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Abstract
Sideritis congesta is a plant native to Mediterranean countries. Infusions of this plant are used to treat various diseases. The anti-inflammatory potential of Sideritis species is widely known. However, the anti-inflammatory potential of an aqueous extract of S. congesta has not been investigated yet. In this study, the phytochemical composition and anti-inflammatory potential of different fractions of an aqueous extract from S. congesta using bioactivity guided fractionation via centrifugal partition chromatography (CPC) were determined. A CPC single-step isolation of a flavonoid stachyspinoside 1 from S. congesta is reported. In addition, a CPC fractionation protocol of the crude aqueous extract was developed. Three aqueous fractions (I, II, and III) of S. congesta were obtained, and their anti-inflammatory potential was evaluated with respect to their ability to inhibit the activity of COX-2 and NF-κB in vitro. Fraction I showed the highest COX-2 inhibition activity (92.3% inhibition at 0.1%). Fraction III showed the highest NF-κB inhibition activity (99.9% at 0.1%) among the CPC produced fractions. The structures of 3 compounds of fraction III could be identified and were validated by HPLC-PDA, HRMS, and NMR spectroscopy. Finally, the phenol, saponin, and flavonoid contents were quantified in the most potent CPC fractions (I and III).
Highlights
Sideritis species belongs to the Lamiaceae family and comprises over 150 species spread in the Western Palearctic zone [1]
Under the genus Sideritis, this study focuses on the plant S. congesta, since among infusions from 7 Sideritis species, the richest infusion in terms of the total phenol and total flavonoid contents belongs to S. congesta [11]
An instrumental analysis (HPLC) of the obtained extract is shown in Figure 3. e use of an internal standard resulted in the determination of the mass fraction of stachyspinoside 1 (61.1%). e presence of the flavonoid stachyspinoside 1 in S. congesta was first reported in 2020 [29]
Summary
Sideritis species belongs to the Lamiaceae family and comprises over 150 species spread in the Western Palearctic zone [1]. The antioxidant and anti-inflammatory activities of different extracts from several Sideritis species have been reported [6,7,8]. Ese activities have been ascribed to the flavonoids, diterpenoids [9], and phenylethanoids isolated from the Sideritis species [10]. Under the genus Sideritis, this study focuses on the plant S. congesta, since among infusions from 7 Sideritis species, the richest infusion in terms of the total phenol and total flavonoid contents belongs to S. congesta [11]. A study of the evaluation of an ethanolic S. congesta extract for anti-inflammatory activity showed no significant results [12]. E presence of entkaurane diterpenoids [9, 13], flavonoids [6, 14], and essential oils [15, 16] in aerial parts of S. congesta has been described A study of the evaluation of an ethanolic S. congesta extract for anti-inflammatory activity showed no significant results [12]. e presence of entkaurane diterpenoids [9, 13], flavonoids [6, 14], and essential oils [15, 16] in aerial parts of S. congesta has been described
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