SIS3, a good candidate for the reverse of type 2 diabetes mellitus in mice.

TGF-ß signaling plays an extremely important role in the occurrence and development of type 2 diabetes mellitus (T2DM), and the blockade of TGF-ß/Smad3 pathway protests against the high-fat diet-induced obesity and diabetes. As a specific small molecule inhibitor of Smad3 protein, the biological activities of compound SIS3 were evaluated by high-fat diet-induced T2DM model mice. In vivo results indicated that SIS3 can not only significantly reduce the body weight, fat mass, and fasting blood glucose in high-fat diet-induced T2DM model mice, but also improve insulin sensitivity and oral glucose tolerance of high-fat diet-induced T2DM model mice after the injection of SIS3 with 5 mg/kg for 45 days.

MDCT Evaluation of Costal Bone Lesions: Comparison of Axial, Multiplanar, and 3D Volume-Rendered Images: A Retrospective Study.

The aim of this retrospective study was to compare accuracies of axial, multiplanar, and volume-rendered 3-dimensional (3D) images in the diagnosis of costal bone lesions.Forty-one patients, aged from 10 to 72-years old, with costal bone lesions underwent multidetector CT (MDCT). Axial, multiplanar, and 3D-volume-rendered images were reviewed by 3 reviewers for the property of the lesions (fracture, tumor, and tumor-like lesions or inflammation). In case of fracture, the diagnosis was demonstrated with the location of the fracture and the amounts of the costal bone involved. In case of a tumor or tumor-like lesions, the diagnosis was demonstrated pathological property. Final diagnosis was determined by biopsy or surgery. Diagnostic accuracy and interreviewers agreement were evaluated.For the diagnosis of fractures, average accuracy was 77%, 100%, and 100% for axial, multiplanar, and 3D-volume-rendered images, respectively. For the diagnosis of tumor and tumor-like lesions, average accuracy was 90% for axial, 96% for multiplanar, and 99% for 3D-volume-rendered images. For the diagnosis of inflammation lesions, average accuracy was 100% for all the 3 image formats. Interobserver agreement independence of imaging formats was high.Multiplanar and 3D-volume-rendered images were superior to axial images in diagnosis of fracture, tumor, and tumor-like lesions; however, for the evaluation of inflammation lesions, there were no difference by 3 image formats.

Reference ranges for atlantodental interval in adults and its variation with age and gender in a large series of subjects on multidetector computed tomography.

BACKGROUND: The atlanto-dental interval measurement in the cervical spine in young adults has been reported on multidetector computed tomography (MDCT), but has not been systematically assessed in all ages. PURPOSE: To evaluate the reference ranges for the atlanto-dental interval (ADI) in a large sample of adult patients on MDCT and to analyze the relationships of these measurements with gender and age of the patients as well as inter-observer performance. MATERIAL AND METHODS: First, a consecutive series of 700 Chinese patients aged over 18 years undergoing an upper cervical MDCT scan were divided equally into seven age groups. Second, the mid-sagittal image of the atlanto-dental joint was chosen for measurement and ADI was defined as the distance intercepted from the segment line linking the center of anterior atlas tubercle with that of posterior tubercle. Third, the correlation of ADI with age and gender was analyzed using linear regression analysis. Finally, the inter-observer performance was assessed using Bland and Altman's limits of agreement. RESULTS: The ADI was 1.77 ± 0.39 mm, 1.61 ± 0.37 mm, 1.58 ± 0.36 mm, 1.41 ± 0.29 mm, 1.31 ± 0.29 mm, 1.34 ± 0.28 mm, and 1.06 ± 0.47 mm in the age groups 18-24 years, 25-29 years, 30-39 years, 40-49 years, 50-59 years, 60-69 years, and older than 70 years, respectively. The range of ADI was 0.85-3.12 mm in the age group 18-39 years, 0.71-2.55 mm in the age group 40-59 years, and 0.00-2.37 mm in the age group older than 60 years. There was no difference between gender and ADI (r = 0.00, P = 1.000). ADI decreased linearly with age (r = -0.511, P = 0.000). The inter-observer performance was reliable. CONCLUSION: ADI measurements on MDCT linearly decrease with increasing age, and these are not affected by gender in adult patients. Different reference values might be used at different ages when diagnosing atlantoaxial anterior dislocation or subluxation.

Synthesis and biological evaluation of novel benzamide derivatives as potent smoothened antagonists.

A series of novel benzamide derivatives were prepared and evaluated using cell-based measurements. Among these compounds, 10f significantly inhibited Hedgehog signaling and showed equivalent or more potency than GDC-0449 in different tests. Furthermore, compound 10f potently inhibited the proliferation of Daoy, a medulloblastoma cell line that is reported to be resistant to GDC-0449, which indicated a promising prospect in the treatment of Hedgehog signaling pathway related cancer in clinical trial.

6-Amino-2-methyl-8-phenyl-1,2,3,4-tetra-hydro-iso-quinoline-5,7-dicarbo-nitrile.

In the title compound, C18H16N4, the dihedral angle between the benzene and phenyl rings is 61.40 (4)°. In the crystal, mol-ecules are linked by N-H⋯N(nitrile) hydrogen bonds, forming inversion dimers. The dimers are further linked by N-H⋯N(amine) hydrogen bonds, and both units are arranged almost perpendicular to each other [angle between dimer mean planes = 84.43 (12)°]. This arrangement is extended to form a ladder-like structure parallel to the c axis.

2-Chloro-N-(4-chloro-3-iodo-phen-yl)-4-(methyl-sulfon-yl)benzamide.

In the title compound, C(14)H(10)Cl(2)INO(3)S, the dihedral angle between the benzene rings is 52.13 (10)°. In the crystal, the components are linked by pairs of N-H⋯O(sulfon-yl) hydrogen bonds into centrosymmetric dimers.