Identification of ferroptosis as a novel mechanism for antitumor activity of natural product derivative a2 in gastric cancer

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

Genome mining combined metabolic shunting and OSMAC strategy of an endophytic fungus leads to the production of diverse natural products

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

Discovery of thiosemicarbazone derivatives as effective New Delhi metallo-β-lactamase-1 (NDM-1) inhibitors against NDM-1 producing clinical isolates

@#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.

Helioscopianoids A-Q, bioactive jatrophane diterpenoid esters from

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.

Chemical constituents from Morus notabilis and their cytotoxic effect / 药学学报

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).

Two novel isocoumarins from Erigeron breviscapus / 药学学报

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.

Chemical constituents of Neoalsomitra integrifoliola / 中国中药杂志

<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>

Chemical constituents from herbs of Erigeron breviscapus / 中国中药杂志

<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>

Study on chemical constituents from branches and leaves of Polyalthia nemoralis / 中国中药杂志

<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>

Alkaloids and anthraquinones from branches and leaves of uvaria kurzii / 中国中药杂志

<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>

2-Pyridinethiolate derivatives from branches and leaves of Polyalthia nemoralis and their cytotoxic activities / 中国中药杂志

<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>

Chemical constituents of Uvaria kurzii / 中国中药杂志

<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>

Aporphine alkaloids from branches and leaves of Polyalthia nemoralis / 中国中药杂志

<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>

Dosimetrical Comparison of Three Dimensional Conformal Radiation Therapy for Esophageal Carcinoma / 医疗卫生装备

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.

Studies on strategies to launch “Traditional Chinese Medicine Genome Project” / 中草药

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

Diels-Alder type adducts in stem bark of Morus mongolica / 中草药

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.

Comparison Between Varian Localization System and Tosplane Localization System / 医疗卫生装备

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.