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A Pharmacological Appraisal of Antimalarial Plant Species
Published in Namrita Lall, Medicinal Plants for Cosmetics, Health and Diseases, 2022
Mahwahwatse J. Bapela, Precious B. Ramontja, Mcebisi J. Mabuza
Aryl-amino alcohols include quinine, mefloquine, halofantrine and lumefantrine, and their antimalarial activity seem to require the presence of an aromatic portion and an amino alcohol portion (Figure 18.2). Like the 4-aminoquinolines, aryl-amino alcohols are assumed to act primarily on the erythrocyte stage of the malaria parasite by inhibiting the formation of hemozoin (Anderson et al., 2006). 8-Aminoquinolines are derived quinoline molecules with an amine group at the 8-position of quinoline. Primaquine is the only 8-aminoquinoline used in malaria therapy, and studies have shown that it interferes with the parasite’s DNA structure and disrupts its mitochondrial membranes (Miller et al., 2013). It is also the only available drug that can prevent transmission of mature gametocytes, although it can cause intravascular hemolysis in patients with glucose-6-phosphate dehydrogenase deficiency (Sinha et al., 2014). The precise mechanisms of action of the above-mentioned quinoline-based antimalarial drugs are not yet fully understood, and are still under investigation.
Animal Source Foods
Published in Chuong Pham-Huy, Bruno Pham Huy, Food and Lifestyle in Health and Disease, 2022
Chuong Pham-Huy, Bruno Pham Huy
Fats in eggs include saturated fatty acids, monounsaturated fatty acids, and polyunsaturated fatty acids (omega-3 and omega-6 fatty acids), and are only concentrated in the egg yolk (112–115). Eggs are also the principal source of dietary cholesterol of which the mean levels are about 400 mg per 100g of whole egg or about 200 mg of a medium egg (55 g). All cholesterols are found in the yolk (111–115). In addition, eggs are a rich source of phospholipids (PL) and choline (111–112, 116–117). The average large egg contains about 1.3 g of phospholipids, also known as egg yolk lecithin, which are almost exclusively found in the yolk (117). Eggs are also an excellent source of choline which is an amino alcohol. Choline is an essential nutrient and is mainly found in the yolk (680 mg/100 g in the egg yolk versus 1 mg/100 g in the egg white) (112, 116). In foods, choline is found in both water-soluble (free choline, phosphocholine, and glycerophosphocholine) and lipid-soluble forms (phosphatidylcholine and sphingomyelin), and has important and diverse functions in both cellular maintenance and growth through all life stages (112). Hard-boiled egg represents the second major source of choline after beef liver and the first source of choline in the US diet (112).
Effects of Antithrombotic and Results of Drug Screening
Published in Josef Hladovec, Antithrombotic Drugs in Thrombosis Models, 2020
Suloctidil, a sulfur-containing aminoalcohol, was originally tested as an antispasmodic with special indications in the central nervous system. It was classified mostly as a loose member of the group of calcium antagonists having a variety of other pharmacological actions including effects on the energy and lipid metabolism.371
New isoxazolidinyl-based N-alkylethanolamines as new activators of human brain carbonic anhydrases
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Doretta Cuffaro, Riccardo Di Leo, Lidia Ciccone, Alessio Nocentini, Claudiu T. Supuran, Elisa Nuti, Armando Rossello
Of note, a large series of amino-alcohol derivatives, inspired by the lead CAA β-amino alcohol timolol, has been recently reported (Figure 1)31. Timolol is selective for hCA I and hCA II isoforms, binding the active site entrance through the formation of a ternary complex with enzyme and CO233. The new amino alcohol series of CAAs were obtained by ring opening of differently substituted epoxides with isopropylamine or tert-butylamine. All the amino alcohol derivatives showed good activation properties, reporting KA values spanning from a micromolar to a nanomolar range. In particular, compound 1 (Figure 1) turned out to be highly selective for hCA II and hCA VII, thus opening new perspectives in the use of amino alcohol scaffolds as potential CAAs.
Recent advances in quantitative structure–activity relationship models of antimalarial drugs
Published in Expert Opinion on Drug Discovery, 2021
Probir Kumar Ojha, Vinay Kumar, Joyita Roy, Kunal Roy
(a) Aryl amino alcohols: Quinine, quinidine (cinchona alkaloids), mefloquine and halofantrine. (b) 4-aminoquinolines: Chloroquine and amodiaquine. (c) Folate synthesis inhibitors: Type-1 competitive inhibitors of dihydropteroate synthase-sulfones, sulfonamides; Type-2 inhibitors dihydrofolate reductase-biguanides like proguanil and chloroproguanil; diaminopyrimidine like pyrimethamine (d) 8-aminoquinolines: Primaquine and WR238, WR605 (e) Antimicrobials: Tetracycline, doxycycline, clindamycin, azithromycin, fluoroquinolones (f) Peroxides: Artemisinin (Qinghaosu) derivatives and analogs-artemether, arteether, artesunate, artelinic acid (g) Naphthoquinones: Atovaquone (h) Iron chelating agents: Desferrioxamin. The groups that receive the most attention of the researchers include the artemisinin-based combination therapy (ACTs) and chloroquine-like compounds which target the food vacuole, heme processing, and detoxification, Proguanil, as an antifolate inhibits the cytosolic DHFR after biotransformation to cycloguanil [2,6–9].
Activation of carbonic anhydrases from human brain by amino alcohol oxime ethers: towards human carbonic anhydrase VII selective activators
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Alessio Nocentini, Doretta Cuffaro, Lidia Ciccone, Elisabetta Orlandini, Susanna Nencetti, Elisa Nuti, Armando Rossello, Claudiu T. Supuran
Amino alcohols 1–16 were here assayed for their activating properties of 4 catalytically active and physiologically relevant hCA isoforms expressed in human brain, that are: the cytosolic hCA I, II, and VII, and the membrane associated hCA IV58. In the CNS context, hCA I is expressed in the motor neurons in human spinal cord59. The physiologically dominant isoform hCA II is located both in the choroid plexus, and in oligodendrocytes, myelinated tracts, astrocytes and myelin sheaths in the vertebrates brain60. hCA IV is located on the luminal surface of cerebral capillaries, associated with the blood–brain barrier, and expressed in layers III and VI in the cortex, thalamus and hippocampus60,61. CA VII is expressed in the cortex, hippocampus and thalamus62,63. CA VII might be considered a brain-associated CA as it is predominantly expressed in the brain, and absent in most other tissues. CA VII is also considered a key molecule in age-dependent neuronal pH regulation.