[Comparison of Time-intensity Curve with Gadobenatedimeglumine and Gadobutrol on Multiphase Contrast-enhanced Breast MRI].

The purpose of this study was to compare the time-intensity curve (TIC) on multiphase contrast-enhanced breast magnetic resonance imaging (MRI) between Gadobenatedimeglumine (Gd-DTPA) and Gadobutrol. We assessed the images of 53 cases obtained from MRI that had malignant findings by pathology from October 2015 to October 2016 in our institute. Gd-DTPA and Gadobutrol were administrated in 16 and 37 cases, respectively. The TIC of the lesion was classified according to the Kuhl's method (type I: persistent pattern, type II: plateau pattern and type III: washout pattern). Type III was the most common TIC pattern in both the groups (Gd-DTPA, 12 cases; Gadobutrol, 18 cases). Type II was the second common TIC pattern in Gadobutrol group (12 cases). As a result, there was no significant difference in TIC analysis between Gd-DTPA and gadobutrol. In conclusion, the contrast between Gd-DTPA and Gadobutrol contrast media did not differ in TIC pattern of multiphasic contrast-enhanced breast MRI.

Total Synthesis of Clavilactones.

Clavilactones A, B, and D are epidermal growth factor receptor tyrosine kinase inhibitors that were isolated from cultures of the fungus Clitocybe clavipes. Here, we report full details of the total synthesis of these clavilactones. A key feature of our synthetic approach is a ring-opening/ring-closing metathesis strategy that allows the concise transformation of a cyclobutenecarboxylate into a γ-butenolide. Coupled with enantioselective Ti/BINOL-catalyzed alkynylation of a multisubstituted benzaldehyde and ring-closing metathesis of a diene-bearing silylene acetal to construct the 10-membered carbocycle, this strategy enabled the total synthesis of the natural enantiomers (+)-clavilactone A and (-)-clavilactone B. In addition, the correct structure of clavilactone D was determined by the synthesis of two newly proposed structures. This research resulted in the asymmetric synthesis of the revised (+)-clavilactone D.

Identification of seco-clavilactone B as a small-molecule actin polymerization inhibitor.

Phenotype-based chemical screening is an attractive strategy for the identification of bioactive compounds. We searched for a compound that induces cellular morphological change and identified a novel compound that we named seco-clavilactone B (Seco-CB). Treatment with Seco-CB decreased the ratio of filament actin (F-actin) to globular actin (G-actin). An in vitro actin polymerization assay revealed that Seco-CB inhibited actin polymerization directly. Further analysis demonstrated that the inhibitory effect of Seco-CB on actin polymerization was associated with Seco-CB binding to either Thr5 or Cys285 of actin. These data indicate that Seco-CB is a novel actin polymerization inhibitor.