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鬼针草的抗分枝杆菌和降血脂活性。

Antimycobacterial and hypolipemiant activities of Bidens odorata (Cavanilles).

机构信息

Departamento de Farmacia, Laboratorio de Toxicología de Productos Naturales, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Av. Wilfrido Massieu, esq. con M. Stampa, Col. Planetario Lindavista, Del. GAM, C.P. 77380 CDMX, Mexico; Departamento de Química Orgánica, Laboratorio de Química de Productos Naturales, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Prol. de Carpio y Plan de Ayala, Del. Miguel Hidalgo, C.P.11340 CDMX, Mexico.

Departamento de Farmacia, Laboratorio de Toxicología de Productos Naturales, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Av. Wilfrido Massieu, esq. con M. Stampa, Col. Planetario Lindavista, Del. GAM, C.P. 77380 CDMX, Mexico.

出版信息

J Ethnopharmacol. 2018 Aug 10;222:159-164. doi: 10.1016/j.jep.2018.04.028. Epub 2018 Apr 26.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Bidens odorata Cavanilles is a medicinal and edible plant known as "mozote blanco, aceitilla, acahual, mozoquelite" which is traditionally used in Mexico as a diuretic, hypoglycaemic, anti-inflammatory, antipyretic, antitussive, to treat gastrointestinal disorders, kidney pain, and lung or respiratory diseases.

AIM OF THE STUDY

This research study was aimed at phytochemical analysis of aerial extracts of B. odorata for antimycobacterial and lipid-lowering activities.

MATERIALS AND METHODS

Compounds 1 (((2R, 3R, 4S, 5S, 6R)-3,4,5-Tryhidroxy-6-(((E)-3-(4-hydroxyphenyl) acryloyl) oxy) tetrahydro-2H-pyran-2-yl) methyl-4-hydroxybenzoate) and 2 (3,5-Dihydroxybenzoic acid) were isolated from B. odorata aerial shoots and their structural elucidation was carried out using 1 and 2D NMR, infrared spectroscopy (IR) and mass spectrometry (ESI-MS). The antimycobacterial activity of various extracts and compounds 1 and 2 was determined using the Microplate Alamar Blue Assay (MABA). The evaluation of the hypolipidemic effect of the ethanolic extract and the glycosylated compound 1 was tested in a murine model of hypercholesterolemia induced by diet and by Triton WR-1339. On the other hand, the LD of the ethanolic extract was evaluated in ICR mice by the OECD protocol TG 423.

RESULTS

Antimycobacterial assay of hexane, CHCl, EtOAc, ethanolic and aqueous extracts, as well as the new glycosidic compound 1 and benzoic acid derivative 2 isolated from B. odorata showed minimal inhibitory concentrations (MIC) of 100, 12.5, 12.5, 12.5, ≥200, 3.125 and 50 μg/mL, respectively, against Mycobacterium tuberculosis H37Rv. Only hexane and CHCl extracts were observed to be active against Mycobacterium smegmatis mc155 at a concentration of 50 and 100 μg/mL, respectively. The ethanolic extract showed lipid-lowering activity at doses of 100 and 1000 mg/kg, while glycosidic compound 1 was active at doses of 50 and 100 mg/kg. In addition, the LD of the ethanolic extract was >2000 mg/kg, meaning that this extract does not cause lethality or adverse effects, and no signs of organs alterations or tissue damage were observed.

CONCLUSION

The hexane, CHCl, EtOAc, and ethanolic extracts of B. odorata, as well as their components 1 and 2, displayed antimycobacterial activity against M. tuberculosis. Moreover, the ethanolic extract and glycosidic compound 1 showed an important lipid-lowering effect, without lethality or secondary effect. The results of this study support the documented traditional use for B. odorata.

摘要

民族药理学相关性

Bidens odorata Cavanilles 是一种药用和食用植物,被称为“mozote blanco、aceitilla、acahual、mozoquelite”,传统上用于墨西哥作为利尿剂、降血糖、抗炎、解热、镇咳,用于治疗胃肠道疾病、肾痛和肺部或呼吸道疾病。

研究目的

本研究旨在对 Bidens odorata 的空气提取物进行植物化学分析,以研究其抗分枝杆菌和降血脂活性。

材料和方法

从 Bidens odorata 空气芽中分离出化合物 1(((2R, 3R, 4S, 5S, 6R)-3,4,5-三羟基-6-(((E)-3-(4-羟基苯基)丙烯酰基)氧基)四氢-2H-吡喃-2-基)甲基-4-羟基苯甲酸酯)和 2(3,5-二羟基苯甲酸),并通过 1 和 2D NMR、红外光谱 (IR) 和质谱 (ESI-MS) 对其结构进行了阐明。使用微量板 Alamar Blue 测定法 (MABA) 测定了各种提取物和化合物 1 和 2 的抗分枝杆菌活性。通过饮食和 Triton WR-1339 诱导的高脂血症小鼠模型,测试了乙醇提取物和糖基化化合物 1 的降血脂作用。另一方面,根据 OECD 协议 TG 423,在 ICR 小鼠中评估了乙醇提取物的 LD。

结果

对正己烷、CHCl、EtOAc、乙醇和水提取物,以及从 Bidens odorata 分离的新糖苷化合物 1 和苯甲酸衍生物 2 的抗分枝杆菌试验表明,对结核分枝杆菌 H37Rv 的最小抑菌浓度 (MIC) 分别为 100、12.5、12.5、12.5、≥200、3.125 和 50μg/mL。只有正己烷和 CHCl 提取物对 Mycobacterium smegmatis mc155 在 50 和 100μg/mL 浓度下显示出活性。乙醇提取物在 100 和 1000mg/kg 剂量下表现出降血脂活性,而糖苷化合物 1 在 50 和 100mg/kg 剂量下具有活性。此外,乙醇提取物的 LD 大于 2000mg/kg,这意味着该提取物不会引起致死或不良反应,也没有观察到器官改变或组织损伤的迹象。

结论

Bidens odorata 的正己烷、CHCl、EtOAc 和乙醇提取物及其成分 1 和 2 对结核分枝杆菌表现出抗分枝杆菌活性。此外,乙醇提取物和糖苷化合物 1 表现出重要的降血脂作用,且无致死性或副作用。本研究的结果支持了 Bidens odorata 的传统用途。

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