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1.
Phytochemistry ; 174: 112336, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32192964

RESUMO

Targeting the transmissible stages of the Plasmodium parasite that develop in the human and mosquito host is a crucial strategy for malaria control and elimination. Medicinal plants offer a prolific source for the discovery of new antimalarial compounds. The recent identification of the gametocytocidal activity of lophirone E, obtained from the African plant Lophira lanceolata (Ochnaceae), inspired the evaluation of the plant also against early sporogonic stages of the parasite development. The bioassay-guided phytochemical study led to the isolation of two known lanceolins and of a new glycosylated bichalcone, named glucolophirone C. Its stereostructure, including absolute configuration of the bichalcone moiety, was elucidated by means of NMR, HRMS, ECD and computational calculations. Lanceolin B proved to be a potent inhibitor of the development of Plasmodium early sporogonic stages indicating that the plant produces two different stage-specific antimalarial agents acting on transmissible stages in the human and mosquito host.


Assuntos
Antimaláricos , Malária , Ochnaceae , Animais , Humanos , Casca de Planta , Extratos Vegetais , Plasmodium falciparum
2.
Nat Prod Res ; 33(10): 1500-1503, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-29338358

RESUMO

The study aimed to evaluate in vitro antioxidant, anticholinesterase and antidiabetic properties of Ouratea hexasperma (A. St.-Hil.) Baill. The inflorescence methanol extract and the ethyl acetate fraction of leaves and stems reported the highest Relative Antioxidant Capacity Index (RACI), whereas the dichloromethane fraction of leaves was the best inhibitor of α-amylase and α-glucosidase. Trans-3-O-methyl-resveratrol-2-C-ß-glucoside, lithospermoside, 2,5-dimethoxy-p-benzoquinone, lup-20(30)-ene-3ß,28-diol, 7-O-methylgenistein, apigenin and luteolin and amentoflavone were isolated from O. hexasperma. Resveratrol derivative was isolated for the first time in Ochnaceae family. Luteolin, followed by apigenin, reported the highest Relative Antioxidant Capacity Index and they were also the best inhibitors of α-glucosidase enzyme.


Assuntos
Antioxidantes/farmacologia , Inibidores da Colinesterase/farmacologia , Hipoglicemiantes/farmacologia , Ochnaceae/química , Antioxidantes/química , Apigenina/isolamento & purificação , Apigenina/farmacologia , Inibidores da Colinesterase/química , Avaliação Pré-Clínica de Medicamentos/métodos , Inibidores de Glicosídeo Hidrolases/farmacologia , Hipoglicemiantes/química , Luteolina/isolamento & purificação , Luteolina/farmacologia , Metanol/química , Extratos Vegetais/química , Folhas de Planta/química , alfa-Amilases/antagonistas & inibidores
3.
Biomed Pharmacother ; 107: 1030-1036, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30257314

RESUMO

The aim of this study was to evaluate the antinociceptive effect of Kaempferol-3-O-rutinoside (KR), isolated from the plant Ouratea fieldingiana, on the orofacial nociception and possible mechanisms of action. Adult zebrafish (Danio rerio) were tested as a behavioral model to study formalin, glutamate, capsaicin, cinnamaldehyde and acidic saline-induced orofacial nociception, using as parameter the number of times the fish crossed the lines between the quadrants of a glass Petri dish during a specific time. Morphine was used as positive control. The effect of KR was tested for modulation by opioid (naloxone), nitrergic (L-NAME), TRPV1 (ruthenium red), TRPA1 (camphor) or ASIC (amiloride) antagonists. The effect of KR on zebrafish locomotor behavior was evaluated with the open field test. KR did not alter the fish's locomotor system and significantly reduced the orofacial nociceptive behavior induced by all noxious agents compared to the control group. The antinociceptive effect of KR was similar to morphine. All antagonists inhibited the antinociceptive effect of KR. KR has pharmacological potential for the treatment of acute orofacial pain and this effect is modulated by the opioid and nitrergic systems as well as TRPV1, TRPA1 and ASIC channels. These results can lead to the development of a new natural product for the treatment of orofacial pain and confirm the popular use of O. fieldingiana leaf for pain relief.


Assuntos
Analgésicos/farmacologia , Dor Facial/tratamento farmacológico , Quempferóis/farmacologia , Ochnaceae/química , Analgésicos/isolamento & purificação , Analgésicos Opioides/farmacologia , Animais , Comportamento Animal/efeitos dos fármacos , Modelos Animais de Doenças , Feminino , Quempferóis/isolamento & purificação , Masculino , Morfina/farmacologia , Naloxona/farmacologia , Nociceptividade/efeitos dos fármacos , Folhas de Planta , Peixe-Zebra
4.
Pharm Biol ; 56(1): 318-324, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29969355

RESUMO

CONTEXT: The roots of Lophira lanceolata Van Tiegh. Ex Keay (Ochnaceae) have numerous medicinal values in the Central African region. Even though the MeOH extract of the roots has shown antimycobacterial activities, the constituents responsible for this inhibitory activity remain unknown. OBJECTIVE: Phytochemical investigation of the MeOH root extract of L. lanceolata and determination of the antimycobacterial activities of that extract and constituents against the growth of Mycobacterium tuberculosis. MATERIALS AND METHODS: Column chromatography was used to provide bioactive phytoconstituents. Those compounds were elucidated using MS and NMR spectroscopic data. Antimycobacterial screening of the extract (4.882-5000 µg/mL in DMSO during 24 h at 37 °C) and isolated compounds (0.244-250 µg/mL in DMSO during 24 h at 37 °C) was performed by microplate alamar blue assay (MABA) against two mycobacterial strains. RESULTS: The investigation of L. lanceolata MeOH roots extract provided of mixture of unseparated biflavonoids with a newly described one, dihydrolophirone A (1a) associated to lophirone A (1b). The bioactive compounds that effectively inhibited the growth of M. tuberculosis AC45 were found to be compounds 1 and 2. They exhibited MIC values of 31.25 and 15.75 µg/mL, respectively, and their MIC was found to be 62.5 µg/mL against resistant strain AC83. DISCUSSION AND CONCLUSIONS: It is clearly evident from the results obtained that the mycobacterial activity of L. lanceolata could be related mainly to its steroid and flavonoid contents. Therefore, this study suggests the potential of the above-mentioned classes of compounds as promising candidate agents for developing new anti-tuberculosis drugs.


Assuntos
Antituberculosos/farmacologia , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Mycobacterium tuberculosis/efeitos dos fármacos , Ochnaceae , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Antituberculosos/isolamento & purificação , Avaliação Pré-Clínica de Medicamentos/métodos , Farmacorresistência Bacteriana Múltipla/fisiologia , Humanos , Testes de Sensibilidade Microbiana/métodos , Mycobacterium tuberculosis/fisiologia , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/isolamento & purificação
5.
Plant Biol (Stuttg) ; 20(5): 848-856, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29673051

RESUMO

The ability of leaves to absorb fog water can positively contribute to the water and carbon balance of plants in montane ecosystems, especially in periods of soil water deficit. However, the ecophysiological traits and mechanisms responsible for variations in the speed and total water absorption capacity of leaves are still poorly known. This study investigated leaf anatomical attributes of seven species occurring in seasonal tropical high-altitude ecosystems (rocky outcrop and forest), which could explain differences in leaf water uptake (LWU) capacities. We tested the hypothesis that different sets of anatomical leaf attributes will be more marked in plant individuals living under these contrasting environmental conditions. Anatomical variations will affect the initial rate of water absorption and the total storage capacity, resulting in different strategies for using the water supplied by fog events. Water absorption by leaves was inferred indirectly, based on leaf anatomical structure and visual observation of the main access routes (using an apoplastic marker), the diffusion of water through the cuticle, and non-glandular or glandular trichomes in all species. The results suggest that three LWU strategies coexist in the species studied. The different anatomical patterns influenced the speed and maximum LWU capacity. The three LWU strategies can provide different adaptive advantages to adjust to temporal and spatial variations of water availability in these tropical high-altitude environments.


Assuntos
Folhas de Planta/anatomia & histologia , Água/metabolismo , Altitude , Asteraceae/anatomia & histologia , Asteraceae/metabolismo , Ecossistema , Fabaceae/anatomia & histologia , Fabaceae/metabolismo , Fluorescência , Malpighiaceae/anatomia & histologia , Malpighiaceae/metabolismo , Melastomataceae/anatomia & histologia , Melastomataceae/metabolismo , Myrtaceae/anatomia & histologia , Myrtaceae/metabolismo , Ochnaceae/anatomia & histologia , Ochnaceae/metabolismo , Folhas de Planta/metabolismo
6.
Mol Phylogenet Evol ; 125: 196-203, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-29625230

RESUMO

Cyclical periods of global cooling have been important drivers of biotic differentiation throughout the Quaternary. Ice age-induced sea level fluctuations can lead to changing patterns of land connections, both facilitating and disrupting gene flow. In this study, we test if species with differing life histories are differentially affected by Quaternary land connections. We used genome-wide SNPs in combination with mitochondrial gene sequences to analyse levels of divergence and gene flow between two songbird complexes across two Wallacean islands that have been repeatedly connected during glaciations. Although the two bird complexes are similar in ecological attributes, the forest and edge-inhabiting golden whistler Pachycephala pectoralis is comparatively flexible in its diet and niche requirements as compared to the henna-tailed jungle-flycatcher Cyornis colonus, which is largely restricted to the forest interior. Using population-genomic and coalescent approaches, we estimated levels of gene flow, population differentiation and divergence time between the two island populations. We observed higher levels of differentiation, an approximately two to four times deeper divergence time and near-zero levels of gene flow between the two island populations of the more forest-dependent henna-tailed jungle-flycatcher as compared to the more generalist golden whistler. Our results suggest that Quaternary land bridges act as semipermeable agents of gene flow in Wallacea, allowing only certain taxa to connect between islands while others remain isolated. Quaternary land bridges do not accommodate all terrestrial species equally, differing in suitability according to life history and species biology. More generalist species are likely to use Quaternary land connections as a conduit for gene flow between islands whereas island populations of more specialist species may continue to be reproductively isolated even during periods of Quaternary land bridges.


Assuntos
Aves/genética , Fluxo Gênico , Animais , Sequência de Bases , DNA Mitocondrial/genética , Genoma , Geografia , Ilhas , Ochnaceae/genética , Filogenia , Polimorfismo de Nucleotídeo Único/genética , Análise de Componente Principal , Aves Canoras/genética , Fatores de Tempo
7.
Drug Res (Stuttg) ; 68(4): 232-237, 2018 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-29190855

RESUMO

Enhanced antimalarial activity of plant extracts used for treatment of malaria in endemic areas is attributed to partial immunity gained by prior infection. This suggests synergy between immunity and extract activity in treatment. Testing this hypothesis, rodent malaria was used to determine efficacy of Lophira alata leaf extracts in treating malaria in prior infected mice. One round of P. berghei infection and Pyrimethamine drug-cure was used to establish partial immunity in mice. Previously Exposed Mice (PEM) and Previously Unexposed Mice (PUM) mice challenged with P. berghei were used to determine influence of partial antimalarial immunity on efficacy of L. alata leaf extracts, administered alone or in combination with Artesunate (ART) in malaria treatment. There was a significant reduction in parasitemia in PEM when compared to PUM animals (P<0.001) irrespective of treatment regimen. Administration of L. alata combined with ART significantly reduced parasitemia (P<0.0032) and prolonged (P=0.0109) survival than when L. alata was administered alone in infected mice. These findings suggest that the action of L. alata in treating malaria infections in a murine model is enhanced by prior exposure to the malaria parasite. Thus the requirements of using plants in treating malaria in endemic populations may differ for those used in western systems, where trials are carried out with non-immune cohorts. Combining artemisinin derivatives and medicinal plants in malaria exposed populations may provide an alternative control measure in endemic regions and may justify the continued use of these plants by indigenous populations in treating malaria.


Assuntos
Artemisininas/farmacologia , Malária/tratamento farmacológico , Ochnaceae/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Plasmodium berghei/efeitos dos fármacos , Animais , Antimaláricos/química , Antimaláricos/farmacologia , Artesunato , Camundongos , Fitoterapia/métodos , Plantas Medicinais/química
8.
Biomed Res Int ; 2017: 5140506, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29204442

RESUMO

Cooccurrence of Diabetes Mellitus and Alzheimer's disease in elder people prompts scientists to develop multitarget agents that combat causes and symptoms of both diseases simultaneously. In line with this modern paradigm and as a follow-up to our previous studies, the present study is designed to investigate the crude methanolic extracts and subsequent CHCl3, n-BuOH, and H2O fractions of Acalypha alnifolia, Pavetta indica, and Ochna obtusata for their inhibitory activities towards specific targets involved in AD and DM, namely, acetylcholinesterase, butyrylcholinesterase, and α-glucosidase (α-Glc). The methanolic extract and its derived chloroform fractions exhibited remarkable inhibitory capacities with IC50 values being found at the µg/mL level. Further studies on most active chloroform fractions presented a prominent ability to scavenge DPPH and ABTS reactive species and highest neuroprotective effect against H2O2 induced cell injury. Phytochemical analysis showed a large amount of phenolics, flavonoids, and terpenoids in active fractions. In conclusion, A. alnifolia, P. indica, and O. obtusata could be promising sources for the treatment of AD and DM since these fractions induced significant anticholinesterase, antidiabetic, antioxidant, and neuroprotection effects attributable to phenolic, flavonoid, and terpenoid contents and encourage further studies for development of multifunctional therapeutic agent for AD and DM dual therapy.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Antioxidantes/administração & dosagem , Diabetes Mellitus/tratamento farmacológico , Compostos Fitoquímicos/administração & dosagem , Plantas Medicinais/química , Acalypha/química , Doença de Alzheimer/patologia , Antioxidantes/química , Linhagem Celular Tumoral , Inibidores da Colinesterase/administração & dosagem , Inibidores da Colinesterase/química , Diabetes Mellitus/patologia , Glucosidases/antagonistas & inibidores , Humanos , Peróxido de Hidrogênio/toxicidade , Hipoglicemiantes/administração & dosagem , Hipoglicemiantes/química , Fármacos Neuroprotetores/administração & dosagem , Fármacos Neuroprotetores/química , Ochnaceae/química , Compostos Fitoquímicos/química , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química
9.
BMC Complement Altern Med ; 17(1): 404, 2017 Aug 14.
Artigo em Inglês | MEDLINE | ID: mdl-28806951

RESUMO

BACKGROUND: Onchocerciasis is one of the tropical neglected diseases (NTDs) caused by the nematode Onchocerca volvulus. Control strategies currently in use rely on mass administration of ivermectin, which has marked activity against microfilariae. Furthermore, the development of resistance to ivermectin was observed. Since vaccine and safe macrofilaricidal treatment against onchocerciasis are still lacking, there is an urgent need to discover novel drugs. This study was undertaken to investigate the anthelmintic activity of Lophira lanceolata on the cattle parasite Onchocerca ochengi and the anthelmintic drug resistant strains of the free living nematode Caenorhabditis elegans and to determine the phytochemical profiles of the extracts and fractions of the plants. METHODS: Plant was extracted in ethanol or methanol-methylene chloride. O. ochengi, C. elegans wild-type and C. elegans drug resistant strains were cultured in RPMI-1640 and NGM-agar respectively. Drugs diluted in dimethylsulphoxide/RPMI or M9-Buffer were added in assays and monitored at 48 h and 72 h. Worm viability was determined by using the MTT/formazan colorimetric method. Polyphenol, tannin and flavonoid contents were determined by dosage of gallic acid and rutin. Acute oral toxicity was evaluated using Swiss albino mice. RESULTS: Ethanolic and methanolic-methylene chloride extracts killed O. ochengi with LC50 values of 9.76, 8.05, 6.39 µg/mL and 9.45, 7.95, 6.39 µg/mL respectively for leaves, trunk bark and root bark after 72 h. The lowest concentrations required to kill 50% of the wild-type of C. elegans were 1200 and 1890 µg/mL with ethanolic crude extract, 1000 and 2030 µg/mL with MeOH-CH2Cl2 for root bark and trunk bark of L. lanceolata, respectively after 72 h. Leave extracts of L. lanceolata are lethal to albendazole and ivermectin resistant strains of C. elegans after 72 h. Methanol/methylene chloride extracted more metabolites. Additionally, extracts could be considered relatively safe. CONCLUSION: Ethanolic and methanolic-methylene chloride crude extracts and fractions of L. lanceolata showed in vitro anthelmintic activity. The extracts and fractions contained polyphenols, tannins, flavonoids and saponins. The mechanism of action of this plant could be different from that of albendazole and ivermectin. These results confirm the use of L. lanceolata by traditional healers for the treatment of worm infections.


Assuntos
Anti-Helmínticos/farmacologia , Caenorhabditis elegans , Infecções por Nematoides/parasitologia , Ochnaceae/química , Onchocerca , Extratos Vegetais/farmacologia , Albendazol/farmacologia , Animais , Bovinos , Resistência a Medicamentos , Flavonoides/análise , Flavonoides/farmacologia , Ivermectina/farmacologia , Camundongos , Infecções por Nematoides/veterinária , Oncocercose/parasitologia , Oncocercose/veterinária , Fitoterapia , Casca de Planta , Extratos Vegetais/química , Raízes de Plantas , Caules de Planta , Polifenóis/análise , Polifenóis/farmacologia , Saponinas/análise , Saponinas/farmacologia , Taninos/análise , Taninos/farmacologia
10.
Chem Biodivers ; 14(11)2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28695668

RESUMO

The study of the MeOH extract of the leaves of Campylospermum excavatum led to the isolation of a nitrile glucoside, named campyloside C (1) and an original derivative of ochnaflavone, 7-O-methylochnaflavone (2), along with three known biflavonoids, amentoflavone, sequoiaflavone, and sotetsuflavone (3 - 5). The linkage site of the sub-units of 2 was confirmed by chemical correlation, after semi-synthesis of a trimethoxylated derivative of ochnaflavone (2a). The structures of these compounds as well as their relative and absolute configurations were assigned by 1D- and 2D-NMR experiments, HR-ESI-MS and Electronic Circular Dichroism (ECD) calculations. A low-pass J filter HMBC experiment was performed in order to define the configuration of the double bond of 1. All of the biflavonoids were evaluated against protozoan parasites. Amentoflavone moderately inhibited the promastigote form of Leishmania infantum.


Assuntos
Biflavonoides/química , Glucosídeos/química , Nitrilos/química , Ochnaceae/química , Animais , Antiprotozoários/química , Antiprotozoários/isolamento & purificação , Antiprotozoários/farmacologia , Biflavonoides/isolamento & purificação , Biflavonoides/farmacologia , Linhagem Celular , Dicroísmo Circular , Flavonoides/síntese química , Flavonoides/química , Glucosídeos/isolamento & purificação , Leishmania/efeitos dos fármacos , Leishmania/fisiologia , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Macrófagos/parasitologia , Espectroscopia de Ressonância Magnética , Camundongos , Conformação Molecular , Ochnaceae/metabolismo , Folhas de Planta/química , Folhas de Planta/metabolismo , Espectrometria de Massas por Ionização por Electrospray
11.
Nat Prod Res ; 31(24): 2875-2884, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28385033

RESUMO

Phytochemical investigation of the stem bark of Campylospermum zenkeri led to the isolation of five known compounds: (Z,Z)-9,12-octadecadienoic acid (1), serotobenine (2), agathisflavone (3), lophirone A (4) and lophirone F (5), together with a new derivative of procyanidin B, a catechin dimer named zenkerinol (6). Serotobenine (2) is structurally related to decursivine which shows moderate activity against D6 and W2 strains of Plasmodium falciparum. For a better understanding of structure-activity relationships, three new semi-synthetic derivatives of serotobenine (2) have been prepared. These are: serotobenine monopropionate (2a), serotobenine monopivalate (2b) and serotobenine cyclohexyl ether (2c) respectively. Two of them (2a) and (2b), were evaluated for their antiplasmodial activity against P. falciparum 3D7 strain in a parasite lactate-dehydrogenase (pLDH) assay. Compound 2b was more active than compound 2a based on their IC50 values (36.6 and 123 µM, respectively).


Assuntos
Antimaláricos/química , Biflavonoides/química , Catequina/química , Indóis/química , Ochnaceae/química , Proantocianidinas/química , Antimaláricos/farmacologia , Biflavonoides/isolamento & purificação , Alcaloides Indólicos/farmacologia , Indóis/isolamento & purificação , Indóis/farmacocinética , Concentração Inibidora 50 , Casca de Planta/química , Extratos Vegetais/química , Plasmodium falciparum/efeitos dos fármacos , Relação Estrutura-Atividade
12.
Z Naturforsch C J Biosci ; 72(1-2): 71-75, 2017 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-27295334

RESUMO

The leaves of Campylospermum elongatum have furnished the cyano-glycoside (lithospermoside), nine isomeric biflavonoid derivatives among which five are I3-II6 linked (robustaflavone; 4'-O-methyl robustaflavone; 4',4″'-di-O-methyl robustaflavone; 7,4',4″-tri-O-methyl robustaflavone; 4',7″-di-O-methyl robustaflavone) and four I3-II8 linked (amentoflavone; 7-O-methyl amentoflavone; 7,7″-di-O-methyl amentoflavone; 7, 4',7″-tri-O-methyl amentoflavone) and a flavone glycoside, 4″-O-methyl-7-O-ß-d-galactosylapigenin. All structures were established from a complete spectroscopic analysis (MS, IR, 1D, and 2D NMR, including HSQC, HMBC, and NOESY) as well as by comparing the obtained spectroscopic data with literature. This is the first report on the characterization of 4'-O-methyl-7-O-ß-d-galactosylapigenin from the genus campylospermum and thus has important chemotaxonomic implications.


Assuntos
Flavonoides/isolamento & purificação , Ochnaceae/química , Etanol , Flavonas/química , Flavonas/isolamento & purificação , Flavonoides/química , Hidrólise , Metanol , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Folhas de Planta/química , Solventes , Espectrometria de Fluorescência , Espectrofotometria Infravermelho , Espectroscopia de Infravermelho com Transformada de Fourier
13.
Nat Prod Res ; 31(18): 2149-2152, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28032512

RESUMO

Anti-proliferative activity of the ethyl acetate fractions of Ochna schweinfurthiana F. Hoffm. and Ochna kibbiensis Hutch. and Dalziel methanol leaf extracts were investigated against glioblastoma multiforme (GBM U-1242 MG) cell line. O. kibbiensis significantly (p < 0.001) and dose dependently (IC50 = 25.74 µg/mL) reduced cell count. At 125 µg/mL, O. kibbiensis extract reduced cell count by about 92% compared to the untreated control. On the other hand, at 125 µg/mL, O. schweinfurthiana extract reduced cell count only by 20%, indicating a much weaker activity (IC50 = 823.51 µg/mL). Following from the result obtained, ethyl acetate fraction of O. kibbiensis was subjected to chromatographic purification. This led to the isolation of ochnaflavone; the structure of the isolated compound was identified by analysis of its nuclear magnetic resonance (NMR) spectral data and comparison with data in the literature. Although the isolated ochnaflavone could not be tested for anti-proliferative activity due to insufficient quantity, the obtained results indicate the presence of bioactive anti-GBM principles in O. kibbiensis.


Assuntos
Flavonoides/química , Flavonoides/farmacologia , Ochnaceae/química , Extratos Vegetais/farmacologia , Acetatos/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Flavonoides/isolamento & purificação , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Extratos Vegetais/química , Folhas de Planta/química
14.
Phytother Res ; 29(10): 1509-15, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26094613

RESUMO

Several plant species are used in Brazil to treat inflammatory diseases and associated conditions. TNF-α plays a pivotal role on inflammation, and several plant extracts have been assayed against this target, both in vitro and in vivo. The effect of 11 Brazilian medicinal plants on TNF-α release by LPS-activated THP-1 cells was evaluated. The plant materials were percolated with different solvents to afford 15 crude extracts, whose effect on TNF-α release was determined by ELISA. Among the evaluated extracts, only Jacaranda caroba (Bignoniaceae) presented strong toxicity to THP-1 cells. Considering the 14 non-toxic extracts, TNF-α release was significantly reduced by seven of them (inhibition > 80%), originating from six plants, namely Cuphea carthagenensis (Lythraceae), Echinodorus grandiflorus (Alismataceae), Mansoa hirsuta (Bignoniaceae), Ouratea semiserrata (Ochnaceae), Ouratea spectabilis and Remijia ferruginea (Rubiaceae). The ethanol extract from O. semiserrata leaves was fractionated over Sephadex LH-20 and RP-HPLC to give three compounds previously reported for the species, along with agathisflavone and epicatechin, here described for the first time in the plant. Epicatechin and lanceoloside A elicited significant inhibition of TNF-α release, indicating that they may account for the effect produced by O. semiserrata crude extract.


Assuntos
Extratos Vegetais , Plantas Medicinais , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Bignoniaceae , Brasil , Cromatografia Líquida de Alta Pressão , Dextranos , Ochnaceae , Extratos Vegetais/farmacologia , Folhas de Planta , Solventes
15.
J Basic Clin Physiol Pharmacol ; 26(6): 523-9, 2015 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-25781676

RESUMO

BACKGROUND: Stem bark and leaves of Lophira alata (Family: Ochnaceae) have been used traditionally for their anti-psychotic, anti-convulsant and anxiolytic properties. Since no existing data was found on the neurobehavioural properties, this study was carried out to evaluate some neurobehavioural properties of the aqueous extract of the stem bark of L. alata in animal models. METHODS: The oral mean lethal dose (LD50) of the extract was estimated, and preliminary phytochemical screening was conducted. Lophira alata extract (200, 400 and 800 mg/kg, p.o.) was investigated for antidepressant effect using the forced swim and tail suspension tests, and the anxiolytic potential was assessed using the stair case and hole board tests. Pentylenetetrazole-induced convulsion test was used to investigate the anticonvulsant potential of the extract. RESULTS: The LD50 was estimated to be >5000 mg/kg. Oral administration of L. alata extract produced a significant (p<0.05) non-dose-dependent decrease in the period of immobility in both the forced swim and tail suspension tests. While a significant decrease (p<0.05) in episodes of grooming was recorded in the staircase test, the number of head dips was not significantly reduced (p>0.05) in the hole board test. In the pentylenetetrazole-induced convulsion, a non-dose-dependent increase in onset of tonic-clonic seizures and protection from death was recorded. CONCLUSIONS: The results obtained suggest that the aqueous stem bark extract of L. alata possesses neurobehavioural properties which may account for its use in ethnomedicine.


Assuntos
Comportamento Animal/efeitos dos fármacos , Ochnaceae/química , Extratos Vegetais/farmacologia , Animais , Ansiolíticos/administração & dosagem , Ansiolíticos/isolamento & purificação , Ansiolíticos/farmacologia , Anticonvulsivantes/administração & dosagem , Anticonvulsivantes/isolamento & purificação , Anticonvulsivantes/farmacologia , Antidepressivos/administração & dosagem , Antidepressivos/isolamento & purificação , Antidepressivos/farmacologia , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Dose Letal Mediana , Masculino , Camundongos , Casca de Planta , Extratos Vegetais/administração & dosagem , Folhas de Planta , Caules de Planta , Convulsões/tratamento farmacológico
16.
Nat Prod Res ; 29(17): 1684-7, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25553908

RESUMO

Seven flavonoids, hemerocallone (1), 6,7-dimethoxy-3',4'-dimethoxyisoflavone (2), amentoflavone (4), agathisflavone (6), cupressuflavone (8), robustaflavone (9) and epicatechin (10), together with three other compounds, lithospermoside (3), ß-D-fructofuranosyl-α-D-glucopyranoside (5) and 3ß-O-D-glucopyranosyl-ß-stigmasterol (7), were isolated from the ethyl acetate extract of the stem bark of Ochna schweinfurthiana F. Hoffm. All the compounds were characterised by spectroscopic and mass spectrometric methods, and by comparison with literature data. Cytotoxicity of the extracts and compounds against cervical adenocarcinoma (HeLa) cells was evaluated by MTT assay. Compounds 4 and 6 exhibited good cytotoxic activity, with IC50 values of 20.7 and 10.0 µM, respectively.


Assuntos
Flavonoides/química , Ochnaceae/química , Casca de Planta/química , Extratos Vegetais/química , Biflavonoides/química , Células HeLa , Humanos , Concentração Inibidora 50 , Estrutura Molecular
17.
Genet Mol Res ; 13(4): 8258-67, 2014 Oct 20.
Artigo em Inglês | MEDLINE | ID: mdl-25366720

RESUMO

Sauvagesia rhodoleuca (Ochnaceae) is an endangered plant that is endemic to southern China. The levels of genetic variation and patterns of population structure in S. rhodoleuca were investigated using inter-simple sequence repeat markers. Eleven primers were used to amplify DNA samples from 117 individuals, and a total of 92 loci were detected. Our results indicated that genetic diversity was quite low both at the species level (percentage of polymorphic bands (PPB) = 41.30%, Nei's gene diversity (h) = 0.1331, and Shannon information index (I) = 0.2028) and the population level (PPB = 16.30-28.26%, h = 0.0496-0.1012, and I = 0.0756-0.1508). A high level of genetic differentiation among populations was detected based on Nei's genetic diversity analysis (0.4344) and analysis of molecular variance (47.03%). The low genetic diversity within population and high population differentiation of S. rhodoleuca were assumed to result largely from limited gene flow, genetic drift, inbreeding, and clonal growth. Conservation strategies for this endangered species are proposed based on the genetic data.


Assuntos
Variação Genética , Genética Populacional , Repetições de Microssatélites , Ochnaceae/genética , China , Espécies em Perigo de Extinção , Evolução Molecular , Geografia , Espécies Introduzidas
18.
J Complement Integr Med ; 11(4): 273-7, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25263311

RESUMO

BACKGROUND: This study investigated the acute toxicity effect of aqueous stem bark extract of Lophira lanceolata and the activities of liver enzymes and other markers of organ damage in rats pretreated with aqueous stem bark extract of L. lanceolata extract and subsequently intoxicated with paracetamol (PCM). METHODS: A total of 30 rats were used to determine the acute toxicity of aqueous extract of L. lanceolata stem. They were divided into six groups consisting of five rats each. The groups (A-F) were administered the increasing doses of the extract (500 mg/kg, 1,000 mg/kg, 2,000 mg/kg, 3,200 mg/kg, 4,000 mg/kg and 5,000 mg/kg) orally. The rats were observed over a period of 24 h for acute toxicity signs such as dullness, anorexia, morbidity and death. Thirty rats of mixed sexes randomly assigned to six groups (A-F) of five rats each were used for the study on the effects of L. lanceolata extract on the haematology, liver enzymes and markers of organ damage of extract-pretreated PCM-intoxicated rats. The rats in groups A-D were pretreated with 100 mg/kg, 200 mg/kg, 300 mg/kg of L. lanceolata extract and 100 mg/kg Silymarin, respectively, twice a day for 7 days. On the seventh day, all the rats in groups A-E received 1,000 mg/kg PCM (per os). Group E rats served as negative control while group F rats were neither intoxicated nor treated with the extract and served as positive control. Eighteen hours after PCM intoxication, blood samples were collected for biochemical analyses. The serum activities of these enzymes (aspartate aminotransferase [AST], alanine aminotransferase [ALT], alkaline phosphatase [ALP]) and other markers of organ damages (bilirubin and total protein) were investigated. Haematologic parameters such as packed cell volume, red blood cell count, white blood cell count and haemoglobin concentration were also determined. RESULTS: The extract did not cause any death in all the groups even at the highest dose (5,000 mg/kg body weight). The results also showed varying degrees in the activity of the enzymes in the serum in comparison with the negative control. The mean serum ALP, ALT and AST activity of group C (rats pretreated with 300 mg/kg of the extract and 1,000 mg/kg PCM) were significantly (p<0.05) lower than that of the group E (rats intoxicated with 1,000 mg/kg PCM only). The AST and ALP activities of groups C-E rats) were statistically comparable. The serum ALT activities of group C rats were significantly (p<0.05) lower than that of group E rats but were statistically comparable (p>0.05) with the group F counterpart. The bilirubin levels were significantly (p<0.05) lower in the groups pretreated with the extract and Silymarin in comparison with the D group. The total protein and the haematologic indices were not significantly different (p>0.05) across the groups. CONCLUSIONS: This study therefore showed that the aqueous stem bark extract of L. lanceolata possesses some active constituents that have antihepatotoxic potentials.


Assuntos
Acetaminofen/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Fígado/efeitos dos fármacos , Ochnaceae , Extratos Vegetais/uso terapêutico , Alanina Transaminase/sangue , Fosfatase Alcalina/sangue , Animais , Aspartato Aminotransferases/sangue , Bilirrubina/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/sangue , Feminino , Fígado/fisiopatologia , Masculino , Casca de Planta , Extratos Vegetais/toxicidade , Caules de Planta , Ratos , Ratos Wistar , Água
19.
J Agric Food Chem ; 62(24): 5595-602, 2014 Jun 18.
Artigo em Inglês | MEDLINE | ID: mdl-24830509

RESUMO

Crude extracts of 33 plant species were assessed for fungal plasma membrane (PM) H(+)-ATPase inhibition. This led to identification of 18 extracts showing more than 95% inhibition at a concentration of 7.5 mg/mL and/or a concentration-dependent activity profile. These extracts were selected for semi-high-resolution fungal PM H(+)-ATPase inhibition screening, and, on the basis of these results, Haplocoelum foliolosum (Hiern) Bullock and Sauvagesia erecta L. were selected for investigation by high-resolution fungal PM H(+)-ATPase inhibition screening. Structural analysis performed by high-performance liquid chromatography-high-resolution mass spectrometry-solid-phase extraction-nuclear magnetic resonance spectroscopy (HPLC-HRMS-SPE-NMR) led to identification of chebulagic acid (1) and tellimagrandin II (2) from H. foliolosum. Preparative-scale isolation of the two metabolites allowed determination of IC50 values for PM H(+)-ATPase, and growth inhibition of Saccharomyces cerevisiae and Candida albicans. Chebulagic acid and tellimagrandin II are both potent inhibitors of the PM H(+)-ATPase with inhibitory effect on the growth of S. cerevisiae.


Assuntos
Cromatografia Líquida de Alta Pressão , Inibidores Enzimáticos/análise , Espectroscopia de Ressonância Magnética , Extratos Vegetais/química , ATPases Translocadoras de Prótons/antagonistas & inibidores , Benzopiranos/análise , Benzopiranos/farmacologia , Candida albicans/efeitos dos fármacos , Candida albicans/crescimento & desenvolvimento , Inibidores Enzimáticos/farmacologia , Fungos/metabolismo , Ácido Gálico/análogos & derivados , Ácido Gálico/análise , Ácido Gálico/farmacologia , Glucosídeos/análise , Glucosídeos/farmacologia , Ochnaceae/química , ATPases Translocadoras de Prótons/metabolismo , Saccharomyces cerevisiae/efeitos dos fármacos , Saccharomyces cerevisiae/crescimento & desenvolvimento , Sapindaceae/química , Extração em Fase Sólida
20.
Mol Phylogenet Evol ; 78: 199-214, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24862223

RESUMO

Ochnaceae s.str. (Malpighiales) are a pantropical family of about 500 species and 27 genera of almost exclusively woody plants. Infrafamilial classification and relationships have been controversial partially due to the lack of a robust phylogenetic framework. Including all genera except Indosinia and Perissocarpa and DNA sequence data for five DNA regions (ITS, matK, ndhF, rbcL, trnL-F), we provide for the first time a nearly complete molecular phylogenetic analysis of Ochnaceae s.l. resolving most of the phylogenetic backbone of the family. Based on this, we present a new classification of Ochnaceae s.l., with Medusagynoideae and Quiinoideae included as subfamilies and the former subfamilies Ochnoideae and Sauvagesioideae recognized at the rank of tribe. Our data support a monophyletic Ochneae, but Sauvagesieae in the traditional circumscription is paraphyletic because Testulea emerges as sister to the rest of Ochnoideae, and the next clade shows Luxemburgia+Philacra as sister group to the remaining Ochnoideae. To avoid paraphyly, we classify Luxemburgieae and Testuleeae as new tribes. The African genus Lophira, which has switched between subfamilies (here tribes) in past classifications, emerges as sister to all other Ochneae. Thus, endosperm-free seeds and ovules with partly to completely united integuments (resulting in an apparently single integument) are characters that unite all members of that tribe. The relationships within its largest clade, Ochnineae (former Ochneae), are poorly resolved, but former Ochninae (Brackenridgea, Ochna) are polyphyletic. Within Sauvagesieae, the genus Sauvagesia in its broad circumscription is polyphyletic as Sauvagesia serrata is sister to a clade of Adenarake, Sauvagesia spp., and three other genera. Within Quiinoideae, in contrast to former phylogenetic hypotheses, Lacunaria and Touroulia form a clade that is sister to Quiina. Bayesian ancestral state reconstructions showed that zygomorphic flowers with adaptations to buzz-pollination (poricidal anthers), a syncarpous gynoecium (a near-apocarpous gynoecium evolved independently in Quiinoideae and Ochninae), numerous ovules, septicidal capsules, and winged seeds with endosperm are the ancestral condition in Ochnoideae. Although in some lineages poricidal anthers were lost secondarily, the evolution of poricidal superstructures secured the maintenance of buzz-pollination in some of these genera, indicating a strong selective pressure on keeping that specialized pollination system.


Assuntos
Ochnaceae/classificação , Filogenia , Teorema de Bayes , DNA de Plantas/química , Ochnaceae/genética , Análise de Sequência de DNA
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