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The results indicate that in the studied group of structurally related isoxazolone derivatives, discrepancies occur between the retention under IAM and RP-LC conditions. Although some correlation between these two chromatographic methods can be found, lipophilicity does not fully explain the affinities of the investigated molecules to phospholipids. QSRR analysis also shows common factors that contribute to retention under IAM and RP-LC conditions. In this context, the significant influences of WHIM and GETAWAY descriptors in all the obtained models should be highlighted.The main challenge in ovarian cancer treatment is the management of recurrences. Facing this scenario, therapy selection is based on multiple factors to define the best treatment sequence. Target therapies, such as bevacizumab and polymerase (PARP) inhibitors, improved patient survival. However, despite their achievements, ovarian cancer survival remains poor; these therapeutic options are highly costly and can be associated with potential side effects. Recently, it has been shown that the combination of repurposed, conventional, chemotherapeutic drugs could be an alternative, presenting good patient outcomes with few side effects and low costs for healthcare institutions. The main aim of this review is to strengthen the importance of repurposed drugs as therapeutic alternatives, and to propose an in vitro model to assess the therapeutic value. Herein, we compiled the current knowledge on the most promising non-oncological drugs for ovarian cancer treatment, focusing on statins, metformin, bisphosphonates, ivermectin, itraconazole, and ritonavir. We discuss the primary drug use, anticancer mechanisms, and applicability in ovarian cancer. Finally, we propose the use of these therapies to perform drug efficacy tests in ovarian cancer ex vivo cultures. This personalized testing approach could be crucial to validate the existing evidences supporting the use of repurposed drugs for ovarian cancer treatment.The evidence on atherosclerosis imaging with 18F-sodium-fluoride (NaF) positron emission tomography (PET) is hotly debated because of the different patient characteristics, methodology, vascular beds, etc. in reported studies. This review is a continuation of a previous review on this topic, which covered the period 2010-2018. The purpose was to examine whether some of the most important questions that the previous review had left open had been elucidated by the most recent literature. Using principles of a systematic review, we ended analyzing 25 articles dealing with the carotids, coronary arteries, aorta, femoral, intracranial, renal, and penile arteries. The knowledge thus far can be summarized as follows by targeting active arterial microcalcification, NaF uptake is considered a marker of early stage atherosclerosis, is age-dependent, and consistently associated with cardiovascular risk. Longitudinal studies on NaF uptake, conducted in the abdominal aorta only, showed unchanged uptake in postmenopausal women for nearly four years and varying uptake in prostate cancer patients over 1.5 years, despite constant or increasing calcium volume detected by computed tomography (CT). Thus, uncertainty remains about the transition from active arterial wall calcification marked by increased NaF uptake to less active or consolidated calcification detected by CT. The question of whether early-phase atherosclerosis and calcification can be modified remains also unanswered due to lack of intervention studies.Hydraulic engineering built in the cold region, such as reservoirs and hydropower stations, is often threatened by static ice pressure from nature. Therefore, it is of vital significance to research the pressure variation in the growth and melting processes of the ice layer for the design and protection of hydraulic structures in cold regions. This paper introduces an optical fiber sensor system based on the fiber loop ring-down spectroscopy technology and field-programmable gate array (FPGA) pulse modulation technology. An electro-optic modulation scheme that relied on FPGA to generate optical pulses with adjustable pulse width and period is proposed, which is more suitable for the in-situ observation. In addition, the temperature stability and repeatability of the system are also discussed. This system was applied to the real-time detection of static ice pressure on the sidewall and bottom of the polyvinyl chloride (PVC) pipe during the ice growth and melting processes. The results indicate that the system has favorable stability and sensitivity, and the relationship obtained between the static ice pressure and temperature could provide some references for the field application in the future.The aim of this work was to investigate the changes of the content of polyphenols in fruits of Capsicum chinense Jacq. at different harvest times and their correlation with the antioxidant activity. Habanero pepper plants grown in black soil (Mayan name Box lu'um) and harvested at 160, 209, 223, 237 and 252 post-transplant days (PTD) were analyzed. The results indicated that subsequent harvesting cycles decreased the content of total polyphenols, catechin, chlorogenic acid and ellagic acid, while the content of gallic and protocatechuic acid increased. The antioxidant activity determined by DPPH (2,2-Diphenyl-1-picrylhydrazyl) radical scavenging and ABTS (2,2'-azino-di-3-ethylbenzthiazoline sulfonic acid) assay decreased through the harvest days. Linear correlation analysis between total polyphenol content and antioxidant activity in peppers resulted in a correlation of r2DPPH = 0.8999 and r2ABTS = 0.8922. Additionally, a good correlation of the antioxidant activity was found with catechin (r2DPPH = 0.8661 and r2ABTS = 0.8989), chlorogenic acid (r2DPPH = 0.8794 and r2ABTS = 0.8934) and ellagic acid (r2DPPH = 0.8979 and r2ABTS = 0.9474), indicating that these polyphenols highly contributed to the antioxidant activity in Habanero peppers. This work contributes to understanding the changes that take place during the development of Capsicum chinense, indicating that fruit harvested at earlier PTD showed the highest concentrations of total polyphenols and antioxidant activity, obtaining the best results at 160 PTD.The NALP3 inflammasome signaling contributes to inflammation within tumor tissues. This inflammation may be promoted by the vesicle trafficking of inflammasome components and cytokines. Rab5, Rab7 and Rab11 regulate vesicle trafficking. However, the role of these proteins in the regulation of inflammasomes remains largely unknown. To elucidate the role of these Rab proteins in inflammasome regulation, HCT-116, a colorectal cancer (CRC) cell line expressing pDsRed-Rab5 wild type (WT), pDsRed-Rab5 dominant-negative (DN), pDsRed-Rab7 WT, pDsRed-Rab7 DN, pDsRed-Rab11 WT and pDsRed-Rab11 DN were treated with lipopolysaccharide (LPS)/nigericin. Inflammasome activation was analyzed by measuring the mRNA expression of NLRP3, Pro-CASP1, RAB39A and Pro-IL-1β, conducting immunofluorescence imaging and western blotting of caspase-1 and analysing the secretion levels of IL-1β using enzyme-linked immunosorbent assay (ELISA). ML198 price The effects of Rabs on cytokine release were evaluated using MILLIPLEX MAP Human Cytokine/Chemokine Magnetic Bead Panel-Premixed 41 Plex. The findings showed that LPS/nigericin-treated cells expressing Rab5-WT indicated increased NALP3 expression and secretion of the IL-1β as compared to Rab5-DN cells. Caspase-1 was localized in the nucleus and cytosol of Rab5-WT cells but was localized in the cytosol in Rab5-DN cells. There were no any effects of Rab7 and Rab11 expression on the regulation of inflammasomes. Our results suggest that Rab5 may be a potential target for the regulation of NALP3 in the treatment of the CRC inflammation.A series of two new and twenty earlier synthesized branched extra-amino-triterpenoids obtained by the direct coupling of betulinic/betulonic acids with polymethylenpolyamines, or by the cyanoethylation of lupane type alcohols, oximes, amines, and amides with the following reduction were evaluated for cytotoxicity toward the NCI-60 cancer cell line panel, α-glucosidase inhibitory, and antimicrobial activities. Lupane carboxamides, conjugates with diaminopropane, triethylenetetramine, and branched C3-cyanoethylated polyamine methyl betulonate showed high cytotoxic activity against most of the tested cancer cell lines with GI50 that ranged from 1.09 to 54.40 µM. Betulonic acid C28-conjugate with triethylenetetramine and C3,C28-bis-aminopropoxy-betulin were found to be potent micromolar inhibitors of yeast α-glucosidase and to simultaneously inhibit the endosomal reticulum α-glucosidase, rendering them as potentially capable to suppress tumor invasiveness and neovascularization, in addition to the direct cytotoxicity. Plausible mechanisms of cytotoxic action and underlying disrupted molecular pathways were elucidated with CellMinner pattern analysis and Gene Ontology enrichment analysis, according to which the lead compounds exert multi-target antiproliferative activity associated with oxidative stress induction and chromatin structure alteration. The betulonic acid diethylentriamine conjugate showed partial activity against methicillin-resistant S. aureus and the fungi C. neoformans. These results show that triterpenic polyamines, being analogs of steroidal squalamine and trodusquemine, are important substances for the search of new drugs with anticancer, antidiabetic, and antimicrobial activities.Cytauxzoon felis is a hemoprotozoal tick-transmitted pathogen of felids. Felids that survive acute disease often remain infected and serve as reservoirs for subsequent tick transmission to other susceptible felines. States adjacent to Kansas have identified C. felis-domestic cat carriers while statewide awareness and concern of cytauxzoonosis have increased. The objective of this study was to determine the prevalence of C. felis-carriers in the eastern Kansas domestic cat population using a sensitive quantitative PCR assay targeting the C. felis Cox3 mitochondrial gene. An overall C. felis infection prevalence of 25.8% was determined for asymptomatic domestic cats in eastern Kansas. Significantly more C. felis-carrier cats were identified in spring and fall, suggesting a seasonal fluctuation of survivors. Additionally, a greater percentage of feral and owned cats were positive for C. felis compared to rescue/rescinded cats. This study demonstrates that C. felis-domestic cat carriers are common among cats that spend at least a portion of time outdoors in eastern Kansas, and that more cats likely survive cytauxzoonosis than expected. Understanding the role of domestic cat carriers of C. felis is essential in developing cytauxzoonosis mitigation strategies, including recommending year-round use of acaricide products for all cats that spend any time outdoors.Alternaria alternata is an important phytopathogen causing fruit black rot and also producing a variety of mycotoxins, such as alternariol (AOH) and alternariol monomethyl ether (AME) as two main contaminants. This could lead to economic losses of agricultural products as well as human health risks. In this study, magnolol extracted from the traditional Chinese herb, Mangnoliaofficinalis, exhibited an obvious antifungal property and could completely suppress the mycelial growth at 100 μM. Morphological differences of A. alternata were observed to be significantly shrunk and wrinkled after the exposure to magnolol. Furthermore, AOH and AME were no longer produced in response to 50 μM of magnolol. To uncover the antifungal and antimycotoxigenic mechanisms, the transcriptomic profiles of A. alternata-treated with or without magnolol-were evaluated. The clustered genes responsible for AOH and AME biosynthesis were obviously less transcribed under magnolol stress and this was further confirmed by qRT-PCR. The global regulators of carbon and nitrogen utilization, such as CreA and NmrA, were significantly down-regulated and this possibly caused the reduction in mycotoxins.