Aged ; Cardiac Pacing, Artificial ; adverse effects ; Echocardiography ; methods ; Heart Failure ; diagnostic imaging ; etiology ; Humans ; Male

Poly(ADP-ribose)polymerase-1 (PARP-1) plays a significant role in the DNA repair process by catalyzing the transfer of ADP-ribose from NAD+ to its receptors. It is a promising anticancer drug target and many PARP-1 inhibitors have been developed and used in the clinical trial. In this work, a series of 3-(2-oxo-2-substituted acetamido)benzamides have been synthesized and their inhibitory activities against PARP-1 were evaluated. Of all the tested compounds, six compounds displayed inhibitory activities with IC50 values ranging from 0.23 to 5.78 µmol.L-1 . The binding pose of compound 5a was predicted using molecular docking to facilitate further structural modification.
Antineoplastic Agents ; Benzamides ; chemistry ; DNA Repair ; Drug Design ; Humans ; Molecular Docking Simulation ; Poly(ADP-ribose) Polymerase Inhibitors ; chemical synthesis ; chemistry ; Poly(ADP-ribose) Polymerases

An endophytic bacterium strain EBS05 from Cinamonum camphra was identified as Bacillus subtilis by morphological taxonomy and sequence analysis of 16S~23S rRNA intergenic spacer regions. Properties of antimicrobial compound produced by EBS05 were assayed. The active compound had the maximum absorbance peak at ?213.5 nm. The antimicrobial activity was stable in solution with pH value from 5 to 8, and decreased significantly in solution with pH value less than 4.0 or more than 9.0. The antimicrobial compound had thermodynamics stability. Its activity changed a little after treated at 60?C~80?C for two hours, and compared with 65% original activity after treated at 1?105 Pa for 30 minutes. The active substance had high resistance to ultraviolet radiation and protease K. Antimicrobial compound was soluble in alcohol solu- tion, which was easily dissolved in methanol and ethanol, but not dissolved in ethyl acetate, acetonitrile and petroleum et al.

Eyelid Diseases ; diagnosis ; immunology ; pathology ; Facial Dermatoses ; diagnosis ; immunology ; pathology ; HIV Infections ; complications ; immunology ; Humans ; Immunocompromised Host ; Male ; Middle Aged ; Molluscum Contagiosum ; complications ; diagnosis ; immunology ; pathology

Vitamin C precusor-2-keto-L-gulonic acid can be prepared directly by mixed culture of Ghiconobacter oxy-dans SCB329 and Guconobacter subaxydans SCB110. To obtained its high yield, firstly, the proportion of the two micro- organisms, the ingredients of medium and the initial pH were optimized in shake flaskd, then L9 (34) orthogonal experiment confirmed that urea, C. S. L had high degree statistical meaning. Based on these data, an optimized fermentation media was obta ined: D-Sorbitol 9g, C. S.L1.5g, Urea1.5g, KH2PO40.1g, CaCO30.2g. By-product can be inhabited to the greatest extent and the yield increases by 20%.

To study the chemical constituents of the inflorescences of Coreopsis tinctoria from Xinjiang, isolation and purification of constituents were carried out by column chromatography on macroporous resin (D101) , MCI gel, MDS gel, silica gel, Sephadex LH-20 and semi-preparative HPLC. The structures of the compounds were identified by physicchemical properties and spectral data analysis. Fourteen compounds were isolated and identified as coretinterpenoid A (1), coretinphenol (2), quercetin (3), quercetin-3-O-β-glucopyranoside (4), luteolin (5), taxifolin (6), 7, 3', 5'-trihydroxyflavanone (7), isookanin (8), isookanin-7-O-β-D-glucopyranoside (9), 5, 7, 3', 5'-tetrahydroxyflavanone-7-O-β-D-glucopyranoside (10), butein (11), okanin (12), sulfuretin (13), and linocinnamarin (14). Compound 1 was a new isabolane-type sesquiterpenoid and compounds 4, 10 and 13 were isolated from this plant for the first time.
Coreopsis ; chemistry ; Sesquiterpenes ; chemistry ; isolation & purification

OBJECTIVEThe SSR information in the transcriptome of Erigeron breviscapus was analyzed in this study, in order to further develop new functional genes SSR markers laid a solid foundation.

METHODSSR loci were searched in all of 52,060 unigenes by using est_timmer. Perl program and SSR primers were designed by Primer3. Furthermore, 36 pairs of primers were randomly selected for the polymorphism analysis on 13 Erigeron breviscapus plants collected from different places.

RESULTA total of 3639 SSRs were found in the transcriptome of Erigeron breviscapus, distributed in 3260 unigenes with the distribution frequency of 6.99%. Di-nucleotide repeat was the main type, account for as much as 34.41% of all SSRs, followed by mono-nucleotide (31.41%) and tri-nucleotide repeat motif (28.08%). The di-nucleotide repeat motifs of AT/AT and AC/GT were the predominant repeat types (28.71%). The tri-nucleotide repeat motifs of AAT/AT was the predominant repeat types (7.94%). For validation the availability of those SSR primers, we randomly selected 36 pairs of primers for PCR amplification. Among them, 34 pair primers (94.44%) produced clear and reproductive bands, 19 pair primers showed polymorphism (52.78%), and 13 Erigeron breviscapus plants were divided into 2 groups.

CONCLUSIONThere are numerous SSRs in Erigeron breviscapus transcriptome with high frequency and various types, this will provide abundant candidate molecular markers for genetic diversity study and genetic map in this plant.

China ; DNA Primers ; genetics ; Erigeron ; classification ; genetics ; Genetic Variation ; Microsatellite Repeats ; Phylogeny ; Polymorphism, Genetic ; Transcriptome

The shape and structure of granules are controlled by the granulation process, which is one of the main factors to determine the nature of the solid dosage forms. In this article, three kinds of granules of a traditional Chinese medicine for improving appetite and promoting digestion, namely, Jianwei Granules, were prepared using granulation technologies as pendular granulation, high speed stirring granulation, and fluidized bed granulation and the powder properties of them were investigated. Meanwhile, synchrotron radiation X-ray computed micro tomography (SR-µCT) was applied to quantitatively determine the irregular internal structures of the granules. The three-dimensional (3D) structure models were obtained by 3D reconstruction, which were more accurately to characterize the three-dimensional structures of the particles through the quantitative data. The models were also used to quantitatively compare the structural differences of granules prepared by different granulation processes with the same formula, so as to characterize how the production process plays a role in the pharmaceutical behaviors of the granules. To focus on the irregularity of the particle structure, the box counting method was used to calculate the fractal dimensions of the granules. The results showed that the fractal dimension is more sensitive to reflect the minor differences in the structure features than the conventional parameters, and capable to specifically distinct granules in structure. It is proved that the fractal dimension could quantitatively characterize the structural information of irregular granules. It is the first time suggested by our research that the fractal dimension difference (Df,c) between two fractal dimension parameters, namely, the volume matrix fractal dimension and the surface matrix fractal dimension, is a new index to characterize granules with irregular structures and evaluate the effects of production processes on the structures of granules as a new indicator for the granulating process control and optimization.
Drugs, Chinese Herbal ; analysis ; Fractals ; Medicine, Chinese Traditional ; Powders ; Quantitative Structure-Activity Relationship ; Synchrotrons ; Technology, Pharmaceutical ; Tomography, X-Ray Computed

According to documents of recent fifty years the article summarized the herbalogical study, processing, chemical constituent, quality standard, pharmacologic action and clinical study of Oroxylum indicum. The chemical constituents mainly are flavonoids, glycoside and volatile oil. It also contains pterocarpan and rhodioside with p-hydroxyphenylethanols and cyclohexanols. Quantitative index was added in the quality standard of china pharmacopeia since 1995, but the quantitative standard is blank at the present, and the baicalin was mostly used for quantitative standard in the documents which lack of mark. Baicalein -7-O-diglucoside didn't existed in the other plants. It's mark will do good to the enhancement of quality standard. Pharmacologic action and clinical study were mainly anti-inflammatory, anti-mutagenesis, antibiosis, anticancera,and coughing.
Animals ; Anti-Bacterial Agents ; chemistry ; pharmacology ; Anti-Inflammatory Agents ; chemistry ; pharmacology ; Antineoplastic Agents, Phytogenic ; chemistry ; pharmacology ; Bignoniaceae ; chemistry ; Humans ; Molecular Structure ; Plant Extracts ; chemistry ; pharmacology ; Plants, Medicinal ; chemistry

Objective To elucidate the association of genetic polymorphisms of key molecules in JAK/STAT signaling pathway with susceptibility of hepatocellular carcinoma (HCC).Methods A total of 367 HCC patients and 367 healthy controls were recruited in this sex- and age-matched case-control study.Genetic polymorphisms of IL-6 (rs1800796,-572C＞G),STAT3 (rs744166,+ 26312T＞C; rs3816769,+ 42240T＞C; rs6503695,+ 40980T＞C),EGFR (rs11543848,+ 142530A＞G),and mTOR (rs7211818,+ 170278A＞G; rs9674559,+ 196983A＞G; rs11653499,+65678G＞A) were genotyped using a mass spectrometry method.Odds ratio (OR) and 95％ confidence interval (CI) were calculated.Results Genotype frequency of the 8 polymorphisms of IL-6,STAT3,EGFR,and mTOR were not significantly different between the patients with HCC and the controls.When stratified by sex,the female subjects who carried STAT3 +26312CC,+ 42240CC,or + 40980CC had a decreased risk of HCC when compared to those who carried TT allele (OR=0.192,95％CI:0.047-0.784; OR=0.180,95％CI:0.045-0.725;OR=0.198,95％ CI:0.049-0.806,respectively).When compared with AA genotype on the site of EGFR + 142530,the (AG+ GG) genotype reduced the risk of HCC in women (OR=0.422,95％CI:0.179-0.994).Conclusion The polymorphisms of IL-6 (rs1800796) and mTOR (rs7211818,rs9674559,and rs11653499) were not associated with the HCC susceptibility.Those carrying CC allele in three loci (rs744166,rs3816769,and rs6503695) of STAT3 and (AG + GG) in rs11543848 of EGFR had a decreased risk of HCC in women.However,these results need to be validated using larger sample size.