Evaluation of five medicinal plants for the management of Sitophilus oryzae in stored rice and identification of insecticidal compound.

Sitophilus oryzae is a kind of stored grain pest. This is controlled by using natural pesticides, which are more reliable, cost-effective, biodegradable, and eco-friendly than synthetic pesticides. Several plants show different insecticidal activities against various pests on their different parts (leaves, seeds, etc.). In this study, methanolic extracts of Lantana camara (leaves), Carica papaya (seeds), Ricinus communis (leaves), Calotropis gigantea (flowers), and Gliciridia sepium (leaves) were used to identify the best insecticidal activity against the rice weevil by doing mortality tests for one week with four replications under laboratory conditions. Gliciridia sepium leaves showed the highest insecticidal activity (100 ± 0) after seven days, and its extract was fractionated by using column chromatography and yielded 12 fractions. A contact bioassay of each fraction was performed, and fraction-11 showed the highest insecticidal activity against Sitophilus oryzae with a 100 % mortality after four days. Fraction-11 was analyzed by using GC-MS and FT-IR. Results revealed that the major constituent identified in fraction-11 was 4-C-methyl-myo-inositol. Therefore, 4-C-methyl-myo-inositol acts as a natural insecticide against rice weevils.

A new acyl derivative of sulfadimethoxine inhibits phagocyte oxidative burst and ameliorates inflammation in a mice model of zymosan-induced generalised inflammation.

Chronic inflammation and oxidative stress play a pivotal role in the pathophysiology of most challenging illnesses, including cancer, Alzheimer's, cardiovascular and autoimmune diseases. The present study aimed to investigate the anti-inflammatory potential of a new sulfadimethoxine derivative N-(4-(N-(2,6-dimethoxypyrimidin-4-yl) sulfamoyl) phenyl) dodecanamide (MHH-II-32). The compound was characterised by applying 1H-, 13C-NMR, EI-MS and HRFAB-MS spectroscopic techniques. The compound inhibited zymosan-induced oxidative bursts from whole blood phagocytes and isolated polymorphonuclear cells with an IC50 value of (2.5 ± 0.4 and 3.4 ± 0.3 µg/mL), respectively. Furthermore, the inhibition of nitric oxide with an IC50 (3.6 ± 2.2 µg/mL) from lipopolysaccharide-induced J774.2 macrophages indicates its in vitro anti-inflammatory efficacy. The compound did not show toxicity towards normal fibroblast cells. The observational findings, gross anatomical analysis of visceral organs and serological tests revealed the non-toxicity of the compound at the highest tested intraperitoneal (IP) dose of 100 mg/kg in acute toxicological studies in Balb/c mice. The compound treatment (100 mg/kg) (SC) significantly (P < 0.001) downregulated the mRNA expression of inflammatory markers TNF-α, IL-1ß, IL-2, IL-13, and NF-κB, which were elevated in zymosan-induced generalised inflammation (IP) in Balb/c mice while upregulated the expression of anti-inflammatory cytokine IL-10, which was reduced in zymosan-treated mice. No suppressive effect was observed at the dose of 25 mg/kg. Ibuprofen was taken as a standard drug. The results revealed that the new acyl derivative of sulfadimethoxine has an immunomodulatory effect against generalised inflammatory response with non-toxicity both in vitro and in vivo, and has therapeutic potential for various chronic inflammatory illnesses.

Antibacterial activity of thymoquinone derivative.

Natural products such as terpenoidal compounds have been extremely tested against pathogenic bacteria. Researches are frequently carried out to find out new natural, semisynthetic and synthetic antibacterial agents due to problems of resistance. Thymoquinone derivative was obtained in our previous study and the current research is a continuation. The antibacterial activity of a monoterpenoid; thymoquinone derivative, 5-isopropyl-2-methyloxepine-1-one (1) has been evaluated for the first time by following the Agar cup bioassay method employed. The bacterial strains used in this study were Escherichia coli and Bacillus subtilis. Compound 1 showed moderate activity against Gram-positive organism; B. subtilis and good activity against Gram-negative species; E. coli with zones of inhibition (ZOI) 10.0 ± 0.2 mm and 11.0 ± 0.2 mm against E. coli and B. subtilis, respectively, and in comparison with antibiotic, imipenem. The zones of inhibition were calculated as the mean of the triplicate. The antibacterial activity of thymoquinone derivative 1 could be explained by the presence of unsaturated lactone.

Synthesis of 1,2,3,triazole modified analogues of hydrochlorothiazide via click chemistry approach and in-vitro α-glucosidase enzyme inhibition studies.

The current study was aimed to discover potent inhibitors of α-glucosidase enzyme. A 25 membered library of new 1,2,3-triazole derivatives of hydrochlorothiazide (1) (HCTZ, a diuretic drug also being used for the treatment of high blood pressure) was synthesized through click chemistry approach. The structures of all derivatives 2-26 were deduced by MS, IR, 1H-NMR, and 13C-NMR spectroscopic techniques. All the compounds were found to be new. Compounds 1-26 were evaluated for α-glucosidase enzyme inhibition activity. Among them, 18 compounds showed potent inhibitory activity against α-glucosidase with IC50 values between 24 and 379 µM. α-Glucosidase inhibitor drug acarbose (IC50 = 875.75 ± 2.08 µM) was used as the standard. Kinetics studies of compounds 6, 9, 11, 12, 15, 20, 23, and 24 revealed that only compound 15 as a mixed-type of inhibitor, while others were non-competitive inhibitors of α-glucosidase enzyme. All the compounds were found to be non-cytotoxic when checked against mouse fibroblast 3T3 cell line.

Allelopathic activity of some Sri Lankan seaweed extracts and the isolation of a new brominated nonaromatic isolaurene type sesquiterpene from red alga Laurencia heteroclada harvey.

This study investigated the allelopathic activity of sixteen seaweed extracts using lettuce seed germination bioassay. The results of the preliminary investigation suggested that the methanol extracts of seven seaweeds demonstrated significant properties inhibitory to seed germination. In addition, chemical investigation of an active extract of the alleopathic Laurencia heteroclada Harvey led to the isolation of four known compounds as well as a new brominated nonaromatic isolaurene type sesquiterpene. The structural elucidation of pure compounds was carried out using spectroscopic methods and by comparison with literature. As seaweeds are highly abundant around Sri Lanka, they could be developed as an ecofriendly natural herbicide in their crude form.

Synthesis of new Enrofloxacin Derivatives as Potential Antibiofilm Drugs Against Staphylococcus Aureus and Klebsiella Pneumoniae.

BACKGROUND: The antimicrobial resistance due to biofilm formation among bacteria is a significant problem in the healthcare and food industries. OBJECTIVE: The current study describes the synthesis of enrofloxacin derivatives 2-17, and the evaluation of their anti-bacterial and anti-biofilm activities. METHODS: Compounds 2-17 were synthesized through the acylation of enrofloxacin with thionyl chloride, followed by reaction with different aromatic amines. The new analogues identified among the sixteen compounds were 2-7, 11, 14, and 17. RESULTS: Compound 2 appeared to be effective against pathogens S. aureus as well as K. pneumonia, whereas, compound 11 was found active against K. pneumonia only. Compound 2 inhibited >75% biofilm formation of S. aureus at 20 µg/mL and K. pneumonia at 10 µg/mL concentrations. These doses are far below the bactericidal concentration of compound 2, suggesting the anti-virulence mechanism of these compounds. Compound 11 inhibited 60% biofilm formation of K. pneumoniae at 70 µg/mL concentration. Compound 5 inhibited the biofilm of K. pneumoniae at 62 µg/mL concentration but also had bactericidal properties at this concentration. Interestingly, compound 2 eradicated the preformed biofilm of both the pathogens at much lower doses as compared to control drug, gentamycin and substrate, enrofloxacin. Cytotoxicity of compounds 2-17 was checked by a standard method using 3T3 normal cell lines (mouse fibroblast), all compounds were found to be noncytotoxic. CONCLUSION: These compounds can be used alone or with FDA approved drugs to overcome biofilm related K. pneumoniae and S. aureus infections.

Sulphamethazine derivatives as immunomodulating agents: New therapeutic strategies for inflammatory diseases.

Sulfamethazine (SMZ) (1) is an antibacterial sulfa drug which suppresses the synthesis of dihydrofolic acid. It is used for the treatment of infections in livestock; such as gastrointestinal, and respiratory tract infections. During the current study, synthesis, characterization, and evaluation of immunomodulatory activities of derivatives of sulfamethazine (SMZ) (3-39) was carried out. These derivatives were synthesized by the reaction of sulfamethazine with a range of acid chlorides. All the compounds were characterized by using modern spectroscopic techniques, such as 1H-, and 13C-NMR, EI-MS, and HRFAB-MS. Compounds 3-10, 14, and 15 were identified as new compounds. Immunomodulatory effect of compounds 3-39 on different parameters of innate immune response was evaluated, including the production of Reactive Oxygen Species (ROS) from human whole blood and isolated polymorphonuclear neutrophils (PMNs), nitric oxide (NO), and pro-inflammatory cytokine TNF-α. All the new compounds, except 14 and 15, showed a significant anti-inflammatory activity. Compounds 3-39 were also evaluated for their anti-bacterial activity and cytotoxicity (3T3 mouse fibroblast cell lines). All the compounds were found to be non-cytotoxic against normal cell lines.