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1.
Molecules ; 25(24)2020 Dec 10.
Artigo em Inglês | MEDLINE | ID: mdl-33321838

RESUMO

Salvia officinalis L. (sage) is one of the most appreciated plants for its plethora of biologically active compounds. The objective of our research was a comparative study, in the Mediterranean context, of chemical composition, anticholinesterases, and antioxidant properties of essential oils (EOs) from sage collected in three areas (S1-S3) of Southern Italy. EOs were extracted by hydrodistillation and analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory properties were investigated by employing Ellman's method. Four in vitro assays, namely, 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric-reducing ability power (FRAP), and ß-carotene bleaching tests, were used to study the antioxidant effects. Camphor (16.16-18.92%), 1,8-cineole (8.80-9.86%), ß-pinene (3.08-9.14%), camphene (6.27-8.08%), and α-thujone (1.17-9.26%) are identified as the most abundant constituents. However, the content of these constituents varied depending on environmental factors and pedoclimatic conditions. Principal component analysis (PCA) was performed. Based on Relative Antioxidant Capacity Index (RACI), S2 essential oil exhibited the highest radical potential with an IC50 value of 20.64 µg/mL in ABTS test and presented the highest protection of lipid peroxidation with IC50 values of 38.06 and 46.32 µg/mL after 30 and 60 min of incubation, respectively. The most promising inhibitory activity against BChE was found for S3 sample (IC50 of 33.13 µg/mL).


Assuntos
Óleos Voláteis/química , Óleos Voláteis/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Salvia officinalis/química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Relação Dose-Resposta a Droga , Cromatografia Gasosa-Espectrometria de Massas , Itália , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Relação Estrutura-Atividade
2.
J Pharm Pharmacol ; 65(12): 1726-35, 2013 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-24236982

RESUMO

OBJECTIVES: This study involves for the first time the evaluation of Berberis aetnensis C. Presl. and Berberis libanotica Ehrenb. ex C.K. Schneid. roots for anticholinesterase and antioxidant properties, with the aim to search compounds possibly useful for the treatment of Alzheimer's disease (AD). METHODS: Samples were evaluated for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The antioxidant activity was assayed by 2,2-diphenyl-1-picrylhydrazyl radical and ß-carotene bleaching tests. Berberine and palmatine were isolated by flash chromatography and identified by spectrometric methods as main constituents. Non-polar compounds were analysed by gas chromatography and gas chromatography-mass spectrometry. KEY FINDINGS: Extracts, fractions and isolated compounds inhibited AChE and BChE to varying degrees. The methanol fractions exhibited the strongest AChE inhibitory activity with inhibitory concentration 50% (IC50 ) of 7.6 and 16.9 µg/ml for B. aetnensis and B. libanotica, respectively. The alkaloid fraction of B. aetnensis inhibited AChE (IC50 of 24.5 µg/ml) and possessed the highest antioxidant activity (IC50 value of 2.2 µg/ml in ß-carotene-bleaching test after 30 min of incubation). Berberine was more potent of palmatine against AChE (IC50 of 2.2 and 7.4 µg/ml, respectively). CONCLUSIONS: These findings raise the possibility of developing B. aetnensis and B. libanotica as a promising candidate for the treatment of AD.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Antioxidantes/farmacologia , Berberis/química , Inibidores da Colinesterase/farmacologia , Extratos Vegetais/farmacologia , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Doença de Alzheimer/metabolismo , Berberina/farmacologia , Humanos , Estresse Oxidativo
3.
Anticancer Agents Med Chem ; 13(5): 768-76, 2013 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-23157592

RESUMO

The search for improved cytotoxic agents continues to be an important line in the discovery of modern anticancer drugs. Sarcopoterium spinosum (L.) Spach is mentioned in ethnobotanical surveys as a medicinal plant used for the treatment of cancer. The aim of this study is to investigate and to compare the aerial parts of S. spinosum collected in Italy and Lebanon for their chemical composition and their antiproliferative activity against ACHN, C32, A375, MCF-7, LNCaP and HeLa human cancer cell lines using SRB assay. The main constituent tormentic acid was isolated by MPLC and characterized by spectroscopic techniques (NMR, MS). Non polar compounds were analyzed by GC and GC-MS. S. spinosum showed an interesting antiproliferative activity against ACHN and C32 cell lines with IC(50) values of 2.4 and 2.7 µg/ml for S. spinosum from Italy and Lebanon, respectively. Remarkable results were obtained also against A375 and LNCaP cell lines. The cytotoxicity against ACHN cell line could be partially attributed to tormentic acid that demonstrated a higher cytotoxicity than the positive control vinblastine. Close association between the radical scavenging activity (evaluated by DPPH and ABTS assay) and cytotoxicity was also demonstrated. This investigation demonstrated the potential cytotoxic activity of S. spinosum taking into account also that none of the tested extracts, fractions and isolated compound affected the proliferation of normal cell line 142BR. Tormentic acid, the major constituent isolated from S. spinosum, play an important role in the cytotoxicity exhibited by the extract.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Componentes Aéreos da Planta , Extratos Vegetais/farmacologia , Plantas Medicinais , Triterpenos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/isolamento & purificação , Sequestradores de Radicais Livres/farmacologia , Inibidores do Crescimento/química , Inibidores do Crescimento/isolamento & purificação , Inibidores do Crescimento/farmacologia , Células HeLa , Humanos , Neoplasias Renais/tratamento farmacológico , Neoplasias Renais/patologia , Células MCF-7 , Masculino , Melanoma Experimental/tratamento farmacológico , Melanoma Experimental/patologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Neoplasias da Próstata/tratamento farmacológico , Neoplasias da Próstata/patologia , Triterpenos/química , Triterpenos/isolamento & purificação
4.
J Enzyme Inhib Med Chem ; 25(5): 622-8, 2010 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-20429778

RESUMO

This study aimed to investigate the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity of the essential oils from Pinus nigra subsp. nigra, P. nigra var. calabrica, and P. heldreichii subsp. leucodermis. This activity is relevant to the treatment of Alzheimer's disease (AD), since cholinesterase drugs are currently the only drugs available to treat AD. P. heldreichii subsp. leucodermis exhibited the most promising activity, with IC(50) values of 51.1 and 80.6 microg/mL against AChE and BChE, respectively. An interesting activity against AChE was also observed with P. nigra subsp. nigra essential oil, with an IC(50) value of 94.4 microg/mL. Essential oils were analyzed by GC and GC-MS with the purpose of investigating their relationships with the observed activities. Among the identified constituents, terpinolene, beta-phellandrene, linalyl acetate, trans-caryophyllene, and terpinen-4-ol were tested. trans-Caryophyllene and terpinen-4-ol inhibited BChE with IC(50) values of 78.6 and 107.6 microg/mL, respectively. beta-Phellandrene was selective against AChE (IC(50) value of 120.2 microg/mL).


Assuntos
Inibidores da Colinesterase/análise , Inibidores da Colinesterase/química , Óleos Voláteis/química , Pinus/química , Terpenos/análise , Terpenos/química , Acetilcolinesterase , Doença de Alzheimer/tratamento farmacológico , Butirilcolinesterase , Descoberta de Drogas , Cromatografia Gasosa-Espectrometria de Massas , Estrutura Molecular , Concentração Osmolar , Fitoterapia , Folhas de Planta/química
5.
Nat Prod Res ; 23(18): 1707-18, 2009.
Artigo em Inglês | MEDLINE | ID: mdl-19921589

RESUMO

This study is aimed to evaluate the in vitro cytotoxicity of Senecio stabianus Lacaita (Asteraceae) against renal adenocarcinoma ACHN, hormone-dependent prostate carcinoma LNCaP, amelanotic melanoma C32 and human breast adenocarcinoma MCF-7 cell lines. The n-hexane extract showed an interesting activity with IC(50) values of 62.7 and 71.1 microg mL(-1) against C32 and LNCaP, respectively. Two compounds identified in the n-hexane extract, linalool and beta-caryophyllene, were found to be active against C32 cells (IC(50) values of 23.2 and 20.1 microg mL(-1), respectively). Among tested constituents, the highest activity was found when alpha-humulene was applied to LNCaP cells (IC(50) of 11.2 microg mL(-1)). In order to complete the phytochemical study on S. stabianus, which has not been investigated previously, the most characteristic secondary metabolites of Senecio genus, pyrrolizidine alkaloids (PAs), were analysed. Here we report the isolation, structural elucidation and identification of nine PAs.


Assuntos
Extratos Vegetais/química , Extratos Vegetais/farmacologia , Senécio/química , Monoterpenos Acíclicos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Hexanos/química , Humanos , Sesquiterpenos Monocíclicos , Monoterpenos/química , Monoterpenos/farmacologia , Sesquiterpenos Policíclicos , Alcaloides de Pirrolizidina/química , Alcaloides de Pirrolizidina/farmacologia , Sesquiterpenos/química , Sesquiterpenos/farmacologia
6.
J Ethnobiol Ethnomed ; 2: 52, 2006 Dec 11.
Artigo em Inglês | MEDLINE | ID: mdl-17156472

RESUMO

BACKGROUND: A series of preliminary research projects on plants used in Calabria (Southern Italy) in veterinary science and in other ethno-botanical fields (minor nourishment, domestic and handicraft sector) was carried out in the last twenty years. From the ethno-botanical point of view, Calabria is one of the most interesting region, since in the ancient times it was subject to the dominant cultures of several people (Greeks, Romans, Byzantines, Arabs, Normans etc.). Until some decades ago the road network was poorly developed and villages were isolated, so that the culture of the "subsistence" and some archaic customs were kept. METHODS: Data were collected by means of "open" interviews to farmers, shepherds and housewives in the last twenty years. More than 100 informants were interviewed, mostly over 50 years old. Plants were identified by local informants through gathering in the area or through examination of the fresh plants collected by the researchers. The collected data were compared with pharmacobotanical papers mainly of southern Italy and with other studies, in order to highlight novelties or concordances of uses. RESULTS: The use of 62 taxa distributed into 34 families are described. Among these, 8 are or were employed in veterinary science, 8 as anti-parasitic agents, 19 in minor nourishment, 5 as seasoning, 38 for other uses. Some toxic species for cattle are also mentioned. CONCLUSION: Among the major findings: the use of Helleborus bocconei for bronchitis of bovines and of Scrophularia canina for lameness in veterinary science; Nerium oleander and Urginea maritima as anti-parasitic agents; Epilobium angustifolium, Centaurea napifolia L. and C. sphaerocephala L. in minor nourishment.


Assuntos
Etnobotânica , Produtos Domésticos , Fitoterapia/veterinária , Plantas Comestíveis , Medicina Veterinária , Idoso , Idoso de 80 Anos ou mais , Animais , Antropologia Cultural , Antiparasitários/administração & dosagem , Feminino , Humanos , Itália , Masculino , Pessoa de Meia-Idade , Preparações de Plantas/administração & dosagem , Plantas Medicinais , Plantas Tóxicas , Terminologia como Assunto
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