Synthesis,Molecular Modeling,and Biological Evaluation of Novel Chiral Thiosemicarbazone Derivatives as Potent Anticancer Agents

A series of new chiral thiosemicarbazones derived from homochiral amines in both enantiomeric forms were synthesized and evaluated for their in vitro antiproliferative activity against A549 (human alveolar adenocarcinoma), MCF‐7 (human breast adenocarcinoma), HeLa (human cervical adenocarcinoma), and HGC‐27 (human stomach carcinoma) cell lines. Some of compounds showed inhibitory activities on the growth of cancer cell lines. Especially, compound 17b exhibited the most potent activity (IC₅₀ 4.6 μM) against HGC‐27 as compared with the reference compound, sindaxel (IC₅₀ 10.3 μM), and could be used as a lead compound to search new chiral thiosemicarbazone derivatives as antiproliferative agents. Chirality 27:177–188, 2015. © 2014 Wiley Periodicals, Inc.     

The in vivo incorporation of linolenic acid into neuronal and glial cells and myelin

Abstract— Neurons, astrocytes, oligodendrocytes, and myelin were prepared from 21-day-old rat brain at various times after intracerebral injection of [1-¹⁴C]linolenate. Comparisons of phospholipid specific radioactivity demonstrated that the oligodendrocytes were much more active than neuronal, astroglial, or myelin fractions. This is consistent with the concept that the oligodendrocyte is responsible for synthesis of the relatively large mass of myelin sheath. Initially the phosphatidylcholine fraction was more active than the phosphatidylethanolamine fraction, but during the 36 h after injection the former decreased in radioactivity while the latter fraction showed an increase. Fatty acid elongation occurred rapidly. Within 2h after injection, 2/3 of the label had been converted to elongated products (20:4. 20:5, 22:5 and 22:6). All three cell types apparently contained the enzymes necessary to incorporate, elongate, and desaturate linolenic acid and this occurred at similar rates in each cell type. No direct precursor-product relationship was found between the lipids of oligodendrocytes and myelin. There was, however, a lag in the appearance of elongated fatty acids in the phosphoglycerides of myelin. indicating that the polyunsaturated fatty acids in myelin were synthesized elsewhere and transported into the myelin sheath.     

Fine‐scale Population Genetic Structure of Two Dioecious Indian Keystone Species,Ficus hispida and Ficus exasperata (Moraceae)

Although Ficus (Moraceae) is a keystone plant genus in the tropics, providing resources to many frugivorous vertebrates, its population genetic structure, which is an important determinant of its long‐term survival, has rarely been investigated. We examined the population genetic structure of two dioecious fig species (Ficus hispida and Ficus exasperata) in the Indian Western Ghats using co‐dominant nuclear microsatellite markers. We found high levels of microsatellite genetic diversity in both species. The regression slopes between genetic relationship coefficients (f_ij) and spatial distances were significantly negative in both species indicating that, on average, individuals in close spatial proximity were more likely to be related than individuals further apart. Mean parent–offspring distance (σ) calculated using these slopes was about 200 m in both species. This should be contrasted with the very long pollen dispersal distances documented for monoecious Ficus species. Nevertheless, overall population genetic diversity remained large suggesting immigrant gene flow. Further studies will be required to analyze broader scale patterns.     

Clonal abortion of bone marrow T cell precursors: T cells acquire specific antigen reactivity prethymically

Lethally irradiated (900 R) mice were reconstituted with bone marrow cells from syngeneic donors that had been tolerized 2 to 3 wk earlier to either DNP or TNP compounds. Five weeks after reconstitution, these animals were tested for their ability to mount a delayed hypersensitivity (DH) response to the tolerizing haptens. Recipient mice were specifically tolerant to the hapten that was used to induce tolerance in the marrow donor. Mixing experiments in which mice were reconstituted with marrow from DNP-tolerant and TNP-tolerant donors showed no indication of active suppression or effective antigen carry-over in this system. This observation held true even in experiments in which mice were reconstituted with a mixture of marrow from tolerant and normal donors at a ratio of 5:1. Thus the reduced responsiveness in recipient mice seemed to be due to the functional elimination of hapten-responsive T cell precursor (pre-T) clones. Recipient unresponsiveness was also shown to be MHC restricted. Maintenance of unresponsiveness appeared to be due to the restricted access of regenerating pre-T cell clones to the maturational influence of the recipient's thymus.     

Significance of partial pre-acidification of glucose for methanogenesis in an anaerobic digestion process

Summary The effect of partial pre-acidification of carbohydrate containing wastewaters on anaerobic digester performance was investigated. The influent was a 1% (w/v) glucose solution in a mineral salts medium imposing carbon-limited growth conditions. Up to 13% of the Chemical Oxygen Demand (COD) was added as volatile fatty acids (VFA).In all cases, addition of VFA to the glucose medium resulted in significant increases in the maximum specific COD-conversion rates of the sludge (both with respect to continuous feeding and following a shock loading), as compared with values found on digestion of glucose media alone.     

Space use and genetic structure do not maintain color polymorphism in a species with alternative behavioral strategies

Space use including territoriality and spatial arrangement within a population can reveal important information on the nature, dynamics, and evolutionary maintenance of alternative strategies in color polymorphic species. Despite the prevalence of color polymorphic species as model systems in evolutionary biology, the interaction between space use and genetic structuring of morphs within populations has rarely been examined. Here, we assess the spatial and genetic structure of male throat color morphs within a population of the tawny dragon lizard, Ctenophorus decresii. Male color morphs do not differ in morphology but differ in aggressive and antipredator behaviors as well as androgen levels. Despite these behavioral and endocrine differences, we find that color morphs do not differ in territory size, with their spatial arrangement being essentially random with respect to each other. There were no differences in genetic diversity or relatedness between morphs; however, there was significant, albeit weak, genetic differentiation between morphs, which was unrelated to geographic distance between individuals. Our results indicate potential weak barriers to gene flow between some morphs, potentially due to nonrandom pre‐ or postcopulatory mate choice or postzygotic genetic incompatibilities. However, space use, spatial structure, and nonrandom mating do not appear to be primary mechanisms maintaining color polymorphism in this system, highlighting the complexity and variation in alternative strategies associated with color polymorphism.