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Food supplements are concentrated sources of nutrients and/or other substances with a nutritional or physiological effect. However, they often contain herbal substances or their preparations. Food supplements belong to category of food and for that reason are regulated by food legislation. European Union regulations and directives established general directions for dietary supplements, dietetic food, which due to their special composition or manufacturing process are prepared for specific groups of people with special nutritional needs, and novel food/novel food ingredients to ensure product safety, suitability and appropriate consumer information.
Plant preparations, especially fractions of biologically active compounds may play an important role in improving the life quality of patients with diagnosed dementia as well as delaying the progress of neurodegenerative diseases through various mechanisms of pharmacological action. Recent years have brought a number of reports on the issue, nevertheless, it seems that there is still a lack of detailed, synthetical analysis. So far, main biological markers of Alzheimer’s disease pathogenesis which is currently the most common form of dementia, are the β-amyloid plaques deposits, neurofibrillary degeneration processes and atrophy of cholinergic neurons in the brain regions crucial for memory processes maintenance. At present, acetylcholinesterase inhibitors are the main drugs for the treatment of Alzheimer’s disease. In our previous review article, we pointed out the interesting mechanisms of action such as inhibition of acetyl-, butyrylcholinesterases and the antioxidant activity of bio-compounds of selected medicinal plants from Lamiaceae family (including rosmarinic acid). The aim of this paper is to systematize the knowledge about the influence of plant extracts and isolated natural compounds (e.g. cryptotanshinone, epigallocatechin gallate) on the pathway of β-amyloid formation and deposition in pharmacological models, especially by interacting with the brain enzyme, α- and β-, γ-secretase or on their genes expression. This is a long-established trend of research in search of new neuroprotective drugs from natural sources which raises new therapeutic hopes. Salvia miltiorrhiza and Camellia sinensis, medicinal plants from Asia, have interesting therapeutic potential in neurodegenerative disorders. In addition to them, there are known at least 10 Asian plants extensively researched in this area (e.g. Aralia cordata, Magnolia officinalis, Perilla frutescens, Polygala tenuifolia, Punica granatum, Sophora flavescens). However, due to the fact that many aspects of their phytochemical, neurochemical and pharmacological activities are not well known, further studies should be performed in this field.
In recent years, many herbal plants and their active components have been tested in different models of neurodegenerative diseases. Some studies are focused rather on studies of chemical compounds of plant origin than on plant extracts. Several natural polyphenols (i.e. flawonoids) are known to exhibit wide spectrum of beneficial effects on brain functioning and to protect against neurodegenerative processes [1, 2]. It seems that influence on β-amyloid is a promising point of pharmacological action of these plant components, because this protein is a major biological risk factor contributing to Alzheimer’s disease (AD)-associated cascade including severe neuronal loss in the brain regions key for memory. In this review the attention is paid to studies on interesting natural chemical compounds of flavonoids (i.g. luteolin, myricetin, icariin) which are a promising study material for research of the potential neuroprotective effects by decreasing the activity of β-secretase (BACE -1) leading to diminish the generation and deposition of β-amyloid (Aβ) in the central nervous system. This range is even more interesting because plant polyphenols can be included in healthy diet and in multi-target drug therapy of neurodegererative diseases.
Rozwój badań nad molekularnymi mechanizmami fitoterapii pozwala na coraz lepszą identyfikację mechanizmów neurochemicznych prowadzących do występowania interakcji pomiędzy lekami roślinnymi a syntetycznymi na poziomie receptorów ośrodkowego układu nerwowego (OUN). W naszej pracy podjęliśmy próbę podsumowania oraz krytycznej analizy doniesień o tego rodzaju interakcjach pomiędzy wybranymi roślinami leczniczymi: Ginkgo biloba (Ginkgo), Hypericum perforatum (St. John’s Worth) (część I cyklu artykułów), Valeriana officinalis (Valerian) oraz Panax ginseng (Ginseng) (część II) a lekami syntetycznymi (np. benzodiazepiny i barbiturany, opioidy) na poziomie receptorów OUN (między innymi: receptorów GABA-ergicznych, glutaminianergicznych, dopaminergicznych, adenozynowych) zarówno wynikających z badań in vitro, jak i z in vivo. Analiza danych bibliograficznych wykazała, że ginkgolidy oraz bilobalid wiążą się z receptorami GABA-ergicznymi (jako antagoniści niekompetycyjni), a także skracają czas snu indukowanego heksobarbitalem oraz uretanem. Inne badania pozwoliły na stwierdzenie, że hiperforyna, hiperycyna oraz amentoflawon wpływają na aktywność różnych receptorów ośrodkowego układu nerwowego (NMDA, DA, GABA, 5-HT). Kilka badań wykazało wiązanie kwasu walerenowego do receptorów GABA, co potwierdziło, że ekstrakty Valeriane radix mogą powodować interakcje z anestetykami, anksjolitykami oraz lekami uspokajającymi i nasennymi oraz mogą nasilać sedatywny efekt działania tych leków. Ponadto stwierdzono, że ginsenozydy mogą powodować interakcje z morfiną oraz apomorfiną na poziomie receptorów dopaminergicznych. Wydaje się, że w celu wyjaśnienia dokładnej natury receptorowych mechanizmów interakcji pomiędzy lekami roślinnymi a syntetycznymi konieczne jest przeprowadzenie dalszych badań neurochemicznych i farmakologicznych.
Choroba Alzheimera (AD) jest związaną z wiekiem, nieodwracalną chorobą neurodegeneracyjną, w przebiegu której dochodzi do postępujących zaburzeń funkcji poznawczych. Charakteryzuje się głównie obecnością w mózgu blaszek starczych, splątków neurofibrylarnych oraz deficytem neurotransmisji cholinergicznej (acetylocholiny). Zahamowanie aktywności acetylocholinoesterazy (AChE) jest uważane za obiecującą strategię w leczeniu chorób neurologicznych, nie tylko AD, lecz także w innych typach demencji (otępienie z ciałami Lewy’ego, otępienie w zespole Downa, otępienie naczyniowe, demencja w przebiegu choroby Parkinsona), ataksji oraz miastenii. W leczeniu zaburzeń funkcji poznawczych oraz utraty pamięci związanej z AD stosuje się kilka leków: takrynę, donepezil, rywastygminę oraz galantaminę, lecz związki te wykazują wiele działań niepożądanych. Aktualne badania dowodzą, że w metabolizm acetylocholiny w mózgu zaangażowane są zarówno AChE, jak i butyrylocholinoesteraza (BuChE), dlatego uważa się, że wpływ na aktywność obu tych enzymów może zwiększać efektywność terapii. Wykazano bowiem, że w mózgach pacjentów z chorobą Alzheimera paradoksalnie aktywność BuChE może się zwiekszać, w przeciwieństwie do zmniejszonego działania AChE. Wzrastające zainteresowanie i zapotrzebowanie na nowe leki przeciwneurodegeneracyjne uzasadnia prowadzenie badań nad poszukiwaniem związków chemicznych pochodzących również z roślin leczniczych. Celem niniejszego artykułu jest dokonanie przeglądu badań nad wybranymi roślinami leczniczymi z rodziny Lamiaceae (Rosmarinus officinalis, Salvia miltiorrhiza, Melissa officinalis) w zakresie ich działania w różnych modelach dotyczących choroby Alzheimera in vitro i in vivo.Wiadomo, że ekstrakty z omawianych roślin leczniczych z rodziny Lamiaceae nie tylko hamują aktywność AChE i odkładanie złogów β-amyloidu, lecz również mogą mieć działanie anty-BuChE. Wykazano, iż te wyciągi działały antyoksydacyjnie, cytoprotekcyjnie, antyapoptotycznie i przeciwzapalnie. Najbardziej aktywne były kwas rozmarynowy, flawonoidy (np. apigenina) i terpenoidy (np. citral, citronelal, tanszinony).
Flavonoids and their conjugates are the most important group of natural chemical compounds in drug discovery and development. The search for pharmacological activity and new mechanisms of activity of these chemical compounds, which may inhibit mediators of inflammation and influence the structure and function of endothelial cells, can be an interesting pharmacological strategy for the prevention and adjunctive treatments of hypertension, especially induced by pregnancy. Because cardiovascular diseases have multifactorial pathogenesis these natural chemical compounds with wide spectrum of biological activities are the most interesting source of new drugs. Extracts from one of the most popular plant used in Traditional Chinese Medicine, Scutellaria baicalensis Georgi could be a very interesting source of flavonoids because of its exact content in quercetin, apigenin, chrysin and scutellarin as well as in baicalin. These flavonoids exert vasoprotective properties and many activities such as: anti-oxidative via several pathways, anti-inflammatory, anti-ischaemic, cardioprotective and anti-hypertensive. However, there is lack of summaries of results of studies in context of potential and future application of flavonoids with determined composition and activity. Our review aims to provide a literature survey of in vitro, in vivo and ex vivo pharmacological studies of selected flavonoids (apigenin, chrysin and scutellarin, baicalin) in various models of hypertension carried out in 2008–2018.
The aim of this study was to investigate the influence of standardized Epilobium angustifolium L. extract [100 mg/kg/day, p.o.] on the expression level of 5α-reductase type 2 (Srd5ar2) mRNA and Mapk3 mRNA a representative of non-genomic xenobiotics signaling pathway. It was shown that plant extract from the E. angustifolium showed a slight tendency to reduce prostate weight in hormonally induced animals (p>0.05) and in testosterone induced animals receiving both, extract and finasteride (p<0.05). Finasteride in rats induced by testosterone caused a smaller decrease in the level of mRNA 5α-steroid reductase 2 (SRd5ar2), than in rats treated with the hormone and studied plant extracts. In general, an increase in the amount of MAPK3 mRNAs in testosterone-induced groups of rats receiving tested plant extract with or without finasteride was observed, while the expression of type 2 5α-steroid reductase decreased (p<0.05). Further experimental studies should be performed in order to understand the molecular basis of interactions, the efficacy and safety of tested plant extracts.
The aim of this study was to investigate the influence of standardized crude aqueous Epilobium angustifolium L. extract [100 mg/kg/day, p.o.] on the expression level of SRC kinase mRNA - a representatives of non-genomics xenobiotics signaling pathway in prostate ventral lobes of testosterone-induced, castrated rats. We have shown that in all analyzed groups induced by testosterone an elevation of SRC kinase mRNA transcription was observed, in comparison to control animals (not receiving the testosterone), (p<0.05). Finasteride in rats induced by testosterone caused the strongest inhibition of SRC mRNA transcription (p<0.05). In rats receiving testosterone and the plant extract a ca. 90% decrease of mRNA level was observed vs. testosterone-induced animals (p<0.05), while in testosterone-induced animals receiving concomitantly E. angustifolium extract and finasteride the observed reduction reached 87.3% (p<0.05). We did not observed, however, any positive feedback between studied plant extract and finasteride in the inhibitory activity (p<0.05). Further experimental studies should be performed in order to the understanding the molecular basis of interactions, the efficacy and safety of tested plant extract.
P-glycoprotein (P-gp) encoded by the MDR1 (multidrug resistance 1) gene is ATP-dependent transporting protein which is localizated in the cell membrane. P-gp is expressed Review Article 130 A. Bogacz, D. Deka-Pawlik, J. Bartkowiak-Wieczorek, M. Karasiewicz, R. Kujawski, A. Kowalska, A. Chałas, B. Czerny, E. Grześkowiak, P. M. Mrozikiewicz mainly in organs with the secretory functions and its physiological role concerns tissue protection against xenobiotics. P-glycoprotein is involved in the permeability barriers of the blood-brain, blood-placenta directly protecting these organs. It participates in the transport of many drugs and other xenobiotics affecting their absorption, distribution, metabolism and excretion. The high P-gp activity in the cell membranes of cancer tissue is a major cause of lack of effectiveness of chemotherapy. Hence, the methods which could increase the sensibility of these pathological cells to cytostatics are still being searched. In the experimental studies it was shown that natural plant substances may have an effect on the expression level and activity of P-glycoprotein. Hypericum perforatum, Ginkgo biloba and Camellia sinensis increase P-gp activity while curcumin from Curcuma longa, piperine and silymarin inhibit this protein. Taking into account a wide substrate spectrum of P-gp, application of our knowledge on interactions of herbals and synthetic drugs should be considered in order to improve drug impact on different tissues.
One of alternative strategies in prevention and therapy of Benign Prostatic Hyperplasia (BPH) is the usage of a number of traditional herbal plants. In recent years, there is an increasing interest in some members of the Epilobium genus in the treatment of BPH. So far there is no data about molecular mechanisms of action of Epilobium angustifolium L. extracts in liver. The aim of this study was to investigate the influence of the standardized water extract from the Epilobium angustifolium L. on expression level of selected P450 cytochromes encoding genes (CYP3A1 and CYP7A1) in rats liver tissues, which protein products are involved in steroids metabolism. The most abundant fraction of active compounds obtained from the extract was a phenolic fraction (24.36% m/m phenolic compounds and small amounts of flavonoglycosides – 0.91% and sterols – 0.09%). The plant extract showed the strongest and significant inhibitory CYP3A1/2 mRNA expression effect in rat liver. Our results suggest that a standardized E. angustifolium extract can regulate transcription level of investigated CYP genes in a different manner since a strong inhibition of CYP3A1 mRNA expression and slight induction of CYP7A1 may be a result of different extract action on the investigated CYP’s transcription machinery in rat liver cells.
As a consequence of ageing of populations and increase of life expectancy a growing interest in searching novel, safe and effective food preparations, plant origin dietary supplements or plant derived drugs, containing numerous substances that may counteract the emergence of age related disorders is observed. A clearly visible example of searching abovementioned herbal preparations is a growing interest among men suffering for urogenital disorders on preparations based in herbal plants such as: Serrenoa repens, Pygeum africanum, Urtica dioica, Cucurbita pepo, Hypoxis rooperi, Secale cereale, Zea mays. In recent years dietary supplements based on Epilobium genus representatives became very popular among patients with lower urinary tract symptoms (LUTS) and suffering for benign prostate hyperplasia (BPH). For the confirmation or justification of the use of preparations based on Epilobium sp. in folk medicine or diet supplementation we summarized the current knowledge on biological activities of herbal extracts and oils derived from this genus and variations of phytochemical compositions. The literature analysis reveals that herb was the substance most often subjected to phytochemical analysis (leaves or stems), the next one was seed oil of Epilobiium sp. representatives. In extracts from herb flavonoids (flavonol 3-O-glycosides based on kaempferol, quercetin, myricetin or guaiaverin aglycones), tannins (macrocyclic ellagitannins – oenothein A and B) and trace amounts of sterols as well as fatty acids were identified, while in extracts from seed oil sterols (β-sitosterol, kaempesterol, stigmasterol and brassicasterol) and fatty acids (mainly stearic, palmitic, oleic, linoleic, linolenic and caproic) were most often present. The conclusions of this paper may be helpful in further extensive research concerning the evaluation the effectiveness and safety of preparations based on the basis of Epilobium sp. and Onagraceae family representatives. A knowledge of bioactive compounds in Epilobium sp. could be especially needed in designing new, safe and effective formulations of nutriceuticals and phytotherapeutics containing medicinal parts of these plants.
For the first time hairy roots of the Rhodiola genus were obtained by infection of the of Rhodiola kirilowii plantlets with Agrobacterium rhizogenes LBA 9402. First transgenic roots appeared 11 days after infection. The transformation process was confirmed by the polymerase chain reaction (PCR ). DNA analysis showed that rol B gene and aux 1 gene from Ri plasmid of Agrobacterium rhizogenes were incorporated into the plant genome of Rhodiola kirilowii.
In last centuries, human diet has been modified due to changes in the technological, economic, and cultural mode of the social life. The rapid development of the technology and advances in food production and processing of plants resulted in changes in the structure of consumption. The consequence is an growing interest among researchers, but also among consumers in searching for new alternatives to classical pharmacology, preventive solutions, and therapeutic strategies of age related, chronic diseases and cancer. In this paper, the authors have attempted to assess the benefits of usage in diet cold-pressed oils extracted from the seeds of Brassica napus (oilseed rape) with particular emphasis on the evidence of possible use of B. napus oil, and other bio-active substances contained therein, in the prevention and symptomatic treatment of prostate diseases, including benign prostatic hyperplasia (BPH). The authors postulate that the information presented in this paper may be important and helpful in the development of new, effective and safe forms of prevention and treatment of progressive age-related disorders (phytotherapeutics) and nutritional strategies (dietary supplements) based on seeds oil of Brassicace family representatives, especially Brassica napus (pollen).
The understanding of the pharmacokinetic properties of synthetic drugs as well as herbal preparations used in treatment of many diseases offers a real opportunity to eliminate or minimize the interaction between the active substances. This is of particular clinical importance because it can decrease or increase the action of drugs what is the major cause of failure of pharmacotherapy. Understanding the molecular basis of interaction of substances with enzymes of drug metabolism is extremely helpful in treatment planning and its practical application. The experimental and clinical studies aimed to complete the characterization of the mechanisms of many factors that modulate the activity of cytochrome P450 enzymes, can provide a lot of evidence guaranteeing the safety of herbal products.
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