Acute, subacute oral toxicity and Ames test of Py-mulin: an antibacterial drug candidate

Fan, Yuan; Fu, Yuejun; Zhou, Yuhang; Liu, Yu; Hao, Baocheng; Shang, Ruofeng

doi:10.1186/s40360-021-00543-5

Cited by 13 publications

(5 citation statements)

References 27 publications

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“…SCA and SCB compounds were assayed for genotoxicity evaluation through the Ames test employing the histidine-requiring Salmonella typhimurium mutant TA98 and TA100 strains allowing to check frameshift mutation and base-pair substitution, with and without metabolic activation induced by S9 Mix [ 16 – 19 ].…”

Section: Resultsmentioning

confidence: 99%

Biological activity of new bioactive steroids deriving from biotransformation of cortisone

et al. 2022

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Cortisone is a metabolite belonging to the corticosteroid class that is used pharmaceutically directly as a drug or prodrug. In addition to its large consumption, its use is linked to several side effects, so pharmaceutical research aims to develop effective drugs with low or no side effects, alternative compounds to cortisone are part of an active investment in ongoing research on drug discovery. Since biotransformation can be considered a source of new molecules with potential therapeutic use, the present work focuses on a preliminary in vitro study aimed at evaluating the mutagenic, anti-inflammatory, antioxidant and neuroprotective activity of SCA and SCB molecules obtained from the biotransformation of cortisone using Rh. Rhodnii strain DSM 43960. The results obtained are very encouraging due to the safety of biotransformed compounds with reference to genotoxicity checked by Ames test, to the very high antioxidant capacity and to the anti-inflammatory activity. In fact, thecompounds inhibited both the TNFα-stimulated expression and secretion of NFkB target cytokines, and COX activity, and can activate the glucocorticoid receptor. Finally SCA and SCB exhibited neuroprotective properties.

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Section: Resultsmentioning

confidence: 99%

Biological activity of new bioactive steroids deriving from biotransformation of cortisone

et al. 2022

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“…Positive controls were used with and without the mammalian microsomal enzyme test (S9). The Ames test was conducted as previously described with modifications ( Mello Silva Oliveira et al, 2016 ; Wahab et al, 2018 ; Fan et al, 2022 ). The experiments were performed in triplicate.…”

Section: Methodsmentioning

confidence: 99%

Safety and efficacy evaluation of halicin as an effective drug for inhibiting intestinal infections

Zhang,

Lin,

Han

et al. 2024

Front. Pharmacol.

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Halicin, the first antibacterial agent discovered by artificial intelligence, exerts broad-spectrum antibacterial effects and has a unique structure. Our study found that halicin had a good inhibitory effect on clinical isolates of drug-resistant strains and Clostridium perfringens (C. perfringens). The safety of halicin was evaluated by acute oral toxicity, genotoxicity and subchronic toxicity studies. The results of acute toxicity test indicated that halicin, as a low-toxicity compound, had an LD50 of 2018.3 mg/kg. The results of sperm malformation, bone marrow chromosome aberration and cell micronucleus tests showed that halicin had no obvious genotoxicity. However, the results of the 90-day subchronic toxicity test indicated that the test rats exhibited weight loss and slight renal inflammation at a high dose of 201.8 mg/kg. Teratogenicity of zebrafish embryos showed that halicin had no significant teratogenicity. Analysis of intestinal microbiota showed that halicin had a significant effect on the intestinal microbial composition, but caused a faster recovery. Furthermore, drug metabolism experiments showed that halicin was poorly absorbed and quickly eliminated in vivo. Our study found that halicin had a good therapeutic effect on intestinal infection model of C. perfringens. These results show the feasibility of developing oral halicin as a clinical candidate drug for treating intestinal infections.

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“…Substation mutations are 20 times more common on the Lagging strand than the Leading strand, according to previous research on the auxotroph's P. mirabilis. Substation mutations can arise either spontaneously as the result of a DNA polymerase III replication error or as a result of physical or chemical influences [14]. The rate of bacterial mutations is typically increased by these genetic alterations, which encourages the accumulation of dangerous alleles.…”

Section: Dna Sequence Of Mete Genementioning

confidence: 99%

Design of a Test to Identify Mutagenic Effects of Hair Dye using Proteus mirabilis

Hezam

Yousif

Mohammed

2023

IOP Conf. Ser.: Earth Environ. Sci.

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The purpose of this study was to determine the possible mutagenicity of hair dye using the auxotroph’s methionine Proteus Mirabilis as a test. The Ames test was employed to identify reverse mutations in auxotroph’s P. Mirabilis treated with hair dyes. The results demonstrated a significant increase (P< 0.05) in reverse colonies of auxotroph’s P. mirabilis treated with 250 and 500 mg/mL of hair dyes in comparison to the negative control. Reverse mutations in the metE gene of the auxotroph’s P. Mirabilis were identified using DNA sequencing and polymerase chain reaction. The results confirmed the presence of the metE gene at a percentage of (100%) in all isolates treated with hair dyes at 250 and 500 mg/mL. Using BLAST software, the metE gene’s sequence was compared to the gene sequence of a standard isolate. Point mutations in the DNA of the metE gene altered protein translation, according to a genetic study of metE gene isolates treated with hair dyes. Finally, point mutations in the metE genes were identified using amino acid translation analysis of auxotroph’s P. mirabilis isolates treated with hair dyes. Point mutations in the metE gene cause many amino acids to be converted to methionine, which enables auxotroph’s P. mirabilis to grow without the need for methionine from an external source. The study found that the test for identifying mutagens in hair dyes was simple to use and cheap. It has also shown high efficacy in altering the amino acid and nitrogenous base sequences in the metE genes, thus their effect on methionine synthesis.

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Acute, subacute oral toxicity and Ames test of Py-mulin: an antibacterial drug candidate

Cited by 13 publications

References 27 publications

Biological activity of new bioactive steroids deriving from biotransformation of cortisone

Biological activity of new bioactive steroids deriving from biotransformation of cortisone

Safety and efficacy evaluation of halicin as an effective drug for inhibiting intestinal infections

Design of a Test to Identify Mutagenic Effects of Hair Dye using Proteus mirabilis

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