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1.
Molecules ; 26(23)2021 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-34885772

RESUMO

Three novel monoterpenoid indole alkaloids gardflorine A (1), gardflorine B (2), and gardflorine C (3) were isolated from the leaves of Gardneria multiflora. Their structures, including absolute configurations, were established on the basis of spectroscopic methods (MS, UV, IR, 1D and 2D NMR) and circular dichroism experiments. All the compounds were evaluated for their vasorelaxant and acetylcholinesterase (AChE) inhibitory activities. Compound 1 exhibited potent vasorelaxant activity, with an EC50 value of 8.7 µM, and compounds 2 and 3 showed moderate acetylcholinesterase (AChE) inhibitory activities, with IC50 values of 26.8 and 29.2 µM, respectively.


Assuntos
Inibidores da Colinesterase/farmacologia , Loganiaceae/química , Folhas de Planta/química , Alcaloides de Triptamina e Secologanina/farmacologia , Vasodilatadores/farmacologia , Inibidores da Colinesterase/química , Dicroísmo Circular , Espectroscopia de Prótons por Ressonância Magnética , Alcaloides de Triptamina e Secologanina/química , Vasodilatadores/química
2.
J Nat Prod ; 84(4): 1409-1413, 2021 04 23.
Artigo em Inglês | MEDLINE | ID: mdl-33825474

RESUMO

Hemitheion (1), a new sulfur-containing vobasane-type indole alkaloid, was isolated, together with three known compounds, vobasine (2), gelsedine (3), and gelsemicine (4), from the alkaloid extract of the stems of Mostuea brunonis Didr. (Gelsemiaceae). Compound 1 could be straightforwardly isolated. Its structure was elucidated by a combination of spectroscopic methods. Besides corresponding to a formerly postulated biosynthetic intermediate toward theionbrunonines, hemitheion (1) stands among the few monomeric vobasanes lacking an oxygen at C-3. Hemitheion (1) showed moderate antiplasmodial activity in the micromolar range against the strain FcB1 of Plasmodium falciparum and no cytotoxic activity against the MRC-5 cell line at 20 µM.


Assuntos
Antimaláricos/farmacologia , Alcaloides Indólicos/farmacologia , Loganiaceae/química , Antimaláricos/isolamento & purificação , Linhagem Celular , Gabão , Humanos , Alcaloides Indólicos/isolamento & purificação , Estrutura Molecular , Oxindóis , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Caules de Planta/química , Plasmodium falciparum
3.
J Sep Sci ; 43(8): 1450-1457, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32031325

RESUMO

Buddleja officinalis Maxim., a deciduous, flowering shrub, is used as a traditional Chinese medicine; the bioactivity of B. officinalis is primarily due to flavonoids and phenylethanoid glycosides. In the study, acteoside and linarin were successfully isolated from B. officinalis by high-speed countercurrent chromatography with a two-phase solvent system composed of ethyl acetate: n-butanol: water (5:0.8:5, v/v/v). The purities of acteoside and linarin were determined to be 97.3 and 98.2%, respectively, using one-step high-speed countercurrent chromatography separation. The chemical structures of the two compounds were identified by electrospray ionization-mass spectrometry and nuclear magnetic resonance. After separation, the anti-inflammatory effects of the two compounds were evaluated using lipopolysaccharide-induced human umbilical vein endothelial cells. Acteoside and linarin inhibited the expression of nitric oxide, tumor necrosis factor α and interleukin 1ß, which demonstrated that acteoside and linarin possessed anti-inflammatory activity.


Assuntos
Anti-Inflamatórios/farmacologia , Flores/química , Glucosídeos/farmacologia , Glicosídeos/farmacologia , Loganiaceae/química , Óxido Nítrico/antagonistas & inibidores , Fenóis/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Células Cultivadas , Distribuição Contracorrente , Glucosídeos/química , Glucosídeos/isolamento & purificação , Glicosídeos/química , Glicosídeos/isolamento & purificação , Humanos , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Medicina Tradicional Chinesa , Estrutura Molecular , Óxido Nítrico/biossíntese , Fenóis/química , Fenóis/isolamento & purificação
4.
J Ethnopharmacol ; 238: 111851, 2019 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-30978458

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Anthocleista vogelii Planch (Loganiaceae) is used in African Traditional Medicine for the treatment of pain and inflammatory disorders as well as sleeping sickness. AIM OF THE STUDY: To determine the in vivo anti-inflammatory and in vitro anti-trypanosomal activities of the extracts of A. vogelii stem bark and identify the phytochemical classes of the fractions responsible for the activities. MATERIALS AND METHODS: The in vivo anti-inflammatory activity of the extracts was evaluated using the egg albumin-induced rat paw oedema model while the in vitro anti-trypanosomal activity was assessed on Trypanosoma brucei brucei. The in vitro cytotoxicity was assessed on HeLa (human cervix adenocarcinoma) cell line. RESULTS: The methanolic extract of A. vogelii stem bark, with 11.2% yield, gave LD50 > 5000 mg/kg. The n-hexane fraction of the extract contains steroids, terpenes and fatty acids and yielded non-cytotoxic terpenoidal column fraction with anti-trypanosomal IC50 of 3.0 µg/mL. The ethylacetate fraction at 100 mg/kg dose significantly (p < 0.05) provoked 37.8, 62.5 and 69.7% inhibition of oedema induced by egg-albumin at the second, fourth and sixth hours respectively. CONCLUSION: The study demonstrated that the anti-inflammatory and anti-trypanosomal activities of A. vogelii are probably due to non-cytotoxic terpenoids and validated the traditional use of A. vogelii in the treatment of inflammation and sleeping sickness.


Assuntos
Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Edema/tratamento farmacológico , Tripanossomicidas/farmacologia , Tripanossomicidas/uso terapêutico , Trypanosoma brucei brucei/efeitos dos fármacos , Animais , Anti-Inflamatórios/química , Sobrevivência Celular/efeitos dos fármacos , Feminino , Células HeLa , Humanos , Dose Letal Mediana , Loganiaceae , Masculino , Camundongos , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Casca de Planta , Caules de Planta , Ratos Wistar , Tripanossomicidas/química
5.
J Complement Integr Med ; 16(1)2019 Jan 19.
Artigo em Inglês | MEDLINE | ID: mdl-30661055

RESUMO

Background Estrogen deficiency in postmenopausal period causes severe neuroendocrine changes in brain which influences memory and other nervous functions. Anthocleista schweinfurthii is used traditionally to treat female infertility and menopause related symptoms. This study was performed to investigate the potential neuroprotective effects of aqueous extract of Anthocleista schweinfurthii on brain in a postmenopause-like model of ovariectomized Wistar rats. Methods Thirty animals were sham-operated or ovariectomized (Ovx) 84 days after surgery, six groups of five rats each were daily treated orally during 28 days with: distilled water for groups 1 (sham-operated) and 2 (Ovx), estradiol valerate (group 3) and the three doses of extracts {groups 4, 5 and 6 (Ovx)}. Biochemical and histological evaluations focused on brain. Results Compared to sham-operated control, ovariectomy decreased total protein levels in brain (p<0.01) which was increased by plant extract at the dose of 300 mg/kg (p<0.05), underlying its anabolic properties. Ovariectomy significantly decreased magnesium levels in brain (p<0.001). Anthocleista schweinfurthii increased significantly magnesium levels (p<0.01), showing its capacity to act on synaptic conduction. Ovariectomy induced oxidative stress by increasing malondialdehyde levels (p<0.05) and decreasing reduced glutathione levels (p<0.05) in brain. The plant extract exhibited antioxidative activity by reducing malondialdehyde levels and increasing glutathione levels in brain. Damage in brain structure which was caused by ovariectomy disappeared following the treatment. Conclusions Results suggest that Anthocleista schweinfurthii may have neuroprotective effects in Ovx Wistar rats by increasing total protein, magnesium levels and reducing oxidative stress in brain.


Assuntos
Loganiaceae/química , Fármacos Neuroprotetores/administração & dosagem , Casca de Planta/química , Extratos Vegetais/administração & dosagem , Pós-Menopausa/efeitos dos fármacos , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Feminino , Glutationa/metabolismo , Humanos , Magnésio/metabolismo , Malondialdeído/metabolismo , Modelos Animais , Fármacos Neuroprotetores/química , Ovariectomia , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Pós-Menopausa/metabolismo , Ratos , Ratos Wistar
6.
Curr Biol ; 28(6): R249-R252, 2018 03 19.
Artigo em Inglês | MEDLINE | ID: mdl-29558636
7.
Am J Chin Med ; 46(1): 1-23, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29298518

RESUMO

Strychnos nux-vomica L. belongs to the genus Strychnos of the family Loganiaceae and grows in Sri Lanka, India and Australia. The traditional medicinal component is its seed, called Nux vomica. This study provides a relevant and comprehensive review of S. nux-vomica L., including its botany, ethnopharmacology, phytochemistry, pharmacology and toxicology, thus providing a foundation for future studies. Up to the present day, over 84 compounds, including alkaloids, iridoid glycosides, flavonoid glycosides, triterpenoids, steroids and organic acids, among others, have been isolated and identified from S. nux-vomica. These compounds possess an array of biological activities, including effects on the nervous system, analgesic and anti-inflammatory actions, antitumor effects, inhibition of the growth of pathogenic microorganisms and regulation of immune function. Furthermore, toxicity and detoxification methods are preliminarily discussed toward the end of this review. In further research on S. nux-vomica, bioactivity-guided isolation strategies should be emphasized. Its antitumor effects should be investigated further and in vivo animal experiments should be performed alongside in vitro testing. The pharmacological activity and toxicology of strychnine [Formula: see text]-oxide and brucine [Formula: see text]-oxide should be studied to explore the detoxification mechanism associated with processing more deeply.


Assuntos
Strychnos nux-vomica/química , Strychnos nux-vomica/toxicidade , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Analgésicos , Animais , Anti-Inflamatórios , Antineoplásicos Fitogênicos , Óxidos N-Cíclicos/farmacologia , Óxidos N-Cíclicos/toxicidade , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Humanos , Técnicas In Vitro , Glicosídeos Iridoides/isolamento & purificação , Glicosídeos Iridoides/farmacologia , Loganiaceae , Fitoterapia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Sementes/química , Estricnina/análogos & derivados , Estricnina/farmacologia , Estricnina/toxicidade
8.
Fitoterapia ; 124: 8-11, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29128600

RESUMO

Six new monoterpenoid indole alkaloids, 19(E)-9-demethoxy-16-dehydroxylchitosenine-17-O- ß-d-glucopyranoside (1), 19(E)-9,10-didemethoxy-16-dehydroxylchitosenine-17-O-ß-d-gluco-pyranoside (2), 19(E)-9,10-didemethoxy-16-dehydroxyl-11-methoxychitosenine (3), 19(E)-9,10-didemethoxy-16-dehydroxyl-11-methoxychitosenine-17-O-ß-d-glucopyranoside (4), 19(Z)-18-carboxylgardneramine (5), and 19(E)-18-demethoxygardneramine-N (4)-oxide (6), along with four known alkaloids, were isolated from Gardneria multiflora, and their structures were elucidated by spectroscopic analysis. Compounds 1, 2 and 4 are the first example of Gardneria alkaloids whose glucose units were attached to C-17. None of the compounds were cytotoxic to any of five human cancer cell lines.


Assuntos
Loganiaceae/química , Alcaloides de Triptamina e Secologanina/química , Linhagem Celular Tumoral , Humanos , Estrutura Molecular , Folhas de Planta/química , Caules de Planta/química
9.
PLoS One ; 12(12): e0189803, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29244856

RESUMO

Gastrointestinal nematodes are a significant concern for animal health and well-being, and anthelmintic treatment is mainly performed through the use of chemical products. However, bioactive compounds produced by plants have shown promise for development as novel anthelmintics. The aim of this study is to assess the anthelmintic activity of protein fractions from Spigelia anthelmia on the gastrointestinal nematode Haemonchus contortus. Plant parts were separated into leaves, stems and roots, washed with distilled water, freeze-dried and ground into a fine powder. Protein extraction was performed with sodium phosphate buffer (75 mM, pH 7.0). The extract was fractionated using ammonium sulfate (0-90%) and extensively dialyzed. The resulting fractions were named LPF (leaf protein fraction), SPF (stem protein fraction) and RPF (root protein fraction), and the protein contents and activities of the fractions were analyzed. H. contortus egg hatching (EHA), larval exsheathment inhibition (LEIA) and larval migration inhibition (LMIA) assays were performed. Proteomic analysis was conducted, and high-performance liquid chromatography (HPLC) chromatographic profiles of the fractions were established to identify proteins and possible secondary metabolites. S. anthelmia fractions inhibited H. contortus egg hatching, with LPF having the most potent effects (EC50 0.17 mg mL-1). During LEIA, SPF presented greater efficiency than the other fractions (EC50 0.25 mg mL-1). According to LMIA, the fractions from roots, stems and leaves also reduced the number of larvae, with EC50 values of 0.11, 0.14 and 0.21 mg mL-1, respectively. Protein analysis indicated the presence of plant defense proteins in the S. anthelmia fractions, including protease, protease inhibitor, chitinase and others. Conversely, secondary metabolites were absent in the S. anthemia fractions. These results suggest that S. anthelmia proteins are promising for the control of the gastrointestinal nematode H. contortus.


Assuntos
Anti-Helmínticos/uso terapêutico , Hemoncose/tratamento farmacológico , Haemonchus/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Animais , Anti-Helmínticos/química , Cromatografia Líquida de Alta Pressão , Hemoncose/parasitologia , Hemoncose/veterinária , Haemonchus/patogenicidade , Larva/efeitos dos fármacos , Larva/patogenicidade , Loganiaceae/química , Extratos Vegetais/química , Folhas de Planta/química , Proteínas de Plantas/administração & dosagem , Proteínas de Plantas/química , Proteômica
10.
J Basic Clin Physiol Pharmacol ; 28(5): 425-435, 2017 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-28777735

RESUMO

BACKGROUND: The root bark of Anthocleista djalonensis A. Chev. (Loganiaceae) is widely used in traditional medicine in Northern Cameroon to treat epilepsy and related conditions, such as migraine, insomnia, dementia, anxiety, and mood disorders. METHODS: To investigate the anticonvulsant effects and the possible mechanisms of this plant, an aqueous extract of Anthocleista djalonensis (AEAD) was evaluated by using animal models of bicuculline-, picrotoxin-, pilocarpine-, and pentylenetetrazole-induced convulsions. Their effects on brain γ-aminobutyric acid (GABA) concentration and GABA-T activity were also determined. RESULTS: This extract significantly protected mice against bicuculline-induced motor seizures. It provided 80% protection against picrotoxin-induced tonic-clonic seizures, and strongly antagonized convulsions induced by pilocarpine. AEAD also protected 100% of mice against pentylenetetrazole-induced seizures. Flumazenil, a central benzodiazepine receptor antagonist and FG7142, a partial inverse agonist in the benzodiazepine site of the GABAA receptor complex, were found to have an inhibitory effect on the anticonvulsant action of AEAD in pentylenetetrazole test. Finally, the brain GABA concentration was significantly increased and GABA-T activity was inhibited by AEAD. CONCLUSIONS: The effects of Anthocleista djalonensis suggested the presence of anticonvulsant properties that might involve an action on benzodiazepine and/or GABA sites in the GABAA receptor complex or by modulating GABA concentration in the central nervous system (CNS).


Assuntos
Anticonvulsivantes/farmacologia , Loganiaceae/química , Casca de Planta/química , Raízes de Plantas/química , Ácido gama-Aminobutírico/metabolismo , Animais , Benzodiazepinas/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Pentilenotetrazol/farmacologia , Fitoterapia/métodos , Extratos Vegetais/farmacologia , Convulsões/tratamento farmacológico , Convulsões/metabolismo
11.
Nat Plants ; 2: 16005, 2016 02 15.
Artigo em Inglês | MEDLINE | ID: mdl-27249345

RESUMO

Fossils preserved in amber may provide significant palaeoevolutionary and biogeographical data regarding the evolution of life on Earth(1). Although amber is particularly noted for its detailed preservation of arthropods, the same degree of preservation can be found for vascular plant remains(2). Mid-Tertiary Dominican amber is a rich source for such fossils, and representatives of several angiosperm families have been described. However, no fossilized examples of the large asterid plant clade have yet been reported. Here we describe the first fossil neotropical flowers found in amber from a representative of the asterids. The asterids are one of the largest lineages of flowering plants, containing groups such as the sunflower, potato, coffee and mint families, totalling over 80,000 species(3). The new fossils are only known as flowers, more precisely corollas with stamens and styles. We here describe them as a new species, Strychnos electri sp. nov, in the plant family Loganiaceae (Gentianales).


Assuntos
Loganiaceae/classificação , Magnoliopsida/classificação , Âmbar , Flores/classificação , Flores/genética , Fósseis , Loganiaceae/genética , Magnoliopsida/genética
12.
Am J Phys Anthropol ; 159(1): 85-92, 2016 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-26345277

RESUMO

OBJECTIVE: The objective of the current study was to investigate the lateral dominance for a bimanually coordinated natural feeding behavior in semi-wild chimpanzees. METHODS: Strychnos spp. fruit consumption behaviors in semi-wild chimpanzees as an ecologically comparable feeding behavior to those found in cerebral lateralization studies of non-primate species was investigated. Video recordings of 33 chimpanzees were assessed while they consumed hard-shelled strychnos fruits. Statistical and descriptive measures of hand dominance to highlight lateralized patterns were explored. RESULTS: Statistical evaluation of feeding bouts revealed a group-level right-handed bias for bimanual coordinated feeding actions, however, few individuals were statistically lateralized. Descriptive analyses revealed that the majority of individuals were lateralized and possessed a right-handed bias for strychnos feeding behavior. CONCLUSIONS: The results provided empirical evidence in support of an early evolutionary delineation of function for the right and left hemispheres. The present findings suggest that great apes express an intermediate stage along the phylogenetic trajectory of human manual lateralization.


Assuntos
Comportamento Alimentar/fisiologia , Lateralidade Funcional/fisiologia , Pan troglodytes/fisiologia , Animais , Antropologia Física , Feminino , Frutas , Loganiaceae , Masculino
13.
Artigo em Inglês | MEDLINE | ID: mdl-26625339

RESUMO

A rapid, specific and sensitive liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed and validated for the simultaneous determination of strychnine, brucine, strychnine N-oxide and brucine N-oxide in rat plasma. Plasma samples were pretreated via simple protein precipitation with methanol and ephedrine hydrochloride was used as internal standard. Chromatographic separation was carried out on an ZORBAX Eclipse XDB-C18 column (2.1×150mm, 3.5µm) by gradient elution with methanol and 10mM ammonium acetate (adjusted to pH 4.0 with formic acid). The quantification of the analytes was performed by mass spectrometry with TurboIonSpray ionization (ESI) inlet in the positive ion multiple reaction monitoring (MRM) mode. The results showed that the calibration curve was linear in the concentration range of 0.510∼306.3ngmL(-1) for strychnine, brucine and 0.102∼306.0ngmL(-1) for strychnine N-oxide and brucine N-oxide, respectively. The intra- and inter-day precisions were less than 14.9%, and the accuracy ranged from 89.4 to 113% at three QC levels for the 4 analytes. The validated method was successfully applied to the pharmacokinetic study of strychnine, brucine, strychnine N-oxide and brucine N-oxide in rat plasma after oral administration of each monomer and the total alkaloids from Semen Strychni. After single oral administration of the total alkaloids from Semen Strychni at 4 dose levels, Cmax, AUC0-t of strychnine and brucine increased and were proportional to the oral doses. In comparative pharmacokinetics studies, no significant difference was found between each monomer and the total strychnos alkaloids on the pharmacokinetic parameters such as Cmax and AUC. Mean Cmax and AUC of strychnine and brucine were slight increased in the monomer groups in comparison to the total strychnos alkaloids groups, which suggested that some other alkaloids in the Semen Strychni may decrease the absorption of strychnine and brucine in body.


Assuntos
Cromatografia Líquida/métodos , Loganiaceae/química , Estricnina/análogos & derivados , Estricnina/farmacocinética , Espectrometria de Massas em Tandem/métodos , Animais , Ratos , Estricnina/administração & dosagem , Estricnina/sangue
14.
J Ethnopharmacol ; 175: 301-14, 2015 Dec 04.
Artigo em Inglês | MEDLINE | ID: mdl-26386382

RESUMO

ETHNOPHARMACOLOGY RELEVANCE: The angiogenesis control at the initiation of rheumatoid arthritis (RA) that mainly blocks the inflammatory cascades expects to attenuate the action of angiogenic mediators, synovial angiogenesis, and to partially reverse the erosive bone damage. Two typical Chinese herbs, Semen Strychni and Tripterygium wilfordii Hook F (TwHF) have been used as a remedy to treat RA since ancient time. However, their functioning mechanisms are still unknown. Thus it is necessary to exploit their underlying mechanism for the treatment of RA. METHODS: This study was undertaken to analyze their underlying mechanism based on a systems biology platform. Firstly, active components of the two herbs were screened out from TcmSP database based on their OB and DL values. Then their potential targets were predicted by using Random Forest, Support Vector Machine, and validated via docking process. Finally, a network of compound-target was constructed. RESULTS: In this work, 27 and 33 active compounds were screened out from Semen Strychni and TwHF, targeting 28 and 32 potential proteins, respectively. The results show that the two herbs modulate the angiogenesis mediators through both direct and indirect pathways, and 21 common targets shared by Semen Strychni and TwHF bear major responsibility for treating RA. CONCLUSIONS: The underlying mechanism of Semen Strychni and TwHF in treatment of RA is through multiple targets interaction by their blocking of the angiogenesis mediator cascades. This may provide us a better understanding of the function of the two herbs for the treatment of RA, as well as a clue to unveil their possible treatment effects of other systemic diseases, and in this way, hopefully the screening models may facilitate the discovery of novel combined drugs.


Assuntos
Inibidores da Angiogênese/farmacologia , Artrite Reumatoide/tratamento farmacológico , Loganiaceae , Extratos Vegetais/farmacologia , Tripterygium , Administração Oral , Inibidores da Angiogênese/farmacocinética , Inibidores da Angiogênese/uso terapêutico , Disponibilidade Biológica , Descoberta de Drogas/métodos , Farmacologia/métodos , Fitoterapia , Extratos Vegetais/farmacocinética , Extratos Vegetais/uso terapêutico , Raízes de Plantas , Sementes , Biologia de Sistemas
15.
BMC Complement Altern Med ; 14: 456, 2014 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-25428165

RESUMO

BACKGROUND: Strychnos spinosa Lam. is a deciduous tree used in traditional medicine to treat infectious diseases. This study is designed to determine the antimicrobial, antioxidant and cytotoxic activities of extracts and fractions from leaves of S. spinosa. METHODS: Extracts were obtained by maceration with acetone, methanol and dichloromethane/methanol (1/1) while fractions were prepared by liquid-liquid fractionation of the acetone extract. A broth serial microdilution method with tetrazolium violet as growth indicator was used to determine the minimum inhibitory concentration (MIC) against fungi, Gram-positive and Gram-negative bacteria. The antioxidant activity was determined using free-radical-scavenging assays, and the 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide reduction assay was used to determine cytotoxicity. RESULTS: Four extracts and five fractions had good to weak antimicrobial activity with MICs ranging from 0.04 to >1.25 mg/ml against both fungi and bacteria. The chloroform and ethyl acetate fractions had an MIC of 0.08 mg/ml against Aspergillus fumigatus. The n-butanol fraction had an MIC of 0.04 mg/ml against Cryptococcus neoformans. The hexane and chloroform fractions had an MIC of 0.08 mg/ml against Staphylococcus aureus. The antioxidant activities were much lower than that of the positive controls. Except for the alkaloid extract, all the extracts and fractions had free-radical-scavenging activity (IC50 ranging from 33.66 to 314.30 µg/ml). The cytotoxicity on Vero cells was reasonable to low with LC50 values ranging between 30.56 and 689.39 µg/ml. CONCLUSION: The acetone extract and the chloroform fraction had the highest antibacterial activity. By solvent-solvent fractionation it was possible to increase the activity against A. fumigatus and to decrease the cytotoxicity leading to a potentially useful product to protect animals against aspergillosis. Our results therefore support the use of S. spinosa leaves in traditional medicine to treat infectious diseases.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Aspergillus fumigatus/efeitos dos fármacos , Cryptococcus neoformans/efeitos dos fármacos , Extratos Vegetais/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Strychnos , Animais , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Chlorocebus aethiops , Bactérias Gram-Negativas/efeitos dos fármacos , Loganiaceae , Medicina Tradicional , Testes de Sensibilidade Microbiana , Extratos Vegetais/efeitos adversos , Folhas de Planta , Células Vero
16.
Mol Phylogenet Evol ; 78: 324-33, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24929247

RESUMO

The angiosperm genus Logania R.Br. (Loganiaceae) is endemic to the mainland of Australia. A recent genetic study challenged the monophyly of Logania, suggesting that its two sections, Logania sect. Logania and Logania sect. Stomandra, do not group together. Additionally, the genus has a disjunct distribution, with a gap at the Nullarbor Plain in southern Australia. Therefore, Logania is a favourable candidate to gain insight into phylogenetic relationships and how these might intersect with Earth-history events. Our phylogenetic analyses of DNA sequences of two chloroplast markers (petD and rps16) showed that Logania sect. Logania and L. sect. Stomandra were each resolved as monophyletic, but the genus (as currently circumscribed) was not. Based on our Bayesian estimates of divergence times, the disjunct distributions within Logania sect. Stomandra could have been caused by flooding of the Eucla Basin. However, this biogeographical process cannot account for the distribution of Logania sect. Logania, with long-distance dispersal and establishment seeming more likely.


Assuntos
Loganiaceae/classificação , Filogenia , Austrália , Teorema de Bayes , Loganiaceae/genética , Filogeografia , Análise de Sequência de DNA
17.
Bioorg Med Chem Lett ; 23(20): 5563-5, 2013 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-24012119

RESUMO

Gardovatine (1), the first Strychnos-Strychnos alkaloid with a C3/C7 cleaved backbone, was isolated from twigs and leaves of Gardneria ovate, together with an analogue divarine (2). The structure was established by extensive spectroscopic methods. Both compounds showed potential cytotoxicities against five human cancer cell lines.


Assuntos
Alcaloides/química , Alcaloides Indólicos/química , Indóis/química , Loganiaceae/química , Strychnos/química , Alcaloides/isolamento & purificação , Alcaloides/toxicidade , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Alcaloides Indólicos/isolamento & purificação , Alcaloides Indólicos/toxicidade , Loganiaceae/metabolismo , Espectroscopia de Ressonância Magnética , Conformação Molecular , Folhas de Planta/química , Folhas de Planta/metabolismo , Strychnos/metabolismo
18.
Pharm Biol ; 51(11): 1378-83, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-23829422

RESUMO

CONTEXT: Semen Strychni is the seed of Strychnos nux-vomica L. (Loganiaceae). Its quality control procedure remains an issue since previous reports only focused on Strychnos alkaloids. To the best of our knowledge, chlorogenic acid (a phenolic acid) and loganin (an iridoid glycoside) are selected for the first time as marker constituents of quality control for Semen Strychni because of their bioactive activity correlating with therapeutic effects. OBJECTIVE: This study aimed to develop a simple and comprehensive quantity control method for Semen Strychni. MATERIALS AND METHODS: The optimal ultrasonic extraction procedure was carried out for 45 min using 50% aqueous methanol with 1% formic acid. The satisfactory chromatographic separation was achieved on an Ultimate LP-C18 column with gradient elution using acetonitrile and water containing 30 mmol/L ammonium acetate and 1% formic acid. The high performance liquid chromatography method with diode array detector was validated for linearity, limit of detection and quantification (LOQ), precision, repeatability, accuracy and stability. RESULTS: All the calibration curves showed good linearity (r(2) ≥ 0.999). The LOQ values for chlorogenic acid, loganin, strychnine, brucine, strychnine N-oxide and brucine N-oxide were 0.54, 0.83, 0.48, 0.50, 0.52 and 0.54 µg/mL, respectively. The method was reproducible with good accuracy in the range 95.6-104.4% and relative standard deviation (RSD) values less than 4.55%. The method was then applied to determine the components of the seed coat, seed leaf, endosperm and whole seed of Semen Strychni. CONCLUSION: This newly established method is validated as a simple and practical tool for authentication and quality control of Semen Strychni.


Assuntos
Ácido Clorogênico/análise , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas/análise , Iridoides/análise , Loganiaceae , Espectrofotometria Ultravioleta , Soluções Tampão , Calibragem , Ácido Clorogênico/normas , Cromatografia Líquida de Alta Pressão/normas , Medicamentos de Ervas Chinesas/normas , Iridoides/normas , Limite de Detecção , Modelos Lineares , Loganiaceae/química , Fitoterapia , Plantas Medicinais , Controle de Qualidade , Padrões de Referência , Reprodutibilidade dos Testes , Sementes , Solventes/química , Espectrofotometria Ultravioleta/normas
19.
Molecules ; 18(4): 3962-71, 2013 Apr 04.
Artigo em Inglês | MEDLINE | ID: mdl-23558539

RESUMO

Three new spermidine alkaloids and two known compounds were isolated from the leaves of Androya decaryi. Their structures were elucidated on the basis of their spectroscopic data (NMR and mass spectrometry), by X-Ray diffraction and by comparison with literature values. Evaluation of the in vitro antiplamosdial properties of the isolated compounds revealed they did not possess any significant activity.


Assuntos
Alcaloides/química , Loganiaceae/química , Extratos Vegetais/química , Espermidina/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Folhas de Planta/química , Difração de Raios X
20.
J Ethnopharmacol ; 146(3): 811-4, 2013 Apr 19.
Artigo em Inglês | MEDLINE | ID: mdl-23422334

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Anthocleista djalonensis (A. Chev) and Anthocleista vogelii Planch are plants being used in West Africa traditionally to treat various diseases such as malaria, hernia, hypertension, stomach aches, hemorrhoids, syphilis, and diabetes. Diabetes causes about 5% of all deaths globally each year. Chemotherapeutic agents such as biguanides, sulfonylureas, and thiozolidinediones are available for the treatment of diabetes, however, they have undesirable side effects. The need for newer, more effective and less toxic drugs is imperative and the biodiversity of Nigeria has a high potential for drug discovery based on plants used in the ethnomedicine. AIM OF THE STUDY: To investigate the leaves, stem bark and roots of these plants for their probable alpha-amylase inhibitory activities and establish their anti-diabetic activities. The overall goal is do bioassay-guided fractionation and isolation of active anti-diabetic compounds. MATERIALS AND METHODS: Powdered samples (leaves, stem bark and roots) macerated with 80% aqueous methanol were evaluated in vitro using alpha-amylase inhibitory assay while in vivo investigations were carried out on hyperglycemic rats. Diabetes was induced in albino rats by an intraperitoneal injection of alloxan monohydrate (80mg/kg). Plant extracts (1g/kg) were given orally for 7 days, while blood glucose levels were monitored using a one touch glucometer. The crude methanol extracts found to be most active were further partitioned into hexane and ethyl acetate fractions which were also tested in vivo on the diabetic animals. RESULTS: The leaves and stem bark crude methanol extracts of Anthocleista djalonensis gave comparable α-amylase inhibition of 73.66% and 72.90%, respectively which were quite higher than the 38.93% and 22.90% of the same plant parts given by Anthocleista vogelii. The crude stem bark extract of Anthocleista djalonensis exhibited significant peak blood glucose reduction on day 6 (72.59%, p<0.05) which was higher than the leaves or roots which gave 45.73% and 47.46% (p<0.05), respectively The stem bark ethyl acetate fraction of Anthocleista djalonensis gave reduction in blood glucose level of 60.86% (p<0.05). CONCLUSION: From our results, the leaves, stem bark and whole root of both plants exhibited α-amylase inhibitory activities with Anthocleista djalonensis also showing good anti-diabetic activities in vivo indicating that they contain active principles for the management of diabetes. There is justification for the use of the plants traditionally to manage diabetes.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Loganiaceae/química , Extratos Vegetais/uso terapêutico , alfa-Amilases/antagonistas & inibidores , Aloxano/farmacologia , Animais , Glicemia/análise , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/enzimologia , Feminino , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Loganiaceae/crescimento & desenvolvimento , Masculino , Medicina Tradicional Africana , Nigéria , Casca de Planta/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Folhas de Planta/química , Raízes de Plantas/química , Ratos , Ratos Wistar
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