Pd-Catalyzed Three-Component Coupling of Cyclopropenones via Sequential C-C Bond Activation and Allylation.

A novel Pd-catalyzed three-component domino reaction for the stereoselective synthesis of highly functionalized allyl cinnamates has been developed. In this protocol, a sequential process of C-C bond activation and intermolecular allylic substitution was well-organized. The key for this transformation is the in situ generated hydrolysis product of cyclopropenone, which triggered a new reaction with vinylethylene carbonates. The reaction mechanism was investigated, demonstrating the high stereoselectivity and excellent atomic economy in this process.

The clinical significance of transcription factor WD repeat and HMG-box DNA binding protein 1 in laryngeal squamous cell carcinoma and its potential molecular mechanism.

BACKGROUND: Currently, high expression of WD repeat and HMG-box DNA binding protein 1 (WDHD1) has been found in a variety of tumors; but there is no research has been conducted concerning the expression of WDHD1 in laryngeal squamous cell carcinoma (LSCC). Our purpose is to investigate the expression and the latent mechanism of WDHD1 in LSCC. METHODS: Firstly, 9 data sets from the Gene Expression Omnibus (GEO), The Cancer Genome Atlas (TCGA), and ArrayExpress were statistically analyzed to explore the expression of WDHD1 in LSCC; immunohistochemistry was performed in 79 LSCC tissues and 44 non-cancer tissues to further verify the result. In addition, the target gene of WDHD1 was predicted and immunohistochemistry was used to detect the expression of the target gene. The potential mechanism of WDHD1 in LSCC was investigated by Gene Ontology (GO), Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analyses and protein-protein interaction network (PPI). RESULTS: The WDHD1 mRNA was expressed at higher levels in the LSCC tissue than in the normal tissue (SMD=1.90, 95% CI=1.50-2.30); and the results of immunohistochemistry were consistent with the conclusion. Using chip-seq analysis, we found that S-phase kinase-associated protein 2 (Skp2) had a significant binding peak with WDHD1, and the expression of these two genes was significantly positively correlated. Immunohistochemistry showed that Skp2 was also highly expressed in LSCC. In addition, GO and KEGG analysis revealed the WDHD1 positively correlated genes was closely related to cell cycle, and PPI analysis identified 10 hub genes: COL7A1, COL4A2, COL4A1, COL4A6, COL11A1, COL5A2, COL1A1, COL13A1, COL8A1 and COL10A1, which may be critical to the progression of LSCC. CONCLUSIONS: WDHD1 was overexpressed in LSCC tissues. Meanwhile, WDHD1 and its target gene Skp2 for transcriptional regulation may play a role in the progression of LSCC by regulating the cell cycle.

Half-Brain Delineation for Prediction of Radiation-Induced Temporal Lobe Injury in Nasopharyngeal Carcinoma Receiving Intensity-Modulated Radiotherapy.

PURPOSE: To investigate the role of half-brain delineation in the prediction of radiation-induced temporal lobe injury (TLI) in nasopharyngeal carcinoma (NPC) receiving intensity-modulated radiotherapy (IMRT). METHODS AND MATERIALS: A total of 220 NPC cases treated with IMRT and concurrent platinum-based chemotherapy were retrospectively analyzed. Dosimetric parameters of temporal lobes, half-brains, and brains included maximum dose (Dmax), doses covering certain volume (DV) from 0.03 to 20 cc and absolute volumes receiving specific dose (VD) from 40 to 80 Gy. Inter-structure variability was assessed by coefficients of variation (CV) and paired samples t-tests. Receiver operating characteristic curve (ROC) and Youden index were used for screening dosimetric parameters to predict TLI. Dose/volume response curve was calculated using the logistic dose/volume response model. RESULTS: CVs of brains, left/right half-brains, and left/right temporal lobes were 9.72%, 9.96%, 9.77%, 27.85%, and 28.34%, respectively. Each DV in temporal lobe was significantly smaller than that in half-brain (P < 0.001), and the reduction ranged from 3.10% to 45.98%. The area under the curve (AUC) of DV and VD showed an "increase-maximum-decline" behavior with a peak as the volume or dose increased. The maximal AUCs of DVs in brain, half-brain and temporal lobe were 0.808 (D2cc), 0.828 (D1.2cc) and 0.806 (D0.6cc), respectively, and the maximal AUCs of VDs were 0.818 (D75Gy), 0.834 (V72Gy) and 0.814 (V70Gy), respectively. The cutoffs of V70Gy (0.86 cc), V71Gy (0.72 cc), V72Gy (0.60 cc), and V73Gy (0.45 cc) in half-brain had better Youden index. TD5/5 and TD50/5 of D1.2cc were 58.7 and 80.0 Gy, respectively. The probability of TLI was higher than >13% when V72Gy>0 cc, and equal to 50% when V72Gy = 7.66 cc. CONCLUSION: Half-brain delineation is a convenient and stable method which could reduce contouring variation and could be used in NPC patients. D1.2cc and V72Gy of half-brain are feasible for TLI prediction model. The dose below 70 Gy may be relatively safe for half-brain. The cutoff points of V70-73Gy could be considered when the high dose is inevitable.

[Scavenging effect of Sarcandra glabra powder on radiation-induced reactive oxygen species in the parotid gland of miniature pigs].

OBJECTIVE: To investigate the effect of Sarcandra glabra in scavenging reactive oxygen species (ROS) produced by γ-ray irradiation in the parotid gland of miniature pigs. METHODS: Forty-five male miniature pigs were randomly divided into control group, radiation group and radiation plus medication group, and each group contained 3 parallel groups (subgroups a, b and c). From 1 week before exposure of the parotid gland region to 15 Gy γ-ray irradiation (which was not administered in the control group), the miniature pigs in radiation plus medication group were given Sarcandra glabra powder, while those in the other groups received an equal amount of saline. Bilateral parotid glands were taken and weighed on the days 10, 40 and 90 following the exposure in subgroups a, b, and c, respectively, and ROS content in the parotid glands were determined by enzyme-linked immunosorbent assay. RESULTS: The content of ROS was significantly lower in radiation plus medication group than in the radiation group (P<0.01). In the radiation plus medication group, the ROS content showed no significant difference between subgroups a and b or between subgroups a and c (P>0.01), but differed significantly between subgroups b and c (P<0.01). Sarcandra glabra showed a strong ROS-scavenging effect 10 days after the irradiation, and the ROS content was similar with that in the control group (P>0.01); at 40 and 90 days, the ROS-scavenging effect of Sarcandra glabra was still observable, but the ROS content was significantly higher in the irradiation plus medication group than in the control group (P<0.01). CONCLUSION: Sarcandra glabra displays a ROS-scavenging effect in the parotid gland of miniature pigs against irradiation, especially at 10 days following the exposure, which may serve as the main mechanism for the protective effect of Sarcandra glabra against radiation injury in the parotid gland.