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Tabernaemontanine
Tabernaemontanine is a naturally occurring monoterpene indole alkaloid found in several species in the genus ''Tabernaemontana'' including ''Tabernaemontana divaricata''. History Tabernaemontanine was first reported in 1939 but its structure was only fully confirmed in the 1970s as there was confusion in the original literature regarding the configuration of the ethyl group in the piperidine ring of this alkaloid and its isomer dregamine, so that their identities had been reversed. Both compounds were isolated from plants of the dogbane (Apocynaceae) family including '' Tabernaemontana coronaria''. They have structures that are reduced versions of vobasine. Biosynthesis As with other Indole alkaloids, the biosynthesis of tabernaemontanine starts from the amino acid tryptophan. This is converted into strictosidine before further elaboration. Natural occurrence Tabernaemontanine is found commonly in the genera ''Tabernaemontana'' and ''Kopsia'', including the species '' Ervatamia h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vobasine
Vobasine is a naturally occurring monoterpene indole alkaloid found in several species in the genus ''Tabernaemontana'' including ''Tabernaemontana divaricata''. History Vobasine was first reported by Renner in 1959 after its isolation from ''Voacanga africana''. The two structurally related compounds, dregamine and tabernaemontanine, where its alkene (=CHCH3) sidechain was reduced to ethyl groups in two configurations, had their relationship confirmed in the 1970s. Vobasine has been found in many plants of the dogbane (Apocynaceae) family including '' Tabernaemontana dichotoma''. Synthesis Biosynthesis As with other Indole alkaloids, the biosynthesis of vobasine starts from the amino acid tryptophan. This is converted into strictosidine before further elaboration. Chemical synthesis The synthesis of alkaloids with the same carbon skeleton as vobasine began in the 1960s and has continued, with some work providing enantiospecific approaches to closely-related compounds. Natur ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 tryptamine with secologanin, catalyzed by the enzyme strictosidine synthase. Thousands of strictosidine derivatives are sometimes referred to by the broad phrase of monoterpene indole alkaloids. Strictosidine is an intermediate in the biosynthesis of numerous pharmaceutically valuable metabolites including quinine, camptothecin, ajmalicine, serpentine, vinblastine, vincristine and mitragynine. Biosynthetic pathways help to define the subgroups of strictosidine derivatives. Distribution Strictosidine is found in the following plant families: *Apocynaceae Here especially in Rhazya stricta and Catharanthus roseus. *Loganiaceae *Rubiaceae *Icacinaceae *Nyssaceae *Alangiaceae Recent efforts in metabolic engineering have permitted the synthesis of strictosidine by yeast (''Saccharomyces cerevisiae ''Saccharomyces ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antimalarial
Antimalarial medications or simply antimalarials are a type of antiparasitic chemical agent, often naturally derived, that can be used to treat or to prevent malaria, in the latter case, most often aiming at two susceptible target groups, young children and pregnant women. As of 2018, modern treatments, including for severe malaria, continued to depend on therapies deriving historically from quinine and artesunate, both parenteral (injectable) drugs, expanding from there into the many classes of available modern drugs. Incidence and distribution of the disease ("malaria burden") is expected to remain high, globally, for many years to come; moreover, known antimalarial drugs have repeatedly been observed to elicit resistance in the malaria parasite—including for combination therapies featuring artemisinin, a drug of last resort, where resistance has now been observed in Southeast Asia. As such, the needs for new antimalarial agents and new strategies of treatment (e.g., new combin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
European Journal Of Medicinal Chemistry
The ''European Journal of Medicinal Chemistry'' is a monthly peer-reviewed scientific journal covering medicinal chemistry and published by Elsevier. It was established in 1966 as ''Chimica Therapeutica'' (CODEN: CHTPBA) and obtained its current title in 1974. From 1974 to 1981 the journal was still subtitled as ''Chimica Therapeutica'' and from 1982 to 1986 the subtitle was ''Chimie Thérapeutique'', indicating its French origin. And now it is the journal of the French Société de Chimie Thérapeutique. The journal covers research on all aspects of medicinal chemistry and publishes original papers, laboratory notes, short or preliminary communications, and invited reviews. The ''European Journal of Medicinal Chemistry'' is abstracted and indexed in the Index medicus and MEDLINE MEDLINE (Medical Literature Analysis and Retrieval System Online, or MEDLARS Online) is a bibliographic database of life sciences and biomedical information. It includes bibliographic information for a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Voacristine
Voacristine is a indole alkaloid occurring in ''Voacanga'' and ''Tabernaemontana'' genus. It is also an iboga type alkaloid. Chemistry Its structure is almost similar to voacangine, an alkaloid used in semi-synthesis of ibogaine. Compared to voacangine, it has an extra O-atom. When it is degraded, iboxygaine and ibogaine are formed. Sources Voacristine is found in multiple species of ''Tabernaemontana'' some of which are Tabernaemontana divaricata, Tabernaemontana heyneana, Tabernaemontana ventricosa and in Voacanga africana. See also * Heyneanine * Voacamine * Vobasine Vobasine is a naturally occurring monoterpene indole alkaloid found in several species in the genus ''Tabernaemontana'' including ''Tabernaemontana divaricata''. History Vobasine was first reported by Renner in 1959 after its isolation from ''Voac ... References Tryptamine alkaloids {{Alkaloid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ibogamine
Ibogamine is an anti-convulsant, anti-addictive, CNS stimulant alkaloid found in ''Tabernanthe iboga'' and Crepe Jasmine (''Tabernaemontana divaricata''). Basic research related to how addiction affects the brain has used this chemical. Ibogamine persistently reduced the self-administration of cocaine and morphine in rats. The same study found that ibogamine (40 mg/kg) and coronaridine (40 mg/kg) did not produce "any tremor effects in rats that differ significantly from saline control". While the related alkaloids ibogaine (20–40 mg/kg), harmaline (10–40 mg/kg) and desethylcoronaridine (10–40 mg/kg) were "obviously tremorgenic". Chemistry Synthesis Ibogamine can be prepared from one-step demethoxycarbonylation process through coronaridine. Pharmacology Like ibogaine, it has seems to have similar pharmacology. It has effects on KOR, NMDAR, nAChR and serotonin sites. It also inhibits acetylcholinesterase and butyrylcholinesterase See also ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Catharanthine
Catharanthine is a terpene indole alkaloid produced by the medicinal plant ''Catharanthus roseus'' and '' Tabernaemontana divaricata''. Catharanthine is derived from strictosidine, but the exact mechanism by which this happens is currently unknown. Catharanthine is one of the two precursors that form vinblastine, the other being vindoline. Pharmacology (+)-Catharanthine competitively inhibits α9α10 nAChRs with potencies higher than that at α3β4 and α4β2 nAChRs and directly blocks CaV2.2. Catharanthine alkaloids are non competitive antagonist of muscle type nAChRs and this is thought to be the case due to presence of catharanthine moiety in those compounds. In ''in vitro'' study, it increased the levels of cAMP by inhibiting cAMP phosphodiesterase in brain. It is a potent inhibitor of TRPM8, similar to BCTC. Structural analysis of catharanthine shows activity on TRPM8, TRPA1, and butyrylcholinesterase. See also * Akuammicine * Conopharyngine * Stemmadenine St ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tabernaemontana Elegans
''Tabernaemontana elegans'', the toad tree, is a shrub or small tree in the family Apocynaceae. It is native to eastern Africa. Description ''Tabernaemontana elegans'' grows up to tall, with a trunk diameter of up to . Its fragrant flowers feature white, creamy or pale yellow corolla lobes. Fruit consists of 2 separate ovoid or ellipsoid pods, up to each. Distribution and habitat ''Tabernaemontana elegans'' grows in forests or bushland from sea level to altitude. The species is native to Somalia, Kenya, Tanzania, Mozambique, Zimbabwe, Eswatini and South Africa. Uses ''Tabernaemontana elegans'' has some local medicinal uses including the treatment of heart disease, cancer, tuberculosis and venereal diseases. The species is also used as an aphrodisiac. The Zulu name for this genus, ''iNomfi'', refers to the use of their sticky, milky latex as bird-lime. Chemistry Fourteen indole alkaloids have been isolated in the callus culture of ''Tabernaemontana elegans'' (isovoacangine ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
