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Atherosclerosis
Published in George Feuer, Felix A. de la Iglesia, Molecular Biochemistry of Human Disease, 2020
George Feuer, Felix A. de la Iglesia
Fenofibrate (1-methylethyl 2[4-(4-chlorobenzoyl)phenoxy]-2-methyl propanoate, Procetofen) has been recently applied in human therapy in Europe. This drug lowers both serum cholesterol and triglycerides. Animal experiments demonstrated that the drug may enhance cholesterol transfer from the tissues by activating HDL.89
Metabolomics and perinatal cardiology
Published in Moshe Hod, Vincenzo Berghella, Mary E. D'Alton, Gian Carlo Di Renzo, Eduard Gratacós, Vassilios Fanos, New Technologies and Perinatal Medicine, 2019
Roberta Pintus, Angelica Dessì, Vassilios Fanos
Metabolomics could be useful in the investigation of the physiological function as well, since the human heart remains mysterious. There is a metabolomics study concerning the physiology of the heart before birth and after birth. It is an animal model: ovine heart. Investigators found that in the term fetal heart, there is a higher activation of butanoate and propanoate metabolism and glycolysis. After birth, in the neonatal heart there are higher levels of purine, fatty acids, and glycerophospholipid oxidative phosphorylation (19). If the monitoring of heart metabolism at the end of pregnancy and immediately after birth will be possible in the future thanks to metabolomics, this information could be useful for the neonate at risk for heart failure, meaning, it would be possible to predict which neonate will be affected by this extremely dangerous condition.
3-Nitropropionate
Published in Dongyou Liu, Handbook of Foodborne Diseases, 2018
In fungi, the free form of 3-NPA has been identified in Arthrinium, Aspergillus, and Penicillium genera as well as in the endophytic species Diaporthe citri, Phomopsis sp. usia5 and mfer5.16,20,24,39,40 The ester form 4-hydroxyphenethyl 3-nitro-propanoate (Figure 88.2) was also isolated from Phomopsis sp. PSU-D15.41 The capability of endophytic fungi to produce 3-NPA gives rise to a debate as to whether 3-NPA in some plants is actually generated by symbiotic fungi.16 The physiological role of 3-NPA in fungi remains unestablished. However, due to its potent antimycobacterial activity,16,42 3-NPA may be utilized by fungi for colonization of ecological niches. The 3-NPA produced by endophytic fungi may be the source of protection against herbivores for their plant hosts.16,42 The naturally occurring 3-NPA from fungi accounts for most of the reported cases of human poisoning. Economically valuable fungi used in the food industry, for example, Aspergillus sp. and A. soyae, were reported to introduce 3-NPA to miso, katsuobushi, and cheese.43–45 At least 884 cases of sugarcane poisoning have been documented in the Northern regions of China from 1972 to 1989,5 with the 3-NPA produced by Arthrinium genus in improperly stored sugarcane being responsible for the mass poisonings.46
Assessment of vaping devices as an alternative respiratory drug delivery system
Published in Drug Development and Industrial Pharmacy, 2022
Zaid Khaled, Eman Zmaily Dahmash, Jasdip Koner, Raad Al Ani, Hamad Alyami, Abdallah Y. Naser
Fluticasone propionate stock solution was made from 10 mg of FP in 100 ml of acetonitrile (100 µg/ml). The HPLC method was employed for the quantitative analysis of fluticasone propanoate in the solution. The Dionex soften HPLC system from Thermo Fisher Scientific Inc. (Waltham, MA), with a gradient pump UV detector set at 256 nm using 5 μm Fortis C-18 analysis column (250 × 4.6 mm) was used. The method was developed using a mobile phase consisting of 60% acetonitrile and 40% DW. The pump flow rate was 1 ml/min with a sample injection volume of 10 μl and run time of 10 min. Validation of the two methods was done according to ICH guidelines in terms of specificity, accuracy, precision, linearity and limits of detection and LOQ [19]. To investigate the specificity of the HPLC method, 50 µl each of the stock solution (FP 100 µg/ml), and mobile phase as a blank were separately injected to the HPLC and chromatograms developed.
The new H2S-releasing compound ACS94 exerts protective effects through the modulation of thiol homoeostasis
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Daniela Giustarini, Valerio Tazzari, Ivan Bassanini, Ranieri Rossi, Anna Sparatore
A solution of cystine tertbutyl ester18 (700 mg; 1.95 mmol) and trietylamine (TEA; 0.659 ml; 4.68 mmol) in anhydrous DMF (4 ml) was added to a solution of ACS48 (1g; 3.9 mmol), HOBt (716.5 mg; 4.68 mmol) and EDAC (896 mg; 4.68 mmol) in anhydrous DMF (4 ml) and the mixture was stirred at r.t. for 24 h, under N2. After the solvent was evaporated to dryness, the crude residue was taken up with CH2Cl2, and the organic solution was washed with water, dried over anhydrous Na2SO4, and evaporated to dryness. The crude compound was then purified by CC (silica gel; CH2Cl2/MeOH; 99:1). After rinsing with ether, pure tertbutyl 3,3′-disulfanediylbis(2-(4-(3-thioxo-3H-1,2-dithiol-4-yl)benzamido)propanoate) was obtained (910 mg; yield 57%). M.p. 88–90 °C. 1H-NMR (DMSO-d6): δ = 9.18 (s, 2H); 8.97 (d, J = 7.43 Hz, 2H); 7.87 (d, J = 8.26 Hz, 4H); 7.65 (d, J = 7.98, 4H); 4.77–4.70 (m, 2H); 3.31–3.09 (m, 4H); 1.48 (s, 18H).
Structure activity evaluation and computational analysis identify potent, novel 3-benzylidene chroman-4-one analogs with anti-fungal, anti-oxidant, and anti-cancer activities
Published in Drug Development and Industrial Pharmacy, 2021
Gaffar Sarwar Zaman, Hossam Kamli, Suresh Radhakrishnan, Irfan Ahmad, Hassan Otifi, Mohamad Y. Alshahrani, Prasanna Rajagopalan
The series of 3-benzylidene chroman-4-ones (45e–64e) as shown in Figure 1 were synthesized in the laboratory. Synthesis of 3-benzylidene-6-(prop-2-enyl)-8-methoxy chroman-4-one was achieved starting from benzaldehyde and methyl acrylate. The synthesis of methyl-α-methylene-β-hydroxy-b-phenyl propanoate was achieved starting from benzaldehyde and methyl acrylate. Baylis-Hillman reaction, with DABCO as a catalyst, was carried out in solid phase using silica gel, in absence of any solvent. In general, Baylis-Hillman reaction was a slow reaction, requiring several days/weeks for completion, depending upon the reactivity or both activated alkenes and electrophile. The application of silica gel on solid phase medium was used for performing the Baylis-Hillman reaction particularly between tertiary-butyl acrylate and aromatic aldehydes under the influence of catalytic amount of DABCO (15 mol%) at increased the rates. The hydroxy propanoate was treated with hydrobromic acid with a catalytic amount of concentrated sulfuric acid at room temperature to give bromomethyl propionate. The bromomethyl propionate was treated with eugenol in presence of potassium carbonate in acetone to give methyl 3-aryl-2-(2-methoxy-4-prop-2-enyl) phenoxy ethyl prop-2-enoate. The ester was hydrolyzed by potassium hydroxide in an aqueous 1,4-dioxane at room temperature. The acid obtained by acidification of the compound is 3-aryl-2 [2-methoxy-4(prop-2-enyl)] phenoxy methyl prop-2-enoic acid. The propenoic acid was subjected to intra molecular Friedel–Crafts acylation by the action of TFAA in methylene dichloride to desired product.