ABSTRACT
ABSTRACT The hemoflagellate protozoan, Trypanosoma cruzi, mainly transmitted by triatomine insects through blood transfusion or from mother-to-child, causes Chagas' disease. This is a serious parasitic disease that occurs in Latin America, with considerable social and economic impact. Nifurtimox and benznidazole, drugs indicated for treating infected persons, are effective in the acute phase, but poorly effective during the chronic phase. Therefore, it is extremely urgent to find innovative chemotherapeutic agents and/or effective vaccines. Since piplartine has several biological activities, including trypanocidal activity, the present study aimed to evaluate it on two T. cruzi strains proteome. Considerable changes in the expression of some important enzymes involved in parasite protection against oxidative stress, such as tryparedoxin peroxidase (TXNPx) and methionine sulfoxide reductase (MSR) was observed in both strains. These findings suggest that blocking the expression of the two enzymes could be potential targets for therapeutic studies.
Subject(s)
Piperidones/pharmacology , Trypanocidal Agents/pharmacology , Trypanosoma cruzi/drug effects , Trypanosoma cruzi/chemistry , Plant Extracts/pharmacology , Proteins/analysis , Reference Values , Mass Spectrometry , Trypanosoma cruzi/metabolism , Electrophoresis, Gel, Two-Dimensional , Reproducibility of Results , Oxidative Stress , ProteomicsABSTRACT
Objective The aim of the study was to investigate the effect of piplartine on the proliferation and apoptosis in human breast cancer MDA‐MB‐231 cells line and the mechanism involved .Methods Human breast cancer MDA‐MB‐231 cells line was cultured in vitro .The inhibitory effect of piplartine on the proliferation of MDA‐MB‐231 cells was measured by CCK‐8 assay after treatment with piplartine at different concentrations .The apoptosis rates were measured by flow cytometry .Western blot was used to explore the effect of piplartine on MDA‐MB‐231 cells Bcl‐2 and Bax protein expression .Results The CCK‐8 assay showed that piplartine had an inhibiting effect on the proliferation of MDA‐MB‐231 cells in a concentration and time dependent manner .Piplar‐tine induced apoptosis of MDA‐MB‐231 cells obviously .The antioxidant N‐acetyl‐L‐cystein inhibited the apoptosis of cells .By Western blot analysis ,we found the expression of Bax was up‐regulated whereas that of Bcl‐2 was down‐regulated in a concentration dependent manner .Conclusion Piplartine possesses a significant function for inhibiting proliferation and inducing apoptosis of MDA‐MB‐231 cells ,and its mechanism would be associated with the down regulation of Bcl‐2 and up regulation of Bax .
ABSTRACT
Piplartine is an alkaloids/amide component of Piper species,having diverse pharmacological and biological activities.Recent studies have indicated that piplartine has inhibitory effects on several kinds of tumors and is a kind of potential antitumor drugs.It can inhibit the proliferation of tumor cells,cause cell cycle arrest and induce apoptosis.More investigations suggest that targeting the reactive oxygen species(ROS) stressresponse pathway is closely related to its antitumor activity.
ABSTRACT
Piper is a notable genus among Piperaceae due to their secondary metabolites such as lignans, amides, esters and long chain fatty acids used as anti-herbivore defenses with comparable effects of pyrethroids, that holds a promise in insect control, including malaria vectors such as Anopheles darlingi, the main vector in the North of Brazil. Methanolic extracts of Piper tuberculatum Jacq., Piperaceae, and P. alatabaccum Trel. & Yunck., Piperaceae, and some isolated compounds, i.e, 3,4,5-trimetoxy-dihydrocinamic acid, dihydropiplartine; piplartine, piplartine-dihydropiplartine and 5,5',7-trimetoxy-3',4'-metilenodioxiflavone were tested as larvicides against A. darlingi. The Lethal Concentrations (LC50 and LC90) of methanolic extracts were 194 and 333 ppm for P. tuberculatum and 235 and 401 ppm for P. alatabacum, respectively. Isolated compounds had lower LC values, e.g. the LC50 and LC90 of the piplartine-dihidropiplartine isolated from both plant species was 40 and 79 ppm, respectively.