Synthesis of some novel 6-benzyl(or substituted benzyl)-2-beta-D-glucopyranosyl-1,2,4-triazolo[4,3-b][1,2,4]triazines as potential antimicrobial chemotherapeutics

Glucosidation of the new 8-amino-6-benzyl(or substituted benzyl)-2,8-dihydro-1,2,4-triazolo[4,3-b][1,2,4]triazin-7(3H)-ones (3a-d) with 2,3,4,6-tetra-O-acetyl-alpha-D-glucopyranosyl bromide 4 gave the corresponding N-glucosides 5a-d. Chemical transformations leading to new functionalities have also been achieved to give compounds 7-12. Antimicrobial activity of compounds 5a-c against Aspergillus fumigatus, Penicillium italicum, Syncephalastrum racemosum, Candida albicans, Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis, Escherichia coli is described.     

Delayed development of the whitefly (Bemisia tabaci) and increased parasitism by Encarsia bimaculata in response to sublethal doses of piperonyl butoxide

Abstract Effects of sublethal piperonyl butoxide (PB) on parasitization of Bemisia tabaci (Gennadius ) (Hemiptera: Aleyrodidae) by Encarsia bimaculata Heraty et Polaszek (Hymenoptera: Aphelinidae) were evaluated both in cage and greenhouse experiments. When first, second and third instar B. tabaci nymphs were treated with PB, all but the first instar were significantly prolonged. Data indicated that sublethal PB could improve E. bimaculata parasitism rates without influencing parasitoid eclosion rates. Prolonged development increased rates of parasitism by E. bimaculata, from 17.6% to 24.7% in cages, presumably by increasing the duration of host exposure. Sublethal PB combined with E. bimaculata as an integrated approach to control B. tabaci was evaluated using life table parameters under greenhouse conditions. Indices of population trend (I) calculated from life tables were estimated at 4.6 for B. tabaci exposed to PB and parasitoids compared to 14.1 with parasitoids alone and 23.5 in untreated controls. The results showed that after PB was sprayed and parasitoids introduced, development of B. tabaci was delayed and the peak of each stage was postponed. The older nymphal stage had highest mortality, primarily due to mortality caused by parasitism by E. bimaculata.     

The promoter of filamentation (POF1) protein from <Emphasis Type="Italic">Saccharomyces cerevisiae</Emphasis> is an ATPase involved in the protein quality control process

Background

The gene YCL047C, which has been renamed promoter of filamentation gene (POF1), has recently been described as a cell component involved in yeast filamentous growth. The objective of this work is to understand the molecular and biological function of this gene.

Results

Here, we report that the protein encoded by the POF1 gene, Pof1p, is an ATPase that may be part of the Saccharomyces cerevisiae protein quality control pathway. According to the results, Δpof1 cells showed increased sensitivity to hydrogen peroxide, tert-butyl hydroperoxide, heat shock and protein unfolding agents, such as dithiothreitol and tunicamycin. Besides, the overexpression of POF1 suppressed the sensitivity of Δpct1, a strain that lacks a gene that encodes a phosphocholine cytidylyltransferase, to heat shock. In vitro analysis showed, however, that the purified Pof1p enzyme had no cytidylyltransferase activity but does have ATPase activity, with catalytic efficiency comparable to other ATPases involved in endoplasmic reticulum-associated degradation of proteins (ERAD). Supporting these findings, co-immunoprecipitation experiments showed a physical interaction between Pof1p and Ubc7p (an ubiquitin conjugating enzyme) in vivo.

Conclusions

Taken together, the results strongly suggest that the biological function of Pof1p is related to the regulation of protein degradation.

     

Profiling the Lipophilic Fractions of Pithecellobium dulce Bark and Leaves Using GC/MS and Evaluation of Their Antioxidant,Antimicrobial and Cytotoxic Activities

Pithecellobium dulce has been used in traditional medicine to treat various ailments owing to its restorative properties. The biological activities and chemical profiles of the lipophilic fraction of P. dulce bark and leaves were assessed herein. Fatty acid methyl esters (FAME) and unsaponifiable matter (USM) were prepared and analyzed by GC/MS. A total of 40 compounds were identified in the bark saponifiable fraction, whereas 9 compounds were annotated in the leaves. Palmitic acid methyl ester was the major compound identified accounting for 41.48 % of the bark and 19.03 % of the leaves composition. Besides, linolenic acid methyl ester (22.40 %) and linoleic acid (12.69 %) were annotated in the leaves saponifiable fraction. A total of 63 compounds were detected in the bark USM and 4 compounds were identified in the leaves. Phytol represented the major component in the leaves (52.57 %) followed by lupeol (20.68 %) and lupenone (8.60 %). Meanwhile, n‐dodecane dominated in the bark USM accounting for 24.69 % of the total composition. The leaves and bark lipophilic fractions revealed moderate antioxidant and antibacterial activities. Both extracts showed no antifungal activity. No cytotoxicity was observed for both lipophilic fractions. P. dulce offers a good source of antioxidant compounds that can be introduced to food and pharmaceutical industry.     

Foliar Concentrations of Selected Elements,Assessment of Oxidative Stress Markers and Role of Antioxidant Defense System is Associated with Fly Ash Stress Tolerance in Withania somnifera

Journal of Plant Growth Regulation - Increased dependence on thermal power has resulted in a significant increase in the generation of fly ash&nbsp;(FA), which exacerbates environmental...     

Review and future prospects on the mechanisms related to cold stress resistance and tolerance in medicinal plants

Medicinal plants play important role in industrial production of medicines. Moreover, they consume without complicated processes around the world. They are considered as healthy cure without any harmful side effects at least among ordinary people. Cold stress is one the harmful abiotic stresses and constrains medicinal plants yielding geographically. Cold acclimation is a process that induces cold stress resistance in temperate plants. Various structural and morphological alterations are involved in this process. Also, enzymatic and non-enzymatic agents play role in cold acclimation. Cell membrane modification and compatible solutes accumulation and so many other changes occur through cold acclimation. Growing under different stressful conditions, medicinal plants synthesize different components such as metabolites. Moreover, ROS can be generated in plant cells under stressful conditions. The accumulation of bioactive components, biosynthesis of phytohormones, ion hemostasis, osmolyte (compatible solutes) accumulation and changes in nutrient uptake, root system modification and systemic resistance are some of new investigations that are considered in this review.     

Selective Synthesis and Structure of 6-Arylvinyl-2- and 4-Glucosyl-1,2,4-triazines of Expected Interesting Biological Activity

Abstract

The 6-β-arylvinyl-2- and 4-glucosyl-3-thioxo-2,3-dihydro-1,2,4-triazin-5(4H)-ones were synthesized with high selectivity using the recently developed amino protecting group strategy. The structure of these new glucosides was established chemically and spectroscopically. Also, some interesting chemical transformations and rearrangements were observed.     

Assessment of Soluble and Biomass K in Culture Medium Is a Reliable Tool for Estimation of K Releasing Efficiency of Bacteria

Abstract

Assessing the amount of released K from minerals in bacterial liquid culture is the main process for screening and isolation of efficient potassium releasing bacteria (KRB). This study was aimed to determine the amount of released K in solution phase or supernatant (SK) as well as microbial biomass K (MBK). Therefore, 20 different bacterial isolates belonging to the 10 bacterial genera (Beijerinckia, Klebsiella, Azotobacter, Pseudomonas, Agrobacterium, Rhizobium, Sphingomonas, Citrobacter, Microbacterium, and Achromobacter) were individually used to inoculate Aleksandrov medium in presence of biotite or muscovite. Our results from in-vitro experiments revealed that the MBK (K in pellet) is more important than in SK. Although some genera such as Azotobacter and Citrobacter released more SK (16?mg/l from biotite and 12.77?mg/l from muscovite, respectively), the Klebsiella isolates with the highest MBK could release an average of 90?mg/l total K. This study indicated that the assimilated K in microbial cells is the main part of K dissolution from minerals. Due to the fast turnover of nutrients in bacterial biomass, it can be concluded that both SK and MBK could be available for plants. It seems that the finding of this research should be considered in the isolation of KRB.

Highlights

• This study reports, assessment of soluble and biomass K in the culture medium is a reliable tool for estimation of K releasing efficiency of bacteria

• Our results from in vitro experiments revealed that the assimilated K in microbial cells is the main part of K dissolved from minerals.

• Although some genera such as Azotobacter released more K in solution phase, the Klebsiella isolates with the highest biomass K could release more total K

     

Phase II Study of Concurrent Capecitabine and External Beam Radiotherapy for Pain Control of Bone Metastases of Breast Cancer Origin

Background

Pain from bone metastases of breast cancer origin is treated with localized radiation. Modulating doses and schedules has shown little efficacy in improving results. Given the synergistic therapeutic effect reported for combined systemic chemotherapy with local radiation in anal, rectal, and head and neck malignancies, we sought to evaluate the tolerability and efficacy of combined capecitabine and radiation for palliation of pain due to bone metastases from breast cancer.

Methodology/Principal Findings

Twenty-nine women with painful bone metastases from breast cancer were treated with external beam radiation in 10 fractions of 3 Gy, 5 fractions a week for 2 consecutive weeks. Oral capecitabine 700 mg/m² twice daily was administered throughout radiation therapy. Rates of complete response, defined as a score of 0 on a 10-point pain scale and no increase in analgesic consumption, were 14% at 1 week, 38% at 2 weeks, 52% at 4 weeks, 52% at 8 weeks, and 48% at 12 weeks. Corresponding rates of partial response, defined as a reduction of at least 2 points in pain score without an increase in analgesics consumption, were 31%, 38%, 28%, 34% and 38%. The overall response rate (complete and partial) at 12 weeks was 86%. Side effects were of mild intensity (grade I or II) and included nausea (38% of patients), weakness (24%), diarrhea (24%), mucositis (10%), and hand and foot syndrome (7%).

Conclusions/Significance

External beam radiation with concurrent capecitabine is safe and tolerable for the treatment of pain from bone metastases of breast cancer origin. The overall and complete response rates in our study are unusually high compared to those reported for radiation alone. Further evaluation of this approach, in a randomized study, is warranted.

Trial Registration

ClinicalTrials.gov {"type":"clinical-trial","attrs":{"text":"NCT01784393","term_id":"NCT01784393"}}NCT01784393{"type":"clinical-trial","attrs":{"text":"NCT01784393","term_id":"NCT01784393"}}NCT01784393