The bacterium is one of the main causes of chronic gastritis, peptic ulcers, and even gastric cancer. It affects an average of half of the world population. Its difficult eradication depends upon multi-drug therapy. Since its classification as a group 1 carcinogenic by International Agency for Research on Cancer (IARC), the importance of eradication has obtained a novel meaning. There is considerable interest in alternative therapies for the eradication of using compounds from a wide range of natural products. In the present study, we investigated the antibacterial property of the isocoumarin paepalantine against and it exhibited significant anti- activity at a minimum inhibitory concentration (MIC) of 128 μg/mL and at a minimum bactericidal concentration (MBC) of 256 μg/mL. The scanning electron microscopy (SEM) revealed significant morphological changes of the bacterial cell as a response to a sub-MIC of paepalantine, suggesting a penicillin-binding protein (PBP) inhibition. Computational studies were carried out in order to study binding modes for paepalantine in PBP binding sites, exploring the active and allosteric sites. The data from the present study indicates that paepalantine exhibits significant anti- activity, most likely by inhibiting membrane protein synthesis.
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http://dx.doi.org/10.3390/molecules22050786 | DOI Listing |
Nat Prod Res
April 2020
Key Laboratory of Tropical Biological Resources of Ministry of Education, College of Material and Chemical Engineering, Hainan University, Haikou, P. R. China.
A new isocoumarin derivative pestalotiopisorin B (), along with six known compounds, ()-(-)- mellein methyl ether (), pestalotiopyrone G (), ()-mevalonolactone (), pestalotiollides A-B () and pestalotiopsol A() were isolated from sp., an endophytic fungus obtained from Chinese mangrove plant Their structures were elucidated unambiguously by the comprehensive analysis of extensive spectroscopic data. Compound exhibited modest antibacterial activity against and with 12.
View Article and Find Full Text PDFBiomed Pharmacother
November 2018
Graduate Program in Pharmaceutical Sciences, Federal University of Espirito Santo - UFES, Avenida Marechal Campos 1468, 29047-105 Vitória, ES, Brazil; Department of Pharmaceutical Sciences, Federal University of Espirito Santo - UFES, Avenida Marechal Campos 1468, 29047-105 Vitória, ES, Brazil. Electronic address:
The naphthopyranones paepalantine and 5-methoxy-3,4-dehydroxanthomegnin isolated from Paepalanthus sp, showed in previous studies antioxidant, anti-inflammatory, antitumour and antimicrobial potential, such as anti-Helicobacter pylori activity. H. pylori infection is one of the main causes of gastric cancer, causing an excessive inflammatory response through the neutrophils and macrophages infiltration, increasing the release of reactive species and thus inducing the production of pro-inflammatory mediators.
View Article and Find Full Text PDFMolecules
May 2017
Graduate Program in Pharmaceutical Sciences, Federal University of Espirito Santo-UFES, Marechal Campos Av., 1468, Vitoria 29043-900, ES, Brazil.
The bacterium is one of the main causes of chronic gastritis, peptic ulcers, and even gastric cancer. It affects an average of half of the world population. Its difficult eradication depends upon multi-drug therapy.
View Article and Find Full Text PDFBioorg Med Chem Lett
October 2011
Instituto de Ciências Biológicas e Naturais, Universidade Federal do Triângulo Mineiro, Uberaba, MG, Brazil.
Human kallikrein 5 and 7 (KLK5 and KLK7) are trypsin-like and chymotrypsin-like serine proteases, respectively, and promising targets for the treatment of skin desquamation, inflammation and cancer. In an effort to develop new inhibitors for these enzymes, we carried out enzymatic inhibition assays and docking studies with three isocoumarin compounds. Some promising inhibitors were uncovered, with vioxanthin and 8,8'-paepalantine being the most potent competitive inhibitors of KLK5 (K(i)=22.
View Article and Find Full Text PDFPhytochemistry
April 2007
Instituto de Química de Araraquara, Universidade Estadual Paulista, Araraquara, SP, Brazil.
The isocoumarins (1-50 microM) paepalantine (9,10-dihydroxy-5,7-dimethoxy-1H-naptho(2,3c)pyran-1-one), 8,8'-paepalantine dimer, and vioxanthin isolated from Paepalanthus bromelioides, were assessed for antioxidant activity using isolated rat liver mitochondria and non-mitochondrial systems, and compared with the flavonoid quercetin. The paepalantine and paepalantine dimers, but not vioxanthin, were effective at scavenging both 1,1-diphenyl-2-picrylhydrazyl (DPPH(*)) and superoxide (O(2)(-)) radicals in non-mitochondrial systems, and protected mitochondria from tert-butylhydroperoxide-induced H(2)O(2) accumulation and Fe(2+)-citrate-mediated mitochondrial membrane lipid peroxidation, with almost the same potency as quercetin. These results point towards paepalantine, followed by paepalantine dimer, as being a powerful agent affording protection, apparently via O(2)(-) scavenging, from oxidative stress conditions imposed on mitochondria, the main intracellular source and target of those reactive oxygen species.
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