Synthesis and biological evaluation of some novel furan derivatives

The present work involved cyclization of Schiff bases to azetidine-2-one and thiazolidine 4-one derivatives. The schiff bases [IIIa-j] were obtained upon reaction between electrophillic carbon atom of furfuraldehyde and nucleophillic nitrogen atom of amines. Azetidine-2-one derivatives [IVa-j] were obtained by reaction between imines and monochloro acetyl chloride in the presence of triethyl amine and 1, 4 dioxan. On the other hand, preparations of thiazolidine-4-ones [Va-j] were preceded by nucleophilic attack of sulphur of thioglycolic acid on imine carbon followed by intramolecular cyclization in the presence of SnCl[2]. The structures of the compounds were confirmed by spectral and elemental analysis. The biological evaluation of the compounds like anti-microbial, antioxidant, analgesic, CNS depressant and anti-diabetic activity were determined. From the pharmacological investigation it was found that out of all the compounds IVa, IVb, IVe, IVf, IVh,Va, Vb, Ve, Vf, Vh had shown more potent activity

Total phenolic, total flavonoid content, and antioxidant capacity of the leaves of Meyna spinosa Roxb., an Indian medicinal plant / 中国天然药物

AIM@#The objective of the present study was to determine the total phenolic and total flavonoid contents, and to evaluate the antioxidant potential of different leaf extracts of Meyna spinosa Roxb. ex Link, a traditional medicinal plant of India.@*METHODS@#Free radical scavenging and antioxidant potential of the methanol, ethyl acetate, and petroleum ether extracts of Meyna spinosa leaves were investigated using several in vitro and ex vivo assays, including the 2, 2-diphenyl-picrylhydrazyl radical scavenging, superoxide anion scavenging, hydroxyl radical scavenging, nitric oxide radical scavenging, hydrogen peroxide scavenging activity, metal chelating assay, and reducing power ability method. Total antioxidant activity of the extracts was estimated by the ferric thiocyanate method. Inhibition assay of lipid peroxidation and oxidative hemolysis were also performed to confirm the protective effect of the extracts. Total phenolic and total flavonoid contents of the extracts were estimated using standard chemical assay procedures.@*RESULTS@#Methanol extracts showed the highest polyphenolic content and possessed the better antioxidant activity than the other two extracts. Total phenolic and total flavonoid contents in the methanol extract were (90.08 ± 0.44) mg gallic acid equivalents/g and (58.50 ± 0.09) mg quercetin equivalents/g, respectively. The IC50 of the methanol extract in the DPPH(·), superoxide anion, hydroxyl radical, nitric oxide radical, hydrogen peroxide scavenging activity and metal chelating assays were (16.4 ± 0.41), (35.9 ± 0.19), (24.1 ± 0.33), (23.7 ± 0.09), (126.8 ± 2.92), and (117.2 ± 1.01) μg·mL(-1), respectively. The methanol extract showed potent reducing power ability, total antioxidant activity, and significantly inhibit lipid peroxidation and oxidative hemolysis which was similar to that of standards.@*CONCLUSION@#The results indicated a direct correlation between the antioxidant activity and the polyphenolic content of the extracts, which may the foremost contributors to the antioxidant activity of the plant. The present study confirmed that the methanol extract of Meyna spinosa leaves is a potential source of natural antioxidants.

Antiinflammatory, antinociceptive and antioxidant activities of Phyllanthus acidus L. extracts

Objective: To evaluate analgesic, anti-inflammatory and in vitro antioxidant potential and determine total phenolic, total flavonoid content of leaves extracts of Phyllanthus acidus, a folk medicinal plant of India. Methods: Anti-inflammatory activity was evaluated using carrageenan induced paw oedema, cotton pellet induced granuloma, membrane stabilizing activity method. Analgesic activity of the extracts was estimated against acetic acid induced writhing, tail immersion method, formalin test. Free radical scavenging and antioxidant potential of the extracts of Phyllanthus acidus leaves was performed using several in vitro and ex vivo assay models. Total phenolic and total flavonoid contents of the extracts were determined using standard chemical methods. Results: The extracts exhibited significant anti-inflammatory and analgesic activities at dose dependent manner. Methanol extract at a dose of 500 mg/kg showed superior activity which was comparable with the standard drugs. Ethyl acetate extract showed moderate activity while petroleum ether extract showed least activity. Total phenolic and total flavonoid content in methanol extract were 73.08±0.682 mg GAE/g and 61.28±0.062 mg QE/g respectively. The extracts possess significant antioxidant activity, methanol extract showed highest IC50 value. The contents of flavonoids and phenolic compounds could be correlated with the antioxidant, analgesic and anti-inflammatory activities observed for Phyllanthus acidus leaves. Conclusion:Our findings suggest that Phyllanthus acidus contains potential antioxidant, analgesic and anti-inflammatory compounds which could be tested as drug candidates against oxidative stress, pain and inflammation related pathological diseases.