RESUMO
Thirteen lipophilic extracts prepared with n-hexane from various parts of Pistacia vera L. tree (Anacardiaceae) growing in Turkey were screened for their in vitro activity against four parasitic protozoa, Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani and Plasmodium falciparum. Melarsoprol, benznidazole, miltefosine, artemisinin and chloroquine were used as reference drugs. The cytotoxic potentials of the extracts on rat skeletal myoblast (L6) cells were also assessed and compared to that of podophyllotoxin. The screening method employed was medium-throughput, where the extracts were tested at two concentrations, at 0.8 and 4.8 microg/ml (T. brucei rhodesiense, L. donovani and Plasmodium falciparum), or at 1.6 and 9.7 microg/ml (T. cruzi and L6 cells). At 4.8 microg/ml concentration, the branch extract of Pistacia vera (PV-BR) significantly inhibited (77.3%) the growth of L. donovani, whereas the dry leaf extract (PV-DL) was active against Plasmodium falciparum (60.6% inhibition). The IC50 values of these extracts were determined as 2.3 microg/ml (PV-BR, L. donovani) and 3.65 microg/ml (PV-DL, Plasmodium falciparum). None of the extracts possessed cytotoxicity on mammalian cells.
Assuntos
Antiprotozoários/farmacologia , Pistacia/química , Plasmodium falciparum/efeitos dos fármacos , Trypanosomatina/efeitos dos fármacos , Animais , Antiprotozoários/análise , Linhagem Celular , Leishmania donovani/efeitos dos fármacos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Ratos , Trypanosoma brucei rhodesiense/efeitos dos fármacos , Trypanosoma cruzi/efeitos dos fármacosRESUMO
The ethanolic extracts of a number of Turkish freshwater macrophytes (Potamogeton perfoliatus, Ranunculus tricophyllus and Cladophora glomerata) and marine macroalgae (Dictyota dichotoma, Halopteris scoparia, Posidonia oceanica, Scinaia furcellata, Sargassum natans and Ulva lactuca) were assayed for their in vitro antiprotozoal activity. Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani and Plasmodium falciparum were used as test organisms. The cytotoxicity of the extracts was also assessed against primary rat skeletal myoblasts (L6 cells). Whereas none of the extracts were active against T. cruzi, all crude extracts displayed appreciable trypanocidal activity against T. brucei rhodesiense, with S. natans being the most active one (IC(50) 7.4microg/ml). Except for the marine alga H. scoparia, all extracts also possessed leishmanicidal potential. The best antileishmanial activity was exerted by U. lactuca and P. oceanica (IC(50)'s 5.9 and 8.0microg/ml, respectively). Five extracts that demonstrated inhibitory activity towards P. falciparum (IC(50)'s 18.1-48.8microg/ml) were simultaneously assayed against FabI, a crucial enzyme of the fatty acid system of P. falciparum, to find out whether FabI was their target. The extracts of C. glomerata and U. lactuca efficiently inhibited the FabI enzyme with IC(50) values of 1.0 and 4.0microg/ml, respectively. None of the extracts were cytotoxic towards mammalian L6 cells. This work reports for the first time antiprotozoal activity of some Turkish marine and freshwater algae, as well as a target-based antiplasmodial screening for the identification of P. falciparum FabI inhibitors from aquatic and marine macrophytes.
Assuntos
Antiprotozoários/farmacologia , Phaeophyceae , Fitoterapia , Extratos Vegetais/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Animais , Antimaláricos/administração & dosagem , Antimaláricos/farmacologia , Antimaláricos/uso terapêutico , Antiprotozoários/administração & dosagem , Antiprotozoários/uso terapêutico , Inibidores Enzimáticos/administração & dosagem , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/uso terapêutico , Ácidos Graxos/biossíntese , Água Doce , Humanos , Leishmania donovani/efeitos dos fármacos , Malária Falciparum/tratamento farmacológico , Testes de Sensibilidade Parasitária , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Plasmodium falciparum/enzimologia , Ratos , Trypanosoma/efeitos dos fármacos , TurquiaRESUMO
A total of 58 extracts of different polarity were prepared from various organs of 16 species of Turkish plants and screened for their antitrypanosomal, antileishmanial and antiplasmodial activities. No significant activity was observed against Trypanosoma cruzi, whereas many extracts showed appreciable trypanocidal potential against T. brucei rhodesiense, with the CHCl(3)-soluble portion of Phlomis kurdica being the most active (IC(50) 2.7 microg[sol ]mL). Almost all extracts, particularly the CHCl(3) phases, exhibited growth inhibition activity against Leishmania donovani amastigotes. The CHCl(3)-solubles of Putoria calabrica roots (IC(50) 1.9 microg[sol ]mL), Wendlandia ligustroides leaves (IC(50) 2.1 microg[sol ]mL) and Rhododendron luteum leaves (IC(50) 2.3 microg[sol ]mL) displayed the highest leishmanicidal potential. The majority of the extracts also possessed antiplasmodial activity against the multi-drug resistant K1 Plasmodium falciparum strain. The most potent antiplasmodial activity was observed with the CHCl(3) extracts of Phlomis kurdica (IC(50) 1.5 microg[sol ]mL), P. leucophracta (IC(50) 1.6 microg[sol ]mL), Scrophularia cryptophila (IC(50) 1.8 microg[sol ]mL), Morina persica (IC(50) 1.9 microg[sol ]mL) and the aqueous root extract of Asperula nitida subsp. subcapitellata (IC(50) 1.6 microg[sol ]mL). Twenty-one extracts with significant antimalarial activity (IC(50) < 5 microg[sol ]mL) were also tested for their ability to inhibit the purified enoyl-ACP reductase (FabI), a crucial enzyme in the fatty acid biosynthesis of P. falciparum. The CHCl(3) extract of Rhododendron ungernii leaves (IC(50) 10 microg[sol ]mL) and the H(2)O-soluble portion of Rhododendron smirnovii leaves (IC(50) 0.4 microg[sol ]mL) strongly inhibited the FabI enzyme. The preliminary data indicate that some (poly)phenolic compounds are responsible for the FabI inhibition potential of these extracts. The presented work reports for the first time the antiprotozoal activity of nine different genera as well as a target specific antimalarial screening for the identification of P. falciparum FabI inhibitors from medicinal plant extracts.
Assuntos
Antiprotozoários/farmacologia , Oxirredutases/antagonistas & inibidores , Fitoterapia , Extratos Vegetais/farmacologia , Plantas Medicinais , Plasmodium falciparum/efeitos dos fármacos , Animais , Antimaláricos/administração & dosagem , Antimaláricos/farmacologia , Antimaláricos/uso terapêutico , Antiprotozoários/administração & dosagem , Antiprotozoários/uso terapêutico , Enoil-(Proteína de Transporte de Acila) Redutase (NADH) , Humanos , Leishmania donovani/efeitos dos fármacos , Leishmaniose Visceral/tratamento farmacológico , Malária Falciparum/tratamento farmacológico , Medicina Tradicional , Testes de Sensibilidade Parasitária , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Folhas de Planta , Raízes de Plantas , Plasmodium falciparum/enzimologia , Trypanosoma/efeitos dos fármacos , Tripanossomíase/tratamento farmacológico , TurquiaRESUMO
From the aerial parts of Putoria calabrica, two new flavonol triglycosides were isolated and their structures were elucidated as quercetin-3-O-[alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranoside]-7-O-beta-D-glucopyranoside (1, calabricoside A) and quercetin-3-O-[4' "-O-caffeoyl-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranoside]-7-O-beta-D-glucopyranoside (2, calabricoside B). Additionally, seven iridoid and three lignan glycosides were isolated and characterized. Radical scavenging activities of all compounds were determined by quantifying their effects on luminol-enhanced chemiluminescence in formyl-methionyl-leucyl-phenylalanine (FMLP) stimulated human polymorphonuclear neutrophils (PMNs). Calabricoside A and B showed strong radical scavenging activity with IC(50) values of 0.25 and 0.3 microM, respectively.
Assuntos
Flavonoides/isolamento & purificação , Sequestradores de Radicais Livres/isolamento & purificação , Glucosídeos/isolamento & purificação , Lignanas/isolamento & purificação , Plantas Medicinais/química , Quercetina , Rubiaceae/química , Cromatografia , Ésteres/química , Flavonoides/química , Flavonoides/farmacologia , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacologia , Glucosídeos/química , Glucosídeos/farmacologia , Humanos , Lignanas/química , Lignanas/farmacologia , Medições Luminescentes , Estrutura Molecular , N-Formilmetionina Leucil-Fenilalanina/farmacologia , Neutrófilos/efeitos dos fármacos , Espectrofotometria Infravermelho , Relação Estrutura-Atividade , TurquiaRESUMO
Four new allose-containing triterpenoid saponosides, scabriosides A, B, C and D were isolated from the roots of Scabiosa rotata. Their structures were established as 3-O-beta-D-xylopyranosyl-28-O-[beta-D-allopyranosyl (1-->6)-beta-D-glucopyranosyl]-pomolic acid, 3-O-[alpha-L-rhamnopyranosyl (1-->2)-beta-D-xylopyranosyl]-28-O-[beta-D-allopyranosyl (1-->6)-beta-D-glucopyranosyl]-pomolic acid, 3-O-[alpha-L-rhamnopyranosyl (1-->2)-alpha-L-arabinopyranosyl]-28-O-[beta-D-allopyranosyl (1-->6)-beta-D-glucopyranosyl]-pomolic acid, and 3-O-[beta-D-glucopyranosyl (1-->3)-alpha-L-rhamnopyranosyl (1-->2)-beta-D-xylopyranosyl]-28-O-[beta-D-allopyranosyl(1-->6) -beta-D-glucopyranosyl]-pomolic acid, respectively, by the help of spectral evidence (IR, 1D- and 2D-NMR, FAB-MS).
Assuntos
Extratos Vegetais/química , Saponinas/química , Triterpenos/química , Configuração de Carboidratos , Sequência de Carboidratos , Glucose/análise , Modelos Moleculares , Dados de Sequência Molecular , Ressonância Magnética Nuclear Biomolecular , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação , TurquiaRESUMO
From the roots of Astragalus melanophrurius eight known saponins (1-8) were isolated. Based on spectral data (IR, 1H- and 13C-NMR, and FABMS), the structures were established as astrasieversianins II (1) and X (4), astragalosides I (2), II (3), IV (5) and VI (7), and cyclocanthosides E (6) and G (8). The isolates were evaluated in a broad range of bioassay systems and found to be inactive. Modest antibacterial activity was observed, however, as was immunomodulatory activity, as indicated by stimulation of isolated human lymphocytes.
Assuntos
Glicosídeos/isolamento & purificação , Raízes de Plantas/química , Adjuvantes Imunológicos/química , Adjuvantes Imunológicos/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Glicosídeos/química , Glicosídeos/farmacologia , Humanos , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Espectrometria de Massas de Bombardeamento Rápido de Átomos , Espectrofotometria Infravermelho , Células Tumorais CultivadasRESUMO
Two new phenylpropanoid glycosides, leonosides A and B, and two known glycosides lavandulifolioside and verbascoside, were isolated from the aerial parts of Leonurus glaucescens. On the basis of chemical and spectral evidence, leonosides A and B were shown to be beta-(3,4-dihydroxyphenyl)-ethyl-O-alpha-L-arabinopyranosyl-(1---- 2)-alpha-L- rhamnopyranosyl-(1----3)-4-O-feruloyl-beta-D-glucopyranoside and beta-(3-hydroxy, 4-methoxyphenyl)-ethyl-O-alpha-L-arabinopyranosyl-(1----2)- alpha-L-rhamnopyranosyl-(1----3)-4-O-feruloyl-beta-D-glucopyranosi de, respectively.