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1.
Alkaloids Chem Biol ; 83: 187-223, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32098650

RESUMO

The tryptamine-derived polycyclic bridged bioactive indole alkaloids subincanadines A-G were isolated in 2002 by Ohsaki and coworkers from the bark of the Brazilian medicinal plant Aspidosperma subincanum. Kobayashi proposed that subincanadines D-F could be biosynthetically resulting from stemmadenine via two different pathways and, furthermore, that the subincanadines A-C could be biogenetically resulting from subincanadines D and E. Kam and coworkers, in their focused efforts, isolated five indole alkaloids from Malaysian Kopsia arborea species, namely valparicine, apparicine, arboridinine, arborisidine, and arbornamine in combination with subincanadine E. On the basis of structural features, it has been proposed and proved in some examples that subincanadine E is a biogenetic precursor of these five different bioactive indole alkaloids bearing complex structural architectures. All important information on isolation, characterization, bioactivity, probable biogenetic pathways, and more specifically racemic and enantioselective total synthesis of subincanadine alkaloids and their biogenetic congeners are summarized in the present chapter. Special importance is given to the total synthesis and the synthetic strategies intended therein, comprising a set of main reactions.


Assuntos
Apocynaceae/química , Alcaloides Indólicos/química , Plantas Medicinais/química , Alcaloides Indólicos/isolamento & purificação , Alcaloides Indólicos/metabolismo , Estrutura Molecular
2.
Food Chem ; 315: 126277, 2020 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-32004983

RESUMO

This study reports the effects of seasonal variation on the total polyphenol and flavonoid content and the in vitro antioxidant activity of Secondatia floribunda A. DC. The extracts were prepared from the inner bark and heartwood of samples harvested in the 2015 to 2016. The total phenolic and flavonoid content was determined by specific qualitative tests. The in vitro antioxidant capacity was analyzed using the following tests: 1-1-diphenyl-2-picrylhydrazyl radical (DPPH), 2,2'-azinobis-3-ethylbenzenothiazoline-6-sulfonic acid (ABTS+), ferric reducing antioxidant power (FRAP) and iron (Fe2+) chelating activity. The total polyphenol and total flavonoid content varied over the harvest period. The DPPH and ABTS tests revealed that in the dry season had the most potent in vitro antioxidant activity, although the extracts obtained during the rainy season presented the higher Fe2+ chelating and Ferric reducing activities. In conclusion, the phenolic content and in vitro antioxidant activity are correlated, and both are influenced by seasonality.


Assuntos
Antioxidantes/análise , Apocynaceae/química , Polifenóis/análise , Flavonoides/química , Extratos Vegetais/química , Estações do Ano
3.
Chem Biol Interact ; 316: 108924, 2020 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-31843629

RESUMO

Parameritannin A-2 (PA-2) is a natural product extracted from the stems of the plant Urceola huaitingii. Our previous studies have shown that PA-2 exhibits significant synergistic anticancer effects with doxorubicin (DOX) in HGC27 gastric cancer cell lines. Here we report that our isobolographic analysis confirms the synergistic cytotoxic effects of PA-2 and DOX in HGC27 cells. Flow cytometry and immunoblotting indicate that PA-2 enhances DOX-mediated apoptosis. Importantly, PA-2 enhances the intracellular accumulation of DOX in HGC27 cells. The combination of DOX and PA-2 remarkably increases the release of cytochrome C and the activation of caspase-3 and caspase-9, compared with DOX treatment alone. Moreover, PA-2 attenuates the DOX-induced activation of Akt, ERK1/2 and p38 signaling pathways, providing a molecular mechanism for the synergistic effects of DOX and PA-2 in the induction of apoptosis. In conclusion, our studies demonstrate that PA-2 and DOX synergistically induce mitochondria-dependent apoptosis as PA-2 inhibits the PI3K/Akt, ERK1/2 and p38 pathways in HGC27 cells. These findings suggest that the combination treatment with PA-2 and DOX may represent a potent therapy for gastric cancer.


Assuntos
Apocynaceae/química , Apoptose/efeitos dos fármacos , Benzopiranos/farmacologia , Produtos Biológicos/farmacologia , Mitocôndrias/metabolismo , Naftalenos/farmacologia , Transdução de Sinais/efeitos dos fármacos , Apocynaceae/metabolismo , Benzopiranos/química , Linhagem Celular Tumoral , Doxorrubicina/farmacologia , Sinergismo Farmacológico , Humanos , Mitocôndrias/efeitos dos fármacos , Proteína Quinase 1 Ativada por Mitógeno/metabolismo , Proteína Quinase 3 Ativada por Mitógeno/metabolismo , Naftalenos/química , Fosfatidilinositol 3-Quinases/metabolismo , Caules de Planta/química , Caules de Planta/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Neoplasias Gástricas/metabolismo , Neoplasias Gástricas/patologia , Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
4.
Phytochemistry ; 168: 112127, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31550672

RESUMO

Five undescribed C21 pregnane glycosides, epigycosides D-H, together with four known analogues, two lignans, and a flavonoid have been isolated from the stems of Epigynum cochinchinensis. The structures of pregnane glycosides were elucidated using spectroscopic techniques and acid hydrolysis. The in vitro immunological activities were assessed against Con A-stimulated proliferation of mice splenocytes. The C21 pregnane glycosides showed immunosuppressive activity in a concentration-dependent manner. Moreover, epigycoside E exhibited a potent immunosuppressive effect, and the IC50 value on Con A-stimulated mice splenocytes was 22.1 ±â€¯6.4 µM. Epigycoside E also caused G0/G1 arrest, and inhibited TNF-α and IL-2 production.


Assuntos
Apocynaceae/química , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Imunossupressores/isolamento & purificação , Imunossupressores/farmacologia , Pregnanos/isolamento & purificação , Pregnanos/farmacologia , Baço/efeitos dos fármacos , Baço/imunologia , Animais , Ciclo Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Concanavalina A/antagonistas & inibidores , Concanavalina A/farmacologia , Cristalografia por Raios X , Relação Dose-Resposta a Droga , Glicosídeos/química , Imunossupressores/química , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Modelos Moleculares , Estrutura Molecular , Caules de Planta/química , Pregnanos/química , Relação Estrutura-Atividade , Linfócitos T/efeitos dos fármacos
5.
Fitoterapia ; 138: 104354, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31473334

RESUMO

Four new alkaloids, melodinines W1-W4 (1-4), together with twenty one known alkaloids (5-25) were isolated from Melodinus henryi. The structures with absolute configurations were elucidated by extensive MS and NMR spectroscopic methods, as well as the single crystal X-ray diffraction and ECD calculations. All compounds were evaluated for their cytotoxicities to five human cancer cell lines. Many compounds showed certain cytotoxicities to five human cancer cell lines with an IC50 range of 1.4-29.4 µM.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apocynaceae/química , Casca de Planta/química , Alcaloides de Triptamina e Secologanina/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , China , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Alcaloides de Triptamina e Secologanina/isolamento & purificação
6.
Fitoterapia ; 138: 104347, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31470065

RESUMO

Five new monoterpenoid indole alkaloids, melotenuines A-E (1-5), along with 18 known indole alkaloids, were isolated from the twigs and leaves of Melodinus tenuicaudatus. The structures of the new alkaloids were determined by a combination of MS, NMR and ECD analysis. Melotenuine A (1) represents the first example of aspidosperma-meloscandonine type bisindole alkaloids characterized by a methylene bridge between the two monomers, while melotenuine B (2) possessed a rare eburnamine-melsocandonine skeleton. All of the new indole alkaloids were evaluated for in vitro cytotoxicities against five human cancer cell lines. Among them, alkaloid 4 showed specific cytotoxicity against HL-60 cell line with IC50 value (5.15 ±â€¯0.16 µM) comparable with that of positive control.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apocynaceae/química , Folhas de Planta/química , Alcaloides de Triptamina e Secologanina/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , China , Ensaios de Seleção de Medicamentos Antitumorais , Células HL-60 , Humanos , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Alcaloides de Triptamina e Secologanina/isolamento & purificação
7.
Fitoterapia ; 137: 104258, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31284017

RESUMO

Four new indole alkaloids (1-4) and twenty known compounds (5-24) were isolated from the leaves and stems, and fruits of Kopsia officinalis. Their structures were confirmed by means of spectroscopic methods. All these isolates were evaluated for their antagonizing high glucose-evoked podocyte injury activity for the first time, and compounds 5-8 showed potent activity with EC50 values of 3.0-12.0 µM.


Assuntos
Apocynaceae/química , Alcaloides Indólicos/farmacologia , Podócitos/efeitos dos fármacos , Animais , Células Cultivadas , China , Frutas/química , Glucose , Alcaloides Indólicos/isolamento & purificação , Camundongos , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Folhas de Planta/química , Caules de Planta/química
8.
Artigo em Inglês | MEDLINE | ID: mdl-31314740

RESUMO

Background We investigated the effects of a polyherbal formulation prepared from the extracts of Mondia whitei (Periplocaceae), Dracaena arborea (Dracaenaceae), and Bridelia ferruginea (Euphorbiaceae) (MDB) on the sexual behavior of normal rats (NR) and prediabetic rats (PR). Methods Male Wistar rats were administered with drinking fructose solution (21%) or tap water for 16 weeks. After induction of prediabetic status, NR (n = 30) and PR (n = 30) were randomly distributed into 10 groups of six animals each and orally treated with distilled water (10 mL/kg), sildenafil citrate (5 mg/kg), or MDB (50, 100, or 500 mg/kg) for 21 days. Sexual behavior parameters per series (S) of ejaculation were evaluated on days 1, 7, 14, and 21. Results Drinking fructose solution (21%) induced prediabetic status in rats, characterized by a significant (p < 0.01) increase in glycemia by 43.41% compared with the control group. MDB improved sexual performances of NR and PR by increasing the mount frequency (MF) and the intromission frequency (IF) as well as the number of rats capable of ejaculating. For instance, the MF and the IF were significantly increased in animals administered with MDB for 7 (50 mg/kg, S1 and S2), 14 (100 mg/kg, S3), or 21 days (100 or 500 mg/kg, S2). This increase was more pronounced on days 7 and 14 in NR and PR treated with sildenafil citrate or MDB extracts, respectively. Conclusions The mixture of MDB improved sexual activity in NR and PR. This result may further justify the traditional use of these plants as sexual performance enhancers.


Assuntos
Apocynaceae/química , Dracaena/química , Euphorbiaceae/química , Extratos Vegetais/farmacologia , Estado Pré-Diabético/tratamento farmacológico , Comportamento Sexual Animal/efeitos dos fármacos , Comportamento Sexual/efeitos dos fármacos , Animais , Ejaculação/efeitos dos fármacos , Masculino , Ratos , Ratos Wistar
9.
Cell Mol Biol (Noisy-le-grand) ; 65(5): 59-63, 2019 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-31304908

RESUMO

Epilepsy is a common chronic disease of the central nervous system that can last for years or even decades, causing serious adverse effects on the body, mind, and psychology of patients. Traditional antiepileptic drugs can effectively control seizures, but because of large individual differences, serious adverse reactions, narrow therapeutic window and other shortcomings, more effective, new treatment drugs are looked for. Streptocaulon griffithii is a plant of Asclepiadaceae. 16-O-acetyldigitoxigenin (ACE) is a strong cardiac glycoside isolated from methanol extract of Streptocaulon griffithii. The aim of this study was to investigate the antiepileptic effect of ACE on Pilocarpine (Pilo) induced epilepsy in mice, and to explore the effect of mTOR signaling pathway on its antiepileptic effect. The results showed that ACE had antiepileptic and neuroprotective effects on Pilo induced epilepsy mice. ACE attenuates Pilo induced seizures by inhibiting the activation of p-mTOR/p-70S6K pathway, and inhibits Pilocarpine induced brain damage by inhibiting mTOR signaling pathway. These results suggest that ACE has a promising future in the treatment of epilepsy and other nervous system diseases.


Assuntos
Anticonvulsivantes/farmacologia , Digitoxigenina/análogos & derivados , Digitoxigenina/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Fármacos Neuroprotetores/farmacologia , Transdução de Sinais/efeitos dos fármacos , Serina-Treonina Quinases TOR/metabolismo , Animais , Anticonvulsivantes/uso terapêutico , Apocynaceae/química , Caspase 3/metabolismo , Digitoxigenina/uso terapêutico , Epilepsia/induzido quimicamente , Epilepsia/tratamento farmacológico , Hipocampo/efeitos dos fármacos , Hipocampo/metabolismo , Hipocampo/patologia , Interleucina-1beta/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos ICR , Neurônios/efeitos dos fármacos , Neurônios/metabolismo , Pilocarpina/administração & dosagem , Pilocarpina/farmacologia , Proteínas Quinases S6 Ribossômicas 90-kDa/metabolismo , Convulsões/induzido quimicamente , Convulsões/tratamento farmacológico , Fator de Necrose Tumoral alfa/metabolismo
10.
Asian Pac J Cancer Prev ; 20(7): 1995-2001, 2019 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-31350956

RESUMO

Objective: To evaluate the antitumor effects of polyethylene glycol (PEG) microspheres with adsorbed Hancornia speciosa ethanolic extract (HSEE) on blood mononuclear (MN) cells co-cultured with MCF-7 breast cancer cells. Methods: PEG microspheres were adsorbed with HSEE and examined by flow cytometry and fluorescence microscopy. MCF-7 and MN cells obtained from volunteer donors were pre-incubated alone or co-cultured (MN and MCF-7 cells) for 24 h with or without HSEE, PEG microspheres or PEG adsorbed with HSEE (PEG-HSEE). Cell viability, superoxide release and superoxide dismutase were determined. Results: Fluorescence microscopy showed that PEG microspheres were able to absorb HSEE throughout their surface. Irrespective of the treatment, the viability index of MN cells, MCF-7 and their co-culture was not affected. Superoxide release increased in co-cultured cells treated with HSEE, adsorbed or not onto PEG microspheres. In co-cultured cells, SOD levels in culture supernatant increased in the treatment with HSEE, adsorbed onto PEG microspheres or not. Conclusion: HSEE has direct effects on MN cells co-cultured with MCF-7 cells. The results suggest the benefits of Hancornia speciosa fruit consumption by women at risk of breast cancer. In addition, because PEG-HSEE maintained oxidative balance in co-cultured cells, it is a promising alternative for the treatment of tumor cells.


Assuntos
Apocynaceae/química , Neoplasias da Mama/tratamento farmacológico , Frutas/química , Leucócitos Mononucleares/efeitos dos fármacos , Microesferas , Extratos Vegetais/farmacologia , Polietilenoglicóis/química , Adolescente , Adulto , Apoptose , Neoplasias da Mama/metabolismo , Neoplasias da Mama/patologia , Proliferação de Células , Técnicas de Cocultura , Feminino , Voluntários Saudáveis , Humanos , Leucócitos Mononucleares/metabolismo , Masculino , Superóxido Dismutase-1/metabolismo , Superóxidos/metabolismo , Células Tumorais Cultivadas , Adulto Jovem
11.
Molecules ; 24(14)2019 Jul 19.
Artigo em Inglês | MEDLINE | ID: mdl-31330950

RESUMO

Wildly grown in most regions of the world, Carissa edulis is a highly underutilised fruit with significant antioxidant characteristics. The phyto and physicochemical properties of C. edulis berries at different stages of ripening are evaluated in this work. Total flavonoids (TF), total phenolic content (TPC) and antioxidant activity were determined spectrophotometrically, while concentration of polyphenols was determined using liquid chromatography coupled to diode array detection and electrospray ionization mass spectrometry. Results showed that antioxidant activity was lowest (18.36 ± 0.12 mg TE/g) in RS3 and decreased with TPC upon increased ripening. Conversely, TF increased with ripening progression with TF found to be highest in RS3 (5.92 ± 0.03 mg CE/g). Identified phenolic acids in C. edulis were quinic acid, protocatechuoyl-hexose, neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid and dicaffeoylquinic acid. Identified flavonoids included rutin, catechin, procyanidin dimer, procyanidin trimer, quercetin-3-O-glucosyl-xyloside, quercetin-3-O-robinobioside, quercetin-3-O-glucoside and quercetin-3-OH-3-methylglutaryl-glucoside. Physicochemical properties of C. edulis varied among samples with sugar/acid ratio of C. edulis ranging from 25.70 for RS1 to 50.36 for RS3. Ripening stage of C. edulis undoubtedly affects the phyto and physicochemical properties of C. edulis.


Assuntos
Apocynaceae/química , Fenômenos Químicos , Frutas/química , Compostos Fitoquímicos/química , Polifenóis/química , Antioxidantes/química , Antioxidantes/farmacologia , Concentração de Íons de Hidrogênio , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Polifenóis/isolamento & purificação , Polifenóis/farmacologia , Solubilidade , Análise Espectral
12.
Food Chem ; 293: 499-510, 2019 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-31151641

RESUMO

This study aims to link morphological and physico-chemical parameters with maturity stages of Natal plum (Carissa macrocarpa), an edible southern African fruit. Harvesting via an integrative holistic approach is recommended for optimal quality and functional compounds. Fruits at dark green (M1), light green (M2), colour break or pink (M3), red (M4), dark red (M5) stages were harvested in 2016 and 2017 seasons. The principal component analysis illustrated the colour value a* (redness), fruit weight, size (length and width), sugars (glucose and fructose), ascorbic acid content, cyanidin derivatives (cyanidin-3-O-pyranoside, cyanidin 3-O-ß-sambubioside, cyanidin-3-O-glucoside), naringenin 4'-O-glucoside, and antioxidant property (FRAP) were higher in the following order of maturity stages M5 > M4 > M3 > M2 > M1. Quercetin 3-O-rhamnosyl galactoside and glucoside were higher in green (h° higher) firm M1 to M3 stages. A strong correlation exists between fruit weight, size, a* value and cyanidin derivatives or naringenin 4'-O-glucoside or ascorbic acid content or antioxidant activity. Thus, the M4 and M5 stages of Natal plum can serve as functional food.


Assuntos
Apocynaceae/química , Antocianinas/análise , Antioxidantes/química , Apocynaceae/metabolismo , Cromatografia Líquida de Alta Pressão , Dissacarídeos/análise , Frutas/química , Frutas/crescimento & desenvolvimento , Frutas/metabolismo , Alimento Funcional/análise , Glucosídeos/análise , Espectrometria de Massas , Análise de Componente Principal , Açúcares/análise
13.
Food Chem Toxicol ; 131: 110534, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31150781

RESUMO

Acute and subacute toxicities of the ethanol extract from Epigynum auritum (EAE) wereperformed by oral administration in pathogen-free mice. Acute toxicity study was performed at a single dose of 5000 mg/kg for 14 consecutive days, while subacute toxicity test was conducted by daily oral administration of EAE at doses of 312, 625, 1250, and 2500 mg/kg for 28 days. Acute toxicity study showed that LD50 of EAE was over 5000 mg/kg. The results of subacute toxicity showed no significant adverse effect of EAE at 312 mg/kg. Moreover, EAE exhibited toxicities to liver, spleen and kidney in mice determined by hematological, serum biochemical and histological analyses during daily oral administration of 1250 mg/kg and 2500 mg/kg EAE. The results revealed that the dose of EAE lower than 625 mg/kg can be regarded as safe.


Assuntos
Apocynaceae/química , Componentes Aéreos da Planta/química , Extratos Vegetais/toxicidade , Administração Oral , Animais , Relação Dose-Resposta a Droga , Etanol/química , Feminino , Rim/patologia , Fígado/patologia , Pulmão/patologia , Masculino , Camundongos Endogâmicos ICR , Extratos Vegetais/administração & dosagem , Extratos Vegetais/isolamento & purificação , Potássio/sangue , Sódio/sangue , Baço/patologia , Testes de Toxicidade Aguda , Testes de Toxicidade Subaguda
14.
Genes (Basel) ; 10(6)2019 06 12.
Artigo em Inglês | MEDLINE | ID: mdl-31212875

RESUMO

This paper reports on the successful management of hyperphagia (exaggerated hunger) in a 14yr-old female with Prader-Willi syndrome (PWS). This child was diagnosed with PWS, (maternal uniparental disomy) at 18 months due to developmental delay, hypertonia, weight gain and extreme eating behaviour. Treatment of a supplement for appetite suppression commenced at 2 years of age. This single-case records ingestion of an Indian cactus succulent Caralluma fimbriata extract (CFE) over 12 years, resulting in anecdotal satiety, free access to food and management of weight within normal range. CFE was administered in a drink daily and dose was slowly escalated by observation for appetite suppression. Rigorous testing determined blood count, vitamins, key minerals, HbA1c, IGF-1 and function of the liver and thyroid all within normal range. The report suggests a strategy for early intervention against hyperphagia and obesity in PWS. This case was the instigator of the successful Australian PWS/CFE pilot and though anecdotal, the adolescent continues to ingest CFE followed by paediatricians at the Royal Children's Hospital Melbourne, Victoria, Australia. Future clinical trials are worth considering, to determine an appropriate dose for individuals with PWS.


Assuntos
Apocynaceae/química , Regulação do Apetite/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Síndrome de Prader-Willi/dietoterapia , Adolescente , Contagem de Células Sanguíneas , Feminino , Hemoglobina A Glicada/metabolismo , Humanos , Fator de Crescimento Insulin-Like I/metabolismo , Fígado/efeitos dos fármacos , Fígado/metabolismo , Minerais/sangue , Extratos Vegetais/química , Síndrome de Prader-Willi/sangue , Síndrome de Prader-Willi/patologia , Glândula Tireoide/efeitos dos fármacos , Vitaminas/sangue
15.
ScientificWorldJournal ; 2019: 7549620, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31223295

RESUMO

Carissa edulis is a plant used in the management of oxidative stress and inflammatory related disorders such as malaria, rheumatism inflammation, and cardiovascular diseases. The present study evaluates the total phenolic content, antioxidant capacity (DPPH, ABTS, and FRAP), and the bioactive compounds present in the various extracts of C. edulis (HEC, MEC, AEC, and PC). An HPLC analysis determined the different compounds present in the extracts. High concentration of total phenolic content was observed in aqueous and methanolic extracts more than in the hydroethanolic extract though not significantly different. Flavonoids were higher in the hydroethanolic and methanolic extracts, respectively, with 14.84 mg RE/g extract and 12.02 mg RE/g extract. Tannins were also found in large amounts in the same two extracts with 26.76 mg TAE/g extract and 34.67 mg TEE/g extract. The percentage radical scavenging activity DPPH ranged between 58.63% and 94.67% for aqueous extract and for ABTS between 51.39% and 94.12% for the methanolic extract. The highest FRAP was obtained in the methanolic extract (6.73 g AAE/100 g extract). HPLC analysis revealed the presence of quercetin, rutin, and gallic acid in the different extracts. C. edulis represents a potential source of bioactive components with antioxidant capacity.


Assuntos
Antioxidantes/farmacologia , Apocynaceae/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Antioxidantes/química , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Flavonoides/química , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/farmacologia , Fenóis/química , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Taninos/química
16.
Life Sci ; 231: 116535, 2019 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-31175857

RESUMO

Latex proteins from P. pudica (LPPp) have anti-inflammatory activity. In the present study, LPPp was evaluated to protect animals against inflammatory ulcerative colitis (UC). UC was induced by intracolonic instillation of a 6% acetic acid solution and the animals received LPPp (10, 20 or 40 mg/kg) by intraperitoneal route 1 h before and 17 h after acetic acid injection. Eighteen hours after instillation of acetic acid, the mice were euthanized and the colons were excised to determine the wet weight, macroscopic and microscopic lesion scores, myeloperoxidase (MPO) activity, IL1-ß levels, glutathione (GSH) and malondialdehyde (MDA) concentration and superoxide dismutase (SOD) activity. The results revealed that LPPp treatment (40 mg/kg) had a protective effect on acetic acid-induced colitis by reducing the wet weight, macroscopic and microscopic scores of intestinal lesions and colonic MPO activity. Additionally, LPPp inhibited tissue oxidative stress, since decreases in GSH consumption, MDA concentration and SOD activity were observed. The treatment with LPPp reduced the levels of cytokine IL-1ß, contributing to the reduction of colon inflammation. Biochemical investigation showed that LPPp comprises a mixture of proteins containing proteinases, chitinases and proteinase inhibitors. These data suggest that LPPp has a protective effect against intestinal damage through mechanisms that involve the inhibition of inflammatory cell infiltration, cytokine release and oxidative stress.


Assuntos
Apocynaceae/química , Colite/tratamento farmacológico , Látex/farmacologia , Proteínas de Plantas/farmacologia , Ácido Acético , Animais , Apocynaceae/metabolismo , Colite/induzido quimicamente , Colite/metabolismo , Colo/efeitos dos fármacos , Citocinas/metabolismo , Glutationa/metabolismo , Inflamação/tratamento farmacológico , Interleucina-1beta/metabolismo , Intestinos/patologia , Látex/isolamento & purificação , Masculino , Camundongos , Estresse Oxidativo/efeitos dos fármacos , Proteínas de Plantas/isolamento & purificação , Substâncias Protetoras/farmacologia , Fator de Necrose Tumoral alfa/metabolismo
17.
Planta Med ; 85(11-12): 965-972, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31250411

RESUMO

Three previously undescribed cardenolides, acovenosigenin A 3-O-α-L-acofriopyranoside (1: ), 14-anhydroacovenosigenin A 3-O-[ß-D-glucopyranosyl-(1″→4')-O-α-L-acofriopyranoside] (2: ), and 14-anhydroacovenosigenin A 3-O-[ß-D-glucopyranosyl-(1″→4')-O-α-L-acovenopyranoside] (3: ), together with the two already known ones, 14-anhydrodigitoxigenin 3-O-ß-D-glucopyranoside (4: ) and acospectoside A (5: ), were isolated from the leaves of Acokanthera oblongifolia. The influence of cardenolides 1:  - 3: and acovenoside A (found in the Acokanthera genus) on three cancer cell lines (HT29, HCT116, and AGS) was also investigated. The most promising results, in comparison with oxaliplatin, were obtained for compound 1: , which was found to be highly cytotoxic for all tested cell lines, HT29 (IC50 = 63.49 nM), HCT116 (IC50 = 67.35 nM), and AGS (IC50 = 80.92 nM). Unfortunately, 1: also showed similar toxicity towards normal lymphocytes (IC50 = 98.03 nM).


Assuntos
Apocynaceae/química , Cardenolídeos/isolamento & purificação , Citotoxinas/isolamento & purificação , Folhas de Planta/química , Cardenolídeos/farmacologia , Linhagem Celular Tumoral/efeitos dos fármacos , Citotoxinas/farmacologia , Humanos , Linfócitos/efeitos dos fármacos
18.
Curr Pharm Biotechnol ; 20(13): 1134-1146, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31237203

RESUMO

BACKGROUND: The vernacular name 'Harmal' is used for two plant species in Saudi Arabia, i.e. Peganum harmala L. and Rhazya stricta Decne. Both are important medicinal plants which offer interesting pharmacological properties. OBJECTIVE: This study aimed to evaluate the genetic diversity among different populations of harmal based on chemical variations of alkaloids and molecular polymorphism. METHODS: Total alkaloids were extracted from plants of three populations of each species and estimated by using spectrophotometer and the chemical compounds were analyzed by Gas chromatography mass spectrometry (GC-MS). Molecular polymorphism was estimated by using the Inter Simple Sequence Repeat (ISSR) fingerprints. RESULTS: The results showed that the alkaloids content of R. stricta was higher than P. harmala populations. The GC-MS analysis revealed the presence of (65-53) compounds in R. stricta and P. harmala, and the percentage of polymorphism was found to be 93.2%. Sixteen ISSR primers produced 170 scorable bands with an average of 9.6 bands per primer and 75%-100% polymorphism. The cluster analysis using the unweighted pair-group method of the arithmetic average (UPGMA) method based on combined data of GC-MS and ISSR markers divided the six harmal genotypes into two major groups. CONCLUSION: The existence of variations in chemical and genetic markers is useful for the selection of potential genotypes for medicinal use, and for breeding lines for medicinal substances production to spare wild plants from uncontrolled harvesting for folk medicine.


Assuntos
Alcaloides/análise , Apocynaceae/genética , Repetições de Microssatélites , Peganum/genética , Polimorfismo Genético , Apocynaceae/química , Biomarcadores/análise , Cromatografia Gasosa-Espectrometria de Massas , Genótipo , Peganum/química , Plantas Medicinais/química , Plantas Medicinais/genética , Arábia Saudita
19.
BMC Complement Altern Med ; 19(1): 152, 2019 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-31253153

RESUMO

BACKGROUND: The leaves of Gongronema latifolium Benth. have long been recognized traditionally as a remedy for a variety of ailments in Africa. This study was conducted to evaluate the safety profile of the ethanolic extract of G. latifolium (GLES) leaves through a repeated dose 90-day oral toxicity study in male and female of Sprague Dawley rats. METHODS: GLES was orally administered at doses of 250, 500 and 1000 mg/kg/day consecutively for 90 days. RESULTS: No behavioral or physiological changes and mortality were observed. GLES did not have a marked impact on general hematological parameters and did not precipitate nephrotoxicity. However, compared to the control, serum triglycerides, total cholesterol and low-density lipoprotein levels were lower and white adipose tissue paired retroperitoneal fat depots were depleted in male rats treated with GLES3 by the end of the experiment. The liver was significantly enlarged in GLES-treated rats of both sexes. Negative gender-specific alterations were observed with the highest dose. Adverse risk was evident in the female rats mainly due to marked body weight gain and cerebrum weight reduction. CONCLUSION: Further research is needed to reach more specific conclusions about to the safety of ingesting high doses of GLES for long periods of time.


Assuntos
Apocynaceae/química , Extratos Vegetais/administração & dosagem , Tecido Adiposo Branco/efeitos dos fármacos , Administração Oral , Animais , Feminino , Fígado/efeitos dos fármacos , Masculino , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Folhas de Planta/química , Ratos , Ratos Sprague-Dawley , Testes de Toxicidade
20.
Curr Pharm Biotechnol ; 20(8): 679-688, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31244420

RESUMO

OBJECTIVE: In the present study, Solenostemma argel effervescent tablets were prepared from Argel methanolic extract. METHODS: The tablets were examined for their ability to impede carbon tetrachloride (CCl4)-induced lipid peroxidation in mice liver. The antioxidant activities of the enzymes; super-oxide dismutase (SOD), glutathione peroxidase (GS-PX) along with malondialdehyde level were tested in liver tissues. RESULTS: The obtained results indicated that the antioxidant enzyme activities were remarkably reduced while the level of Malondialdehyde (MDA), which shows lipid peroxidation, and the activity of alanine aminotransferase (a liver function test) were remarkably intensified following intra-peritoneal i.p injection with the single sub-lethal hepatotoxic dose of CCl4 compared to the control. A necrotic lesion in the liver of mice injected with CCl4 was observed by the histopathological examination. The damaging influence of CCl4 was improved by the retreatment with Argel or BHT, which could also be observed in the normal appearance of the liver tissue. CONCLUSION: In this study, it was concluded that S. Argel and butylated hydroxytoluene (BHT) could be effective by decreasing lipid peroxidation and increasing the activities of antioxidant enzymes. Therefore, Argel might be applied as a hepatoprotective agent without any side effects.


Assuntos
Antioxidantes/farmacologia , Apocynaceae/química , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Fígado/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Antioxidantes/isolamento & purificação , Tetracloreto de Carbono , Doença Hepática Induzida por Substâncias e Drogas/enzimologia , Doença Hepática Induzida por Substâncias e Drogas/patologia , Fígado/enzimologia , Fígado/patologia , Masculino , Camundongos , Extratos Vegetais/isolamento & purificação , Comprimidos
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