ABSTRACT
A first derivative spectrophotometric [[1]D] and derivative ratio [1DD] methods were utilized to determine raubasine [I] and almitrine dismesylate respectively using methanol as a solvent. A linear relationship was obtained in the range from 6-20 microg ml[-1] raubasine for the [[1]D] method and 10- 24 microg ml[-1] almitrine dismesylate for the [[1]DD] method. By applying the proposed methods, it was possible to determine raubasine in its pure powdered from with accuracy 99.94 +/- 0.860 [n = 8] for the [[1]D] method and almitrine dismesylate with accuracy 100.07 +/- 0.784 [n = 8] for the [[1]DD] method. Laboratory prepared mixtures containing different ratios of [I], [II] were analyzed by the proposed methods. The proposed methods were validated and found to be suitable assay methods for raubasine [I] and almitrine dismesylate [II] in pharmaceutical formulations
Subject(s)
Secologanin Tryptamine Alkaloids , SpectrophotometryABSTRACT
<p><b>OBJECTIVE</b>To predict the absorption of corynanthine (COR), yohimbine (YOH), ajmalicine (AMC) and ajmaline (AML) as chemical constituents of some traditional Chinese medicines in human intestinal epithelial.</p><p><b>METHOD</b>By using Caco-2 (the human colonic adenocarcinoma cell lines) cell monolayers as a human intestinal epithelial cell model, the permeability of COR, YOH, AMC and AML were studied from apical side (AP side) to basolateral side (BL side) or from BL side to AP side. The four alkaloids were measured by high performance liquid chromatography (HPLC) coupled with UV detector. Transport parameters and apty) and atenolol (a control substance of poor permeability). The relationship between P(app) and log D values of four alkaloids was investigated by using drugs ADMET predict software.</p><p><b>RESULT</b>The P(app) values of COR, YOH, AMC and AML were (1.863 +/- 0.055) x 10(-5), (1.540 +/- 0.082) x 10(-5), (2.522 +/- 0.246) x 10(-5) and (1.155 +/- 0.099) x 10(-5) cm x s(-1) from AP side to BL side, and (2.390 +/- 0.017) x 10(-5), (1.987 +/- 0.154) x 10(-5), (1.374 +/- 0.260) x 10(-5) and (2.418 +/- 0.124) x 10(-5) cm x s(-1) from BL side to AP side, respectively, which P(app) values were identical with that of propranolol [(2.23 +/- 0.10) x 10(-5) cm x s(-1) from AP to BL side]. The ratio of P(app B --> A)/P(app A -->B) of COR, YOH, AMC and AML were 1.28, 1.29, 0.54 and 2.09, respectively, which suggested that the efflux transport of AML was 2.09 times higher more than its influx transport.</p><p><b>CONCLUSION</b>COR, YOH, AMC and AML can be transported and absorbed across the human Caco-2 cells monolayers, and they belong to completely absorbed compounds. AML may have been involved in efflux mechanism in Caco-2 cells monolayers model from the BL to AP side direction. The oil-water partition coefficient play key roles in the transport and absorption of the four alkaloids.</p>
Subject(s)
Humans , Ajmaline , Metabolism , Caco-2 Cells , Chromatography, High Pressure Liquid , Epithelial Cells , Metabolism , Intestinal Mucosa , Cell Biology , Molecular Structure , Secologanin Tryptamine Alkaloids , Metabolism , Yohimbine , MetabolismABSTRACT
Although recently developed drugs have brought significant improvement, the treatment of psychotic disorders still presents serious drawbacks. Since inherent complexity and lack of satisfactory understanding of the underlying pathophysiology impose limits for rational drug design, resourceful approaches in the search for antipsychotics are pertinent. This paper reports pharmacological properties of alstonine, a heteroyohimbine type alkaloid, Which exbitited an antipsychotic-like profile, inhibiting amphetamine-induced lethaly, apomorphine-induced steotypy and potentiating barbiturate-induced slleping time. Atypical features of alstonine were the prevention of haloperidol-induced catalepsy and lack of direct interaction with D1, D2 and 5-HT2A receptors, classically linked to antipsychotic mechanism of action.
Subject(s)
Animals , Male , Mice , Antipsychotic Agents/pharmacology , Plants, Medicinal , Secologanin Tryptamine Alkaloids/pharmacology , Amphetamine/antagonists & inhibitors , Apomorphine/antagonists & inhibitors , Barbiturates/antagonists & inhibitors , Central Nervous System Stimulants/antagonists & inhibitors , Chlorpromazine/pharmacology , Clozapine/pharmacology , Diazepam/pharmacology , Emetics/antagonists & inhibitors , Haloperidol/pharmacology , Hypnotics and Sedatives/antagonists & inhibitors , Nigeria , Pentobarbital/pharmacology , Reserpine/pharmacology , Sleep/drug effects , Stereotyping , Sulpiride/pharmacologyABSTRACT
Se realizó un estudio químico de la raíz de la especie Rauvolfia viridis Roem. et Schult que crece en Cuba, con el objetivo de profundizar en este tema. Se aislaron, purificaron y caracterizaron diferentes alcaloides correspondientes a las bases débiles, entre los que se encuentran la ajmalidina, la -yohimbina, la quebrachidina, la reserpinina y la yohimbina. Se descarta la presencia de reserpina
Subject(s)
Secologanin Tryptamine Alkaloids/isolation & purification , Plant Roots/chemistry , RauwolfiaABSTRACT
Se realizó un estudio químico de la raíz de la especie de Rauvolfia viridis Roem. et Schult que crece en Cuba, con el objetivo de profundizar en este tema. Se ailaron, purificaron y caracterizaron diferentes alcaloides correspondientes a las bases débiles, entre los que se encuentran la ajmalidina, la Alfa-yohimbina, la quebrachidina, la reserpina y la yohimbina. Se descarta la presencia de reserpina
Subject(s)
Plant Roots , Rauwolfia , Secologanin Tryptamine AlkaloidsABSTRACT
Indole alkaloids in Catharanthus roseus have been in focus because of their medicinal value. These alkaloids consist of an indole moiety provided by tryptamine and a terpenoid portion provided by the secologanin. The most important catharanthus alkaloids are vinblastine (VLB), vincristine (VCR) and ajmalicine. VLB and VCR are clinically useful anticancer agents whereas ajmalicine is used for the treatment of circulatory diseases. VCR and VLB are the most expensive because of their low abundance in the plant, and are formed by the coupling of monomeric indole alkaloids vindoline and catharanthine, catalysed by peroxidases. The pathway that lead to monomeric indole alkaloids involves more than 20 enzymes of which 16 enzymes have been isolated and characterized biochemically, and only three at the molecular level. The present state of knowledge on enzymes and genes involved in indole alkaloid biosynthesis and various aspects of their regulation has been discussed.
Subject(s)
Alkaloids/biosynthesis , Genes, Plant , Genetic Engineering , Indoles/metabolism , Plants, Medicinal/enzymology , Secologanin Tryptamine Alkaloids , Vinblastine/biosynthesis , Vincristine/biosynthesis , Yohimbine/analogs & derivativesABSTRACT
Se le realiza un estudio a la fracción alcaloidal obtenida a partir de la corteza del tallo de la Rauwolfia viridis Roem. et Schult. El fraccionamiento en gradiente ácido y por distribución en contracorriente ha permitido aislar y purificar 7 alcaloides que se identifican como las bases (-) tabernaemontanina, (-) vobasina, (+) ajmalina, (+) quebrachidina y (+) serpentina. Otros 2 componentes novedosos purificados pertenecen al grupo de las bases 2-acilindólicas, los que se denominan rauviridina y epi-rauviridina. Se incluyen las constantes de distribución de los alcaloides aislados en varias combinaciones de fases inmiscibles
Subject(s)
Secologanin Tryptamine Alkaloids/isolation & purificationABSTRACT
El análisis espectroscópico (UV, IR, 1H, 13C-RMN y MS) de las bases rauviridina y epi-rauviridina ha permitido establecer una constitución correspondiente a la Nb-metil-4,5-seco-5,6-deshidro vobasina para ambos productos aislados de la corteza del tallo de Rauwolfia viridis Roem. et Schult. Se incluyen ensayos preliminares encaminados a determinar el posible origen de estas bases
Subject(s)
Secologanin Tryptamine Alkaloids/isolation & purification , Spectrum Analysis/methodsABSTRACT
Se le realiza un estudio fitoquímico preliminar a la corteza del tallo de la Rauwolfia cubana A. dC. que crece en Cuba. El fraccionamiento cromatográfico, asociado con una distribución en gradiente de acidez, permite purificar el alcaloide más abundante en esta parte del vegetal, que se identifica como 16-epi affinina, atendiendo a sus propiedades físicas y espectroscópicas. Se incluyen los espectros de 1H y 13C-RMN
Subject(s)
Secologanin Tryptamine Alkaloids/isolation & purification , Spectrum Analysis/methodsABSTRACT
Se realizaron estudios farmacológicos preliminares de las decocciones y los extractos de raíces de dos especies de Rauwolfia salicifolia y la Rauwolfia caffra Sond, comparando sus efectos hipotensores con el de la Rauwolfia serpentina empleada en la clínica por su contenido en reserpina. Se muestra el efecto de estas Rauwolfias sobre el aparato cardiovascular, mediante el empleo de diversas técnicas, y se observa un efecto hipotensor en los alcaloides totales de raíces de Rauwolfia caffra Sond y en las decocciones de la Rauwolfia salicifolia