Nejvíce citovaný článek - PubMed ID 26273725
Hydnocarpin-Type Flavonolignans: Semisynthesis and Inhibitory Effects on Staphylococcus aureus Biofilm Formation
Biofilm is a complex community of microorganisms residing within a polysaccharide and/or protein matrix. Biofilm can be produced by several microorganisms, including various bacteria and fungi. Nowadays, the resistance of biofilm-growing cells to antimicrobials originated from the structural nature of biofilms, and phenotypic alteration of sessile cells is becoming a global issue. Bacterial biofilms are important in various aspects of human health, including chronic infections, dental plaque, and infection of indwelling medical devices such as catheters. They are also a major problem in other industries, including oil recovery, drinking water distribution, papermaking, metalworking, and food processing. Estimates indicate that more than 80% of infectious diseases are biofilm-derived. The aim of this study is to describe mechanisms of antibiotic resistance to provide a better perspective on how to manage it. Moreover, the current strategies for biofilm inhibition were described. Considering that plants are a valuable source of abundant natural chemicals to create prophylactic and therapeutic medicines against biofilm-based infections, significant natural compounds with anti-biofilm properties were highlighted. Finally, natural anti-biofilm compounds under clinical trial evaluation were summarized to provide a background for more extensive researches and assist in opening a new window to novel treatments.
- MeSH
- antibakteriální látky farmakologie MeSH
- antiinfekční látky * MeSH
- Bacteria MeSH
- biofilmy * MeSH
- houby MeSH
- lidé MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
- Názvy látek
- antibakteriální látky MeSH
- antiinfekční látky * MeSH
The increase in antibiotic resistance among Gram-positive bacteria underscores the urgent need to develop new antibiotics. New antibiotics should target actively growing susceptible bacteria that are resistant to clinically accepted antibiotics including bacteria that are not growing or are protected in a biofilm environment. In this paper, we compare the in vitro activities of two new semisynthetic glycopeptide antibiotics, MA79 and ERJ390, with two clinically used glycopeptide antibiotics-vancomycin and teicoplanin. The new antibiotics effectively killed not only exponentially growing cells of Staphylococcus aureus, but also cells in the stationary growth phase and biofilm.
- Klíčová slova
- Staphylococcus aureus, antibiotic resistance, glycopeptide antibiotics, teicoplanin pseudoaglycon,
- Publikační typ
- časopisecké články MeSH
This review focuses on the specific biological effects of optically pure silymarin flavo-nolignans, mainly silybins A and B, isosilybins A and B, silychristins A and B, and their 2,3-dehydro derivatives. The chirality of these flavonolignans is also discussed in terms of their analysis, preparative separation and chemical reactions. We demonstrated the specific activities of the respective diastereomers of flavonolignans and also the enantiomers of their 2,3-dehydro derivatives in the 3D anisotropic systems typically represented by biological systems. In vivo, silymarin flavonolignans do not act as redox antioxidants, but they play a role as specific ligands of biological targets, according to the "lock-and-key" concept. Estrogenic, antidiabetic, anticancer, antiviral, and antiparasitic effects have been demonstrated in optically pure flavonolignans. Potential application of pure flavonolignans has also been shown in cardiovascular and neurological diseases. Inhibition of drug-metabolizing enzymes and modulation of multidrug resistance activity by these compounds are discussed in detail. The future of "silymarin applications" lies in the use of optically pure components that can be applied directly or used as valuable lead structures, and in the exploration of their true molecular effects.
- Klíčová slova
- Silybum marianum, chirality, dehydroflavonolignan, diastereomer, flavonoid, flavonolignan, isosilybin, milk thistle, silibinin, silybin, silychristin, silydianin, silymarin,
- MeSH
- antiinfekční látky chemie farmakologie MeSH
- antioxidancia chemie farmakologie MeSH
- fytogenní protinádorové látky chemie farmakologie MeSH
- lidé MeSH
- silibinin chemie farmakologie MeSH
- stereoizomerie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
- Názvy látek
- antiinfekční látky MeSH
- antioxidancia MeSH
- fytogenní protinádorové látky MeSH
- silibinin MeSH
Various Mitsunobu conditions were investigated for a series of flavonolignans (silybin A, silybin B, isosilybin A, and silychristin A) to achieve either selective esterification in position C-23 or dehydration in a one-pot reaction yielding the biologically important enantiomers of hydnocarpin D, hydnocarpin and isohydnocarpin, respectively. This represents the only one-pot semi-synthetic method to access these flavonolignans in high yields.
- Klíčová slova
- Mitsunobu, dehydration, flavonoid, hydnocarpin, silybin,
- Publikační typ
- časopisecké články MeSH