Synthesis and in vitro antitumor activity of 1,3,4-oxadiazole derivatives based on benzisoselenazolone.

A series of novel 1,3,4-oxadiazole derivatives based on benzisoselenazolone has been prepared and tested for antiproliferative activity in vitro against the cells of human cancer cell lines: SSMC-7721 (human liver cancer cell), MCF-7 (human breast cancer cell) and A549 (human lung cancer cell). All the compounds obtained exhibited antiproliferative activity and showed selective cytotoxicity against different cancer cells. Compounds 7d and 7i showed significant antiproliferative activities against MCF-7 cells, with IC50 values of 1.07 and 1.76 µM respectively. Compound 7d were found to be the most potent compound against SSMC-7721 cells, with IC50 values 4.46 µM.

[Gene detection of Neisseria spp. isolated from male patients with genitourinary tract infections].

OBJECTIVE: To detect the genes of Neisseria spp. isolated from patients with male genitourinary tract infections, and to study the pathogenicity of non-gonococcal strains of Neisseria and the laboratory diagnosis for the infections caused by Neisseria spp. METHODS: Using polymerase chain reaction and nucleotide sequencing, we amplified and sequenced 4 genes of Neisseria spp. isolated from patients with male genitourinary tract infections, including 16S rRNA, orfl, cppB and nspA. RESULTS: Fourteen Neisseria strains were identified through analysis of the 16S rRNA gene, including 3 N. mucosa strains, 3 N. cinerea strains, 2 N. gonorrhoea strains, 2 N. sicca strains, 2 N. subflava strains, 1 N. lactamica strain, and 1 N. polysaccharea strain. Among them, 9 showed positive results in gonococcal fluorescence-labeled multiplex-PCR detection, 1 in cppB gene reaction, 5 in orfl gene reaction, and 3 in nspA gene reaction. The consistency rate was 85.7% between the above results from our gene detection and those from the routine bacteriological methods. CONCLUSION: The cppB gene is absent in the non-gonococcal strains of Neisseria spp. that can cause male genitourinary tract infection. Most of the strains not only lack virulence-associated orfl and nspA genes, but also show positive results in gonococcal fluorescence-labeled multiplex-PCR detection, which is one of the important reasons for the misdiagnosis and missed diagnosis of gonorrhea infection. The combination of routine bacteriological methods and gene detection in laboratory examinations may help improve the accuracy rates of Neisseria species identification and clinical diagnosis of the infections caused by Neisseria spp.

Quality markers for processed products of Morinda officinalis how based on the "oligosaccharides-spectrum-effect".

Morinda officinalis How (MO) possesses prominent tonifying kidney yang and strengthening bone and muscle effects in traditional Chinese medicine (TCM). Due to the complexity of MO components, the chemical mechanism leading to efficacy changes of MO caused by processing remain unclear. This study aimed to investigate and discover quality markers (Q-markers) related to the clinical efficacy of processed MO. The different processed products of MO have different clinical applications, although they originate from the same medicinal herb. The active chemical components from raw and processed MO that protect against reproductive oxidative stress damage were evaluated. The processed products of MO were prepared by different processing methods. The changes in oligosaccharides during processing were characterized by high-performance liquid chromatography with an evaporative light scattering detector (HPLC-ELSD), and the differential components in raw and processed MO were analyzed using SA, HCA, PCA, and OPLS-DA methods. The protective effects of raw and processed MO oligosaccharides (MOOs) against reproductive oxidative stress damage were evaluated based on the spermatic number, spermatic survival rate, abnormal sperm ratio and serum biochemical indicators in cyclophosphamide-induced (CTX-induced) male mice. The results revealed that processed MOOs had better pharmacological effects than raw MOOs. Therefore, gray correlation analysis (GRA) and the technique for order preference by similarity to ideal solution (TOPSIS) methods were used to investigate the spectrum-effect relationships of MOOs. Spectrum-effect relationship analysis revealed that all of the characteristic peaks contributed to the treatment of reproductive oxidative stress damage, and the relative correlation degrees were greater than 0.6. Among them, the peaks 1 F-fructofuranosylnystose, nystose, and 1-kestose and the peaks X2-X5, which were most closely correlated to the treatment of reproductive oxidative stress damage, were identified as inulin-oligosaccharides and inulo-oligosaccharides, respectively. It was proposed that these constituents could be considered Q-markers for processed products of MO. Thus, this study aimed to explore chemical markers that correlate with the clinical efficacy of processed MO.

[The characteristics of type I, III collagen and LN in pulmonary fibrosis induced by uranium ore dust in rats].

OBJECTIVE: To explore the characteristics of LN and type I, III collagen in pulmonary fibrosis induced by uranium ore dust in rats. METHODS: 60 adult Wistar rats were divided randomly into two groups, control group (30 rats) and uranium ore dust group (30 rats). Non-exposed intratracheal instillation method was used. Uranium ore dust group was exposed 20 mg/ml uranium ore dust suspension 1ml per rat, meanwhile control group was exposed normal saline 1ml per rat. Post-exposed the 7, 14, 21, 30 and 60 d, 6 rats in each group were killed randomly, lung tissue were collected. The pathological changes in lung tissue were observed by microscope using HE staining, the collagen I and III in lungs were observed by polarizing microscope using Biebrich scarlet staining. The expression of LN protein in lung tissue was observed by immunohistochemistry-SP. RESULTS: During lung fibrosis, a large amount of the proliferated I and III collagen in lungs were observed. Post-exposure to uranium ore dust, the characteristics in proliferated collagen in lungs were type I collagen deposited in lung interstitium mainly in the early stage. The area percentage of collagen I and III was increased significantly at 7, 14, 21, 30 and 60d in the experimental group as compared with that in the control group (P < 0.05 or P < 0.01). The over expression of LN in the lung tissue were observed. The expression of LN was distributed in the lung tissue as thickening of the linear or cluster. The integral optical density of LN was increased significantly at 21, 30 and 60 d in the experimental group as compared with that in the control group (P < 0.05 or P < 0.01). CONCLUSIONS: After exposure to uranium ore dust, the characteristics in proliferated collagen in lungs are the type of I collagen deposited in lung interstitium mainly in the early stage, while the type of III collagen increase significantly at the later period. The overexpression of LN exists in the process of pulmonary fibrosis. It suggests that LN has a role effect in the process of pulmonary fibrosis.

Intrahepatic cholangiocarcinoma is more complex than we thought: A case report.

BACKGROUND: Brain metastasis from intrahepatic cholangiocarcinoma is rare. To the best of our knowledge, only a few cases have been reported. The biological behavior was complex, and treatment requires further investigation. CASE SUMMARY: A 62-year-old woman complained of left limb weakness. Abdominal computed tomography showed a 5.0 cm × 5.6 cm lesion in the left lobe of the liver. Tumor markers were normal. Serological analysis indicated absence of hepatitis virus. Brain magnetic resonance imaging revealed a 1.0 cm × 1.3 cm mass in the right frontal lobe. Intrahepatic cholangiocarcinoma with brain metastasis was diagnosed by our liver cancer multidisciplinary team. After sufficient preparation, the patient underwent partial frontal lobotomy and left hemihepatectomy. Histopathological results confirmed that both the lesions were cholangiocarcinoma. Six cycles of gemcitabine combined with S1 were administered. During a 39 mo postoperative follow-up, no sign of local recurrence or distant metastasis was observed. CONCLUSION: This case expands our knowledge concerning the complex and heterogeneous nature of tumor metastasis.

[Diagnosis and treatment of genitourinary infection with non-gonococcal Neisseria in men].

OBJECTIVE: To explore the influence of non-gonococcal Neisseria on the diagnosis and treatment of male genitourinary infection. METHODS: The samples of urethral exudates, prostatic secretions or/and semen were collected from 8 cases of male patients with acute urethritis or chronic prostatitis, then inoculated into gonococcal agar medium, blood agar medium, Sabouraud agar medium and Mycoplasma agar medium, respectively. Neisseria gonorrhoeae, Mycoplasmae, fungi and other bacteria were isolated, Chlamydiae examined by Gemenez staining, and the gram-negative diplococci from the samples identified by oxidase test, biochemical examination and drug sensitivity test. The PCR products of the cryptic plasmid pJD1 gene of the isolated strains were amplified for the identification of Neisseria gonorrhoeae. Based on the results of drug sensitivity tests, intravenous or oral antibiotics were selected for treatment. RESULTS: Eight strains of gram-negative diplococci were isolated in this study, 3 identified as N. mucosa, 4 as N. cinerea and the other 1 as N. lactamica. The PCR identification test of the cryptic plasmid pJD1 gene showed the same positive results in all the strains as in N. gonorrhoeae. The non-gonococcal Neisseria isolated from the male genital tract secretions exhibited a multidrug resistance, especially to quinolones and fosfomycin. All the symptoms disappeared and no pathogens were detected in the patients after a 7-day treatment with Cephalosporins or/and Minocycline. CONCLUSION: Some Neisseria species normally parasitizing the upper respiratory tract can also cause male genitourinary infections, such as gonorrhea-like urethritis and chronic prostatitis. Neisseria gonorrhea could be clinically and etiologically misdiagnosed through such conventional methods as morphological examination, oxidase test and PCR identification test of cryptic plasmid and other nonspecific genes. Intravenous and/or oral antibiotic medication based on the results of drug sensitivity tests can cure acute urethritis and chronic prostatitis induced by non-gonococcal Neisseria in males. Drug resistance of non-gonococcal Neisseria directly affects the success of treatment.

[Penetrability of amikacin into prostate tissues in rat models of chronic bacterial prostatitis].

OBJECTIVE: To establish the rat model of chronic bacterial prostatitis and investigate the penetrability of amikacin to chronic inflammatory prostatic tissues. METHODS: A total of 180 male rats were randomly divided into a normal control group (NC, n=48), a chronic bacterial prostatitis group (CBP, n = 84) and a CBP treatment group (CBPT, n = 48). The prostates of the animals were injected with Xiaozhiling and E. coli respectively to make CBP and CBPT models. The animals of the CBPT group were treated with amikacin by intramuscular injection, their prostate tissues and sera isolated at 1-150 min after the treatment and detected for antibiotic activities, bacteria counts and pathological changes. RESULTS: Obvious chronic inflammatory pathological changes including leukocyte invasion and fibre hyperplasia were observed and E. coli isolated from the prostate tissues of the rats in the CBP and CBPT groups, but no pathological changes, antibiotic activity and bacteria were detected in the the NC group. The numbers of E. coli in the prostate tissues markedly decreased with the time in the two model groups, 30 CFU/mg in the CBP rats at 28 days and 0 CFU/mg in the CBPT group at 10 days after the treatment. Obvious antibiotic activities were found in both the prostate tissues and sera at 2-150 min after the injection. No antimicrobial activities were detected at 12 hours after the treatment either in the sera or in the prostate samples. With the increase of the treatment time and decrease of the bacteria counts, the chronic inflammatory pathological changes were obviously alleviated in the CBPT group. CONCLUSION: Rat models of CBP with chronic inflammatory pathological changes can be successfully established by direct injection of Xiaozhiling and E. coli into the prostate. Amikacin, given by intramuscular injection, can penetrate into the prostate of the CBP rat and produce an antibiotic activity equal to or higher than that of the sera, which may kill sensitive bacteria in the prostate and help to reduce the inflammatory pathological changes and repair the damage to the prostate tissues.

[Effect of Jingang Jiangu pill (see text) on expression of integrin beta1 and alphavbeta3 in ovariectomized osteoporosis model rats].

OBJECTIVE: To investigate the regulatory effect of Jingang Jiangu pill (see text, JGJG) on expression of integrin in ovariectomized rats. METHODS: Fifty ovariectomized 10 months old female rats were randomly divided into 5 groups: Fushanmei group (FSM), Jingang Jiangu pill (see text) group (JGJG), Gusongbao granule group (GSB), Model group (OVX), Sham group. After ovariectomized,the rats were raised in the same environment for 13 weeks. The rats in JGJG group took 0.13 g JGJG pill orally each day for each rat; the rats in GSB group took 0.86 g GSB granule orally each day for each rat; the rats in FSM group took 0.28 mg FSM orally each day for each rat; and the rats in OVX and sham groups took sodium. The treatment duration of rats in above 5 groups was 13 weeks. Bone mineral density (BMD) and the expression of integrin beta1 and alphavbeta3 were detected in each group after the treatment. RESYKTS: The BMD and the expression of integrin beta1 in FSM group, JGJG group and GSB group improved obviously than that of OVX group. There were statistical difference between these groups (P<0.05). The expression of integrin alphavbeta3 of the three treating groups significantly depressed. CONCLUSION: The JGJG pill improves BMD and express of integrin beta1, in ovariectomized rats and reduces express of integrin alphavbeta3 through the regulation of the coupling of osteoblasts and osteoclasts.

[Influence of different surface roughness of opaque porcelain on reflectance and L* value of porcelain fused to metal].

OBJECTIVE: The purpose of this study was to investigate how different surface roughness of opaque porcelain influence reflectance and CIE L* value of porcelain fused to metal (PFM) restorations. METHODS: 48 casted Ni-Cr alloy metal specimens (12.0 mm x 1.0 mm) were fabricated with ShoFu Vintage Halo porcelain and divided into six groups, eight pieces for each group. The specimens in the first group without polishing were used as control. Other groups were polished against 200-, 400-, 600-, 800-, and 1000-grit sandpaper after sintered, respectively. Surface roughness and color parameters of the specimens were measured with a Surface Roughometer EX2154-13 and a spectrocolorimeter, respectively. Ra (arithmetical mean deviation of the profile) was the main standard value to describe the surface roughness of many kinds of meatal or porcelain materials, and here we used it to express surface roughness of opaque porcelain. The data were statistically analyzed by one-way analysis of variance (alpha = 0.05) in SPSS 13.0. RESULTS: The reflectance value increased from 72.386 +/- 3.953 to 78.671 +/- 3.408, and CIE L* value from 90.189 +/- 1.200 to 93.496 +/- 1.070 with the increasing of surface roughness (Ra) of opaque porcelain from (0.226 +/- 0.069) microm to (0.706 +/- 0.082) microm. The same magnitude were also observed after body porcelain and enamel porcelain were sintered on with reflectance increased from 76.301 +/- 3.097 to 81.529 +/- 4.028, and CIE L* value from 80.694 +/- 1.564 to 84.604 +/- 2.964. CONCLUSION: The surface roughness of opaque porcelain had effects on the reflectance and value of PFM restorations. Within the limitation of this study, the recommended Ra range of opaque porcelain was 0.23-0.50 microm.