INTRODUCTION: The widespread importance of the synthesis and modification of anticancer agents has given rise to many numbers of medicinal chemistry programs. In this regard, triazine derivatives have attracted attention due to their remarkable activity against a wide range of cancer cells. This evaluation covers work reports to define the anticancer activity, the most active synthesized compound for the target, the SAR and, when described, the probable MOA besides similarly considered to deliver complete and target-pointed data for the development of types of anti-tumour medicines of triazine derivatives. Triazine scaffold for the development of anticancer analogues. Triazine can also relate to numerous beneficial targets, and their analogues have auspicious in-vitro and in-vivo anti-tumour activity. Fused molecules can improve efficacy, and drug resistance and diminish side effects, and numerous hybrid molecules are beneath diverse stages of clinical trials, so hybrid derivatives of triazine may offer valuable therapeutic involvement for the dealing of tumours. OBJECTIVE: The objective of the recent review was to summarize the recent reports on triazine as well as its analogues with respect to its anticancer therapeutic potential. CONCLUSION: The content of the review would be helpful to update the researchers working towards the synthesis and designing of new molecules for the treatment of various types of cancer disease with the recent molecules that have been produced from the triazine scaffold. Triazine scaffolds based on 1,3,5-triazine considerably boost molecular diversity levels and enable covering chemical space in key medicinal chemistry fields.

• Klíčová slova
• Triazine, anticancer, breast cancer, cell line, therapeutic potential., toxicity,
• MeSH
• antitumorózní látky * farmakologie   chemie   terapeutické užití   MeSH
• léky antitumorózní - screeningové testy MeSH
• lidé MeSH
• nádory farmakoterapie   MeSH
• triaziny * farmakologie   chemie   terapeutické užití   MeSH
• vyvíjení léků metody   MeSH
• vztahy mezi strukturou a aktivitou MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• přehledy MeSH
• Názvy látek
• antitumorózní látky * MeSH
• triaziny * MeSH

Coccidiosis is a protozoan intestinal disease that reduces the production of the sheep industry and causes large economic losses for sheep. Although chemically synthesised drugs are routinely employed to treat coccidiosis in sheep, the anticoccidial drug resistance and drug residues in edible meat have prompted an urgent search for alternatives. Herein, the anticoccidial properties of diclazuril, a conventional anticoccidial drug, and Allium sativum, Houttuynia cordata and Portulaca oleracea were assessed. Forty 45-day-old lambs naturally infected with Eimeria spp. were selected and randomly divided into five groups. The results showed that the sheep treated for coccidiosis had considerably decreased average daily gain (ADG) during both administration and withdrawal of the drug compared to the control group. Furthermore, at days 14, 21, 28 and 35, respectively, the three herbs and diclazuril had similar anticoccidial effects, with lower oocysts per gram (OPG) than the control group. On day 78, OPG in the three herbal groups was significantly lower than in the diclazuril group. In addition, the abundance and composition of the gut microbiota were changed in sheep treated with the three herbs and diclazuril compared to the untreated sheep. Moreover, some intestinal microorganisms have a correlation with OPG and ADG when using Spearman correlation analysis. In summary, our results suggest that all three herbs produce anticoccidial effects similar to diclazuril and modulate the balance of gut microbiota in growing lambs.

• Klíčová slova
• Eimeria, Epizootiology, microbiome, prevention and treatment, sheep,
• MeSH
• Eimeria účinky léků   fyziologie   MeSH
• kokcidiostatika farmakologie   aplikace a dávkování   MeSH
• kokcidióza * veterinární   farmakoterapie   parazitologie   MeSH
• léky rostlinné čínské farmakologie   aplikace a dávkování   MeSH
• nemoci ovcí * parazitologie   farmakoterapie   MeSH
• oocysty účinky léků   MeSH
• ovce MeSH
• střevní mikroflóra * účinky léků   MeSH
• triaziny farmakologie   aplikace a dávkování   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• kokcidiostatika MeSH
• léky rostlinné čínské MeSH
• triaziny MeSH

Herein we introduce 3-vinyl-1,2,4-triazines derivatives as dual-reactive linkers that exhibit selectivity towards cysteine and specific strained alkynes, enabling conjugate addition and inverse electron-demand Diels-Alder (IEDDA) reactions. This approach facilitates site-selective bioconjugation of biologically relevant peptides, followed by rapid and highly selective reactions with bicyclononyne (BCN) reagents.

• MeSH
• alkyny MeSH
• cykloadiční reakce MeSH
• elektrony MeSH
• peptidy * MeSH
• triaziny * MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• alkyny MeSH
• peptidy * MeSH
• triaziny * MeSH

Human exposure to organic contaminants is widespread. Many of these contaminants show adverse health effects on human population. Human biomonitoring (HBM) follows the levels and the distribution of biomarkers of exposure (BoE), but it is usually done in a targeted manner. Suspect and non-targeted screening (SS/NTS) tend to find BoE in an agnostic way, without preselection of compounds, and include finding evidence of exposure to predicted, unpredicted known and unknown chemicals. This study describes the application of high-resolution mass spectrometry (HRMS)-based SS/NTS workflow for revealing organic contaminants in urine of a cohort of 200 children from Slovenia, aged 6-9 years. The children originated from two regions, urban and rural, and the latter were sampled in two time periods, summer and winter. We tentatively identified 74 BoE at the confidence levels of 2 and 3. These BoE belong to several classes of pharmaceuticals, personal care products, plasticizers and plastic related products, volatile organic compounds, nicotine, caffeine and pesticides. The risk of three pesticides, atrazine, amitraz and diazinon is of particular concern since their use was limited in the EU. Among BoE we tentatively identified compounds that have not yet been monitored in HBM schemes and demonstrate limited exposure data, such as bisphenol G, polyethylene glycols and their ethers. Furthermore, 7 compounds with unknown use and sources of exposure were tentatively identified, either indicating the entry of new chemicals into the market, or their metabolites and transformation products. Interestingly, several BoE showed location and time dependency. Globally, this study presents high-throughput approach to SS/NTS for HBM. The results shed a light on the exposure of Slovenian children and raise questions on potential adverse health effects of such mixtures on this vulnerable population.

• Klíčová slova
• Biomarker, Exposome, Exposure, HBM4EU, High resolution mass spectrometry, Non-targeted,
• MeSH
• atrazin * analýza   MeSH
• biologické markery MeSH
• biologický monitoring MeSH
• diazinon MeSH
• dítě MeSH
• ethery MeSH
• kofein analýza   MeSH
• léčivé přípravky MeSH
• lidé MeSH
• monitorování životního prostředí metody   MeSH
• nikotin analýza   MeSH
• pesticidy * analýza   MeSH
• plastické hmoty MeSH
• polyethylenglykoly MeSH
• těkavé organické sloučeniny * MeSH
• vystavení vlivu životního prostředí analýza   MeSH
• zvláčňovadla analýza   MeSH
• Check Tag
• dítě MeSH
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• atrazin * MeSH
• biologické markery MeSH
• diazinon MeSH
• ethery MeSH
• kofein MeSH
• léčivé přípravky MeSH
• nikotin MeSH
• pesticidy * MeSH
• plastické hmoty MeSH
• polyethylenglykoly MeSH
• těkavé organické sloučeniny * MeSH
• zvláčňovadla MeSH

OBJECTIVE: To analyse the concentrations of lamotrigine in maternal serum, colostrum, and serum of breastfed newborns, and to evaluate the effect of comedication with enzyme-inducing antiseizure medication and valproic acid. METHODS: This cohort study collected data from 158 women and 143 breastfed newborns. Maternal serum, milk (i.e., colostrum), and newborn serum samples were collected between the 2nd and 5th postnatal days, and lamotrigine concentrations were measured by high-performance liquid chromatography. RESULTS: The median lamotrigine concentrations were 2.7 mg/L in maternal serum, 1.4 mg/L in milk, and 1.7 mg/L in newborn serum. The median milk/maternal serum concentration ratio was 0.60, the median newborn/maternal serum concentration ratio was also 0.60, and the median newborn serum/milk concentration ratio was 1.00. A significant correlation was observed between milk and maternal serum concentrations and between newborn serum and milk concentrations, maternal serum concentrations, maternal daily dose, and dose related to maternal body weight. CONCLUSIONS: Exposure to lamotrigine in breastfed newborns is lower than exposure during pregnancy. However, by the same dose by the same mother, lamotrigine concentrations in both maternal serum and milk increase significantly after delivery. This finding, together with the immature function of eliminating enzymes in newborns, may be the reason for reaching concentrations in the reference range used for the general epileptic population in breastfed newborns. Therapeutic monitoring of breastfed newborns serum concentrations of lamotrigine is not mandatory; however, if signs of possible adverse events are noted, newborn serum concentrations should be analysed.

• Klíčová slova
• Breastfeeding, Concentration, Epilepsy, Infant, Lamotrigine, Therapeutic monitoring,
• MeSH
• antikonvulziva terapeutické užití   MeSH
• kohortové studie MeSH
• kojení * MeSH
• kolostrum chemie   MeSH
• lamotrigin farmakologie   MeSH
• lidé MeSH
• mateřské mléko chemie   MeSH
• matky * MeSH
• novorozenec MeSH
• poporodní období MeSH
• těhotenství MeSH
• Check Tag
• lidé MeSH
• novorozenec MeSH
• těhotenství MeSH
• ženské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antikonvulziva MeSH
• lamotrigin MeSH

Electrophoretic focusing on an inverse electromigration dispersion profile is a relatively new electrophoretic separation method for the analysis of ionisable analytes. Although it offers alternative selectivity, powerful concentration capability and high sensitivity, so far only several systems for the analysis of anionic compounds were reported. This work describes for the first time a functional electrolyte system for the separation of cationic analytes by this method. Based on computer simulations and calculations, a functional electrolyte system was designed, based on 1-ethylpiperazine and pivalic acid. It is suitable for the analysis of weak bases with pKa values between 4.5 and 6 and due to the volatility of both components, it can be operated in combination with ESI-MS detection. Its practical applicability is demonstrated on direct analysis of four 2-hydroxy-s-triazines in waters. Separation in an uncoated capillary with application of negative pressure at the inlet provides very satisfactory results with good reproducibility of peak areas, peak heights and detection times, and with LODs at the 0.5-1 nM (100 ngL-1) level. The robustness of the method is shown on analyses of real tap and river water samples used without any pretreatment.

• Klíčová slova
• Capillary electrophoresis, ESI-MS detection, Electrophoretic focusing, Triazine herbicides, Weak bases,
• MeSH
• anionty MeSH
• elektroforéza kapilární * MeSH
• kationty MeSH
• reprodukovatelnost výsledků MeSH
• triaziny * MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• anionty MeSH
• kationty MeSH
• triaziny * MeSH

Since the beginning of the outbreak, a large number of clinical trials have been registered worldwide, and thousands of drugs have been investigated to face new health emergency of highly contagious COVID-19 caused by the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). Drug repurposing, i.e., utilizing an approved drug for a different indication, offers a time- and cost-efficient alternative for making new (relevant) therapies available to physicians and patients. Considering given strategy, many approved and investigational antiviral compounds, alone or in various relevant combinations, used in the past to fight Severe Acute Respiratory Syndrome Coronavirus-1, Middle East Respiratory Syndrome Coronavirus, Human Immunodeficiency Virus type 1, or Influenza viruses are being evaluated against the SARS-CoV-2. Triazavirin (TZV), a non-toxic broad--spectrum antiviral compound, is efficient against various strains of the Influenza A virus (Influenza Virus A, Orthomyxoviridae), i.e., swine flu (H1N1, or H3N2), avian influenza (H5N1, H5N2, H9N2, or highly pathogenic H7N3 strain), Influenza B virus (Influenza Virus B, Orthomyxoviridae), Respiratory Syncytial Virus (Orthopneumovirus, Pneumoviridae), Tick-Borne Encephalitis Virus (known as Forest-Spring Encephalitis Virus; Flavivirus, Flaviviridae), West Nile Virus (Flavivirus, Flavaviridae), Rift Valley Fever Virus (Phlebovirus, Bunyaviridae), and Herpes viruses (Simplexviruses, Herpesviridae) as well. In regard to COVID-19, the molecule probably reduced inflammatory reactions, thus limiting the damage to vital organs and reducing the need for therapeutic support, respectively. In addition, in silico computational methods indicated relatively satisfactory binding affinities of the TZV ligand to both structural (E)- and (S)-proteins, non-structural 3-chymotrypsin-like protease (3-CLpro) of SARS-CoV-2 as well as human angiotensin-I converting enzyme-2 (ACE-2). The interactions between TZV and given viral structures or the ACE-2 receptor for SARS-CoV-2 might effectively block both the entry of the pathogen into a host cell and its replication. Promising treatment patterns of COVID-19 positive patients might be also based on a suitable combination of a membrane fusion inhibitor (umifenovir, for example) with viral RNA synthesis and replication inhibitor (TZV).

• Klíčová slova
• 3-chymotrypsin-like protease, ACE-2, COVID-19, SARS-CoV-2, Structural proteins, drug repurposing, triazavirin,
• MeSH
• azoly MeSH
• farmakoterapie COVID-19 * MeSH
• lidé MeSH
• SARS-CoV-2 * MeSH
• triaziny terapeutické užití   MeSH
• triazoly MeSH
• virus chřipky A, podtyp H1N1 MeSH
• virus chřipky A, podtyp H3N2 MeSH
• virus chřipky A, podtyp H5N1 MeSH
• virus chřipky A, podtyp H5N2 MeSH
• virus chřipky A, podtyp H7N3 MeSH
• virus chřipky A, podtyp H9N2 MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• azoly MeSH
• riamilovir MeSH Prohlížeč
• triaziny MeSH
• triazoly MeSH

Piglet coccidiosis due to Cystoisospora suis is a major cause of diarrhea and poor growth worldwide. It can effectively be controlled by application of toltrazuril (TZ), and oral formulations have been licensed for many years. Recently, the first parenteral formulation containing TZ in combination with iron (gleptoferron) was registered in the EU for the prevention of coccidiosis and iron deficiency anemia, conditions in suckling piglets requiring routine preventive measures. This study evaluated the absorption and distribution of TZ and its main metabolite, toltrazuril sulfone (TZ-SO2), in blood and intestinal tissues after single oral (20 mg/kg) or single intramuscular (45 mg/piglet) application of TZ. Fifty-six piglets were randomly allocated to the two treatment groups. Animals were sacrificed 1-, 5-, 13-, and 24-days post-treatment and TZ and TZ-SO2 levels were determined in blood, jejunal tissue, ileal tissue, and mixed jejunal and ileal content (IC) by high performance liquid chromatography (HPLC). Intramuscular application resulted in significantly higher and more sustained concentrations of both compounds in plasma, intestinal tissue, and IC. Higher concentrations after oral dosing were only observed one day after application of TZ in jejunum and IC. Toltrazuril was quickly metabolized to TZ-SO2 with maximum concentrations on day 13 for both applications. Remarkably, TZ and TZ-SO2 accumulated in the jejunum, the primary predilection site of C. suis, independently of the administration route, which is key to their antiparasitic effect.

• Klíčová slova
• Isospora suis, anticoccidials, coccidiosis, pharmacokinetics, prevention, swine, tissue distribution,
• MeSH
• aplikace orální MeSH
• ileum metabolismus   MeSH
• injekce intramuskulární MeSH
• jejunum metabolismus   MeSH
• kokcidiostatika aplikace a dávkování   metabolismus   farmakokinetika   MeSH
• kokcidióza prevence a kontrola   veterinární   MeSH
• nemoci prasat prevence a kontrola   MeSH
• prasata MeSH
• střevní sliznice metabolismus   MeSH
• sulfony aplikace a dávkování   metabolismus   farmakokinetika   MeSH
• tělesná hmotnost účinky léků   MeSH
• triaziny aplikace a dávkování   metabolismus   farmakokinetika   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• kokcidiostatika MeSH
• sulfony MeSH
• toltrazuril MeSH Prohlížeč
• triaziny MeSH

Despite their low concentrations in many aquatic environments, evidence exists to suggest that herbicides do affect non-target organisms. Given that burrowing is a primary life-history trait in crayfish, herbicides could potentially have serious negative effects on these ecologically important freshwater macroinvertebrates. In this study, we exposed the red swamp crayfish Procambarus clarkii to terbuthylazine (a triazine) and metazachlor (a chloroacetanilide) at an environmental concentration of 2.0 μg/L for 28 days, and then observed their burrowing behaviour for two days. The metazachlor-exposed males excavated a greater number of burrows than the other tested groups, with comparable depths and volumes relative to individual specimen weight. The relative depth and volume of female burrows were identical in all groups. The natural habit of female crayfish of constructing deeper burrows than males was marginally significant in the control and META groups but was not significant for relative volume. The hypothesized adverse effects of chronic exposure to real environmental concentrations of herbicides were not documented in terms of either relative depth or volume. However, the increased number of burrows in metazachlor-exposed animals may mean that this invasive species will cause greater damage to embankments and river banks. The mechanisms behind these effects require closer study.

• Klíčová slova
• Drought, Macroinvertebrate, Metazachlor, Procambarus clarkii, Terbuthylazine, Weed control,
• MeSH
• acetamidy MeSH
• herbicidy * toxicita   MeSH
• severní raci * MeSH
• triaziny toxicita   MeSH
• zvířata MeSH
• Check Tag
• mužské pohlaví MeSH
• ženské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• acetamidy MeSH
• herbicidy * MeSH
• metazachlor MeSH Prohlížeč
• terbutylazine MeSH Prohlížeč
• triaziny MeSH

Artificial microswimmers that can replicate the complex behavior of active matter are often designed to mimic the self-propulsion of microscopic living organisms. However, compared with their living counterparts, artificial microswimmers have a limited ability to adapt to environmental signals or to retain a physical memory to yield optimized emergent behavior. Different from macroscopic living systems and robots, both microscopic living organisms and artificial microswimmers are subject to Brownian motion, which randomizes their position and propulsion direction. Here, we combine real-world artificial active particles with machine learning algorithms to explore their adaptive behavior in a noisy environment with reinforcement learning. We use a real-time control of self-thermophoretic active particles to demonstrate the solution of a simple standard navigation problem under the inevitable influence of Brownian motion at these length scales. We show that, with external control, collective learning is possible. Concerning the learning under noise, we find that noise decreases the learning speed, modifies the optimal behavior, and also increases the strength of the decisions made. As a consequence of time delay in the feedback loop controlling the particles, an optimum velocity, reminiscent of optimal run-and-tumble times of bacteria, is found for the system, which is conjectured to be a universal property of systems exhibiting delayed response in a noisy environment.

• MeSH
• algoritmy MeSH
• biomimetické materiály * MeSH
• hydrodynamika MeSH
• kovové nanočástice MeSH
• plavání * MeSH
• počítačová simulace MeSH
• počítačové systémy MeSH
• pohyb těles MeSH
• posilování (psychologie) * MeSH
• strojové učení MeSH
• triaziny MeSH
• zlato MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• melamine MeSH Prohlížeč
• triaziny MeSH
• zlato MeSH