R = O-CH2-CH2-OH:2-[(9-amino-7-ethoxyacridin-3-yl)oxy]ethanol.
Panel reference strains of bacteria from the American Type Culture Collection or Polish Collection of Microorganisms, including aerobic Gram-positive bacteria: Staphylococcus aureus ATCC 25923 and Staphylococcus epidermidis ATCC 12228, and aerobic Gram-negative bacteria: Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 9027, as well as microaerobic Gram-positive bacteria: Lactobacillus spp., Lactobacillus acidophilus PCM 2105, Streptococcus mutans PCM 2502 and Streptococcus sanguinis PCM 2335, were used. Microbial suspensions with an optical density of 0.5 McFarland standard at 1.5 × 108 CFU/mL (CFU: colony forming unit) were prepared in sterile 0.9 % NaCl. Mueller–Hinton (M–H) broth and M–H agar (Oxoid Ltd., England) for aerobic strains, and MRS Broth Lactobacillus, MRS Agar Lactobacillus (BioMaxima S.A., Poland), BHI Broth and BHI agar (BioMaxima S.A., Poland) for microaerobic strains were used in the microbial tests. All stock solutions of the newly synthesized compounds were prepared in DMSO (the final DMSO concentration used in bacterial tests did not inhibit microbial growth and was less than 1.5 %). The antibacterial activity of the newly synthesized compounds was compared with the controls: cefepime dihydrochloride (Maxipime, Bristol-Myers Squibb Latina), chlorhexidine digluconate ((CLX) Amara Poland) and ethacridine lactate (Rivanolum, PharmaSwiss, Czech Republic).
Ethacridine lactate monohydrate | CAS#6402-23-9 | …
The TI values below 1 obtained by the tested substances correspond to the lack of therapeutic safety. Among the synthesized compounds, derivatives 1, 6 and 10 showed the highest values of therapeutic index. Compound 6 exhibited the in vitro therapeutic potential against S. aureus, S. epidermidis, E. coli and, which is important, against S. mutans and S. sanguinis, with the TI values of 3.67, 1.83, 14.68, 3.67 and 58.7, respectively. The essential observation is that the in vitro therapeutic indices of compound 6 were approximately 4–133 times higher than the in vitro TI values of ethacridine lactate and 58 times higher than the TI value obtained by CLX against S. mutans. Compound 1 also showed high in vitro TI values (6.82, 13.7, 3.41, 6.83 against S. aureus, S. epidermidis, E. coli and L. species, respectively). Additionally, the TI values of compound 10 against S. aureus, S. epidermidis and S. mutans were greater than those of compound 1. Nevertheless, among all the tested agents, CLX exhibited the highest in vitro TI values. It should be noted that antibacterial agents which possess a value of therapeutic index higher than 10 can be administered to perform in vivo evaluation (Kashyap et al., ; Ghareb et al., ). Our two newly synthesized compounds (1 and 6) had antibacterial activity and exhibited excellent TI values higher than 10 against some bacterial strains.
In this study, we reported the synthesis and antibacterial activity of new compounds with pyridinecarbonyl group connected to the thiosemicarbazide system. It should be noted that two thiosemicarbazide derivatives, i.e., 2 and 4, exhibited good or moderate inhibition of all the most common caries-associated Gram-positive and Gram-negative bacterial strains. Moreover, these compounds strongly suppressed human hepatocellular carcinoma and human breast adenocarcinoma cell proliferation. The structure–activity relationship of the compounds showed that substitution at the position 2 of the pyridine ring enhances biological activity. The prominent antibacterial and antiproliferative effect of compounds 2 and 4 may be due to changing the number of chlorine atoms in the phenyl ring. Thus, it is worth underlying that 4-(2-chloro/2,4-dichlorophenyl)-1-(pyridine-2yl)carbonylthiosemicarbazide derivatives will be auspicious as potential agents for caries treatment and caries-associated cancer diseases. The physicochemical analysis indicates that the polar surface area is an important parameter for biological activity of the investigated compounds. Our results will have an impact on further investigation in this field in search of thiosemicarbazide compounds as antibacterial and antiproliferative agents.
Ethacridine Lactate | Spectrum Chemical
The preliminary antibacterial activity of the carbazide derivatives against human pathogenic Gram-positive, Gram-negative aerobic and microaerobic bacteria was evaluated by measuring the zones of inhibition in the disk diffusion method (Murray et al., ). Each compound (100 µg) was placed on Petri plates with agar medium (previously inoculated with 0.5 McFarland standards with the tested bacterial strains). After 18 h of incubation at 37 °C (for aerobic strains) or 40 h at 35 °C (for microaerobic strains), zones of microbial growth produced around the tested substances were measured and recorded as the diameters of inhibition.
ethacridine lactate CHARACTERS Appearance Yellow crystalline powder
Lactate also rescues DAB induced impairment of memory when injected either immediately after training or 10-20 min later (Figure ). So, in contrast to the action of glutamine, lactate rescues memory from loss caused by DAB only at times when memory is NOT susceptible to DAB. These are the same time periods over which lactate normally enhances weakly reinforced learning (5-20 min; ). Because of the difference in timing of the effect of lactate and glutamine, it is unlikely that they are producing the same end result of increasing glutamate. Lactate is readily taken up by neurons and astrocytes, but lactate uptake into astrocytes inhibits glycolysis (). In that paper we discussed the fluxes of lactate into astrocytes, neurons, and between astrocytes and the multifunctional roles for lactate. Transport of lactate between brain cells is mainly between astrocytes via gap junctions and release into extracellular space leads to significant exit of lactate from the brain via the blood and via the perivascular-lymphatic drainage system ().
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1 ml of solution contains:
1.25 mg Malachite green oxalate
0.10 mg Ethacridine lactate monohydrate
0.10 mg Methylthionine chloride
0.05 mg Methylrosaniline chloride