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(产自埃及)中甲氧基黄酮的抗炎作用。

Anti-inflammatory effect of methoxyflavonoids from ( growing in Egypt.

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt.

Department of Pharmacognosy, College of Pharmacy, Arab Academy for Science, Technology and Maritime Transport, Alexandria, Egypt.

出版信息

Nat Prod Res. 2021 Dec;35(24):5909-5913. doi: 10.1080/14786419.2020.1802272. Epub 2020 Aug 4.

Abstract

is a medicinal plant that grows in Sinai Peninsula in Egypt. Phytochemical investigation of methanolic extract led to the isolation of five methoxy flavonoids; Chrysosplenol-D 5,7,4'-trihydroxy- 3,3'-dimethoxy flavone , 5,7-dihydroxy -3,3',4'-trimethoxyflavone , Bonanzin , 3,5,6,7,4'-pentamethoxy flavone a sesquiterpene, Cryptomeridiol and stigmast-5,22-dien-3-O-β-D-glucopyranoside . The anti-inflammatory activity of compounds and was assessed on CaCo2 cells stimulated by lipopolysaccharide (LPS). Both compounds downregulated LPS-induced expression of inflammatory cytokines; tumor necrosis factor alpha (TNFα), interleukin 1β (IL1β), nuclear factor kappa B (NFκB), cyclooxygenase 1 (Cox1), cyclooxygenase 2 (Cox2), and 5-lipoxygenase (5Lox). In vivo, both compounds significantly decreased paw edema thickness in rats relative to carrageenan, showing better anti-inflammatory activity than celecoxib (36.98%) after 1 h (46.60% and 48.11%, respectively). An study was performed, where both compounds were docked into the active site of the crystal structure of the human Cox2 enzyme.

摘要

是一种生长在埃及西奈半岛的药用植物。对其甲醇提取物的植物化学研究导致了五个甲氧基黄酮类化合物的分离;Chrysosplenol-D 5,7,4'-三羟基-3,3'-二甲氧基黄酮、5,7-二羟基-3,3',4'-三甲氧基黄酮、Bonanzin、3,5,6,7,4'-五甲氧基黄酮、一种倍半萜、Cryptomeridiol 和豆甾-5,22-二烯-3-O-β-D-吡喃葡萄糖苷。化合物 和 对脂多糖(LPS)刺激的 CaCo2 细胞的抗炎活性进行了评估。这两种化合物均下调了 LPS 诱导的炎症细胞因子的表达;肿瘤坏死因子-α(TNFα)、白细胞介素 1β(IL1β)、核因子 kappa B(NFκB)、环氧化酶 1(Cox1)、环氧化酶 2(Cox2)和 5-脂氧合酶(5Lox)。在体内,与角叉菜胶相比,这两种化合物均显著降低了大鼠足肿胀的厚度,在 1 小时后显示出比塞来昔布(36.98%)更好的抗炎活性(分别为 46.60%和 48.11%)。进行了一项 研究,其中将这两种化合物分别对接到人 Cox2 酶的晶体结构的活性部位。

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