Studies on the antimicrobial activity and brine shrimp toxicity of Zeyheria tuberculosa (Vell.) Bur. (Bignoniaceae) extracts and their main constituents
Studies on the antimicrobial activity and brine shrimp toxicity of Zeyheria tuberculosa (Vell.) Bur. (Bignoniaceae) extracts and their main constituents
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DOI：
10.1186/1476-0711-8-16
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发表时间：
2009-01-01
影响因子：
5.7
通讯作者：
Lemos, Rosangela P. L.
中科院分区：
文献类型：
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作者：
Bastos, Maria Lysete A.;Lima, Maria Raquel F.;Lemos, Rosangela P. L.
背景：由于抗菌药物的滥用，人类对主要抗生素类抗生素耐药的病原微生物增多，在感染性疾病的治疗中造成了许多临床问题。因此，本研究的目的是首次评价瘤纹藻提取物和分离出的化合物的体外抑菌活性和对卤虾的致死性。方法：采用纸片扩散法、生物自显影测定法和卤水对虾毒性试验，研究了提取物和化合物对革兰氏阳性菌(金黄色葡萄球菌)和革兰氏阴性菌(铜绿假单胞菌)和酵母菌(白色念珠菌)的抗菌活性和致死性。提取物对金黄色葡萄球菌(8.0+/-0.0~14.0+/-0.0 mm)和白色念珠菌(15.3+/-0.68~25.6+/-0.4 mm)的生长有抑制作用。在卤水对虾试验中，只有两种提取物表现出毒性(LC_(50)29.55~398.05 mU/m L)，部分提取物无毒或表现出弱致死性(LC_(50)705.02~1000 mU/g/m L)。从这些提取物中分离得到4个黄酮类化合物：5，6，7，8-四甲氧基黄酮(1)，5，6，7-三甲氧基黄酮(2)，4‘-羟基-5，6，7，8-四甲氧基黄酮(3)和4’-羟基-5，6，7-三甲氧基黄酮(4)。通过生物自显影分析，化合物1[金黄色葡萄球菌(16.0+/-0.0 mm)和白色念珠菌(20.0+/-0.0 mm)]和3[金黄色葡萄球菌(10.3+/-0.6 mm)和白色念珠菌(19.7+/-0.6 mm)]对这两种微生物都有抑制作用，而化合物2只抑制金黄色葡萄球菌(11.7+/-0.6 mm)。结论：化合物4对金黄色葡萄球菌和白色念珠菌两种致病微生物有明显的抑制作用。这些结果可能证明该物种的广泛使用是合理的，因为所测试的一些组分具有抗菌活性，而其他组分对盐水虾具有显着的毒性作用。然而，为了评估其在感染性疾病治疗中可能的临床应用，还需要对分离化合物的安全性和毒性进行进一步的研究。
Background: Due to the indiscriminate use of antimicrobial drugs, the emergence of human pathogenic microorganisms resistant to major classes of antibiotics has been increased and has caused many clinical problems in the treatment of infectious diseases. Thus, the aim of this study was to evaluate for the first time the in vitro antimicrobial activity and brine shrimp lethality of extracts and isolated compounds from Zeyheria tuberculosa (Vell.) Bur., a species used in Brazilian folk medicine for treatment of cancer and skin diseases.Methods: Using the disc diffusion method, bioautography assay and brine shrimp toxicity test (Artemia salina Leach), we studied the antimicrobial activity and lethality of extracts and isolated compounds against three microorganisms strains, including Gram-positive (Staphylococcus aureus) and Gram-negative (Pseudomonas aeruginosa) bacteria and yeasts (Candida albicans).Results: In this study, the extracts inhibited S. aureus (8.0 +/- 0.0 to 14.0 +/- 0.0 mm) and C. albicans (15.3 +/- 0.68 to 25.6 +/- 0.4 mm) growth. In the brine shrimp test, only two of them showed toxic effects (LC50 29.55 to 398.05 mu g/mL) and some extracts were non-toxic or showed weak lethality (LC50 705.02 to > 1000 mu g/mL). From these extracts, four flavones [5,6,7,8-tetramethoxyflavone (1), 5,6,7-trimethoxyflavone (2), 4'-hydroxy-5,6,7,8-tetramethoxyflavone (3), and 4'-hydroxy-5,6,7-trimethoxyflavone (4)] were isolated through bioassay-guided fractionation and identified based on the 1D and 2D NMR spectral data. By bioautography assays, compounds 1 [S. aureus (16.0 +/- 0.0 mm) and C. albicans (20.0 +/- 0.0 mm)] and 3 [S. aureus (10.3 +/- 0.6 mm) and C. albicans (19.7 +/- 0.6 mm)] inhibited both microorganisms while 2 inhibited only S. aureus (11.7 +/- 0.6 mm). Compound 4 did not restrain the growth of any tested microorganism.Conclusion: Our results showed that extracts and isolated flavones from Z. tuberculosa may be particularly useful against two pathogenic microorganisms, S. aureus and C. albicans. These results may justify the popular use this species since some fractions tested had antimicrobial activity and others showed significant toxic effects on brine shrimps. However, in order to evaluate possible clinical application in therapy of infectious diseases, further studies about the safety and toxicity of isolated compounds are needed.