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从乌桕(大戟科)茎皮中分离和鉴定具有抗炎和镇痛作用的化合物。

Isolation and characterization of anti-inflammatory and analgesic compounds from Uapaca staudtii Pax (Phyllanthaceae) stem bark.

机构信息

Department of Pharmacognosy and Natural Medicine, University of Uyo, Ikpa Road, Uyo, Nigeria.

Department of Chemistry, University of Uyo, Ikpa Road, Uyo, Nigeria.

出版信息

J Ethnopharmacol. 2021 Apr 6;269:113737. doi: 10.1016/j.jep.2020.113737. Epub 2021 Jan 5.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Uapaca species including Uapacastaudtii Pax (Phyllanthaceae) are used in West Africa ethnomedicine to treat diverse ailments including pile, rheumatism, oedema and wound healing. However, the anti-inflammatory and analgesic potential as well as constituents of the Uapacastaudtii stem bark has not been investigated.

AIM OF THE STUDY

The study was designed to evaluate the anti-inflammatory, analgesic, and antioxidant activities of extract and fractions ofU. staudtii stem bark, and to isolate the bioactive constituents.

MATERIALS AND METHODS

The anti-inflammatory, analgesic and antioxidant activities of the ethanol extract, dichloromethane, ethyl acetate, butanol, and aqueous fractions of U. staudtii stem bark, as well as protocatechuic acid and betulinic acid isolated from the bioactive ethyl acetate fraction were evaluated in different mice models of inflammation and pain; furthermore, antioxidant assays were carried out. Chemical structures of isolated compounds were established based on spectroscopic studies and comparison with literature data.

RESULTS

The ethanol extract and ethyl acetate fraction exhibited good anti-inflammatory, analgesic, and antioxidant capacity in all studied models, comparable with those of the standard drugs used. Protocatechuic acid also gave significant (p < 0.05) anti-inflammatory (83%and 88% inhibition for egg-albumin induced and xylene induced oedema, respectively), analgesic (56% inhibition and 22 s of pain suppression for acetic acid-induced and hot plate-induced pain, respectively), and antioxidant effects (97% inhibition and absorbance of 2.516 at 100 μg/mL for DPPH and FRAP assay, respectively) in all the models, whereas betulinic acid only exhibited significant (p < 0.05) anti-inflammatory and antioxidant activity.

CONCLUSIONS

The result supports the medicinal uses of the U. staudtii stem bark in the management of pain and inflammatory disease. This is the first report on the biological activities and characterization of compounds inU. staudtii, and presence of protocatechuic acid in Uapaca genus.

摘要

民族药理学相关性

包括 Uapaca staudtii Pax(叶下珠科)在内的 Uapaca 物种在西非民族医学中用于治疗多种疾病,包括痔疮、风湿病、水肿和伤口愈合。然而,Uapaca staudtii 树皮的抗炎和镇痛潜力以及成分尚未得到研究。

研究目的

本研究旨在评估 U. staudtii 茎皮提取物和馏分的抗炎、镇痛和抗氧化活性,并分离生物活性成分。

材料和方法

在不同的炎症和疼痛小鼠模型中评估了 U. staudtii 茎皮的乙醇提取物、二氯甲烷、乙酸乙酯、正丁醇和水馏分以及从生物活性乙酸乙酯馏分中分离出的原儿茶酸和白桦脂酸的抗炎、镇痛和抗氧化活性;此外,还进行了抗氧化测定。根据光谱研究和与文献数据的比较,确定了分离化合物的化学结构。

结果

乙醇提取物和乙酸乙酯馏分在所有研究模型中均表现出良好的抗炎、镇痛和抗氧化能力,与所用标准药物相当。原儿茶酸也表现出显著的抗炎作用(卵清蛋白诱导和二甲苯诱导水肿分别为 83%和 88%的抑制作用)、镇痛作用(乙酸诱导和热板诱导疼痛分别为 56%的抑制作用和 22 s 的疼痛抑制作用)和抗氧化作用(DPPH 和 FRAP 测定分别为 97%的抑制作用和 100μg/mL 时的吸光度为 2.516),而白桦脂酸仅表现出显著的抗炎和抗氧化活性。

结论

该结果支持 U. staudtii 茎皮在疼痛和炎症性疾病管理中的药用用途。这是首次报道 U. staudtii 中的生物活性和化合物特征,以及原儿茶酸在 Uapaca 属中的存在。

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