梨果皮乙醇提取物（Kainth）：一种具有生物利用度的多酚来源，具有体外和体内抗炎活性。
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.
机构信息
Department of Fruit and Vegetable Technology, CSIR-Central Food Technological Research Institute, Mysuru, Karnataka, 570020, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, Uttar Pradesh, 201002, India.
Department of Molecular Nutrition, CSIR-Central Food Technological Research Institute, Mysuru, Karnataka, 570020, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, Uttar Pradesh, 201002, India.
出版信息
J Ethnopharmacol. 2022 Jan 10;282:114628. doi: 10.1016/j.jep.2021.114628. Epub 2021 Sep 11.
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.
民族药理学相关性
喜马拉雅地区的梨果木（Pyrus pashia Buch ham ex. D. Don（Kainth）果实），其传统用法为药汤，用于治疗各种临床病症，包括炎症性疾病。然而，关于 Kainth 果实生物功能特性的科学研究仍然很少。
研究目的
本研究旨在通过体外和体内炎症模型研究 Kainth 果实提取物的抗炎作用。
材料和方法
从 Kainth 乙醇提取物中制备游离、酯化和结合部分，以确定抗炎作用。体外测定 5-脂氧合酶和 COX-2 的水平。通过 ELISA 法定量测定脂多糖刺激的 RAW 巨噬细胞中细胞因子（IL-6、TNF-α和 IL-10）的蛋白水平。此外，还通过角叉菜胶诱导的小鼠足肿胀模型来确定 Kainth 果实提取物的抗炎潜力。使用模拟体外消化系统（唾液、胃和肠）来测量 Kainth 果实提取物的生物可及性。
结果
Kainth 果实提取物经过部分纯化，得到游离、酯化和结合酚类。Kainth 果实的游离和结合酚类物质抑制了 5-脂氧合酶、环氧化酶-2 的活性和促炎细胞因子（白细胞介素-6 和肿瘤坏死因子-α）的表达。此外，这些提取物口服给予角叉菜胶注射的小鼠，通过降低促炎细胞因子和减少足组织中的细胞浸润，显示出抗炎作用。此外，这两种提取物在体外和体内研究中均显示出更好的生物利用度和生物可及性。
结论
结果表明，富含儿茶素、表儿茶素、熊果苷和绿原酸的 Kainth 果实中的游离和结合酚类物质具有抗炎作用，可能可用于治疗炎症性疾病。
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