This review summarizes data on the in vitro antimicrobial effectiveness of volatile agents of plant origin and in vitro methods for evaluating their activity in the vapour phase. As a result of literature analysis, the antimicrobial efficacy of vapours from 122 different plant species and 19 pure compounds examined in 61 studies using different in vitro tests against a broad spectrum of microorganisms was identified and summarized. In addition, 11 different techniques found in the literature are described in detail. An original classification of methods based on the solid and liquid matrix volatilization principle is proposed because carrier medium/matrix selection is crucial for the volatilization of any agents tested. This review should be useful for medicinal, pharmaceutical, food, and agricultural experts working in areas related to the management of infectious diseases (especially respiratory and skin infections), food preservation (active packaging), and protection of agriculture products (controlled atmosphere). It may also stimulate the interest of pharmaceutical, cosmetic, food, and agriculture industries in the research and development of new antimicrobial agents of natural origin. Since several original apparatuses previously developed for antimicrobial susceptibility testing in the vapour phase are described in this review, labware manufacturers may also be interested in this topic. The review also provides specific guidelines and recommendations for researchers studying the antimicrobial activity of volatile agents. The article will therefore appeal to communities of industrial stakeholders, pharmacists, physicians, food experts, agriculturists, and researchers in related areas such as pharmacology, medicinal chemistry, microbiology, natural product chemistry, food preservation and plant protection.
- MeSH
- antibakteriální látky MeSH
- antiinfekční látky * MeSH
- konzervace potravin MeSH
- volatilizace MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
- Názvy látek
- antibakteriální látky MeSH
- antiinfekční látky * MeSH
The dietary intake of flavonoids seems to be inversely related to cardiovascular mortality. The consumption of isoflavonoids is increasing in the general population, especially due to the use of food supplements and a variety of isoflavonoid-rich foods. However, detailed studies on the vascular influence of individual pure isoflavonoids are mostly missing. For this study, 16 isoflavonoids were initially screened for their vasorelaxant properties on rat aortas. The 2 most potent of them, biochanin A and glycitein, were further tested for the mechanism of action on porcine coronary arteries. They both induced an endothelium independent vascular relaxation, with EC50 below 6 and 17 µM, respectively. Biochanin A, but not glycitein, was able to block the vasoconstriction caused by KCl, CaCl2, serotonin, and U46619 in a dose-dependent manner. Another series of experiments suggested that the major mechanism of action of biochanin A was the inhibition of L-type calcium channels. Moreover, biochanin A in relatively small concentrations (2 - 4 µM) interfered with the cGMP, but not cAMP, pathway in isolated coronary arteries. These results indicate that some isoflavonoids, in particular biochanin A, are able to have vasodilatory effects in micromolar concentrations, which is of potential clinical interest for the management of cardiovascular pathologies.
- MeSH
- cévní endotel MeSH
- genistein MeSH
- isoflavony * MeSH
- koronární cévy MeSH
- krysa rodu Rattus MeSH
- lidé MeSH
- prasata MeSH
- vápník MeSH
- vápníkové kanály * MeSH
- vazodilatace MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- biochanin A MeSH Prohlížeč
- genistein MeSH
- isoflavony * MeSH
- vápník MeSH
- vápníkové kanály * MeSH
Scoparone, a major constituent of the Chinese herbal medicine Yin Chen Hao, expresses beneficial effects in experimental models of various diseases. The intrinsic doses and effects of scoparone are dependent on its metabolism, both in humans and animals. We evaluated in detail the metabolism of scoparone in human, mouse, rat, pig, dog, and rabbit liver microsomes in vitro and in humans in vivo. Oxidation of scoparone to isoscopoletin via 6-O-demethylation was the major metabolic pathway in liver microsomes from humans, mouse, rat, pig and dog, whereas 7-O-demethylation to scopoletin was the main reaction in rabbit. The scoparone oxidation rates in liver microsomes were 0.8 - 1.2 µmol/(min*g protein) in mouse, pig, and rabbit, 0.2 - 0.4 µmol/(min*g protein) in man and dog, and less than 0.1 µmol/(min*g) in rat. In liver microsomes of all species, isoscopoletin was oxidized to 3-[4-methoxy-ρ-(3, 6)-benzoquinone]-2-propenoate and esculetin, which was formed also in the oxidation of scopoletin. Human CYP2A13 exhibited the highest rate of isoscopoletin and scopoletin oxidation, followed by CYP1A1 and CYP1A2. Glucuronidation of isoscopoletin and scopoletin was catalyzed by the human UGT1A1, UGT1A6, UGT1A7, UGT1A8, UGT1A9, UGT1A10, and UGT2B17. Dog was most similar to man in scoparone metabolism. Isoscopoletin glucuronide and sulfate conjugates were the major scoparone in vivo metabolites in humans, and they were completely excreted within 24 h in urine. Scoparone and its metabolites did not activate key nuclear receptors regulating CYP and UGT enzymes. These results outline comprehensively the metabolic pathways of scoparone in man and key preclinical animal species.
- MeSH
- jaterní mikrozomy metabolismus MeSH
- králíci MeSH
- krysa rodu Rattus MeSH
- kumariny metabolismus farmakokinetika MeSH
- léky rostlinné čínské metabolismus farmakokinetika MeSH
- lidé MeSH
- myši inbrední DBA MeSH
- myši MeSH
- oxidace-redukce MeSH
- potkani Wistar MeSH
- prasata MeSH
- psi MeSH
- zvířata MeSH
- Check Tag
- králíci MeSH
- krysa rodu Rattus MeSH
- lidé MeSH
- mužské pohlaví MeSH
- myši MeSH
- psi MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- kumariny MeSH
- léky rostlinné čínské MeSH
- scoparone MeSH Prohlížeč
An advanced Mendelian Cannabis breeding program has been developed utilizing chemical markers to maximize the yield of phytocannabinoids and terpenoids with the aim to improve therapeutic efficacy and safety. Cannabis is often divided into several categories based on cannabinoid content. Type I, Δ9-tetrahydrocannabinol-predominant, is the prevalent offering in both medical and recreational marketplaces. In recent years, the therapeutic benefits of cannabidiol have been better recognized, leading to the promotion of additional chemovars: Type II, Cannabis that contains both Δ9-tetrahydrocannabinol and cannabidiol, and cannabidiol-predominant Type III Cannabis. While high-Δ9-tetrahydrocannabinol and high-myrcene chemovars dominate markets, these may not be optimal for patients who require distinct chemical profiles to achieve symptomatic relief. Type II Cannabis chemovars that display cannabidiol- and terpenoid-rich profiles have the potential to improve both efficacy and minimize adverse events associated with Δ9-tetrahydrocannabinol exposure. Cannabis samples were analyzed for cannabinoid and terpenoid content, and analytical results are presented via PhytoFacts, a patent-pending method of graphically displaying phytocannabinoid and terpenoid content, as well as scent, taste, and subjective therapeutic effect data. Examples from the breeding program are highlighted and include Type I, II, and III Cannabis chemovars, those highly potent in terpenoids in general, or single components, for example, limonene, pinene, terpinolene, and linalool. Additionally, it is demonstrated how Type I - III chemovars have been developed with conserved terpenoid proportions. Specific chemovars may produce enhanced analgesia, anti-inflammatory, anticonvulsant, antidepressant, and anti-anxiety effects, while simultaneously reducing sequelae of Δ9-tetrahydrocannabinol such as panic, toxic psychosis, and short-term memory impairment.
- MeSH
- biologické markery metabolismus MeSH
- Cannabis genetika metabolismus MeSH
- kanabidiol metabolismus MeSH
- kanabinoidy biosyntéza farmakologie MeSH
- šlechtění rostlin MeSH
- tetrahydrokanabinol analogy a deriváty metabolismus MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- biologické markery MeSH
- delta(9-11)-tetrahydrocannabinol MeSH Prohlížeč
- kanabidiol MeSH
- kanabinoidy MeSH
- tetrahydrokanabinol MeSH
Boldine is an aporphine alkaloid widely consumed in the folk medicine of some regions. Its anticancer potential has been shown but not yet elucidated. We compared the antitumor effect of orally and parenterally applied boldine in mice bearing solid Ehrlich tumor. We also explored the effects of boldine on breast adenocarcinoma MCF-7 cells in vitro. Repeated i. p. injections of 30, 60, or 90 mg boldine/kg, either alone or combined with doxorubicin, slowed tumor growth in vivo. The latter two doses also prolonged the post-therapeutic survival of the mice. When fed food supplemented with boldine at a dose of 90 mg/kg, the tumor-bearing mice survived significantly longer, but there was no effect on tumor size. Interestingly, continuous p. o. administration did not produce detectable levels of boldine in plasma or tissue samples, in contrast to high but short-lived concentrations after i. p. injections. There was neither antagonism nor synergism between boldine and doxorubicin, except a possible synergism of i. p. boldine 90 mg/kg combined with doxorubicin when compared with doxorubicin alone.Boldine was cytotoxic to MCF-7 cells and reduced their viability and proliferation in vitro. Exposure to boldine decreased bromodeoxyuridine incorporation and histone H3 phosphorylation but did not induce apoptosis. Boldine treatment resulted in p38, ERK, and JNK activation in the mitogen-activated protein kinase pathway in a dose-dependent manner. Since bioavailability in mice seems to be different from that reported in rats, pharmacokinetic studies in humans are needed to evaluate the role of boldine in the beneficial effects of Boldo infusions.
- MeSH
- adenokarcinom farmakoterapie MeSH
- antioxidancia farmakologie terapeutické užití MeSH
- aporfiny farmakologie terapeutické užití MeSH
- doxorubicin MeSH
- experimentální nádory mléčných žláz farmakoterapie MeSH
- fytoterapie MeSH
- lidé MeSH
- MFC-7 buňky MeSH
- myši MeSH
- screeningové testy protinádorových léčiv MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- myši MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- antioxidancia MeSH
- aporfiny MeSH
- boldine MeSH Prohlížeč
- doxorubicin MeSH
Steroidal glycoalkaloids present in Solanaceae are toxic compounds biosynthesised for the protection of the plants. However, many health benefits of these compounds have been reported so far. One of their promising targets might be cancer, as demonstrated in a large number of studies. However, the main mechanism of action seems to be unclear. It could include the induction of apoptosis or trigger a necrosis with a subsequent inflammatory response. The relatively high systemic toxicity of steroidal compounds is another effect that must be taken into account in anticancer research. The main aim of this work was to summarise the recent progress in the investigation of the mechanisms of their antitumour action and to discuss their potential.
- MeSH
- alkaloidy Solanaceí izolace a purifikace farmakologie toxicita MeSH
- fytogenní protinádorové látky izolace a purifikace farmakologie toxicita MeSH
- lidé MeSH
- rostlinné extrakty izolace a purifikace farmakologie toxicita MeSH
- Solanaceae chemie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- přehledy MeSH
- Názvy látek
- alkaloidy Solanaceí MeSH
- fytogenní protinádorové látky MeSH
- rostlinné extrakty MeSH
Essential oil from the leaves of Myrica rubra, a subtropical Asian fruit tree traditionally used in folk medicines, has a significant antiproliferative effect in several intestinal cancer cell lines. Doxorubicin belongs to the most important cytostatics used in cancer therapy. The present study was designed to evaluate the effects of defined essential oil from M. rubra leaves on efficacy, prooxidative effect, and accumulation of doxorubicin in cancer cell lines and in non-cancerous cells. For this purpose, intestinal adenocarcinoma CaCo2 cells were used. Human fibroblasts (periodontal ligament) and a primary culture of rat hepatocytes served as models of non-cancerous cells. The results showed that the sole essential oil from M. rubra has a strong prooxidative effect in cancer cells while it acts as a mild antioxidant in hepatocytes. Combined with doxorubicin, the essential oil enhanced the antiproliferative and prooxidative effects of doxorubicin in cancer cells. At higher concentrations, synergism of doxorubicin and essential oil from M. rubra was proved. In non-cancerous cells, the essential oil did not affect the toxicity of doxorubicin and the doxorubicin-mediated reactive oxygen species formation. The essential oil increased the intracellular concentration of doxorubicin and enhanced selectively the doxorubicin accumulation in nuclei of cancer cells. Taken together, essential oil from M. rubra leaves could be able to improve the doxorubicin efficacy in cancer cells due to an increased reactive oxygen species production, and the doxorubicin accumulation in nuclei of cancer cells.
- MeSH
- Caco-2 buňky MeSH
- doxorubicin farmakologie MeSH
- fytogenní protinádorové látky farmakologie MeSH
- hepatocyty účinky léků MeSH
- krysa rodu Rattus MeSH
- kultivované buňky MeSH
- lidé MeSH
- Myrica chemie MeSH
- oleje prchavé farmakologie MeSH
- potkani Wistar MeSH
- proliferace buněk účinky léků MeSH
- reaktivní formy kyslíku metabolismus MeSH
- rostlinné extrakty farmakologie MeSH
- střevní nádory MeSH
- synergismus léků MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- lidé MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- doxorubicin MeSH
- fytogenní protinádorové látky MeSH
- oleje prchavé MeSH
- reaktivní formy kyslíku MeSH
- rostlinné extrakty MeSH
Flavonoids, important components of human diet, have been claimed to possess a significant antiplatelet potential, in particular due to their effects on the arachidonic acid cascade. Due to variable and incomplete results, this study was aimed at delivering a detailed analysis of the effects of 29 structurally relevant, mainly natural flavonoids on three consecutive steps of the arachidonic acid cascade.Only the isoflavonoids genistein and daidzein were shown to possess a marked cyclooxygenase-1 inhibitory activity, which was higher than that of acetylsalicylic acid using the isolated ovine enzyme, and physiologically relevant, although lower than acetylsalicylic acid in human platelets. None of the tested flavonoids possesses an effect on thromboxane synthase in a clinically achievable concentration. Contrarily, many flavonoids, particularly those possessing an isolated 7-hydroxyl group and/or a 4'-hydroxyl group, acted as antagonists on thromboxane receptors. Interestingly, the substitution of the free 7-hydroxyl group by glucose might not abolish the activity.In conclusion, the consumption of few flavonoids in a diet, particularly of the isoflavonoids genistein and daidzein, may positively influence platelet aggregation.
- MeSH
- cyklooxygenasa 1 metabolismus MeSH
- flavonoidy chemie farmakologie MeSH
- inhibitory agregace trombocytů chemie farmakologie MeSH
- inhibitory cyklooxygenasy farmakologie MeSH
- kyselina arachidonová antagonisté a inhibitory metabolismus MeSH
- lidé MeSH
- receptory thromboxanů antagonisté a inhibitory MeSH
- thromboxan-A-synthasa antagonisté a inhibitory MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- cyklooxygenasa 1 MeSH
- flavonoidy MeSH
- inhibitory agregace trombocytů MeSH
- inhibitory cyklooxygenasy MeSH
- kyselina arachidonová MeSH
- receptory thromboxanů MeSH
- thromboxan-A-synthasa MeSH
Inhibition of the cardiac human ether-a-go-go-related gene channel is a problematic off-target pharmacological activity and, hence, a major safety liability in clinical practice. Several non-cardiac drugs have been restricted in their use, or even removed from the market due to this potentially fatal adverse effect. Comparatively little is known about the human ether-a-go-go-related gene inhibitory potential of plant-derived compounds. In the course of an ongoing human ether-a-go-go-related gene in vitro study, a total of 32 structurally diverse alkaloids of plant origin as well as two semi-synthetically obtained protoberberine derivatives were screened by means of an automated Xenopus oocyte assay. Protopine, (+)-bulbocapnine, (+)-N-methyllaurotetanine, (+)-boldine, (+)-chelidonine, (+)-corynoline, reserpine, and yohimbine reduced the human ether-a-go-go-related gene current by ≥ 50% at 100 µM, and were submitted to concentration-response experiments. Our data show that some widely occurring plant-derived alkaloids carry a potential risk for human ether-a-go-go-related gene toxicity.
- MeSH
- akční potenciály účinky léků MeSH
- alkaloidy farmakologie MeSH
- berberinové alkaloidy farmakologie MeSH
- biologické přípravky farmakologie MeSH
- blokátory draslíkových kanálů farmakologie MeSH
- draslíkové kanály ether-a-go-go antagonisté a inhibitory MeSH
- inhibiční koncentrace 50 MeSH
- lidé MeSH
- metoda terčíkového zámku MeSH
- oocyty MeSH
- Xenopus laevis MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- alkaloidy MeSH
- berberinové alkaloidy MeSH
- biologické přípravky MeSH
- blokátory draslíkových kanálů MeSH
- draslíkové kanály ether-a-go-go MeSH
- KCNH1 protein, human MeSH Prohlížeč
- protoberberine MeSH Prohlížeč
