Sesuvium sesuvioides (Fenzl) Verdc (Aizoaceae) has been traditionally used in the treatment of inflammation, arthritis, and gout. However, its antiarthritic potential has not been evaluated scientifically. The current study was designed to assess the antiarthritic properties of the n-butanol fraction of S. sesuvioides (SsBu) by phytochemical analysis, in vitro and in vivo pharmacological activities, and in silico studies. Phytochemical analysis showed total phenolic contents (90.7 ± 3.02 mg GAE/g) and total flavonoid contents (23.7 ± 0.69 mg RE/g), and further analysis by GC-MS identified possible bioactive phytocompounds belonging to phenols, flavonoids, steroids, and fatty acids. The in vitro antioxidant potential of SsBu was assessed by DPPH (175.5 ± 7.35 mg TE/g), ABTS (391.6 ± 17.1 mg TE/g), FRAP (418.2 ± 10.8 mg TE/g), CUPRAC (884.8 ± 7.97 mg TE/g), phosphomolybdenum (5.7 ± 0.33 mmol TE/g), and metal chelating activity (9.04 ± 0.58 mg EDTAE/g). Moreover, in the in vitro studies, inhibition (%) of egg albumin and bovine serum albumin denaturation assays showed that the anti-inflammatory effect of SsBu at the dose of 800 μg/ml was comparable to that of diclofenac sodium used as a standard drug. The in vivo antiarthritic activity was assessed to determine the curative impact of SsBu against formalin-induced (dose-dependent significant (p < 0.05) effect 72.2% inhibition at 750 mg/kg compared to standard; 69.1% inhibition) and complete Freund’s adjuvant-induced arthritis (40.8%; inhibition compared to standard, 42.3%). SsBu significantly controlled PGE-2 level compared to the control group (p < 0.001) and restored the hematological parameters in rheumatoid arthritis. Treatment with SsBu significantly reduced oxidative stress by reinstating superoxide dismutase, GSH, and malondialdehyde along with pro-inflammatory markers (IL-6 and TNF-α) in arthritic rats. Molecular docking revealed the antiarthritic role of major identified compounds. Kaempferol-3-rutinoside was found to be more potent for COX-1 (−9.2 kcal/mol) and COX-2 inhibition (−9.9 kcal/mol) than diclofenac sodium (COX-1, −8.0 and COX-2, −6.5 kcal/mol). Out of the 12 docked compounds, two for COX-1 and seven for COX-2 inhibition showed more potent binding than the standard drug. The results from the in vitro, in vivo, and in silico approaches finally concluded that the n-butanol fraction of S. sesuvioides had antioxidant and antiarthritic potential, which may be due to the presence of potential bioactive compounds.
Objective: Nowadays antibacterial drugs resistance is major problem in the world. To overcome this problem, some novel derivates of doxycycline were synthesized by single step condensation reaction with ten different types of aromatic and aliphatic aldehydes and ketones in ethanol as solvent and acetic acid as catalyst. In these reactions, deprotonation of primary amine occurs that results in formation of imine. Methods: All the derivatives physically characterized and confirmed by analytical techniques i.e. FTIR and 1H NMR and 13C NMR. The derived compounds have exhibited significantly more active against both gram positive as well as gram negative bacterial strains as compared to parent drug. Results: Derived Schiff bases RDC2, RDC4 and RDC10 showed zone of inhibition against Bacillus subtilis as compared to doxycycline and derived Schiff bases RDC1, RDC2, RDC5, RDC6, RDC7 and RDC8 showed more zone of inhibition against Micrococcus luteus as compared to doxycycline. Yield (75%), m.p. 180-185°C, Mol. Wt. 1063, Elemental Analysis: (Calculated) for C58H54N4O16: iC, 65.53; H, 5.12; N, 5.27; (Found): C, 65.49; H, 5.18; N, 5.37; FTIR (ν, cm‐1): 3066 (=C-H), 1665(C=N), 1585, 1490(C=C, phenyl), 3650(OH), 1692 (C=O); 1H NMR (DMSO−d6, δ, ppm), 6.02-6.03 d, 6.91-6.92 d, (=CH-); 6.88-6.89 t (=CH), 2.89-2.90 d, (-CH); 1.07-1.08 q, (-CH3), 3.38-3.39 d; 3.17-3.18 d, (CH), 1.47-1.48 t (CH), 1.48 s, (CH3), 6.96-6.97d, 7.577-7.588 d, (-CH=) 15.21 s (OH); 4.62 s (OH); 1.46-1.47 s (OH); 13C NMR (DMSO−d6, δ, ppm). Conclusion: Doxycycline is among broad-spectrum tetracycline. The Schiff bases derived from doxycycline show significantly highly active against gram negative bacteria as compared to doxycycline. In future further study on these derived compounds will help in market new derivative of doxycycline, which will have more broad-spectrum activity than doxycycline.
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