Isatin-derived antibacterial and antifungal compounds and their transition metal complexes

A series of isatins incorporating thiazole, thiadiazole, benzothiazole and p-toluene sulfonyl hydrazide moieties, along with their cobalt(II), copper(II), nickel(II) and zinc(II) metal complexes have been synthesized and characterized by elemental analyses, molar conductances, magnetic moments, IR, NMR and electronic spectral data. These compounds have been screened for antibacterial activity against Escherichia coli, Bacillus subtillis, Shigella flexneri, Staphylococcus aureus, Pseudomonas aeruginosa and Salmonella typhi, and for antifungal activity against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani and Candida glaberata using the agar-well diffusion method. All the synthesized compounds have shown good affinity as antibacterial and/or antifungal agents which increased in most of the cases on complexation with the metal ions.     

Antibacterial Co(II), Cu(II), Ni(II) and Zn(II) Complexes of Thiadiazole Derived Furanyl,Thiophenyl and Pyrrolyl Schiff Bases

2-Amino-1,3,4-thiadiazole undergoes a condensation reaction with furane-, thiophene- and pyrrole-2-carboxaldehyde to form tridentate NNO, NNS and NNN donor Schiff bases. These Schiff bases were further used to obtain complexes of the type [M(L) 2] X, where M=Co(II), Cu(II), Ni(II) or Zn(II), L=L 1, L 2 or L 3 and X=Cl 2. The new compounds described here have been characterized by their physical, spectral and analytical data, and have been screened for antibacterial activity against several bacterial strains such as Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. The antibacterial potency of the Schiff bases increased upon chelation/complexation in comparison to the uncomplexed Schiff bases against the tested bacterial species thus, opening new approaches to find new ways in the fight against antibiotic-resistant strains.     

Why do neonates of aphidophagous ladybird beetles preferentially consume conspecific eggs in presence of aphids?

The neonates of aphidophagous ladybird beetles, Propylea dissecta, Coccinella transversalis and Coelophora saucia preferentially consumed conspecific eggs in presence of essential aphid prey, Aphis gossypii. This preference was strongest in P. dissecta and recorded in all density combinations of conspecific eggs and aphids. The neonates of all three species developed faster resulting in heavier second instars with lower mortality when fed on conspecific eggs as compared to mobile or defenceless aphids. In addition, they required less dry biomass of conspecific eggs than that of aphids. These results reveal that neonates are benefitted intrinsically when they feed on conspecific eggs. The neonates of P. dissecta exhibited discrimination for more nutritious food, as they contacted and ate conspecific eggs more frequently than aphids as their first meal. This discrimination was not found in Coccinella transversalis and Coelophora saucia possibly due to their bigger sizes and possible higher energy requirements. Although, the major effect of chemical cues was only noticed in P. dissecta, it could be concluded that chemicals (surface and within) of conspecific eggs possibly attract neonates for egg-cannibalism, as both eggs and aphids were consumed in greater numbers when coated with egg extracts. The reverse occurred when eggs and aphids were coated with aphid extracts.     

Polymorphisms of phase II xenobiotic-metabolizing and DNA repair genes and in vitro N-ethyl-N-nitrosourea-induced O6-ethylguanine levels in human lymphocytes

This study tested the hypothesis that genetic variants of phase II detoxification enzymes and DNA repair proteins affect individual response to DNA damage from alkylating agents. In 171 healthy individuals, an immunoslot blot assay was used to measure O6-ethylguanosine (O6-EtGua) adduct levels in peripheral blood lymphocytes treated with N-ethyl-N-nitrosourea (ENU) in vitro. The genotypes of GSTM1, GSTT1, GSTP1 I(105)V and A(114)V, MGMT L(84)F and I(143)V, XPD D(312)N and K(751)Q, and XRCC3 T(241)M were determined. Demographic and exposure information was collected by in-person interview. Student's t-test, analysis of (co)variance, and multiple linear regression models were used in statistical analyses. The mean and median (range) O6-EtGua levels were 94.6 and 84.8 (3.2-508.1)fmol/g DNA, respectively. The adduct level was significantly lower in people who smoked >or=25 years than that in never-smokers (square-root transformed mean values 8.20 versus 9.37, P=0.03). Multiple linear regression models revealed that GSTT1 (beta=-2.36, P=0.009) polymorphism was a significant predictor of the level of adducts in 82 never-smokers, whereas the number of years smoked (beta=-0.08, P=0.005) and XRCC3 T(241)M (beta=2.22, P=0.007) in 89 ever-smokers. The association between GSTP1 I(105)V, MGMT I(143)V, and XPD D(312)N with the level of adducts was not conclusive. Each polymorphism could explain 2-10% of the variation of the adduct level. These observations suggest that GSTT1 null and XRCC3 T(241)M polymorphism may have some functional significance in modulating the level of ENU-induced DNA damage and these effects are smoking-dependent. Results from this exploratory study need to be confirmed in other experimental systems.     

Management of <Emphasis Type="Italic">Nymphoides peltatum</Emphasis> using water level fluctuations in freshwater lakes of Kashmir Himalaya

Lakes have an esthetic significance that is particularly important for attracting tourism. In this context, it is often preferable for lakes to have clear water, so many lake managers attempt to achieve clear lake water by various means. However, the lakes of Kashmir Himalaya are undergoing several complex ecological changes due to, for example, increasing tourism, overfishing, and intensive agriculture, which are making these lakes less clear. One such change is the vigorous growth and development of aquatic weeds in the shallow-water areas of Kashmir Himalayan lakes. We thus, investigated the response of Nymphoides peltatum, a rapidly multiplying clonal species, to water depth, in order to determine whether water depth can be used to control the spread of this proliferating macrophyte. Different traits of the given plant species, such as the mean number of ramets, were significantly higher (F = 55.412, p = 0.000) at depth zone D1 (0–100 cm) than at depth zones D2 (101–200 cm) and D3 (201–300 cm). In all of the lakes, mean spacer length—a tool for facilitating plant spread—was observed to be significantly higher (F = 45.890, p = 0.000) at lower water levels (0–100 cm). Also, the reproductive structures (flowers) of N. peltatum showed significant variation with depth (F = 51.909, p = 0.000) and with the lake examined (F = 9.909, p = 0.001). Thus, the results obtained during the present study indicate the importance of water depth in the management of N. peltatum in various Kashmir Himalayan lakes.     

Antioxidant response and proteomic modulations in Indian mustard grown under salt stress

Productivity of Indian mustard (Brassica juncea L. Czern. and Coss.) is markedly reduced by salt stress. To develop salt tolerance in this important oilseed crop is a need of the hour. This study, based on analysis of growth parameters and antioxidant profile of fourteen Indian mustard genotypes treated with 50, 100, 150 and 200 mM of sodium chloride, was performed to identify the salt-sensitive and salt-tolerant genotypes. Salinity stress inhibited biomass accumulation and reduced the protein and chlorophyll contents in a dose-dependent manner. The reduction was the highest in genotype Pusa Agrani and lowest in CS-54, depicting their contrasting sensitivity to salt stress. Salt treatments triggered a concentration-dependent overproduction of reactive-oxygen species and a concurrent upregulation of the expression of different antioxidants. Genotype CS-54 showed the least damage and maintained a high antioxidant level with almost each salt treatment, exhibiting its competence to withstand the damage provoked by salinity stress. Genotype Pusa Agrani, on the contrary, depicted a salt-sensitive nature by way of its very high lipid peroxidation and low intensity of antioxidants. These two genotypes were further investigated through gel-based proteomic approach, which resulted in the identification and quantification of 42 salinity-responsive proteins related to different metabolic modifications. Molecular processes, including photosynthesis, redox homeostasis, nitrogen metabolism, ATP synthesis, protein synthesis and degradation, signal transduction and respiratory pathways, have exhibited significant changes. The identified stress-responsive proteins could pave the way to develop salt tolerance in Indian mustard plant, thus sustaining its productivity under salinity.     

Pyranocoumarins: A new class of anti-hyperglycemic and anti-dyslipidemic agents

A series of pyranocoumarin derivatives were synthesized and evaluated in vivo for their anti-hyperglycemic as well as anti-dyslipidemic activities. Compounds 7a, 7c, 8a, 8b, 8c, 8e and 8f have shown promising anti-hyperglycemic activities in sucrose loaded model (SLM) as well as sucrose challenged streptozotocin induced diabetic rat model (STZ). Compounds 8a and 8b were showing 38.0% and 42.0% blood glucose lowering activity in db/db mice model. In vitro anti-hyperglycemic activity evaluation exhibited that compounds 8a (IC₅₀ = 24.5 μM) and 8b (IC₅₀ = 36.2 μM) are potential PTP-1B inhibitors thereby revealing their possible mechanism of anti-diabetic action. Compounds 7a, 7b, 8a, 8b, 8d, 8e and 8f have shown significant anti-dyslipidemic activity in triton induced dyslipidemia in rats.     

Drought stress revealed physiological,biochemical and gene-expressional variations in ‘Yoshihime’ peach (Prunus Persica L) cultivar

It is indispensable to comprehend the mechanism that regulates plant responses to drought conditions to intensify the water use efficiency of stone fruits. The physiological, biochemical and molecular responses of drought-treated peach leaves were investigated. Results revealed that drought-treated plants manifested a significant attenuation in water potential as compared to control plants. Furthermore, sorbitol and proline contents were accumulated contrary to glucose, fructose, and sucrose that were dwindled significantly throughout the drought period. Similarly, the activities of antioxidant enzymes and expression pattern of related genes were hoisted to counter the lipid peroxidation in drought-treated plants. Moreover, reduced stomatal conductance has repressed the photosynthesis process and linked genes during drought stress. The expression level of regulatory genes (dehydration-responsive element-bindings and WRKYs) exhibited up-regulation in the drought-treated group. Overall, this study asserts that ‘Yoshihime’ peach cultivar possesses unique physiological, biochemical, and molecular responses under different spells of drought stress.     

Molecular characterization of Ephedra species found in Pakistan

Ephedra, also known as "ma huang", is a dioecious, drought- and frost-resistant, perennial, evergreen shrub with compelling medicinal value. The genus is represented by 42 species around the world, 9 of which were provisionally reported from Pakistan. Species of the genus have a controversial taxonomy due to their overlapping morphological features. Conventional tools alone are not sufficient for characterizing the species. The objective of present study was to assess the genetic variability present in different biotypes of Ephedra growing in Pakistan using molecular markers. A total of six genotypes collected from diverse geographic zones of Pakistan were used. The DNA of all genotypes was amplified using nine randomly amplified polymorphic DNA (RAPD) primers to study genetic variability at the molecular level. The dissimilarity coefficient matrix based on the data of 9 RAPD primers was used to construct a dendrogram which was then used to group the genotypes in clusters. Based on the dendrogram and dissimilarity coefficient matrix, the RAPD markers used here revealed a moderate to high level of genetic polymorphism (6 to 49%) among the genotypes. It was found that the collection of genotype accessions from Swat Valley in northwestern Pakistan was most distantly related to the other five collections. More molecular markers including functional genes and ribosomal spacer regions are suggested to find a better estimate of the genetic diversity present in Ephedra growing in Pakistan. The information provided here is useful for identifying valuable Ephedra variants which will be used for medicinal purposes and earning foreign currency.