Benzyl α-l-rhamnopyranoside 4, obtained by both conventional and microwave assisted glycosidation techniques, was subjected to 2,3-O-isopropylidene protection to yield compound 5 which on benzoylation and subsequent deprotection of isopropylidene group gave the desired 4-O-benzoylrhamnopyranoside 7 in reasonable yield. Di-O-acetyl derivative of benzoate 7 was prepared to get newer rhamnopyranoside. The structure activity relationship (SAR) of the designed compounds was performed along with the prediction of activity spectra for substances (PASS) training set. Experimental studies based on antimicrobial activities verified the predictions obtained by the PASS software. Protected rhamnopyranosides 5 and 6 exhibited slight distortion from regular 1C4 conformation, probably due to the fusion of pyranose and isopropylidene ring. Synthesized rhamnopyranosides 4–8 were employed as test chemicals for in vitro antimicrobial evaluation against eight human pathogenic bacteria and two fungi. Antimicrobial and SAR study showed that the rhamnopyranosides were prone against fungal organisms as compared to that of the bacterial pathogens. Interestingly, PASS prediction of the rhamnopyranoside derivatives 4–8 were 0.49 < Pa < 0.60 (where Pa is probability ‘to be active’) as antibacterial and 0.65 < Pa < 0.73 as antifungal activities, which showed significant agreement with experimental data, suggesting rhamnopyranoside derivatives 4–8 were more active against pathogenic fungi as compared to human pathogenic bacteria thus, there is a more than 50% chance that the rhamnopyranoside derivative structures 4–8 have not been reported with antimicrobial activity, making it a possible valuable lead compound.
A new series of multipotent antioxidants (MPAOs), namely Schiff base-1,2,4-triazoles attached to the oxygen-derived free radical scavenging moiety butylated hydroxytoluene (BHT) were designed and subsequently synthesized. The structure-activity relationship (SAR) of the designed antioxidants was established alongside the prediction of activity spectra for substances (PASS). The antioxidant activities of the synthesized compounds 4-10 were tested by the DPPH bioassay. The synthesized compounds 4-10 inhibited stable DPPH free radicals at a level that is 10´4 M more than the well-known standard antioxidant BHT. Compounds 8-10 with para-substituents were less active than compounds 4 and 5 with trimethoxy substituents compared to those with a second BHT moiety (compounds 6 and 7). With an IC 50 of 46.13˘0.31 µM, compound 6 exhibited the most promising in vitro inhibition at 89%. Therefore, novel MPAOs containing active triazole rings, thioethers, Schiff bases, and BHT moieties are suggested as potential antioxidants for inhibiting oxidative stress processes and scavenging free radicals, hence, this combination of functions is anticipated to play a vital role in repairing cellular damage, preventing various human diseases and in medical therapeutic applications.
One of the biggest problems for humans and animals worldwide is the harmful effects of the antibiotics, due to excessive use as a treatment for animal diseases. An alternative to overcome this problem is the use of certain growth promoters such as probiotics that have a good effect on host health and performance. Eight isolates included the following probiotic strains: Lactobacillus plantarum, L. acidophilus, L.rhamnosus, L. salivarius, and L. paracasei, as well as Bifidobacterium longum, B. adolescentis, and B. breve were investigated for low pH and bile salt tolerance, anti-bacterial and yeast activity using supernatant cell-free culture were assessed using agar-well diffusion method against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, , Escherichia coli MC1400 Listeria ivanovii and Candida albicans. Co-culture has determined the antifungal activities with Aspergillus niger, As. flavous, As. fumigatus and Penicillium chrysogenum. The antibiotic sensitivity was tested using the agar disc diffusion method. Each of the strains examined had variable antibacterial activity. All the isolates showed a variable inhibition level, as well. All of the isolates were Ciprofloxacin resistant. Additionally, the lactobacilli strains were Vancomycinresistant, and all of the strains show intermediate Clindamycin resistance. All isolates were Penicillin, Ampicillin, Tetracycline, Erythromycin, Gentamycin, Streptomycin, Florfenicol, Chloramphenicol, and Sulfamethoxazole & Trimethoprim susceptible. Collectively, the probiotic capacity of the strains tested and the antimicrobial activity without the transfer of antibiotic resistance suggested that these strains can be used as bio-preservatives in food products and medicinal preparations.
Probiotic strains were isolated from different cheeses (turkey and domiatii and cottage and kariesh cheese) and fermented products (yoghurt, raib, zeer milk and kishk). The isolates were screened for rate of growth increase in MSR broth at pH 3, pH4, acid production after 48 hours and degree of bile salt (0.3%) tolerance, strength of adhesion and clotting time (3 to 48 hrs) of skim milk. The good fourteen isolates identified as two Lactobacillus spp (S4b1 and S2a3), eleven Bifidobacterium spp. (RC1 b8, RC2 b1, SC1a4, RC4b2, FC1b1, RC2b4, RC4a3, LZ1a3 and LZa7) and one Streptoococcus spp. (RC2b3), were used against several human (Staphyllococcus aureus. and Eschericia coli) and plant (Rhizoctonia solani and Fusarium oxysporum) pathogens by examining their in vitro antimicrobial properties. Antibacterial activity of the good fourteen selected probiotic isolates in this test exhibited varying degrees of inhibitory activity against human pathogenic Staphyllococcus aureus. The isolates LZb8, S4b1 and RC2b3 exhibited the superior antibacterial activity with inhibition zones (I.Z.) ranged 8.3-8.4 mm followed by the isolates Kb2, LZa7 and Y2a5. The least activity was recorded for the isolates SCa4 and RC4b2 (I.Z.) ranged 2.3-2.5 mm. The antibacterial activity of the same probiotic isolates against human pathogenic Eschericia coli was almost similar to that obtained against S. aureus, and followed the same pattern. The isolates LZb8, S4b1 and RC2b3 possessed the highest activity, while the isolates SCa4 and RC4b2 were highly significantly the least active. It seems that the inhibitory activity of the isolates against E. coli was slightly less as compared to that obtained against S. aureus. The antifungal activity of the same14 probiotic isolates was tested against the plant pathogenic Rhizoctonia solani and Fusarium oxysporum. All probiotic isolates were highly significantly active on both fungi as compared to the control, showing % growth inhibition (%GI) ranges of 26.7-52.3 %, and 17.1-51.2 % against the first and the latter fungi, respectively. The most active isolates against R. solani were RC4b2 (52.3 % GI), followed by both RC4b3 and RC1b8 (47.6 % GI). Also, the most active isolate against F. oxysporum was Y2a5 (51.2 GI).
The effect of Herbaspirillum seropedicae inoculation and/or maize straw (0, 5 and 10 Mg/hm2) amendment on the growth and N2 fixation of wheat was determined in pot experiments using 15N-dilution method. Inoculation resulted in accumulation of fixed nitrogen, and % N from atmosphere being 24.6 and 26.5% in wheat shoot and grain, respectively. Straw amendment reduced % Natm to 16.1 and 20.2% at high straw level (10 Mg/hm2). Rational nitrogen fertilization (180 kg N/hm2) completely inhibited N2 fixation by H. seropedicae inoculation. Bacterial inoculation increased dry shoot and grain yield up to 23 and 31%, respectively. The highest levels of shoot and grain dry mass (46.5 and 42.4%) were obtained by N-fertilization in both inoculated and uninoculated plants. Total shoot and grain N-yield increased irrespective of organic matter amendment by inoculation up to 9 and 25%, respectively. N-fertilized plants recorded a maximum increase in N-yield (57 and 51%). H. seropedicae was reisolated from inoculated wheat histosphere after harvesting (90 d from sowing). Neither organic matter nor mineral nitrogen applications had any marked effect on bacterial total counts colonizing wheat histosphere. Moreover, no symptoms of mottled stripe disease were observed on leaves and stems of inoculated plants.
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