Scutellarin inhibits hypoxia-induced epithelial-mesenchymal transition in bladder cancer cells.

Scutellarin, an active component of flavonoid, displays a variety of physiological actions and has been applied for the treatment of diverse diseases including hypertension and cerebral infarction as well as cerebral thrombosis. In recent time, Scutellarin has been demonstrated to possess the anticancer activity. But the biological significance of Scutellarin in bladder cancer (BC) remains to be elucidated. In the current study, we explored the specific effect of Scutellarin on BC progression. We found that Scutellarin inhibited hypoxia-induced BC cell migration and invasion in vitro as well as suppressed hypoxia-induced BC metastasis in vivo. Moreover, Scutellarin significantly reversed hypoxia-promoted epithelial-mesenchymal transition (EMT) in BC cells and the PI3K/Akt and MAPK pathways were implicated in the suppressive effect. Taken together, we suggested the potential value of Scutellarin as a novel anticancer agent for BC treatment.

[Preparation and Synchronized Release Behavior on Porosity Osmotic Pump Tablets of Total Glucosides of Paeony].

Objective: To prepare porosity osmotic pump tablets of total glucosides of paeony( TGP),and to study the behavior on synchronous release of its main components. Methods: Taking the accumulative release of TGP as indexes, through single-factor test and orthogonal design to investigate the optimal formulation porosity osmotic pump tablets of TGP. The main components, paeoniflorin, albiflorin and benzoylpaeoniflorin were employed to study synchronous release of the optimal formulation. Results: The membrane weight, and the content of PEG 400,and diethyl phthalate( DEP) were the main factors influencing the behavior of TGP release. The accumulated release of the prepared osmotic pump release tablets achieved about 90%. Three main components achieved the desired zero-order release profile and had a synchronized release behavior. Conclusion: The prepared porosity osmotic pump tablets of TGP can achieve the behavior of synchronized release of multi-components with good reproducibility.

[Comparison of bioavailability of two kinds of solid dispersion from 10-hydroxycamptothecin in SD rats in vivo].

To improve the bioavailability of 10-hydroxycamptothecin, 10-hydroxycamptothecin solid dispersion(HCPT-SD) and 10-hydroxycamptothecin-phospholipid complex-solid dispersion(HCPT-PC-SD) were prepared, and their solubility and dissolution rate were evaluated in this study. SD rates were administered intragastrically with HCPT-SD or HCPT-PC-SD respectively, then their blood samples were collected at different time intervals. The concentration of HCPT in blood was detected by HPLC method with camptothecin as internal standard, and then its pharmacokinetic parameters were calculated and obtained. The results showed that the Cmax, AUC0-t and AUC0-∞ of both kinds of solid dispersion of HCPT were significantly increased than those of crude drug. The AUC0-t of HCPT-SD was increased by 176.87%, and AUC0-t of HCPT-PC-SD was increased by 254.31% as compared with crude drug. Therefore, the two kinds of solid dispersion of HCPT could significantly enhance the bioavailability of HCPT in SD rates, and the effect of HCPT-PC-SD was more obvious.

[Study and Evaluation on Preparation of Monolithic Osmotic Pump Tablet of Resveratrol].

OBJECTIVE: To prepare monolithic osmotic pump tablet of resveratrol. METHODS: Inclusion technology was adopted to enhance its solubility. The optimal formulation of resveratrol inclusion complex osmotic pump tablets was selected by the single-factor method and orthogonal design. The release in vitro of the optimized formulation was also fitted to different models. RESULTS: The tablets with optimized formulation achieved the desired zero-order release profile in 12 h (r = 0.9963) with the cumulative release over 90%. CONCLUSION: Resveratrol can be prepared into monolithic osmotic pump tablets based on the intermediate of inclusion technology, which have obvious characteristic of zero release.

[Protective effect of polysaccharides extracts from corn silk against cyclophosphamide induced host damages in mice bearing H22 tumors].

OBJECTIVE: To study the protective effect of polysaccharides from corn silk (PCS) against cyclophosphamide (CTX) induced host damages in mice bearing H22 tumors. METHODS: The ascitic and solid tumor bearing mice model were established to investigate the anti-tumor effects of different dose of PCS (100, 200 and 300 mg/kg). The effects of PCS alone and with combination of CTX on tumor weight, survival time, thymus and spleen index, white blood cell, nucleated cell of marrow, serum ALT and AST level were tested. RESULTS: The high-dose PCS (300 mg/kg) had significant inhibitory effects on tumor. After combination with CTX, the tumor inhibitory ratio was enhanced to 68.71%, the survival time of tumor-burdened ascites tumor mice was significantly prolonged to 72.07% compared with CTX group. The Q value of combination group was 0.997. Thymus and spleen index, white blood cell, nucleated cell of marrow decreased by CTX were ameliorated significantly. The level of ALT and AST increased by CTX were reduced by combination with PCS. CONCLUSION: PCS has a potent inhibitory effect on the growth of implanted H22 tumors in mice and has a synergetic effect and an attenuated toxic effect in combination with CTX.

Clinical analysis of percutaneous computed tomography-guided injection of cyanoacrylate for localization of 115 small pulmonary lesions in 113 asymptomatic patients.

OBJECTIVE: This study was performed to assess the clinical feasibility, safety, and effectiveness of a computed tomography (CT)-guided cyanoacrylate injection system and investigate the relationship between clinical features and pathologic characteristics of diminutive pulmonary lesions. METHODS: In total, 115 pulmonary nodules from 113 patients (63 female, 50 male) with a diameter of <20 mm were percutaneously localized with a CT-guided cyanoacrylate injection system and then resected. RESULTS: Of the pure ground-glass opacities (GGOs), 16.0% were atypical adenomatous hyperplasia (AAH), 18.7% were adenocarcinoma in situ (AIS), 49.3% were lung adenocarcinoma (ADC), and 16.0% were benign inflammatory fibrosis/fibrotic scars. Of the mixed GGOs, 18.2% were AAH, 22.7% were AIS, 22.7% were ADC, and 36.4% were benign lesions. Lesions of >10 mm and those located in relation to vessels were significantly more likely to be malignant. The success rate of both the cyanoacrylate injection system and video-assisted thoracoscopic surgery was 100% with no severe complications. CONCLUSIONS: Preoperative localization of small pulmonary nodules using a cyanoacrylate injection system is a safe, simple, and useful technique.

Long-term results of CT-guided percutaneous radiofrequency ablation of inoperable patients with stage Ia non-small cell lung cancer: A retrospective cohort study.

BACKGROUND: This study was performed to retrospectively evaluate the 10-year overall survival (OS), progression-free survival (PFS), and local control rates of patients with inoperable stage Ia non-small cell lung cancer (NSCLC) who underwent computed tomography (CT)-guided radiofrequency ablation (RFA) in a single center. MATERIALS AND METHODS: Fifty patients with inoperable NSCLC underwent RFA between 2004 and 2016. Thoracic surgeons evaluated the patients and performed RFA under CT guidance. Follow-up CT and positron emission tomography/CT scans were obtained. Local control rates and recurrence patterns were analyzed. RESULTS: Seventy-three lesions in 50 patients (M:F = 22:28; median age: 73 years; range: 52-82 years) were treated with CT-guided RFA. The mean lesion size was 2.2 cm (range: 1-3 cm). No procedure-related deaths occurred. Low-grade fever was the most common post-ablation complication, with an incidence rate of 36%. The 1-, 2-, 3-, 5-, and 10-year OS rates of patients with Ia NSCLC were 96.0%, 86.5%, 67.1%, 36.3%, and 1%, respectively, and the 1-, 2-, 3-, and 5-year PFS rates were 94.0%, 77.5%, 43.5%, and 10.8%, respectively. The most common pattern of recurrence was local, and 15 patients with recurrence were treated with repeat RFA. Tumor size <2.0 cm was associated with a significantly improved 3-year survival rate of 78.9%. CONCLUSION: CT-guided RFA is feasible and well tolerated by inoperable patients with inoperable stage Ia NSCLC.

Long-term Observation of CT-guided Radiofrequency Ablation of Lung Neoplasm in 476 Consecutive Patients by a Thoracic Surgical Service: A Single-institutional Experience.

RATIONALE AND OBJECTIVES: The aim of the study was to evaluate the overall survival (OS) rate, progression survival rate, and local control rate over 10 years of medically inoperable patients with lung cancer undergoing computed tomography (CT)-guided radiofrequency ablation (RFA). MATERIALS AND METHODS: Between September 2004 to March 2016, 668 neoplasms were treated in 476 medically inoperable patients (294 men, 60 women; median age 74 years; range 29-84) who underwent CT-guided RFA. All patients had clinical or pathologic evidence of the neoplastic lesion: 22.1% patients with primary non-small cell lung cancer (NSCLC), 22.3% patients with recurrent NSCLC, 45.2% with metastases, and 10.3% with small cell lung cancer. The mean size of the lesions was 3.8 cm (range of 1-16 cm). Twenty-one lesions were re-treated from one to as many as four times. RESULTS: The procedure was technically successful in all cases. No procedure-related deaths occurred in the RFA procedures. Major complications consisted in 104 (21.8%) cases of low-grade fever, 46 (9.6%) of the pneumothorax. The mean follow-up was 32 months. The probabilities of 1-, 2-, 3-, 5-, and 10-year OS rate were 98.1%, 86.6%, 68.9% 34.5%, and 9.5% for primary NSCLC; 59.7%, 18.5%, 8%, 3.4%, and 1.5% for metastases; 93.3%, 59.1%, 49.6%, 19.7%, and 0% for recurrence; and 89.4%, 67.5%, 39.1%, 16.5%, and 0% for small cell lung cancer. In primary NSCLC, progression-free survival (PFS) and OS were significantly related to tumor size, but there was no significant difference in recurrent NSCLC, metastasis, and peripheral SCLC. The median OS of metastases of NSCLC was significantly related to nodal or distant metastases. The most common pattern of recurrence was local; any type of recurrence at 1-year follow-up imaging was seen in 7.1% of primary NSCLC diameter less than 3 cm. CONCLUSIONS: Our experience indicates that CT-guided RFA done by the thoracic surgeons is feasible and safe in high-risk patients. Maximum tumor diameter less than 3 cm and lack of extrapulmonary metastasis are all positive prognostic factors of survival after RFA. RFA offers good local control of recurrent NSCLC, lung metastases, and SCLC, also in the long-term period. RFA should continue to offer an alternative option in medically inoperable patients.

Expression, purification, crystallization and crystallographic analysis of the N-terminal domain of translocated intimin receptor.

Translocated intimin receptor (Tir) is an Escherichia coli-encoded protein that is transported into the host cell through a sophisticated bacterial type III secretion system (T3SS). Tir anchors the infected cell membrane twice using both its N- and C-termini from inside the host cytoplasm for signalling. It plays a key role in enterohemorrhagic Escherichia coli (EHEC) infection, attaching and effacing (A/E) lesions and intracellular signal transduction. Here, the overexpression, purification and crystallization of its N-terminal intracellular domain are reported. The crystal belonged to the orthorhombic space group I4122, with unit-cell parameters a = b = 59.79, c = 183.11 Å. The asymmetric unit contained one molecule, with a solvent content of 51% and a VM of 2.55 Å(3) Da(-1).