Anti-Obesity Natural Products Tested in Juvenile Zebrafish Obesogenic Tests and Mouse 3T3-L1 Adipogenesis Assays

(1) Background: The obesity epidemic has been drastically progressing in both children and adults worldwide. Pharmacotherapy is considered necessary for its treatment. However, many anti-obesity drugs have been withdrawn from the market due to their adverse effects. Instead, natural products (NPs) have been studied as a source for drug discovery for obesity, with the goal of limiting the adverse effects. Zebrafish are ideal model animals for in vivo testing of anti-obesity NPs, and disease models of several types of obesity have been developed. However, the evidence for zebrafish as an anti-obesity drug screening model are still limited. (2) Methods: We performed anti-adipogenic testing using the juvenile zebrafish obesogenic test (ZOT) and mouse 3T3-L1 preadipocytes using the focused NP library containing 38 NPs and compared their results. (3) Results: Seven and eleven NPs reduced lipid accumulation in zebrafish visceral fat tissues and mouse adipocytes, respectively. Of these, five NPs suppressed lipid accumulation in both zebrafish and 3T3-L1 adipocytes. We confirmed that these five NPs (globin-digested peptides, green tea extract, red pepper extract, nobiletin, and Moringa leaf powder) exerted anti-obesity effects in diet-induced obese adult zebrafish. (4) Conclusions: ZOT using juvenile fish can be a high-throughput alternative to ZOT using adult zebrafish and can be applied for in vivo screening to discover novel therapeutics for visceral obesity and potentially also other disorders.     

Far-infrared spectroscopy by synchrotron radiation at the UVSOR Facility

At the UVSOR Facility, Institute for Molecular Science, the practical use of the synchrotron radiation as a far-infrared light source has started. A spectroscopic system has been constructed at the beam line BL6A1 of UVSOR storage ring, which covers the wavenumber region from 5 to 250 cm^–1. The cross sectional diameter of the light beam at the sample position is as small as 3 mm with the angular divergence of about 100 mrad. The system has been made mainly for the transmission and reflection measurements of small samples with small angular divergence by the use of the high brightness of the synchrotron radiation. Examples of observed transmission and reflectivity spectra are shown.     

Insoluble polystyrenes containing amide moieties and N-alkylated nylon-66 as phase transfer catalysts

Insoluble polystrenes containing formamide and acetamide moieties were prepared by free radical terpolymerization of the corresponding vinyl monomers, styrene, and divinylbenzene. These polymers served as phase transfer catalysts for the reaction of n-octyl bromide with potassium thiocyanate in toluene–water system. The activity of these catalysts was affected by some factors such as stirring speed particle size, and degree of crosslinking. The activity also depended strongly on the structure of active site, copolymer composition, and spacer length which cause the difference in the adsorption of potassium ion and in the microenvironment around the active site. Furthermore, nylon-66 was found to display the activity for phase transfer reactions, and the activity was remarkably increased by replacing the amide hydrogen with an alkyl group.     

Ionization process of the hydrogen atom in intense laser fields: Non–Born-Oppenheimer 1D model calculations

The ionization process of the hydrogen atom in two-color laser field is investigated based on non–Born-Oppenheimer one-dimensional model. In this model, both electron and nucleus are described by the time-dependent Hartree equations. By numerically solving the equations, the influence of the relative phase ϕ of the laser field with the spatial distribution of electron and nucleus is investigated. For ϕ = 0, the electron is moved to the direction in which the maximum of the asymmetric combined electric field pointed. For ϕ = π/2, the electron is shown to be pulled in the opposite direction. © 2003 Wiley Periodicals, Inc. Int J Quantum Chem, 2004     

Regio- and chemoselective manipulation under mild conditions on glucosamine derivatives for oligosaccharide synthesis and its application toward N-acetyl-d-lactosamine and Lewis X trisaccharide

Special emphasis on regio- and chemoselective manipulation on a new glucosamine scaffold was laid, toward the short-step and efficient synthetic routes for oligosaccharides. First, the blocking of two hydroxyl groups at C-1 and C-6 positions of N-protected glucosamine at once by silylation followed by an oxazolidinone formation between C-3 hydroxyl and C-2 amino groups were established, to lead an expeditious way for a glycosyl acceptor for lactosamine synthesis. Second, without any effect on acetyl protective groups in the same molecule, the ring-opening of oxazolidinone and hydrolysis of resulting carbonate under mild conditions allowed the C-3 hydroxyl group to be free, which is indispensable for further extension to oligosaccharides, such as a LeX trisaccharide.     

Intersection properties of radial solutions and global bifurcation diagrams for supercritical quasilinear elliptic equations

We study the positive solution \({u(r,\rho)}\) of the quasilinear elliptic equation

$$\begin{cases}r^{-(\gamma-1)}(r^{\alpha}|u^{\prime}|^{\beta-1}u^{\prime})^{\prime}+|u|^{p-1}u=0, & 0 < r < \infty,\\ u(0) = \rho > 0,\ u^{\prime}(0)=0.\end{cases}$$

This class of differential operators includes the usual Laplace, m-Laplace, and k-Hessian operators in the space of radial functions. The equation has a singular positive solution u ^*(r) under certain conditions on \({\alpha}\), \({\beta}\), \({\gamma}\), and p. A generalized Joseph–Lundgren exponent, which we denote by \({p^*_{JL}}\), is obtained. We study the intersection numbers between \({u(r,\rho)}\) and u ^*(r) and between \({u(r,\rho_0)}\) and \({u(r,\rho_1)}\), and see that \({p^*_{JL}}\) plays an important role. We also determine the bifurcation diagram of the problem

$$\begin{cases}r^{-(\gamma-1)}(r^{\alpha}|u^{\prime}|^{\beta-1}u^{\prime})^{\prime} + \lambda(u+1)^p=0, & 0 < r < 1,\\ u(r) > 0, & 0 \le r < 1,\\ u^{\prime}(0)=0,\ u(1)=0.\end{cases}$$

The main technique used in the proofs is a phase plane analysis.

     

Effect of types of proximal femoral fractures on physical function such as lower limb function and Activities of Daily Living

Objectives: This study aimed to assess physical function such as lower limb function and Activities of Daily Living after surgery for proximal femoral fractures ( unstable medial femoral neck fracture and trochanteric fracture). Methods: This study enrolled 68 patients with proximal femoral fractures. Isometric knee extension strength (IKES), the Japanese Orthopedic Association (JOA) hip score, and the number of days required to develop straight leg raising, transfer, and T-caneassisted gait abilities to become independent were assessed. Patients were classified based on the types of proximal femoral fractures, namely unstable medial femoral neck fracture (bipolar hip arthroplasty [BHA] group), stable trochanteric fracture (S group), and unstable trochanteric fracture (US group). Results: IKES and the JOA hip score were significantly better in the BHA group than in the S and US groups. IKES and the JOA hip score were significantly worse in the US group than in the BHA and S groups. Both transfer and T-cane-assisted gait abilities of patients in the BHA and S groups were indifferent. However, all physical functions were significantly worse in the US group. Conclusions: Our study results suggested that physical therapists plan the different rehabilitation program for the patients with proximal femoral fractures who were classified into three types, namely unstable medial femoral neck fracture, stable trochanteric fracture, and unstable trochanteric fracture, instead of two types.     

Generalized Joseph–Lundgren exponent and intersection properties for supercritical quasilinear elliptic equations

We study the solution \({u(r,\rho)}\) of the quasilinear elliptic problem

$$\begin{cases}r^{-(\gamma-1)}(r^{\alpha}|u'|^{\beta-1}u')'+|u|^{p-1}u=0, & 0 < r < \infty, \\u(0)=\rho > 0,\ u'(0)=0.\end{cases}$$

The usual Laplace, \({m}\)-Laplace, and \({k}\)-Hessian operators are included in the differential operator \({r^{-(\gamma-1)}(r^{\alpha}|u'|^{\beta-1}u')'}\). Under certain conditions on \({\alpha}\), \({\beta}\), \({\gamma}\), and \({p}\), the equation has a singular positive solution \({u^*(r)}\) and the solution \({u(r,\rho)}\) is positive for \({r\ge 0}\). We study the intersection numbers between \({u(r,\rho)}\) and \({u^*(r)}\) and between \({u(r,\rho_0)}\) and \({u(r,\rho_1)}\). A generalized Joseph–Lundgren exponent \({p^*_{JL}}\) plays a crucial role. The main technique is a phase plane analysis. In particular, we use two changes of variables which transform the equation into two autonomous systems.

     

Direct substitution of the hydroxy group with highly functionalized nitrogen nucleophiles catalyzed by Au(III)

A direct catalytic substitution of various allylic and benzylic alcohols with synthetically useful, but acid-sensitive Boc, Bus, and Dios protected amine nucleophiles, which have not been well utilized for Lewis acid catalysis, with various functionalities (OTBS, OTHP, etc.) was efficiently catalyzed by 1 mol% of Au(III) under mild conditions.