Ethanolic extract of Pyrus pashia buch ham ex. D. Don (Kainth): A bioaccessible source of polyphenols with anti-inflammatory activity in vitro and in vivo.

ETHNOPHARMACOLOGICAL RELEVANCE: Pyrus pashia Buch ham ex. D. Don (Kainth) fruit from the Himalayan region is traditionally consumed by native people in the form of decoctions for various clinical conditions including inflammatory diseases. However, scientific studies on the biofunctional properties of Kainth fruits are still scarce. AIM OF THE STUDY: The study is aimed to investigate the anti-inflammatory effects of Kainth fruit extracts using in vitro and in vivo inflammation models. MATERIAL AND METHODS: Free, esterified and bound fractions from the Kainth ethanolic extracts were prepared for determining the anti-inflammatory effect. The levels of 5-LOX and COX-2 were determined in vitro. The protein levels of cytokines (IL-6, TNF-α & IL-10) were quantitated by ELISA method in lipopolysaccharide-stimulated RAW macrophages. Also, the anti-inflammatory potential of the Kainth fruit extracts was determined using the carrageenan-induced mice paw edema model. The bioaccessibility of Kainth fruit extracts was measured using a simulated in vitro digestion system (salivary, gastric and intestinal). RESULTS: The Kainth fruit extracts were partially purified to yield free, esterified and bound phenolics. Free and bound phenolics of Kainth fruits inhibited 5-Lipoxygenase, Cyclooxygenase-2 activities and pro-inflammatory cytokines (Interleukin-6 and tumour necrosis factor-α) expression in vitro. Also, oral administration of these extracts to the carrageenan-injected mice showed an anti-inflammatory effect by decreasing the pro-inflammatory cytokines and reducing the cellular infiltration in paw tissues. Also, both the extracts showed better bioavailability and bioaccessibility in in vitro and in vivo studies. CONCLUSIONS: The results indicated that free and bound phenolics from Kainth fruits that are rich in catechin, epicatechin, arbutin and chlorogenic acid exhibited anti-inflammatory effects and could potentially be used to treat inflammatory diseases.

Characterization, quantification of free, esterified and bound phenolics in Kainth (Pyrus pashia Buch.-Ham. Ex D.Don) fruit pulp by UPLC-ESI-HRMS/MS and evaluation of their antioxidant activity.

UPLC-ESI-HRMS/MS was used to identify the free, esterified and bound phenolic compounds in Kainth fruit extracts. In total, around 17, 15 and 18 free, esterified and bound phenolic compounds respectively were identified. Among these, Procyanidin B2, Epicatechin, Phloridzin, Hesperetin, etc. are being reported for the first time. The total phenolic content of free, esterified and bound fractions were 178.33 ±â€¯6.90, 151.33 ±â€¯7.73 and 707.16 ±â€¯19.77 mg GAE/100 g of fruit. The major phenolic compounds quantified were chlorogenic acid (7.97 mg/100 g), arbutin (7.05 mg/100 g) and catechin (44.56 mg/100 g) in free, esterified and bound form respectively. Various antioxidant assays (DPPH, ABTS, TAC and FRAP) were performed for all the extracts. Among different extracts, the bound phenolics exhibited the highest antioxidant activity. Systematic identification and quantitative profiling of phenolics in Kainth fruit being presented for the first time would help in utilising this fruit for designing functional food formulations.