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1.
Acta Pharmaceutica Sinica B ; (6): 1513-1525, 2021.
Article in English | WPRIM | ID: wpr-888817

ABSTRACT

Ferroptosis is a type of cell death accompanied by iron-dependent lipid peroxidation, thus stimulating ferroptosis may be a potential strategy for treating gastric cancer, therapeutic agents against which are urgently required. Jiyuan oridonin A (JDA) is a natural compound isolated from Jiyuan

2.
Acta Pharmaceutica Sinica B ; (6): 572-587, 2021.
Article in English | WPRIM | ID: wpr-881155

ABSTRACT

Endophytic fungi are promising producers of bioactive small molecules. Bioinformatic analysis of the genome of an endophytic fungus

3.
Acta Pharmaceutica Sinica B ; (6): 203-221, 2021.
Article in English | WPRIM | ID: wpr-881133

ABSTRACT

@#New Delhi metallo-β-lactamase-1 (NDM-1) is capable of hydrolyzing nearly all β-lactam antibiotics, posing an emerging threat to public health. There are currently less effective treatment options for treating NDM-1 positive “superbug”, and no promising NDM-1 inhibitors were used in clinical practice. In this study, structure–activity relationship based on thiosemicarbazone derivatives was systematically characterized and their potential activities combined with meropenem (MEM) were evaluated. Compounds 19bg and 19bh exhibited excellent activity against 10 NDM-positive isolate clinical isolates in reversing MEM resistance. Further studies demonstrated compounds 19bg and 19bh were uncompetitive NDM-1 inhibitors with Ki = 0.63 and 0.44 μmol/L, respectively. Molecular docking speculated that compounds 19bg and 19bh were most likely to bind in the allosteric pocket which would affect the catalytic effect of NDM-1 on the substrate meropenem. Toxicity evaluation experiment showed that no hemolysis activities even at concentrations of 1000 mg/mL against red blood cells. In vivo experimental results showed combination of MEM and compound 19bh was markedly effective in treating infections caused by NDM-1 positive strain and prolonging the survival time of sepsis mice. Our finding showed that compound 19bh might be a promising lead in developing new inhibitor to treat NDM-1 producing superbug.

4.
Acta Pharmaceutica Sinica B ; (6): 805-817, 2018.
Article in English | WPRIM | ID: wpr-690862

ABSTRACT

The EtOH extracts of the whole plants of afforded 17 new jatrophane diterpenoid esters, helioscopianoids A-Q (-), along with eight known compounds (-). Their structures were elucidated by extensive spectroscopic methods and Mo(OAc)-induced ECD analysis, and the structures of compounds , , and were confirmed by X-ray crystallography. Compounds - were evaluated for inhibitory effects on P-glycoprotein (P-gp) in an adriamycin (ADM)-resistant human breast adenocarcinoma cell line (MCF-7/ADR) and neuroprotective effects against serum deprivation-induced and rotenone-induced PC12 cell damage. Compounds and increased the accumulation of ADM in MCF-7/ADR cells by approximately 3-fold at a concentration of 20 μmol/L. Compound could attenuate rotenone-induced PC12 cell damage, and compounds , , and showed neuroprotective activities against serum deprivation-induced PC12 cell damage.

5.
Acta Pharmaceutica Sinica ; (12): 579-82, 2015.
Article in Chinese | WPRIM | ID: wpr-483364

ABSTRACT

Une new flavonoids named as notabilisin K (1), together with four known compounds, morusin (2), mulberrofuran A (3), neocyclomorusin (4) and mornigrol F (5) are separated from 95% ethanol extracts of the twigs of Morus notabilis. Compounds 2-5 are separated from this plant for the first time. Notabilisin I, notabilisin J exhibits certain effect against cells of HCT-116, HepG2 and A2780 with IC50 values ranging from 1.47 μmol x L(-1) to 5.46 μmol x L(-1). Morusin exhibits strong effect against five kinds of human cancer cells (BGC823, A2780, HCT-116, HepG2 and NCI-H1650) with IC50 values ranging from 0.74 μmol x L(-1) to 1.58 μmol x L(-1).

6.
Acta Pharmaceutica Sinica ; (12): 1128-30, 2013.
Article in Chinese | WPRIM | ID: wpr-445576

ABSTRACT

Two novel isocoumarins, erigeronone C (1) and D (2), were isolated from the ethanol extract of the whole plant of Erigeron breviscapus (Vant.) Hand.-Mazz (Compositae). Their structures were respectively elucidated as 8, 9-dihydroxypyrano [3, 2-c] isochromen-4, 6-dione (1) and 4, 7-dihydroxy-3-(3-hydroxy-4-oxo-4H-pyran-2-yl)-1H-isochromen-1-one (2) on the basis of spectral analyses. Both structures of 1 and 2 possess a gamma-pyrone moiety and that is rare in natural products.

7.
Article in Chinese | WPRIM | ID: wpr-266969

ABSTRACT

<p><b>OBJECTIVE</b>To study the chemical constituents of the n-BuOH fraction of 95% ethanolic extract of leaves of Neoalsomitra integrifoliola.</p><p><b>METHOD</b>The compounds were isolated with kinds of column chromatography. The structures were determined by MS and NMR spectroscopic techniques.</p><p><b>RESULT</b>Eight compounds were isolated from the n-BuOH fraction of 95% ethanolic extract and their structures were identified as 2-phenylethyl rutinoside (1), rutin (2), kaempferol-3-O-alpha-L-rhamnopyranosyl-(1-->6)-beta-D-glucopyranoside (3), isorhamnetin-3-O-alpha-L-rhamnopyranosyl-(1-->6)-beta-D-glucopyranoside (4), methyl chlorogenate (5), guanosine (6), adenosine (7), myo-inositol (8), respectively.</p><p><b>CONCLUSION</b>All compounds were isolated from this genus for the first time.</p>


Subject(s)
Cucurbitaceae , Chemistry , Drugs, Chinese Herbal , Chemistry , Organic Chemicals , Chemistry
8.
Article in Chinese | WPRIM | ID: wpr-356098

ABSTRACT

<p><b>OBJECTIVE</b>To study the chemical constituents from herbs of Erigeron breviscapus.</p><p><b>METHOD</b>The compounds were isolated and purified by various chromatographic techniques. Their structures were identified on the basis of physicochemical properties and spectral analysis.</p><p><b>RESULT</b>Twelve compounds were isolated and structurally identified as quercetin-3-O-beta-D-glucoside (1), 5, 7-dihydroxychromone (2), 3-O-caffeoyl-gamma-quinide (3), naringenin (4), 3, 5-di-O-caffeoylquinic acid (5), 3,4-di-O-caffeoylquinic acid (6), 4, 5-di-O-caffeoylquinic acid (7), 1,3-di-O-caffeoylquinic acid (8), 1, 5-di-O-caffeoylquinic acid (9), 3-O-caffeoylquinic acid (10), 4-O-caffeoylquinic acid (11) and chlorogenic acid (12).</p><p><b>CONCLUSION</b>Compounds 1-4 were isolated from this plant for the first time.</p>


Subject(s)
Chlorogenic Acid , Chromatography , Chromones , Erigeron , Chemistry , Flavanones , Magnetic Resonance Spectroscopy , Mass Spectrometry , Plants, Medicinal , Chemistry , Quercetin , Quinic Acid
9.
Article in Chinese | WPRIM | ID: wpr-252950

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the chemical constituents of the branches and leaves of Polyalthia nemoralis.</p><p><b>METHOD</b>The compounds were isolated and purified by silica gel, macroporous adsorption resin and Sephadex LH-20 column chromatographic methods. Their chemical structures were elucidated on the basis of physicochemical properties and spectral data.</p><p><b>RESULT</b>Fourteen compounds were isolated and identified as syringic acid (1), 3-methoxy-4-hydroxycinnamic acid (2), vanillic acid (3), 4-hydroxybenzoic acid (4), mauritianin (5), (+)-xylopinidine (6), (+)-oblongine(7), (+)-tembetarine (8), eythritol (9), D-mannitol (10), ethyl-beta-D-glucopyranoside (11), (+)-magnoflorine (12), stepharanine (13), (2S, 4R)-4-hydroxy-2-piperidine-carboxylic acid (14), respectively.</p><p><b>CONCLUSION</b>All the compounds were isolated from the genus Polyalthia for the first time; compounds 6 and 13 showed inhibitation activities against multi tumor cell lines.</p>


Subject(s)
Alkaloids , Chemistry , Pharmacology , Antineoplastic Agents, Phytogenic , Chemistry , Pharmacology , Aporphines , Chemistry , Pharmacology , Cell Line, Tumor , Cell Survival , Chromatography, Agarose , Methods , Coumaric Acids , Chemistry , Pharmacology , Gallic Acid , Chemistry , Pharmacology , Humans , Kaempferols , Chemistry , Pharmacology , Parabens , Chemistry , Pharmacology , Plant Extracts , Chemistry , Pharmacology , Plant Leaves , Chemistry , Plant Stems , Chemistry , Polyalthia , Chemistry , Vanillic Acid , Chemistry , Pharmacology
10.
Article in Chinese | WPRIM | ID: wpr-252884

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the chemical constituents of the branches and leaves of Uvaria kurzii.</p><p><b>METHOD</b>The compounds were isolated and purified by silica gel and Sephadex LH-20 column chromatographic methods. Their chemical structures were elucidated on the basis of physicochemical properties and spectral data.</p><p><b>RESULT</b>Nine compounds were isolated and identified as: bidebiline A(1), annobraine (2), oxoputerine (3), atherospermidine (4), liriodenine (5), physcion (6), questin (7), rubiadin 3-methyl ether (8), emodin (9).</p><p><b>CONCLUSION</b>Compound 1-4, 6-9 were isolated from the genus Uvaria for the first time. Compound 3-5 showed inhabitation activities against tumor cell lines A549, Bel7402, BGC823, HCT-8, A2780, respectively.</p>


Subject(s)
Alkaloids , Chemistry , Anthraquinones , Chemistry , Aporphines , Chemistry , Emodin , Chemistry , Magnetic Resonance Spectroscopy , Plant Leaves , Chemistry , Plant Stems , Chemistry , Uvaria , Chemistry
11.
Article in Chinese | WPRIM | ID: wpr-346947

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the active constituents of the branches and leaves of Polyalthia nemoralis.</p><p><b>METHOD</b>The compounds were isolated and purified by silica gel, macroporous adsorption resin and Sephadex LH-20 column chromatographic methods. Their chemical structures were elucidated on the basis of physicochemical properties and spectral data.</p><p><b>RESULT</b>Eight compounds were isolated and identified as: zincpolyanemin (1), nickel bis-(pyridine-N-oxide-2-thiolate) (2), cupric bis (pyridine-N-oxide-2-thiolate (3), 2-methanesulfonyl-pyridine (4), 2-pyridinethiolate N-oxide (5), 2,2'-dithiodipyridine (6), 2-thiohydroxypyridin-N-oxide-2-S-beta-D-gluco pyranoside (7) and pyridine-N-oxide (8), respectively.</p><p><b>CONCLUSION</b>Compounds 2, 4-6, 8 were new natural products. The bioassays in vitro against five human tumor cell lines with MTT method showed stronger cytotoxic activities (IC50 0.05-0.09 mg x L(-1)) for compounds 1-3 and 6, and weaker cytotoxic activities (IC50 5.49-7.71 mg x L(-1)) for compound 5.</p>


Subject(s)
Cell Line, Tumor , Cell Survival , Drugs, Chinese Herbal , Chemistry , Pharmacology , Humans , Magnetic Resonance Spectroscopy , Plant Leaves , Chemistry , Plant Stems , Chemistry , Polyalthia , Chemistry , Pyridines , Chemistry
12.
Article in Chinese | WPRIM | ID: wpr-307618

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the chemical constituents of the branches and leaves of (Jvariu kurzii.</p><p><b>METHOD</b>Compounds were isolated and purified by silica gel and Sephadex LH-20 column chromatography. Their chemical structures were identified on the basis of physicoc hemical properties and spectral data.</p><p><b>RESULT</b>Nineteen compounds were isolated and identified as: beta-sitosterol hexadecanoate (1), stigmasterol hexadecanoate (2), beta-acetylsitosterol (3), beta-acetylstigmasterul (4), tetratriacontanol (5), dotriacontanoic acid (6), beta-sitosterol (7), stigmasterol (8), 5alpha-stigmast-3 , 6-dione (9) , 5alpha-stigmast-22-ene-3,6-dione (10), vanillic acid (11), protocatechuic acid (12), N-(p-trans-collmaroyl) tyramine (13). kaempferol-3-O-beta-D-(6"-O-p-coumaryoyl) galactopyraunoside (14), kaempferol-3-O-rutinoide (15), rutin (16), daucosterol (17), L-quebrachitol (18), allantoin (19), respectively.</p><p><b>CONCLUSION</b>Compounds 1-6, 9, 10, 13, 18, 19 were isolated from Annonaceac plants; Compounds 14-16 were obtained from the gemis Uvaria; an 7, 8, 11, 12, 17 were separated from this plant respectively for the first time.</p>


Subject(s)
Plant Extracts , Chemistry , Uvaria , Chemistry
13.
Article in Chinese | WPRIM | ID: wpr-307588

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the aporphine alkaloids in the branches and leaves of Polyalthia nemoralis.</p><p><b>METHOD</b>The compounds were isolated and purified by silica gel and Sephadex LH-20 column chromatographies. Their chemical structures were elucidated on the basis of physicochemical properties and spectral data.</p><p><b>RESULT</b>Five aporphine alkaloids were isolated and identified as: bidebiline A (1), annobraine (2), lanuginosine (3), liriodenine (4), oxostephanosine (5), respectively.</p><p><b>CONCLUSION</b>For the first time, Compounds 2 and 5 were obtained from Polyalthia while 1, 3 and 4 isolated from this plant. The bioassays in vitro against five human tumor cell lines with MTT method showed moderate cytotoxic activities (IC50 1 mg x L(-1)) of compounds 3-5.</p>


Subject(s)
Antineoplastic Agents, Phytogenic , Chemistry , Pharmacology , Aporphines , Chemistry , Pharmacology , Cell Line, Tumor , Humans , Plant Leaves , Chemistry , Plant Stems , Chemistry , Polyalthia , Chemistry
14.
Article in Chinese | WPRIM | ID: wpr-595849

ABSTRACT

Objective To assess and compare the advantages and disadvantages of five fields of three dimensional conformal radiation therapy(3DCRT),three fields of 3DCRT and the simulator-guided radiation therapy for patients with esophageal carcinoma.Methods Twenty patients with esophageal carcinoma were treated by three dimensional conformal radiation therapy,at the same TPS,three Dimensional conformal radiation therapy target and normal tissue of three radiotherapies were simulated.The treatment planning was five days per week with 1.8~2.0 Gy per fraction。 5 fractions per week,5OGy per 5~6 weeks. Results Compared with simulator-guided radiation therapy,3DCRT planning has better dose distribution and protection of normal tissue. Conclusion Esophageal cancer conformal radiotherapy can reduce the radiation injury of the normal tissue and complications,and improve treatment of conformal radiotherapy and the target dose distribution.

15.
Article in Chinese | WPRIM | ID: wpr-680964

ABSTRACT

The fundamental principle of the “Traditional Chinese Medicine (TCM) Genome Project” is to carry out genomic studies from the molecular level to discover effective functional genes in medicinal plants which may be cloned and expressed in factories or to transfer into plants for field cultivation Another approach is to carry out research studies to obtain enzymic genes capable of synthesizing bioactive compounds to be replicated in laboratory metabolic engineering processes The subject matter of “TCM Genome Project” and its significance for the modernization of TCM were expounded

16.
Article in Chinese | WPRIM | ID: wpr-575515

ABSTRACT

Objective To study the Diels-Alder type adducts in the stem bark of Morus mongolica.Methods The compounds were isolated and purified by silic gel column chromatography,RP18 and Sephadex LH-20.The structures were identified by various spectral evidence.Results Six Diels-Alder type adducts were obtained and they were albanin F(Ⅰ),kuwanon L(Ⅱ),dimoracin(Ⅲ),kuwanon J(Ⅳ),mulberrofuran J(Ⅴ),mulberrofuran Q(Ⅵ).Conclusion Compounds Ⅱ,Ⅲ,and Ⅴ are isolated from the plant for the first time and compounds ⅣⅥ show the anti-oxidation activities.

17.
Article in Chinese | WPRIM | ID: wpr-593563

ABSTRACT

Objective To investigate precision error between Varian auri-point localization system and Tosplane digital-bed localization system. Methods Varian Eclipse localization method and Topslane localization method were used separately to locate one target area for one same patient. Then deviations on the tumor center coordinate were measured under the simu- lation localization machine. Results Under two localization methods, the length error: 1.7mm ?0.3mm; the width error: 0.5mm?0.4mm; the altitude error: 1.2mm?0.4mm. Conclusion The curative effect of radiotherapy would be improved by applying the Topslane localization bed to the Varian Eclipse plan system.

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