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The theoretical calculations of ADME parameters molecular
2024-02-21
The theoretical calculations of ADME parameters (molecular weight (MW), log P, topological polar surface are (tPSA), number of hydrogen donors (nON) and acceptors (nOHNH), and volume) and DLS are presented in along with the violations of Lipinski’s rule. According to these data, all compounds (–) c
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As summarized in Fig autophagy up regulation
2024-02-21
As summarized in Fig. 1, autophagy up-regulation in terms of Beclin 1 induction, increase of LC3 II and p62 down-regulation were observed between 24 and 72 h of cell incubation, this coinciding with the end of the period 27-OH caused slight reduction of cell viability and proliferation as previously
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Polyphenols like flavonoids have the potential to
2024-02-21
Polyphenols like flavonoids have the potential to penetrate into lipid bilayers which is vital for enabling protection against oxidation. Rosmarinic lactacystin is a natural polyphenol antioxidant isolated from Sphaeranthus amaranthoides. Polyphenols can inhibit the propagation of lipid oxidation b
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In pancreatic islets we found an increase in protein
2024-02-21
In pancreatic islets we found an increase in protein expression of leukocyte 12/15-LO that paralleled the metabolic decline characterized by severe hyperglycemia and reduced islet numbers. Similar increase in 12/15-LO expression by Western blot was found in the control mice, which have a normal meta
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We subsequently performed immunohistochemistry on sections o
2024-02-21
We subsequently performed immunohistochemistry on sections obtained from mice at 16 weeks after surgery. Type II collagen expression was detected in all articular cartilage zones, but was weak in the upper zone in the vehicle-treated group. MMP-13 and type X collagen expression were increased in the
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Previous studies have thus demonstrated that AR activation g
2024-02-20
Previous studies have thus demonstrated that AR activation generally correlates with the promotion of urothelial carcinogenesis and cancer growth. In this article, we review available data suggesting their modulation through the AR pathway as well as correlations of AR signals with sensitivity to co
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It was reported that oral administration
2024-02-20
It was reported that oral administration of CSZ to C57BL/6J mice significantly improved spatial learning and memory, and prevented Aβ-induced immunoresponse in Aβ25-35-injected mice. However, post-treatment with CSZ after Aβ25-35 administration, when Aβ was already accumulated, did not prevent Aβ-in
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In our previous work diffuse deposition patterns of neocorti
2024-02-20
In our previous work, diffuse deposition patterns of neocortical Aβ and a hierarchical upward spreading pattern of tau were determined with in vivo 18F-florbetaben and 18F-flortaucipir positron emission tomography (PET) studies, based on the regional frequency of involvement by tau and Aβ (Cho et al
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It remains to elucidate whether proteolytic activity is the
2024-02-20
It remains to elucidate whether proteolytic activity is the cause or the consequence of changing levels of peptidergic substrates. In fact, in some cases, the expression of the enzyme does not necessarily parallel with its activity [26], [55], [57] and other factors such as a definite biochemical en
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Introduction Aldose reductase ALR is the
2024-02-20
Introduction Aldose reductase (ALR2) is the first enzyme of the polyol pathway that catalyzes the reduction of glucose to sorbitol utilizing NADPH as a cofactor. The intracellular accumulation of sorbitol, due to increased aldose reductase activity at high blood glucose levels, such as those occurr
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br Conclusion br Conflict of interest
2024-02-20
Conclusion Conflict of interest Introduction Oral cancer may originate from lips, lower and upper alveolar ridges, hard palate, sublingual region, buccal mucosa, anterior two-thirds of the tongue as well as retromolar trigone and floor of the mouth (World Health Organization, 2013). As the
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The inflammatory cytokine IL is
2024-02-20
The inflammatory cytokine IL-6 is an additional factor that has been hypothesized to contribute to epinephrine-mediated repression of drug detoxifying proteins such as CYP3A4 (Aninat et al., 2008). Indeed, this CYP is well-known to be repressed by IL-6 (Dickmann et al., 2011) and epinephrine has pre
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In the late s Solvay Pharmaceuticals discontinued the Phase
2024-02-20
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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Taken together our results indicated
2024-02-20
Taken together, our results indicated that 5-LOX can be induced in mice by MPTP injection, and the 5-LOX inhibitor MK-886 reduced the death of dopaminergic neurons. MK-886 also reduced the LTB4 BAY 61-3606 induced by MPTP. The development of the novel 5-LOX or FLAP inhibitors may provide a new thera
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The central problem in amnesia
2024-02-20
The central problem in amnesia developing following impairment of long-term memory consolidation or reconsolidation is a question of the underlying mechanisms, whether it is caused by impairment of retrieval or memory storage mechanisms [3,8,9,[15], [16], [17], [18]]. To answer this question, severa
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