de Farias Pablo Antonio Maia, Figueredo Fernando Gomes, Lucas Aline Maria Brito, de Moura Rafael Barbosa, Coutinho Henrique Douglas Melo, da Silva Tania Maria Sarmento, Martin Ana Luiza de Aguiar Rocha, Fonteles Marta Maria de França
Development and Technological Innovation in Medicines, Universidade Federal do Ceará - UFC, Juazeiro do Norte-CE, PE, Brazil ; College of Pharmacy, Faculdade de Medicina Estácio de Juazeiro do Norte-Estácio, Juazeiro do Norte-CE, PE, Brazil.
College of Biomedicine, Faculdade Leão Sampaio-FLS, Juazeiro do Norte-CE, PE, Brazil ; College of Pharmacy, Faculdade de Medicina Estácio de Juazeiro do Norte-Estácio, Juazeiro do Norte-CE, PE, Brazil.
Drug Des Devel Ther. 2015 Jun 15;9:3067-72. doi: 10.2147/DDDT.S84676. eCollection 2015.
The search for new active compounds from the Brazilian flora has intensified in recent years, especially for new drugs with antibiotic potential. Accordingly, the aim of this study was to determine whether riachin has antibiotic activity in itself or is able to modulate the activity of conventional antibiotics.
A non-cyanogenic cyanoglycoside known as riachin was isolated from Bauhinia pentandra, and was tested alone and in combination with three antibiotics (clindamycin, amikacin, and gentamicin) against multiresistant bacterial strains (Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus).
Riachin did not show significant antibiotic activity when tested alone against any strain (P>0.05). However, when combined with conventional antibiotics, it showed drug-modifying activity against strains of S. aureus exposed to clindamycin (P<0.001) as well as against P. aeruginosa exposed to amikacin (P<0.001). Although riachin did not show direct antibiotic activity, it had synergistic activity when combined with amikacin or clindamycin. The mechanism of action of this synergism is under investigation.
The results of this work demonstrate that some substances of natural origin can enhance the effectiveness of certain antibiotics, which means a substantial reduction in the drug dose required and possibly in consequent adverse events for patients.
近年来,从巴西植物群中寻找新的活性化合物的研究日益加强,特别是寻找具有抗生素潜力的新药。因此,本研究的目的是确定利亚钦本身是否具有抗生素活性,或者是否能够调节传统抗生素的活性。
从五叶羊蹄甲中分离出一种名为利亚钦的非氰化氰苷,并单独以及与三种抗生素(克林霉素、阿米卡星和庆大霉素)联合针对多重耐药菌株(大肠杆菌、铜绿假单胞菌和金黄色葡萄球菌)进行测试。
利亚钦单独针对任何菌株进行测试时均未显示出显著的抗生素活性(P>0.05)。然而,当与传统抗生素联合使用时,它对暴露于克林霉素的金黄色葡萄球菌菌株(P<0.001)以及暴露于阿米卡星的铜绿假单胞菌菌株(P<0.001)显示出药物修饰活性。尽管利亚钦未显示出直接的抗生素活性,但与阿米卡星或克林霉素联合使用时具有协同活性。这种协同作用的作用机制正在研究中。
这项工作的结果表明,一些天然来源的物质可以提高某些抗生素的有效性,这意味着所需药物剂量大幅减少,并且可能减少患者随后出现的不良事件。