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Purpose: To formulate Cannabis sativa-based syrup and investigate its anti-inflammatory potential and the stability of the formulation under stress conditions. Methods: The syrup was prepared using different combinations of crude C. sativa resin, propylene glycol, aspartame, sucrose, sodium metabisulphite (SMBs) and ethylenediaminetetraacetic acid (EDTA). The stability of the formulations was determined under accelerated temperature conditions. The anti-inflammatory activity of the resin and different formulations were evaluated by the egg albumin induced paw edema model in rats. Biochemical assay was determined by Reitman and Frankel colorimetric assay method while hematological assay was evaluated by standard protocols. Results: EDTA-containing syrup (CE) was the most stable with estimated shelf-life of 2204 days (K25ºC, 4.78 x 10-5/day). Higher propylene glycol levels significantly improved anti-inflammatory activity compared to those containing a lower amount. All the formulations showed anti-inflammatory activity higher than the crude resin with a dose-dependent inhibition of paw edema compared with the control. There was no significant difference (p < 0.05) between the serum glutamate-oxaloacetate transaminase (SGOT, 13.821 ± 0.190 - 16.008 ± 1.012), serum glutamate-pyruvate transaminase (SGPT, 19.241 ± 1.027 - 22.901 ± 1.093) and urea (9.812 ± 0.252 - 10.054 ± 0.252) levels of the treated and 16.856 ± 1.053, 24.960 ± 0.101 and 10.654 ± 0.925 units/L of the control animals respectively. With the exception of eosinophil that disappeared from the blood in the third week, all the hematological parameters showed a gradual increase in lymphocytes, neutrophils, monocytes, packed cell volume (PCV), white and red blood cell counts in the third week compared to control. Conclusion: Formulation of C. sativa as syrup using efficient carriers improves the pharmacological activity of the crude extract. SMBs and EDTA significantly enhance the stability of the syrup with no observable biochemical and hematological changes in treated animals [ABSTRACT FROM AUTHOR]

Twelve new derivatives of benzothiazole bearing benzenesulphonamide and carboxamide were synthesised and investigated for their in vivo anti-inflammatory, analgesic and ulcerogenic activities. Molecular docking showed an excellent binding interaction of the synthesised compounds with the receptors, with 17c showing the highest binding energy (-12.50 kcal/mol). Compounds 17c and 17i inhibited carrageenan-induced rat paw oedema at 72, 76, and 80% and 64, 73, and 78% at 1 h, 2 h, and 3 h, respectively. In the analgesic activity experiment, compounds 17c, 17 g, and 17i had ED50 (µM/kg) of 96, 127, and 84 after 0.5 h; 102, 134, and 72 after 1 h and 89, 156, and 69 µM/kg after 2 h, respectively, which were comparable with 156, 72, and 70 µM/kg for celecoxib. The ulcerogenic index of the most active derivatives 17c and 17i were 0.82 and 0.89, respectively, comparable to 0.92 for celecoxib. The physicochemical studies of the new derivatives showed that they will not have oral bioavailability problems. [ABSTRACT FROM AUTHOR]

Purpose: To evaluate the in vitro anti-oxidant and anti-inflammatory potential of the most potent and abundant metabolite, 3-methoxy quercetin (3-MQ), from extract fractions of mistletoe, Loranthus micranthus Linn (Loranthaceae) parasitic on Kola acuminata Schott & Endl, (Malvaceae), also known as Garcinia kola Heckel, (Clusiaceae). Methods: Compounds isolated through a combination of chromatographic techniques were screened for in vitro antioxidant potential using the diphenyl picrazyl hydrazine (DPPH) radical-based model. Cell viability at 1-1000 μM 3-MQ in 24 h was evaluated by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) test. Lipopolysaccharide (LPS), phorbol 12-myristate 13-acetate (n = 5) five (5) replicates. Results: Ten (10) known compounds including 3-MQ (1) were isolated and characterized. 3-MQ exhibited highly significant (p < 0.05) antioxidant activity with 50 % inhibitory concentration (IC50) of 15.0 μM; concentrations ≤100 μM did not exert cytotoxic effect. 3-MQ, at 25 and 125 μM concentrations, significantly (p < 0.05) inhibited the production of TNF-a by 82 and 100 %, respectively, compared to controls. Conclusion: The results demonstrate the potent anti-inflammatory activity of 3-MQ and suggests its use as a potential alternative therapy for inflammation and related diseases. [ABSTRACT FROM AUTHOR]

• Inflammatory disease are prevalent worldwide and can be life threatening. • The need to develop newer anti-inflammatory agents is eminent. • Carboxamides and sulphonamides are antioxidant, antimicrobial anti-inflammatory agents. • The novel compounds are good antioxidant, antimicrobial and anti-inflammatory agents. Ten new derivatives of benzenesulphonamide bearing carboxamide functionality were synthesized and investigated for their in vitro antimicrobial, antioxidant and in vivo anti-inflammatory activities. Compound 9d inhibited carrageenan induced rat-paw oedema at 93.81, 88.79 and 86.09% at 1 h, 2 h and 3 h administration respectively. In the antimicrobial activity, compound 9a (6.54, 6.69 and 6.64 mg/mL) was most potent against S. aureus , B. subtilis and C. albicans respectively, compound 9e (6.45 and 6.46 mg/mL) was most active against P. aeruginosa and A. niger respectively while compound 9i (6.24 mg/mL) was most active against E. coli. Only compound 9a (IC 50 0.3052 mg/mL) had comparable activity with Vitamin C (IC 50 0.2090 mg/mL) in the antioxidant assay. [ABSTRACT FROM AUTHOR]