Synthesis of 2-{(5-phenyl-1,3,4-Oxadiazol-2-yl)sulfanyl}-N-substituted acetamides as potential antimicrobial and hemolytic agents.

A new series of N-substituted derivatives of 2-{(5-phenyl-1,3,4-Oxadiazol-2-yl)sulfanyl}acetamides was synthesized. The synthesis was carried out by converting benzoic acid (1) into ethyl benzoate (2), benzohydrazide (3) and then 5-pheny-1,3,4-Oxadiazol-2-thiol (4) step by st0ep. The target compounds 6a-p were synthesized by reaction of compound 4 with equimolar ratios of different N-alkyl/aryl substituted 2-bromoacetamide (5a-p) in the presence of DMF and sodium hydride (NaH). The spectral (EI-MS, IR, (1)H-NMR) characterization of all the synthesized compounds reveal their successful synthesis. The compounds were also screened for antimicrobial & hemolytic activity and most of them were found to be active against the selected microbial species at variable extent relative to reference standards. But 6h was the most active against the selected panel of microbes. This series showed less toxicity and may be considered for further biological screening and application trial except 6m, possessing higher cytotoxicity.

Plant-endophyte mediated improvement in physiological and bio-protective abilities of marigold (Tagetes patula).

Endophytic bacteria improve the growth, physiology, and metabolite profile of plants. They are known as potential biocontrol agents of soil-borne diseases. This study evaluated the effects of endophytic bacterial strains on growth, vase life, biochemical attributes, and antioxidant and nematicidal activities of French marigold (Tagetes patula). French marigold seeds were sole and consortium inoculated with three promising endophytic bacterial strains, Burkholderia phytofirmans (PsJN), Enterobacter sp. (MN17), and Bacillus sp. (MN54). The vase life of French marigold was promoted by 66.6% in the individual application of PsJN and 100% in plants treated with consortium compared to the uninoculated control. The shoot and root fresh weights were also increased by 65.9 and 68.7%, with the combined application of all three strains. The total phenolics, flavonoid, and protein contents were higher in consortium treatment with an increase of up to 38.0, 55.9, and 65.9%, respectively, compared to the uninoculated control. Furthermore, combined application of endophytic bacterial strains promoted DPPH radical scavenging, mortality of plant-parasitic nematodes, and ferric reducing antioxidant power activities with increase of up to 278.0, 103.8, and 178.0%, respectively, compared to uninoculated control. An increase in antioxidant activities of ascorbate peroxidase (APX), catalase (CAT), glutathione peroxidase (GPX), and superoxide dismutase (SOD) were observed up to 77.3, 86.0, 91.6, and 102.9%, respectively by combined application of endophytic bacterial strains. So, given the economic importance of floriculture crops, endophytic bacterial isolates studied here have shown a great potential for improving the productivity of cultivated ornamental French marigold.

Co-composted Biochar Enhances Growth, Physiological, and Phytostabilization Efficiency of Brassica napus and Reduces Associated Health Risks Under Chromium Stress.

Among heavy metals, chromium (Cr) contamination is increasing gradually due to the use of untreated industrial effluents for irrigation purposes, thereby posing a severe threat to crop production. This study aimed to evaluate the potential of compost, biochar (BC), and co-composted BC on the growth, physiological, biochemical attributes, and health risks associated with the consumption of Brassica grown on Cr-contaminated soil. Results revealed that Cr stress (Cr-25) significantly reduced the growth and physiological attributes and increased antioxidant enzyme activities in Brassica, but the applied amendments considerably retrieved the negative effects of Cr toxicity through improving the growth and physiology of plants. The maximum increase in plant height (75.3%), root length (151.0%), shoot dry weight (139.4%), root dry weight (158.5%), and photosynthetic rate (151.0%) was noted with the application of co-composted BC under Cr stress (Cr-25) in comparison to the control. The application of co-composted BC significantly reduced antioxidant enzyme activities, such as APX (42.5%), GP (45.1%), CAT (45.4%), GST (47.8%), GR (47.1%), and RG (48.2%), as compared to the control under Cr stress. The same treatment reduced the accumulation of Cr in grain, shoot, and roots of Brassica by 4.12, 2.27, and 2.17 times and enhanced the accumulation in soil by 1.52 times as compared to the control. Moreover, the application of co-composted BC significantly enhanced phytostabilization efficiency and reduced associated health risks with the consumption of Brassica. It is concluded that the application of co-composted BC in Cr-contaminated soil can significantly enhance the growth, physiological, and biochemical attributes of Brassica by reducing its uptake in plants and enhanced phytostabilization efficiency. The tested product may also help in restoring the soils contaminated with Cr.

Astragalin: A Bioactive Phytochemical with Potential Therapeutic Activities.

Natural products, an infinite treasure of bioactive chemical entities, persist as an inexhaustible resource for discovery of drugs. This review article intends to emphasize on one of the naturally occurring flavonoids, astragalin (kaempferol 3-glucoside), which is a bioactive constituent of various traditional medicinal plants such as Cuscuta chinensis. This multifaceted compound is well known for its diversified pharmacological applications such as anti-inflammatory, antioxidant, neuroprotective, cardioprotective, antiobesity, antiosteoporotic, anticancer, antiulcer, and antidiabetic properties. It carries out the aforementioned activities by the regulation and modulation of various molecular targets such as transcription factors (NF-κB, TNF-α, and TGF-ß1), enzymes (iNOS, COX-2, PGE2, MMP-1, MMP-3, MIP-1α, COX-2, PGE-2, HK2, AChe, SOD, DRP-1, DDH, PLCγ1, and GPX), kinases (JNK, MAPK, Akt, ERK, SAPK, IκBα, PI3K, and PKCß2), cell adhesion proteins (E-cadherin, vimentin PAR-2, and NCam), apoptotic and antiapoptotic proteins (Beclin-1, Bcl-2, Bax, Bcl-xL, cytochrome c, LC3A/B, caspase-3, caspase-9, procaspase-3, procaspase-8, and IgE), and inflammatory cytokines (SOCS-3, SOCS-5, IL-1ß, IL-4, IL-6, IL-8, IL-13, MCP-1, CXCL-1, CXCL-2, and IFN-γ). Although researchers have reported multiple pharmacological applications of astragalin in various diseased conditions, further experimental investigations are still mandatory to fully understand its mechanism of action. It is contemplated that astragalin could be subjected to structural optimization to ameliorate its chemical accessibility, to optimize its absorption profiles, and to synthesize its more effective analogues which will ultimately lead towards potent drug candidates.