Synthesis, antimicrobial and in vitro antitumor activities of a series of 1,2,3-thiadiazole and 1,2,3-selenadiazole derivatives.

Three derivatives of substituted 1,2,3-thia- or 1,2,3-selenadiazole (4a-c) were prepared and characterized by different chemical techniques. These compounds were evaluated for their antimicrobial and antitumor activities. Compounds 4a (propenoxide derivative), 4b (carbaldehyde derivative), and 4c (benzene derivative) were active against the yeast-like fungi Candida albicans. Compound 4a was active against gram-negative Escherichia coli, and compound 4c was active against the gram-positive Staphylococcus aureus. For the antitumor activity, both compounds 4b and 4c were active against all tested tumor cell lines, namely, SW480, HCT116, C32, MV3, HMT3522, and MCF-7. The activity of compound 4c was greater than that of compound 4b and more than that of the reference antitumor 5-flourouracil against the SW480, HCT116, and MCF-7 tumor cell lines. In conclusion, a number of the prepared 1,2,3-thia- or 1,2,3-selenadiazole compounds showed promising antifungal, antibacterial, and in vitro antitumor activities. Further investigations are required to explore the mechanism by which active compound are inducing their cytotoxicity.

Altholactone displays promising antimicrobial activity.

The antimicrobial activity of altholactone, a naturally extracted styryllactone isolated from Goniothalamus malayanus, was determined against Gram positive (S. aureus ATTC 25923, S. aureus ATTC 25392, and E. faecalis ATTC 29212) and Gram negative (E. coli ATTC 35218, S. typhi ATTC 14023 and P. aeruginosa ATCC 27853) reference bacteria and against the fungus C. albicans ATTC 10231. Different concentrations of altholactone (0, 12, 25, and 50 µg/mL) were used. Results revealed that altholactone inhibited the growth of all tested microbes except P. aeruginosa ATCC 27853 in a dose-dependent manner, with the highest cytotoxic effects occurring at 50 µg/mL. The average of the inhibition zones of the different concentrations was between 0-30 mm. Furthermore, altholactone-induced antimicrobial activity against the more sensitive microbes was assessed by measuring the minimal inhibitory concentration (MIC). Results indicated that Gram positive (S. aureus ATTC 25923, S. aureus ATTC 25392, and E. faecalis ATTC 29212) cells were more sensitive to altholactone than Gram negative ones (E. coli ATTC 35218, S. typhi ATTC 14023). C. albicans showed moderate sensitivity. These results indicate that altholactone might be a potential antimicrobial agent, particularly in ciprofloxacin-refractory S. aureus and E. faecalis infections. Further investigations are required to illustrate the mechanism(s) by which altholactone produces its antimicrobial effects.

Synthesis, characterization and antimicrobial activity of new 1,2,3-selenadiazoles.

The commercially available aromatic polyketones 1a-d were utilized for the synthesis of the multi-arm1,2,3-selenadiazole derivatives 3a-d. The preparation starts with the reaction between compounds 1a-d and p-toluenesulfonyl hydrazide to give the corresponding tosylhydrazones 2a-d. Subsequent reaction with selenium dioxide leads to regiospecific ring closure of the tosylhydrazones to give the target multi-arm 1,2,3-selenadiazole derivatives in high yield. A 1,2,3-selenadiazole derivative 3e containing an epoxide ring was also prepared. The structures of all the synthesized compounds were confirmed on the basis of spectral and analytical data. The compounds were screened in vitro for their antimicrobial activity against various pathogenic bacterial and Candida strains obtained from King Abdullah Hospital in Irbid -Jordan. Compounds 3a, 3c and 3e were found to be highly active against all the selected pathogens. Compound 3e showed an inhibition zone of 13 mm against the highly resistant P. aruginosa.

Susceptibility of local Agrobacterium tumefaciens strains to streptomycetes isolates from Jordan soils.

Five strains of Agrobacterium tumefaciens were isolated and characterized from 12 different plant tumors. The susceptibility of these phytopathogens to antibiotics and to soil Streptomyces isolates was tested. Among the 90 Streptomyces isolates, only 12 were able to inhibit the growth of at least one A. tumefaciens strain. Four strains of A. tumefaciens were susceptible to streptomycin and cefotaxime. In addition, Streptomyces 404 strain was able to inhibit the growth of four strains of the Agrobacterium pathogens with an inhibition zone diameter ranged between 10 and 16 mm. The strong inhibitory effects of Streptomyces 404 strain on A. tumefaciens suggest the use of this strain as a promising agent to control crown gall disease.

Assessment of heavy metals concentrations in soil samples from the vicinity of busy roads: influence on Drosophila melanogaster life cycle.

An assessment of Cd, Cu, Pb, and Zn in 25 soil samples collected near busy roads in Irbid city, Jordan indicated contamination of these soil samples with different concentrations of 624, 1.243, 242, and 847 microg/g for Pb, Cd, Cu, and Zn, respectively. The survival percentage of Drosophila melanogaster third-instar larvae on synthetic medium containing these concentrations for the first generation shows a significant reduction in their growth and development or metamorphosis for most soil extracts. Moreover, there was a significant reduction in survival growth and development in the second generation. The survival percentages of the second generation at pupa stage was higher than the first generation, whereas at the adult stage, there was a lower survival percentage indicating some effects on metamorphosis caused by concentration of heavy metals on Drosophila melanogaster.

Uptake of zinc and copper by halophilic bacteria isolated from the Dead Sea shore, Jordan.

Ten Gram-positive and gram-negative bacterial cultures were recovered from nine water, mud, and soil samples collected from the Dead Sea shore at Suwaymah. All bacterial cultures were able to grow at 10% NaCl and at 45 degrees C. They were able to grow in nutrient media supplemented with 1250 ppm of Zn. Most of them, except cultures 2 and 8, were able to grow in nutrient medium supplemented with 1000 ppm of Cu. After 2 wk of incubation of these 10 cultures at different concentrations (5, 25, 100, and 500 ppm), stock solutions of both Zn and Cu elements, the maximum absorption using atomic absorption spectrometry for Zn was achieved by culture 7 at 11.2%, 1.0%, 38.4%, and 84.54%, respectively, from the previous stock solutions, whereas the maximum absorption of the same concentration of Cu was achieved by culture 3 at 6.2%, 55.56%, 85.66%, and 90.82%, respectively, of the different concentrations. After 3 wk of incubation, the estimated absorption for Zn was achieved by cultures 2, 9, and 10 at 19.2%, 16.68%, 42.92%, and 76.5%, 18.2%, 21.56%, 32.22%, and 77.43%, and 20.8%, 23.52%, 32.22%, and 82.84% of the previous stocks. The maximum absorption of the same concentration of Cu was achieved by culture 3 at 32.6%, 49.88%, 90.44%, and 91.86%, respectively. The accumulation of the absorbed metals was found to be maximum in the protoplast of all cultures. The accumulation at the cell wall was maximum for cultures 2 and 6 for Zn and Cu, respectively, and between the cell wall and the plasma membrane, it was maximum for cultures 2 and 8 for Zn and Cu, respectively.

Removal of lead and cadmium by halophilic bacteria isolated from the Dead Sea shore, Jordan.

Ten Gram-positive and Gram-negative bacterial cultures were recovered from nine water, mud, and soil samples from the Dead Sea shore at Suwaymah. They were able to grow at 10% NaCl and at 45 degrees C. Bacterial cultures 6 and 8 were able to grow in nutrient media supplemented with 2250 ppm of Pb. Bacterial cultures 1, 3-6, 9, and 10 were able to grow in nutrient medium supplemented with 1000 ppm of Cd. Atomic absorption spectrometry was used to estimate the absorbed Pb and Cd by bacterial cultures from 5-, 25-, 100-, and 500-ppm stock solutions of both elements. After 2 wk, the results showed that the maximum absorption for Pb was achieved by culture 6 in the following percentages: 79.8%, 70.48%, 89.48%, and 83.39%, respectively. The maximum absorption of the same concentration of Cd was achieved by culture 9 with the following percentages: 69.2%, 32.24%, 44.98%, and 60.0%, respectively. After 3 wk of incubation, the estimated absorption of both heavy metals was achieved by the same cultures (6 and 9), respectively, in the following percentages: 86.8%, 76.72%, 96.25%, and 96.0% for Pb and 82.60%, 93.2%, 92.74%, and 89.79% for Cd. The accumulation of the absorbed metals was found to be maximum in the protoplast of all the cultures. The accumulation at the cell wall was maximum in culture 2, and between the cell wall and the plasma membrane, it was maximum in cultures 2 and 8 for Pb and Cd, respectively.

Effect of different heavy-metal concentrations on Drosophila melanogaster larval growth and development.

The survival percentage of Drosophila melanogaster larvae on synthetic media containing different concentrations of heavy metals, including Cd, Cu, Pb, and Zn, in the first generation indicated no significant reduction in their growth and development up to 500 ppm for all tested heavy-metal concentrations. At 500 ppm, results showed that there was a significant reduction in pupa and adult stages: 65% and 25% for Cd, 50% and 25% for Cu, 100% and 95% for Pb, and 85% and 75% for Zn, respectively. The survival percentages at 1000 ppm were further significantly reduced: 15% and 0% for Cd, 35% and 15% for Cu, 45% and 90% for Pb, and 65% and 35% for Zn, respectively for pupa and adult stages. For the second generation, there was no significant reduction in survival growth and development up to 100 ppm, but above 500 ppm, there was a significant reduction. For most of these heavy-metal concentrations, the survival percentages of the second generation at the pupa stage was higher than the first generation, whereas for the adult, there was a lower survival percentage, indicating some effect on metamorphosis of these heavy-metal concentrations on Drosophila melanogaster Comparing the survival percentage between first and second generations at 500 ppm for pupa indicate a significant increase on Cu only, and for the adult, there was a significant reduction for Cd.

Molecular characterization of local Bacillus thuringiensis strains recovered from Northern Jordan.

A total of 80 isolates of Bacillus thuringiensis were recovered from different habitats of Northern Jordan. These isolates were grouped into three classes based on crystal morphology (spherical, bipyramidal, and both bipyramidal and cuboidal). The isolates that produced spherical crystals were the most common and the most toxic to diptera. SDS-PAGE analysis of the isolates and some reference strains with similar crystal morphology showed similar protein profiles with heterogeneous multiple protein components. The plasmid DNA content of the isolates in comparison with B. thuringiensis serovar israelensis gave a similar single intense DNA band.