This review summarizes the current knowledge on essential vitamins B1, B2, B3, and B5. These B-complex vitamins must be taken from diet, with the exception of vitamin B3, that can also be synthetized from amino acid tryptophan. All of these vitamins are water soluble, which determines their main properties, namely: they are partly lost when food is washed or boiled since they migrate to the water; the requirement of membrane transporters for their permeation into the cells; and their safety since any excess is rapidly eliminated via the kidney. The therapeutic use of B-complex vitamins is mostly limited to hypovitaminoses or similar conditions, but, as they are generally very safe, they have also been examined in other pathological conditions. Nicotinic acid, a form of vitamin B3, is the only exception because it is a known hypolipidemic agent in gram doses. The article also sums up: (i) the current methods for detection of the vitamins of the B-complex in biological fluids; (ii) the food and other sources of these vitamins including the effect of common processing and storage methods on their content; and (iii) their physiological function.
Učební texty Univerzity Karlovy v Praze
4., nezměněné vydání 94 stran : ilustrace, tabulky ; 30 cm
Vysokoškolská učebnice obsahující praktická cvičení, která se zaměřují na farmakognozii.
- MeSH
- Pharmacognosy MeSH
- Conspectus
- Farmacie. Farmakologie
- Učební osnovy. Vyučovací předměty. Učebnice
- NML Fields
- farmacie a farmakologie
- NML Publication type
- učebnice vysokých škol
- praktická cvičení
Three new alkaloids, bersavine (3), muraricine (4), and berbostrejdine (8), together with seven known isoquinoline alkaloids (1-2, 5-7, 9, and 10) were isolated from an alkaloidal extract of the root bark of Berberis vulgaris. The structures of the isolated compounds were determined by spectroscopic methods, including 1D and 2D NMR techniques, HRMS, and optical rotation, and by comparison of the obtained data with those in the literature. The NMR data of berbamine (5), aromoline (6), and obamegine (7) were completely assigned employing 2D NMR experiments. Alkaloids isolated in sufficient amounts were evaluated for their in vitro acetylcholinesterase, butyrylcholinesterase (BuChE), prolyl oligopeptidase, and glycogen synthase kinase-3β inhibitory activities. Selected compounds were studied for their ability to permeate through the blood-brain barrier. Significant human BuChE ( hBuChE) inhibitory activity was demonstrated by 6 (IC50 = 0.82 ± 0.10 μM). The in vitro data were further supported by computational analysis that showed the accommodation of 6 in the active site of hBuChE.
- MeSH
- Acetylcholinesterase metabolism MeSH
- Alkaloids chemistry isolation & purification therapeutic use MeSH
- Alzheimer Disease drug therapy MeSH
- Berberis chemistry MeSH
- Butyrylcholinesterase metabolism MeSH
- Cholinesterase Inhibitors therapeutic use MeSH
- Blood-Brain Barrier drug effects MeSH
- Isoquinolines chemistry isolation & purification therapeutic use MeSH
- Humans MeSH
- Magnetic Resonance Spectroscopy MeSH
- Plant Exudates analysis MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
Glycogen synthase kinase-3β (GSK-3β) is a multifunctional serine/threonine protein kinase that was originally identified as an enzyme involved in the control of glycogen metabolism. It plays a key role in diverse physiological processes including metabolism, the cell cycle, and gene expression by regulating a wide variety of well-known substances like glycogen synthase, tau-protein, and β-catenin. Recent studies have identified GSK-3β as a potential therapeutic target in Alzheimer´s disease, bipolar disorder, stroke, more than 15 types of cancer, and diabetes. GSK-3β is one of the most attractive targets for medicinal chemists in the discovery, design, and synthesis of new selective potent inhibitors. In the current study, twenty-eight Amaryllidaceae alkaloids of various structural types were studied for their potency to inhibit GSK-3β. Promising results have been demonstrated by alkaloids of the homolycorine-{9-O-demethylhomolycorine (IC50 = 30.00 ± 0.71 µM), masonine (IC50 = 27.81 ± 0.01 μM)}, and lycorine-types {caranine (IC50 = 30.75 ± 0.04 μM)}.
- MeSH
- Amaryllidaceae Alkaloids chemistry pharmacology MeSH
- Glycogen Synthase Kinase 3 beta antagonists & inhibitors metabolism MeSH
- Inhibitory Concentration 50 MeSH
- Protein Kinase Inhibitors chemistry pharmacology MeSH
- Humans MeSH
- Drug Evaluation, Preclinical MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Publication type
- Meeting Abstract MeSH
Alzheimer's disease is an age-related, neurodegenerative disorder, characterized by cognitive impairment and restrictions in activities of daily living. This disease is the most common form of dementia with complex multifactorial pathological mechanisms. Many therapeutic approaches have been proposed. Among them, inhibition of acetylcholinesterase, butyrylcholinesterase, and prolyl oligopeptidase can be beneficial targets in the treatment of Alzheimer's disease. Roots, along with aerial parts of Argemone platyceras, were extracted with ethanol and fractionated on an alumina column using light petrol, chloroform and ethanol. Subsequently, repeated preparative thin-layer chromatography led to the isolation of (+)-laudanosine, protopine, (-)-argemonine, allocryptopine, (-)-platycerine, (-)-munitagine, and (-)-norargemonine belonging to pavine, protopine and benzyltetrahydroisoquinoline structural types. Chemical structures of the isolated alkaloids were elucidated by optical rotation, spectroscopic and spectrometric analysis (NMR, MS), and comparison with literature data. (+)-Laudanosine was isolated from A. platyceras for the first time. Isolated compounds were tested for human blood acetylcholinesterase, human plasma butyrylcholinesterase and recombinant prolyl oligopeptidase inhibitory activity. The alkaloids inhibited the enzymes in a dose-dependent manner. The most active compound (-)-munitagine, a pavine alkaloid, inhibited both acetylcholinesterase and prolyl oligopeptidase with IC50 values of 62.3 ± 5.8 µM and 277.0 ± 31.3 µM, respectively.
- MeSH
- Alkaloids chemistry isolation & purification pharmacology MeSH
- Alzheimer Disease drug therapy MeSH
- Argemone chemistry MeSH
- Butyrylcholinesterase drug effects MeSH
- Cholinesterases drug effects MeSH
- Chromatography, Thin Layer methods MeSH
- Enzyme Assays methods MeSH
- Inhibitory Concentration 50 MeSH
- Enzyme Inhibitors chemistry pharmacology MeSH
- Plant Roots chemistry MeSH
- Humans MeSH
- Magnetic Resonance Spectroscopy methods MeSH
- Drug Discovery MeSH
- Plant Extracts chemistry MeSH
- Serine Endopeptidases drug effects MeSH
- Dose-Response Relationship, Drug MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
OBJECTIVES: The aim of this work was to assess the possible beneficial effects of aqueous extracts of Hibiscus sabdariffa L. calyces and anthocyanins isolated therefrom in an adenine-induced chronic kidney disease (CKD) model. METHODS: Rats were orally given, for 28 consecutive days, either adenine alone or together with either aqueous extract of H. sabdariffa calyces (5 and 10%) or anthocyanins (50, 100 and 200 mg/kg of anthocyanin concentrate). For comparative purposes, two groups of rats were given lisinopril (10 mg/kg). KEY FINDINGS: When either H. sabdariffa aqueous extract or the anthocyanins isolated from it was administered along with adenine, the adverse effects of adenine-induced CKD were significantly lessened, mostly in a dose-dependent manner. The positive effects were similar to those obtained by administration of lisinopril. CONCLUSIONS: The results obtained show that both H. sabdariffa and its anthocyanins could be considered as possible promising safe dietary agents that could be used to attenuate the progression of human CKD. This could have added significance as H. sabdariffa tea is widely consumed in many parts of Africa and Asia and is thus readily available.
- MeSH
- Adenine toxicity MeSH
- Anthocyanins administration & dosage isolation & purification pharmacology MeSH
- Administration, Oral MeSH
- Renal Insufficiency, Chronic drug therapy physiopathology MeSH
- Hibiscus chemistry MeSH
- Rats MeSH
- Lisinopril pharmacology MeSH
- Disease Models, Animal MeSH
- Rats, Wistar MeSH
- Plant Extracts administration & dosage pharmacology MeSH
- Dose-Response Relationship, Drug MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Male MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Comparative Study MeSH
- Publication type
- Meeting Abstract MeSH
- Publication type
- Meeting Abstract MeSH
Byl sledován vliv exogenní aplikace kyseliny jasmonové (JA) v kombinaci s vápníkem a verapamilem (blokátor vápníkového kanálu) na produkci flavonoidů a isoflavonoidů suspenzní kulturou Trifolium pratense L. Kultura byla kultivována při teplotě 25 °C a světelné periodě 16 hodin světlo/8 hodin tma na živném médiu podle Gamborga s přídavkem 2 mg.l-1 2,4-dichlorfenoxyoctové kyseliny a 2 mg.l-1 6-benzylaminopurinu. Nejlepší vliv kyseliny jasmonové na produkci flavonoidů a isoflavonoidů se projevil po 24hodinové aplikaci koncentrace 50 μmol.l-1. Maximální produkce elicitované suspenzní kultury byla zjištěna, když buňky byly ošetřeny vysokou dávkou vápníku (10 mmol.l-1). Přidání všech koncentrací verapamilu k suspenzní kultuře elicitované JA snížilo produkci flavonoidů a isoflavonoidů.
Effect of exogenously applied jasmonic acid (JA) in combination with calcium and verapamil (a calcium channels blocker) on the production of flavonoids and isoflavonoids in suspension cultures of Trifolium pratense L. was investigated. The culture was cultivated in Gamborg medium with an addition of 2 mg.l-1 of 2,4-dichlorophenoxyacetic acid and 2 mg.l-1 of 6-benzylaminopurine, at the temperature of 25 °C, 16-hr light/8-hr dark period. The best effect of jasmonic acid on the production of flavonoids and isoflavonoids was manifested after a 24-hour application of the 50 μmol.l-1 concentration. The maximum production of JA-induced suspension culture was observed when cells were treated with a high level of calcium (10 mmol.l-1). The addition of all concentrations of verapamil to JA-induced suspension culture decreased production of flavonoids and isoflavonoids.
- MeSH
- 2-Aminopurine analogs & derivatives chemistry MeSH
- Cell Culture Techniques methods instrumentation MeSH
- Technology, Pharmaceutical MeSH
- Flavonoids * chemistry isolation & purification MeSH
- Phytoestrogens * chemistry isolation & purification MeSH
- Isoflavones * chemistry isolation & purification MeSH
- Culture Media MeSH
- Culture Techniques methods instrumentation utilization MeSH
- 2,4-Dichlorophenoxyacetic Acid chemistry MeSH
- alpha-Linolenic Acid analogs & derivatives chemistry MeSH
- Membrane Transport Modulators MeSH
- Calcium-Calmodulin-Dependent Protein Kinases chemistry MeSH
- Plant Growth Regulators chemistry MeSH
- Plant Extracts chemistry isolation & purification MeSH
- Spectrophotometry methods utilization MeSH
- Trifolium * chemistry MeSH
- Calcium chemistry MeSH
- Calcium Channels chemistry MeSH
- Verapamil chemistry MeSH
- Publication type
- Research Support, Non-U.S. Gov't MeSH