scholarly journals Synthesis of Chalcone Derivatives and Their in vitro Anticancer Test Against Breast (T47D) and Colon (WiDr) Cancer Cell Line

2018 ◽  
Vol 18 (1) ◽  
pp. 102 ◽  
Author(s):  
Chairil Anwar ◽  
Yogo Dwi Prasetyo ◽  
Sabirin Matsjeh ◽  
Winarto Haryadi ◽  
Eti Nurwening Sholikhah ◽  
...  

The synthesis of chalcone derivatives as target compounds and anticancer test against breast (T47D) and colon (WiDr) cell line had been performed. The synthesis was performed by Claisen-Schmidt condensation by using acetophenone and benzaldehyde derivatives. The anticancer activity test of chalcone derivatives was carried out by MTT assay against T47D and WiDr cell lines. The synthesis was started by reacting 4-hydroxyacetophenone and benzaldehyde derivatives such as p-anisaldehyde (chalcone A [(E)-4'-hydroxy-4-methoxychalcone]), veratraldehyde (chalcone B [(E)-4'-hydroxy-3,4-dimethoxychalcone]), 4-chlorobenzaldehyde (chalcone C [(E)-4'-hydroxy-4-chlorochalcone]) and 2,4-dihydroxyacetophenone with 4-chlorobenzaldehyde (chalcone D [(E)-2',4'-dihydroxy-4-chlorochalcone]) in methanol as solvent. The synthesis was carried out in alkaline condition (KOH) by stirring the mixture at room temperature for 48 h. The structures of products were identified by FTIR, GC-MS, 1H- and 13C-NMR spectrometers. The results showed that the chalcone derivatives (A-D) were yielded in 96; 97; 96; and 93%, respectively as yellow solid. The anticancer test indicated that the chalcone D was the most active towards T47D cell line with IC50 of 42.66 μg/mL and the chalcone C was the most active against WiDr cell line with IC50 of 20.42 μg/mL.

2020 ◽  
Vol 9 (1) ◽  
pp. 14-20
Author(s):  
Mohammad Zamani Rarani ◽  
Fahimeh Zamani Rarani ◽  
Ali Valiani ◽  
Zeinolabedin Shrifian Dastjerdi ◽  
Elias Kargar Abargouei ◽  
...  

Background: Adenosine receptor family, especially A1 type is-overexpressed in breast-derived tumor cells and the P53 gene is mutant in some of these cells while the casps gene is of wild type as well. The aim of this study was to evaluate the effect of the A1 receptor function on cell programmed death or proliferation, as well as the relationship between this receptor stimulation/inhibition and caspase 3 (casp3) expression in T47D cell line that has a mutant and non-functional P53 gene. Materials and Methods: The expression of casps3 was measured by real-time polymerase chain reaction and then flow cytometery and MTT assay were used to assess the apoptotic and proliferation cell rate after the treatment of T47D cells with specific agonist N6-cyclopentyladenosine (CPA) and antagonist 1,3-dipropyl-8-cyclopentylxanthine (DPCPX) of this receptor 24, 48, and 72 hours after treatment. Result: Our results indicated that DPCPX significantly induces apoptosis in T47D cells and the rate of survival cell after the reduction of this treatment, especially 72 hours after treatment. Finally, the expression of casp3 was up-regulated by DPCPX treatment, especially in 72 hours while CPA treatment had opposite results (P>0.05). Conclusion: In general, DPCPX could up-regulate casp3 gene expression and subsequently increase the apoptosis rate in T47D cells with casp3 expression without the P53 gene interference. Therefore, adenosine A1 receptor antagonists may be introduced as anti-cancer agents.


F1000Research ◽  
2019 ◽  
Vol 8 ◽  
pp. 168
Author(s):  
Woro Anindito Sri Tunjung ◽  
Puspa Restu Sayekti

Background: Breast cancer is the second leading cause of death in women. Alternative medicine with high efficacy is needed for breast cancer treatments, for example induction of apoptosis using natural products. It has been found that many natural apoptosis-inducing compounds are isolated from marine sponge. The objective of this study is to analyze the ability of extracts of the sponge Ancorina sp. to induce apoptosis on human breast cancer T47D cell line and find out its mechanism. Methods: T47D cells were treated with crude extracts of methanol, dichloromethane:methanol (1:1) and dichloromethane Ancorina sp. for 24 h, and doxorubicin was used as a positive control. Methods used for this study were MTT assay to examine cell viability and determine IC50 of the three extracts, while the percentage of apoptosis and caspase-3 were investigated by flow cytometry. Results: IC50 values of methanol, dichloromethane:methanol (1:1), and dichloromethane extract were 84.25, 121.45, and 99.85μg/mL respectively. The percentages of apoptotic cells after treatment with methanol, dichloromethane:methanol (1:1), and dichloromethane extracts were 88.68, 27.54 and 53.63% respectively, whereas the percentage of caspase-3 was 77.87, 12.66 and 12.97%, respectively. Conclusions: These results revealed that all extracts of Ancorina sp. have strong or moderate cytotoxicity and have the ability to induce apoptosis on T47D human breast cancer cell line. However, methanol crude extract has high efficacy to induce apoptosis through caspase-3 activation compared to the other extracts. Hence methanol extract warrants further investigation as a natural medicine for human breast cancer.


2020 ◽  
Vol 1 (1) ◽  
pp. 32-40
Author(s):  
Makbruri Amin ◽  
Irsan Saleh

Anticancer drugs are primarily aimed at inhibiting the growth andproliferation of cancer cells. The soursop plant (Annona squamosa L.) has thepotential to be developed as an anticancer drug. This plant contains severalactive compounds including flavonoids, borneol, camphor, alkaloids, terpenes,saponins, tannins, polyphenols and polyketide compounds. This study wasconducted to assess the efficacy of the polar fraction of soursop leaves oncytotoxic activity based on the IC₅₀ value in T47D cells. This research isexperimental in vitro study using cell line T47D. The methanol fraction ofsoursop leaves was diluted with DMSO and DMEM to obtain a concentration of500; 250; 125; 62.5; 31.25 µg/ mL cisplatin with a concentration of 50:25:12,5:6,25:3,125 µg/mL. The methanol fraction of soursop from the highestconcentration of 500 µg/ml has average viability of 46.77% and the averagepercentage of viability will increase in proportion to the decrease in theconcentration of the test compound. The IC50 value shows the concentrationvalue that results in the inhibition of cell proliferation by 50% of the population.In conclusion, methanol fraction of soursop leaves have an anticytotoxic effecton T47D cell line through the role of flavonoid metabolites.


Author(s):  
Rina Andriyani ◽  
Chandra Risdian ◽  
Zalinar Udin

Drug discovery for cancer medication is the most important effort that researcher do at this time. Indonesia bio diversities have possibility as a cancer medicine sources. Finding a herbal medicine for cancer treatment is a first step to find a right cancer medicine in the future. This research has already completed for the earlier another research. Some fractions of Hedyotis corymbosa extract has been analyzed using Sulforhodamine B method with UV wavelength 515 nm against T47D cell line, a human breast cancer. There are Hexane extract, Methylene chloride extract and Ethyl acetate extract, and give inhibitory concentration 50 (IC50)  of 33.45 µg/ml, 54.59 µg/ml and 52.58 µg/ml, respectively. Ethanolic extract, itself has IC50 of 61.57 µg/ml, whereas IC50 value of Cisplatinum is  9.63 µg/ml. There is a difference between the ethanolic extracts with the other fraction.Keywords: breast cancer, herbal medicine, T47D, Hedyotis corymbosa


2021 ◽  
Vol 18 (1) ◽  
pp. 38-46
Author(s):  
Juwita Rahmawati ◽  
Maryati Maryati

Avocado plants are widely used as traditional medicine in Indonesia. This research aimed to determine the cytotoxic and antiproliferation activity of avocado seed extract and fractions on the T47D breast cancer cell line. Extraction was done by maceration method using 96% ethanol, then fractionation was done by liquid-liquid partition using n-hexane, chloroform, and ethyl acetate. Cytotoxic and antiproliferation tests were done by the MTT method. Apoptosis activity was investigated by the double staining method, using acridine orange-propidium iodide as a staining reagent. Results showed that the n-hexane fraction of avocado seed had a cytotoxic activity with IC50 27.9 µg/mL. N-hexane fraction of avocado seed inhibited proliferation and induced apoptosis of T47D cell line.


2014 ◽  
Vol 2 (2) ◽  
pp. 53-58 ◽  
Author(s):  
Iin Tusanti ◽  
Andrew Johan ◽  
RA Kisdjamiatun

Background: Several studies focused on phytochemical as agents of cancer prevention and co-chemotherapy. One of Indonesian plant which has edible fruit but it hasn’t been completely explored is Medinilla speciosa (Reinw.ex Bl.). Objective : The aim of this study is to examine the cytotoxic activity (IC50 value) of Medinilla speciosa (Reinw.ex Bl.) fruit ethanolic extract. Methods : Medinilla speciosa (Reinw.ex Bl.) fruit ethanolic extract was used in this study. The cytotoxic activity was investigated in vitro on human breast cancer T47D cell-line. The cells viability were assessed using MTT colorimetric assay. Breast cancer T47D cell lines was treated with fruit ethanolic extract (10, 25, 50, 100, 250, 500 and 1000 µg/ml) for 24 hour of incubation. This study also identified phytochemical compound of the fruit with thin layer chromatography (TLC). Results: The result showed that ethanolic extract of Medinilla speciosa (Reinw.ex Bl.) has moderate cytotoxicity on breast cancer T47D cell line with IC50 value of 614.50 µg/ml and yield the decrease of cell viability at higher concentration. Medinilla speciosa fruit can not be used as anticancer agent but chemoprevention agent. Phytochemical test showed that the fruit extract contain flavonoid and saponin compound. Conclusion: Ethanolic extract of Medinilla speciosa fruit exhibited moderate cytotocicity on breast cancer T47D cell lines with IC50 value was 614,50 µg/ml thus it can be used as chemopreventioan agent.


F1000Research ◽  
2019 ◽  
Vol 8 ◽  
pp. 168
Author(s):  
Woro Anindito Sri Tunjung ◽  
Puspa Restu Sayekti

Background: Breast cancer is the second leading cause of death in women. Alternative medicine with high efficacy is needed for breast cancer treatments, for example induction of apoptosis using natural products. It has been found that many natural apoptosis-inducing compounds are isolated from marine sponge. The objective of this study is to analyze the ability of extracts of the sponge Ancorina sp. to induce apoptosis on human breast cancer T47D cell line and find out its mechanism. Methods: T47D cells were treated with crude extracts of methanol, dichloromethane:methanol (1:1) and dichloromethane Ancorina sp. for 24 h, and doxorubicin was used as a positive control. Methods used for this study were MTT assay to examine cell viability and determine IC50 of the three extracts, while the percentage of apoptosis and caspase-3 were investigated by flow cytometry. Results: IC50 values of methanol, dichloromethane:methanol (1:1), and dichloromethane extract were 84.25, 121.45, and 99.85μg/mL respectively. The percentages of apoptotic cells after treatment with methanol, dichloromethane:methanol (1:1), and dichloromethane extracts were 88.68, 27.54 and 53.63% respectively, whereas the percentage of caspase-3 was 77.87, 12.66 and 12.97%, respectively. Conclusions: These results revealed that all extracts of Ancorina sp. have strong or moderate cytotoxicity and have the ability to induce apoptosis on T47D human breast cancer cell line. However, methanol crude extract has high efficacy to induce apoptosis through caspase-3 activation compared to the other extracts. Hence methanol extract warrants further investigation as a natural medicine for human breast cancer.


2019 ◽  
Vol 19 (4) ◽  
pp. 1081
Author(s):  
Artania Adnin Tri Suma ◽  
Tutik Dwi Wahyuningsih ◽  
Mustofa Mustofa

The synthesis of N-phenylpyrazolines 1-5 was performed by the cyclocondensation of phenylhydrazine and appropriate chalcones that have been synthesized from our previous work. All of the compounds were elucidated for their structure using GC-MS, FTIR, 1H, and 13C-NMR spectrometers. Their anticancer activity was evaluated against breast cancer cell line (T47D) and colorectal cancer cell line (WiDr). Compound 4 (4-(3-(4-chlorophenyl)-1-phenyl-4,5-dihydro-1H-pyrazol-5-yl)-2-methoxyphenol) was found to be the most potent compound with IC50 value of 13.11 µg/mL in T47D cell line and 3.29 µg/mL in WiDr cell line. Docking study was conducted to evaluate the interaction between all compounds and EGFR receptor on cancer cells. Among the tested compounds, compound 4 is the only compound that has interaction with MET769 residue through hydrogen bonding due to the presence of hydroxyl group on its structure. Our findings suggest that the synthesized N-phenylpyrazolines in this study have a promising anticancer activity.


2020 ◽  
Vol 23 (7) ◽  
pp. 611-623
Author(s):  
Ahmed A. Soliman ◽  
Fawzy A. Attaby ◽  
Othman I. Alajrawy ◽  
Azza A.A. Abou-hussein ◽  
Wolfgang Linert

Aim and Objective: Platinum (II) and platinum (IV) of pyrophosphate complexes have been prepared and characterized to discover their potential as antitumor drugs. This study was conducted to prepare and characterize new ternary platinum (II) complexes with formamidine and pyrophosphate as an antitumor candidate. Materials and Methods: The complexes have been characterized by mass, infrared, UV-Vis. spectroscopy, elemental analysis, magnetic susceptibility, thermal analyses, and theoretical calculations. They have been tested for their cytotoxicity, which was carried out using the fastcolorimetric assay for cellular growth and survival against MCF-7 (breast cancer cell line), HCT- 116 (colon carcinoma cell line), and HepG-2 (hepatocellular cancer cell line). Results: All complexes are diamagnetic, and the electronic spectral data displayed the bands due to square planar Pt(II) complexes. The optimized complexes structures (1-4) indicated a distorted square planar geometry where O-Pt-O and N-Pt-N bond angles were 82.04°-96.44°, respectively. Conclusion: The complexes showed noticeable cytotoxicity and are considered as promising antitumor candidates for further applications.


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