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1.
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
2.
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
3.
West Indian med. j ; 56(1): 17-21, Jan. 2007.
Artigo em Inglês | LILACS | ID: lil-471843

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
Humanos , Compostos de Benzil/uso terapêutico , Fitoterapia , Extratos Vegetais , Sulfetos/uso terapêutico , Antígenos CD/fisiologia , Caderinas/fisiologia , Compostos de Benzil/farmacologia , Regulação para Cima/fisiologia , Sulfetos/farmacologia , Transdução de Sinais/efeitos dos fármacos
4.
West Indian med. j ; 56(1): 5-10, Jan. 2007.
Artigo em Inglês | LILACS | ID: lil-471845

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 79.24and 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.


Assuntos
Humanos , Furanos/farmacologia , Myoporaceae , Neuroblastoma/tratamento farmacológico , Fitoterapia , Pentanonas/farmacologia , Sarcoma/tratamento farmacológico , Linhagem Celular Tumoral , Sobrevivência Celular , Ensaios de Seleção de Medicamentos Antitumorais , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Furanos/química , Folhas de Planta , Caules de Planta , Pentanonas/química , Proliferação de Células/efeitos dos fármacos
5.
Ear Nose Throat J ; 68(8): 626-32, 635, 1989 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-2684602

RESUMO

Chondrosarcoma of the skull base is a rare neoplasm. The most common presenting symptoms are hoarseness, dysphagia, and diplopia, which is associated with palsies of cranial nerves X, IX, and VI. The temporal bone is the most common site of tumor origin, followed by the sphenoid bone. These tumors must be differentiated from chordoma, chondroid chordoma, osteogenic sarcoma, enchondroma, and meningioma. Diagnosis is made by patient history, radiologic imaging, and biopsy. The treatment is surgical excision followed by radiation therapy. Five-year survival rates for grades I, II, and III are 90, 81, and 43%, respectively.


Assuntos
Condrossarcoma , Neoplasias Cranianas , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade
6.
J Am Acad Dermatol ; 10(6): 986-8, 1984 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-6736343

RESUMO

Six keloids from five patients heterozygous for the X-linked glucose-6-phosphate dehydrogenase (G6PD) locus were studied. Both the B and A enzymes were found in the keloids in similar proportions to the normal tissues. This finding indicates that keloids have a multicellular origin and that they do not develop clonally as do most neoplasms.


Assuntos
Glucosefosfato Desidrogenase/genética , Isoenzimas/genética , Queloide/enzimologia , Adolescente , Adulto , Células Sanguíneas/enzimologia , Divisão Celular , Feminino , Fibroblastos/enzimologia , Humanos , Queloide/genética , Queloide/patologia , Pele/patologia
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