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从苦丁茶的叶子中分离和鉴定具有抗菌和细胞毒性的化合物。

Isolation and identification of antibacterial and cytotoxic compounds from the leaves of Muntingia calabura L.

机构信息

Faculty of Pharmacy, Universiti Teknologi MARA, Puncak Alam Campus, 42300 Kuala Selangor, Malaysia.

出版信息

J Ethnopharmacol. 2013 Mar 7;146(1):198-204. doi: 10.1016/j.jep.2012.12.032. Epub 2012 Dec 28.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Muntingia calabura (Elaeocarpaceae) is one of the most common roadside trees in Malaysia. Its leaves, barks, flowers and roots have been used as a folk remedy for the treatment of fever, incipient cold, liver disease, as well as an antiseptic agent in Southeast Asia. The aim of this study is to isolate and identify the antibacterial and cytotoxic compounds from the leaves of Muntingia calabura L.

MATERIALS AND METHODS

Antibacterial and cytotoxic activities were determined by micro-broth dilution and MTT assays, respectively. Seven fractions (F1-F7), three flavones and a chalcone were isolated from the active EtOAc extract using bioassay-guided screening. The structures of four compounds were elucidated by spectroscopic methods and compared with published data. The compounds were further tested for their antibacterial and cytotoxic activities.

RESULTS

Three flavones and a chalcone [5,7-dihydroxy-3,8-dimethoxyflavone (1), 2',4'-dihydroxychalcone (2), 5-hydroxy-3,7-dimethoxyflavone (3) and 3,5,7-trihydroxy-8-methoxyflavone (4)] were isolated from the active fraction F5 of EtOAc extract. Compounds 1 and 3 were isolated for the first time from Muntingia calabura L. Antibacterial activity indicates that compound 2 exhibited the most significant activity with MIC value of 50 μg/mL and 100 μg/mL against MSSA and MRSA, respectively. Cytotoxic activity indicates that compounds 2 and 3 exhibited very strong activity against HL60 with IC50 values of 3.43 μg/mL and 3.34 μg/mL, respectively.

CONCLUSION

The antibacterial activity of the leaves of Muntingia calabura L. is ascribable to the active compound 2 while the cytotoxic activity is ascribable to the active compounds 2 and 3.

摘要

植物亲缘关系学相关性

Muntingia calabura(铁青树科)是马来西亚最常见的路边树种之一。其叶子、树皮、花朵和根部被用作民间疗法,用于治疗发热、初期感冒、肝病以及作为东南亚地区的防腐剂。本研究旨在从 Muntingia calabura L. 的叶子中分离和鉴定具有抗菌和细胞毒性的化合物。

材料和方法

通过微量肉汤稀释法和 MTT 测定法分别测定抗菌和细胞毒性活性。采用生物活性导向筛选从活性 EtOAc 提取物中分离出七个馏分(F1-F7)、三种类黄酮和一种查尔酮。通过光谱方法阐明了四个化合物的结构,并与已发表的数据进行了比较。进一步测试了这些化合物的抗菌和细胞毒性活性。

结果

从活性 EtOAc 提取物的 F5 部分分离出三种类黄酮和一种查尔酮[5,7-二羟基-3,8-二甲氧基黄酮(1)、2',4'-二羟基查尔酮(2)、5-羟基-3,7-二甲氧基黄酮(3)和 3,5,7-三羟基-8-甲氧基黄酮(4)]。化合物 1 和 3 是首次从 Muntingia calabura L. 中分离出来的。抗菌活性表明,化合物 2 对 MSSA 和 MRSA 的 MIC 值分别为 50 μg/mL 和 100 μg/mL,表现出最显著的活性。细胞毒性活性表明,化合物 2 和 3 对 HL60 的 IC50 值分别为 3.43 μg/mL 和 3.34 μg/mL,表现出很强的活性。

结论

Muntingia calabura L. 叶子的抗菌活性归因于活性化合物 2,而细胞毒性活性归因于活性化合物 2 和 3。

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