Highlights
Leaves of
Raphanus sativus var. Longipinnatus
is often ignored in southern part of India and utilized as livestock feed.
Solid waste management of leaves of
Raphanus sativus var. Longipinnatus
for lung cancer treatment.
Synthesized ZnO NPs using
Raphanus sativus var. Longipinnatus
leaves extract proved to have cytotoxicity against A549 cell lines.
Synthesized ZnO NPs using
Raphanus sativus var. Longipinnatus
leaves extract proved to have cytotoxicity against A549 cell lines.
BackgroundDrugs that inhibit cyclooxygenase-2 (COX-2) while sparing cyclooxygenase-1 (COX-1) represent a new attractive therapeutic development and offer new perspective for further use of COX-2 inhibitors. Intention of this work is to develop safer, selective COX-2 inhibitors that do not produce harmful effects.ResultsA series of 55 tyrosine derivatives were designed for evaluation as selective COX-2 inhibitors and investigated by in silico for their anti-inflammatory activities using C-Docker. The results of docking study showed that 35 molecules were found to selectively inhibit the enzyme COX-2. These molecules formed stable π hydrophobic and additional van der Waals interactions in the active site side pocket of COX-2. The molecules selected from docking studies were examined through ADMET descriptors and Osiris property explorer to find its safety profile as well. The tyrosine derivatives containing toxic fragments were eliminated.ConclusionThe results conclude that out of 55, 19 molecules possessed best binding energy (< −3.333 kcal/mol) and these molecules had more selective and safer COX-2 inhibitor profile compared to the standard celecoxib.Graphical abstract3-D structural interactions of COX-2 inhibiting tyrosine derivatives.
The objective of this study was to isolate a new compound from methanol extracts of Indigofera aspalathoides Vahl ex DC. aerial parts and to determine the immunomodulatory activity of the isolated compound. The methanolic extract yielded compounds 1 (0.65 mg), 2 (0.52 mg), and 3 (1.80 g) on chromatography, which was characterized using spectral techniques, namely Fourier transform infrared, 1 H nuclear magnetic resonance, 13 C nuclear magnetic resonance, and mass spectroscopy. Owing to the paucity of compounds 1 and 2, kaempferol 5-O-b-Dglucopyranoside (compound 3) was evaluated for immunomodulatory activity. Compound 3 was assessed in a neutrophil adhesion and a delayed-type hypersensitivity test, and humoral antibody titers were measured in albino rats. Administration of compound 3 at oral doses of 10, 20, 50, and 100 mg/kg of body weight resulted in a significant (p \ 0.05) increase in percent neutrophil adhesion to nylon fibers, a dose-dependent increase in antibody titers, and potentiation of the delayed-type hypersensitivity reaction induced using sheep red blood cells. We concluded that compound 3, methanol extracted from aerial parts of I. aspalathoides Vahl ex DC. possessed significant immunomodulatory activity and therefore has promising therapeutic potential for the prevention of autoimmune diseases.
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