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31.
Dharam Pal Pathak Vidushi Sharma Sachin Kumar 《Bioorganic & medicinal chemistry letters》2018,28(9):1566-1569
Coumarin containing pyrazoline derivatives have been synthesized and tested as inhibitors of in vitro development of a chloroquine-sensitive (MRC-02) and chloroquine-resistant (RKL-2) strain of Plasmodium falciparum and in vivo Plasmodium berghei malaria. Docking study was also done on cysteine protease falcipain-2 which showed that the binding pose of C-14 molecule and epoxysuccinate, inhibitor of falcipain-2, binds in the similar pattern. The most active antimalarial compound was 3-(1-benzoyl-5-(4-flurophenyl)-4,5-dihydro-1H-pyrazol-3yl)-7-(diethyamino)-2H-chromen-2-one C-14, with an IC50 of 4.21?µg/ml provided complete protection to the infected mice at 24?mg/kg X 4?days respectively. 相似文献
32.
Incorporation of photosynthetically fixed 14C was studied at different time intervals of 12, 24, and 36 h in various plant parts—leaf 1 to 4 from apex, roots, and rhizome—into primary metabolites—sugars, amino acids, and organic acids, and secondary metabolites—essential oil and curcumin—in turmeric. The youngest leaves were most active in fixing 14C at 24 h. Fixation capacity into primary metabolites decreased with leaf position and time. The primary metabolite levels in leaves were maximal in sugars and organic acids and lowest in amino acids. Roots as well as rhizome received maximum photoassimilate from leaves at 24 h; this declined with time. The maximum metabolite concentrations in the roots and rhizome were high in sugars and organic acids and least in amino acids. 14C incorporation into oil in leaf and into curcumin in rhizome was maximal at 24 h and declined with time. These studies highlight importance of time-dependent translocation of 14C-primary metabolites from leaves to roots and rhizome and their subsequent biosynthesis into secondary metabolite, curcumin, in rhizome. This might be one of factors regulating the secondary metabolite accumulation and rhizome development. 相似文献
33.
Established populations of Pseudodacrylogyrus anguillae are reported from eels in England for the first time. Prevalence and abundance peak in late summer in all three localities and the parasite overwinters at low levels on eels. 相似文献
34.
35.
H. Llaneza Coalla J.M. Blanco FernándezM.A. Morís Morán M.R. López Bobo 《Bioresource technology》2009,100(17):3843-3847
In view of the pressing problem that appears in our region (Asturias, north of Spain) with the residues from the cider production, it was decided to test this kind of material as a co-substrate joint with slaughterhouse waste in a laboratory unit. 相似文献
36.
37.
Hiroyuki Kimura Saki Yamauchi Hidekazu Kawashima Kenji Arimitsu Yusuke Yagi Yuji Nakamoto Kaori Togashi Masahiro Ono Hideo Saji 《Bioorganic & medicinal chemistry letters》2018,28(17):2949-2952
The tripeptide formyl–Met–Leu–Phe (fMLF) is a prototype of N-formylated chemotactic peptides for neutrophils owing to its ability to bind and activate the G protein-coupled formyl peptide receptor (FPR). Here, we developed an 18F-labeled fMLF derivative targeting FPR as a positron emission tomography (PET) imaging probe for bacterial infections. The study demonstrates that the fMLF derivative fMLFXYk(FB)k (X?=?Nle) has a high affinity for FPR (Ki?=?0.62?±?0.13?nM). The radiochemical yield and purity of [18F]fMLFXYk(FB)k were 16% and >96%, respectively. The in vivo biodistribution study showed that [18F]fMLFXYk(FB)k uptake was higher in the bacterial infected region than in the non-infected region. We observed considerably higher infection-to-muscle ratio of 4.6 at 60?min after [18F]fMLFXYk(FB)k injection. Furthermore, small-animal PET imaging studies suggested that [18F]fMLFXYk(FB)k uptake in the bacterial infected region was clearly visualized 60?min after injection. 相似文献
38.
39.
Hilde De Boeck Frank G. Loontiens Halina Lis Nathan Sharon 《Archives of biochemistry and biophysics》1984,234(1):297-304
Erythrina cristagalli agglutinin, a dimeric lectin [J. L. Iglesias, et al. (1982) Eur. J. Biochem.123, 247–252] was shown by equilibrium dialysis to be bivalent for 4-methylumbelliferyl-β-d-galactoside. Upon binding to the lectin, this ligand showed a difference absorption spectrum with two maxima (at 322 and 336 nm) of equal intensity (Δ? = 1.2 × 103m?1 cm?1). A similar spectrum with a comparable value of Δ? was obtained with 4-methylumbelliferyl-N-acetyl-β-d-galactosaminide. Binding of methyl-α-d-galactoside, lactose, and N-acetyllactosamine all produced small but equally intense protein difference spectra with a maximum (Δ? = 2.8 × 102 M?1 cm?1) at 291.6 nm. Upon binding of N-dansyl-d-galactosamine to the lectin, there was a fivefold increase in fluorescence intensity of this ligand. The association constant for N-dansyl-d-galactosamine was caused by a very favorable ΔS° of the dansyl group without affecting the strictly carbohydrate-specific character of binding. N-Dansyl-d-galactosamine was employed as a fluorescent indicator ligand in substitution titrations. This involved the use of simple carbohydrates, N-acetyllactosamine, and oligosaccharides which occur in the carbohydrate units of N-glycoproteins; the latter were Gal(β → 4)GlcNAc(β1 → 2)Man, Gal(β1 → 4)GlcNAc(β1 → 6)Man, and Gal(β1 → 4)GlcNAc(β1 → 6)[Gal(β1 → 4)GlcNAc(β1 → 2)]Man. The titrations were performed at two temperatures to determine the thermodynamic parameters. In the series N-acetyl-d-galactosamine, methyl-α-d-galactoside, and lactose, ?ΔH° increased from 24 to 41 kJ mol?1; it increased further for N-acetyllactosamine and then remained unchanged for the N-acetyllactosamine-containing oligosaccharides (55 ± 1 kJ mol?1). This indicated that the site specifically accommodated the disaccharide structure with an important contribution of the 2-acetamido group in the penultimate sugar. Beyond this, no additional contacts seemed to be formed. This conclusion also followed from considerations of ΔS° values which became more unfavorable in the above series (?23 to ?101 ± 4 J mol?1 K?1); the most negative value of ΔS° was observed with N-acetyllactosamine and the three N-acetyllactosamine-containing oligosaccharides. 相似文献
40.
Understanding the factors that influence plant distributions is a considerable challenge for ecologists in the face of environmental
change. Here, we quantify spatial and temporal variation in the finite rate of population increase of the annual grass Vulpia fasciculata. Specifically, we test the hypothesis that the northern range boundary is associated with finite rates of population increase
of less than one. Seeds of three ecotypes of the annual grass V. fasciculata were introduced annually across a range of sites in Great Britain both within (11) and to the north (4) of its current range
boundary in each of 4 years. Populations failed to establish at 17% of target sites due to disturbance. At the remaining target
sites, the finite rate of population increase, λ, varied from 0.06 to 33.3 with a geometric mean of 1.88. Of the total variance
in the rate of population growth, site and year effects accounted independently for 40% of the variation and in interaction
for 50%; ecotype accounted for less than 5% of the variation. Variation in the weather between sites and years had little
impact on plant performance, and there was no indication that the rate of population growth was lower to the north of the
current range boundary. We conclude that current climatic conditions on the coast of Great Britain are not limiting the distribution
of V. fasciculata and that seeds from across its current range have roughly equivalent colonising potential. 相似文献