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Multitargeting Antibacterial Activity of a Synthesized Mn2+ Complex of Curcumin on Gram-Positive and Gram-Negative Bacterial Strains.
ACS Omega ( IF 3.7 ) Pub Date : 2020-07-06 , DOI: 10.1021/acsomega.9b04079 Tanmoy Saha 1 , Prince Kumar 2 , Nayim Sepay 1 , Durba Ganguly 3 , Kanchan Tiwari 2 , Kasturi Mukhopadhyay 2 , Saurabh Das 1
ACS Omega ( IF 3.7 ) Pub Date : 2020-07-06 , DOI: 10.1021/acsomega.9b04079 Tanmoy Saha 1 , Prince Kumar 2 , Nayim Sepay 1 , Durba Ganguly 3 , Kanchan Tiwari 2 , Kasturi Mukhopadhyay 2 , Saurabh Das 1
Affiliation
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Curcumin is an important molecule with a plethora of pharmacological activities and therapeutic potentials. Despite its efficacy, it remained a potential drug candidate owing to hydrolytic instability and poor aqueous solubility. To overcome the limitations related to low solubility, low bioavailability, and the fact that curcumin is never present in solution as a “single unit”, its complex was prepared with MnII with the idea that binding to a metal ion might help to resolve these issues. The complex was characterized by elemental and spectral analysis. The structure of the complex was determined by density functional theory calculations. The complex was stable at physiological buffer conditions, unlike curcumin. It did not have any detrimental effect on mammalian cells. There was a significant enhancement in the antibacterial activity of the complex compared to curcumin against both Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria. It showed a strong affinity for deoxyribonucleic acid (DNA) evident from a high binding constant value with calf thymus DNA and also from the retarded electrophoretic mobility of bacterial plasmid DNA. The complex showed “superoxide dismutase-like” activity leading to the generation of reactive oxygen species (ROS). The complex caused bacterial membrane perturbation evident from calcein leakage assay, which was further corroborated by scanning and transmission electron microscopic experiments. Overall, the present study shows improved stability and antibacterial potency of a nontoxic complex over curcumin. Its multitargeting mode of action such as ROS-production, effective binding with DNA, and permeabilization of bacterial membrane together allows it to be an effective antibacterial agent that could be taken further for therapeutic use against bacterial infections.
中文翻译：
合成的姜黄素 Mn2+ 复合物对革兰氏阳性和革兰氏阴性菌株的多靶点抗菌活性。
姜黄素是一种重要的分子，具有多种药理活性和治疗潜力。尽管具有功效，但由于水解不稳定性和水溶性差，它仍然是一种潜在的候选药物。为了克服与低溶解度、低生物利用度以及姜黄素从不作为“单一单元”存在于溶液中这一事实相关的限制，用 Mn II制备其复合物，其想法是与金属离子结合可能有助于解决这些问题问题。通过元素和光谱分析对该配合物进行了表征。通过密度泛函理论计算确定了配合物的结构。与姜黄素不同，该复合物在生理缓冲条件下稳定。它对哺乳动物细胞没有任何有害影响。与姜黄素相比，该复合物对革兰氏阳性菌（金黄色葡萄球菌）和革兰氏阴性菌（大肠杆菌）的抗菌活性显着增强。它对脱氧核糖核酸 (DNA) 表现出很强的亲和力，这可以从与小牛胸腺 DNA 的高结合常数值以及细菌质粒 DNA 的延迟电泳迁移率中看出。该复合物表现出“超氧化物歧化酶样”活性，导致活性氧（ROS）的产生。从钙黄绿素渗漏测定中可以明显看出该复合物引起细菌膜扰动，并通过扫描和透射电子显微镜实验进一步证实。总体而言，本研究表明无毒复合物比姜黄素具有更好的稳定性和抗菌效力。 其多靶点作用模式，如 ROS 产生、与 DNA 的有效结合以及细菌膜的透化作用，使其成为一种有效的抗菌剂，可进一步用于治疗细菌感染。
更新日期：2020-07-14
中文翻译：
合成的姜黄素 Mn2+ 复合物对革兰氏阳性和革兰氏阴性菌株的多靶点抗菌活性。
姜黄素是一种重要的分子，具有多种药理活性和治疗潜力。尽管具有功效，但由于水解不稳定性和水溶性差，它仍然是一种潜在的候选药物。为了克服与低溶解度、低生物利用度以及姜黄素从不作为“单一单元”存在于溶液中这一事实相关的限制，用 Mn II制备其复合物，其想法是与金属离子结合可能有助于解决这些问题问题。通过元素和光谱分析对该配合物进行了表征。通过密度泛函理论计算确定了配合物的结构。与姜黄素不同，该复合物在生理缓冲条件下稳定。它对哺乳动物细胞没有任何有害影响。与姜黄素相比，该复合物对革兰氏阳性菌（金黄色葡萄球菌）和革兰氏阴性菌（大肠杆菌）的抗菌活性显着增强。它对脱氧核糖核酸 (DNA) 表现出很强的亲和力，这可以从与小牛胸腺 DNA 的高结合常数值以及细菌质粒 DNA 的延迟电泳迁移率中看出。该复合物表现出“超氧化物歧化酶样”活性，导致活性氧（ROS）的产生。从钙黄绿素渗漏测定中可以明显看出该复合物引起细菌膜扰动，并通过扫描和透射电子显微镜实验进一步证实。总体而言，本研究表明无毒复合物比姜黄素具有更好的稳定性和抗菌效力。 其多靶点作用模式，如 ROS 产生、与 DNA 的有效结合以及细菌膜的透化作用，使其成为一种有效的抗菌剂，可进一步用于治疗细菌感染。
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