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Anti-Inflammatory Properties of Bioactive Compounds from Medicinal Plants
Published in Hafiz Ansar Rasul Suleria, Megh R. Goyal, Health Benefits of Secondary Phytocompounds from Plant and Marine Sources, 2021
Muhammad Imran, Abdur Rauf, Anees Ahmed Khalil, Saud Bawazeer, Seema Patel, Zafar Ali Shah
The phytochemicals (such as uracil, caffeic acid, and S-allyl cysteine (SAC)) from garlic modulate UVB-stimulated formation of wrinkles and influence the propagation of matrix-metalloproteinase (MMP) and NF-κB signaling. In vivo, these phytomolecules suppressed MMPs expression and type-I pro-collagen degradation and reduced histological collagen fiber disorder and oxidative stress conditions. Moreover, SAC, and caffeic acid diminished inflammatory and oxidative stress conditions due to modulation of NF-κB activity. Indirect antioxidant potential of uracil was also noticed, as it inhibited the expression of COX-2 and iNOS and downregulated transcriptional factors [53].
Sleep-Promoting Substance (SPS) and Nucleosides
Published in Shojiro Inoué, Biology of Sleep Substances, 2020
In spite of the structural similarity of uracil to barbital and to uridine, we found no somnogenic activity of uracil at three doses of 1, 10, and 100 pmol after the long-term nocturnal i.c.v. infusion assay in rats3,22,23,52 (see Figure 13). Consequently, it was suggested that a sugar moiety of uridine may have an importance in eliciting the sleep-promoting effect, or some other uridine metabolites may be active. Recently, we have compared the somnogenic activity of several uridine-related nucleosides by the same bioassay method.23,53,54 The results are summarized in Table 2.
Introduction to hyperammonemia and disorders of the urea cycle
Published in William L. Nyhan, Georg F. Hoffmann, Aida I. Al-Aqeel, Bruce A. Barshop, Atlas of Inherited Metabolic Diseases, 2020
William L. Nyhan, Georg F. Hoffmann, Aida I. Al-Aqeel, Bruce A. Barshop
Overproduction of pyrimidines leads to the presence of large amounts of uracil and increased amounts of uridine in the urine. In most patients with OTCD, orotic aciduria is always present. However, we have reported one patient [6] and studied others with partial variants in whom orotic acid excretion was not present when they were clinically well and could not be induced by means of a protein load, but was readily evident at the time of illness induced by infection.
Synthesis, computational study and biological evaluation of 9-acridinyl and 1-coumarinyl-1,2,3-triazole-4-yl derivatives as topoisomerase II inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Gehan A. Abdel-Hafez, Abdel-Maaboud I. Mohamed, Adel F. Youssef, Claire Simons, Ahmed S. Aboraia
In this study, three component ligands were built with a 1,2,3-triazole ring bridging acridine/coumarin nuclei to heteroaryl/aryl/alkyl pharmacologically active molecules (Figure 2). The coumarin and acridine moieties were ligated, via the triazole ring, to different heterocycles to generate the hybrid molecules. Uracil and 6-Me-uracil were chosen owing to the ability of these pyrimidines to form crosslinks with the DNA duplex. Uracil itself is a reversible dihydropyrimidine dehydrogenase (DPD) inhibitor, which has been shown to be beneficial in reducing drug toxicity of other uracil anticancer agents, for example, 5-fluorouracil, tegafur, and capecitabine16,17 and therefore, may have additional protective properties. Phenytoin, used clinically in the treatment of epilepsy, has multiple modes of action18 with promising results in studies against breast cancer19 and phenytoin has also been shown to have cardioprotective effects on doxorubicin-induced cardiotoxicity20. Valproic acid, used clinically in the treatment of seizures, has been shown to be an inhibitor of histone deacetylases resulting in anticancer activity21,22, while the non-steroidal anti-inflammatory drug (NSAID) naproxen has been shown to display anticancer activity either directly or indirectly through inhibition of COX-2 and several kinases, including PI3K, have been implicated in the anticancer mechanism of action resulting in the induction of cell-cycle arrest and apoptosis23,24.
An in vitro approach to simulate the process of 5-fluorouracil degradation with dihydropyrimidine dehydrogenase: the process in accordance to the first-order kinetic reaction
Published in Xenobiotica, 2021
Wei Qin, Xiaoxue Wang, Wenqian Chen, Wenwen Du, Dan Zhang, Xianglin Zhang, Pengmei Li
Stability of 5-Fluorouracil in whole blood and plasma had been discussed by previous study (Murphy et al., 1987). However, the regular pattern of the degradation process has not been studied yet. This study replicates the 5-FU degradation process in whole blood through mixing 5-FU with blank matrix in vitro and might be used to detect DPD activity. Clinical verification tests have implied that the activity of DPD enzyme in patients’ whole blood in vivo might be predicted through this approach. There is no need to take extra medication during this detection, and it can be used for prediction before 5-FU is administered compared with therapeutic drug monitoring. This method is more direct than gene detection and does not have race-specific differences. Moreover, this approach is limited for following reason. Among DPD (partial) deficiency patients, the impaired breakdown process of uracil might cause elevated endogenous uracil levels (van Staveren et al., 2013). Since the elevated uracil could compete with 5-FU on DPD reaction, which would lead to overestimating DPD activity. However, if the level of uracil concentration in DPD deficient patient is stable, below approach could accurately evaluate the apparent reaction rate of DPD. Owing to renal impairment or other incidence, if the level of uracil concentration changes, the apparent reaction rate of DPD will be reconsidered.
In silico molecular docking and in vitro antioxidant activity studies of novel α-aminophosphonates bearing 6-amino-1,3-dimethyl uracil
Published in Journal of Receptors and Signal Transduction, 2020
Rasool Shaik Nayab, Suresh Maddila, Murthy Potla Krishna, Salam J.J. Titinchi, Basha Shaik Thaslim, Venkataramaiah Chintha, Rajendra Wudayagiri, Venkateswarlu Nagam, Vijaya Tartte, Sampath Chinnam, Naga Raju Chamarthi
The uracil is one of the most prominent structures found in nucleic acid chemistry. Uracil derivatives play a key role as intermediates in the synthesis of purines [5], which constitute the basic nucleus of a number of medicinally active molecules such as caffeine (1), penciclovir (2), theobromine (3), theophylline (4) and uramustine (5) depicted in Figure 1. It is a common and naturally occurring pyrimidine derivative and one of the four nucleobases in the nucleic acid of RNA. In RNA, uracil binds to adenine via two hydrogen bonds. In DNA, the uracil nucleobase is replaced by thymine. Uracils are considered as privileged structures in drug discovery with a wide variety of biological activities [6] such as anti-viral [6], anti-tumour [7], anti-oxidant [8], anti-protozoal [9], anti-microbial [10], anti-angiogenesis [11] and anti-tuberculosis [12] agents. Further, they also possess herbicidal, insecticidal and bactericidal activities [13].