pharmacology , Drug Evaluation, Preclinical/methods , Fabaceae , Glucosides/pharmacology , Heterocyclic Compounds, 4 or More Rings/pharmacology , Rats, Wistar
17.
Article in Chinese | WPRIM | ID: wpr-315363

ABSTRACT

<p><b>OBJECTIVE</b>To develop a Quantitative Assay of Multi-components by Single - marker (QAMS) for simultaneous determination of three components in Fructus Evodiae, and examine the feasibility of using the relative correction factors between the different types of compounds.</p><p><b>METHOD</b>Rutaecarpine was selected as the internal reference substance; the relative correction factors of evodin and evodiamine were calculated. The contents of three components in 11 batches of samples were determined by both external standard method and QAMS. The validity of the QAMS method was evaluated by comparison of their quantitative results.</p><p><b>RESULT</b>No obvious differences (RSD < 5%) were found in the quantitative results of evodin and evodiamine in 11 batches of Fructus Evodiae determined by the two methods.</p><p><b>CONCLUSION</b>It is feasible and suitable to determine evodin and evodiamine in Fructus Evodiae by QAMS, and this method can be used for a certain different types of compounds.</p>


Subject(s)
Chromatography, High Pressure Liquid , Methods , Drugs, Chinese Herbal , Evodia , Chemistry , Furans , Heterocyclic Compounds, 4 or More Rings , Indole Alkaloids , Plant Extracts , Quinazolines
18.
Article in Chinese | WPRIM | ID: wpr-264841

ABSTRACT

<p><b>OBJECTIVE</b>To study the chemical constituents of Pholidota cantonensis.</p><p><b>METHOD</b>The compounds were isolated and purified on silica gel, Sephadex LH-20, Chromatorex ODS column chromatography and the structures were determined based on the spectral and chemical evidences.</p><p><b>RESULT</b>Four compounds were obtained and characterized as pholidonone (1), ephemeranthoquinone (2), orchinol (3), batatasin III (4).</p><p><b>CONCLUSION</b>They have been isolated from this plant for the first time and pholidonone (1) was a new compound.</p>


Subject(s)
Benzoquinones , Chemistry , Chromatography , Drugs, Chinese Herbal , Chemistry , Heterocyclic Compounds, 4 or More Rings , Chemistry , Magnetic Resonance Spectroscopy , Molecular Structure , Orchidaceae , Chemistry , Resorcinols , Chemistry , Stilbenes , Chemistry
19.
Acta Pharmaceutica Sinica ; (12): 505-510, 2007.
Article in Chinese | WPRIM | ID: wpr-268608

ABSTRACT

Fourteen compounds were isolated from the ethanol extraction of Saposhnikovia divaricata (Turcz.) Schischk using column chromatographic methods after enrichment by macroporous adsorptive resins. They were identified as fangfengalpyrimidine (1), clemiscosin A (2), 5-hydroxy-8-methoxypsoralen (3), sec-O-glucosylhamaudol (4), hamaudol (5), nodakenetin (6), prim-O-glucosylcimifugin (7), cimifugin (8), 4'-O-beta-D-glucosyl-5-O-methylvisamminol (9), 5-O-methylvisamminol (10), marmesin (11), adenosine (12), daucosterol (13) and beta-sitosterol (14) by physico-chemical properties and spectral data. Compound 1 is a new compound. Compounds 2 and 3 were isolated from umbelliferae plants and Saposhnikovia divaricata (Turcz.) Schischk for the first time respectively.


Subject(s)
Apiaceae , Chemistry , Chromatography, Thin Layer , Chromones , Chemistry , Coumarins , Chemistry , Heterocyclic Compounds, 4 or More Rings , Chemistry , Magnetic Resonance Spectroscopy , Mass Spectrometry , Methoxsalen , Chemistry , Molecular Conformation , Molecular Structure , Monosaccharides , Chemistry , Plant Roots , Chemistry , Plants, Medicinal , Chemistry , Pyrimidines , Chemistry , Resins, Synthetic , Xanthenes , Chemistry
20.
Acta Pharmaceutica Sinica ; (12): 1259-1265, 2007.
Article in Chinese | WPRIM | ID: wpr-268194

ABSTRACT

Alternol is purified from fermentation productions of microorganisms named as Alternaria alternata var. monosporus. The research is to investigate the apoptosis-inducing effect of alternol on mouse lymphocyte leukemia (L1210) cells and the possible mechanisms. MTT method was used to evaluate the viability of L1210 cells. Apoptosis of L1210 cells was detected by morphological assessment, DNA electrophoresis assay and flow cytometry. Western blotting analysis was carried out to determine the apoptosis-related proteins. Proliferation inhibition of L1210 cells by alternol was found remarkably in a dose-dependent manner. When treated with alternol, apoptotic morphological features of L1210 cells were observed by fluorescent microscopy (AO/EB) and the apoptosis rate was also elevated in a time-dependent manner. After treatments with various concentrations of alternol for 48 h, DNA laddering appeared. The increase of reactive oxygen species (ROS) production was found after cells were exposed to alternol for 6 h, while the decrease of mitochondrial transmembrane potential (delta psi m) was not found until cells were exposed to alternol for 24 h. Furthermore, the level of Bcel-2 and Bcl-2/Bax was down-regulated, while the level of caspase-3 and caspase-9 but not caspase-8 was up-regulated when alternol was added for 72 h. In summary, the results suggested that alternol could inhibit the proliferation of L1210 cells and induce apoptosis of L1210 cells, which was mediated by mitochondria-dependent pathway.


Subject(s)
Alternaria , Chemistry , Animals , Apoptosis , Caspase 3 , Metabolism , Caspase 8 , Metabolism , Caspase 9 , Metabolism , Cell Line, Tumor , Cell Proliferation , Dose-Response Relationship, Drug , Heterocyclic Compounds, 4 or More Rings , Pharmacology , Leukemia L1210 , Metabolism , Pathology , Membrane Potential, Mitochondrial , Mice , Proto-Oncogene Proteins c-bcl-2 , Metabolism , Reactive Oxygen Species , Metabolism , bcl-2-Associated X Protein , Metabolism
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