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
- adenin toxicita MeSH
- anthokyaniny aplikace a dávkování izolace a purifikace farmakologie MeSH
- aplikace orální MeSH
- chronická renální insuficience farmakoterapie patofyziologie MeSH
- Hibiscus chemie MeSH
- krysa rodu rattus MeSH
- lisinopril farmakologie MeSH
- modely nemocí na zvířatech MeSH
- potkani Wistar MeSH
- rostlinné extrakty aplikace a dávkování farmakologie MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- srovnávací studie MeSH
Two new isoquinoline alkaloids, named fumaranine (2) and fumarostrejdine (10), along with 18 known alkaloids were isolated from aerial parts of Fumaria officinalis. The structures of the isolated compounds were elucidated on the basis of spectroscopic analyses and by comparison with literature data. The absolute configuration of the new compound 2 was determined by comparing its circular dichroism spectra with those of known analogs. Compounds isolated in sufficient amounts were evaluated for their acetylcholinesterase, butyrylcholinesterase, prolyl oligopeptidase (POP), and glycogen synthase kinase-3β inhibitory activities. Parfumidine (8) and sinactine (15) exhibited potent POP inhibition activities (IC50 99±5 and 53±2 μM, resp.).
- MeSH
- acetylcholinesterasa metabolismus MeSH
- alkaloidy chemie izolace a purifikace farmakologie MeSH
- Alzheimerova nemoc farmakoterapie enzymologie MeSH
- butyrylcholinesterasa metabolismus MeSH
- Fumaria chemie MeSH
- inhibitory enzymů chemie izolace a purifikace farmakologie MeSH
- isochinoliny chemie izolace a purifikace farmakologie MeSH
- kinasa 3 glykogensynthasy antagonisté a inhibitory metabolismus MeSH
- lidé MeSH
- molekulární struktura MeSH
- serinové endopeptidasy metabolismus MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Prolyl oligopeptidase is a cytosolic serine peptidase that hydrolyses proline-containing peptides at the carboxy terminus of proline residues. It has been associated with schizophrenia, bipolar affective disorder, and related neuropsychiatric disorders and therefore may have important clinical implications. Thirty-one isoquinoline alkaloids of various structural types, previously isolated in our laboratory, were screened for their ability to inhibit prolyl oligopeptidase. Promising results have been showed by alkaloids californidine (IC50=55.6±3.5 μM), dihydrosanquinarine (IC50=99.1±7.6 μM), corypalmine (IC50=128.0±10.5 μM) and N-methyllaurotetanine (IC50=135.0±11.7 μM).
- MeSH
- alkaloidy chemie MeSH
- aporfiny chemie MeSH
- dioxoly chemie MeSH
- heterocyklické sloučeniny tetra- a více cyklické chemie MeSH
- inhibitory serinových proteinas chemie MeSH
- isochinoliny chemie MeSH
- molekulární struktura MeSH
- serinové endopeptidasy chemie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
