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11.
[structure: see text] Covalently linked dimers of amphotericin B were prepared by cross-linking its carboxylic acid. Among these, a dimer with a linkage of 1,6-hexanediamine revealed potent hemolytic activity (EC50, 0.25 microM) while its N-acetyl derivative gave rise to large K+ ion flux in phosphatidylcholine liposomes, regardless of the presence or absence of sterols, suggesting that the dimers may serve as a tool for elucidating the structure of the ion channel assemblage formed by amphotericin B. 相似文献
12.
The solution behavior of homologously obtained crystalline surfactant molecular complexes (SMCs) that are generated between quaternary ammonium bromide and several additive materials has shed light on the recognition of fundamentals of solubilization. It has been revealed that the SMCs derived from long-alkyl-chain surfactants are sufficiently dissolved in water through the path of micellar dispersion above the cmc's of the complex surfactants, whereas the short-chain homologues cannot dissolve in water but dissociate the complexes, resulting in a heterogeneous phase made up of the liberated additives. The fact agrees perfectly with the familiar aspects of solubilization by surfactant; i.e., the longer the alkyl chain of the surfactant becomes, the more effective it is for solubilization. Based on these results, it has been deduced that the possibility for any pair of surfactant and solubilizate (additive) to realize solubilization simply depends on the relative importance of equilibrium of dissociation or association of the SMC species in aqueous medium. 相似文献
13.
Yongqiang Liu Alfarius E. Nugroho Asami Nakata Nahoko Uchiyama Osamu Shirota Haji Akber Aisa 《Tetrahedron letters》2010,51(50):6584-6587
Two novel elemanolide dimers, vernodalidimers A (1) and B (2), possessing a rare tricyclic ortho ester moiety, were isolated from the seeds of Vernonia anthelmintica. Their structures were elucidated by 1D and 2D NMR data and CD spectra. Vernodalidimers A (1) and B (2) exhibited potent cell growth inhibitory activity against HL-60 cells (IC50 0.72 and 0.47 μM, respectively). 相似文献
14.
The speed of image processing is limited by image acquisition circuitry. While optical pattern recognition techniques can reduce the computational burden on digital image processing, their image correlation rates are typically low due to the use of spatial optical elements. Here we report a method that overcomes this limitation and enables fast real-time analog image recognition at a record correlation rate of 36.7 MHz--1000 times higher rates than conventional methods. This technique seamlessly performs image acquisition, correlation, and signal integration all optically in the time domain before analog-to-digital conversion by virtue of optical space-to-time mapping. 相似文献
15.
In relation to the development of the interfacial area transport equation, local flow measurements of vertical downward air–water flows in a pipe with an inner diameter of 50.8 mm were performed at three axial locations of z/D=6.50, 34.0, and 66.5 as well as ten radial locations from r/R=0 to r/R=0.9 using a multi-sensor probe. In the experiment, the superficial liquid velocity and the void fraction ranged from –0.620 m/s to –2.49 m/s and from 0.21% to 8.4%, respectively. The dependence of the interfacial area transport on the liquid velocity, void fraction, and bubble size is discussed in detail. 相似文献
16.
Kikura-Hanajiri R Kawamura M Miyajima A Sunouchi M Goda Y 《Analytical and bioanalytical chemistry》2011,400(1):165-174
In order to develop an analytical method for the discrimination of dextromethorphan (an antitussive medicine) from its enantiomer,
levomethorphan (a narcotic) in biological samples, chiral analyses of these drugs and their O-demethyl and/or N-demethyl metabolites in rat plasma, urine, and hair were carried out using LC-MS/MS. After the i.p. administration of dextromethorphan
or levomethorphan to pigmented hairy male DA rats (5 mg/kg/day, 10 days), the parent compounds and their three metabolites
in plasma, urine and hair were determined using LC-MS/MS. Complete chiral separation was achieved in 12 min on a Chiral CD-Ph
column in 0.1% formic acid–acetonitrile by a linear gradient program. Most of the metabolites were detected as being the corresponding
O-demethyl and N, O-didemethyl metabolites in the rat plasma and urine after the hydrolysis of O-glucuronides, although obvious differences in the amounts of these metabolites were found between the dextro and levo forms.
No racemation was observed through O- and/or N-demethylation. In the rat hair samples collected 4 weeks after the first administration, those differences were more clearly
detected and the concentrations of the parent compounds, their O-demethyl, N-demethyl, and N, O-didemethyl metabolites were 63.4, 2.7, 25.1, and 0.7 ng/mg for the dextro forms and 24.5, 24.6, 2.6, and 0.5 ng/mg for the
levo forms, respectively. In order to fully investigate the differences of their metabolic properties between dextromethorphan
and levomethorphan, DA rat and human liver microsomes were studied. The results suggested that there might be an enantioselective
metabolism of levomethorphan, especially with regard to the O-demethylation, not only in DA rat but human liver microsomes as well. The proposed chiral analyses might be applied to human
samples and could be useful for discriminating dextromethorphan use from levomethorphan use in the field of forensic toxicology,
although further studies should be carried out using authentic human samples. 相似文献
17.
A homology cylinder over a surface consists of a homology cobordism between two copies of the surface and markings of its
boundary. The set of isomorphism classes of homology cylinders over a fixed surface has a natural monoid structure and it
is known that this monoid can be seen as an enlargement of the mapping class group of the surface. We now focus on abelian
quotients of this monoid. We show that both the monoid of all homology cylinders and that of irreducible homology cylinders
are not finitely generated and moreover they have big abelian quotients. These properties contrast with the fact that the
mapping class group is perfect in general. The proof is given by applying sutured Floer homology theory to homologically fibered
knots studied in a previous paper. 相似文献
18.
It was found that (2 + 2) cycloaddition reaction of diketene with Schiff bases was effectively promoted by imidazole as a catalyst to afford 3-acetyl-2-azetidinone derivatives 4. As an application of this new method, a practical asymmetric synthesis of 4 and its conversion into (3S,4S)-4-carboxy-1-(di-p-anisylmethyl)-3-[(R)-1-hydroxyethyl]-2- azetidinone, which is a key intermediate for the synthesis of carbapenem and penem antibiotics, were accomplished. 相似文献
19.
Kinoshita T Haga Y Narimatsu S Shimada M Goda Y 《Chemical & pharmaceutical bulletin》2005,53(6):717-720
New cassane diterpene-acids, neocaesalpins H and I, were isolated from the leaves of Caesalpinia crista (Fabaceae), and their structures were deduced on the basis of the spectroscopic and chemical basis. These compounds were characterized as having an alpha,beta-butenolide hemiacetal ring that is rare in nature. The lacking of 5-hydroxy group also distinguished neocaesalpins H and I from cassane diterpenes (caesalpins) occurring in other Caesalpinia species from the phytochemical viewpoint. The nomenclature of three Caesalpinia species was also reviewed, and it was found that some species belonging to the genus Caesalpinia are improperly named and should be changed to valid names. 相似文献
20.
Chen Y Pai A Somiya K Kawamura S Sato S Kokeyama K Ward RL Goda K Mikhailov EE 《Physical review letters》2006,97(15):151103
We propose a class of displacement- and laser-noise-free gravitational-wave-interferometer configurations, which does not sense nongeodesic mirror motion and laser noise, but provides a nonvanishing gravitational-wave signal. Our interferometers consist of four mirrors and two beam splitters, which form four Mach-Zehnder interferometers. By contrast to previous works, no composite mirrors with multiple reflective surfaces are required. Each mirror in our configuration is sensed redundantly, by at least two pairs of incident and reflected beams. Displacement- and laser-noise-free detection is achieved when output signals from these four interferometers are combined appropriately. Our 3-dimensional interferometer configuration has a low-frequency response proportional to f2, which is better than the f3 achievable by previous 2-dimensional configurations. 相似文献