Gold(I) NHC Complexes: Antiproliferative Activity, Cellular Uptake, Inhibition of Mammalian and Bacterial Thioredoxin Reductases, and Gram-Positive Directed Antibacterial Effects

2017 ◽  
Vol 23 (8) ◽  
pp. 1869-1880 ◽  
Author(s):  
Claudia Schmidt ◽  
Bianka Karge ◽  
Rainer Misgeld ◽  
Aram Prokop ◽  
Raimo Franke ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Antiproliferative Activity ◽  
Antibacterial Effects ◽  
Gram Positive ◽  
Uptake Inhibition ◽  
Thioredoxin Reductases

Fluorescent Copper(II) Complexes of Asymmetric Bis(Thiosemicarbazone)s: Electrochemistry, Cellular Uptake and Antiproliferative Activity

2021 ◽  
Vol 6 (24) ◽  
pp. 6063-6070
Author(s):  
Deepti U. Kirtani ◽  
Niraj S. Ghatpande ◽  
Komal R. Suryavanshi ◽  
Prasad P. Kulkarni ◽  
Anupa A. Kumbhar
Keyword(s):  
Cellular Uptake ◽  
Antiproliferative Activity

MEMBRANE-ACTIVE METHANOLIC CRUDE EXTRACT OF THERMOTOLERANT, Aspergillus fumigatus SSH01 AND ITS MODE OF ACTION AGAINST GRAM-POSITIVE PATHOGENS

2017 ◽  
Vol 80 (1) ◽  
Author(s):  
Mohamad Khairil Radzali ◽  
Akmal Hayat Abdul Karim ◽  
Syahida Ahmad ◽  
Wan Zuhainis Saad
Keyword(s):  
Aspergillus Fumigatus ◽  
Crude Extract ◽  
Inhibitory Concentration ◽  
Minimum Bactericidal Concentration ◽  
Antibacterial Properties ◽  
Bacterial Membrane ◽  
Antibacterial Effects ◽  
Gram Positive ◽  
Bacillus Subtilis Atcc ◽  
Time Kill

This study was undertaken to investigate the antibacterial properties and the mode of actions of crude extract of Aspergillus fumigatus SSH01. Antibacterial properties was observed against Gram-positive pathogens and showed inhibition against Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 6538, methicillin-resistant S. aureus S547 (MRSA) and Listeria monocytogenes L10 with minimum inhibitory concentration (MIC, 0.097- 12.5 mg/ml) and minimum bactericidal concentration (MBC, 0.195 – 25 mg/ml). No surviving cells were detected after 15 h of treatment with the 2MIC of extracts for time-kill assay. Leakage of cellular contents of the treated test pathogens were identified and increased as the concentrations of the extracts increased. The study of morphological surface has shown the bacterial membrane was disrupted and caused loss of viability. This implies the antibacterial effects of A. fumigatus SSH01 extract may serve as the potential antibiotic. 

scholarly journals Antibacterial Activities of 5-Nitro-2-uryl and 5-Nitro-2-Imidazolyl Derivatives of 1,3,4-Thiadiazole

2019 ◽  
Vol 4 (2) ◽  
Author(s):  
Mohammad Hassan Moshafi ◽  
Ali Peymani ◽  
Alireza Foroumadi ◽  
Mohammad Reza Zabihi ◽  
Farzad Doostishoar
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Positive Control ◽  
Klebsiella Pneumonia ◽  
Bacterial Strains ◽  
Antibacterial Effects ◽  
Gram Positive ◽  
Gram Negative ◽  
Derivatives Of

Introduction: Nitrofurans and nitroimidazoles are broad-spectrum antimicrobial agents, which affect the microbial DNA. The aim of the present study was to evaluate the new derivatives of these two groups of antimicrobials against certain Gram-positive and Gram-negative bacterial strains. Materials and Methods: Seven new derivatives of nitrofurans and nitroimidazoles were synthesized, and 6.4 mg of each derivative was dissolved in dimethyl sulfoxide. Then, 8 serial dilutions (0.5, 1, 2, 4, 8, 16, 32, and 64 μg/ml) of each derivative was prepared using Muller-Hinton broth, and the minimum inhibitory concentration for each derivative was measured and compared to ciprofloxacin (standard). Results: All the derivatives had no antibacterial effects against Gram-negative bacteria (minimum inhibitory concentration > 64 μg/ml); only 2-(5-nitro-2-furyl)-5-(n-pentylsulfunyl)-1,3,4-thiadiazole exhibited mild antibacterial effects against Klebsiella pneumonia (minimum inhibitory concentration of 16-32 μg/ml). The antibacterial effects of the derivatives against Gram-positive bacteria also showed variations from complete inhibition of the growth of Staphylococcus epidermidis and Bacillus subtilis (minimum inhibitory concentration < 0.5 μg/ml) by 2-(5-nitro-2-furyl)-5-(n-buthylthio)-1,3,4-thiadiazole to no inhibition of S. epidermidis and streptococcus pyogenes. Conclusion: These compounds have weak antibacterial effects; only two derivatives showed antibacterial effects similar to that of the positive control.

scholarly journals Anticancer and Structure Activity Relationship of Non-Symmetrical Choline Kinase Inhibitors

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1360
Author(s):  
Santiago Schiaffino-Ortega ◽  
Elena Mariotto ◽  
Pilar María Luque-Navarro ◽  
María Kimatrai-Salvador ◽  
Pablo Rios-Marco ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Kinase Inhibitors ◽  
Human Tumor ◽  
Structure Activity Relationship ◽  
Inhibitory Effect ◽  
Activity Relationship ◽  
Choline Kinase ◽  
Choline Uptake ◽  
Uptake Inhibition ◽  
Structure Activity

Choline kinase inhibitors are an outstanding class of cytotoxic compounds useful for the treatment of different forms of cancer since aberrant choline metabolism is a feature of neoplastic cells. Here, we present the most in-depth structure-activity relationship studies of an interesting series of non-symmetric choline kinase inhibitors previously reported by our group: 3a–h and 4a–h. They are characterized by cationic heads of 3-aminophenol bound to 4-(dimethylamino)- or 4-(pyrrolidin-1-yl)pyridinium through several linkers. These derivatives were evaluated both for their inhibitory activity on the enzyme and their antiproliferative activity in a panel of six human tumor cell lines. The compounds with the N-atom connected to the linker (4a–h) show the best inhibitory results, in the manner of results supported by docking studies. On the contrary, the best antiproliferative compounds were those with the O-atom bounded to the linker (3a–h). On the other hand, as was predictable in both families, the inhibitory effect on the enzyme is better the shorter the length of the linker. However, in tumor cells, lipophilicity and choline uptake inhibition could play a decisive role. Interestingly, compounds 3c and 4f, selected for both their ability to inhibit the enzyme and good antiproliferative activity, are endowed with low toxicity in non-tumoral cells (e.g., human peripheral lymphocytes) concerning cancer cells. These compounds were also able to induce apoptosis in Jurkat leukemic cells without causing significant variations of the cell cycle. It is worth mentioning that these derivatives, besides their inhibitory effect on choline kinase, displayed a modest ability to inhibit choline uptake thus suggesting that this mechanism may also contribute to the observed cytotoxicity.

Correlating FAAH and anandamide cellular uptake inhibition using N-alkylcarbamate inhibitors: From ultrapotent to hyperpotent

2014 ◽  
Vol 92 (4) ◽  
pp. 669-689 ◽  
Author(s):  
Simon Nicolussi ◽  
Andrea Chicca ◽  
Mark Rau ◽  
Sabine Rihs ◽  
Michael Soeberdt ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Uptake Inhibition
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