scholarly journals Autophagic Cell Death Is Induced by Acetone and Ethyl Acetate Extracts fromEupatorium odoratum In Vitro: Effects on MCF-7 and Vero Cell Lines

2012 ◽  
Vol 2012 ◽  
pp. 1-9 ◽  
Author(s):  
Faizah Bt. Harun ◽  
Syed Mohsin Syed Sahil Jamalullail ◽  
Khoo Boon Yin ◽  
Zulkhairi Othman ◽  
Anita Tilwari ◽  
...  

Eupatorium odoratum (EO)contains many biologically active compounds, the anticancer effects of which are not well documented. This study evaluates the cytotoxic effects and mechanism of action ofEOextracts on MCF-7 and Vero cell lines. Evaluation of the cytotoxic activity using MTT assay, morphological alterations, and apoptosis were carried out. Autophagy was evaluated by LC3-A protein expression. Cytotoxic activity, membrane blebbing and ballooning at 24 hours, replacement by mass vacuolation, and double membrane vesicles mimicking autophagy and cell death were observed in the cancer cells. No apoptosis was observed by DNA fragmentation assay. Overexpression of LC3-A protein indicated autophagic cell death. Cell cycle analysis showed G0 and G2/M arrest. The Vero cells did not show significant cell death at concentrations <100 μg/mL. These results thus suggest that acetone and ethyl acetate extracts ofEOinduce cell death through induction of autophagy and hold potential for development as potential anticancer drugs.

Author(s):  
PINUS JUMARYATNO ◽  
ARDE TOGA NUGRAHA ◽  
ADILIA TRI HIDAYATI ◽  
BAIQ RISKY WAHYU LISNASARI ◽  
WIDYANUR MAYA DIAHANDARI ◽  
...  

Objective: This study aimed to evaluate the cytotoxic activity of the extracts and fractions of Eriocaulon cinereum against HeLa and Vero cell lines,which represent cervical cancer and normal cells, respectively. In addition, a phytochemical screening was carried out to determine the chemicalconstituents in the extracts and the active fractions.Materials and Methods: The extracts of E. cinereum were obtained by ultrasound-assisted extraction method using n-hexane, ethyl acetate, andmethanol, successively. The active extract was fractionated using vacuum liquid chromatography with dichloromethane followed by ethyl acetate. Thecytotoxic activity was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay method and was measured using microplatereader at the wavelength 595 nm. The data were analyzed with PROBIT from SPSS 16 for Windows®. In addition, phytochemical screening wasperformed using standard procedures.Results: The cytotoxic evaluation of the extracts of E. cinereum showed that the ethyl acetate extract was the most active extract against HeLa cell linewith the half maximal inhibitory concentration (IC50) value of 580.07 μg/ml. The dichloromethane and ethyl acetate fractions from the active extractof E. cinereum exhibited cytotoxic activity against HeLa cell with the IC50 values of 466.61 μg/ml and 267.34 μg/ml, respectively. In addition, the ethylacetate fraction showed a low cytotoxic effect against Vero cell line. The phytochemical screening of the ethyl acetate fraction indicated the presenceof terpenoids and alkaloids.Conclusion: This finding revealed the anticancer potential of E. cinereum and warranted further investigation for the discovery of new anticanceragents from natural resources for cervical cancer.


2021 ◽  
Vol 11 (11) ◽  
pp. 5300
Author(s):  
Jozef Hudec ◽  
Jan Mojzis ◽  
Marta Habanova ◽  
Jorge A. Saraiva ◽  
Pavel Hradil ◽  
...  

Sarcopoterium spinosum (L.) is a medicinal plant traditionally used for the treatment of various diseases including cancer in the Near- and Middle East. The fractions and constituents of the ethanol extract of S. spinosum were screened for in vitro cytotoxic activities on Jurkat (acute T-lymphoblastic leukemia), HeLa (cervical adenocarcinoma), MCF-7 (mammary gland adenocarcinoma), Caco-2 (human colorectal adenocarcinoma), and MDA-MB-231 (mammary gland adenocarcinoma) cell lines using the MTT (3-(dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The ethanol extract was subsequently re-extracted with ethyl acetate and in its sub-fraction obtained by column chromatography three compounds (stachydrine, benzalkonium chloride and rutine) were the first time identified by nuclear magnetic resonance (NMR) analyses. The most active subfraction showed cytotoxic activity against HeLa, MCF-7, and Caco-2 cell lines. The three compounds mentioned, as standards of high-performance liquid chromatography (HPLC) quality, were studied individually and in combination. Cytotoxic activity observed might be due to the presence of benzalkonium chloride and rutin. Benzalkonium chloride showed the strongest growth suppression effect against HeLa cells (IC50 8.10−7 M) and MCF-7 cells (IC50 5.10−6 M). The mixture of stachydrine and benzalkonium chloride allowed a synergistic cytotoxic effect against all tested cancer and normal cells to be obtained. Anti-cancer activity of the plant extract of S. spinosum remains under-investigated, so this research describes how the three major compounds identified in the ethyl acetate extract can exert a significant dose dependent in vitro cytotoxicity.


2018 ◽  
Vol 13 (8) ◽  
pp. 1934578X1801300
Author(s):  
Uraiwan Sriphana ◽  
Chavi Yenjai ◽  
Siriporn Tungnoi ◽  
Jongjai Srirapa ◽  
Auemporn Junsongduang

Two known chalcones (1–2), five known flavonol derivatives (3 and 5–8) and one flavone (4) were isolated for the first time from fruits of Millettia leucantha Kurz. In addition, 5 was found for the first time from this genus. Their structures were elucidated on the basis of IR, MS, 1D and 2D NMR techniques. Chalcone 1 exhibited moderate cytotoxicity against the MCF-7 cell line with an IC50 value of 50.93 μM, whereas this compound showed inactive cytotoxicity against Vero cells. Compound 2 exhibited cytotoxicity against the KB, NCI-H187 and Vero cell lines with IC50 values of 63.64, 114.44 and 28.44 μM, respectively. Compound 8 only showed cytotoxic activity against the KB cell line with an IC50 value of 110.23 μM.


2020 ◽  
Vol 17 (4) ◽  
pp. 434-444 ◽  
Author(s):  
Swathi Krishna ◽  
Byran Gowramma ◽  
Manal Mohammed ◽  
Rajagopal Kalirajan ◽  
Lakshman Kaviarasan ◽  
...  

Background: 1,3,4-thiadiazole is a lead molécule which is versatile for a wide variety of biological activities and in continuation of our interest in establishing some novel heterocyclic compounds for antitumor activity. Objective: The objective of the study was to synthesize series of 5-(1,3-benzodioxol-5-yl)-1,3,4- thiadiazol-2-amine derivative and evaluated for their possible in vitro and in vivo anticancer activity. Methods: The synthesis of 2-aminonaphthoxy-1,3,4-thiadiazole and 5-(1,3-benzodioxol-5-yl)-1,3,4- thiadiazol-2-amine as intermediates were carried out by cyclization method. A mixture of thiosemicarbazide and naphthoxyacetic acid/piperonylic acid and phosphoryl chloride were subjected to cyclization with phosphorous oxychloride to obtain compound 3. Further compounds 1 and 3 were reacted with different aromatic aldehydes in methanol to form compounds 2a-e and 4a-e. The compounds 2a-e and 4a-e were characterized for the melting points, IR, Proton NMR and Mass spectra. The compounds were further evaluated for their anticancer activity. The docking study was performed using Discovery studio 4.1 (Accelrys) software against DNA-binding domain of STAT3. The compounds were analyzed for the ligand-protein binding interaction(s) by molecular docking into the active site of STAT3β using the CDOCKER protocol of Discovery studio (v4.1). Results: The title compounds were screened for in vitro anticancer on human breastadenocarcinoma cells (MCF-7 and Vero). Compounds 4c, 4d and 2d against MCF 7 and 4d against Vero cell lines were found to be the most active dérivatives with IC50 values of 1.03, 2.81 and 3.45 µg/ml against MCF 7 and 31.81 µg/ml against Vero cell lines, respectively. Conclusion: From the in vivo anticancer studies, it was concluded that the synthesized compounds 4c and 4d displayed anticancer activity comparable to the standard drug, while the rest of the compounds demonstrated mild potency for anticancer studies.


Author(s):  
Arif Ayar ◽  
Masuk Aksahin ◽  
Seda Mesci ◽  
Burak Yazgan ◽  
Melek Gül ◽  
...  

Background: Pyrrole compounds having a heterocyclic structure are the most researched and biological activities such as antioxidant and anticancer. Objective: Herein is a first effort to study the significance of heterocyclic compounds to include pyrrole and triazolidine-3,5-dion moiety, on the pharmacokinetic, antioxidant activity and cytotoxic activity on MCF-7 and MCF-12A cell lines. Method: The molecular structures of compounds I-XIV were simulated by the theoretical B3LYP/DFT method. Pharmacokinetic studies of PhTAD-substituted heterocyclic compounds (I-XIV) were analyzed to show Lipinski's rules via in-silico methods of Swiss-ADME. The drug likeness calculations were carried out Molinspiration analyses. The some toxicity risk parameter can be quantified using Osiris. Antioxidant activities determined by DPPH, Fe+2 ions chelating and reducing. Cytotoxic activity measured by MTT and RTCA. Results: Compared with the DPPH activity, the metal chelating activity exhibited serious similar antioxidant effects by PhTAD substituted pyrrole compounds. The same compounds showed the highest activity among the two antioxidant activities. The IC50 values of the compounds are in the range of 12 and 290 µM in MCF-7 cell line. In the MTT and RTCA assays, All compounds showed cytotoxic activity, but about half of the fourteen compounds showed high cytotoxicity. IC50 values of the compounds are in the range of 5 and 54 µM for MTT and range of 1.5 and 44 µM for RTCA. Conclusion: Data of the antioxidant and cytotoxic activity of PhTAD-substituted dihydropyrrole-derived compounds in MCF-7 and MCF-12A cell lines confirmed that the compounds are a biologically active compound and is notable for anti-cancer researches.


Author(s):  
Tahany Amir Tawfeeq ◽  
Ghaith Ali Jasim ◽  
Abdulmutalib A. Nasser ◽  
Basma Talib Al-Sudani

Conocarpus erectus L. is a perennial, evergreen shrub belonging to Combretaceae family. Conocarpus plant reported to contain phenolic acid, flavonoids, lignan, terpenes and tannins. Aim of study was to isolate lupeol from hexane fraction and gallic acid from ethyl acetate fraction and investigate the effects of (hexane and ethyl acetate) fractions on viability of pancreatic AsPC-1 and breast MCF-7 cell lines by MTT assay. The presence of lupeol in the hexane and gallic acid in the ethyl acetate extracts was detected by TLC. The identification of isolated lupeol and gallic acid by HPTLC and HPLC comparing with standard lupeol and gallic acid. Structural elucidation of isolated compounds done by FTIR and UV spectrophotometer. The cytotoxic activity showed more at high concentration (30µg/ml) in both ethyl acetate and hexane fractions against MCF-7 cell line, the percentage of cellular inhibition for ethyl acetate at 30mg/ml was (73% and 79%) more than the hexane fraction in which the inhibition was (60% and 76%) at 48hr and 72 hr respectively. Furthermore, the cytotoxic activity more at high concentration (30µg/ml) in both fractions against AsPC-1 cell line with cellular inhibition (58% and 70%) for ethyl acetate fraction and (50% and 66%) for hexane fraction in compared with Cisplatin.


2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Moulay Ali Oukerrou ◽  
Mounir Tilaoui ◽  
Hassan Ait Mouse ◽  
Inass Leouifoudi ◽  
Abdeslam Jaafari ◽  
...  

The aim of this work is to investigate the in vitro cytotoxic and antibacterial effects of the essential oils of Aloysia citriodora Palau, harvested in different regions of Morocco. The chemical profile was established using gas chromatography-mass spectrometry analysis. The cytotoxic activity against P815, MCF7, and VERO cell lines as well as the normal human peripheral blood mononuclear cells (PBMCs) was evaluated using the MTT assay. Standard, ATCC, strains of bacteria (Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa) were cultivated in Muller Hinton media. Then, agar disc diffusion, minimum inhibitory concentrations (MICs), and minimal bactericidal concentrations (MBCs) were determined using microdilution method. The essential oils obtained were predominantly composed of β-spathulenol (15.61%), Ar-curcumene (14.15%), trans-caryophyllene oxide (14.14%), and neral (10.02%). The results of the assays showed that the cytotoxic effect of the essential oil of A. citriodora was high on P815 and moderate on MCF7 and on VERO cell lines. However, no cytotoxic effect was observed on PBMCs. On the other hand, essential oils showed a significant antimicrobial activity against both Gram-negative and Gram-positive bacteria. MICs ranged between 2.84 and 8.37 mg/ml. Essential oil of A. citriodora leaves possesses significant antibacterial effect and cytotoxic activity against tumor cell lines.


2021 ◽  
Vol 53 (1) ◽  
pp. 109-117
Author(s):  
Ratna Asmah Susidarti ◽  
Edy Meiyanto ◽  
Muthi' Ikawati ◽  
Normaidah Normaidah ◽  
Nurramadhani A. Sida

Isolation and identification of compounds and pharmacological activity of the Micromelum minutum grown in some countries has been done, but the Indonesian M. minutum has not been studied, either phytochemically or pharmacologically. This study aimed to determine the cytotoxic activity of Indonesian M. minutum leave extracts toward MCF-7 and 4T1 breast cancer cell lines. The leaves were obtained from M. minutum grow in Bantimurung National Park, Bulusaraung, South Sulawesi, and then were macerated gradually in hexane, ethyl acetate, and methanol. The cytotoxic activity of obtained extracts was determined by MTT assay. The extraction yielded hexane (HEM), ethyl acetate (EEM), and methanol (MEM) extracts of 2.65, 6.12, and 6.49%, respectively. HEM was the most potent extract with IC50 values of 148 and 87 µg/mL on MCF-7 and 4T1 cells, respectively, followed by EEM (185 and 170 µg/mL). MEM possessed a weak potency with an IC50 value of 384 µg/mL on MCF-7 cells and was not toxic toward 4T1 cells. Therefore, HEM is important to be further investigated for its active constituents.


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