Synthesis and Evaluation of Some 17-Acetamidoandrostane and N,N-Dimethyl-7-deoxycholic Amide Derivatives as Cytotoxic Agents: Structure/Activity Studies

Using pregnenolone and 7-deoxycholic acid as starting materials, some 17-acetamidoandrostane and N,N-dimethyl-7-deoxycholic amide derivatives were synthesized. The cytotoxicity of the synthesized compounds was tested in vitro against two tumor cell lines: SGC 7901 (human gastric carcinoma) and Bel 7404 (human liver carcinoma). The result showed that the blockage of the interaction of the amide group with outside groups might cause a decrease of the cytotoxicity, and an O-benzyloximino group at the 3-position of N,N-dimethyl-7-deoxycholic amide could enhance the cytotoxic activity of the compound. The information obtained from the studies provides the structure-activity relationship for these compounds and may be useful for the design of novel chemotherapeutic drugs

Synthesis and Evaluation of Some 17-Acetamidoandrostane and N,N-Dimethyl-7-deoxycholic Amide Derivatives as Cytotoxic Agents: Structure/Activity Studies

Using pregnenolone and 7-deoxycholic acid as starting materials, some 17-acetamidoandrostane and N,N-dimethyl-7-deoxycholic amide derivatives were synthesized. The cytotoxicity of the synthesized compounds was tested in vitro against two tumor cell lines: SGC 7901 (human gastric carcinoma) and Bel 7404 (human liver carcinoma). The result showed that the blockage of the interaction of the amide group with outside groups might cause a decrease of the cytotoxicity, and an O-benzyloximino group at the 3-position of N,N-dimethyl-7-deoxycholic amide could enhance the cytotoxic activity of the compound. The information obtained from the studies provides the structure-activity relationship for these compounds and may be useful for the design of novel chemotherapeutic drugs

Synthesis and Evaluation of Some 17-Acetamidoandrostane and N,N-Dimethyl-7-deoxycholic Amide Derivatives as Cytotoxic Agents: Structure/Activity Studies

Using pregnenolone and 7-deoxycholic acid as starting materials, some 17-acetamidoandrostane and N,N-dimethyl-7-deoxycholic amide derivatives were synthesized. The cytotoxicity of the synthesized compounds was tested in vitro against two tumor cell lines: SGC 7901 (human gastric carcinoma) and Bel 7404 (human liver carcinoma). The result showed that the blockage of the interaction of the amide group with outside groups might cause a decrease of the cytotoxicity, and an O-benzyloximino group at the 3-position of N,N-dimethyl-7-deoxycholic amide could enhance the cytotoxic activity of the compound. The information obtained from the studies provides the structure-activity relationship for these compounds and may be useful for the design of novel chemotherapeutic drugs

Mapping of Powdery Mildew Resistance Gene pmCH89 in a Putative Wheat-Thinopyrum intermedium Introgression Line

Powdery mildew, caused by Blumeria graminis f. sp. tritici (Bgt), is a globally serious disease adversely affecting wheat production. The Bgt-resistant wheat breeding line CH09W89 was derived after backcrossing a Bgt resistant wheat-Thinopyrum intermedium partial amphiploid TAI7045 with susceptible wheat cultivars. At the seedling stage, CH09W89 exhibited immunity or high resistance to Bgt pathotypes E09, E20, E21, E23, E26, Bg1, and Bg2, similar to its donor line TAI7045 and Th. intermedium. No Th. intermedium chromatin was detected based on genomic in situ hybridization of mitotic chromosomes. To determine the mode of inheritance of the Bgt resistance and the chromosomal location of the resistance gene, CH09W89 was crossed with two susceptible wheat cultivars. The results of the genetic analysis showed that the adult resistance to Bgt E09 in CH09W89 was controlled by a single recessive gene, which was tentatively designated as pmCH89. Two polymorphic SSR markers, Xwmc310 and Xwmc125, were linked to the resistance gene with genetic distances 3.1 and 2.7 cM, respectively. Using the Chinese Spring aneuploid and deletion lines, the resistance gene and its linked markers were assigned to chromosome arm 4BL in the bin 0.68–0.78. Due to its unique position on chromosome 4BL, pmCH89 appears to be a new locus for resistance to powdery mildew. These results will be of benefit for improving powdery mildew resistance in wheat breeding programs

Assessing spatial likelihood of flooding hazard using naïve Bayes and GIS: a case study in Bowen Basin, Australia

Flooding hazard evaluation is the basis of flooding risk assessment which has significances to natural environment, human life and social economy. This study develops a spatial framework integrating naïve Bayes (NB) and geographic information system (GIS) to assess flooding hazard at regional scale. The methodology was demonstrated in the Bowen Basin in Australia as a case study. The inputs into the framework are five indices: elevation, slope, soil water retention, drainage proximity and density. They were derived from spatial data processed in ArcGIS. NB as a simplified and efficient type of Bayesian methods was used, with the assistance of remotely sensed flood inundation extent in the sampling process, to infer flooding probability on a cell-by-cell basis over the study area. A likelihood-based flooding hazard map was output from the GIS-based framework. The results reveal elevation and slope have more significant impacts on evaluation than other input indices. Area of high likelihood of flooding hazard is mainly located in the west and the southwest where there is a high water channel density, and along the water channels in the east of the study area. High likelihood of flooding hazard covers 45 % of the total area, medium likelihood accounts for about 12 %, low and very low likelihood represents 19 and 24 %, respectively. The results provide baseline information to identify and assess flooding hazard when making adaptation strategies and implementing mitigation measures in future. The framework and methodology developed in the study offer an integrated approach in evaluation of flooding hazard with spatial distributions and indicative uncertainties. It can also be applied to other hazard assessments

Integrating Entropy-Based Naïve Bayes and GIS for Spatial Evaluation of Flood Hazard

Regional flood risk caused by intensive rainfall under extreme climate conditions has increasingly attracted global attention. Mapping and evaluation of flood hazard are vital parts in flood risk assessment. This study develops an integrated framework for estimating spatial likelihood of flood hazard by coupling weighted naïve Bayes (WNB), geographic information system, and remote sensing. The north part of Fitzroy River Basin in Queensland, Australia, was selected as a case study site. The environmental indices, including extreme rainfall, evapotranspiration, net-water index, soil water retention, elevation, slope, drainage proximity, and density, were generated from spatial data representing climate, soil, vegetation, hydrology, and topography. These indices were weighted using the statistics-based entropy method. The weighted indices were input into the WNB-based model to delineate a regional flood risk map that indicates the likelihood of flood occurrence. The resultant map was validated by the maximum inundation extent extracted from moderate resolution imaging spectroradiometer (MODIS) imagery. The evaluation results, including mapping and evaluation of the distribution of flood hazard, are helpful in guiding flood inundation disaster responses for the region. The novel approach presented consists of weighted grid data, image-based sampling and validation, cell-by-cell probability inferring and spatial mapping. It is superior to an existing spatial naive Bayes (NB) method for regional flood hazard assessment. It can also be extended to other likelihood-related environmental hazard studies.The authors appreciate the China Scholarship Council for providing a scholarship to Rui Liu to support this research at CSIRO Land and Water (CLW). The authors also want to thank the CLW for providing the data for this study. The study was funded by the National Natural Science Foundation of China (41130744/D0107, 41371343, and 41501460

Molecular Characterization of a New Wheat-Thinopyrum intermedium Translocation Line with Resistance to Powdery Mildew and Stripe Rust

A new wheat-Thinopyrum translocation line CH13-21 was selected from the progenies derived from a cross between wheat-Th. intermedium partial amphiploid TAI7047 and wheat line Mianyang11. CH13-21 was characterized by using genomic in situ hybridization (GISH), multicolor-GISH (mc-GISH), multicolor-fluorescence in situ hybridization (mc-FISH) and chromosome-specific molecular markers. When inoculated with stripe rust and powdery mildew isolates, CH13-21 displayed novel resistance to powdery mildew and stripe rust which inherited from its Thinopyrum parent. The chromosomal counting analyses indicated that CH13-21 has 42 chromosomes, with normal bivalent pairing at metaphase I of meiosis. GISH probed by Th. intermedium genomic DNA showed that CH13-21 contained a pair of wheat-Th. intermedium translocated chromosomes. Sequential mc-FISH analyses probed by pSc119.2 and pAs1 clearly revealed that chromosome arm 6BS of CH13-21 was replaced by Thinopyrum chromatin in the translocation chromosome. The molecular markers analysis further confirmed that the introduced Th. intermedium chromatin in CH13-21 belonged to the long arm of homoeologous group 6 chromosome. Therefore, CH13-21 was a new T6BS.6Ai#1L compensating Robertsonian translocation line. It concludes that CH13-21 is a new genetic resource for wheat breeding programs providing novel variation for disease resistances

Genome-wide identification and expression analysis of fatty acid-binding proteins (FABPs) in Chinese perch Siniperca chuatsi and their circadian rhythm responses to cadmium exposure

Fatty acid-binding proteins (FABPs) function as fatty acid chaperones, and they play a key role in lipid metabolism. The diversity of fabp gene family members is important for different fatty acid absorption and transport. In the present study, we identified 13 fabp genes from Chinese perch (Siniperca chuatsi). The spatiotemporal expression profiles of these 13 Sc-fabp genes, their circadian rhythm expression characteristics in intestine, and transcriptional regulation under cadmium exposure were investigated. Phylogenetic analysis indicated that the teleost-specific genome duplication event made a contribution to the expansion of Sc-fabp genes. The protein coding regions of all the 13 Sc-fabp genes were composed of 4 exons. These 13 genes exhibited similar protein length, but a low identity in protein sequences. The tissue expression profiles of most fabp genes in Chinese perch (Sc-fabp2a, Sc-fabp2b, Sc-fabp3, Sc-fabp6a, Sc-fabp7a, and Sc-fabp7b) were consistent with those of their orthologous genes in mammalian, but the Sc-fabp1, Sc-fabp6ba, and Sc-fabp6bb showed distinct tissue expression patterns from their orthologous genes in mammalian. The total expression level of Sc-fabps was increased with embryonic development, but it was decreased significantly after hatching. Sc-fabp1, Sc-fabp3, Sc-fabp11a, and Sc-fabp11b were the mainly expressed subtypes in embryonic development stages. Under natural conditions, the expression of these 4 subtypes Sc-fabp1, Sc-fabp2a, Sc-fabp2b, and Sc-fabp6a exhibited significant circadian rhythm in intestine, and their peak expression levels were observed from ZT 8.83 h to ZT 13.54 h. Cadmium exposure resulted in the up-regulation of fabp gene expression and the loss of circadian rhythm in Chinese perch intestine. Our results provide reference for further investigation of the biological functions of fabp gene subtypes in fish