RESUMO
In the present work we carried out a phytochemical and biological investigation on three endemic Hypericum species, i.e.Hypericum thymbrifolium (H. thymbrifolium), Hypericum spectabile (H. spectabile) and Hypericum pseudolaeve (H. pseudolaeve) from Anatolia in order to discover new sources of natural compounds for the treatment of inflammatory and neurodegenerative disorders. HPLC-DAD analysis indicated that two naphthodianthrones (pseudohypericin and hypericin) together with chlorogenic acid, rutin, hyperoside, isoquercitrin, kaempferol, quercitrin, quercetin, amentoflavone, and hyperforin are the main compounds present in the methanol extracts. After chemical characterization, all extracts were in-vitro biologically assayed for antioxidant potential by lipid peroxidation inhibitory activity, DPPH, FRAP assays, and superoxide radical scavenging activity, for AChE inhibitory activity by Ellman's method, for COX inhibitory activity by using enzyme immunoassay (EIA) kit, for cytotoxic activity on HeLa and NRK-52E cell lines by MTT assay. The superoxide radical scavenging activity and lipid peroxidation inhibitory activity of H. spectabile (EC50 = 0.430 mg/mL) were more remarkable than that of H. thymbrifolium and H. pseudolaeve. The extracts showed moderate inhibitory activity on AChE (from 49.37% to 63.41%). The best inhibitory activity against COX-1 (71.77% and 77.04%, respectively) and COX-2 ( 64.14% and 72.23%, respectively) were shown by H. thymbrifolium and H. spectabile, which may be due to their richest chlorogenic acid content (0.29576% and 0.23567%, respectively). Cytotoxicity screening results showed that the extracts did not demonstrate significant cytotoxic activity. It was concluded that the most promising extract with antioxidant, anti-inflammatory, and AChE inhibition potential is H. spectabile.
RESUMO
OBJECTIVE: To evaluate the methanolic extracts of aerial parts of Hypericum scabroides (HSM) (200 mg/kg, p.o.) for in vivo anti-inflammatory activity. METHODS: The anti-inflammatory activity of HSM was tested in mice weighting (25±5) g. Either vehicle (control group), the methanolic extracts (200 mg/kg) or diclofenac (50 mg/kg), was administered (p.o.) for 60 min before an edema was induced in the mice paw by subcutaneous injection of carrageenin. The mouse-paw volume was measured 1 h, 3h and 6 h after injection of carrageenin. RESULTS: The HSM showed significant reduction of edema in carrageenan induced mice paw edema model at 1 h and 3 h for (78.03±15.54)% and (40.44±16.36)%, respectively. The diclofenac 50 mg/kg exhibited % reduction in paw volume (31.00±11.52)%, (0.80±0.09)% and (9.39±1.99)% after 1 h, 3 h and 6 h, respectively compared to control group. The obtained results revealed that HSM has significant anti inflammatory activity. Furethermore, the chemical composition of HSM was analyzed by using high performance liquid chromatography-diode array dedector. The plant contained pseudohypericin (trace) hypericin (trace), chlorogenic acid (0.014 0±0.000 5)%, rutin (0.005 0±0.000 6)%, hyperoside (0.016±0.005)%, isoquercitrin (0.034 0±0.000 5)% and kaempferol (trace). CONCLUSIONS: The obtained results of the present investigation revealed that methanol extract of Hypericum scarbroides has significant anti-inflammatory activity.
