Metabolites, biological activities

Metabolite Biological Activity Year of First Literature Report... 

Desogestrel. Desogestrel (44) is rapidly and nearly completely converted to the biologically active metabolite 3-ketodesogestrel [14048-10-1]... 

The held of marine natural products chemistry, which encompasses the study of the chemical structures and biological activities of secondary metabolites produced by marine plants, animals, and microorganisms, began in earnest in the early 1960s. " This is in stark contrast to the study of terrestrial plant natural... 

The hormone peptide YY (PYY) is a 36 amino acid peptide, which is closely related to neuropeptide Y and pancreatic polypeptide. PYY is predominantly synthesised and released by intestinal endocrine cells, and can also coexist with glucagon in pancreatic acini and enteroglucagon in endocrine cells of the lower bowel. It acts on the same receptors as neuropeptide Y. The endogenous long C-terminal PYY fragment PYY3 36 is a biologically active and subtype-selective metabolite. 

Although a -trans- and 9-cis-RA are only minor metabolites of ROL and (3-carotene, they display 100-1000-fold higher biological activity. Whereas all-trans-RA binds only to RARs, 9-cis-RA binds both RARs and RXRs. The stereoisomer of all-irarcs-RA, 13-cis-RA, exhibits a much lower affinity for RARs and RXRs and exerts its molecular effects mostly through its isomerization into all-irarcs-RA. 

Benzo[a]pyrene, a molecule with five, fused, hexagonal rings, is among the most carcinogenic of the polycyclic aromatic hydrocarbons (PAHs). Such biological activity may be related to the electronic structure of benzo[a]pyrene and its metabolites. Ionization energies of these molecules therefore have been investigated with photoelectron spectroscopy [28]. 

H)2-D3 is a weak agonist and must be modified by hydroxylation at position Cj for full biologic activity. This is accomplished in mitochondria of the renal proximal convoluted tubule by a three-component monooxygenase reaction that requires NADPFl, Mg, molecular oxygen, and at least three enzymes (1) a flavoprotein, renal ferredoxin reductase (2) an iron sulfur protein, renal ferredoxin and (3) cytochrome P450. This system produces l,25(OH)2-D3, which is the most potent namrally occurring metabolite of vitamin D. 

Morphine and its derivatives continue to be considered the gold standard for alleviating pain. Morphine is metabolized in the liver via N-dealkylation and glu-coronidation at the third (M3G) or sixth position (M6G). Although M3G are the most common metabolites (accounts for 50% of the metabolites produced), they elicit no biological activity when bound to MOR. It is the M6G metabolite (accounts for 10% of the metabohtes produced) that elicits the nociceptive/analgesic effect upon binding to the p opioid receptor (Dahan et al. 2008). M6G is predominately eliminated via renal excretion. 

Savi P, Pereillo JM, Uzabiaga ME, Combalbert J, Picard C, Maffrand JP, Pascal M, Herbert JM. Identification and biological activity of the active metabolite of clopidogrel. Thromb Haemost 2000 84 891-896. 

Phytochemicals are biologically-active, non-nutritive secondary metabolites which provide plants with colour, flavour and natural toxicity to pests. The classification of this huge range of compounds is still a matter of debate, but they fall into three main groups ... 

The discovery that, in industrialised societies, diets deficient in fruits and vegetables can effectively double the risk of developing many different types of cancer has focused renewed attention on the beneficial properties of these foods (Block e/a/., 1992 Patterson ef a/., 1990 Southon and Faulks, 2002). As we have seen, plant foods are rich in micronutrients, but they also contain an immense variety of biologically active secondary metabolites providing colour, flavour and natural toxicity to pests and sometimes humans (Johnson et ah, 1994). The chemistry and classification of such substances is still a matter for much research and debate, but this has not prevented attempts to isolate and exploit substances that have variously been termed protective factors , phytoprotectants , phytochemicals and nutraceuticals . Phytochemical compounds include ... 

If, for example, the route from parent carcinogen to the actual biologically-active metabolite is considered as a multi-step pathway, the terms that appear in the model equation can be thought of as representing the rate-determining steps. 

Marine sponges are a source of an array of polycyclic diamine alkaloids of common biogenetic origin. This class of secondary metabolites has been the subject of four previous reviews [4-7]. Therefore, the present review will include literature reports previously not discussed, dealing with the isolation, structure determination, biological activities, and total synthesis of polycycUc diamine alkaloids isolated from marine sponges. This review will not include guanidine alkaloids [8,9] or the manzamine alkaloids [10,11], since these compounds have been recently reviewed elsewhere. Only polycycUc... 

Application of Preparative Layer Chromatography for the Separation of Secondary Metabolites from Plant Tissues for Their Biological Activity Determination... 

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