ABSTRACT
Corydalis hendersonii(CH) is a Tibetan folk medicine with the functions of clearing heat, detoxifying, cooling blood, checking diarrhea, and lowering blood pressure. It is often used to treat high altitude polycythemia, vasculitis, peptic ulcer, and diarrhea. Nine compounds were separated from the ethanol extract of CH by silica gel, ODS, Sephadex LH-20 chromatography and semi-preparative HPLC. Their structures were identified as hendersine H(1),hendersine I(2), dehydrocheilanthifoline(3), protopine(4), izmirine(5), 6,7-methylenedioxy-1(2H)-isoquinolinone(6), icariside D_2(7), ethyl 4-(β-D-glucopyranosyloxy)-3-methoxybenzoate(8), 3-hydroxy-4-methoxybenzoic acid(9), respectively, by the spectroscopic data analysis and comparison with those in the literature. Among them, compounds 1 and 2 are new isoquinoline alkaloids, and compounds 7-9 are reported the first time for Corydalis. The hypoglycemic model of H9c2 cardiomyocytes and the inflammatory model of H9c2 cardiomyocytes induced by conditional supernatant were employed to determine the activities of the above compounds. The results showed that 20 μmol·L~(-1) compound 1 had a protective effect on H9c2 cardiomyocytes and 10 μmol·L~(-1) compounds 4 and 5 inhibited H9c2 cardiomyocyte inflammation induced by conditional supernatant.
Subject(s)
Humans , Corydalis/chemistry , Alkaloids/chemistry , Inflammation , Spectrum Analysis , Isoquinolines/pharmacologyABSTRACT
Cytisine derivatives are a group of alkaloids containing the structural core of cytisine, which are mainly distributed in Fabaceae plants with a wide range of pharmacological activities, such as resisting inflammation, tumors, and viruses, and affecting the central nervous system. At present, a total of 193 natural cytisine and its derivatives have been reported, all of which are derived from L-lysine. In this study, natural cytisine derivatives were classified into eight types, namely cytisine type, sparteine type, albine type, angustifoline type, camoensidine type, cytisine-like type, tsukushinamine type, and lupanacosmine type. This study reviewed the research progress on the structures, plant sources, biosynthesis, and pharmacological activities of alkaloids of various types.
Subject(s)
Alkaloids/chemistry , Quinolizines/pharmacology , Azocines/chemistry , FabaceaeABSTRACT
Abstract This study aimed to evaluate the anthelmintic and ultrastructural effects of Calotropis procera latex on Haemonchus contortus. C. procera latex was twice centrifuged at 10,000×g and dialyzed to obtain a fraction rich in proteins, named LP (latex protein), and at 3,000 rpm to obtain a fraction rich in secondary metabolites, named LNP (latex non-protein). Specimens of H. contortus exposed to LNP, LP and PBS in the Adult Worm Motility Test (AWMT) were submitted to scanning (SEM) and transmission (TEM) electron microscopy to verify changes in their ultrastructure. Phytochemical tests in the LNP indicated the presence of phenols, steroids, alkaloids and cardenolides. High-Performance Liquid Chromatography (HPLC) characterized the presence of the compounds gallic acid and quercetin in the LNP. The protein content in the LP was 43.1 ± 1.1 mg/mL and 7.7 ± 0.3 mg/mL in LNP. In AWMT, LNP and LP inhibited the motility of 100% of the nematodes, with LNP being more effective than LP and ivermectin more effective than both (p <0.05). Cuticle changes were observed by SEM and TEM in nematodes treated with LP and LNP. Calotropis procera latex has anthelmintic effects against H. contortus, causing damage to its cuticle and other alterations in its ultrastructure.
Resumo Este estudo objetivou avaliar os efeitos anti-helmínticos e ultraestruturais do látex de Calotropis procera sobre Haemonchus contortus. Látex de C. procera foi centrifugado duas vezes à a 10.000xg e dialisado para obter uma fração rica em proteínas, denominada proteínas do látex (LP). E centrifugado e centrifugado a 3.000 rpm, para obter uma fração rica em metabólitos secundários, denominada LNP (látex não proteico). Espécimes de H. contortus expostos à LNP, LP e PBS no Teste de Motilidade dos Nematoides Adultos (TMNA) foram submetidos a microscopia eletrônica de varredura (MEV) e de transmissão (MET), para verificar alterações em sua ultraestrutura. Testes fitoquímicos em LNP indicaram a presença de fenóis, esteroides, alcaloides e cardenolídeos. A presença dos compostos ácido gálico e quercetina em LNP foi caracterizada por Cromatografia Líquida de Alta Eficiência (CLAE). O conteúdo de proteínas em LP foi de 43,1 ± 1,1 mg/mL e de 7,7 ± 0,3 mg/mL em LNP. No TMNA, LNP e LP inibiram a motilidade de 100% dos nematoides, sendo LNP mais eficaz que LP, e a ivermectina mais eficaz que ambos (p <0,05). Alterações na cutícula de nematoides tratados com LP e LNP foram observadas por MEV e MET. O látex de C. procera apresenta efeito anti-helmíntico sobre H. contortus, causando danos à sua cutícula e outras alterações em sua ultraestrutura.
Subject(s)
Animals , Calotropis/chemistry , Haemonchus/drug effects , Haemonchus/ultrastructure , Latex/chemistry , Anthelmintics/pharmacology , Phenols/chemistry , Phytosterols/chemistry , Saponins/chemistry , Sheep Diseases/parasitology , Tannins/chemistry , Triterpenes/chemistry , In Vitro Techniques , Brazil , Drug Resistance , Sheep/parasitology , Microscopy, Electron, Scanning , Cardenolides/chemistry , Chromatography, High Pressure Liquid , Alkaloids/chemistry , Haemonchiasis/veterinary , Haemonchus/isolation & purification , Haemonchus/physiology , Latex/isolation & purification , Anthocyanins/chemistryABSTRACT
Pictet-Spenglerases (P-Sases) catalyze the Pictet-Spengler (P-S) reactions and exhibit high stereoselectivity and regioselectivity under mild conditions. The typical P-S reaction refers to the condensation and recyclization of β-arylethylamine with aldehyde or ketone under acidic conditions to form tetrahydroisoquinoline and β-carboline alkaloid derivatives. The related enzymatic products of P-Sases are the backbones of various bioactive compounds, including clinical drugs: morphine, noscapine, quinine, berberine, ajmaline, morphine. Furthermore, the activity of P-Sases in stereoselective and regioselective catalysis is also valuable for chemoenzymatic synthesis. Therefore, this review summarizes the research progress in the discovery, functional identification, biological characteristics and catalytic applications of P-Sases, which provide the useful theoretical reference in future P-Sases research and development.
Subject(s)
Alkaloids/chemistry , Catalysis , Enzymes/metabolism , Research/trends , Tetrahydroisoquinolines/chemistryABSTRACT
Chemical constituents and biological activities of the aerial parts of Piper erecticaule C.DC. have been studied for the first time. Fractionation and purification of the extracts afforded aristolactam AII (1), aristolactam BII (2), piperolactam A (3), piperolactam C (4), piperolactam D (5), together with terpenoids of ß-sitosterol, ß-sitostenone, taraxerol, and lupeol. The structures of these compounds were obtained by analysis of their spectroscopic data, as well as the comparison with that of reported data. Acetylcholinesterase inhibitory activity revealed that compounds 1 and 3 showed strong AChE inhibitory effects with the percentage inhibition of 75.8% and 74.8%, respectively.
Se estudiaron por primera vez los constituyentes quiÌmicos y actividad bioloÌgica de las partes aeÌreas de Piper erecticaule C.DC. El fraccionamiento y la purificacioÌn de los extractos proporcionaron aristolactama AII (1), aristolactama BII (2), piperolactama A (3), piperolactama C (4), piperolactama D (5), junto con terpenoides de ß-sitosterol, ß-sitostenona, taraxerol, y el lupeol. Las estructuras de estos compuestos se obtuvieron mediante el anaÌlisis de sus datos espectroscoÌpicos, asiÌ como mediante la comparacioÌn con datos ya informados. La actividad inhibidora de la acetilcolinesterasa reveloÌ que los compuestos 1 y 3 mostraron un potente efecto inhibidor de la AChE con un porcentaje de inhibicioÌn del 75.8% y 74.8%, respectivamente.
Subject(s)
Aporphines/pharmacology , Acetylcholinesterase/drug effects , Plant Extracts/chemistry , Cholinesterase Inhibitors/pharmacology , Piper/chemistry , Alkaloids/pharmacology , Aporphines/chemistry , Terpenes/isolation & purification , Cholinesterase Inhibitors/chemistry , Indole Alkaloids/chemistry , Alkaloids/chemistry , Lactams/chemistryABSTRACT
Plants of the genera Werneria (Asteraceae) and Xenophyllum (genus extracted from Werneria) are used in traditional medicine of Latin America for the treatment of mountain sickness, hypertension and gastrointestinal disorders. Only a small number of species of these genera have been studied, leading to the isolation of compounds belonging to the classes of benzofurans, chromenes, acetophenones, coumarates, diterpenes and pyrrolizidine alkaloids. Some of the plant extracts and/or compounds have shown antimicrobial, anti-HIV, hypotensive and photoprotective activities.
Las plantas de los geÌneros Werneria (Asteraceae) y Xenophyllum (geÌnero extraido de Werneria) son usadas en la medicina tradicional de AmeÌrica Latina para el tratamiento del mal de montanÌa, hipertensioÌn y desoÌrdenes gastrointestinales. Solo un pequenÌo nuÌmero de especies de estos geÌneros ha sido investigado, lograÌndose aislar compuestos que pertenecen a las clases de benzofuranos, cromenos, acetofenonas, cumaratos, diterpenos y alcaloides pirrolizidiÌnicos. Algunos de los extractos y/o compuestos de dichas plantas han mostrado actividades antimicrobianas, anti-HIV, hipotensoras y fotoprotectoras.
Subject(s)
Plants, Medicinal/chemistry , Plant Extracts/therapeutic use , Asteraceae/chemistry , Acetophenones/chemistry , Terpenes/analysis , Benzopyrans/chemistry , Flavonoids/chemistry , Chlorogenic Acid/chemistry , Coumaric Acids/chemistry , Alkaloids/chemistry , Altitude Sickness/drug therapy , Hypertension/drug therapy , Medicine, TraditionalABSTRACT
Se evaluó la actividad sinérgica de los alcaloides crotsparina y esparsiflorina, aislados de Croton bomplandianum Baill. con los antibacterianos gentamicina y ciprofloxacina frente a Pseudomonas aeruginosa, microorganismo frecuentemente responsable de infecciones intrahospitalarias. Se empleó el método del "tablero de damas". Se encontraron combinaciones que presentaban efecto sinérgico, logrando la reducción de 87,5% de la CMI de gentamicina, mientras que para ciprofloxacina se logró una reducción del 25,0%. Esto abre interesantes perspectivas sobre el uso combinado de productos naturales puros y fármacos en uso clínico para el tratamiento de infecciones producidas por este microrganismo(AU)
Subject(s)
Pseudomonas aeruginosa/drug effects , Gentamicins/pharmacology , Ciprofloxacin/pharmacology , Croton , Alkaloids/pharmacology , Anti-Bacterial Agents/pharmacology , Gentamicins/isolation & purification , Drug Synergism , Alkaloids/chemistryABSTRACT
The Annonaceae family is one of the largest, with 130 genre and 2500 species, consisting of trees, shrubs and a few vines. Within this family, the Pseudoxandra genus of neotropical distribution is found. In Colombia, there are endemic and native species, distributed in the Amazon region and along the valley of the Magdalena River in the Chocó. Of the total of 22 species that form the genus in Colombia, Pseudoxandra sclerocarpa Maas is exclusive of the Antioquia region, receiving the common name of garrapato or frisolo. From this tree, bisbenzylisoquinolinic alkaloids like antioquine, medellline, obaberine, among others, has been isolated. Also neolignans: dieugenol and dehydro-1-O-methydehydrodieugenol. It is used in traditional medicine as an antiparasitic. From the pharmacological point of view, the alkaloids have shown activity against leishmaniasis and also have spasmolytic activity. Within the bisbenzylisoquinolinic alkaloids, antioquine has properties of being calcium antagonist.
La familia Annonaceae es uno de los más grandes, con 130 géneros y 2.500 especies, que consiste en árboles, arbustos y algunos bejucos. Dentro de esta familia, el género Pseudoxandra es de distribución neotropical. En Colombia existen especies endémicas y nativas, distribuidas en la región del Amazonas ya lo largo del valle del río Magdalena en el Chocó. Del total de 22 especies que forman el género en Colombia, Pseudoxandra sclerocarpa es exclusiva de la región de Antioquia, recibiendo el nombre común de garrapato o frisolo. De este árbol se ha aislado alcaloides bisbencilisoquinolínicos como antioquina, medelllina, obaberina, entre otros. También neolignanos: dieugenol y dehidro-1-O-metil-dehidrodieugenol. Se utiliza en la medicina tradicional como un antiparasitario. Desde el punto de vista farmacológico, los alcaloides han mostrado actividad contra la leishmaniasis y también tienen actividad espasmolítica. Dentro de los alcaloides bisbencilisoquinolínicos, antioquina tiene propiedades de ser antagonista del calcio.
Subject(s)
Alkaloids/chemistry , Annonaceae/chemistry , Antiparasitic Agents/chemistry , Benzylisoquinolines/chemistry , Plants, Medicinal , Alkaloids/isolation & purification , Benzylisoquinolines/isolation & purification , Colombia , Medicine, TraditionalABSTRACT
The genus Nectandra belongs to the Ocotea complex and these species (Nectandra) are generally trees. It is considered endemic in the Neotropics. This genus has been reported uses in folk medicine as antifungal, anti-inflammatory, antimalarial, analgesic, treatment of ulcers, and febrifuge, among others; have also been reported some biological activity assays including: antitumor and antimalarial activity, activity against cardiovascular disease, among others. The genus Nectandra contains different secondary metabolites and they have been reported: Alkaloids; such as aporfinic, proaporfin, benzylisoquinoline, bisbenzylisoquinoline, and morfinandienone-type; lignans and neolignans, furofuran, benzofuran, tetrahydrofuran and dihydrofuran, and 3,3-neolignans-type; terpenes and sesquiterpenoid (monocyclic and bicyclic); Phytosterols and derived from those (3-hydroxy and the 3-ketone pentacyclic compounds); flavonoids, particularly O- glycosylated; xanthones, phenolic acids, polyalcohol, and alkene-alkyne, especially rubrenolide and rubrynolide.
El género Nectandra pertenece al complejo Ocotea y estas especies (Nectandra) son por lo general árboles. Se considera endémica en el Neotrópico. Este género se ha informado de usos en medicina popular como antifúngico, anti-inflamatorio, antimalárico, analgésico, el tratamiento de las úlceras, y febrífugo, entre otros; También se han informado de algunos ensayos de actividad biológica, incluyendo: antitumoral y actividad antipalúdica, actividad contra las enfermedades cardiovasculares, entre otros. El género Nectandra contiene diferentes metabolitos secundarios y se han reportado alcaloides; tales como aporfinas, proaporfina, benzylisoquinolina, y del tipo morfinandienona; lignanos y neolignanos, furofuran, benzofurano, tetrahidrofurano y dihidrofurano, y del tipo 3,3-neolignanos; terpenos y sesquiterpenoide (monocíclicos y bicíclicos); Los fitoesteroles se derivan de aquellos (3-hidroxi y los compuestos pentacíclicos 3-cetona); flavonoides, particularmente O-glicosilada; xantonas, ácidos fenólicos, polialcohol, y alqueno-alquino, especialmente rubrenolide y rubrynolida.
Subject(s)
Alkaloids/chemistry , Lauraceae/chemistry , Medicine, Traditional , Ethnobotany , Lauraceae/classificationABSTRACT
OBJECTIVE@#To develop a liquid chromatography-tandem mass spectrometry (LC-MS/MS) screening method for 45 poisonous alkaloids in blood.@*METHODS@#Identification was based on the compound's retention time and two precursor-to-production transitions. The method involved a liquid-liquid extraction (LLE) followed by LC-MS/MS with multiple-reaction monitoring (MRM). When 1 mL of blood was extracted with diethyl ether at pH = 9.2 with SKF525A as the internal standard, the target compounds were analyzed with LC-MS/MS in the positive ionization mode.@*RESULTS@#The target alkaloids had good linearity (r>0.995 1), both the intra-day precision and inter-day precision being less than 14.77%. The limits of detection ranged from 0.05 to 25 ng/mL in blood.@*CONCLUSION@#The method is selective and sensitive in detecting poisonous alkaloids with a total running time of 12 minutes; therefore it was successfully applied to some actual cases of suspected alkaloids poisoning.
Subject(s)
Humans , Alkaloids/chemistry , Chromatography, Liquid/methods , Forensic Medicine , Liquid-Liquid Extraction , Mass Spectrometry , Sensitivity and Specificity , Tandem Mass Spectrometry/methodsABSTRACT
Punarnavine (20 and 40 mg/kg) and fluoxetine (20 mg/kg) per se administered orally for 14 successive days significantly decreased immobility periods of both unstressed and stressed mice in forced swim test. These drugs also significantly decreased sucrose preference in both stressed and unstressed mice as compared to their respective controls, indicating significant antidepressant-like activity. The drugs did not show any significant effect on locomotor activity of mice. The alkaloid also significantly decreased monoamine oxidase (MAO-A) activity, malondialdehyde levels in both unstressed and stressed mice; and significantly reversed the stress-induced decrease in reduced glutathione and catalase activity. It also significantly attenuated the stress-induced increase in plasma nitrite and corticosterone levels. Thus, punarnavine showed antidepressant-like activity in unstressed and stressed mice probably through inhibition of brain MAO-A activity, decrease in plasma nitrite levels and due to its antioxidant activity. In addition, punarnavine also showed antidepressant-like activity in stressed mice possibly through decrease in plasma corticosterone levels.
Subject(s)
Alkaloids/administration & dosage , Alkaloids/chemistry , Animals , Antidepressive Agents/administration & dosage , Antidepressive Agents/chemistry , Depression/drug therapy , Depression/pathology , Humans , Mice , Motor Activity/drug effects , Nyctaginaceae/chemistry , Plant Extracts/administration & dosage , Plant Extracts/chemistry , Stress, PsychologicalABSTRACT
An alkaloid from Maclurodendron porteri has been isolated and characterized. Extraction process was conducted by acid-base extraction method followed by column chromatography. The structure was established by nuclear magnetic resonance spectroscopy and mass spectrometry. The compound was identified as haplophytin B which occurs commonly in the Rutaceae family. However, this is the first time this alkaloid was isolated and reported from the species. The compound showed no inhibition against Staphylococus aureus, Pseudomonas aeruginosa, Bacillus cereus and Escherichia coli and no cytotoxic activity against H199 and A549 cell lines.
Subject(s)
Heterocyclic Compounds, 3-Ring/isolation & purification , Alkaloids/chemistry , Alkaloids/isolation & purification , Magnetic Resonance SpectroscopyABSTRACT
Mulungu (Erythrina verna Vell., Fabaceae.) is an arboreal specie native to southeastern Brazil, used for medicinal purposes. This plant is characterized by the presence of alkaloids that have demonstrated anxiolytic activity. Due to this activity, this plant is listed by the Brazilian National Program of Medicinal Plants and Herbal Medicines. However, bibliographic information is lacking regarding this species. This study aims to describe E. verna barks, macro and microscopically, as well as some physicochemical parameters for the quality control of its raw material. In addition, the chromatographic profile of its alkaloid fraction and optimization of extraction methods for crude extract production has also been performed.
Mulungu (Erythrina verna Vell., Fabaceae.) es una especie arborea nativa del sudeste de Brasil, utilizada con fines medicinales. Esta planta se caracteriza por la presencia de alcaloides que han demostrado actividad ansiolítica. Debido a esta actividad, esta planta se encuentra en la lista del Programa Nacional Brasileño de las Plantas Medicinales y Medicinas Herbarias. Sin embargo, la información bibliográfica es escasa con respecto a esta especie. Este estudio tiene como objetivo describir E. Verna corteza, macro y microscópicamente, así como algunos parámetros físico-químicos para el control de la calidad de la materia prima fresca. Además, el perfil cromatográfico de la fracción alcaloidica y la optimización de métodos de extracción para la producción de extracto crudo también fue realizada.
Subject(s)
Alkaloids/chemistry , Erythrina/anatomy & histology , Erythrina/chemistry , Brazil , Chromatography, High Pressure Liquid , Erythrina/ultrastructure , Plants, Medicinal , Quality ControlABSTRACT
Alzheimer’s disease (AD), a progressive neurodegenerative disorder with many cognitive and neuropsychiatric symptoms is biochemically characterized by a significant decrease in the brain neurotransmitter acetylcholine (ACh). Plant-derived metabolites, including alkaloids have been reported to possess neuroprotective properties and are considered to be safe, thus have potential for developing effective therapeutic molecules for neurological disorders, such as AD. Therefore, in the present study, thirteen plant-derived alkaloids, namely pleiocarpine, kopsinine, pleiocarpamine (from Pleiocarpa mutica, family: Annonaceae), oliveroline, noroliveroline, liridonine, isooncodine, polyfothine, darienine (from Polyalthia longifolia, family: Apocynaceae) and eburnamine, eburnamonine, eburnamenine and geissoschizol (from Hunteria zeylanica, family: Apocynaceae) were analyzed for their anti-cholinergic action through docking with acetylcholinesterase (AChE) as target. Among the alkaloids, pleiocarpine showed promising anti-cholinergic potential, while its amino derivative showed about six-fold higher anti-cholinergic potential than pleiocarpine. Pleiocarpine and its amino derivative were found to be better inhibitors of AChE, as compared to commonly used drugs tacrine (brand name: Cognex) and rivastigmine (brand name: Exelon), suggesting development of these molecules as potential therapeutics in future.
Subject(s)
Alkaloids/chemistry , Alkaloids/pharmacology , Alzheimer Disease/metabolism , Catalytic Domain , Chemistry, Pharmaceutical/methods , Cholinergic Antagonists/pharmacology , Cholinesterase Inhibitors/pharmacology , Crystallography, X-Ray/methods , Drug Design , Humans , Hydrogen Bonding , Ligands , Models, Chemical , Models, Molecular , Phytotherapy , Protein Binding , Protein Conformation , Quantitative Structure-Activity RelationshipABSTRACT
Wild and tissue culture raised regenerants of Artemisia amygdalina, a critically endangered and endemic plant of Kashmir and North West Frontier Provinces of Pakistan were screened for the amount of bioactive principles and in particular antimalarial compound artemesinin. Phytochemical screening of extracts revealed the presence of terpenes, alkaloids, phenolics, tannins [polyphenolics], cardiac glycosides and steroids in wild [aerial, inflorescence] and tissue culture regenerants [in vitro grown plant, callus and green house acclimatized plants]. HPLC of Artemisia amygdalina revealed the presence of artemesinin in petroleum ether extracts of wild aerial part, tissue culture raised plant and green house acclimatized plants. Acetonitrile and water in 70:30 ratios at flow rate of 1ml/min was standardised as mobile phase. Retention time for standard chromatogram was 6.7. Wild inflorescences and callus does not produce artemesinin. This is the first report of phytochemical screening and artemesinin estimation of wild and tissue culture raised regenerants of Artemisia amygdalina
Subject(s)
Biological Factors/chemistry , Cardiac Glycosides/chemistry , Phenols/chemistry , Plant Extracts/chemistry , Steroids/chemistry , Tannins/chemistry , Terpenes/chemistry , Tissue Culture Techniques/methods , Alkaloids/chemistry , AntimalarialsABSTRACT
Vasicine [1] was isolated from the ethanolic extract of Adhatoda vasica Nees [Acanthaceae] and the structure was confirmed using spectroscopic techniques. Acetylcholine esterase, trypsin, DPPH inhibition potential and FRAP assay were carried out using in vitro models. The results showed 38.4 +/- 1.2% and 37.4 +/- 1.1% activity in acetylcholine and trypsin inhibition assays respectively. The compound [1] exhibited significant DPPH inhibition activity [70.4 +/- 1.3%, IC[50] = 212.3 +/- 1.9 microM]. A dose dependant behavior of vasicine [1], was indicated in the FRAP assay. Antibacterial activity was checked according to agar well diffusion assay and results revealed that vasicine [1] showed moderate activity
Subject(s)
Anti-Bacterial Agents/pharmacology , Antioxidants/pharmacology , Quinazolines/pharmacology , /pharmacology , Alkaloids/chemistry , Microbial Sensitivity Tests , Biphenyl Compounds/antagonists & inhibitors , Picrates/antagonists & inhibitorsABSTRACT
Malaria remains one of the most serious world health problem and the major cause of mortality and morbidity in the endemic regions. Brazil is among the 30 high-burden countries and most of the cases occur in the Legal Amazonian Region. New chemotherapeutical agents are needed for the treatment of malaria. Many plant species are used in traditional medicines of malarious countries and a relatively few number of these have been investigated for evaluation of their antimalarial effect. Still lower is the number of those that have had the active natural compounds isolated and the toxicity determined. This area is, then, of great research interest. discovery project of antimalarial natural products from plants traditionally used to treat malaria must include in vitro and in vivo assays as well as bioguided isolation of active compounds. The final products would be antimalarial chemical entities, potential new drugs or templates for new drugs development, and/or standardized antimalarial extracts which are required for pre-clinical and clinical studies when the aim is the development of effective and safe phythomedicines. This review discusses these two approaches, presents briefly the screening methodologies for evaluation of antimalarial activity and focuses the activity of alkaloids belonging to different structural classes as well as its importance as new antimalarial drugs or leads and chemical markers for phytomedicines.
A malária ainda é um dos mais sérios problemas de saúde pública e a principal causa de mortalidade e morbidade nas regiões endêmicas. O Brasil está entre os 30 países com maior incidência de malária e a maior parte dos casos ocorre na Amazônia Legal. Novos agentes terapêuticos são necessários para o tratamento da malária. Muitas espécies vegetais são utilizadas na medicina tradicional de vários países endêmicos mas é relativamente reduzido o número daquelas que já foram investigadas quanto à sua atividade antimalárica. Menor ainda é o número de espécies das quais foram isoladas substâncias ativas e tiveram sua toxidade determinada. Esta área de pesquisa é, portanto, de alta relevância. Um projeto de descoberta de produtos naturais antimaláricos a partir de plantas de uso tradicional deve incluir ensaios in vitro e in vivo bem como o isolamento biomonitorado de substâncias ativas. Os produtos finais serão substâncias naturais antimaláricas, potenciais fármacos ou protótipos para o desenvolvimento de novos fármacos, e/ou extratos padronizados, com atividade antimalárica, os quais são necessários para estudos pré-clínicos e clínicos quando o objetivo é o desenvolvimento de fitoterápicos (fitomedicamentos) eficazes e seguros. A presente revisão discute estas duas abordagens, apresenta resumidamente as metodologias de bioensaios para avaliação de atividade antimalárica e focaliza a atividade de alcalóides pertencentes a diferentes classes estruturais bem como sua importância como fármacos ou protótipos e como marcadores químicos de fitoterápicos.
Subject(s)
Animals , Humans , Alkaloids , Antimalarials , Plants, Medicinal/chemistry , Alkaloids/chemistry , Alkaloids/isolation & purification , Alkaloids/pharmacology , Antimalarials/chemistry , Antimalarials/isolation & purification , Antimalarials/pharmacology , Drug Design , PhytotherapyABSTRACT
OBJECTIVE@#To establish a liquid chromatography-tandem mass chromatography (LC-MS/MS) method for the simultaneous screening for 22 poisonous alkaloids in blood.@*METHODS@#This method involves a liquid-liquid extraction (LLE) followed by liquid chromatography-tandem mass spectrometry with multi-ple-reaction monitoring (MRM). After blood was extracted with buprenorphine as the internal standard, the target compounds were analyzed with LC-MS/MS-ESI in the positive ionization mode.@*RESULTS@#Identification was based on the compound's retention time and two precursor-to-product ion transitions. The limits of detection ranged from 0.1 ng/mL to 20 ng/mL in blood.@*CONCLUSION@#The method was sufficiently selective and sensitive to detect poisonous alkaloids and can be applied in forensic and clinical toxicology.
Subject(s)
Humans , Aconitine/blood , Alkaloids/chemistry , Chromatography, Liquid/methods , Colchicine/blood , Forensic Medicine , Sensitivity and Specificity , Strychnine/blood , Tandem Mass Spectrometry/methodsABSTRACT
The antifungal properties of aqueous and ethanol extracts of Funtumia elastica and Mallotus oppositifolius were carried out using the disc diffusion agar assay. The crude extracts exhibited definite significant antifungal activity on most of the fungi. The zone of inhibition varied for the fungi, which were: Aspergillus flavus, Candida albicans, Microsporium audouinii, Penicillium sp, Trichophyton mentagrophytes, Trichoderma sp and Trichosporon cutaneum with respect to the type of plant extract. The aqueous extracts of Mallotus oppositifolius had the highest zone of inhibition of 24.75 +/- 0.86 mm on Penicillium sp. The fulcin antibiotic had zone of inhibition of 11.94 +/- 0.43 mm on Microsporium audouinii, being its highest inhibition on any of the fungi tested. Preliminary phytochemical studies of F elastica and M oppositifolius extracts revealed that they contain anthocyanins, butacyanin, flavonoids, steroids and tannins. Phytobutanin was absent in the extracts. Heavy metal analysis of plant materials showed absence of cadmium, zinc, lead, chromium and nickel, while the presence of copper iron and manganese was less than 0.95.
Las propiedades antifúngicas de los extractos acuosos y etanólicos de Funtumia elastica y Mallotus oppositifolius fueron probadas mediante ensayo de difusión con discos en agar. Los extractos crudos mostraron poseer una actividad antifúngica definitivamente significativa sobre la mayoría de los hongos. La zona de inhibición varió en correspondencia con los hongos, a saber, Aspergillus flavus, Candida albicans, Microsporium audouinii, Penicillium sp, Trichophyton mentagrophytes, Trichoderma sp y Trichosporon cutaneum, con respecto al tipo de extracto de planta. Los extractos acuosos de Mallotus oppositifolius presentaron la zona de inhibición más alta, a saber, 24.75 ± 0.86 mm, al aplicarse sobre Penicillium sp. El antibiótico fulcin presentó una zona de inhibición de 11.94 ± 0.43 mm al aplicarse sobre Microsporium audouinii, resultando ser ésta la inhibición más alta en relación con todos los hongos sometidos a prueba. Los estudios fitoquímicos de los extractos de F elastica y M oppositifolius revelaron contenidos de antocianinas, butacianinas, flavonoides, esteroides, y taninas. La fitobutanina estuvo ausente en todos los extractos. El análisis de metales pesados en las muestras de plantas mostró ausencia de cadmio, zinc, plomo, cromo y níquel, en tanto que la presencia de cobre, hierro y manganeso estuvo por debajo de 0.95%.
Subject(s)
Humans , Mycoses , Alkaloids/chemistry , Alkaloids/pharmacology , Antifungal Agents/pharmacology , Plant Extracts/chemistry , Phytotherapy , Plants, Medicinal/chemistry , Apocynaceae/chemistry , Mallotus Plant/chemistry , Nigeria , Pilot ProjectsABSTRACT
Los géneros de la familia leguminosae se caracterizan por contener alcaloides con esqueleto quinolizidínico. Entre ellos se encuentra el género Lupinos, el cual está representado en Venezuela por varias especies, poco estudiadas botánicamente. En este trabajo se presentan los resultados obtenidos del estudiante de los alcaloides de Lupinos eremonomos S. y L. meridanus Mortiz