diethyl ether
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Increasing data has confirmed the potential anticancer properties of Dendrobium, a traditional Chinese herb. However, most anticancer compositions from the plant of Dendrobium were usually extracted by high polar solvent, while weak polar compositions with excellent anticancer activity remained largely unexplored. In this study, the differences between ether extract and ethanol extract of Dendrobium nobile Lindl. on chemical components and anticancer activities were investigated, as well as the anticancer mechanisms among different extracts. The results demonstrated that the ether extract exhibited a stronger anticancer effect than ethanol extract, and its anticancer effect was mainly due to weak polar compounds rather than polysaccharides and alkaloids. Quantitative proteomics suggested that the ether extract significantly stimulated the over-expression of immature proteins, the endoplasmic reticulum stress and unfolded protein response were subsequently induced, the intracellular reactive oxygen species level was seriously elevated, and oxidative stress occurred in the meanwhile. Eventually, autophagy and apoptosis were activated to cause cell death. Our findings demonstrate that the ether extract of D. nobile is a potential candidate for anticancer drug development, and that future research on anticancer drugs derived from medicinal plants should also concentrate on weak polar compounds.
V celé Evropě se rozmáhá okrádání řidičů kamionů nebo lidí v obytných přívěsech po předchozím uspání. Také v Německu došlo v lednu 2022 k loupeži součástek kol v hodnotě 250 milionů korun na odpočívadle pro kamiony. Hlavní roli měl hrát „uspávací plyn“. Článek podává přehled o základních farmakologických účincích látek, které by přicházely v úvahu. Jsou to oxid uhličitý, oxid uhelnatý, oxid dusný, stará inhalační anestetika dietyléter a chloroform a nová inhalační anestetika isofluran, sevofluran, desfluran a v poslední době znovu používaný metoxyfluran. Z analýzy vyplývá, že žádná z těchto látek nepřichází v úvahu a že se patrně jedná o tzv. městskou legendu. Neexistuje dosud žádný případ, v němž by bylo prokázáno použití uspávacího plynu. Při osvobozování rukojmích v moskevském divadle na Dubrovce v říjnu 2002 použily speciální jednotky ruské armády aerosolovou směs remifentanilu s carfentanilem s nosným plynem – inhalačním anestetikem halotanem. Z počtu 830 rukojmích zahynulo vlivem tohoto uspávacího plynu přibližně 130 osob. Řidiči však mohou být omámeni a následně okradeni po podání četných farmak, která spadají do kategorie tzv. rape drugs.
The robbery of truck drivers or caravaners after being put under is rising across Europe. In January 2022, bicycle parts worth 250 million were robbed at a truck stop in Germany. The central role was attributed to the so-called sleeping gas. The article provides an overview of the fundamental pharmacological effects of the substances that could be considered. These are carbon dioxide, carbon monoxide, nitrous oxide, diethyl ether and chloroform, the old, inhaled anesthetics, as well as isoflurane, sevoflurane, desflurane and the recently re-used methoxyflurane as the new inhaled anesthetics. The analysis shows that none of these substances is the possible cause, and it is probably an urban legend. The use of a sleeping gas has not been demonstrated in any case yet. During the release of hostages in the Dubrovka theatre in Moscow in October 2002, special units of the Russian army used an aerosol mixture of remifentanil and carfentanil with a carrier gas – halothane, an inhalation anesthetic. Out of 830 hostages, about 130 died from this sleeping gas. However, drivers may be drugged and subsequently robbed after administering numerous drugs that fall into the category of rape drugs.
- MeSH
- anestetika inhalační * chemie dějiny terapeutické užití MeSH
- chloroform dějiny MeSH
- lidé MeSH
- naftochinony dějiny terapeutické užití MeSH
- oxid dusný dějiny terapeutické užití MeSH
- oxid uhelnatý chemie MeSH
- oxid uhličitý dějiny otrava škodlivé účinky terapeutické užití MeSH
- specializované použití chemických látek MeSH
- terorismus MeSH
- zločin MeSH
- Check Tag
- lidé MeSH
If guided by the right principles, even a short life can bring rich scientific and pedagogical fruits. Despite his premature death Johann Jakob Geelhausen (1692−1738), a hitherto little-known professor at the Charles University, who died on 16th February 1738 at the age of only forty-six, proves to be an important pioneer of chemistry at the Charles University. The presented first detailed study of his pedagogical and scientific legacy not only demonstrates the continuity of teaching chemistry at the Charles University since the early 18th century, but also offers an opportunity for self‑reflection and strengthening the identity of contemporary chemists. A graduate of philosophy and medicine at Charles University, Geelhausen underwent another fundamental formation while studying chemistry with the famous Dutch chemist-reformer Herman Boerhaave. Geelhausen brought Boerhaave's modern methods of teaching chemistry to the Charles University, where he was a professor of medicine from 1721. He also held four times the office of the Dean of the Faculty of Medicine and became the Rector of the University. Thanks to Professor Geelhausen's innovative spirit and as a result of the fruitful encounter of the ancient tradition of the Charles University and the busy atmosphere of Boerhaave's lectures, chemistry began to be taught indirectly at the Faculty of Medicine, long before the first professor of chemistry was appointed there. Already in his dissertation, Geelhausen proved his zeal in the promotion of chemistry, recommending that the drugs “studiosius a chymicis passim inquiruntur” (should be more eagerly sought after by chemists). This study presents a complete, annotated bibliography of Geelhausen's scientific works. Articles on the preparation of diethyl ether, the use of Papin's pot for extractions, and the analysis of mineral waters in Bechyně (a town in the South Bohemian Region of the Czech Republic) stand out from his work. Chemistry is also abundant in dissertations supervised by Geelhausen at the University. Moreover, Geelhausen took an active part in the scientific and social life of Central Europe. He was a member of the Königlich Preußische Sozietät der Wissenschaften and the Academia caesarea Leopoldino‑Carolina naturae curiosorum. He is also a co-author of the first domestic pharmacopoeia, Dispensatorium medico-pharmaceuticum Pragense, published shortly after his death in 1739. With his work and experience with Boerhaave and his writings, Geelhausen probably influenced one of his pupils and successors, Jan Antonín Scrinci. Scrinci was then appointed the first full professor of chemistry at our university in 1738 (in the death year of Professor Geelhausen). Since then, chemistry has been taught continuously at the Charles University.
V oblasti celkových inhalačných prchavých anestetík od použitia oxidu dusného, dietyléteru, chloroformu a cyklopropánu nastal vďaka zavedeniu fluórovaných anestetík a s nimi spojených chirálnych technológií pokrok, v dôsledku ktorého došlo pri anestézii k zníženiu úmrtnosti. Z fluórovaných chirálnych prchavých anestetík sa do oblasti anestézie dostali halotan (Fluotan®), izoflurán (Foran®), dezflurán (Supran®) a enflurán (Ehran®). Z nechirálnych sa používajú metoxyflurán (Penthrox®) a sevoflurán (Sevoran®). Chirálne anestetiká majú v svojej štruktúre stereogénne centrum a existujú vo forme dvoch enantiomérov (S)-(+) a (R)-(–). Hoci sa tieto chirálne anestetiká používajú vo forme racemátov, z hľadiska účinnosti a bezpečnosti je u nich dôležité študovať okrem biologickej aktivity racemátov i biologickú aktivitu ako i ďalšie vlastnosti jednotlivých enantiomérov. V predloženom prehľade je pozornosť venovaná skupine liečiv známych ako inhalačné anestetiká vo vzťahu k ich chirálnym aspektom. Boli u nich zistené významné rozdiely (R) a (S)-enantiomérov vo farmakodynamickej, farmakokinetickej aktivite, ako i v toxicite. Na rozdelenie jednotlivých racemátov na enantioméry sa využíva hlavne plynová chromatografia (GC). V prehľade sú uvedené jednotlivé chirálne fázy, resp. selektory využívané pri ich enantioseparácii, ako i pri farmakokinetických štúdiách. Príprava jednotlivých enantiomérov okrem preparatívnej GC je možná aj pomocou metód stereoselektívnej syntézy.
Since the advent of nitric oxide, diethyl ether, chloroform and cyclopropane, the greatest advancement in the area of general inhalational anesthetics has been achieved by the introduction of fluorinated anesthetics and the relevant chiral techniques. This progress led to marked decrease in mortality rates in anesthesia. In the group of chiral fluorinated compounds, halothane (Fluotan®), isoflurane (Foran®), desflurane (Supran®) and enflurane (Ehran®) are deployed as volatile anesthetics. Chiral anesthetics possess a stereogenic center in their molecules and thus exist as two enantiomers (S)-(+) and (R)-(–). Although these chiral anesthetics are used as racemates, it is crucial to study besides the bioactivities of the racemic compounds also the biological activity and other properties of the particular enantiomers. The present survey discusses the drug category known as inhalational anesthetics in regard to their chiral aspects. These compounds exhibit marked differences between the (R) and (S)-enantiomers in their pharmacodynamics, pharmacokinetics and toxicity. The main analytical technique employed in the enantioseparation of these compounds is gas chromatography (GC). This review lists the individual chiral phases (chiral selectors) used in the enantioseparation as well as in pharmacokinetic studies. The possibilities of preparation of these compounds in their enantiomerically pure form by means of stereoselective synthesis are also mentioned.
- MeSH
- anestetika celková * farmakokinetika farmakologie MeSH
- anestetika inhalační * farmakokinetika farmakologie MeSH
- lidé MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- přehledy MeSH
- MeSH
- anestezie a analgezie * dějiny MeSH
- chloroform dějiny MeSH
- cyklopropany dějiny MeSH
- ether dějiny MeSH
- kokain dějiny MeSH
- oxid dusný MeSH
- spinální anestezie dějiny MeSH
- Publikační typ
- zprávy MeSH
The paper describes transesterification of oil by methanol with use of cosolvents such as ethyl acetate, tetrahydrofuran, hexane, acetone and diethyl ether at catalyst homogeneous (potassium hydroxide) and heterogeneous (mixed oxides). The cosolvents dissolve oil and methanol to form a single (homogeneous) phase, which increases the reaction rate. Therefore, the biodiesel production will be environmentally friendly because less energy is consumed, which increases sustainability. The whole binodal curve of ternary plots of oil, methanol and cosolvent was determined to find the molar ratio, in which the reaction mixture forms a single phase. The ethyl acetate and tetrahydrofuran have relatively small heterogeneous region, because of the similarity of their electric dipole moment with methanol. After transesterification, the detailed analysis of ester and also glycerol phase was carried out. For homogeneous catalyst, the highest esters content in the ester phase was achieved with tetrahydrofuran. For heterogeneous catalyst, the ester content was lower with cosolvent than without cosolvent, probably due to dilution of reaction components by cosolvent or bonding of cosolvent to the active sites of the catalyst.
- MeSH
- biopaliva * MeSH
- esterifikace MeSH
- estery * MeSH
- katalýza MeSH
- methanol MeSH
- oleje rostlin MeSH
- Publikační typ
- časopisecké články MeSH
Světová zdravotnická organizace (WHO) byla o výskytu závažného onemocnění způsobeného novým typem koronaviru ve Wuhanu v Číně poprvé informována v prosinci 2019. Onemocnění je nyní označováno jako COVID19 a jeho původce jako SARSCoV2 (severe acute respiratory syndrome coronavirus 2). Výskyt COVID19 se postupně rozšířil do celého světa a WHO vyhlásila pandemii. Protože jde o nový typ onemocnění, neexistuje žádná ověřená terapie. Byla však zahájena řada studií účinnosti různých léčivých látek v terapii COVID19.
- Klíčová slova
- remdesivir, umifenovir, favipiravir, tocilizumab,
- MeSH
- amidy terapeutické užití MeSH
- antimalarika terapeutické užití MeSH
- antimetabolity terapeutické užití MeSH
- antivirové látky terapeutické užití MeSH
- azithromycin terapeutické užití MeSH
- chlorochin terapeutické užití MeSH
- COVID-19 * MeSH
- farmakoterapie COVID-19 MeSH
- humanizované monoklonální protilátky terapeutické užití MeSH
- hydroxychlorochin terapeutické užití MeSH
- indoly terapeutické užití MeSH
- inhibitory cytochromu P450 CYP3A terapeutické užití MeSH
- inhibitory HIV-proteasy terapeutické užití MeSH
- interferon alfa terapeutické užití MeSH
- interferon beta terapeutické užití MeSH
- krevní plazma MeSH
- kyselina askorbová terapeutické užití MeSH
- lidé MeSH
- Lopinavir MeSH
- pyraziny terapeutické užití MeSH
- sulfidy terapeutické užití MeSH
- Check Tag
- lidé MeSH
BACKGROUND AND AIMS: General anaesthetics are compounds that induce loss of responsiveness to environmental stimuli in animals and humans. The primary site of action of general anaesthetics is the nervous system, where anaesthetics inhibit neuronal transmission. Although plants do not have neurons, they generate electrical signals in response to biotic and abiotic stresses. Here, we investigated the effect of the general volatile anaesthetic diethyl ether on the ability to sense potential prey or herbivore attacks in the carnivorous plant Venus flytrap (Dionaea muscipula). METHODS: We monitored trap movement, electrical signalling, phytohormone accumulation and gene expression in response to the mechanical stimulation of trigger hairs and wounding under diethyl ether treatment. KEY RESULTS: Diethyl ether completely inhibited the generation of action potentials and trap closing reactions, which were easily and rapidly restored when the anaesthetic was removed. Diethyl ether also inhibited the later response: jasmonic acid (JA) accumulation and expression of JA-responsive genes (cysteine protease dionain and type I chitinase). However, external application of JA bypassed the inhibited action potentials and restored gene expression under diethyl ether anaesthesia, indicating that downstream reactions from JA are not inhibited. CONCLUSIONS: The Venus flytrap cannot sense prey or a herbivore attack under diethyl ether treatment caused by inhibited action potentials, and the JA signalling pathway as a consequence.
- MeSH
- anestezie * MeSH
- cyklopentany MeSH
- Droseraceae * MeSH
- ether MeSH
- oxylipiny MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
Poly(lactic acid)-block-poly(oxirane)s (PLA-b-POE) of various compositions were prepared using a one-pot approach and then extended in a reaction with l-lysine diethyl ester diisocyanate, thereby forming polyester-ether-urethanes (PEU) with prolonged chains and units with increased degradability. The PEUs are processed by electrospinning to prepare degradable nanofibrous sheet materials with and without encapsulating the antibiotic Vancomycin (VAC). PLA block isomerism and POE blocks oligomeric content (1000 g/mol) affect the thermal properties, processability, nanofibrous sheet morphology, abiotic degradation, cytocompatibility, and encapsulated antibiotic release rate of prepared PEUs. Therefore, our findings provide an effective approach to tuning the functional properties of these advanced biocompatible materials. © 2019 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater 107B: 2378-2387, 2019.
- MeSH
- antibakteriální látky * chemie farmakologie MeSH
- buňky NIH 3T3 MeSH
- lékové transportní systémy * MeSH
- myši MeSH
- nanovlákna chemie MeSH
- polyestery chemie farmakologie MeSH
- polyethylenglykoly chemie farmakologie MeSH
- polyurethany chemie farmakologie MeSH
- testování materiálů * MeSH
- vankomycin * chemie farmakologie MeSH
- zvířata MeSH
- Check Tag
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH