scholarly journals The Selectivity of Ethanolic Extract of Buah Makassar (Brucea javanica) on Metastatic Breast Cancer Cells

1970 ◽  
Vol 2 (1) ◽  
pp. 1
Author(s):  
Ika Rahmawati Sutejo ◽  
Herwandhani Putri ◽  
Edy Meiyanto

Treatment of cancer such as surgery, radiotherapy and chemotherapy has many side effects. Chemopreventive agent is needed to reduce the side effect and increase the effectivity of therapy. The discovery of cochemopreventive agent should consider on its selectivity to reduce side effects. The selective cochemopreventive agents work effectively in cancer cells and safe for normal cells. Buah Makassar (Brucea javanica) is a natural product that is empirically used for anti-inflammatory and antitumor. The purpose of this study is to determine the cytotoxic effect of ethanolic extract of buah Makassar against 4T1, MCF7, HeLa, and Vero cell lines. The cytotoxic test is performed by MTT assay. The parameter obtained from the cytotoxic test was IC50. Selectivity index is determined from IC50 ratio of cancer cells to normal cells. The results showed that ethanolic extract of buah Makassar has a cytotoxic activity on 4T1, MCF7, HeLa, and Vero cells with IC50 were 49,9±0,83 μg/mL; 107,6±8,14 μg/mL; 228,9±4,16 μg/mL and 395,5± 4,21 μg/mL respectively. It also has high selectivity on 4T1 metastatic breast cancer cell with selectivity index of 7,93. It can be concluded that the ethanolic extract of buah Makassar has potential to be delevoped as cochemopreventive agent especially on metastatic breast cancer. Keywords: Brucea javanica, MTT assay, selectivity index, 4T1, MCF7, HeLa, Vero

Author(s):  
Lodyta Nawang Tika ◽  
Layung Sekar Sih Wikanthi ◽  
Shofa Annur ◽  
Retno Murwanti

Metastasis is the main cause of death among brast cancer patient. Pleorotus ostreatus is known as anticancer agent that inhibits angiogenesis. Ethanolic extract of Pleorotus ostreatus (EEP) which contains lovastatin is predicted to inhibit metastatic cancer through inhibition of MMP-2 and MMP-9. The aim of this study was to determined antiproliferative and anti metastatic activity of EEPw (Ethanolic extract of wet Pleorotus ostreatus) and EEPd (Ethanolic extract of dried Pleorotus ostreatus ) in 4T1 metastatic breast cancer cells line. Qualitative analysis of lovastatin was determined by thin layer chromatography (TLC) using dicloromethan and etil acetat as mobile phase and lovastatin standard. Scratch wound healing assay was used to determine migration inhition ability of EEP while MMP-9 and MMP-2 activity were analysed by gelatine zymography. Molecular docking was performed to know the interaction between lovastatin and MMP-2 & MMP-9. The result showed that EEPw and EEPd contain lovastatin which were proved by spray reaction with anisaldehid. Each of EEPw and EPPd had cytotoxic activity with IC50 760 and 400 μg/mL respectively. Both of them inhibited closure for about 50 % on 4T1 metastatic breast cancer cells line compared to control. Either EEPw or EEPd decreased MMP-9 expression level compared to control. Lovastatin had higher affinity to bond with either MMP-2 or MMP-9 than native ligand. Overall, EEP could be developed as anticancer agent which was targeted on MMP-2 and MMP-9.Keywords : Pleurotus ostreatus, 4T1 metastatic cells, MMP-2, MMP-2, antimetastatic


2019 ◽  
Vol 18 (15) ◽  
pp. 2156-2168 ◽  
Author(s):  
Magda F. Mohamed ◽  
Nada S. Ibrahim ◽  
Ahmed H.M. Elwahy ◽  
Ismail A. Abdelhamid

Background: Cancer is a complex genetic disease which is characterized by an abnormal cell growth, invasion and spreading to other parts of the body. There are several factors that lead to cancer by causing DNA damage and the impairment of its repair. Treatment of cancer using the chemotherapeutic drugs have adverse side effects such as toxicity as they lose their specificity toward cancer cells and affect also normal cells. Moreover, the cancer cells can resist the chemotherapeutic agents and make them ineffective. For these reasons, much attentions have been paid to develop new drugs with limited side effects on normal cells and to diminish cancer resistance to drug chemotherapy. Recently, some 1,4-dihydropyridine derivatives were reported to act as Multi-Drug Resistance (MDR) modulators that inhibit p-glycoprotein which is responsible for the inability of drugs to enter the cancer cells. Also 1,4-DHPs have antimutagenic properties against chemicals via modulating DNA repair when studied on drosophila. Objective: The objective of this study is the synthesis of bis 1,4-DHPs incorporating ester as well as ether linkages and evaluate the anticancer activity of new compounds for synergistic purpose. Different genetic tools were used in an attempt to know the mechanism of action of this compound against lung cancer. Method: An efficient one pot synthesis of bis 1,4-DHPs using 3-aminocrotononitrile and bis(aldehydes) has been developed. The cytotoxic effect against human cell lines MCF7, and A549 cell lines was evaluated. Results: All compounds exhibited better cytotoxicity toward lung carcinoma cells than breast cancer cells. With respect to lung carcinoma cell line (A549), compound 10 was the most active compound and the three other compounds 7, 8, and 9 showed comparable IC50 values. In case of breast cancer cell line (MCF7), the most active one was compound 7, while compound 8 recorded the least activity. Conclusion: we have developed an efficient method for the synthesis of novel bis 1,4-dihydropyridine derivatives incorporating ester or ether linkage. All compounds showed better cytotoxicity results against A549 than MCF7, so that lung carcinoma cell line was chosen to perform the molecular studies on it. The results showed that all compounds (7, 8, 9 and 10) caused cell cycle arrest at G1 phase. The molecular docking study on CDK2 confirmed the results of cell cycle assay which showed good binding energy between the compounds and the active site of enzyme indicating the inhibition of the enzyme.


Heliyon ◽  
2021 ◽  
Vol 7 (2) ◽  
pp. e06252
Author(s):  
Wei Chen ◽  
Shihyun Park ◽  
Chrishma Patel ◽  
Yuxin Bai ◽  
Karim Henary ◽  
...  

2020 ◽  
Vol 107 ◽  
pp. 65-77 ◽  
Author(s):  
Akshay A. Narkhede ◽  
James H. Crenshaw ◽  
David K. Crossman ◽  
Lalita A. Shevde ◽  
Shreyas S. Rao

2016 ◽  
Vol 76 (18) ◽  
pp. 5209-5218 ◽  
Author(s):  
Shreyas S. Rao ◽  
Grace G. Bushnell ◽  
Samira M. Azarin ◽  
Graham Spicer ◽  
Brian A. Aguado ◽  
...  

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