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1.
Fitoterapia ; 81(8): 1113-6, 2010 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-20627119

RESUMO

We investigated the in vitro effect of dibenzyl trisulfide (DTS), a secondary metabolite of Petiveria alliacea, on erythrocyte elasticity, relaxation time and membrane morphology. Blood samples from 8 volunteers with hemoglobin AA were exposed to 100, 200, 400, 800 and 1000 ng/ml of DTS respectively and the elasticity and relaxation time measured. There were statistically significant, dose-dependent increases in elasticity and relaxation times. The changes in membrane morphology observed also increased with increased concentration of DTS. This suggests that DTS interaction with membrane protein resulted in increased elasticity, relaxation time and deformation of the erythrocyte membrane.


Assuntos
Compostos de Benzil/química , Compostos de Benzil/farmacologia , Membrana Eritrocítica/efeitos dos fármacos , Phytolaccaceae/química , Phytolaccaceae/metabolismo , Sulfetos/química , Sulfetos/farmacologia , Feminino , Humanos , Masculino , Estrutura Molecular
3.
West Indian Med J ; 58(5): 407-9, 2009 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-20441056

RESUMO

Studies conducted on the secondary metabolite (natural product), dibenzyl trisulphide (DTS), which was isolated from the sub-tropical shrub Petiveria alliacea (guinea hen weed, anamu) [Phytolaccaceae] have shown tremendous pharmaceutical promise as a drug prototype. This is now reflected in the development of the broad spectrum anti-cancer molecule, fluorapacin (bis(4-fluorobenzyl) trisulphide) which has an excellent safety profile. The mode of action elucidated for DTS is the mitogen activated protein extracellular regulated kinases 1 and 2 (MAPKinases ERK 1 and ERK 2). The MAPKinase signal transduction biochemical pathways are important in the regulation of a wide range of cellular processes which are important in disease establishment. These processes include: cancer cell proliferation, nerve repair, memory enhancement, autoimmune diseases, which are linked to thymic cell involution and bone marrow functions, cerebrovascular and cardiovascular diseases. In addition to the MAPkinase signal transduction mode of action, DTS also prevents the denaturation of serum albumin which is a feature of nonsteroidal anti-inflammatory drugs, thus supporting the molecule's possible role in the treatment of inflammatory ageing diseases.


Assuntos
Compostos de Benzil/farmacologia , Desenho de Fármacos , MAP Quinases Reguladas por Sinal Extracelular/efeitos dos fármacos , Fluorbenzenos/farmacologia , Phytolaccaceae , Transdução de Sinais/efeitos dos fármacos , Sulfetos/farmacologia , Diferenciação Celular/efeitos dos fármacos , Proliferação de Células/efeitos da radiação , Humanos , Células-Tronco Mesenquimais/efeitos dos fármacos , Degeneração Neural/tratamento farmacológico , Extratos Vegetais/farmacologia
4.
West Indian Med J ; 58(2): 181-2, 2009 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-21866606

RESUMO

The present article reports on the comparative cost of using the Bovine Serum Albumin as an assay for detecting natural products with anti-inflammatory activities relative to the use of animals. This is an addendum to the West Indian Medical Journal article; 2008; 57(4); 327-31.


Assuntos
Bioensaio , Soroalbumina Bovina/análise , Alternativas aos Testes com Animais/economia , Animais , Bioensaio/economia , Ratos , Ratos Sprague-Dawley
5.
West Indian Med J ; 57(4): 327-31, 2008 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-19566010

RESUMO

There are emerging ethical issues with regards to the use of animals in the early stages of drug discovery for anti-inflammatory and degenerative diseases from natural products using the activity-directed isolation pathways when many compounds (eg > 100) are present in the crude extract or fraction and are to be tested The above-mentioned is the main reason for proposing the use of the in vitro anti-denaturation (stabilization) effects of heat treated (immunogenic) bovine serum albumin (BSA) as an assay. Current methods used for detecting and isolating a wide range of anti-inflammatory compounds in the early stages of the drug discovery process utilize a large number of animals. When BSA is heated and is undergoing denaturation, it expresses antigens associated to Type III hypersensitive reaction and which are related to diseases such as serum sickness, glomerulonephritis, rheumatoid arthritis and systemic lupus erythematosus. Thus, the assay that is being proposed should be applicable to the discovery of drugs for treating the above mentioned diseases and others, once the compounds stabilize the denaturation process.


Assuntos
Anti-Inflamatórios/sangue , Preparações de Plantas/farmacologia , Desnaturação Proteica/efeitos dos fármacos , Soroalbumina Bovina/análise , Animais , Bioensaio , Bovinos , Descoberta de Drogas , Temperatura Alta/efeitos adversos , Doenças do Sistema Imunitário/tratamento farmacológico , Técnicas In Vitro , Programas de Rastreamento
6.
West Indian med. j ; 56(6): 487-490, Dec. 2007. tab
Artigo em Inglês | LILACS | ID: lil-507260

RESUMO

Mixed lymphocyte responses assays were conducted at 25.0 and 250.0 microg/mL of the crude ethanolic extract of Boehmeria jamaicensis Urb (coded as BJE) using peripheral lymphocytes obtained from individuals suffering from the common cold after four days of infection and from healthy individuals (without the common cold infection). At a concentration of 25 ug/mL, gamma interferon (IFN-gamma) was increased by 24.03 fold and interleukin 4 (IL-4) by 1.71 fold for the cells obtained from individuals with the common cold (Group A). The extract suppressed IFN-gamma by 8.3% while IL-4 was stimulated by 9.90 fold from peripheral lymphocytes obtained from healthy individuals (Group B). Gamma interferon was suppressed at 250 microg/mL while IL-4 was elevated by 1.86 fold for cells obtained from individuals suffering from the common cold (Group A). In conclusion, BJE could have implications for the treatment of the common cold.


Ensayos de reacci¨®n linfocitaria mixta fueron realizados a 25.0 y 250.0 ¦Ìg/mL de extracto etan¨®lico crudo de Boehmeria jamaicensis Urb (codificado como BJE), usando linfocitos perif¨¦ricos obtenidos de individuos con catarro com¨²n luego de cuatro d¨ªas de infecci¨®n, y de individuos sanos (sin la infecci¨®n del catarro com¨²n). Se hall¨® que el interfer¨®n-gamma (IFN-¦Ã) aument¨® en 24.03 veces, y la interleucina 4 (IL-4) en 1.71 veces para las c¨¦lulas obtenidas de individuos con catarro com¨²n, a 25¦Ìg/mL. El extracto inhibi¨® IFN-¦Ã en un 8.3 % en tanto que el IL-4 fue estimulado en 9.90 veces a partirde los linfocitos perif¨¦ricos obtenidos de individuos sanos. El gamma-interfer¨®n fue inhibido a 250 ¦Ìg/mL, mientras que la IL-4 se elev¨® en 1.86 veces para las c¨¦lulas obtenidas de individuos que sufren de catarro com¨²n.


Assuntos
Humanos , Boehmeria , Fitoterapia/métodos , Interferon gama/imunologia , /imunologia , Resfriado Comum/imunologia , Resfriado Comum/terapia , Sinusite/imunologia , Sinusite/terapia , Sinusite/microbiologia
7.
West Indian Med J ; 56(1): 5-10, 2007 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-17621837

RESUMO

Epingaione (4-Methyl-1-(5-methyl-2, 3,4,5-tetrahydro-[2,3']bifuranyl-5-yl)-pentan-2-one) was isolated as one of the major lipophilic secondary metabolites from the leaves and stems of Bontia daphnoides L. The compound gave 79.24% and 50.83% anti-proliferation/cytotoxic activity on the human SH-SY5Y neuroblastoma and TE-671 sarcoma cells in vitro at 50 pg/mL, respectively. Epingaione was transformed into eleven derivatives under laboratory conditions using ethanol, some gave greater anti-proliferation/cytotoxic activity on the cancer cell lines tested. One of the derivatives (compound 2) with enhanced cytotoxic activity was elucidated as 5'-Ethoxy-5-methyl-5-(4-methyl-2-oxo-pentyl)-2,3,4,5-tetrahydro-5'H-[2,3']bifuranyl-2'-one. Both epingaione and compound 2 caused an accumulation of arrested or dead SH-SY5Y neuroblastoma in the m-phase of the cell cycle as revealed by the m-phase specific marker KE 67.


Assuntos
Furanos/farmacologia , Myoporaceae , Neuroblastoma/tratamento farmacológico , Pentanonas/farmacologia , Fitoterapia , Sarcoma/tratamento farmacológico , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular , Ensaios de Seleção de Medicamentos Antitumorais , Furanos/química , Humanos , Pentanonas/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta , Caules de Planta
8.
West Indian Med J ; 56(1): 17-21, 2007 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-17621839

RESUMO

The data compiled in the present review on dibenzyl trisulphide (DTS) isolated from Petiveria alliacea L (the guinea hen weed or anamu) revealed that the compound and its derivatives could be of tremendous pharmaceutical interest. The mode of action elucidated for DTS revealed that it is a mitogen activated protein extracellular regulated kinases 1 and 2 (MAPKinases erk1 and erk 2) signal transduction molecule. Dibenzyl trisulphide caused hyper-phosphorylation of growth factor induced MAPKinases (erk 1 and erk 2) phosphorylation, a process critical for the improvement of long term memory, and is implicated in neuronal growth. Dibenzyl trisulphide and its derivatives exhibited potent anti-proliferation/cytotoxic activity on a wide range of cancer cell lines. The cytotoxic activity of DTS was increased by 70-1000 fold when bound to albumin in vitro. Dibenzyl trisulphide seems to have a cytokine switching mechanism in which it down regulates cytokines from the Type I helper cells (Th -1 cell) pathway which contained several pro-inflammatory cytokines and up-regulates those on the Type 2 helper cells (Th-2) pathway. The trisulphide up-regulates some reticuloendothelial system parameters eg granulocyte counts and increased thymic and Peyer's patches masses via cell proliferation processes which are known to be regulated via the MAPKinase signal transduction pathway. When the zygotes ofAsternia pectinifera (Starfish) were exposed to DTS at concentration of 10 mM, a dose lethal to all cancer cells tested, it was observed that the sensitive process of protein biosynthesis was not affected Similarly, the proliferation of the HOFA human fibroblast, a noncancerous cell line, was not severely affected by DTS at 8.9 microM over seven days, a concentration also lethal to most cancer cell lines tested The implications of the findings will be highlighted in the present review.


Assuntos
Compostos de Benzil/uso terapêutico , Fitoterapia , Extratos Vegetais , Sulfetos/uso terapêutico , Antígenos CD/fisiologia , Compostos de Benzil/farmacologia , Caderinas/fisiologia , Humanos , Transdução de Sinais/efeitos dos fármacos , Sulfetos/farmacologia , Regulação para Cima/fisiologia
9.
West Indian Med J ; 56(6): 487-90, 2007 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-18646490

RESUMO

Mixed lymphocyte responses assays were conducted at 25.0 and 250.0 microg/mL of the crude ethanolic extract of Boehmeria jamaicensis Urb (coded as BJE) using peripheral lymphocytes obtained from individuals suffering from the common cold after four days of infection and from healthy individuals (without the common cold infection). At a concentration of 25 ug/mL, gamma interferon (IFN-gamma) was increased by 24.03 fold and interleukin 4 (IL-4) by 1.71 fold for the cells obtained from individuals with the common cold (Group A). The extract suppressed IFN-gamma by 8.3% while IL-4 was stimulated by 9.90 fold from peripheral lymphocytes obtained from healthy individuals (Group B). Gamma interferon was suppressed at 250 microg/mL while IL-4 was elevated by 1.86 fold for cells obtained from individuals suffering from the common cold (Group A). In conclusion, BJE could have implications for the treatment of the common cold.


Assuntos
Infecções Bacterianas/imunologia , Infecções Bacterianas/terapia , Boehmeria , Resfriado Comum/imunologia , Resfriado Comum/terapia , Interferon gama/imunologia , Interleucina-4/imunologia , Fitoterapia/métodos , Sinusite/imunologia , Sinusite/terapia , Infecções Bacterianas/complicações , Humanos , Sinusite/microbiologia
10.
West Indian Med J ; 55(4): 215-6, 2006 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-17249307
11.
West Indian Med J ; 53(4): 208-19, 2004 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-15622673

RESUMO

Sixty natural products belonging to the following structural classes: artemisinins, coumarins, flavonoids, tannins, tetrahydroberberine alkaloids, tetracyclic triterpenes, tetranortriterpenoids and polysulphides were screened against the human SH-SY5Y neuroblastoma cell line revealing differences in their effects on cell morphology and in anti-proliferation/cytotoxic activity. Based on the data obtained, dibenzyl trisulphide is the most effective anti-proliferative/cytotoxic compound. In addition, we hereby propose the human SH-SY5Y cell line as a sensitive and uncomplicated in vitro test system for detecting compounds with potential anti-proliferation/cytotoxic activity.


Assuntos
Antineoplásicos/farmacologia , Compostos de Benzil/farmacologia , Neuroblastoma/patologia , Extratos Vegetais/farmacologia , Sulfetos/farmacologia , Divisão Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Extratos Vegetais/química
12.
Naturwissenschaften ; 90(10): 468-72, 2003 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-14564407

RESUMO

Electron micrograph examination of the leaf and stem surfaces of Cleome viscosa L (Family Capparaceae) revealed the presence of secretory glandular trichomes with club-cylinder and cylinder morphologies. In the present study, the leaves and stems of C. viscosa were extracted with hexane and the extract was evaluated for the following biological activities: anti-bacterial, anti-fungal, contact insecticidal and nematicidal. The extract was found to be a potent anti-bacterial agent according to the thin layer chromatography autobiographic assay. Activity-directed isolation studies of the anti-bacterially active compounds led to a 14-member ring cembranoid diterpene being identified as one of the effective agents. Minimum inhibitory concentration (MIC) values (microg/spot) of 5.0 microg/spot and 1.0 microg/spot were found for the diterpene on Bacillus subtilis (Gram-positive) and Pseudomonas fluorescens (Gram-negative), respectively. The diterpene did not inhibit the growth of the fungus Cladosporium cucumerinum. The extract demonstrated a pyrethroid type of contact insecticidal activity on adult Cylas formicarius elegantulus Summer (Coleoptera: Curculionidae). The extract also had high nematicidal activity with a percentage Abbott's value of 72.69 on the plant parasitic nematode Meloidogyne incognita Chitwood; however, the extract lost its potency upon subfractionation.


Assuntos
Cleome/fisiologia , Extratos Vegetais/farmacologia , Animais , Bactérias/efeitos dos fármacos , Cromatografia em Camada Delgada , Cleome/química , Cleome/ultraestrutura , Fungos/efeitos dos fármacos , Inseticidas/isolamento & purificação , Testes de Sensibilidade Microbiana , Microscopia Eletrônica de Varredura , Extratos Vegetais/isolamento & purificação , Tylenchoidea/crescimento & desenvolvimento
13.
West Indian Med J ; 52(1): 10-3, 2003 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-12806747

RESUMO

The anti-cancer therapeutic promise of cantharidin is limited because of its high mammalian toxicity. In order to find new anti-cancer lead compounds with reduced toxicity of the cantharidin prototype, the following seven derivatives were screened against the human SH-SY5Y neuroblastoma and MCF-7 breast cancer cells in vitro: 2,3-dimethyl-7-oxabicylo-[2.2.1]heptane-2,3-dicarboxylic anhydride (cantharidin) [1], 1-cyclohexen-1,2-dicarboxylic anhydride [2], cis-4-cyclohexen-1,2-dicarboxylic anhydride [3], cis-1, 2-cyclohexanedicarboxylic anhydride [4], exo-7-oxabicyclo[2.2.1]hept-5-ene-2-3 dicarboxylic anhydride [5], exo-7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic anhydride (norcantharidin) [6], and (S)-(-)-O-acetylmalic anhydride [7]. Cantharidin, was found to be the most effective anti-proliferative compound on both cell lines. However, on the human neuroblastoma cells cantharidin was of equal toxicity to compound [6]. Mode of action studies revealed that cantharidin inhibited growth factor-mediated activation of mitogen activated protein kinase (MAPkinase) and attenuated the de-phosphorylation of the extracellular regulated kinases 1 and 2 (erk1 and erk2).


Assuntos
Anidridos/toxicidade , Cantaridina/toxicidade , Inibidores Enzimáticos/toxicidade , Neoplasias da Mama/tratamento farmacológico , Transformação Celular Neoplásica/efeitos dos fármacos , Ativação Enzimática/efeitos dos fármacos , Matriz Extracelular/efeitos dos fármacos , Matriz Extracelular/enzimologia , Fator 2 de Crescimento de Fibroblastos/farmacologia , Humanos , Proteínas Quinases Ativadas por Mitógeno/efeitos dos fármacos , Neuroblastoma/tratamento farmacológico , Células Tumorais Cultivadas
14.
Chemosphere ; 51(8): 701-6, 2003 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-12668029

RESUMO

In the present study, the biologically active natural product dibenzyl trisulphide (DTS) which was previously isolated from the sub-tropical shrub Petiveria alliacea was transformed to methyl benzyl sulphonic anhydride (MBSA) using a "one pot" transformation method. The anhydride was evaluated for anti-microbial activities on the bacteria, Bacillus subtilis and Pseudomonas fluorescens and found to be 2.5 fold more effective than the commercial agents isoniazid and ampicillin in inhibiting the growth of B. subtilis, while on P. fluorescens it was 2.5, 5.0 and 10.0 fold more inhibitory than isoniazid, ampicillin and dibenzyl trisulphide, respectively. DTS was inactive on B. subtillis. The MIC value (microgram/spot) found for DTS on the plant pathogenic fungus, Cladosporium cucumerinum was 5.0 microgram/spot, while MBSA gave a value of 0.1 microgram/spot, compared with 1.25 and 0.16 microgram/spot for the commercial agents ketoconazole and nystatin, respectively. On the larval nematode (Meloidogyne incognita) MBSA inflicted 97.72% and 57.47% Abbotts nematicidal activities at 125.0 and 62.5 ppm, respectively, while DTS had no effect at 125.0 ppm. Nematodes which were immobilized by the low concentrations of MBSA were unable to re-activate when exposed to 10.0 ppm picrotoxin, thus suggesting that the anhydride nematicidal activity is independent of the GABA-ergic neurophysiological pathway.MBSA demonstrated a strong dose dependent radicular suppression effect (r=0.984), on the radicles of Latuca sativa germinating seeds. DTS was weakly active.


Assuntos
Compostos de Benzil/farmacologia , Sulfetos/farmacologia , Animais , Bacillus subtilis , Compostos de Benzil/química , Cladosporium , Larva , Nematoides , Controle de Pragas , Pseudomonas fluorescens , Sulfetos/química , Testes de Toxicidade
15.
West Indian med. j ; 39(4): 213-17, Dec. 1990.
Artigo em Inglês | LILACS | ID: lil-101047

RESUMO

In vitro bioassay of (a) aqueous methanol extracts (AME) of the green leaves of mimosa (Mimosa pudica), love weed (Cuscuta americana), vervine (Stachytarpheta jamaicensis), chicken weed (Salvia serotina) and breadfruit (Artocarpus altilis); (b) methanol-water fraction (MWF) of breadfruit leaves, and (c) commercially available drugs albendazole, thiabendazole and levamisole were assayed for nematode inactivating potential, using filariform larvae of Strongyloides stercoralis. Test larvae were obtained from a 10-day-old charcoal coproculture. Bioassays were conducted in Locke's solution, using 100 larvae in each of three replicates. Inactivation was recorded microscopically at 1, 2, 6 and 12 hours, then every 24 hours up to 5 days' incubation. It(50) (time for inactivation of 50%of larvae) values read: levamisole and mimosa extract < 1 hour; love weed extract, approximately 2 hours; breadfruit (MWF), 9.5 hours; chicken weed, 20 hours; albendazole, 35 hours; breadfruit (AME), 49 hours; thiabendazole, 74 hours and vervine extract, 81.5 hours. It(95) values followed a similar trend, and were approximately double the It(50) measures. A potential role for locally available natural products in the treatment of strongyloidiasis is highlighted


Assuntos
Humanos , Animais , Anti-Helmínticos/farmacologia , Extratos Vegetais/farmacologia , Plantas Medicinais , Strongyloides/efeitos dos fármacos , Bioensaio , Fezes/parasitologia , Jamaica , Larva/efeitos dos fármacos , Estrongiloidíase/tratamento farmacológico
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