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In Vitro Selective Growth-Inhibitory Activities of Phytochemicals, Synthetic Phytochemical Analogs, and Antibiotics against Diarrheagenic/Probiotic Bacteria and Cancer/Normal Intestinal Cells.

ABSTRACT: A desirable attribute of novel antimicrobial agents for bacterial diarrhea is decreased toxicity toward host intestinal microbiota. In addition, gut dysbiosis is associated with an increased risk of developing intestinal cancer. In this study, the selective growth-inhibitory activities of ten phytochemicals and their synthetic analogs (berberine, bismuth subsalicylate, ferron, 8-hydroxyquinoline, chloroxine, nitroxoline, salicylic acid, sanguinarine, tannic acid, and zinc pyrithione), as well as those of six commercial antibiotics (ceftriaxone, ciprofloxacin, chloramphenicol, metronidazole, tetracycline, and vancomycin) against 21 intestinal pathogenic/probiotic (e.g., Salmonella spp. and bifidobacteria) bacterial strains and three intestinal cancer/normal (Caco-2, HT29, and FHs 74 Int) cell lines were examined in vitro using the broth microdilution method and thiazolyl blue tetrazolium bromide assay. Chloroxine, ciprofloxacin, nitroxoline, tetracycline, and zinc pyrithione exhibited the most potent selective growth-inhibitory activity against pathogens, whereas 8-hydroxyquinoline, chloroxine, nitroxoline, sanguinarine, and zinc pyrithione exhibited the highest cytotoxic activity against cancer cells. None of the tested antibiotics were cytotoxic to normal cells, whereas 8-hydroxyquinoline and sanguinarine exhibited selective antiproliferative activity against cancer cells. These findings indicate that 8-hydroxyquinoline alkaloids and metal-pyridine derivative complexes are chemical structures derived from plants with potential bioactive properties in terms of selective antibacterial and anticancer activities against diarrheagenic bacteria and intestinal cancer cells.

SUBMITTER: Kudera T

PROVIDER: S-EPMC7558399 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature

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In Vitro Selective Growth-Inhibitory Activities of Phytochemicals, Synthetic Phytochemical Analogs, and Antibiotics against Diarrheagenic/Probiotic Bacteria and Cancer/Normal Intestinal Cells.

Kudera Tomas T Doskocil Ivo I Salmonova Hana H Petrtyl Miloslav M Skrivanova Eva E Kokoska Ladislav L

Pharmaceuticals (Basel, Switzerland) 20200903 9

A desirable attribute of novel antimicrobial agents for bacterial diarrhea is decreased toxicity toward host intestinal microbiota. In addition, gut dysbiosis is associated with an increased risk of developing intestinal cancer. In this study, the selective growth-inhibitory activities of ten phytochemicals and their synthetic analogs (berberine, bismuth subsalicylate, ferron, 8-hydroxyquinoline, chloroxine, nitroxoline, salicylic acid, sanguinarine, tannic acid, and zinc pyrithione), as well as ...[more]

PMID: 32899218

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Project description:Hedychium flavum Roxb., a medicinal, edible, and ornamental plant, is widely cultivated throughout China, India, and Southeast Asia. The rhizome from this plant has been used for food flavoring and in traditional Chinese medicine to treat diverse diseases, but the detailed constituents and bioactivities are still limited known. Therefore, phytochemical analysis by GC-MS and UHPLC-Q-Orbitrap-MS, and antioxidant, antibacterial, cytotoxic, and enzyme inhibitory activities tests have been conducted in the current study. Based on the GC-MS results, the essential oil (EO) of rhizome was mainly composed of coronarin E (20.3%), β-pinene (16.8%), E-nerolidol (11.8%), and linalool (8.5%). Among them, coronarin E was reported in H. flavum EO firstly. Furthermore, the spectrophotometric indicated rhizome had high total phenolic content (TPC, 50.08-57.42 mg GAEs/g extract) and total flavonoid content (TFC, 12.45-21.83 mg REs/g extract), no matter in water extract (WE) or in 70% ethanol extract (EE). UHPLC-Q-Orbitrap-MS was applied to further characterize composition, and 86 compounds were putatively identified from WE and EE, including 13 phenolic components. For the bioactivities, both WE and EE showed remarkable antioxidant activity by DPPH and ABTS tests, being superior to the positive control (butylated hydroxytoluene, BTH). EO revealed significant antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, and Proteus vulgaris with DIZ (10.34-24.43 mm), MIC (78.13-312.50 μg/mL), and MBC (156.25-625.00 μg/mL). Moreover, EO exhibited a considerable selectivity to human tumor cell K562 (IC50 = 27.16 μg/mL), and its toxicity was more than 3.5-fold different from that of non-cancerous MRC-5 cell (IC50 = 95.96 μg/mL) and L929 cell (IC50 = 129.91 μg/mL). A series of apoptosis analysis demonstrated that EO induced apoptosis against K562 cells in a dose-dependent manner. In enzyme inhibitory effect assays, WE and EE showed strong α-glucosidase inhibition activity, being superior to the positive control (acarbose). Besides, the EO, WE, and EE didn't show a promising inhibition on tyrosinase (19.30-32.51 mg KAEs/g sample) and exhibited a weak inhibitory effect on cholinesterase. Based on the current results, H. flavum could be considered as a source of bioactive compounds and has high exploitation potential in the cosmetics, food, and pharmaceutical industries.

Project description:The aim of this work was to enrich the knowledge on the potential applications of Elaeagnus mollis leaf extracts. For this purpose, the bioactive compounds (phenolic, flavonoid, alkaloid, proanthocyanidin, chlorophyll and carotene content), antioxidant activity, anti-HepG2 cell proliferation, and cholinesterase inhibitory potential (AChE and BChE) of E. mollis leaves which obtained from different habitats were quantitatively analyzed using various solvents (water, methanol, ethanol, and n-hexane). The results showed that the methanol extracts exhibited the strongest 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity and the water extracts showed the best antioxidant activity in the 2,2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) free radical scavenging activity, ferric reducing antioxidant power (FRAP), and reducing power (RP) assays. Moreover, the methanol extracts showed the best inhibitory activity against cholinesterase and HepG2 cancer cells. Correlation analysis revealed that the high antioxidant and anti-HepG2 cell proliferation activities were mainly attributed to the total phenolics, flavonoids, and proanthocyanidins while AChE inhibition was attributed to the total alkaloid and carotene content. The statistical results showed that the effect of habitats was lower than that of different solvents used. Additionally, the metabolic profiles of E. mollis leaves were evaluated using HPLC-ESI-Q TRAP-MS/MS, and a total of 1,017 chemical components were detected and classified into 23 classes. The organic acids and derivatives ranked the first, followed by flavone, amino acid and derivatives, and so on. In conclusion, the effects of different solvents were more significant than the effects of different habitats and the methanol extracts of E. mollis leaves could be used as an effective source of functional active components, provide benefits to physical health care and be applied to the food and pharmaceutical industries.

Dataset Information

In Vitro Selective Growth-Inhibitory Activities of Phytochemicals, Synthetic Phytochemical Analogs, and Antibiotics against Diarrheagenic/Probiotic Bacteria and Cancer/Normal Intestinal Cells.

Publications

In Vitro Selective Growth-Inhibitory Activities of Phytochemicals, Synthetic Phytochemical Analogs, and Antibiotics against Diarrheagenic/Probiotic Bacteria and Cancer/Normal Intestinal Cells.

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