ABSTRACT
Abstract Lepechinia mutica (Benth.) Epling, Lamiaceae, and Vallea stipularis L.f., Elaeocarpaceae, are the object of the present study. These plants are endemic to the Andean region and have attracted our attention on the basis of interesting results obtained in a preliminary anticholinesterase screening. Actually, carnosol and tiliroside, isolated from L. mutica and V. stipularis, respectively, have shown a promising selective inhibitory activity against butyrylcholinesterase. Specifically, the anti-butyrylcholinesterase activity of carnosol was 5.15 µM and that of tiliroside was 52.9 µM, compared to 8.568 ± 0.570 µM of the positive control Donepezil. Carnosol and tiliroside were purified chromatographically from the ethyl acetate extract of L. mutica and V. stipularis, respectively. Spectrophotometric methods were used for enzymatic studies.
ABSTRACT
Objective To establish an HPLC-DAD method for simultaneous determination of main anti-oxidant constituents in leaves and stem of Rosmarinus officinalis. Methods The separation was performed on an Agilent Zorbax SB-Aq C18 column(250 mm × 4.6 mm,5 μm), using methanol (A) and potassium dihydrogen phosphate solution (B) (pH 3.0) as the mobile phase at the flow rate of 1.0 mL/min for a gradient elution. The detection wavelength was set at 328 nm for the detection of chlorogenic acid, caffeic acid, rosmarinic acid, luteolin, apigenin, and genkwanin, and 284 nm for the detection of paeonol, rosmanol, hesperetin, carnosol, and carnosic acid. Column temperature was set at 30 ℃, and the volume of sample injection was 10 μL. Results The linear range was 2.02-64.64 μm/mL for chlorogenic acid, 1.74-55.68 μmol/mL for caffeic acid, 2.76-88.32 μmol/mL for rosmarinic acid, 0.24-7.68 μmol/mL for paeonol, 0.46-14.72 μmol/mL for rosmanol, 0.22-7.04 μmol/mL for hesperetin, 0.72-23.04 μmol/mL for luteolin, 3.74-119.68 μmol/mL for apigenin, 5.1-163.28 μmol/mL for carnosol, 0.4-12.8 μmol/mL for genkwanin, and 5.22-167.04 μmol/mL for carnosic acid. The average recoveries of the 11 constituents were from 98.1%-100.5%, and the RSD values were 0.67%-2.14%. Conclusion The method is simple and accurate,which can be used for quality and quantity analysis of the main anti-oxidant constituents in leaves and stem of R. officinalis.
ABSTRACT
Carnosol is a phenolic antioxidant present in rosemary (Rosmarinus officinalis). It is known for anti-inflammatory effects, analgesic activity and anti-cancer effects. However, no study has been dedicated yet to its effect on atopic dermatitis (AD). Here, we show that carnosol effectively inhibited LPS-induced nitric oxide (NO) generation and expression of inflammatory marker proteins (iNOS and COX-2) in RAW 264.7 cells. In addition, carnosol effectively inhibits the phosphorylation of STAT3 and DNA binding activity in RAW 264.7 cells. Pull down assay and docking model analysis showed that carnosol directly binds to the DNA binding domain (DBD) of STAT3. We next examined the anti-atopic activity of carnosol (0.05 μg/cm²) using 5% Phthalic anhydride (PA)-induced AD model in HR1 mice. Carnosol treatment significantly reduced 5% PA-induced AD like skin inflammation in skin tissues compared with control mice. Moreover, carnosol treatment inhibits the expression of iNOS and COX-2 in skin tissue. In addition, the levels of TNF-α, IL-1β, and Immunoglobulin-E in blood serum was significantly decreased in carnosol treated mice compared with those of 5% PA treated group. Furthermore, the activation of STAT3 in skin tissue was decreased in carnosol treated mice compared with control mice. In conclusion, these findings suggest that carnosol exhibited a potential anti-AD activity by inhibiting pro-inflammatory mediators through suppression of STAT3 activation via direct binding to DBD of STAT3.