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Conolidine
Conolidine is an indole alkaloid. Preliminary reports suggest that it could provide analgesic effects with few of the detrimental side-effects associated with opioids such as morphine, though at present it has only been evaluated in mouse models. Conolidine was first isolated in 2004 from the bark of the ''Tabernaemontana divaricata'' (crepe jasmine) shrub which is used in traditional Chinese medicine. The first asymmetric total synthesis of conolidine was developed by Micalizio and coworkers in 2011. This synthetic route allows access to either enantiomer (mirror image) of conolidine via an early enzymatic resolution. Notably, evaluation of the synthetic material resulted in the discovery that both enantiomers of the synthetic compound show analgesic effects. Syntheses The Micalizio route (2011) achieved the end product in 9 steps from a commercially available acetyl-pyridine. Notable reactions include a ,3Still-Wittig rearrangement and a conformationally-controlled int ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tabernaemontana Divaricata
''Tabernaemontana divaricata'', commonly called pinwheel flower, crape jasmine, East India rosebay, and Nero's crown, is an evergreen shrub or small tree native to South Asia, Southeast Asia and China. In zones where it is not hardy it is grown as a house/glasshouse plant for its attractive flowers and foliage. The stem exudes a milky latex when broken, whence the name milk flower. Description The plant generally grows to a height of and is dichotomously branched. The large shiny leaves are deep green and about in length and in width. The waxy blossoms are found in small clusters on the stem tips. The (single) flowers have the characteristic 'pinwheel' shape also seen in other genera in the family Apocynaceae such as ''Vinca'' and ''Nerium''. Both single and double-flowered forms are cultivated, the flowers of both forms being white. The plant blooms in spring but flowers appear sporadically all year. The flowers have a pleasing fragrance. More than 66 alkaloids are found ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Conotoxin
A conotoxin is one of a group of neurotoxic peptides isolated from the venom of the marine cone snail, genus ''Conus''. Conotoxins, which are peptides consisting of 10 to 30 amino acid residues, typically have one or more disulfide bonds. Conotoxins have a variety of mechanisms of actions, most of which have not been determined. However, it appears that many of these peptides modulate the activity of ion channels. Over the last few decades conotoxins have been the subject of pharmacological interest. The LD50 of conotoxin ranges from 5-25 μg/kg. Hypervariability Conotoxins are hypervariable even within the same species. They do not act within a body where they are produced (endogenously) but act on other organisms. Therefore, conotoxin genes experience less selection against mutations (like gene duplication and nonsynonymous substitution), and mutations remain in the genome longer, allowing more time for potentially beneficial novel functions to arise. Variability in c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesics
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It is typically used to induce cooperation with a medical procedure. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, traditional analgesics are less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Conofoline
Conofoline is an alkaloid of the vinca alkaloid class which is closely related to conophylline. It is found in the leaves of some species in the genus ''Tabernaemontana'', including ''Tabernaemontana divaricata'', and in '' Ervatamia peduncularis''. See also * Conolidine * Conopharyngine Conopharyngine is the major alkaloid present in the leaves and stem-bark of '' Tabernaemontana pachysiphon'' and '' Conopharyngia durissima''. It is closely related voacangine and coronaridine. Conopharyngine pseudoindoxyl, a derivative of it, i ... References Indolizidines Indolines Carbazoles Heterocyclic compounds with 6 rings Epoxides Methoxy compounds {{alkaloid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Stemmadenine
Stemmadenine is a terpene indole alkaloid. Stemmadenine is believed to be formed from preakuammicine by a carbon-carbon bond cleavage. Cleavage of a second carbon-carbon bond is thought to form dehydrosecodine. The enzymes forming stemmadenine and using it as a substrate remain unknown to date. It is thought to be intermediate compound in many different biosynthetic pathways such as in Aspidosperma species. Many alkaloids are proposed to be produced through intermediate stemmadenine. Some of them are: * Catharanthine and Tabersonine in ''Catharanthus roseus'' * Subincanadines D-F in '' Aspidosperma subincanum'' It is also present as product in plant like in '' Tabernaemontana dichotoma'' seeds. Pharmacology It has hypotensive and weak muscle relaxant properties. See also *Secologanin *Strictosidine Strictosidine is a natural chemical compound and is classified as a glucoalkaloid and a vinca alkaloid. It is formed by the Pictet–Spengler condensation reaction of tr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pericine
Pericine is one of a number of indole alkaloids found in the tree '' Picralima nitida'', commonly known as akuamma. As with some other alkaloids from this plant such as akuammine, pericine has been shown to bind to mu opioid receptors ''in vitro'', and has an IC50 of 0.6 μmol, within the range of a weak analgesic. It may also have convulsant effects. Pericine has been prepared in the laboratory by total synthesis Total synthesis is the complete chemical synthesis of a complex molecule, often a natural product, from simple, commercially-available precursors. It usually refers to a process not involving the aid of biological processes, which distinguishes i .... See also * Vobasine * Isovoacristine References Opioids Indole alkaloids Alkaloids found in Apocynaceae Bridged heterocyclic compounds Mu-opioid receptor agonists Azocines {{alkaloid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lochnericine
Lochnericine is a major monoterpene indole alkaloid present in the roots of ''Catharanthus roseus''. It is also present in ''Tabernaemontana divaricata''. Chemistry Synthesis Lochnericine is formed from stereoselective epoxidation of carbons 6 and 7 of tabersonine. Derivatives See also * Pericine * Pervine * Tabersonine * Vincamine Vincamine is a monoterpenoid indole alkaloid found in the leaves of ''Vinca minor'' (lesser periwinkle), comprising about 25-65% of its indole alkaloids by weight. It can also be synthesized from related alkaloids. Uses Vincamine is sold in Eu ... References {{Reflist Indole alkaloids Alkaloids found in Apocynaceae ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bioorganic & Medicinal Chemistry
''Bioorganic & Medicinal Chemistry'' is a scientific journal focusing on the results of research on the molecular structure of biological organisms and the interaction of biological targets with chemical agents.Bioorganic & Medicinal Chemistry' It is published by Elsevier Elsevier () is a Dutch academic publishing company specializing in scientific, technical, and medical content. Its products include journals such as '' The Lancet'', '' Cell'', the ScienceDirect collection of electronic journals, '' Trends'', ..., which also publishes the related journal '' Bioorganic & Medicinal Chemistry Letters''. References Biochemistry journals Elsevier academic journals English-language journals Medicinal chemistry journals {{biochem-journal-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bioorganic & Medicinal Chemistry Letters
''Bioorganic & Medicinal Chemistry Letters'' is a scientific journal focusing on the results of research on the molecular structure of biological organisms and the interaction of biological targets with chemical agents. It is published by Elsevier, which also publishes ''Bioorganic & Medicinal Chemistry ''Bioorganic & Medicinal Chemistry'' is a scientific journal focusing on the results of research on the molecular structure of biological organisms and the interaction of biological targets with chemical agents.Bioorganic & Medicinal Chemistry' It ...'' for longer works. Biochemistry journals Elsevier academic journals English-language journals Medicinal chemistry journals {{biochem-journal-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
