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Structural and Pharmacological Properties of Alkaloids with Special Reference to Thebaine Type Alkaloids

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Structural and Pharmacological Properties of Alkaloids with Special Reference to Thebaine Type Alkaloids Research Article ISSN: 2574 -1241 DOI: 10.26717/BJSTR.2019.17.002993 Structural and Pharmacological Properties of Alkaloids with Special Reference to Thebaine Type Alkaloids Tugba Taskin Tok1 and Sivakumar JT Gowder2 ,3* 1Department of Chemistry, Gaziantep University, 27310, Gaziantep, Turkey 2Department for Management of Science and Technology Development, Ton Duc Thang University, Vietnam 3Faculty of Applied Sciences, Ton Duc Thang University, Vietnam *Corresponding author: Sivakumar JT Gowder, Department for Management of Science and Technology Development, Ton Duc Thang University, Ho Chi Minh City, Faculty of Applied Sciences, Vietnam, email: ARTICLE INFO abstract Received: April 10, 2019 Alkaloids are pharmacologically active compounds and have a wide array of ther Published: April 24, 2019 apeutic value. Though they exhibit medicinal properties, we need to evaluate the ad verse effects of alkaloids though their structural pharmacological properties. By using a- - Citation: Tugba T T, Sivakumar J G. Structural and Pharmacological includeDiels-Alder heteroaromatic reaction (D-A), rings. we Gaussian09 identified novel and DiscoveryD-A adducts, Studio obtained 3.5 softwares with thebaine were perand Properties of Alkaloids with Special formedvarious fromdienophiles, basic to benzylidene advance basis malononitrile sets for these (1-28) compounds and metilen by using malononitrile quantum chemical (29-38) Reference to Thebaine Type Alka - 2019. BJSTR. MS.ID.002993. - descriptors such as electrophilicity index, (ω), global hardness (η) and electronic charge loids. Biomed J Sci & Tech Res 17(3)- (ΔN) to predict the probable chemical and biochemical activities of thebaine derivatives. Keywords: Alkaloids; Cytotoxicity; The endo forms of 2-(4-nitrobenzylidene)malononitrile, (o-4 and p-5) display significant- Abbreviations: ly high tendency in the electrophilicity index (ω) and electronic charge (ΔN) values. Thebaine D-A = Diels-Alder reaction; ω = Electrophilicity index; η = Global hard- Diels-Alder Reaction; Inhibitors; ness; ΔN = Electronic charge; E = Total energy; HOMO = The energy of the highest occu- ylenemalononitrilepied molecular orbital; LUMO = The energy of the lowest unoccupied molecular orbital; DM = Dipole moments; G09 = Gaussian 09; DS 3.5 = Discovery studio 3.5; MMN = 2-meth- Introduction Alkaloids century, alkaloids were first isolated successfully, and alkaloid- Alkaloids are pharmacologically active with two or more fused alkaloid, namely coniine, was established in the year 1870 by Schiff. containing drugs were marketed [2]. The structure of the first organic compounds including heteroatoms in it. These atoms Catharanthus alkaloids and paclitaxel came into the market as determine the properties of alkaloids. Especially, an alkaloid researchers looked for plant drugs with anticancer properties. containing one or more nitrogen atoms as primary or another Alkaloids are optically active, bitter in taste (except papaverine), form of amines may provide basicity to the alkaloid. Alkaloids levorotatory (exception is coniine, which is dextrorotatory), are found mainly in plants, but to the lesser extent in animals and colourless (except berberine which is yellow, and harmaline and microorganisms [1]. Many alkaloids are toxic, but they often have betanidine, which are reddish), crystalline solids (except nicotine pharmacological effects. Extraction of alkaloids from plants has and coniine, which are liquids), and soluble in organic solvents. been widely used by researchers for therapeutic and recreational They are basic and form salts with the acids; some of the alkaloids purposes. For example, Ephedra, opium poppies, and cocoa leaves form as salts called quaternary amines (e.g. cinchona alkaloids have been used medicinally since ancient times. In the nineteenth Copyright@ Sivakumar JT Gowder | Biomed J Sci & Tech Res| BJSTR. MS.ID.002993. 12767 Volume 17- Issue 3 10.26717/BJSTR.2019.17.002993 DOI: with quininic acid), while some exist as free bases (e.g. nicotine). antitussive. Cocaine is used as a local anesthetic, especially for eye Alkaloids also exist as glycosides (e.g. solanum alkaloids) and esters surgery. Morphine is an indispensable analgesic reagent that is (e.g. atropine). The biological activity of the alkaloids frequently used for the treatment of severe pain. depends on the amine function being transferred into a quaternary amine at physiological pH by protonation. In summary, alkaloids Classification of Alkaloids behave as curare or arrow poisons. Curare alkaloids, which have muscle relaxant properties, are the active ingredients of arrow Alkaloids containing wide families are classified using different poisons used by South American Indians. is based on the clinical use or pharmacological activity (analgesic techniques [4]. These techniques: Pharmacological classification Alkaloids as Medicines In general, many alkaloids are pharmacologically active and cardioactive alkaloids). Taxonomic classification is based on the family or genus (rauwolfia and cinchona alkaloids). substances which possess various physiological activities in humans or building block compounds used by plants to synthesize alkaloids Biosynthetic classification is also based on the type of precursors and animals. The use of alkaloids containing plants as dyes, drugs, (morphine, papaverine, narcotine and colchicine may be listed as or poisons can be traced back almost to the beginning of civilization phenylalanine- and tyrosine-derived bases). The last one, chemical medicine in ancient Greece, Egypt and Rome. More recently, China (Thebaine, for example, is an isoquinoline derivative alkaloids of [3]. Opium that derived from Papaver somniferum L. was used as classification, is based on the chemical structure of the alkaloid. learned about it via Arabian traders in the eighth century A.D. Today, opium; aspidospermine is an indole alkaloid.). Alkaloids are often a lot of alkaloids are still in use as drugs, against their poisonous effects. Caffeine, mostly obtained from the decaffeination of coffee described in Figure 1. species, is used a psychostimulant reagent. Codeine is used as an classified on the basis of chemical structure. These groups are Figure 1: Chemical classification of alkaloids. Opioid Structure Figure 2: Structures of morphine, codine and thebaine. Copyright@Sivakumar JT Gowder | Biomed J Sci & Tech Res| BJSTR. MS.ID.002993. 12768 Volume 17- Issue 3 10.26717/BJSTR.2019.17.002993 DOI: Morphine includes a benzene ring with a phenolic hydroxyl such as morphine or codeine. An opioid is a term used broadly to from the poppy seed. Opiates are naturally occurring alkaloids the nitrogen atom in Figure 2. When both hydroxyl groups are describe all compounds that work at the opioid receptors [6]. The group at 3-position, an alcohol hydroxyl group at 6-position, and converted to ethers, codeine and thebaine as morphine derivatives common term narcotic (from the Greek word for stupor) originally are obtained. The tertiary form of the nitrogen appears to be crucial was used to describe medications for sleep, and then was used to to the analgesic properties of morphine. The nitrogen quaternary describe opioids, but now is a legal term for drugs that are abused. widely decreases the analgesia, since morphine cannot pass into the central nervous system. Also, if the methyl group on the Opioid Receptors nitrogen is changed, it will again decrease analgesia. Morphine is Definition of an Opioid Receptor also optically active, and only the levorotatory isomer exhibits the analgesic effect. Furthermore, they have many effects on the central effects by acting at opioid receptors and whose actions are reversed Thus, the opioid is a substance that produces the above-listed nervous system. These are analgesia, respiratory depression, by naloxone. a) euphoria, and depression of cough reflex. Morphine undergoes [7]. strong first-pass metabolism by the liver if taken orally, limiting Extraction/purification of active poppy ingredient: morphine Effects: analgesia, respiratory depression, somnolence, the effective time of analgesia, unless a sustained-release form is b) depression, sedation, dizziness, nausea, vomiting, itching, and decreased GI motility. given [5]. The adverse effects of morphine include CNS respiration other complications. c) constipation. CNS respiratory depression is the serious one among meperidine > codeine > 0 Apart from these severe effects, morphine is still considered to Agonist structure-activity relationships: morphine ≥ be the most effective drug clinically available for the management of d) Structurally similar agents such as naloxone act as antagonists; severe pain associated with cancer. The opium poppy was cultivated have no effect alone but reverse the effects of an agonist. e) Opioidin Mesopotamia Receptor around Subtypes 3400 BC. Opium is a mixture of alkaloids Opioid binding interactions showed high-affinity binding sites. Figure 3: Locations of opioid receptors [kappa (κ), mu (µ) and delta (∂)]. Figure 4: Opioid receptor structure. EL: Extracellular loop, TM: Transmembrane helix, IL: Intracellular loop [8]. Copyright@ Sivakumar JT Gowder | Biomed J Sci & Tech Res| BJSTR. MS.ID.002993. 12769 Volume 17- Issue 3 10.26717/BJSTR.2019.17.002993 DOI: They may be responsible for psychomimetic and dysphoric (µ ) receptors (Figures Three types of opioid receptors have been identified so far: mu 3 & 4). Mu ( ) (agonist morphine) Mu receptors are found mainly in Sigma ( ) receptors, delta (∂) receptors, and kappa (κ
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