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Antimalarial and antimicrobial activities of 8-Aminoquinoline-Uracils metal complexes.

Phopin K, Sinthupoom N, Treeratanapiboon L, Kunwittaya S, Prachayasittikul S, Ruchirawat S, Prachayasittikul V - EXCLI J (2016)

Bottom Line: 8-Aminoquinoline (8AQ) derivatives have been reported to have antimalarial, anticancer, and antioxidant activities.Interestingly, all of these metal complexes (1-6) showed fair antimalarial activities.The results reveal application of 8AQ and its metal complexes as potential compounds to be further developed as novel antimalarial and antibacterial agents.

View Article: PubMed Central - PubMed

Affiliation: Center for Research and Innovation, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand; Department of Clinical Microbiology and Applied Technology, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand.

ABSTRACT
8-Aminoquinoline (8AQ) derivatives have been reported to have antimalarial, anticancer, and antioxidant activities. This study investigated the potency of 8AQ-5-substituted (iodo and nitro) uracils metal (Mn, Cu, Ni) complexes (1-6) as antimalarial and antimicrobial agents. Interestingly, all of these metal complexes (1-6) showed fair antimalarial activities. Moreover, Cu complexes 2 (8AQ-Cu-5Iu) and 5 (8AQ-Cu-5Nu) exerted antimicrobial activities against Gram-negative bacteria including P. shigelloides and S. dysenteriae. The results reveal application of 8AQ and its metal complexes as potential compounds to be further developed as novel antimalarial and antibacterial agents.

No MeSH data available.


Antimicrobial activity of metal complexes (1-6) and ligands
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T3: Antimicrobial activity of metal complexes (1-6) and ligands

Mentions: The agar dilution method (Prachayasittikul et al., 2011[28]) was performed to determine the activity of 8AQ metal complexes (1-6), 5Iu, 5Nu, and 8AQ, as antimicrobial agents against twenty-six microbes. DMSO was used as a control. The results revealed that only Cu-complexes 2 and 5 inhibited the growth of Gram-negative bacteria (Table 3(Tab. 3)), and the DMSO showed no effect toward the tested microorganisms. The Cu-complex 5 exhibited antigrowth activity against P. Shigelloides with MIC value of 256 µg/mL. In addition, the P. shigelloides was partially inhibited by compound 5 at 128 µg/mL and 64 µg/mL showing 75 % and 25 % inhibition, respectively. The Cu-complex 2 at 256 µg/mL exerted 25 % inhibition against P. shigelloides and S. dysenteriae. Other metal complexes (1, 3, 4 and 6) were found to be inactive antimicrobials. It should be noted that the free ligands (8AQ, 5Iu and 5Nu) displayed no antimicrobial activity. This might be suggested that the lipophilic property of Cu-complexes 2 and 5 deriving from complexation of mixed ligands, 8AQ-5Iu and 8AQ-5Nu, could enhance absorption of compounds to their target sites of action. It was observed that the metal complex 5 showed better antimicrobial activity as compared to the complex 2. It could be reasonably explained that the higher electron withdrawing group (5-nitro) of 5Nu ligand facilitated the better dissociation of the complex 5 to give charged complex (8AQ-Cu)+ and free ligand (5Nu) comparing to the complex 2 with lower electron withdrawing group (5-iodo). The charged complex (8AQ-Cu)+ will interact and block the metal binding on the enzyme accounting for antimicrobial activity of the metal complexes (Anjaneyulu et al., 1982[1]; Srisung et al., 2013[38]).


Antimalarial and antimicrobial activities of 8-Aminoquinoline-Uracils metal complexes.

Phopin K, Sinthupoom N, Treeratanapiboon L, Kunwittaya S, Prachayasittikul S, Ruchirawat S, Prachayasittikul V - EXCLI J (2016)

Antimicrobial activity of metal complexes (1-6) and ligands
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4834669&req=5

T3: Antimicrobial activity of metal complexes (1-6) and ligands
Mentions: The agar dilution method (Prachayasittikul et al., 2011[28]) was performed to determine the activity of 8AQ metal complexes (1-6), 5Iu, 5Nu, and 8AQ, as antimicrobial agents against twenty-six microbes. DMSO was used as a control. The results revealed that only Cu-complexes 2 and 5 inhibited the growth of Gram-negative bacteria (Table 3(Tab. 3)), and the DMSO showed no effect toward the tested microorganisms. The Cu-complex 5 exhibited antigrowth activity against P. Shigelloides with MIC value of 256 µg/mL. In addition, the P. shigelloides was partially inhibited by compound 5 at 128 µg/mL and 64 µg/mL showing 75 % and 25 % inhibition, respectively. The Cu-complex 2 at 256 µg/mL exerted 25 % inhibition against P. shigelloides and S. dysenteriae. Other metal complexes (1, 3, 4 and 6) were found to be inactive antimicrobials. It should be noted that the free ligands (8AQ, 5Iu and 5Nu) displayed no antimicrobial activity. This might be suggested that the lipophilic property of Cu-complexes 2 and 5 deriving from complexation of mixed ligands, 8AQ-5Iu and 8AQ-5Nu, could enhance absorption of compounds to their target sites of action. It was observed that the metal complex 5 showed better antimicrobial activity as compared to the complex 2. It could be reasonably explained that the higher electron withdrawing group (5-nitro) of 5Nu ligand facilitated the better dissociation of the complex 5 to give charged complex (8AQ-Cu)+ and free ligand (5Nu) comparing to the complex 2 with lower electron withdrawing group (5-iodo). The charged complex (8AQ-Cu)+ will interact and block the metal binding on the enzyme accounting for antimicrobial activity of the metal complexes (Anjaneyulu et al., 1982[1]; Srisung et al., 2013[38]).

Bottom Line: 8-Aminoquinoline (8AQ) derivatives have been reported to have antimalarial, anticancer, and antioxidant activities.Interestingly, all of these metal complexes (1-6) showed fair antimalarial activities.The results reveal application of 8AQ and its metal complexes as potential compounds to be further developed as novel antimalarial and antibacterial agents.

View Article: PubMed Central - PubMed

Affiliation: Center for Research and Innovation, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand; Department of Clinical Microbiology and Applied Technology, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand.

ABSTRACT
8-Aminoquinoline (8AQ) derivatives have been reported to have antimalarial, anticancer, and antioxidant activities. This study investigated the potency of 8AQ-5-substituted (iodo and nitro) uracils metal (Mn, Cu, Ni) complexes (1-6) as antimalarial and antimicrobial agents. Interestingly, all of these metal complexes (1-6) showed fair antimalarial activities. Moreover, Cu complexes 2 (8AQ-Cu-5Iu) and 5 (8AQ-Cu-5Nu) exerted antimicrobial activities against Gram-negative bacteria including P. shigelloides and S. dysenteriae. The results reveal application of 8AQ and its metal complexes as potential compounds to be further developed as novel antimalarial and antibacterial agents.

No MeSH data available.