This review comprehensively describes the recent advances in the synthesis and pharmacological evaluation of steroid polyamines squalamine, trodusquemine, ceragenins, claramine, and their diverse analogs and derivatives, with a special focus on their complete synthesis from cholic acids, as well as an antibacterial and antiviral, neuroprotective, antiangiogenic, antitumor, antiobesity and weight-loss activity, antiatherogenic, regenerative, and anxiolytic properties. Trodusquemine is the most-studied small-molecule allosteric PTP1B inhibitor. The discovery of squalamine as the first representative of a previously unknown class of natural antibiotics of animal origin stimulated extensive research of terpenoids (especially triterpenoids) comprising polyamine fragments. During the last decade, this new class of biologically active semisynthetic natural product derivatives demonstrated the possibility to form supramolecular networks, which opens up many possibilities for the use of such structures for drug delivery systems in serum or other body fluids.
- MeSH
- antiinfekční látky chemická syntéza chemie farmakologie MeSH
- antitumorózní látky chemická syntéza chemie farmakologie MeSH
- biologické přípravky chemie farmakologie MeSH
- cholestanoly chemie MeSH
- cholestany chemie MeSH
- inhibitory angiogeneze chemická syntéza chemie farmakologie MeSH
- lidé MeSH
- neuroprotektivní látky chemická syntéza chemie farmakologie MeSH
- spermin analogy a deriváty chemie MeSH
- steroidy chemická syntéza chemie farmakologie MeSH
- triterpeny chemická syntéza chemie farmakologie MeSH
- vodní organismy chemie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
Pregnane X Receptor (PXR) is a ligand-activated transcription factor which binds many structurally different molecules. The receptor is able to regulate the expression of a wide array of genes and is involved in cancer and different key physiological processes such as the metabolism of drugs/xenobiotics and endogenous compounds including lipids and carbohydrates, and inflammation. Algae, sponges, sea squirts, and other marine organisms are some of the species from which structurally new molecules have been isolated that have been subsequently identified in recent decades as ligands for PXR. The therapeutic potential of these natural compounds is promising in different areas and has recently resulted in the registration of trabectedin by the FDA as a novel antineoplastic drug. Apart from being potentially novel drugs, these compounds can also serve as models for the development of new molecules with improved activity. The aim of this review is to succinctly summarize the currently known natural molecules isolated from marine organisms with a proven ability to interact with PXR.
- MeSH
- biologické přípravky chemie izolace a purifikace farmakologie MeSH
- lidé MeSH
- ligandy MeSH
- molekulární struktura MeSH
- Porifera chemie MeSH
- pregnanový X receptor metabolismus MeSH
- regulace genové exprese účinky léků MeSH
- Urochordata chemie MeSH
- vodní organismy chemie MeSH
- vyvíjení léků * MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
Synthetic musk compounds are extensively used in personal care and cosmetic products all over the world. Afterwards, they are discharged into the environment mainly because they are not completely removed in wastewater treatment plants. The aim of this study was to investigate if a passive sampler is applicable for the monitoring of tonalide, a polycyclic musk compound, in the aquatic environment and to compare the levels of tonalide in pesticide-polar organic chemical integrative sampler (POCIS) and biota. For this purpose, four sampling localities on the three biggest rivers in the Czech Republic were selected. Tonalide was determined in POCIS at all sampling sites in the concentration ranging from 9 ng/POCIS (Labe River, Hradec Králové) to 25 ng/POCIS (Morava River, Blatec). The locality with the most frequent occurrence of tonalide in biota samples was the Morava River which well corresponded with the highest tonalide concentration in POCIS among sampling sites. The highest number of positive tonalide detections among all studied biota samples was found in fish plasma. To the best of our knowledge, this is the first evidence that tonalide bioaccumulates in fish blood. Tonalide levels were below the limit of quantification in benthos samples at all sampling sites.
- MeSH
- chemické látky znečišťující vodu analýza MeSH
- kosmetické přípravky analýza MeSH
- limita detekce MeSH
- monitorování životního prostředí přístrojové vybavení metody MeSH
- odpadní voda chemie MeSH
- pesticidy analýza MeSH
- řeky chemie MeSH
- společenstvo MeSH
- tetrahydronaftaleny analýza MeSH
- vodní organismy chemie MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Geografické názvy
- Česká republika MeSH
Oceány pokrývají velkou část povrchu naší planety a jsou domovem nepřeberného množství organismů. Řada z nich teprve čeká na své objevení, podobně jako chemické látky, které syntetizují. Odvětví farmakologie označované v zahraniční literatuře termínem „marine pharmacology“ se zabývá studiem právě těchto látek a jejich využitím v medicíně. Původ v mořských organismech je pro většinu z nich jediným pojítkem a tato různorodost se promítá i do širokého spektra možného využití. Mnohé se vyznačují zcela unikátním mechanismem účinku nabízejícím nové možnosti terapeutického působení. Ačkoliv jich do klinické praxe zatím proniklo jen několik (například eribulin či cytarabin), potenciál je obrovský. V klinických studiích v současnosti sice převažují farmaka pro terapii nádorových onemocnění, zkoumány jsou ale i látky s potenciálním využitím v léčbě bolesti či Alzheimerovy choroby a mnoha dalších.
Oceans cover a large part of our planet and they are a home for an enormous amount of species. A lot of them are still waiting to be discovered by man, much like the chemicals they synthesize. Marine pharmacology concerns itself with the study of these chemicals and their potential use in medicine. Origin in marine species is for the most part the only thing this large and diverse group of substances have in common, so the spectrum of possible applications is quite wide. Many of these substances have a unique mechanism of action, offering new therapeutic possibilities. Although just a few of them are used in a clinical practice today (e.g. eribulin, cytarabine), the future looks quite promising. Current clinical trials focus mostly on the therapy of cancer, but trials for therapy of pain or Alzheimer’s disease and many others are also underway.
- Klíčová slova
- léčiva mořského původu, zikonotid, trabectedin, eribulin mesylát, glembatumumab vedotin, DMXBA, marizomib,
- MeSH
- Alzheimerova nemoc farmakoterapie MeSH
- analgetika terapeutické užití MeSH
- antitumorózní látky * farmakologie klasifikace terapeutické užití MeSH
- antivirové látky MeSH
- brentuximab vedotin MeSH
- bryostatiny farmakologie terapeutické užití MeSH
- cytarabin farmakologie MeSH
- depsipeptidy farmakologie klasifikace MeSH
- klinická studie jako téma MeSH
- lidé MeSH
- nádory farmakoterapie MeSH
- oceány a moře MeSH
- tetrodotoxin farmakologie MeSH
- vidarabin farmakologie MeSH
- vodní organismy * chemie klasifikace mikrobiologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- práce podpořená grantem MeSH
- přehledy MeSH
- Geografické názvy
- oceány a moře MeSH
- Klíčová slova
- Pectinatella magnifica, tempo růstu, cinemicrography, bioaktivní substance, buněčná linie L929,
- MeSH
- biomasa MeSH
- Bryozoa * chemie MeSH
- cytoskelet MeSH
- modulátory mitózy MeSH
- pilotní projekty MeSH
- proliferace buněk * MeSH
- vodní organismy chemie MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- práce podpořená grantem MeSH
Persistent organic pollutants (POPs) have been used in a wide range of agricultural and industrial commodities, resulting in vigorous deterioration of environment and human health. A number of studies on the occurrence of POPs confirm their presence in various environmental compartments and human body. In order to deal with this global concern, India has recently prepared the National Implementation Plan (NIP) of the Stockholm Convention. Common beliefs point at India as a hot spot of POP contamination and human exposure; however no systematic analysis was ever performed so far considering all available past data on POP occurrence. This review aims to examine the distribution pattern of POPs in multicompartment environment and human samples, meta-analysis of time trends in exposure levels to environment and humans, and cross country comparison of POP contamination with China. Based on this review, it can be concluded that the Indian environment and human population are highly contaminated by DDTs and HCHs; however scarcity of data on other POPs makes it challenging to assess their nationwide human and environmental exposure. No evidence of a general decline in DDT and HCH residues in the environment and human body come out from the meta-analysis of time trend. While comparing contamination levels between India and China, tendency towards decline in POP contamination is visible in China, unlike India.
- MeSH
- geologické sedimenty chemie MeSH
- látky znečišťující životní prostředí analýza krev MeSH
- lidé MeSH
- monitorování životního prostředí MeSH
- organické látky analýza krev MeSH
- voda chemie MeSH
- vodní organismy chemie MeSH
- vystavení vlivu životního prostředí * MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
- Geografické názvy
- Indie MeSH
Consumption of aquatic plants is rare among cervids, despite the common occurrence of this form of vegetation. However, the paucity of literature reporting on this feeding behaviour suggests that Na (but also other minerals), protein, and the ubiquitous availability of aquatic vegetation may play a role in its consumption. We present results quantifying those factors that regulate the consumption of aquatic plants in the Iberian red deer. We focussed our study primarily on two questions: (i) what nutritional values are red deer seeking in the aquatic plants?; and (ii) why do red deer primarily use aquatic plants during the summer? A comparison of the seasonal variations in Na content between terrestrial vs. aquatic vegetation did not fully support the hypothesis that aquatic plants are being consumed more in summer because of any seasonal variation in Na availability. The Na content in the aquatic vegetation was adequate all the year-round; whereas, the Na content in the terrestrial vegetation was consistently deficient. However, a greater summer content of essential minerals and protein in the aquatic vegetation may be the cause for their consumption exclusively during the summer. We suggest that seasonal variations in the consumption of aquatic vegetation by cervids is primarily driven by temporal variations in the nutrient content, combined with seasonal variations in the physiological demands for these nutrients.
- MeSH
- dieta MeSH
- minerály analýza MeSH
- nutriční hodnota MeSH
- roční období MeSH
- rostlinné proteiny ve výživě analýza MeSH
- rostliny * chemie MeSH
- rybníky MeSH
- sodík analýza MeSH
- stravovací zvyklosti fyziologie MeSH
- vodní organismy * chemie MeSH
- vysoká zvěř fyziologie MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
