ZnCl2 catalyzed new coumarinyl-chalcones as cytotoxic agents

A new series of coumarin-yl-chalcone derivatives (3a-m) had been designed and synthesized through different reactions such as aromatic addition, cyclization and Claisen-Schmidt reactions in good yields (54–78%). 5-acetyl-4-(2-hydroxyphenyl) -6-methyl-3, 4-dihydropyrimidin-2(1H) -one (1) has been synthesized by multi-component one pot reaction of salicylaldehyde, methyl acetoacetate and urea, which was further reacted with malonic acid employing ZnCl₂ catalyst to yield 5-acetyl-4-(4-hydroxy-2-oxo-2H-chromen-8-yl) -6-methyl-3, 4-dihydropyrimidin-2(1H) -one (2). The title compounds (3a-m) were synthesised by reacting 5-acetyl-4-(4-hydroxy-2-oxo-2H-chromen-8-yl) -6-methyl-3, 4-dihydropyrimidin-2(1H)-one (2) with different aromatic aldehydes in the presence of potassium hydroxide. In silico studies, a preliminary screening method for predicting the anti-cancer activity was performed for the synthesized compounds (3a-m) against Src, Alb tyrosine kinase and homology model protein (PDB ID: 4csv). The derivatives 3h and 3m showed moderate binding energies. The in vitro cytotoxic activity was evaluated for the compounds 3h and 3m by using human cancer cell-line morphology and MTT assay against three human cell-lines A549 (Lung), Jurkat (Leukemia) and MCF-7 (Breast). The results indicate that the derivatives 3h and 3m display significant anti-cancer activity, however it was found to be less cytotoxic when compared to the standard used i.e. Imatinib.     

Concerted evolution of the cow epsilon 2 and epsilon 4 beta-globin genes

The nucleotide sequences of the cow epsilon 2 and epsilon 4 globin genes were determined. The sequences were 95% identical. These genes arose via a four-gene block duplication that also gave rise to the bovine fetal (gamma) and adult (beta) genes. Their deduced amino acid sequences are unlike any previously reported fetal or adult globins; rather, comparison to other mammalian globin genes indicates that they are embryonic in nature. The sequence data indicate that these two genes have converted each other during evolution. Pairwise comparison to the corresponding goat genes shows greater similarity between paralogues than between more directly related orthologues. This is in direct contrast to the situation between the cow and goat fetal and adult genes. These observations suggest that the frequency of DNA conversion or the fixation of conversion events may vary in different locations of the cow beta-globin cluster.      

Chromium VI Induced Structural and Ultrastructural Changes in Bush Bean Plants (Phaseolus vulgaris L.)

The effect of a growth reducing chromium VI concentration (9.6x 10^–5M Cr as Na₂CrO₄) on the structure and ultrastructureof different organs of bush bean plants (Phaseolus vulgarisL.) grown on perlite was studied using light, transmission electronand scanning electron microscopy. The structural and ultrastructuralalterations observed were quite different in the various organsanalysed and did not always stay in direct relation to the averageCr content of the whole organ. The primary toxicity effect seemedto be membrane damage, due to the high oxidation power of CrVI. It is suggested that chromium is retained in vacuoles andcell walls of roots, and that the chromium reaching the leavesmay be principally Cr III and present in cell walls. The alterationsobserved in the upper plant parts seemed principally due toindirect Cr effects on the content of essential mineral nutrients. Phaseolus vulgaris L., bush bean, chromium VI toxicity, structure, ultranstructure, light microscopy, transmission electron microscopy, scanning electron microscopy     

A seasonal study of phosphorus deficiency in a eutrophic reservoir

• 1 Seston elemental composition (C, N, P) and the orthophosphate uptake rate constant, k(upt), were measured in the epilimnion of the eutrophic ?ímov Reservoir in the period March-August 1989.
• 2 Seasonal series of log C/P, log N/P and log [k(upt)] values were highly correlated (r² in the range 0.84–0.93), but, based on literature-derived criteria, k(upt) values indicated stronger P deficiency than did the C/P values.
• 3 The results showed moderate to strong phosphorus deficiency in summer, moderate deficiency at the end of the spring peak of phytoplankton, and no deficiency early in the spring or during the spring clear-water period.

     

Synthesis of α-<Emphasis Type="SmallCaps">D</Emphasis>-Glucose 1,6-Diphosphate in Potentially Prebiotic Conditions

A NOVEL method for the phosphorylation of sugars by orthophosphate in the presence of cyanogen in dilute aqueous neutral or slightly alkaline solutions has been described, suggesting a plausible model of the prebiotic phosphorylation of sugars^1–3. This reaction has now been applied to the synthesis of glucose 1,6-diphosphate, starting either from α-D-glucose 1-phosphate or from D-glucose 6-phosphate. The formation of α-D-glucose 1,6-diphosphate from α-D-glucose 1-phosphate would indicate a possible route for the synthesis of this compound on the primitive Earth. It is known that α-D-glucose 1,6-diphosphate is the coenzyme in the inter-conversion of α-D-glucose 1-phosphate with glucose 6-phosphate catalysed by phosphoglucomutase*. The formation of α-D-glucose 1,6-diphosphate seems to be interesting in view of our model for the chemical evolution of the metabolism of sugars⁵, as it may connect α-D-glucose 1-phosphate with the glycolytic pathway.     

Use of fatty acids for the assessment of zooplankton grazing on bacteria, protozoans and microalgae

1. The distribution of fatty acids in different groups of bacteria, ciliated protozoans and microalgae is reviewed emphasizing specific fatty acids like odd-branched fatty acids and ( n -3) polyunsaturated fatty acids.
2. Odd-branched fatty acids and ( n -6) fatty acids appear to be good indicators of zooplankton grazing on bacteria and ciliates when they are detected in microcrustacean triacylglycerols. We give several examples where these fatty acids may be used as markers. The value of ( n -3) fatty acids in describing zooplankton grazing on phytoplankton seems to be low.     

A molecular phylogeny of the cosmopolitan hyperdiverse genus Hydraena Kugelann (Coleoptera,Hydraenidae)

With almost 900 described species, Hydraena Kugelann (Hydraenidae) is one of the largest genera among Coleoptera. The subgeneric classification of Hydraena has been controversial, with 11 subgeneric names having so far been attributed to it. Some of these, Haenydra Rey and Spanglerina Perkins, have been treated as valid genera, as subgenera or as species groups. The most recent complete treatment of the genus, based on a cladistic analysis of morphological characters, recognized two major lineages, and only these were classified as subgenera: Hydraenopsis (mainly Gondwanan distribution), and Hydraena s.str. (mainly Laurasian). Here, we reconstruct the phylogeny of Hydraena using 212 species plus several outgroups and approximately 4 kb of sequence data from two nuclear (SSU and LSU) and four mitochondrial genes (cox1, rrnL, trnL and nad1). Data were aligned with two different strategies of multiple alignment (implemented in mafft and prank ), and the phylogenies reconstructed using maximum likelihood and Bayesian methods. We estimated approximate ages of the main nodes using a relaxed molecular clock with Bayesian methods, and an a priori evolutionary rate of 0.01 substitutions/site/million years (Ma) plus a calibration point based on a biogeographical split. We found strong support for the monophyly of Hydraena and many of the clades recognized with morphological data. The following clades are considered as subgenera: Phothydraena Kuwert, Spanglerina Perkins, Holcohydraena Kuwert, Hydraenopsis Janssens and Hydraena s.str. The placement of three species groups, two Neotropical (H. multispina group, H. paeminosa group) and one South African/Madagascan (H. monikae group), is uncertain, and they are considered incertae sedis within Hydraena. The origin of the genus was estimated to be in the Lower Eocene, with many species complexes diversifying in the Pleistocene. Dispersal events seem to have played a key role in order to determine the current distribution of the species groups in the southern hemisphere (mainly in Hydraenopsis).