Abstract
Salicylate-rich plants are an attractive alternative to synthetic anti-inflammatory drugs due to a better safety profile and the advantage of complementary anti-inflammatory and antioxidant effects of the co-occurring non-salicylate phytochemicals. Here, the phytochemical value and biological effects in vitro and ex vivo of the stems of one of such plants, Gaultheria procumbens L., were evaluated. The best extrahent for effective recovery of the active stem molecules was established in comparative studies of five extracts. The UHPLC-PDA-ESI-MS3, HPLC-PDA, and UV-photometric assays revealed that the selected acetone extract (AE) accumulates a rich polyphenolic fraction (35 identified constituents; total content 427.2 mg/g dw), mainly flavanols (catechins and proanthocyanidins; 201.3 mg/g dw) and methyl salicylate glycosides (199.9 mg/g dw). The extract and its model components were effective cyclooxygenase-2, lipoxygenase, and hyaluronidase inhibitors; exhibited strong antioxidant capacity in six non-cellular in vitro models (AE and procyanidins); and also significantly and dose-dependently reduced the levels of reactive oxygen species (ROS), and the release of cytokines (IL-1β, IL-8, TNF-α) and proteinases (elastase-2, metalloproteinase-9) in human neutrophils stimulated ex vivo by lipopolysaccharide (LPS) and N-formyl-L-methionyl-L-leucyl-L-phenylalanine (fMLP). The cellular safety of AE was demonstrated by flow cytometry. The results support the application of the plant in traditional medicine and encourage the use of AE for development of new therapeutic agents.
Highlights
Gaultheria L. (Ericaceae) is a large plant genus of about 150 species distributed through the Americas, Asia and Australasia
Stems of Gaultheria procumbens L. were collected in October 2017 in the gardening center of Ericaceae plants, Gospodarstwo Szkolkarskie Jan Cieplucha (54 44 N, 19 18 E), Konstantynow Lodzki, Poland, where the plants grew in an open area
The suspension of neutrophils (940 μL; 3.5 × 105/mL) in an RPMI 1640 culture medium with 10% FBS, 10 mM N-(2-hydroxyethyl)piperazine-N -(2-ethanesulfonic acid) (HEPES), 1% Penicillin-Streptomycin, and 2 mM L-glutamine was pre-incubated in 96-well plates for 1 h at 37 ◦C with 5% CO2, with the presence or absence of the tested extracts (50 μL) at the final concentrations of 25–150 μg/mL
Summary
Gaultheria L. (Ericaceae) is a large plant genus of about 150 species distributed through the Americas, Asia and Australasia. The aerial parts (stems and leaves) of G. procumbens and other Gaultheria species, as well as methyl salicylate-rich essential oils distilled from the plants, are used (both externally and internally) in the treatment of disorders connected with inflammation, pain, and/or infection, including rheumatoid arthritis, influenza, the common cold, tracheitis, pharyngitis, pleurisy, fever, prostatitis, swelling and muscular pain, and some skin and periodontal problems [1,3,5]. According to our previous research, the leaf extracts of G. procumbens contain a variety of non-salicylate polyphenols (flavan-3-ols, A- and B-type procyanidins, flavonoids, and caffeoylquinic acids), which are strong antioxidants and exhibit relatively high inhibitory activity towards pro-inflammatory enzymes, lipoxygenase, and hyaluronidase [10,11]. Numerous procyanidin oligomers have been shown to significantly modulate the pro-inflammatory response of human immune cells (neutrophils) [13] and murine macrophages [14]
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