Pd-Catalyzed Stereoselective Construction of Benzo-Fused Decalines with a Quaternary Carbon.

The Pd-catalyzed stereoselective construction of decalins with one-carbon units bearing heteroatoms at the ring junction is described. The Pd-catalyzed cyclization of silyl enol ether resulted in exclusive formation of the cis isomer (89%, >100/1 cis/trans). On the contrary, Pd-catalyzed carboiodination and carboborylation (with oxidative workup) provided products in 56% yield (1/>100 cis/trans) and 69% yield (1/11 cis/trans), respectively.

Characterizing the Asymmetry in Hardness between Synthesis and Destruction of Heteropolymers.

We present a simple model describing the assembly and disassembly of heteropolymers consisting of two types of monomers A and B. We prove that no matter how we manipulate the concentrations of A and B, it takes longer than the exponential function of d to synthesize a fixed amount of the desired heteropolymer, where d is the number of A-B connections. We also prove the decomposition time is linear for chain length n. When d is proportional to n, synthesis and destruction have an exponential asymmetry. Our findings may facilitate research on the more general asymmetry of operational hardness.

Palladium-Catalyzed Carbothiolation via Trapping of the σ-Alkyl Palladium Intermediate with RSTIPS.

A palladium-catalyzed carbothiolation via the reaction of a σ-alkyl palladium intermediate with a TIPS thioether is described. It was found that the use of Cs2CO3, (IPr)Pd(allyl)Cl, and a TIPS thioether was key to obtaining alkyl aryl and dialkyl sulfides in high yield through the reaction of a σ-alkyl palladium intermediate. The developed reaction is applicable to a wide range of substrates and thiols.

Effects of high-sodium intake on systemic blood pressure and vascular responses in spontaneously diabetic WBN/Kob-Leprfa/fa rats.

The prevalence of type 2 diabetes mellitus (T2DM) and hypertension has markedly increased worldwide. The purpose of the present study was to examine the effects of a high-salt intake on the systolic blood pressure (SBP) and vascular responses in WBN/Kob-Leprfa/fa (WBKDF) rats, a new spontaneous animal model of T2DM. Male WBKDF rats and age-matched Wistar rats at 6 weeks of age were each divided into two groups and fed either a normal-sodium (NS, 0.26%) diet or high-sodium (HS, 8%) diet for 14 weeks: (i) Wistar rats on NS diet (Wistar-NS); (ii) Wistar rats on HS diet (Wistar-HS); (iii) WBKDF rats on NS diet (WBKDF-NS); (iv) WBKDF rats on HS diets (WBKDF-HS). Neither WBKDF-NS nor Wistar-NS rats showed significant changes in SBP throughout the experiment, but both WBKDF-HS and Wistar-HS exhibited significant elevation of SBP, which was more prominent (P<.01) in WBKDF-HS than in Wistar-HS. Phenylephrine-induced contractions of isolated thoracic aortic rings were significantly (P<.01) enhanced in WBKDF-HS and Wistar-HS compared with the respective strain of rats on the NS diet. In contrast, acetylcholine- and nitroprusside-induced relaxation were significantly (P<.01) diminished in both WBKDF-HS and Wistar-HS, and these HS diet-induced changes were more profound (P<.01) in WBKDF rats than in Wistar rats. Significantly (P<.05) higher plasma concentrations of 8-iso-prostaglandin F2α and sodium ions were observed in WBKDF-HS than in Wistar-HS. The current study demonstrated that WBKDF-HS rats developed salt-sensitive hypertension associated with vascular dysfunction. The WBKDF rat may be a useful model for investigating the etiology of hypertension with T2DM.

[A case of locally advanced breast cancer successfully treated with Mohs paste].

We report a case of primary advanced breast cancer that was locally controlled by treatment with Mohs paste. A 57- year-old woman presented with right locally advanced breast cancer with massive exudate and oozing blood. Histopathological examination indicated an invasive ductal carcinoma. Moreover, the patient had lung, liver, and bone metastases. She received chemotherapy, following which the breast tumor was treated using Mohs paste and dissected. The bleeding and exudate stopped almost completely, and the breast tumor became flat. Therefore, it is suggested that locally advanced breast cancer could be controlled by treatment with Mohs paste.

Provision of a voluntary exercise environment enhances running activity and prevents obesity in Snark-deficient mice.

The present study was performed to investigate the involvement of SNARK in physical activity levels in mice. To examine the acute effect of SNARK deficiency on voluntary running, Snark-deficient mice (Snark(+/-): n = 16) and their wild-type counterparts (Snark(+/+): n = 16) were assigned to sedentary or exercise (1 wk voluntary wheel running) groups. In addition, to clarify the differences in voluntary running activity and its effect between genotypes, mice (Snark(+/+): n = 16; Snark(+/-): n = 16) were also kept in individual cages with/without a running wheel for 5 mo. Unexpectedly, in both voluntary running experiments, running distances were increased in Snark(+/-) mice compared with Snark(+/+) mice. Under sedentary conditions, body and white adipose tissue weights were increased significantly in Snark(+/-) mice. However, no significant differences were observed between the two genotypes under exercise conditions, and the values were significantly less than those under sedentary conditions in the long-term experiment. In the short-term experiment, serum interleukin-6 level in exercised Snark(+/+) mice was the same as that in sedentary Snark(+/+) mice, whereas that in sedentary Snark(+/-) mice was significantly lower than in the other groups. In contrast, serum leptin level was reduced significantly in exercised Snark(+/-) mice compared with sedentary Snark(+/-) mice. The results of this study demonstrated that exposure to an environment that allows voluntary exercise promotes increased running activity and prevents obesity in Snark-deficient mice.