[en] Curcumin (diferuloyl methane), a natural yellow pigment in the roots of turmeric, has been considered as one of the most promising chemopreventive agents against a variety of human cancers. Curcumin is known to exhibit its antiproliferative effect against various cancer cells through cell cycle arrest and induction of apoptosis. Although not as potent as many other cytotoxic agents, curcumin has been demonstrated to be safe in humans at relatively high doses (10 grams/day), making it an attractive target for chemotherapeutic drug discovery efforts. Two compounds with meta-methoxy substituents (2 and 3) maintained comparable antiproliferative activity with curcumin (1). In contrast, the acetoxy-curcuminoids (8-14) showed moderate to potent activity against all three cancer cell lines tested (Table 1). In particular, the colon cancer cell (HCT116) was most susceptible to the acetoxy-curcuminoids (8-12, Table 1) to show 2-2.5 times increase in EC₅₀ values compared with that of curcumin (1, Table 1). In this series, like the simple curcuminoids (2-7), the aromatic meta-methoxy substituent turned out to be critical for the antiproliferative effect, and the corresponding acetoxy-curcuminoids 10 and 11 showed the most potent activity against HCT116 with EC₅₀ values of 18.5 μM and 16.9 μM, respectively. Also noteworthy is the broad spectrum antiproliferative effect of the acetoxy-curcuminoid 11 with a free catechol moiety, which exhibited almost similar antiproliferative activity against all three cancer cell lines tested. Taken together, through evaluation of solubility as well as antiproliferative effect of the acetoxy-curcuminoids, we figured out that the acetoxy group substituted at the central methylene unit which served to enhance the solubility of the corresponding curcuminoids also played a key role in potentiating their antiproliferative effect. Thus, upon combination of the methylenyl acetoxy group and the aromatic meta-methoxy group on the curcumin framework, we could come up with a novel soluble curcuminoids with potent antiproliferative effect

[en] The synthesized macrocycle L is the novel fluorescent receptor having the switching ability by the external stimuli as well as having the recognizing ability of various metal ions. In particular, this macrocycle L shows the possibility of the selectivity of metal ions even in the same charge ions of a different metal, and the values of association constant (M^-1) of that for metal ions are consistent with the tendency of increasing charge number of metal ion. In addition, the values of quantum yield (PHI_F) of metal complexes of macrocycle L were ranged from 0.021 to 0.111 enough to recognize the metal ions in macrocycle L. We know from the fluorescent pH titration of macrocycle L by acid/base that the change of fluorescence intersects at about pH=5

[en] We investigated the ALMA science verification data of Orion KL and found a spectral signature of the vibrationally excited H₂O maser line at 232.68670 GHz (ν₂ = 1, 5_5,0-6_4,3). This line has been detected previously in circumstellar envelopes of late-type stars but not in young stellar objects such as Orion KL. Thus, this is the first detection of the 232 GHz vibrationally excited H₂O maser in star-forming regions. The distribution of the 232 GHz maser is concentrated at the position of the radio Source I, which is remarkably different from other molecular lines. The spectrum shows a double-peak structure at the peak velocities of –2.1 and 13.3 km s^–1. It appears to be consistent with the 22 GHz H₂O masers and 43 GHz SiO masers observed around Source I. Thus, the 232 GHz H₂O maser around Source I would be excited by the internal heating by an embedded protostar, being associated with either the root of the outflows/jets or the circumstellar disk around Source I, as traced by the 22 GHz H₂O masers or 43 GHz SiO masers, respectively.

[en] We present an observational study of the vibrationally excited H₂O line at 658 GHz (${\mathrm{\nu <!--\; ??\; -->}}_2$ = 1, $1_{1,0}$-1${}_{0,1}$) toward Orion KL using the Atacama Large Millimeter/Submillimeter Array (ALMA). This line is clearly detected at the position of the massive protostar candidate,  Source I. The spatial structure is compact, with a size of about 100 AU, and is elongated along the northeast–southwest low-velocity (18 km ⁻¹) bipolar outflow traced by 22 GHz H₂O masers, SiO masers, and thermal SiO lines. A velocity gradient can be seen perpendicular to the bipolar outflow. The overall spatial and velocity structure seems to be analogous to that of the 321 GHz H₂O maser line previously detected with ALMA and vibrationally excited SiO maser emission. The brightness temperature of the 658 GHz H₂O line is estimated to be higher than 2 × 10⁴ K, implying that it is emitted via maser action. Our results suggest that the 658 GHz H₂O maser line is emitted from the base of the outflow from a rotating and expanding accretion disk as observed for the SiO masers and the 321 GHz H₂O maser. We also search for two other H₂O lines at 646 GHz (9${}_{7,3}$-8${}_{8,0}$ and $9_{7,2}$-8${}_{8,1}$), but they are not detected in Orion KL.

[en] We report new Atacama Large Millimeter/Submillimeter Array (ALMA) observations of a circumstellar disk around Source I in Orion KL, an archetype of massive protostar candidates. We detected two ortho-H₂O lines at 321 GHz (10_{2, 9}-9_{3, 6}) and 336 GHz (ν₂ = 1, 5_{2, 3}-6_{1, 6}) for the first time in Source I. The latter one is in a vibrationally excited state at the lower state energy of 2939 K, suggesting evidence of hot molecular gas close to Source I. The integrated intensity map of the 321 GHz line is elongated along the bipolar outflow while the 336 GHz line map is unresolved with a beam size of 0.''4. Both of these maps show velocity gradients perpendicular to the bipolar outflow. The velocity centroid map of the 321 GHz line implies a spatial and velocity structure similar to that of vibrationally excited SiO masers tracing the root of the outflow emanating from the disk surface. In contrast, the 336 GHz line is most likely emitting from the disk midplane with a diameter of 0.''2 (84 AU) as traced by radio continuum emission and a dark lane devoid of the vibrationally excited SiO maser emission. The observed velocity gradient and the spectral profile of the 336 GHz H₂O line can be reconciled with a model of an edge-on ring-like structure with an enclosed mass of >7 M_☉ and an excitation temperature of >3000 K. The present results provide further evidence of a hot and neutral circumstellar disk rotating around Source I with a diameter of ∼100 AU scale

[en] We have carried out high-resolution observations with the Atacama Large Millimeter/Submillimeter Array (ALMA) of continuum emission from the Orion Kleinmann–Low (KL) region. We identify 11 compact sources at ALMA band 6 (245 GHz) and band 7 (339 GHz), including the Hot Core, Compact Ridge, SMA1, IRc4, IRc7, and a radio source I (Source I). A spectral energy distribution (SED) of each source is determined by using previous 3 mm continuum emission data. Physical properties such as size, mass, hydrogen number density, and column density are discussed based on the dust graybody SED. Among 11 identified sources, Source I, a massive protostar candidate, is a dominant energy source in Orion KL. We extensively investigate its SED from centimeter to submillimeter wavelengths. The SED of Source I can be fitted with a single power-law index of 1.97, suggesting an optically thick emission. We employ the H"− free–free emission as an opacity source of this optically thick emission. The temperature, density, and mass of the circumstellar disk associated with Source I are constrained by the SED of H"− free–free emission. Still, the fitting result shows a significant deviation from the observed flux densities. Combined with the thermal dust graybody SED to explain excess emission at higher frequency, a smaller power-law index of 1.60 for the H"− free–free emission is obtained in the SED fitting. The power-law index smaller than two would suggest a compact source size or a clumpy structure unresolved with the present study. Future higher resolution observations with ALMA are essential to reveal more detailed spatial structure and physical properties of Source I

[en] We have measured continuum flux densities of a high-mass protostar candidate, a radio source I in the Orion KL region (Orion Source I) using the Atacama Large Millimeter/Submillimeter Array (ALMA) at band 8 with an angular resolution of 0.″1. The continuum emission at 430, 460, and 490 GHz associated with Source I shows an elongated structure along the northwest–southeast direction perpendicular to the so-called low-velocity bipolar outflow. The deconvolved size of the continuum source, 90 au × 20 au, is consistent with those reported previously at other millimeter/submillimeter wavelengths. The flux density can be well fitted to the optically thick blackbody spectral energy distribution, and the brightness temperature is evaluated to be 700–800 K. It is much lower than that in the case of proton–electron or H⁻ free–free radiations. Our data are consistent with the latest ALMA results by Plambeck and Wright, in which the continuum emission was proposed to arise from the edge-on circumstellar disk via thermal dust emission, unless the continuum source consists of an unresolved structure with a smaller beam filling factor.

[en] We observed polarization of the SiO rotational transitions from Orion Source I (SrcI) to probe the magnetic field in bipolar outflows from this high-mass protostar. Both 43 GHz J = 1–0 and 86 GHz J = 2–1 lines were mapped with ∼20 au resolution, using the Very Large Array (VLA) and Atacama Large Millimeter/Submillimeter Array (ALMA), respectively. The ²⁸SiO transitions in the ground vibrational state are a mixture of thermal and maser emission. Comparison of the polarization position angles in the J = 1–0 and J = 2–1 transitions allows us to set an upper limit on possible Faraday rotation of 10⁴ rad m⁻², which would twist the J = 2–1 position angles typically by less than 10°. The smooth, systematic polarization structure in the outflow lobes suggests a well-ordered magnetic field on scales of a few hundred au. The uniformity of the polarization suggests a field strength of ∼30 mG. It is strong enough to shape the bipolar outflow and possibly lead to sub-Keplerian rotation of gas at the base of the outflow. The strikingly high fractional linear polarizations of 80%–90% in the ²⁸SiO v = 0 masers require anisotropic pumping. We measured circular polarizations of 60% toward the strongest maser feature in the v = 0 J = 1–0 peak. Anisotropic resonant scattering is likely to be responsible for this circular polarization. We also present maps of the ²⁹SiO v = 0 J = 2–1 maser and several other SiO transitions at higher vibrational levels and isotopologues.

[en] In 2011 February, a burst event of the H₂O maser in Orion KL (Kleinmann-Low object) has started after a 13 year silence. This is the third time such phenomena has been detected in Orion KL, followed by the events in 1979-1985 and 1998. We have carried out astrometric observations of the bursting H₂O maser features in Orion KL with the VLBI Exploration of Radio Astrometry (VERA), a Japanese very long baseline interferometry network dedicated for astrometry. The total flux of the bursting feature at the local standard of rest (LSR) velocity of 7.58 km s^-1 reaches 4.4 x 10⁴ Jy in 2011 March. The intensity of the bursting feature is three orders of magnitude larger than that of the same velocity feature in the quiescent phase in 2006. Two months later, another new feature appears at the LSR velocity of 6.95 km s^-1 in 2011 May, separated by 12 mas north of the 7.58 km s^-1 feature. Thus, the current burst occurs at two spatially different features. The bursting masers are elongated along the northwest-southeast direction as reported in the previous burst in 1998. We determine the absolute positions of the bursting features for the first time ever with a submilliarcsecond (mas) accuracy. Their positions are coincident with the shocked molecular gas called the Orion Compact Ridge. We tentatively detect the absolute proper motions of the bursting features toward the southwest direction. It is most likely that the outflow from the radio source I or another young stellar object interacting with the Compact Ridge is a possible origin of the H₂O maser burst.

[en] Gastrin-releasing peptide (GRP) is a neuropeptide that plays roles in various pathophysiological conditions including inflammatory diseases in peripheral tissues; however, little is known about whether GRP can directly regulate endothelial inflammatory processes. In this study, we showed that GRP promotes the adhesion of leukocytes to human umbilical vein endothelial cells (HUVECs) and the aortic endothelium. GRP increased the expression of intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) by activating nuclear factor-κB (NF-κB) in endothelial cells. In addition, GRP activated extracellular signal-regulated kinase 1/2 (ERK1/2), p38MAPK, and AKT, and the inhibition of these signaling pathways significantly reduced GRP-induced monocyte adhesion to the endothelium. Overall, our results suggested that GRP may cause endothelial dysfunction, which could be of particular relevance in the development of vascular inflammatory disorders. - Highlights: • GRP induces adhesion of monocytes to vascular endothelium. • GRP increases the expression of endothelial adhesion molecules through the activation of NF-κB. • ERK1/2, p38MAPK, and Akt pathways are involved in the GRP-induced leukocyte adhesiveness to endothelium.