Artemisia rupestris je součástí tradiční kazašské medicíny. Výtažky získané z této rostliny se používají k léčbě různých onemocnění včetně rakoviny. Tato studie hodnotí antimikrobiální, cytotoxické a protirakovinné účinky různých extraktů z této rostliny. Byly použity různé extrakční metody a výsledné biologické aktivity byly navzájem porovnány. Extrakty z A. rupestris byly připraveny z květů a listů, a ze stonků. Byla testována antimikrobiální aktivita proti Candida albicans a Staphylococcus aureus. Pro vyhodnocení cytotoxického potenciálu extraktů byly použity buněčné linie L1210 a THP-1. Vodný extrakt ze stonků byl nejúčinnější proti C. albicans, zatímco růst S. aureus inhiboval nejvíce methanolický extrakt z květů a listů. Vodné extrakty nevykazovaly cytotoxický účinek ani u jedné buněčné linie na rozdíl od lipofilních extraktů. Testované extrakty nevykazovaly účinek proti rakovině in vivo. Získané výsledky svědčí o relativně bezpečném použití vodných výluhů z A. rupestris, lipofilní extrakty vykazují toxické účinky, a proto je při jejich užití potřeba více opatrnosti.
Artemisia rupestris is a part of traditional Kazakh folk medicine. Extracts obtained from this plant are used to treat various diseases, including cancer. This study evaluates the anti-microbial, cytotoxic, and anti-cancer effects of different extracts of the plant. Different extraction techniques were used and the resultant activities were compared. Extracts of A. rupestris were prepared from the flowers plus the leaves and from the stems. The antimicrobial activity against Candida albicans and Staphylococcus aureus was quantified. Cell lines L1210 and THP-1 were used to evaluate the cytotoxic potential of these extracts in vitro. The anti-cancer effect was tested using L1210-induced tumorgenesis in mouse model. The aqueous extract of stems was the most active against C. albicans, whereas the methanolic extract of flowers plus leaves especially inhibited the growth of S. aureus. The aqueous extracts were found to be non-cytotoxic for both cell lines, whereas the lipophilic extracts showed cytotoxic effects. The extract obtained from flowers plus leaves was more cytotoxic than that from stems. The tested extracts showed no anti-cancer potential. The results obtained testify to the relatively safe consumption of aqueous extracts of A. rupestris, but lipophilic extracts showed toxic effects and their consumption should be considered more carefully.
- Klíčová slova
- THP-1 buněčná linie, Artemisia rupestris,
- MeSH
- antiinfekční látky analýza MeSH
- Candida albicans MeSH
- cytotoxické testy imunologické MeSH
- fytonutrienty analýza MeSH
- interpretace statistických dat MeSH
- leukemie L1210 MeSH
- mikrovlny MeSH
- modely u zvířat MeSH
- nádorové buněčné linie MeSH
- pelyněk * toxicita MeSH
- Staphylococcus aureus MeSH
- ultrazvuk MeSH
A series of novel octahedral ruthenium(III) complexes involving 6-benzylaminopurine (L) derivatives as N-donor ligands has been prepared by the reaction of [(DMSO)(2)H][trans-RuCl(4)(DMSO)(2)] with the corresponding L derivative. The complexes 1-12 have the general compositions trans-[RuCl(4)(DMSO)(n-Cl-LH)]⋅xSol (1-3), trans-[RuCl(4)(DMSO)(n-Br-LH)]·xSol (4-6), trans-[RuCl(4)(DMSO)(n-OMe-LH)]·xSol (7-9) and trans-[RuCl(4)(DMSO)(n-OH-LH)]·xSol (10-12); n=2, 3, and 4, x=0-1.5; and Sol = H(2)O, DMSO, EtOH and/or (Me)(2)CO. The complexes have been thoroughly characterized by elemental analysis, UV-visible, FTIR, Raman, and EPR spectroscopy, ES+(positive ionization electrospray) mass spectrometry, thermal analysis, cyclic voltammetry, magnetic and conductivity measurements. The X-ray molecular structure of trans-[RuCl(4)(DMSO)(3-Br-LH)]⋅(Me)(2)CO (5) revealed the distorted octahedral coordination in the vicinity of the central atom, and also confirmed that the 3-Br-L ligand is present as the N3-protonated N7-H tautomer and is coordinated to Ru(III) through the N9 atom of the purine moiety. The tested complexes have been found to be in vitro non-cytotoxic against K562, G361, HOS and MCF7 human cancer cell lines with IC(50)>100μM in contrast to the moderate results regarding the antiradical activity with IC(50)≈10(-3)M. On the contrary, in vivo antitumor activity screening showed that the prepared Ru(III) complexes possess higher pro-apoptotic activity than NAMI-A. The reduction of Ru(III) to Ru(II) and Ru(II)-species formation in tumor tissues was confirmed by means of a simple method of detection and visualization of intracellular Ru(II) by fluorescence microscopy. The originality of this method is based on the preparation of a Ru(II)-bipyridine complex in situ.
- MeSH
- antitumorózní látky chemická syntéza chemie farmakologie MeSH
- apoptóza účinky léků MeSH
- dimethylsulfoxid analogy a deriváty farmakologie MeSH
- kinetin chemická syntéza chemie farmakologie MeSH
- komplexní sloučeniny chemická syntéza chemie farmakologie MeSH
- krystalografie rentgenová MeSH
- léky antitumorózní - screeningové testy MeSH
- leukemie L1210 farmakoterapie patologie MeSH
- lidé MeSH
- mitóza účinky léků MeSH
- molekulární konformace MeSH
- myši inbrední DBA MeSH
- myši MeSH
- nádorové buněčné linie MeSH
- nekróza MeSH
- organokovové sloučeniny farmakologie MeSH
- ruthenium MeSH
- transplantace nádorů MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- myši MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
Nitrogen heterocyclic compounds are used in the pharmaceutical industry, in medicine and in agriculture for their biological activity. 4-Amino-3-acetylquinoline, a new synthetically prepared quinoline derivative, was the most effective compound in our primary cytotoxic screening. In this study, we evaluated cytotoxic/antiproliferative activity of quinoline using murine leukemia cell line L1210. Its ability to induce apoptosis was studied, too. Quinoline derivative acted cytotoxically on tumor cell line L1210, the IC(100) value were 50 microg/ml (for 24 h), 25 microg/ml (for 48 h) and 10 microg/ml (for 72 h). The IC(50) values was found to be less than 4 microg/ml, a limit put forward by the National Cancer Institute (NCI) for classification of he compound as a potential anticancer drug. The cytotoxic concentrations of 4-amino-3-acetyl quinoline induced morphological changes of L1210 cells and the apoptotic DNA fragmentation.
- MeSH
- antitumorózní látky farmakologie MeSH
- apoptóza účinky léků MeSH
- chinoliny farmakologie MeSH
- léky antitumorózní - screeningové testy MeSH
- leukemie L1210 patologie MeSH
- myši MeSH
- nádorové buňky kultivované MeSH
- proliferace buněk účinky léků MeSH
- zvířata MeSH
- Check Tag
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
Isothiocyanates (ITCs) are phytochemicals with promising cancer-preventive potential. To elucidate the mechanism of cytotoxicity of ITCs, their accumulation by cells and the role of intracellular glutathione, fluorescent 9-isothiocyanatoacridine (AcITC) was synthesized. The kinetic parameters for the reactions of AcITC with thiols were estimated and the influence of AcITC on human chronic myeloid leukemia cell line (K562) in regard to intracellular glutathione was studied. Cytotoxicity was evaluated by MTT assay, IC(50)=29.2 +/- 2.5 microM (48 h incubation). This acridine derivative was able to induce apoptosis of cells (morphological changes of cells and DNA fragmentation were observed) at least within certain dose that only decreased the level of intracellular glutathione, excessive doses (completely depleted intracellular pool of glutathione) induced necrosis rather than apoptosis. Our results indicated that apoptosis of leukemia cells induced by ITC is possible only if intracellular glutathione is not entirely depleted.
- MeSH
- akridiny toxicita MeSH
- apoptóza účinky léků MeSH
- buňky K562 MeSH
- fragmentace DNA účinky léků MeSH
- glutathion metabolismus MeSH
- leukemie L1210 MeSH
- lidé MeSH
- myši MeSH
- nádorové buňky kultivované účinky léků MeSH
- viabilita buněk účinky léků MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
3-(3-Methylisoxazol-5-yl) and 3-(pyrimidin-2-yl)-2-styrylquinazolin-4(3H)-ones 8a-l and 9a,c-e,h-l were synthesized by refluxing in acetic acid the corresponding 2-methylquinazolinones 6 and 8 with the opportune benzoic aldehyde for 12 h. The synthesized styrylquinazolinones 8a-l and 9a,c-e,h-l were tested in vitro for their antileukemic activity against L-1210 (murine leukemia), K-562 (human chronic myelogenous leukemia) and HL-60 (human leukemia) cell lines showing in some cases good activity.
- MeSH
- antitumorózní látky chemická syntéza farmakologie terapeutické užití MeSH
- buňky K562 MeSH
- chinazoliny chemická syntéza farmakologie terapeutické užití MeSH
- HL-60 buňky MeSH
- kolchicin farmakologie MeSH
- leukemie L1210 MeSH
- lidé MeSH
- molekulární struktura MeSH
- oxazoly chemická syntéza farmakologie terapeutické užití MeSH
- preklinické hodnocení léčiv metody MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- srovnávací studie MeSH
- Geografické názvy
- Česká republika MeSH
- MeSH
- finanční podpora výzkumu jako téma MeSH
- glykogen metabolismus MeSH
- konkanavalin A toxicita MeSH
- leukemie L1210 genetika MeSH
- mnohočetná léková rezistence MeSH
- myši MeSH
- oligosacharidy MeSH
- P-glykoprotein genetika MeSH
- polysacharidy metabolismus MeSH
- zvířata MeSH
- Check Tag
- myši MeSH
- zvířata MeSH
