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Akuammicine
Akuammicine is a monoterpene indole alkaloid of the Vinca sub-group. It is found in the Apocynaceae family of plants including ''Picralima nitida'', ''Vinca minor'' and the ''Aspidosperma''. History The alkaloids are a large group of natural products which are classified according to the part-structure which members of a particular group contain. Akuammicine is a monoterpene indole alkaloid of the Vinca sub-group which shares a common biosynthesis with other members, namely that they are derived from strictosidine. It was first isolated in 1927 and had been investigated by Sir Robert Robinson and others before its structure was correctly deduced. This was confirmed by X-ray crystallography in 2017. Natural occurrence Akuammicine is found in plants of the Apocynaceae family and was first isolated from ''Picralima nitida''. It has also been reported in ''Catharanthus roseus''. Synthesis Biosynthesis As with other indole alkaloids, the biosynthesis of akuammicine starts from t ...
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Strychnine Total Synthesis
Strychnine total synthesis in chemistry describes the total synthesis of the complex biomolecule strychnine. The first reported method by the group of Robert Burns Woodward in 1954 is considered a classic in this research field. At the time it formed the natural conclusion to an elaborate process of molecular structure elucidation that started with the isolation of strychnine from the beans of ''Strychnos ignatii'' by Pierre Joseph Pelletier and Joseph Bienaimé Caventou in 1818. Major contributors to the entire effort were Sir Robert Robinson with over 250 publications and Hermann Leuchs with another 125 papers in a time span of 40 years. Robinson was awarded the Nobel Prize in Chemistry in 1947 for his work on alkaloids, strychnine included. The process of chemical identification was completed with publications in 1946 by Robinson and later confirmed by Woodward in 1947. X-ray structures establishing the absolute configuration became available between 1947 and 1951 ...
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Monoterpene
Monoterpenes are a class of terpenes that consist of two isoprene units and have the molecular formula C10H16. Monoterpenes may be linear (acyclic) or contain rings (monocyclic and bicyclic). Modified terpenes, such as those containing oxygen functionality or missing a methyl group, are called monoterpenoids. Monoterpenes and monoterpenoids are diverse. They have relevance to the pharmaceutical, cosmetic, agricultural, and food industries. Biosynthesis Monoterpenes are derived biosynthetically from units of isopentenyl pyrophosphate, which is formed from acetyl-CoA via the intermediacy of mevalonic acid in the HMG-CoA reductase pathway. An alternative, unrelated biosynthesis pathway of IPP is known in some bacterial groups and the plastids of plants, the so-called MEP-(2-methyl-D-erythritol-4-phosphate) pathway, which is initiated from C5 sugars. In both pathways, IPP is isomerized to DMAPP by the enzyme isopentenyl pyrophosphate isomerase. Geranyl pyrophosphate is the precurso ...
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Amino Acid
Amino acids are organic compounds that contain both amino and carboxylic acid functional groups. Although hundreds of amino acids exist in nature, by far the most important are the alpha-amino acids, which comprise proteins. Only 22 alpha amino acids appear in the genetic code. Amino acids can be classified according to the locations of the core structural functional groups, as Alpha and beta carbon, alpha- , beta- , gamma- or delta- amino acids; other categories relate to Chemical polarity, polarity, ionization, and side chain group type (aliphatic, Open-chain compound, acyclic, aromatic, containing hydroxyl or sulfur, etc.). In the form of proteins, amino acid '' residues'' form the second-largest component (water being the largest) of human muscles and other tissues. Beyond their role as residues in proteins, amino acids participate in a number of processes such as neurotransmitter transport and biosynthesis. It is thought that they played a key role in enabling life ...
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Vinervine
Vinervine is a monoterpene indole alkaloid of the Vinca sub-group. It is a derivative of akuammicine, with one additional hydroxy (OH) group in the indole portion, hence it is also known as 12-hydroxyakuammicine. History The alkaloids are a large group of natural products which are classified according to the part-structure which members of a particular group contain. Vinervine is a monoterpene indole alkaloid of the Vinca sub-group which shares a common biosynthesis with other members, namely that they are derived from strictosidine. It was first characterised in 1964 and the structures of closely related materials including akuammicine were confirmed in 1983. Natural occurrence Vinervine is found in a variety of plants of the Apocynaceae family, including ''Vinca erecta'', ''Tabernaemontana divaricata'' and several other flowering plants species that are native to Africa, Asia, and Europe. Biosynthesis As with other indole alkaloids, the biosynthesis of vinervine starts fro ...
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Ajmalicine
Ajmalicine, also known as δ-yohimbine or raubasine, is an antihypertensive drug used in the treatment of high blood pressure. It has been marketed under numerous brand names including Card-Lamuran, Circolene, Cristanyl, Duxil, Duxor, Hydroxysarpon, Iskedyl, Isosarpan, Isquebral, Lamuran, Melanex, Raunatin, Saltucin Co, Salvalion, and Sarpan. It is an alkaloid found naturally in various plants such as ''Rauvolfia'' spp., ''Catharanthus roseus'', and ''Mitragyna speciosa''. Ajmalicine is structurally related to yohimbine, rauwolscine, and other yohimban derivatives. Like corynanthine, it acts as a α1-adrenergic receptor antagonist with preferential actions over α2-adrenergic receptors, underlying its hypotensive rather than hypertensive effects. Additionally, it is a very strong inhibitor of the CYP2D6 liver enzyme, which is responsible for the breakdown of many drugs. Its binding affinity at this receptor is 3.30 nM. See also * Corynanthine * Rauwolscine * Spegatrine * Yo ...
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μ-opioid Receptor
The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical μ-opioid receptor agonist is morphine, the primary psychoactive alkaloid in opium. It is an inhibitory G-protein coupled receptor that activates the Gi alpha subunit, inhibiting adenylate cyclase activity, lowering cAMP levels. Structure The structure of the μ-opioid receptor has been determined with the antagonist β-FNA, the agonist BU72, and in a complex with DAMGO and Gi protein. Splice variants Three variants of the μ-opioid receptor are well characterized, though RT-PCR has identified up to 10 total splice variants in humans. Location They can exist either presynaptically or postsynaptically depending upon cell types. The μ-opioid receptors exist mostly presynaptically in the periaqueductal gray region, and in the superfi ...
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Kappa Opioid Receptor
Kappa (uppercase Κ, lowercase κ or cursive ; el, κάππα, ''káppa'') is the 10th letter of the Greek alphabet, representing the voiceless velar plosive sound in Ancient and Modern Greek. In the system of Greek numerals, has a value of 20. It was derived from the Phoenician letter kaph . Letters that arose from kappa include the Roman K and Cyrillic К. The uppercase form is identical to the Latin K. Greek proper names and placenames containing kappa are often written in English with "c" due to the Romans' transliterations into the Latin alphabet: Constantinople, Corinth, Crete. All formal modern romanizations of Greek now use the letter "k", however. The cursive form is generally a simple font variant of lower-case kappa, but it is encoded separately in Unicode for occasions where it is used as a separate symbol in math and science. In mathematics, the kappa curve is named after this letter; the tangents of this curve were first calculated by Isaac Barrow in ...
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Glucose
Glucose is a simple sugar with the molecular formula . Glucose is overall the most abundant monosaccharide, a subcategory of carbohydrates. Glucose is mainly made by plants and most algae during photosynthesis from water and carbon dioxide, using energy from sunlight, where it is used to make cellulose in cell walls, the most abundant carbohydrate in the world. In energy metabolism, glucose is the most important source of energy in all organisms. Glucose for metabolism is stored as a polymer, in plants mainly as starch and amylopectin, and in animals as glycogen. Glucose circulates in the blood of animals as blood sugar. The naturally occurring form of glucose is -glucose, while -glucose is produced synthetically in comparatively small amounts and is less biologically active. Glucose is a monosaccharide containing six carbon atoms and an aldehyde group, and is therefore an aldohexose. The glucose molecule can exist in an open-chain (acyclic) as well as ring (cyclic) form. Gluco ...
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Ethnobotanical
Ethnobotany is the study of a region's plants and their practical uses through the traditional knowledge of a local culture and people. An ethnobotanist thus strives to document the local customs involving the practical uses of local flora for many aspects of life, such as plants as medicines, foods, intoxicants and clothing. Richard Evans Schultes, often referred to as the "father of ethnobotany", explained the discipline in this way: Ethnobotany simply means ... investigating plants used by societies in various parts of the world. Since the time of Schultes, the field of ethnobotany has grown from simply acquiring ethnobotanical knowledge to that of applying it to a modern society, primarily in the form of pharmaceuticals. Intellectual property rights and benefit-sharing arrangements are important issues in ethnobotany. History The idea of ethnobotany was first proposed by the early 20th century botanist John William Harshberger. While Harshberger did perform ethnobotanical ...
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Biological Activity
In pharmacology, biological activity or pharmacological activity describes the beneficial or adverse effects of a drug on living matter. When a drug is a complex chemical mixture, this activity is exerted by the substance's active ingredient or pharmacophore but can be modified by the other constituents. Among the various properties of chemical compounds, pharmacological/biological activity plays a crucial role since it suggests uses of the compounds in the medical applications. However, chemical compounds may show some adverse and toxic effects which may prevent their use in medical practice. Activity is generally dosage-dependent. Further, it is common to have effects ranging from beneficial to adverse for one substance when going from low to high doses. Activity depends critically on fulfillment of the ADME criteria. To be an effective drug, a compound not only must be active against a target, but also possess the appropriate ADME (Absorption, Distribution, Metabolism, and ...
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Metabolite
In biochemistry, a metabolite is an intermediate or end product of metabolism. The term is usually used for small molecules. Metabolites have various functions, including fuel, structure, signaling, stimulatory and inhibitory effects on enzymes, catalytic activity of their own (usually as a cofactor to an enzyme), defense, and interactions with other organisms (e.g. pigments, odorants, and pheromones). A primary metabolite is directly involved in normal "growth", development, and reproduction. Ethylene exemplifies a primary metabolite produced large-scale by industrial microbiology. A secondary metabolite is not directly involved in those processes, but usually has an important ecological function. Examples include antibiotics and pigments such as resins and terpenes etc. Some antibiotics use primary metabolites as precursors, such as actinomycin, which is created from the primary metabolite tryptophan. Some sugars are metabolites, such as fructose or glucose, which are both p ...
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Strychnine
Strychnine (, , US chiefly ) is a highly toxic, colorless, bitter, crystalline alkaloid used as a pesticide, particularly for killing small vertebrates such as birds and rodents. Strychnine, when inhaled, swallowed, or absorbed through the eyes or mouth, causes poisoning which results in muscular convulsions and eventually death through asphyxia. While it is no longer used medicinally, it was used historically in small doses to strengthen muscle contractions, such as a heart and bowel stimulant and performance-enhancing drug. The most common source is from the seeds of the ''Strychnos nux-vomica'' tree. Biosynthesis Strychnine is a terpene indole alkaloid belonging to the ''Strychnos'' family of '' Corynanthe'' alkaloids, and it is derived from tryptamine and secologanin. The biosynthesis of strychine was solved in 2022. The enzyme, strictosidine synthase, catalyzes the condensation of tryptamine and secologanin, followed by a Pictet-Spengler reaction to form strictosidine ...
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