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Pesquisa : B01.650.940.800.575.912.250.456.500.303 [Categoria DeCS]
Referências encontradas : 30 [refinar]
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[PMID]:26879905
[Au] Autor:Forkuo AD; Ansah C; Boadu KM; Boampong JN; Ameyaw EO; Gyan BA; Arku AT; Ofori MF
[Ad] Endereço:Department of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, College of Health Sciences, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana. forkuoarnold@yahoo.com.
[Ti] Título:Synergistic anti-malarial action of cryptolepine and artemisinins.
[So] Source:Malar J;15:89, 2016 Feb 16.
[Is] ISSN:1475-2875
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Cryptolepine (CPE) is the major indoloquinoline isolated from the popular West African anti-malarial plant, Cryptolepis sanguinolenta. CPE possesses various pharmacological activities with potent anti-malarial activity against both chloroquine (CQ)-resistant and -sensitive strains. The search for safe and novel anti-malarial agents and combinations to delay resistance development to Plasmodium falciparum directed this work aimed at evaluating the anti-malarial interaction and safety of CPE in combination with some artemisinin derivatives. METHODS: The in vitro SYBR Green I, fluorescent-based, drug sensitivity assay using a fixed ratio method was carried out on the CQ-sensitive plasmodial strain 3D7 to develop isobolograms from three CPE-based combinations with some artemisinin derivatives. CPE and artesunate (ART) combinations were also evaluated using the Rane's test in ICR mice infected with Plasmodium berghei NK-65 strains in a fixed ratio combination (1:1) and fractions of their ED50s in order to determine the experimental ED50 (Zexp) of the co-administered compounds. Isobolograms were constructed to compare the Zexp to the Zadd. RESULTS: CPE exhibited promising synergistic interactions in vitro with ART, artemether and dihydroartemisinin. In vivo, CPE combination with ART again showed synergy as the Zexp was 1.02 ± 0.02, which was significantly less than the Zadd of 8.3 ± 0.31. The haematological, biochemical, organ/body weight ratio and histopathology indices in the rats treated with CPE at all doses (25, 50, 100 mg kg(-1) po) and in combination with ART (4 mg kg(-1)) showed no significant difference compared to the control group. CONCLUSION: The combination of CPE with the artemisinin derivatives were safe in the rodent model and showed a synergistic anti-malarial activity in vivo and in vitro. This study supports the basis for the selection of CPE as a prospective lead compound as the search for new anti-malarial combinations continues.
[Mh] Termos MeSH primário: Antimaláricos/uso terapêutico
Malária/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Antimaláricos/farmacologia
Artemisininas/farmacologia
Artemisininas/uso terapêutico
Cryptolepis/química
Sinergismo Farmacológico
Quimioterapia Combinada
Alcaloides de Indol/farmacologia
Alcaloides de Indol/uso terapêutico
Masculino
Camundongos
Camundongos Endogâmicos ICR
Plasmodium berghei/efeitos dos fármacos
Plasmodium berghei/fisiologia
Quinolinas/farmacologia
Quinolinas/uso terapêutico
Ratos
Ratos Sprague-Dawley
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antimalarials); 0 (Artemisinins); 0 (Indole Alkaloids); 0 (Quinolines); 480-26-2 (cryptolepine); 9RMU91N5K2 (artemisinine)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160217
[St] Status:MEDLINE
[do] DOI:10.1186/s12936-016-1137-5


  2 / 30 MEDLINE  
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[PMID]:26634775
[Au] Autor:Akinrinmade FJ; Akinrinde AS; Soyemi OO; Oyagbemi AA
[Ad] Endereço:a Department of Veterinary Surgery and Reproduction, Faculty of Veterinary Medicine, University of Ibadan , Ibadan , Nigeria.
[Ti] Título:Antioxidant Potential of the Methanol Extract of Parquetina nigrescens Mediates Protection Against Intestinal Ischemia-Reperfusion Injury in Rats.
[So] Source:J Diet Suppl;13(4):420-32, 2016.
[Is] ISSN:1939-022X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Parquetina nigrescens is a medicinal herb with recognized antioxidant properties and potential to alleviate conditions associated with oxidative stress, including gastric ulcers. We investigated the protective potential of methanol extract of Parquetina nigrescens (MEPN) against ischemia-reperfusion injury in the intestine of rats. Thirty (30) male Wistar albino rats were randomly assigned into five groups with Group I made up of control rats and Group II consisting of rats experimentally subjected to ischemia and reperfusion (IR) by clamping of the superior mesenteric artery (SMA) for 30 minutes and 45 minutes, respectively. Groups III and IV rats also had IR, but were initially pre-treated with MEPN at 500 mg/kg and 1000 mg/kg respectively, for seven days. Rats in Group V were also pre-treated with Vitamin C, for seven days, before induction of IR. The results showed marked reduction in intestinal epithelial lesions in groups treated with MEPN, compared to the IR group which had severe villi erosion, inflammatory cell infiltration and hemorrhages. There were significant increases in Malondialdehyde (MDA) and significant reductions in reduced glutathione (GSH) and Glutathione S-transferase (GST) activity with IR injury, while pre-treatment with either MEPN or Vitamin C prevented these effects. Increases in Glutathione peroxidase (GPX), Catalase (CAT) and Superoxide dismutase (SOD) with IR provided evidence for adaptive responses to oxidative injury during IR and preservation of enzyme activity by MEPN and Vitamin C. Taken together, Parquetina nigrescens provided considerable alleviation of intestinal injury produced by IR, at values much as effective as that offered by Vitamin C.
[Mh] Termos MeSH primário: Antioxidantes/farmacologia
Cryptolepis/química
Extratos Vegetais/farmacologia
Traumatismo por Reperfusão/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Ácido Ascórbico/farmacologia
Catalase/metabolismo
Modelos Animais de Doenças
Glutationa/metabolismo
Glutationa Peroxidase/metabolismo
Glutationa Transferase/metabolismo
Enteropatias/induzido quimicamente
Enteropatias/tratamento farmacológico
Masculino
Malondialdeído/metabolismo
Metanol/química
Estresse Oxidativo/efeitos dos fármacos
Ratos
Ratos Wistar
Espécies Reativas de Oxigênio/metabolismo
Superóxido Dismutase/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Plant Extracts); 0 (Reactive Oxygen Species); 4Y8F71G49Q (Malondialdehyde); EC 1.11.1.6 (Catalase); EC 1.11.1.9 (Glutathione Peroxidase); EC 1.15.1.1 (Superoxide Dismutase); EC 2.5.1.18 (Glutathione Transferase); GAN16C9B8O (Glutathione); PQ6CK8PD0R (Ascorbic Acid); Y4S76JWI15 (Methanol)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151205
[St] Status:MEDLINE
[do] DOI:10.3109/19390211.2015.1103828


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[PMID]:26178441
[Au] Autor:Saurí J; Bermel W; Buevich AV; Sherer EC; Joyce LA; Sharaf MH; Schiff PL; Parella T; Williamson RT; Martin GE
[Ad] Endereço:Process & Analytical Chemistry, Merck Research Laboratories, Mailstop: 800-D133, 126 E. Scott Ave, Rahway, NJ 07065 (USA).
[Ti] Título:Homodecoupled 1,1- and 1,n-ADEQUATE: Pivotal NMR Experiments for the Structure Revision of Cryptospirolepine.
[So] Source:Angew Chem Int Ed Engl;54(35):10160-4, 2015 Aug 24.
[Is] ISSN:1521-3773
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Cryptospirolepine is the most structurally complex alkaloid discovered and characterized thus far from any Cryptolepis specie. Characterization of several degradants of the original, sealed NMR sample a decade after the initial report called the validity of the originally proposed structure in question. We now report the development of improved, homodecoupled variants of the 1,1- and 1,n-ADEQUATE (HD-ADEQUATE) NMR experiments; utilization of these techniques was critical to successfully resolving long-standing structural questions associated with crytospirolepine.
[Mh] Termos MeSH primário: Alcaloides/química
Cryptolepis/química
Espectroscopia de Ressonância Magnética/métodos
Extratos Vegetais/química
[Mh] Termos MeSH secundário: Alcaloides de Indol/química
Estrutura Molecular
Quinolinas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Alkaloids); 0 (Indole Alkaloids); 0 (Plant Extracts); 0 (Quinolines); 0 (cryptospirolepine)
[Em] Mês de entrada:1605
[Cu] Atualização por classe:150820
[Lr] Data última revisão:
150820
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150717
[St] Status:MEDLINE
[do] DOI:10.1002/anie.201502540


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[PMID]:25725608
[Au] Autor:Figueiras M; Coelho L; Wicht KJ; Santos SA; Lavrado J; Gut J; Rosenthal PJ; Nogueira F; Egan TJ; Moreira R; Paulo A
[Ad] Endereço:Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003 Lisboa, Portugal.
[Ti] Título:N10,N11-di-alkylamine indolo[3,2-b]quinolines as hemozoin inhibitors: design, synthesis and antiplasmodial activity.
[So] Source:Bioorg Med Chem;23(7):1530-9, 2015 Apr 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:We recently reported that potent N10,O11-bis-alkylamine indolo[3,2-b]quinoline antimalarials act as hemozoin (Hz) growth inhibitors. To improve access and binding to the target we have now designed novel N10,N11-di-alkylamine bioisosteres. 3-Chloro derivatives (10a-f) showed selectivity for malaria parasite compared to human cells, high activity against Plasmodium falciparum chloroquine (CQ)-resistant strain W2 (IC50s between 20 and 158nM), good correlation with ß-hematin inhibition and improved vacuolar accumulation ratios, thus suggesting inhibition of Hz growth as one possible mechanism of action for these compounds. Moreover, our studies show that Hz is a valid target for the development of new antimalarials able to overcome CQ resistance.
[Mh] Termos MeSH primário: Antimaláricos/síntese química
Desenho de Drogas
Hemeproteínas/antagonistas & inibidores
Plasmodium falciparum/efeitos dos fármacos
Quinolinas/síntese química
[Mh] Termos MeSH secundário: Antimaláricos/farmacologia
Cryptolepis
Hemeproteínas/metabolismo
Seres Humanos
Quinolinas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antimalarials); 0 (Hemeproteins); 0 (Quinolines); 39404-00-7 (hemozoin)
[Em] Mês de entrada:1601
[Cu] Atualização por classe:150317
[Lr] Data última revisão:
150317
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150302
[St] Status:MEDLINE


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[PMID]:25247198
[Au] Autor:Hanprasertpong N; Teekachunhatean S; Chaiwongsa R; Ongchai S; Kunanusorn P; Sangdee C; Panthong A; Bunteang S; Nathasaen N; Reutrakul V
[Ad] Endereço:Department of Pharmacology and Center of Excellence for Innovation in Chemistry, Faculty of Medicine, Chiang Mai University, Indhawaroros Road, Chiang Mai 50200, Thailand.
[Ti] Título:Analgesic, anti-inflammatory, and chondroprotective activities of Cryptolepis buchanani extract: in vitro and in vivo studies.
[So] Source:Biomed Res Int;2014:978582, 2014.
[Is] ISSN:2314-6141
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Cryptolepis buchanani Roem. & Schult. is widely used in folk medicine in Southeast Asia for treating muscle tension and arthritis. This study aimed to investigate an analgesic activity of the methanol extract of C. buchanani (CBE) in acetic acid-induced writhing response in mice, and to examine its anti-inflammatory activity in ethyl phenylpropiolate- (EPP-) induced ear edema and carrageenan-induced paw edema in rats. Its effects on cartilage degradation induced by interleukin-1ß (IL-1ß) in porcine cartilage explant culture were also determined. This study demonstrated that CBE significantly reduced acetic acid-induced writhing response. It also inhibited edema formation in both EPP-induced ear edema and carrageenan-induced paw edema models. In cartilage explant culture, CBE significantly reduced the sulfated glycosaminoglycan and hyaluronan released into culture media while it reserved the uronic acid and collagen within the cartilage tissues. It also suppressed the matrix metalloproteinase-2 activity with no effect on cell viability. In conclusion, CBE shows analgesic, anti-inflammatory, and chondroprotective effects in this preliminary study. Therefore, CBE may be useful as an alternative treatment for osteoarthritis.
[Mh] Termos MeSH primário: Analgésicos/farmacologia
Anti-Inflamatórios/farmacologia
Condrócitos/efeitos dos fármacos
Cryptolepis/química
Inflamação/tratamento farmacológico
Dor/tratamento farmacológico
Extratos Vegetais/farmacologia
[Mh] Termos MeSH secundário: Animais
Células Cultivadas
Citoproteção/efeitos dos fármacos
Citoproteção/fisiologia
Inflamação/diagnóstico
Masculino
Camundongos
Dor/diagnóstico
Ratos
Ratos Sprague-Dawley
Suínos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Analgesics); 0 (Anti-Inflammatory Agents); 0 (Plant Extracts)
[Em] Mês de entrada:1506
[Cu] Atualização por classe:151029
[Lr] Data última revisão:
151029
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140924
[St] Status:MEDLINE
[do] DOI:10.1155/2014/978582


  6 / 30 MEDLINE  
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[PMID]:24391229
[Au] Autor:Ansah C; Mensah KB
[Ad] Endereço:Department of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, College of Health Sciences, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana.
[Ti] Título:A review of the anticancer potential of the antimalarial herbal cryptolepis sanguinolenta and its major alkaloid cryptolepine.
[So] Source:Ghana Med J;47(3):137-47, 2013 Sep.
[Is] ISSN:0016-9560
[Cp] País de publicação:Ghana
[La] Idioma:eng
[Ab] Resumo:Cryptolepis sanguinolenta (Lindl.) Schltr (Periplocaceae), has a longstanding traditional use in the treatment of malaria in the West African region. Recent evidence suggests that the aqueous extract from the roots and the major alkaloid from the plant, cryptolepine, have prospects as cancer chemotherapeutic agents on account of their potent cytotoxicity to mammalian cells. Several mechanisms have been proposed to explain the cytotoxic activities of the agents. However, emerging evidence from their anti-inflammatory actions suggest that the mechanism of the cytotoxicity may be closely related to its anti-inflammatory activity. This review looks at the mechanisms of cryptolepis-induced cytotoxicity, its link with inflammation and its potential as anticancer agent. The elucidation of these interwoven mechanisms may be useful in the development of cryptolepine or other analogues as new anticancer agents.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/uso terapêutico
Neoplasias da Mama/tratamento farmacológico
Cryptolepis
Alcaloides de Indol/uso terapêutico
Fitoterapia
Neoplasias da Próstata/tratamento farmacológico
Quinolinas/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Antimaláricos/uso terapêutico
Antineoplásicos Fitogênicos/efeitos adversos
Feminino
Seres Humanos
Alcaloides de Indol/efeitos adversos
Inflamação/tratamento farmacológico
Masculino
NF-kappa B/antagonistas & inibidores
Preparações de Plantas/efeitos adversos
Preparações de Plantas/uso terapêutico
Quinolinas/efeitos adversos
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antimalarials); 0 (Antineoplastic Agents, Phytogenic); 0 (Indole Alkaloids); 0 (NF-kappa B); 0 (Plant Preparations); 0 (Quinolines); 480-26-2 (cryptolepine)
[Em] Mês de entrada:1409
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140107
[St] Status:MEDLINE


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[PMID]:23507189
[Au] Autor:Olajide OA; Bhatia HS; de Oliveira AC; Wright CW; Fiebich BL
[Ad] Endereço:Pharmacy and Pharmaceutical Sciences, School of Applied Sciences, University of Huddersfield, Huddersfield, West Yorkshire HD1 3DH, United Kingdom. o.a.olajide@hud.ac.uk
[Ti] Título:Anti-neuroinflammatory properties of synthetic cryptolepine in human neuroblastoma cells: possible involvement of NF-κB and p38 MAPK inhibition.
[So] Source:Eur J Med Chem;63:333-9, 2013 May.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Cryptolepis sanguinolenta and its bioactive alkaloid, cryptolepine have shown anti-inflammatory activity. However, the underlying mechanism of anti-inflammatory action in neuronal cells has not been investigated. In the present study we evaluated an extract of C. sanguinolenta (CSE) and cryptolepine (CAS) on neuroinflammation induced with IL-1ß in SK-N-SH neuroblastoma cells. We then attempted to elucidate the mechanisms underlying the anti-neuroinflammatory effects of CAS in SK-N-SH cells. Cells were stimulated with 10 U/ml of IL-1ß in the presence or absence of different concentrations of CSE (25-200 µg/ml) and CAS (2.5-20 µM). After 24 h incubation, culture media were collected to measure the production of PGE2 and the pro-inflammatory cytokines (TNFα and IL-6). Protein and gene expressions of cyclooxygenase (COX-2) and microsomal prostaglandin synthase-1 (mPGES-1) were studied by immunoblotting and qPCR, respectively. CSE produced significant (p < 0.05) inhibition of TNFα, IL-6 and PGE2 production in SK-N-SH cells. Studies on CAS showed significant and dose-dependent inhibition of TNFα, IL-6 and PGE2 production in IL-1ß-stimulated cells without affecting viability. Pre-treatment with CAS (10 and 20 µM) was also found to inhibit IL-1ß-induced protein and gene expressions of COX-2 and mPGES-1. Further studies to determine the mechanism of action of CAS showed inhibition of NF-κBp65 nuclear translocation, but not IκB phosphorylation. At 10 and 20 µM, CAS inhibited IL-1ß-induced phosphorylation of p38 MAPK. Studies on the downstream substrate of p38, MAPK-activated protein kinase 2 (MAPKAPK2) showed that CAS produced significant (p < 0.05) and dose dependent inhibition of MAPKAPK2 phosphorylation in IL-1ß-stimulated SK-N-SH cells. This study clearly shows that cryptolepine (CAS) inhibits neuroinflammation through mechanisms involving inhibition of COX-2 and mPGES-1. It is suggested that these actions are probably mediated through NF-κB and p38 signalling.
[Mh] Termos MeSH primário: Anti-Inflamatórios/farmacologia
Alcaloides de Indol/farmacologia
Quinolinas/farmacologia
Fator de Transcrição RelA/metabolismo
Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
[Mh] Termos MeSH secundário: Transporte Ativo do Núcleo Celular/efeitos dos fármacos
Anti-Inflamatórios/síntese química
Anti-Inflamatórios/química
Linhagem Celular Tumoral
Cryptolepis/química
Ciclo-Oxigenase 2/genética
Ciclo-Oxigenase 2/metabolismo
Citocinas/metabolismo
Dinoprostona/metabolismo
Relação Dose-Resposta a Droga
Regulação Enzimológica da Expressão Gênica/efeitos dos fármacos
Seres Humanos
Immunoblotting
Alcaloides de Indol/síntese química
Alcaloides de Indol/química
Interleucina-1beta/farmacologia
Oxirredutases Intramoleculares/genética
Oxirredutases Intramoleculares/metabolismo
Estrutura Molecular
Neuroblastoma/genética
Neuroblastoma/metabolismo
Neuroblastoma/patologia
Fosforilação/efeitos dos fármacos
Extratos Vegetais/química
Extratos Vegetais/farmacologia
Prostaglandina-E Sintases
Quinolinas/síntese química
Quinolinas/química
Reação em Cadeia da Polimerase Via Transcriptase Reversa
Transdução de Sinais/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Cytokines); 0 (Indole Alkaloids); 0 (Interleukin-1beta); 0 (Plant Extracts); 0 (Quinolines); 0 (Transcription Factor RelA); 480-26-2 (cryptolepine); EC 1.14.99.1 (Cyclooxygenase 2); EC 1.14.99.1 (PTGS2 protein, human); EC 2.7.11.24 (p38 Mitogen-Activated Protein Kinases); EC 5.3.- (Intramolecular Oxidoreductases); EC 5.3.99.3 (PTGES protein, human); EC 5.3.99.3 (Prostaglandin-E Synthases); K7Q1JQR04M (Dinoprostone)
[Em] Mês de entrada:1311
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130320
[St] Status:MEDLINE


  8 / 30 MEDLINE  
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[PMID]:22975492
[Au] Autor:Jaromin A; Korycinska M; Pietka-Ottlik M; Musial W; Peczynska-Czoch W; Kaczmarek L; Kozubek A
[Ad] Endereço:Department of Lipids and Liposomes, Faculty of Biotechnology, University of Wroclaw, Wroclaw, Poland. ajaromin@ibmb.uni.wroc.pl
[Ti] Título:Membrane perturbations induced by new analogs of neocryptolepine.
[So] Source:Biol Pharm Bull;35(9):1432-9, 2012.
[Is] ISSN:1347-5215
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Indoloquinoline alkaloids represent an important class of antimalarial, antibacterial and antiviral compounds. Indolo[2,3-b]quinolines are a family of DNA intercalators and inhibitors of topoisomerase II, synthetic analogs of neocryptolepine, an alkaloid traditionally used in African folk medicine. These cytotoxic substances are promising anticancer agents. Active representatives of indolo[2,3-b]quinolines affect model and natural membranes. The distinct structure and hydrophobicity of the compounds leads to marked differences in the disturbing effects on membrane organization and function. Our results also indicated a strong relationship between the presence of the chain and the Poct of the molecule as well as the capacity for incorporation into carboxyfluorescein-trapped liposomes in the 0.02-0.06 mM range. Moreover, a correlation between binding to neutral dimyristoylphosphatidylcholine (DMPC) or negative charged dimyristoylphosphatidylcholine:dimyristoylphosphatidylglycerol (DMPC:DMPG, 9:1 w/w) liposomes, as well as to erythrocyte ghosts and pKa, was also found. All the compounds cause hemolysis in isotonic conditions with concentration causing 50% hemolysis (HC50) in the 0.12-0.88 mM range. The concentration-dependent inhibitory effect of the tested agents on erythrocyte ghosts' acetylcholinesterase activity was also studied.
[Mh] Termos MeSH primário: Alcaloides/farmacologia
Antineoplásicos Fitogênicos/farmacologia
Membrana Celular/efeitos dos fármacos
Cryptolepis/química
Eritrócitos/efeitos dos fármacos
Hemólise/efeitos dos fármacos
Extratos Vegetais/farmacologia
Quinolinas/farmacologia
[Mh] Termos MeSH secundário: Acetilcolinesterase/metabolismo
Alcaloides/química
Animais
Antineoplásicos Fitogênicos/química
Membrana Celular/metabolismo
Dimiristoilfosfatidilcolina/química
Relação Dose-Resposta a Droga
Eritrócitos/metabolismo
Interações Hidrofóbicas e Hidrofílicas
Substâncias Intercalantes/química
Substâncias Intercalantes/farmacologia
Lipossomos
Medicina Tradicional Africana
Fosfatidilgliceróis/química
Extratos Vegetais/química
Quinolinas/química
Ovinos
Relação Estrutura-Atividade
Inibidores da Topoisomerase II/química
Inibidores da Topoisomerase II/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkaloids); 0 (Antineoplastic Agents, Phytogenic); 0 (Intercalating Agents); 0 (Liposomes); 0 (Phosphatidylglycerols); 0 (Plant Extracts); 0 (Quinolines); 0 (Topoisomerase II Inhibitors); 0 (neocryptolepine); BI71WT9P3R (dimyristoylphosphatidylglycerol); EC 3.1.1.7 (Acetylcholinesterase); U86ZGC74V5 (Dimyristoylphosphatidylcholine)
[Em] Mês de entrada:1301
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120915
[St] Status:MEDLINE


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[PMID]:22709723
[Au] Autor:Mills-Robertson FC; Tay SC; Duker-Eshun G; Walana W; Badu K
[Ad] Endereço:Department of Microbiology, Centre for Scientific Research into Plant Medicine, Mampong-Akwapim, Ghana.
[Ti] Título:In vitro antimicrobial activity of ethanolic fractions of Cryptolepis sanguinolenta.
[So] Source:Ann Clin Microbiol Antimicrob;11:16, 2012 Jun 18.
[Is] ISSN:1476-0711
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Following claims that some plants have antimicrobial activities against infectious microbes, the in vitro antimicrobial activities of different solvent fractions of ethanolic extract of Cryptolepis sanguinolenta were evaluated against eight standard bacteria and clinical isolates. METHODS: The solvent partitioning protocol involving ethanol, petroleum ether, chloroform, ethyl acetate and water, was used to extract various fractions of dried pulverized Cryptolepis sanguinolenta roots. Qualitative phyto-constituents screening was performed on the ethanol extract, chloroform fraction and the water fraction. The Kirby Bauer disk diffusion method was employed to ascertain the antibiogram of the test organisms while the agar diffusion method was used to investigate the antimicrobial properties of the crude plant extracts. The microplate dilution method aided in finding the MICs while the MBCs were obtained by the method of Nester and friends. The SPSS 16.0 version was used to analyze the percentages of inhibitions and bactericidal activities. RESULTS: The phytochemical screening revealed the presence of alkaloids, reducing sugars, polyuronides, anthocyanosides and triterpenes. The ethanol extract inhibited 5 out of 8 (62.5%) of the standard organisms and 6 out of 8 (75%) clinical isolates. The petroleum ether fraction inhibited 4 out of 8 (50%) of the standard microbes and 1 out of 8 (12.5%) clinical isolates. It was also observed that the chloroform fraction inhibited the growth of all the organisms (100%). Average inhibition zones of 14.0 ± 1.0 mm to 24.67 ± 0.58 mm was seen in the ethyl acetate fraction which halted the growth of 3 (37.5%) of the standard organisms. Inhibition of 7 (87.5%) of standard strains and 6 (75%) of clinical isolates were observed in the water fraction. The chloroform fraction exhibited bactericidal activity against all the test organisms while the remaining fractions showed varying degrees of bacteriostatic activity. CONCLUSION: The study confirmed that fractions of Cryptolepis sanguinolenta have antimicrobial activity. The chloroform fraction had the highest activity, followed by water, ethanol, petroleum ether and ethyl acetate respectively. Only the chloroform fraction exhibited bactericidal activity and further investigations are needed to ascertain its safety and prospects of drug development.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Bactérias/efeitos dos fármacos
Cryptolepis/química
Extratos Vegetais/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/química
Antibacterianos/isolamento & purificação
Bactérias/genética
Bactérias/isolamento & purificação
Infecções Bacterianas/microbiologia
Seres Humanos
Testes de Sensibilidade Microbiana
Extratos Vegetais/química
Extratos Vegetais/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Plant Extracts)
[Em] Mês de entrada:1301
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120620
[St] Status:MEDLINE
[do] DOI:10.1186/1476-0711-11-16


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[PMID]:22338119
[Au] Autor:El Bardicy S; El Sayed I; Yousif F; Van der Veken P; Haemers A; Augustyns K; Pieters L
[Ad] Endereço:Department of Medical Malacology and Schistosome Biological Supply Centre, Theodor Bilharz Research Institute, Imbaba, Egypt. samiaelbardicy21@yahoo.com
[Ti] Título:Schistosomicidal and molluscicidal activities of aminoalkylamino substituted neo- and norneocryptolepine derivatives.
[So] Source:Pharm Biol;50(2):134-40, 2012 Feb.
[Is] ISSN:1744-5116
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:CONTEXT: The cryptolepines originate from the roots of the climbing shrub Cryptolepis sanguinolenta (Lindi) Schitr(Periplocaeae) which is used in Central and West Africa in traditional medicine for the treatment of malaria. OBJECTIVES: Evaluation for the first time of a series of chloro- and aminoalkylamino derivatives of neo- and norneocryptolepines for potential schistosomicidal and molluscicidal activities. MATERIALS AND METHODS: A series of chloro- and aminoalkylamino substituted neo- and norneocryptolepine derivatives were synthesized. They were tested in vitro against viable Schistosoma mansoni Sambon mature worms in culturemedium with fetal serum and antibiotics and in dechlorinated water against the snail vector Biomphalaria alexandrina Ehrenberg. Active compounds were further subjected to determination of their IC50 values. RESULTS: Results showed that six neocryptolepine and two norneocryptolepine derivatives had in vitro schistosomicidal activity on Egyptian and Puerto Rican strains of S. mansoni. The most effective derivative (2-chloro-5-methyl-N-(2-morpholin-4-ethyl)-5H-indolo[2,3b]quinoline-11-amine) has IC50 and IC90 1.26 and 4.05 µM and 3.54 and 6.83 µM with the Egyptian and Puerto Rican strains of Schistosoma, respectively. All eight derivatives showed molluscicidal activity against the vector snail B. alexandrina. The most active compound (2-chloro-11-(4-methylpiperazin-1-yl)-6H-indolo[2,3-b] quinoline) has LC50 0.6 and LC90 3.9 ppm after 24 h. DISCUSSION AND CONCLUSIONS: The findings demonstrate that introducing chloro- and aminoalkylamino side chain initiated both schistosomicidal and molluscicidal activities in these derivatives. The structure­activity relationship of this series of compounds is discussed.
[Mh] Termos MeSH primário: Alcaloides/farmacologia
Moluscocidas/farmacologia
Quinolinas/farmacologia
Esquistossomicidas/farmacologia
[Mh] Termos MeSH secundário: Alcaloides/administração & dosagem
Alcaloides/síntese química
Animais
Biomphalaria/efeitos dos fármacos
Cryptolepis/química
Egito
Concentração Inibidora 50
Dose Letal Mediana
Medicina Tradicional Africana
Moluscocidas/administração & dosagem
Moluscocidas/síntese química
Porto Rico
Quinolinas/administração & dosagem
Quinolinas/síntese química
Schistosoma mansoni/efeitos dos fármacos
Esquistossomicidas/administração & dosagem
Esquistossomicidas/síntese química
Relação Estrutura-Atividade
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkaloids); 0 (Molluscacides); 0 (Quinolines); 0 (Schistosomicides); 0 (neocryptolepine)
[Em] Mês de entrada:1205
[Cu] Atualização por classe:120215
[Lr] Data última revisão:
120215
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120217
[St] Status:MEDLINE



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