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来自大萼金莲木具有细胞毒性和抗菌活性的双黄酮类化合物。

Biflavonoids with cytotoxic and antibacterial activity from Ochna macrocalyx.

作者信息

Tang Sharon, Bremner Paul, Kortenkamp Andreas, Schlage Christina, Gray Alexander I, Gibbons Simon, Heinrich Michael

机构信息

Centre for Pharmacognosy and Phytotherapy, The School of Pharmacy, London, UK.

出版信息

Planta Med. 2003 Mar;69(3):247-53. doi: 10.1055/s-2003-38478.

Abstract

Six biflavonoid and related compounds were isolated from the ethanolic extract of Ochna macrocalyx bark. One is a new compound, the isoflavanone dimer dehydroxyhexaspermone C ( 1). Previously isolated compounds obtained from the bark are biisoflavonoid hexaspermone C ( 2). tetrahydrofuran derivative ochnone ( 3). furobenzopyran derivative cordigol ( 4). and biflavonoids calodenin B ( 5). and dihydrocalodenin B ( 6). Although 3 has already been isolated, its spectral data are presented here for the first time. Isolated compounds were tested for cytotoxic activity on MCF-7 breast cancer cells using the MTT reduction assay method. Compound 5 showed cytotoxic activity (7 +/- 0.5 microM) and 6 showed moderate cytotoxicity (35 +/- 7 microM). In antibacterial assays performed using three strains of multi-drug resistant (mdr) Staphylococcus aureus (RN4220, XU212 and SA-1199-B) compounds 5 and in particular 6 showed strong antibacterial activity (MICs 5 : 64, 8, 16 microg/mL 6 : 8, 8, 8 microg/mL, respectively). The ethanolic extract of the bark also showed NF-kappaB inhibitory activity.

摘要

从大萼金莲木树皮的乙醇提取物中分离出六种双黄酮及相关化合物。其中一种是新化合物,异黄酮二聚体脱氢六籽酮C(1)。先前从该树皮中分离得到的化合物有双异黄酮六籽酮C(2)、四氢呋喃衍生物金莲酮(3)、呋喃苯并吡喃衍生物可地果醇(4)以及双黄酮卡洛德宁B(5)和二氢卡洛德宁B(6)。尽管化合物3已被分离出来,但其光谱数据在此首次呈现。采用MTT还原法对分离得到的化合物进行了MCF - 7乳腺癌细胞的细胞毒性活性测试。化合物5表现出细胞毒性活性(7±0.5微摩尔),化合物6表现出中等细胞毒性(35±7微摩尔)。在使用三株多重耐药金黄色葡萄球菌(RN4220、XU212和SA - 1199 - B)进行的抗菌试验中,化合物5尤其是化合物6表现出较强的抗菌活性(化合物5的最低抑菌浓度分别为64、8、16微克/毫升;化合物6的最低抑菌浓度分别为8、8、8微克/毫升)。该树皮的乙醇提取物还表现出NF - κB抑制活性。

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