ETHNOPHARMACOLOGICAL RELEVANCE: Paulownia tomentosa Steud. (P. tomentosa) is a medium-sized tree traditionally used in Chinese folk medicine for the treatment of infectious diseases. It is a rich source of prenylated phenolic compounds that have been extensively studied for their promising biological activities. AIM OF THE STUDY: Due to the increasing development of antibiotic resistance, our study investigated plant-derived natural products from the fruits of P. tomentosa that could control Staphylococcus aureus infections with novel targets/modes of action and reduce antimicrobial resistance. MATERIALS AND METHODS: The ethanolic extract was fractionated and detected by liquid chromatography. The antistaphylococcal effects of the plant formulations were studied in detail in vitro by various biological methods, including microdilution methods for minimum inhibitory concentration (MIC), the checkerboard titration technique for synergy assay, fluorescence measurements for membrane disruption experiments, autoinducer-2-mediated bioassay for quorum sensing inhibition, and counting of colony-forming units for relative adhesion. Morphology was examined by transmission electron microscopy. RESULTS: Total ethanolic extract and chloroform fraction showed MICs of 128 and 32 μg/mL, respectively. Diplacol, diplacone, and 3'-O-methyl-5'-hydroxydiplacone inhibited S. aureus growth in the range of 8-16 μg/mL. Synergistic potential was shown in combination with mupirocin and fusidic acid. The ethanolic extract and the chloroform fraction destroyed the cell membranes by 91.61% and 79.46%, respectively, while the pure compounds were less active. The ethanolic extract and the pure compounds reduced the number of adhered cells to 47.33-10.26% compared to the untreated control. All tested plant formulations, except diplacone, inhibited quorum sensing of S. aureus. Transmission electron microscopy showed deformation of S. aureus cells. CONCLUSIONS: The products from the fruit of P. tomentosa showed antimicrobial properties against S. aureus alone and in combination with antibiotics. By affecting intracellular targets, geranylated flavonoids proposed novel approaches in the control of staphylococcal infections.
- MeSH
- antibakteriální látky chemie MeSH
- antiinfekční látky * farmakologie MeSH
- chloroform MeSH
- ethanol farmakologie MeSH
- hluchavkotvaré * MeSH
- mikrobiální testy citlivosti MeSH
- ovoce chemie MeSH
- rostlinné extrakty chemie MeSH
- stafylokokové infekce * MeSH
- Staphylococcus aureus MeSH
- Publikační typ
- časopisecké články MeSH
Epilepsy is a neurological disease characterized by recurrent seizures that can lead to uncontrollable muscle twitching, changes in sensitivity to sensory perceptions, and disorders of consciousness. Although modern medicine has effective antiepileptic drugs, the need for accessible and cost-effective medication is urgent, and products derived from plants could offer a solution. For this review, we have focused on natural compounds that have shown anticonvulsant activity in in vivo models of epilepsy at relevant doses. In some cases, the effects have been confirmed by clinical data. The results of our search are summarized in tables according to their molecular targets. We have critically evaluated the data we present, identified the most promising therapeutic candidates, and discussed these in the text. Their perspectives are supported by both pharmacokinetic properties and potential interactions. This review is intended to serve as a basis for future research into epilepsy and related disorders.
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
Benign prostatic hyperplasia affects men from the age of 40 and its prevalence increases with age. Millions of men worldwide suffer from this disease, with many of them choosing an alternative treatment approach using phytotherapeutics, which are available in the form of registered preparations or food supplements. These preparations contain extracts that have been tested in clinical studies. Many of these studies have been critically evaluated by systematic reviews and meta-analyses. Recent data shows that saw palmetto (Serenoa repens) has a significant effect. Other drugs used in the treatment of BPH/LUTS include stinging nettle, lycopene, pumpkin, pygeum and rye pollen. However, the results of studies cannot be extrapolated to specific products unless proper extraction techniques, phytochemical analysis and dosage have been followed. The present paper aims to provide an overview of the latest knowledge in the field of BPH/LUTS phytotherapy with an emphasis on the clinical effect, side effects, interactions and rational dosage.
Benigní hyperplazie prostaty sužuje muže již od věku 40 let a její prevalence vzrůstá s věkem. Na světě tímto onemocněním trpí miliony mužů a mnozí z nich volí alternativní léčebný přístup pomocí fytoterapeutik, která jsou dostupná ve formě registrovaných přípravků anebo doplňků stravy. Tyto přípravky obsahují extrakty drog, jež byly testovány v rámci klinických studií. Mnohé z těchto studií byly kriticky vyhodnoceny systematickými review a metaanalýzami. Z dostupných dat plyne, že signifikantní efekt vykazuje serenoa plazivá (Serenoa repens). Mezi další drogy používané v terapii BHP/LUTS patří kopřiva dvoudomá, lykopen, slivoň africká, tykev obecná a žitný pyl. Nicméně výsledky studií nelze extrapolovat do konkrétních produktů, pokud u nich nebyly dodrženy správné extrakční techniky, fytochemické analýzy a dávkování. Tento příspěvek si klade za cíl přehled nejnovějších poznatků z oblasti fytoterapie BHP/LUTS s důrazem na klinický efekt, nežádoucí účinky, interakce a racionální dávkování.
- MeSH
- Cucurbita chemie MeSH
- fytoterapie MeSH
- hyperplazie prostaty * farmakoterapie MeSH
- lidé MeSH
- lykopen chemie terapeutické užití MeSH
- Prunus africana chemie MeSH
- rostlinné extrakty * aplikace a dávkování terapeutické užití MeSH
- Serenoa chemie MeSH
- symptomy dolních močových cest farmakoterapie MeSH
- Urtica dioica chemie MeSH
- Check Tag
- lidé MeSH
Medicinal plants are rich sources of valuable molecules with various profitable biological effects, including antimicrobial activity. The advantages of herbal products are their effectiveness, relative safety based on research or extended traditional use, and accessibility without prescription. Extensive and irrational usage of antibiotics since their discovery in 1928 has led to the increasing expiration of their effectiveness due to antibacterial resistance. Now, medical research is facing a big and challenging mission to find effective and safe antimicrobial therapies to replace inactive drugs. Over the years, one of the research fields that remained the most available is the area of natural products: medicinal plants and their metabolites, which could serve as active substances to fight against microbes or be considered as models in drug design. This review presents selected flavonoids (such as apigenin, quercetin, kaempferol, kurarinone, and morin) and tannins (including oligomeric proanthocyanidins, gallotannins, ellagitannins, catechins, and epigallocatechin gallate), but also medicinal plants rich in these compounds as potential therapeutic agents in oral infectious diseases based on traditional usages such as Agrimonia eupatoria L., Hamamelis virginiana L., Matricaria chamomilla L., Vaccinium myrtillus L., Quercus robur L., Rosa gallica L., Rubus idaeus L., or Potentilla erecta (L.). Some of the presented compounds and extracts are already successfully used to maintain oral health, as the main or additive ingredient of toothpastes or mouthwashes. Others are promising for further research or future applications.
- MeSH
- antiinfekční látky * farmakologie terapeutické užití MeSH
- flavonoidy terapeutické užití MeSH
- hydrolyzovatelné taniny metabolismus MeSH
- infekční nemoci * MeSH
- léčivé rostliny * metabolismus MeSH
- rostlinné extrakty MeSH
- taniny metabolismus MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
Antimicrobial resistance is a public health threat and the increasing number of multidrug-resistant bacteria is a major concern worldwide. Common antibiotics are becoming ineffective for skin infections and wounds, making the search for new therapeutic options increasingly urgent. The present study aimed to investigate the antibacterial potential of prenylated phenolics in wound healing. Phenolic compounds isolated from the root bark of Morus alba L. were investigated for their antistaphylococcal potential both alone and in combination with commonly used antibiotics. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined by microdilution and agar method. Synergy was investigated using the checkerboard titration technique. Membrane-disrupting activity and efflux pump inhibition were evaluated to describe the potentiating effect. Prenylated phenolics inhibited bacterial growth of methicillin-resistant Staphylococcus aureus (MRSA) at lower concentrations (MIC 2-8 μg/ml) than commonly used antibiotics. The combination of active phenolics with kanamycin, oxacillin, and ciprofloxacin resulted in a decrease in the MIC of the antimicrobial agent. Kuwanon C, E, T, morusin, and albafuran C showed synergy (FICi 0.375-0.5) with oxacillin and/or kanamycin. Prenylated phenolics disrupted membrane permeability statistically significantly (from 28 ± 16.48% up to 73 ± 2.83%), and membrane disruption contributes to the complex antibacterial activity against MRSA. In addition, kuwanon C could be considered an efflux pump inhibitor. Despite the antibacterial effect on MRSA and the multiple biological activities, the prenylated phenolics at microbially significant concentrations have a minor effect on human keratinocyte (HaCaT) viability. In conclusion, prenylated phenolics in combination with commonly used antibiotics are promising candidates for the treatment of MRSA infections and wound healing, although further studies are needed.
- Publikační typ
- časopisecké články MeSH
Benigní hyperplazie prostaty sužuje muže již od věku 40 let a její prevalence vzrůstá s věkem. Na světě tímto onemocněním trpí miliony mužů a mnozí z nich volí alternativní léčebný přístup pomocí fytoterapeutik, která jsou dostupná ve formě registrovaných přípravků anebo doplňků stravy. Tyto přípravky obsahují extrakty drog, jež byly testovány v rámci klinických studií. Mnohé z těchto studií byly kriticky vyhodnoceny systematickými review a metaanalýzami. Z dostupných dat plyne, že signifikantní efekt vykazuje serenoa plazivá (Serenoa repens). Mezi další drogy používané v terapii BHP/LUTS patří kopřiva dvoudomá, lykopen, slivoň africká, tykev obecná a žitný pyl. Nicméně výsledky studií nelze extrapolovat do konkrétních produktů, pokud u nich nebyly dodrženy správné extrakční techniky, fytochemické analýzy a dávkování. Tento příspěvek si klade za cíl přehled nejnovějších poznatků z oblasti fytoterapie BHP/LUTS s důrazem na klinický efekt, nežádoucí účinky, interakce a racionální dávkování.
Benign prostatic hyperplasia affects men from the age of 40 and its prevalence increases with age. Millions of men worldwide suffer from this disease, with many of them choosing an alternative treatment approach using phytotherapeutics, which are available in the form of registered preparations or food supplements. These preparations contain extracts that have been tested in clinical studies. Many of these studies have been critically evaluated by systematic reviews and meta-analyses. Recent data shows that saw palmetto (Serenoa repens) has a significant effect. Other drugs used in the treatment of BPH/LUTS include stinging nettle, lycopene, pumpkin, pygeum and rye pollen. However, the results of studies cannot be extrapolated to specific products unless proper extraction techniques, phytochemical analysis and dosage have been followed. The present paper aims to provide an overview of the latest knowledge in the field of BPH/LUTS phytotherapy with an emphasis on the clinical effect, side effects, interactions and rational dosage.
- MeSH
- Cucurbita chemie MeSH
- fytoterapie MeSH
- hyperplazie prostaty * farmakoterapie MeSH
- lidé MeSH
- lykopen chemie terapeutické užití MeSH
- Prunus africana chemie MeSH
- rostlinné extrakty * aplikace a dávkování terapeutické užití MeSH
- Serenoa chemie MeSH
- symptomy dolních močových cest farmakoterapie MeSH
- Urtica dioica chemie MeSH
- Check Tag
- lidé MeSH
The review presents prenylated flavonoids as potential therapeutic agents for the treatment of topical skin infections and wounds, as they can restore the balance in the wound microenvironment. A thorough two-stage search of scientific papers published between 2000 and 2022 was conducted, with independent assessment of results by two reviewers. The main criteria were an MIC (minimum inhibitory concentration) of up to 32 μg/mL, a microdilution/macrodilution broth method according to CLSI (Clinical and Laboratory Standards Institute) or EUCAST (European Committee on Antimicrobial Susceptibility Testing), pathogens responsible for skin infections, and additional antioxidant, anti-inflammatory, and low cytotoxic effects. A total of 127 structurally diverse flavonoids showed promising antimicrobial activity against pathogens affecting wound healing, predominantly Staphylococcus aureus strains, but only artocarpin, diplacone, isobavachalcone, licochalcone A, sophoraflavanone G, and xanthohumol showed multiple activity, including antimicrobial, antioxidant, and anti-inflammatory along with low cytotoxicity important for wound healing. Although prenylated flavonoids appear to be promising in wound therapy of humans, and also animals, their activity was measured only in vitro and in vivo. Future studies are, therefore, needed to establish rational dosing according to MIC and MBC (minimum bactericidal concentration) values, test potential toxicity to human cells, measure healing kinetics, and consider formulation in smart drug release systems and/or delivery technologies to increase their bioavailability.
- MeSH
- antibakteriální látky farmakologie MeSH
- antiinfekční látky * farmakologie MeSH
- antioxidancia * farmakologie MeSH
- flavonoidy farmakologie MeSH
- hojení ran MeSH
- lidé MeSH
- mikrobiální testy citlivosti MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
Stále více pacientů vyhledává samoléčebné postupy, včetně fytoterapie, jejíž popularita neustále roste. Pacienti se mylně domnívají, že je užívání rostlinných přípravků naprosto bezpečné. Kromě možné toxicity samotné rostliny se zde objevuje i riziko lékových interakcí. Nejvíce ohroženou skupinou jsou lidé nad 65 let, pacienti s polyfarmacií, polymorbidní, případně se závažnými chronickými onemocněními. Nejnovější vědecké studie poukazují na rizika spojená s koadministrací grepu, ginkga, lékořice a třezalky s mnohými léčivy. Tyto interakce mohou mít až fatální následky, proto je orientace praktického lékaře v této problematice nezbytná. Jeho odborné zaměření spočívá v péči o pacienty s různými zdravotními potížemi a komplikacemi, proto tento příspěvek poukazuje na klinicky významné interakce rostlin s léčivy z různých farmakoterapeutických skupin.
More and more patients are choosing self-medication procedures, including phytotherapy whose popularity is constantly growing. Patients mistakenly believe that the use of herbal preparations is completely safe. In addition to the possible toxicity of the plant itself, there is also a risk of drug interactions. The ones most at risk are people over 65 years old, patients with polypharmacy, polymorbidity, or with severe chronic diseases. Recent scientific studies have highlighted the risks associated with the co-administration of grapefruit, ginkgo, licorice, and St. John's wort with many drugs. These interactions may have fatal consequences, so a general practitioner's competence in this issue is highly required. His or her professional focus is on the care of patients with various health problems and complications; accordingly, this paper presents clinically relevant interactions of herbal preparations with drugs from different pharmacotherapeutic groups.
Stále více pacientů vyhledává samoléčebné postupy, včetně fytoterapie, jejíž popularita neustále roste. Pacienti se mylně domnívají, že je užívání rostlinných přípravků naprosto bezpečné. Kromě možné toxicity samotné rostliny se zde objevuje i riziko lékových interakcí. Nejvíce ohroženou skupinou jsou lidé nad 65 let, pacienti s polyfarmacií, polymorbidní, případně se závažnými chronickými onemocněními. Nejnovější vědecké studie poukazují na rizika spojená s koadministrací grepu, ginkga, lékořice a třezalky s mnohými léčivy. Tyto interakce mohou mít až fatální následky, proto je orientace praktického lékaře v této problematice nezbytná. Jeho odborné zaměření spočívá v péči o pacienty s různými zdravotními potížemi a komplikacemi, proto tento příspěvek poukazuje na klinicky významné interakce rostlin s léčivy z různých farmakoterapeutických skupin.
More and more patients are choosing self-medication procedures, including phytotherapy whose popularity is constantly growing. Patients mistakenly believe that the use of herbal preparations is completely safe. In addition to the possible toxicity of the plant itself, there is also a risk of drug interactions. The ones most at risk are people over 65 years old, patients with polypharmacy, polymorbidity, or with severe chronic diseases. Recent scientific studies have highlighted the risks associated with the co-administration of grapefruit, ginkgo, licorice, and St. John's wort with many drugs. These interactions may have fatal consequences, so a general practitioner's competence in this issue is highly required. His or her professional focus is on the care of patients with various health problems and complications; accordingly, this paper presents clinically relevant interactions of herbal preparations with drugs from different pharmacotherapeutic groups.
BACKGROUND: The indole derivatives and the N-phenylpiperazine fragment represent interesting molecular moieties suitable for the research of new potentially biologically active compounds. This study was undertaken to identify if indol-2-carboxylic acid esters containing N-phenylpiperazine moiety possess acetylcholinesterase and butyrylcholinesterase inhibitory activity. MATERIALS AND METHODS: The study dealt with the synthesis of a novel series of analogs of 1H-indole-2- carboxylic acid and 3-methyl-1H-indole-2-carboxylic acid. The structure of the derivatives was represented by the indolylcarbonyloxyaminopropanol skeleton with the attached N-phenylpiperazine or diethylamine moiety, which formed a basic part of the molecule. The final products were synthesized as dihydrochloride salts, fumaric acid salts, and quaternary ammonium salts. The first step of the synthetic pathway led to the preparation of esters of 1H-indole-2-carboxylic acid from the commercially available 1H-indole-2-carboxylic acid. The Fischer indole synthesis was used to synthesize derivatives of 3-methyl-1H-indole-2-carboxylic acid. RESULTS AND DISCUSSION: Final 18 indolylcarbonyloxyaminopropanols in the form of dihydrochlorides, fumarates, and quaternary ammonium salts were prepared using various optimization ways. The very efficient way for the formation of 3-methyl-1H-indole-2-carboxylate (Fischer indole cyclization product) was the one-pot synthesis of phenylhydrazine with methyl 2-oxobutanoate with acetic acid and sulphuric acid as catalysts. CONCLUSION: Most of the derivatives comprised of an attached N-phenylpiperazine group, which formed a basic part of the molecule and in which the phenyl ring was substituted in position C-2 or C-4. The synthesized compounds were subjected to cholinesterase-inhibiting activity evaluation, by modified Ellman method. Quaternary ammonium salt of 1H-indole-2-carboxylic acid which contain N-phenylpiperazine fragment with nitro group in position C-4 (7c) demonstrated the most potent activity against acetylcholinesterase.
- MeSH
- acetylcholinesterasa chemie MeSH
- butyrylcholinesterasa chemie MeSH
- cholinesterasové inhibitory chemická syntéza chemie MeSH
- Electrophorus MeSH
- enzymatické testy MeSH
- estery chemická syntéza chemie MeSH
- indoly chemická syntéza chemie MeSH
- koně MeSH
- piperaziny chemická syntéza chemie MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
