Abstract
Several species of the genus
Cistus
(Cistaceae) have been reported to exhibit a variety of pharmacological activities including anti-inflammatory and anti-viral potential [1].
In vitro
pharmacological activities of
Cistus
extracts were previously shown to be in strong correlation with the samples' total phenol content [2]. In order to obtain an extract enriched in phenolic compounds, a new ethanolic-water extract containing 60% polyphenols was developed (Patent application, Finzelberg GmbH & Co. KG). This extract ECce60 was further investigated for
in vitro
anti-inflammatory activity focusing on NF-κB inhibition in the luciferase-reporter gene assay [2] and for radical scavenging capacity (DPPH-TLC). The extract fractionation resulted in the separation of polyphenolic and terpenoid constituents and overall 7 fractions were obtained and characterized using 1D and 2D TLC techniques, HPLC as well as NMR. Fraction 5 demonstrated considerable anti-inflammatory effect (IC50 59.2µg/ml) which was stronger than that of the ECce60 (IC50: 77.5µg/ml). This fraction 5 represents only 2,1% of the ECce60 extract and contains relatively 1.4% Catechin, 0.7% Epigallocatechin and 3.9% of flavonoids. No terpenoids were detected in the active fraction. Other factions were inactive up to a concentration of 100µg/ml. Consequently, fractionation led to enrichment of active constituents in the sample. All the samples exhibited antioxidant potential and fractions 4, 5 and 6 are considered to be good candidates for isolation of individual actives. Overall, this study provides further
in vitro
evidence for the potential anti-inflammatory effects of
Cistus
-derived extracts and especially of ECce60.
References:
[1] Pomponio, R. et al. (2003)J. Chromatogr. A 990:215–223
[2] Taila, S. et al. (2008)J. Pharm. Pharmacol. 60:A62-A63.
[3] Obolskiy, D. (2008) Phytochemical and
in vitro
NF-kappa B inhibitory/Antioxidant Profiling of
Cistus creticus
L. subsp.
eriocephalus
(Viv.) Greuter Burdet; MSc dissertation, The School of Pharmacy, University of London.
[4] Bremner, P. et al. (2004) Planta Med. 70:914–918.