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1.
Int J Mol Sci ; 17(2): 143, 2016 Feb 14.
Artigo em Inglês | MEDLINE | ID: mdl-26907251

RESUMO

The mammalian hyaluronidase degrades hyaluronic acid by the cleavage of the ß-1,4-glycosidic bond furnishing a tetrasaccharide molecule as the main product which is a highly angiogenic and potent inducer of inflammatory cytokines. Ursolic acid 1, isolated from Prismatomeris tetrandra, was identified as having the potential to develop inhibitors of hyaluronidase. A series of ursolic acid analogues were either synthesized via structure modification of ursolic acid 1 or commercially obtained. The evaluation of the inhibitory activity of these compounds on the hyaluronidase enzyme was conducted. Several structural, topological and quantum chemical descriptors for these compounds were calculated using semi empirical quantum chemical methods. A quantitative structure activity relationship study (QSAR) was performed to correlate these descriptors with the hyaluronidase inhibitory activity. The statistical characteristics provided by the best multi linear model (BML) (R² = 0.9717, R²cv = 0.9506) indicated satisfactory stability and predictive ability of the developed model. The in silico molecular docking study which was used to determine the binding interactions revealed that the ursolic acid analog 22 had a strong affinity towards human hyaluronidase.


Assuntos
Histona Acetiltransferases/antagonistas & inibidores , Hialuronoglucosaminidase/antagonistas & inibidores , Triterpenos Pentacíclicos/síntese química , Triterpenos Pentacíclicos/farmacologia , Rubiaceae/química , Antígenos de Neoplasias/química , Antígenos de Neoplasias/metabolismo , Simulação por Computador , Histona Acetiltransferases/química , Histona Acetiltransferases/metabolismo , Humanos , Hialuronoglucosaminidase/química , Hialuronoglucosaminidase/metabolismo , Modelos Moleculares , Simulação de Acoplamento Molecular , Triterpenos Pentacíclicos/química , Extratos Vegetais/química , Relação Quantitativa Estrutura-Atividade , Triterpenos/química , Triterpenos/isolamento & purificação , Triterpenos/farmacologia , Ácido Ursólico
2.
ScientificWorldJournal ; 2014: 321943, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25126594

RESUMO

Curcuma zedoaria also known as Temu putih is traditionally used in food preparations and treatment of various ailments including cancer. The cytotoxic activity of hexane, dichloromethane, ethyl acetate, methanol, and the methanol-soxhlet extracts of Curcuma zedoaria rhizomes was tested on two human cancer cell lines (Ca Ski and MCF-7) and a noncancer cell line (HUVEC) using MTT assay. Investigation on the chemical components in the hexane and dichloromethane fractions gave 19 compounds, namely, labda-8(17),12 diene-15,16 dial (1), dehydrocurdione (2), curcumenone (3), comosone II (4), curcumenol (5), procurcumenol (6), germacrone (7), zerumbone epoxide (8), zederone (9), 9-isopropylidene-2,6-dimethyl-11-oxatricyclo[6.2.1.0(1,5)]undec-6-en-8-ol (10), furanodiene (11), germacrone-4,5-epoxide (12), calcaratarin A (13), isoprocurcumenol (14), germacrone-1,10-epoxide (15), zerumin A (16), curcumanolide A (17), curcuzedoalide (18), and gweicurculactone (19). Compounds (1-19) were evaluated for their antiproliferative effect using MTT assay against four cancer cell lines (Ca Ski, MCF-7, PC-3, and HT-29). Curcumenone (3) and curcumenol (5) displayed strong antiproliferative activity (IC50 = 8.3 ± 1.0 and 9.3 ± 0.3 µg/mL, resp.) and were found to induce apoptotic cell death on MCF-7 cells using phase contrast and Hoechst 33342/PI double-staining assay. Thus, the present study provides basis for the ethnomedical application of Curcuma zedoaria in the treatment of breast cancer.


Assuntos
Neoplasias da Mama/tratamento farmacológico , Proliferação de Células/efeitos dos fármacos , Curcuma/química , Fitoterapia/métodos , Extratos Vegetais/farmacologia , Rizoma/química , Análise de Variância , Cromatografia em Camada Fina , Feminino , Células Endoteliais da Veia Umbilical Humana , Humanos , Indonésia , Células MCF-7 , Malásia , Microscopia de Fluorescência , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Sais de Tetrazólio , Tiazóis
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