Current Medicinal Chemistry - Volume 11, Issue 10, 2004

The pathogenesis of numerous cardiovascular, pulmonary, inflammatory, and thromboembolic diseases can be related to arachidonic acid (AA) metabolites. One of these bioactive metabolites of particular importance is thromboxane A2 (TXA2). It is produced by the action of thromboxane synthase on the prostaglandin endoperoxide H2 (PGH2), which results from the enzymatic degradation of AA by the cyclooxygenases. T Read More

Prostacyclin (PGI2) is a potent endogenous inhibitor of platelet function and possesses a strong vasodilator effect. Furthermore, prostacyclin is currently presented as the physiologic antagonist of thromboxane A2 (TXA2), which exhibits pro-aggregatory and vasoconstrictor properties. So, the balance between PGI2 and TXA2 production is crucial for the cardiovascular system. Indeed, an imbalance in the production or effec Read More

Peptide nucleic acids (PNAs) are recently described DNA mimics, in which the sugar-phosphate backbone is replaced by N-(2-aminoethyl)glycine units. These molecules efficiently hybridize with complementary DNA, forming Watson-Crick double helices. In addition, the interest of PNAs and PNA-based analogs is related to the fact that they are resistant to DNases and proteinases. While applications of PNAs as antisense and Read More

Artemisinin, the first and last naturally occurring 1, 2, 4-trioxane originated from Artemisia annua, L. and its derivatives are a potent class of antimalarial drugs. The clinical efficacy of these drugs is characterized by an almost immediate onset and rapid reduction of parasitemia, and it is high in such areas as well where multidrug-resistance is rampant. Furthermore, artemisinin and many of its analog possess not only anti Read More

Semicarbazide-sensitive amine-oxidase (SSAO) is present in various human tissues and in plasma. Oxidative deamination of short-chain aliphatic amines is catalyzed by this enzyme to afford the corresponding aldehydes, ammonia and hydrogen peroxide. Methylamine and aminoacetone have been recognized to be physiological substrates for SSAO. There are several pathological states where increased serum SSAO activity ha Read More

Compelling experimental and epidemiological evidence involves oxygen radicals in carcinogenesis, acting reactive oxygen species both as endogenous genotoxins during cell initiation and as messenger molecules in mitogenesis and in tumor promotion. Moreover, oxidants stimulate neoangiogenesis, which is a prerequisite for tumor growth. However, while several natural as well as synthetic antioxidant compounds a Read More

Cyclodepsipeptides comprise a wide variety of cyclic peptides of natural origin and are characterized by the occurrence of at least one ester linkage. The great interest that this class of natural products has elicited in scientific community is explained by their wide range of biological activities, intriguing mechanisms of action and attractive molecular architecture. For example, they display a variety of biological effects Read More

Estrogens are steroid hormones exhibiting a broad range of physiological activities, which are important in the homeostatic regulation of many cellular and biochemical events. Estradiol (E2) is an estrogen which is active in the development of the mammary glands and the uterus, in the maintenance of pregnancy and bone density, in protection from cardiovascular diseases, and in the relief of menopausal symptoms. Ho Read More

Polyphenolic compounds are widely distributed in higher plants and are an integral part of the human diet. Recent interest in these substances has been stimulated by their potential health benefits, which are believed to arise mainly from their antioxidant activity. In the past years, the antioxidant activity of flavonoids has been studied in detail. An important but often overlooked group of polyphenols is that of the proant Read More