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A new protocol for radical transformations of thioamides promoted by Lewis base-boryl radicals is reported. The desulfurizative reduction to access organic amines was enabled utilizing 4-dimethylaminopyridine-BH3 as the boryl radical precursor and PhSH as the polarity reversal catalyst. Alternatively, the chain process for unsaturated thioamides was switched to an annulation reaction using N-heterocyclic carbene-BH3 as the boryl radical precursor and sterically bulky Ph3CSH as the catalyst, allowing for the construction of N-heterocyclic and carbocyclic skeletons.

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BACKGROUND: Saponins identified from fenugreek (Trigonella foenum-graecum) seeds are reported effective on dyslipidemia. However, the definite mechanism is still not elucidated systematically. In this study, we evaluate the effects of saponin extract on cholesterol absorption, metabolism, synthesis, and reverse cholesterol transport in vivo. METHODS: Saponin extract was prepared according to a craft established in our previous study. After the establishment of dyslipidemia model, 40 male Sprague-Dawley rats were divided into five groups, namely the control group (normal diet plus normal saline), HFD group (high fat diet plus normal saline), Lipitor group (high fat diet plus Lipitor (2 mg/kg)), and L, M, and H-saponin groups (high fat diet plus saponin in dosages of 6, 12, and 24 mg/kg, respectively). Rats were sacrificed at the end of the 9th week after treatment. Biochemical characteristics of rats were tested, histopathological sections of liver tissue were observed, and the protein and mRNA expression of related factors of cholesterol in the intestine and liver were determined. One-way ANOVA test (SPSS software version 11.5, Chicago, IL, USA) was used to determine statistically significant differences between the HFD and other groups. RESULTS: In saponin groups, the serum lipid, bile acid efflux, anti-peroxide activities, and lipid area of liver tissue improved. Cholesterol 7alpha-hydroxylase and scavenger receptor class B type I elevated in the liver. 3-hydroxy-3-methylglutaryl coenzyme A reductase levels were suppressed in both the serum and liver. However, significant cholesterol efflux was not found and Niemann-Pick C1-Like 1 levels elevated in the intestine. CONCLUSION: The mechanisms of saponin in Fenugreek effect on ameliorating dyslipidemia are probably related to accelerated cholesterol metabolism, inhibited cholesterol synthesis, and facilitated reverse cholesterol transport, but not cholesterol absorption.

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OBJECTIVE: To study the accuracy of endoscopic polyp size measurement by disposable graduated biopsy forceps (DGBF). METHODS: Accurate gradation of 1 mm was made in the wire of disposable graduated biopsy forceps, which was used to measure the size of tumors under endoscopy. Fifty-eight polyps from 43 patients underwent endoscopy in our department from May to June 2013 were enrolled. Size of polyp was measured and compared among DGBF, routine estimation and direct measurement after resection. The accuracy of polyp size measurement was investigated by four colonoscopists who had finished at least 2000 procedures of colonoscopy. RESULTS: The mean diameter of post-polypectomy measurement was (1.02±0.84) cm. Diameter was less than 1 cm in 36 polyps, 1 to 2 cm in 15, and over 2 cm in 7. The mean diameter of visual estimation was (1.29±1.07) cm, and the difference was significant as compared with actual size (P=0.000). The mean diameter measured by DGBF was (1.02±0.82) cm, and the difference was not significant as compared with actual size (P=0.775). The ratio of visual estimation to actual size was 1.29±0.31, and DGBF estimation to actual size was 1.02±0.11 with significant difference (P=0.000). The accurate rate of DGBF in estimating polyp size was 77.6% (45/58), which was obviously higher as compared to visual estimation [19.0% (11/58), P=0.000]. CONCLUSION: The accuracy of DGBF as a scale in the estimation of poly size increases as compared to visual estimation.

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OBJECTIVES: This study aims to determine the efficacy and tolerability of capecitabine (CAP) plus bevacizumab (BEV) as treatment for frontline metastatic colorectal cancer (mCRC) in frail and/or elderly patients. MATERIALS AND METHODS: This was an open label, multi-site, single arm, phase II study in frontline mCRC. In this study, patients (pts) who were frail (ECOG 2) or older patients with ECOG 1 performance status (PS) received CAP (1000 mg/m(2) bid, 14 days of every 21 days) plus BEV (7.5mg/kg iv once every 21 days). The primary objective was progression free survival (PFS). Secondary objectives were overall response rate (ORR) and toxicity. RESULTS: In terms of patients: 50 were enrolled; 5 withdrew consent prior to treatment; 45 were treated, and 41 were evaluable. The mean age was 75.9 (range 54-93) and 62% had an ECOG 2 PS. The median PFS was 6.87 months (95% CI, 5.1-11.5 months) and median overall survival was 12.7 months (95% CI, 6.9-12.7 months). The most common grades 3-4 toxicities were: diarrhea (17.8%), fatigue (13.3%), hand-foot syndrome (13.3%), dehydration (8.9%), hypertension (6.7%) and vomiting (6.7%). CONCLUSIONS: The results of this trial support the use of CAP plus BEV as first-line treatment for frail/elderly patients with metastatic CRC. The ORR (40%) is comparable to pooled data in elderly on fluorouracil (5-FU)+BEV. The median PFS (7.2 months) in this study is slightly lower than that seen with 5-FU+BEV but this study had a high percentage of ECOG PS 2 patients. Side effects were manageable with no new safety signals.

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<p><b>OBJECTIVE</b>To study the accuracy of endoscopic polyp size measurement by disposable graduated biopsy forceps (DGBF).</p><p><b>METHODS</b>Accurate gradation of 1 mm was made in the wire of disposable graduated biopsy forceps, which was used to measure the size of tumors under endoscopy. Fifty-eight polyps from 43 patients underwent endoscopy in our department from May to June 2013 were enrolled. Size of polyp was measured and compared among DGBF, routine estimation and direct measurement after resection. The accuracy of polyp size measurement was investigated by four colonoscopists who had finished at least 2000 procedures of colonoscopy.</p><p><b>RESULTS</b>The mean diameter of post-polypectomy measurement was (1.02±0.84) cm. Diameter was less than 1 cm in 36 polyps, 1 to 2 cm in 15, and over 2 cm in 7. The mean diameter of visual estimation was (1.29±1.07) cm, and the difference was significant as compared with actual size (P=0.000). The mean diameter measured by DGBF was (1.02±0.82) cm, and the difference was not significant as compared with actual size (P=0.775). The ratio of visual estimation to actual size was 1.29±0.31, and DGBF estimation to actual size was 1.02±0.11 with significant difference (P=0.000). The accurate rate of DGBF in estimating polyp size was 77.6% (45/58), which was obviously higher as compared to visual estimation [19.0% (11/58), P=0.000].</p><p><b>CONCLUSION</b>The accuracy of DGBF as a scale in the estimation of poly size increases as compared to visual estimation.</p>

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Lymphatic mapping and sentinel node biopsy are well-established techniques for staging and managing patients with melanoma, breast cancer and other malignancies that spread initially to the regional lymph nodes. Identification of tumor in the sentinel node is the most precise staging technique currently available. The sentinel node is the site of metastatic melanoma in approximately 20% of melanoma patients and if tumor is present in the sentinel node it is customary to perform a complete dissection of the lymph nodes of the affected nodal basin. This may be overtreatment for some patients as tumor is identified in the nonsentinel nodes of only one-third of sentinel node-positive melanoma patients treated by completion lymphadenectomy. If it were possible accurately to identify the minority of patients with tumor in the nonsentinel nodes, the patients most likely to benefit from lymphadenectomy, the remaining patients could be spared a potentially morbid operation that is unlikely to confer clinical advantage. In 90 patients with a melanoma-positive sentinel node, who subsequently had a completion lymphadenectomy, we evaluated and compared the capacity of characteristics of the primary melanoma and of the sentinel node to predict individuals likely to have tumor in nonsentinel nodes. We assessed the Breslow thickness of the primary, the amount of tumor in the sentinel node (relative tumor area) and, as an index of immune modulation of the sentinel node, the density of dendritic leukocytes in the nodal paracortex. The relative area of tumor in the sentinel node and Breslow thickness of the primary melanoma most accurately predicted the presence of tumor in the nonsentinel nodes (P=0.0001 in both cases-Wilcoxon rank sums). The presence of melanoma in the nonsentinel nodes was also predicted by the density of dendritic leukocytes in the paracortex (P=0.008-Wilcoxon rank sums). These three observations assessed alone and in combination predict the presence of tumor in the nonsentinel nodes with high accuracy. The same characteristics also significantly correlated with tumor recurrence (tumor burden, P=0.0001, Breslow, P=0.0001 and dendritic cell density, P=0.0007) and death from melanoma (tumor burden, P=0.0001, Breslow, P=0.0001 and dendritic cell density, P=0.0026).

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