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一种新型化合物通过调节大鼠肝组织中的 COX-2 和炎症细胞因子来治疗炎症。

A Novel Distachionate from Treats Inflammations by Modulating COX-2 and Inflammatory Cytokines in Rat Liver Tissue.

机构信息

Department of Pharmaceutical Chemistry, Government College University, Faisalabad 38000, Pakistan.

Faculty of Pharmacy, Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.

出版信息

Molecules. 2022 Apr 18;27(8):2596. doi: 10.3390/molecules27082596.

DOI:10.3390/molecules27082596
PMID:35458792
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9027007/
Abstract

Breynia distachia is a plant of genus Breynia belonging to family Phyllanthaceae. This study was conducted to isolate and examine the anti-inflammatory attributes of the roots of Breynia distachia. Methanol extract from roots were prepared by simple maceration. For phytochemical studies, isolation, purification, structure elucidation, metal analysis, total phenolic content, and solubility test were done by chromatographic and spectroscopic techniques. Anti-inflammatory activity was evaluated by cotton pallet edema model and carrageenan paw edema model, and antioxidant potential was evaluated by DPPH, FRAP, and ABTS antioxidants assays. Metal analysis of BD.Me revealed the presence of Na > Mg > K > Mn > Fe = Zn in respective order. Four phytochemicals such as gallic acid, quercetin, sinapic acid, and p-coumaric acid are found in Breynia distachia. Quercetin is present in relatively larger quantity, and shows antioxidant activity by reducing the ferric iron to ferrous iron. Novel distachionate shows high antioxidant activity in ABTS assay by reducing reactive oxygen species. Quantitative or qualitative analysis performed by HPLC indicates the ascending peaks or presence of secondary products (metabolites) respectively. Histopathology analysis of liver, spleen, heart, and kidney was done, revealing mild inflammations in spleen and liver, and no cytotoxicity in heart and kidney. Oral administration of BD.Me and ditachionate significantly inhibits the carrageenan and cotton pellet-induced paw edema in 1st and 2nd h with (ns = p > 0.05) than control. After 3rd, 4th, 5th, and 6th h, BD.Me and ditachionate showed inhibition of paw edema in a highly significant (*** = p < 0.001) manner as compared to control. In cotton-pellet edema model, distachionate shows a %inhibition of 57.3% at a dose level of 5 mg/kg. Docking values obtained from distachionate-COX-2 complex suggest a potent inhibitor evaluated for this protein. The distachionate shows effective anti-inflammatory activity. Methanol extracts of roots showed significant lipoxygenase inhibitory activity by IC50 values of 155.7 ± 0.55 and 132.9 ± 0.33 μg/mL. Data from various in vitro and in vivo models suggest that novel distachionate isolated from Breynia distachia shows strong antioxidant and anti-inflammatory activities; it should be further studied for the exploration of its medicinal potential.

摘要

算盘子是算盘子属的一种植物,属于叶下珠科。本研究旨在分离和研究算盘子根的抗炎特性。通过简单的浸渍法从根部制备甲醇提取物。对于植物化学研究,通过色谱和光谱技术进行分离、纯化、结构解析、金属分析、总酚含量和溶解度测试。通过棉花垫肿胀模型和角叉菜胶足肿胀模型评估抗炎活性,通过 DPPH、FRAP 和 ABTS 抗氧化剂测定评估抗氧化潜力。BD.Me 的金属分析表明,Na > Mg > K > Mn > Fe = Zn 的顺序存在。在 Breynia distachia 中发现了四种植物化学物质,如没食子酸、槲皮素、芥子酸和对香豆酸。槲皮素的含量相对较高,通过将三价铁还原为二价铁表现出抗氧化活性。新型二萜在 ABTS 测定中表现出高抗氧化活性,通过还原活性氧来减少活性氧。HPLC 进行的定量或定性分析分别表示上升峰或存在次级产物(代谢物)。对肝、脾、心和肾进行组织病理学分析,结果显示脾和肝有轻度炎症,心和肾无细胞毒性。BD.Me 和二萜酸盐经口给药可显著抑制角叉菜胶和棉花球诱导的爪肿胀,在第 1 小时和第 2 小时(ns = p > 0.05)与对照组相比,第 3 小时、第 4 小时、第 5 小时和第 6 小时,BD.Me 和二萜酸盐对爪肿胀的抑制作用呈高度显著(*** = p < 0.001)。在棉花球肿胀模型中,二萜酸盐在 5 mg/kg 剂量水平下显示出 57.3%的抑制率。从二萜酸盐-COX-2 复合物获得的对接值表明,该蛋白被评估为一种有效的抑制剂。二萜酸盐表现出有效的抗炎活性。根的甲醇提取物通过 IC50 值 155.7 ± 0.55 和 132.9 ± 0.33 μg/mL 显示出显著的脂氧合酶抑制活性。来自各种体外和体内模型的数据表明,从 Breynia distachia 中分离出的新型二萜具有很强的抗氧化和抗炎活性;应进一步研究其药用潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/73d97ecb87e5/molecules-27-02596-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/b2edf89c2e75/molecules-27-02596-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/4f1f6e1903e1/molecules-27-02596-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/b47698f5aba5/molecules-27-02596-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/bdfa06a82637/molecules-27-02596-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/e6533251fe07/molecules-27-02596-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/488f849b71ec/molecules-27-02596-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/73d97ecb87e5/molecules-27-02596-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/b2edf89c2e75/molecules-27-02596-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/4f1f6e1903e1/molecules-27-02596-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/b47698f5aba5/molecules-27-02596-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/bdfa06a82637/molecules-27-02596-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/e6533251fe07/molecules-27-02596-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/488f849b71ec/molecules-27-02596-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a322/9027007/73d97ecb87e5/molecules-27-02596-g007.jpg

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