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1.
West Indian med. j ; 56(6): 487-490, Dec. 2007. tab
Article in English | LILACS | ID: lil-507260

ABSTRACT

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.


Subject(s)
Humans , Boehmeria , Phytotherapy/methods , Interferon-gamma/immunology , /immunology , Common Cold/immunology , Common Cold/therapy , Sinusitis/immunology , Sinusitis/therapy , Sinusitis/microbiology
2.
West Indian med. j ; 56(1): 17-21, Jan. 2007.
Article in English | LILACS | ID: lil-471843

ABSTRACT

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.


Los datos compilados en el presente estudio sobre el trisulfuro de dibencilo (TSD) aislado a partir de Petiveria alliacea L (yerba de Guinea, ó anamú) revelaron que el compuesto y sus derivados podrían tener extraordinario interés farmacéutico. El modo de acción esclarecido en el TSD, reveló que se trata de una molécula de transducción de señales de proteínas kinasas 1 y 2 (MAP quinasas ERk 1 y 2) reguladas extracelularmente y activadas por mitógenos. El trisulfuro de dibencilo causó hiperfosforilación de la fosforilación de las quinasas MAP (Erk 1 y 2) inducidas mediante factor de crecimiento, un proceso crítico para el mejoramiento de la memoria a largo plazo, y que está implicado en el crecimiento neuronal. El trisulfuro de dibencilo y sus derivados mostraron una poderosa actividad citotóxica y antiproliferativa en una amplia gama de líneas celulares de cáncer. La actividad citotóxica del TSD se incrementaba de 70 á 1000 veces, cuando se vinculaba a la albúmin in vitro. El trisulfuro de dibencilo parece poseer un mecanismo conmutador citoquínico que regula por decremento las citoquinas provenientes de la vía de las células auxiliares de tipo 1 (células Th-1), que contiene varias citoquinas pro-inflamatorias y regula por incremento las de la vía de las células auxiliares de tipo 2 (Th-2). El trisulfuro regula por incremento los parámetros del sistema reticuloendotelial, p.ej. los conteos de granulocitos y el aumento tanto de las masas tímicas como de las masas de placas de Peyer, a través de los procesos de proliferación celular, de los cuales se sabe que son regulados mediante la vía de la transducción de señales de la quinasa MAP. Cuando los cigotos de Asternia pectinifera (estrella de mar) fueron expuestos al TSD a una concentración de 10 mM ­ una dosis letal para todas las células cancerosas sometidas a prueba ­ se observó que el proceso sensible de biosíntesis de la proteína no era afectado. De modo similar, la proliferación del fibroblasto humano HOFA ­ una línea celular no cancerosa ­ no fue afectada severamente por el TSD a 8.9 µM en siete días ­ una concentración letal para la mayoría de las líneas celulares cancerosas sometidas a prueba. Las implicaciones de los hallazgos se pondrán de relieve en el presente estudio


Subject(s)
Humans , Benzyl Compounds/therapeutic use , Plant Extracts , Phytotherapy , Sulfides/therapeutic use , Antigens, CD/physiology , Cadherins/physiology , Benzyl Compounds/pharmacology , Up-Regulation/physiology , Sulfides/pharmacology , Signal Transduction/drug effects
3.
West Indian med. j ; 56(1): 5-10, Jan. 2007.
Article in English | LILACS | ID: lil-471845

ABSTRACT

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 79.24and 50.83anti-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.


La epingaiona (4-Metil-1-(5-metil-2,3,4,5-tetrahidro-[2,3']bifuranil-5-il)-pentan-2-uno) fue aislada como uno de los principales metabolitos lipofilicos secundarios de las hojas y tallos de Bontia daphnoides L. El compuesto produjo 79.24 % y 50.83 % de actividad citotóxica/anti-proliferación sobre el neuroblastoma humano SH-SY5Y y las células del sarcoma TE-671 in vitro a 50 µg/mL, respectivamente. La epingaiona fue transformada en once derivados en condiciones de laboratorio, utilizando etanol. Algunos produjeron mayor actividad citotóxica y antiproliferativa sobre las líneas celulares cancerosas sometidas a ensayo. Uno de los derivados (compuesto 2) de elevada actividad citotóxica fue identificado como 5'-Etoxi-5-metil-5-(4-metil-2-oxo-pentil)-2,3,4,5-tetrahidro-5'H- [2,3']bifuranil-2'-uno. Tanto la epingaiona como el compuesto 22 causaron una acumulación de neuroblastomas SH-SY5Y muertos o detenidos en la fase m del ciclo celular, según lo revela el marcador KE 67 específico de la fase m.


Subject(s)
Humans , Phytotherapy , Furans/pharmacology , Myoporaceae , Neuroblastoma/drug therapy , Pentanones/pharmacology , Sarcoma/drug therapy , Plant Stems , Drug Screening Assays, Antitumor , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Leaves , Furans/chemistry , Cell Line, Tumor , Pentanones/chemistry , Cell Proliferation/drug effects , Cell Survival
4.
West Indian med. j ; 55(4): 215-216, Sept. 2006.
Article in English | LILACS | ID: lil-472128
5.
West Indian med. j ; 53(4): 208-219, Sept. 2004.
Article in English | LILACS | ID: lil-410433

ABSTRACT

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


Subject(s)
Humans , Antineoplastic Agents/pharmacology , Benzyl Compounds/pharmacology , Plant Extracts/pharmacology , Neuroblastoma/pathology , Sulfides/pharmacology , Cell Division/drug effects , Drug Screening Assays, Antitumor , Plant Extracts/chemistry , Cell Line, Tumor , Cell Survival/drug effects
6.
West Indian med. j ; 52(1): 10-13, Mar. 2003.
Article in English | LILACS | ID: lil-410842

ABSTRACT

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)


Subject(s)
Humans , Anhydrides/toxicity , Cantharidin/toxicity , Enzyme Inhibitors/toxicity , Enzyme Activation/drug effects , Tumor Cells, Cultured , /pharmacology , Extracellular Matrix/drug effects , Extracellular Matrix/enzymology , Breast Neoplasms/drug therapy , Neuroblastoma/drug therapy , Mitogen-Activated Protein Kinases/drug effects , Cell Transformation, Neoplastic/drug effects
7.
West Indian med. j ; 39(4): 213-17, Dec. 1990.
Article in English | LILACS | ID: lil-101047

ABSTRACT

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


Subject(s)
Humans , Animals , Plants, Medicinal , Strongyloides/drug effects , Plant Extracts/pharmacology , Anthelmintics/pharmacology , Strongyloidiasis/drug therapy , Biological Assay , Feces/parasitology , Jamaica , Larva/drug effects
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