Abstract

Here we report the comprehensive characterization of the secondary metabolites from the leaves of Colebrookea oppositifolia Smith, a species used as medicinal plant in the traditional medicine of Nepal. Phytochemical screening of bioactives was performed using an integrated LC-MSn and high resolution MS (Mass Spectrometry) approach. Forty-three compounds were tentatively identified, mainly aglyconic and glycosilated flavonoids and phenolic acids, as well as other bioactives such as coumarins and terpenes were detected. Furthermore, the NF-κB and AP-1 inhibitory activity of C. oppositifolia extract were evaluated, as well as its cytotoxicity against THP-1 cells, in order to assess the potential use of this herb as a source of anti-inflammatory and cytotoxic compounds. The results so far obtained indicate that C. oppositifolia leaves extract could significantly reduce the viability of THP-1 cells (IC50 = 6.2 ± 1.2 µg/mL), as well as the activation of both NF-κB and AP-1 at the concentration of 2 μg/mL. Our results indicate that Nepalese C. oppositifolia is a valuable source of anti-inflammatory and cytotoxic compounds. The phytochemical composition reported here can partially justify the traditional uses of C. oppositifolia in Nepal, especially in the treatment of inflammatory diseases, although further research will be needed to assess the full potential of this species.

Highlights

  • Colebrookea oppositifolia Smith is the only species of the Colebrookea genus (Lamiaceae)

  • Here we report the comprehensive characterization of the secondary metabolites from the leaves of Colebrookea oppositifolia Smith, a species used as medicinal plant in the traditional medicine of Nepal

  • The phytochemical composition reported here can partially justify the traditional uses of C. oppositifolia in Nepal, especially in the treatment of inflammatory diseases, further research will be needed to assess the full potential of this species

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Summary

Introduction

Colebrookea oppositifolia Smith is the only species of the Colebrookea genus (Lamiaceae). To the best of our knowledge, the phytochemical composition of this plant remains scarcely explored, and the majority of these bioactivities have not been attributed to specific compounds yet Flavonoids such as apigenin, alnustin, mosloflavone [12], and flavonoid glycosides such as negletein-6-O-β-d-glucopyranoside and 5,7,2 -trihydroxyflavone-2 -O-β-d-glucopyranoside [7] have been identified in the aerial parts, together with the terpenes phytol [1] and (+)-14,15-dinor-9α-hydroxy-cis-labd-11(E)-en-13-one [12]. Due to the importance of this medicinal plant in Nepal and due to the relatively scarce literature regarding its phytochemical composition and its biological activities, we selected C. oppositifolia to proceed with our studies on the valorization of Nepalese medicinal herbs [15,16,17]. In vitro biological activity of the same extract was evaluated, and results from anti-NF-κB (Nuclear factor-κB), anti-AP-1 (Activator protein-1), and cytotoxicity assays on human cells are here presented

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