OBJECTIVE: To design and synthesize a series of novel amino acid-modified ursolic acid derivatives containing primary amino-group and to investigate their antitumor activities against gastric carcinama in vitro. METHODS: 1, 2-Ethylenediamine was added to the C28 site of ursolic acid(UA) and the resulting intermediates were conjugated to amino acid to get the amino acid-modified ursolic acid derivatives. The effects of these UA derivatives on the growth of BGC823 cells and AGS cells were assessed by MTT assay. Meanwhile, Annexin V/PI dual staining and cell cycle analysis were performed to investigate the anti-tumor mechanism. RESULTS: Most of the derivatives exhibited more powerful cytotoxicity than UA against these two gastric cancer cell lines. The apoptosis of BGC823 cells incubated with compound 3 or compound 4 were observed. Cell cycle analysis showed that compound 3-6 triggered 44.69% -92.64% of the treated AGS cells into apoptotic status. CONCLUSION: Potent anticancer abilities of these UA derivatives bearing primary amido are achieved by inducing apoptosis. Introducing primary amino group to UA is an effective way to develop new UA derivatives with enhanced anti-proliferative activities. Copyright 2012 by the Chinese Pharmaceutical Association.

Objective　To evaluate the effect of tamoxifen on the endometrium. Methods　Hysteroscopy and endometrial biopsies were performed in 26 patients with breast cancer receiving tamoxifen and having vaginal bleeding or endometrial thickness detected by ultrasound. In addition 78 women with postmenopausal bleeding without receiving tamoxifen underwent the same examination. Results　Thirteen (50.0%) patients receiving tamoxifen had endometrial or endocervical polyps, whereas 14 cases(17.9%) not receiving tamoxifen developed the polyps （P＜0.05）. Nine (34.6%) patients receiving tamoxifen had thyperplasias, which was significantly higher than that of women not receiving tamoxifen (P<0.05). Conclusions　The incidence of endometria disease in the patient with breast cancer receiving tamoxifen was increased. These patients should be closely monitored by transvaginal sonography and hysteroscopy.

Animals ; Cardiomyopathy, Dilated ; Disease Models, Animal ; Mice ; Mice, Transgenic

OBJECTIVETo investigate in situ visualization using near-infrared quantum dots (QDs) conjugated with arginine- glycine-aspartic acid (ROD) peptide fluorescent probes in oral squamous cell carcinoma (08CC).

METHODSQDs with emission wavelength of 800 nm (QD800) were conjugated with RGD peptides to produce QD800-RGD fluorescent probes. Human OSCC cell line BcaCD885 was inoculated in nude mice cheeks to establish OSCC mouse models. Frozen BcaCD885 tumor slices were immunofluorescence double stained by using QD800-RGD and CD105 monoclonal antibody and were observed using a laser scanning confocal microscope. QD800-RGD was injected into the OSCC models through the tail veins, and the in situ visualization was analyzed at different time points. The mice were sacrificed 12 h after injection to isolate tumors for the ex vivo analysis of probe localization in the tumors.

RESULTSQD800-RGD specifically targeted the integrin avβ3 expressed in the endothelial cells of tumor angiogenic vessels in vitro and in vivo, producing clear tumor fluorescence images after intravenous injection. The most complete tumor images with maximal signal-to-noise ratios were observed 0.5 h to 6 h after injection of the probe and significantly reduced 9 h after the injection. However, the tumor image was still clearly visible at 12 h.

CONCLUSIONUsing intravenously injected QD800-RGD generates high quality OSCC images when integrin avβ3, which is expressed in the endothelial cells of tumor angiogenic vessels, is used as the target. The technique offers great potential in the diagnosis and individual treatment of OSCC.

Animals ; Arginine ; Aspartic Acid ; Carcinoma, Squamous Cell ; Cell Line, Tumor ; Fluorescent Dyes ; Glycine ; Humans ; Mice ; Mice, Nude ; Mouth Neoplasms ; Oligopeptides ; Peptides ; Quantum Dots

Objective To assess the clinical value of HRCT in diagnosis of cholesteatomatous tympanitis.Methods HRCT findings of 26 patients with cholesteatomatous tympanitis proved by surgery and pathology were analyzed.Results HRCT findings of cholesteatomatous tympanitis included:soft tissue mass in the superior tympanium,tympanal sinus and mastoid(100%,26/26),destruction of the bone includeing ossicles chain (92%,24/26),secutum(46%,12/26),facial nerve canal (54%,14/26);enlargement of the tympaniosinus with sclerosing borders;intracranial complications including temple abscess(1 case),meningitis(1 case).Conclusion HRCT is of great value in diagnosis of cholesteatomatous tympanitis.

Objective To investigate changes of serum levels of interleukin(IL)-4,-6,-8 and tumor necrosis factor-?(TNF-?),and probe their clinical significance in children with Henoch-Schonlein purpura(HSP)/ HenochSchonlein purpura nephritis(HSPN).Methods Serum levels of IL-4,-6,-8 and TNF-? of 45 children with HSP/HSPN and 43 healthy children were examined by enzyme linked immunosorbent assay(ELISA),changes and correlation between the aforementioned cytokines in children with HSP /HSPN were analyzed.Results 1.Serum levels of IL-4,-6,-8 and TNF-? of children with HSP were higher than those of control group(P0.05);The serum level of TNF-? was positively correlated to the serum levels of IL-6,-8 of patients with HSP(r=0.670 P

Object To study the chemical structures and DNA cleavage activity of the water-soluble constituents from Polygonum bistorta L.Methods To isolate the constituents by reverse phase chromatography, and characterize their structures by the analysis of chemical property and spectral data.Results Ten compounds were isolated from the 60% acetone extract of the rhizoma from P.bistorta.Their structures were elucidated as gallic acid (Ⅰ), tryptophan (Ⅱ), 2, 6-dihydroy-bezoic acid (Ⅲ), (+)-catechin (Ⅳ), chlorogenic acid (Ⅴ), (-)-epicatechin-5-O-?-D-glucopyranoside (Ⅵ), (+)-catechin-7-O-?-D-glucopyranoside (Ⅶ), 1-(3-O-?-D-glucopyranosyl-4, 5-dihydroxy-phenyl)-ethanone (Ⅷ), (+)-catechin-5-O-?-D-glucopyranoside (Ⅸ) and (-)-epicatechin (Ⅹ), respectively.Conclusion Compounds Ⅱ, Ⅲ, Ⅴ-Ⅹ were isolated from the plant for the first time.Compounds Ⅰ, Ⅳ, Ⅵ, Ⅶ, Ⅸ, Ⅹ showed significant DNA cleavage activity.

Object To study the chemical structures and bioactivity of the water-soluble constituents from Polygonum cuspidatum Sieb. et Zucc. Methods To isolate the constituents by reverse phase methods, and characterize their structures by the analysis of chemical property and spectral data. Results Six compounds were isolated from the 60% aqueous acetone extract from the rhizome of P. cuspidatum. Their structures were elucidated as reveratrol (Ⅰ); piceid (Ⅱ); 2, 3-dihydro-2-(4′-O-?-D-glucopyranosyl-3′-methoxy-phenyl)-3-hydroxymethyl-5-(3-hydroxypropyl)-7-methoxybenzofuran (Ⅲ); 2, 6-dimethoxy-p-hydroquinone-1-O-?-D-glucopyranoside (Ⅳ); 5, 7-dihydroxy-isobenzofuran (Ⅴ) and 5, 7-dihydroxy-isobenzofuran-7-O-?-D-glucopyranoside(Ⅵ), respectively. Conclusion Compounds Ⅲ-Ⅵ are isolated from the plant for the first time. Compounds Ⅰ-Ⅵ show no DNA cleavage activity. Compound Ⅱ exhibits weak cytotoxicity against two human cancer cell lines (KB and MCF-7) in vitro.

Objective To investigate the effectiveness and safety of minimal invasive surgery combined with ventriculoscope for the treatment of basal ganglia hemorrhage.Methods From June 2014 to June 2015 there were 57 patients with basal ganglia hemorrhage were selected into this study.These patients were signed into the minimal invasive surgery combined with ventriculoscope group and the craniotomy group according to the methods of surgery they received.And the clinical outcomes of the two groups were compared.Results Compared with the craniotomy group,patients in the minimal invasive surgery combined with ventriculoscope group got a significantly lower Glasgow coma scale at 7 days,14 days and 28 days after the operation (P =0.02,0.04,0.04);the hospital stays were significantly reduced in the minimal invasive surgery combined with ventriculoscope group [(21.45 ±5.67)d vs.(25.67 ±7.45)d,P =0.02];and the operation time were significantly reduced as well [(134.45 ±21.11)min vs.(178.65 ±45.32)min,P =0.000)].There was no significant difference in intra-cranial pressure,rate of hematoma clearance,rate of organ functional failure,rate of re-bleeding and mortality 28 days after operation (P >0.05).Conclusion The minimal invasive surgery combined with ventriculoscope is effective and safe for the treatment of basal ganglia hemorrhage,which is worthy of popularization.