Genotoxic and Cytotoxic Activities of Lantadene A-Loaded Gold Nanoparticles (LA-AuNPS) in MCF-7 Cell Line: An in vitro Assessment

2020 ◽  
Vol 39 (5) ◽  
pp. 422-432
Author(s):  
Noor Dheyaa Jaafar ◽  
Ali Z. Al-Saffar ◽  
Emad A. Yousif
Keyword(s):  
Gold Nanoparticles ◽  
Cell Line ◽  
Synthesis Method ◽  
Tumor Cell Line ◽  
Terminal Deoxynucleotidyl Transferase ◽  
Cytotoxic Activities ◽  
P53 Expression ◽  
Lantadene A ◽  
Mcf 7

Gold nanoparticles (AuNPs) have been widely used in many applications. Their usage as drug delivery vehicles has also gained considerable attention due to their chemical and optical properties as well as their good biocompatibility. The present study was conducted to evaluate the efficiency of AuNPs in enhancing the cytotoxic and apoptotic induction activity of lantadene A (LA), separated from Lantana camara leaves, on the breast tumor cell line MCF-7 in vitro. By utilizing plant-mediated synthesis method of nanostructures, LA-loaded AuNPs (LA-AuNPs) were prepared and their formation was confirmed by means of ultraviolet–visible spectroscope, atomic force microscope, scanning electron microscope, and zeta potential. The cytotoxic effect of LA-AuNPs was analyzed using a methylthiazol tetrazolium assay and compared to free AuNPs and LA. The results indicated a significant increase in the reduction of MCF-7 cells viability after incubation with LA-AuNPs. As determined by terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay, LA-AuNPs induced a greater ratio of DNA-fragmented cells compared to LA-treated and untreated cells. Also, by operating real-time polymerase chain reaction, LA-AuNPs-treated cells displayed an increased upregulation of p53 expression and downregulation of BCL-2 expression in addition to a significant reduction in the level of BCL-2-BAX ratio. No significant effect was shown on the expression of BAX. Collectively, our results indicate that LA-AuNPs showed promising cytotoxicity to MCF-7 cells as a novel nanoscale preparation, likely via induction of apoptotic genes and stimulation of DNA fragmentation.

Melatonin inhibits telomerase activity in the MCF-7 tumor cell line both in vivo and in vitro

2003 ◽  
Vol 35 (3) ◽  
pp. 204-211 ◽  
Author(s):  
Mercedes M. Leon-Blanco ◽  
Juan M. Guerrero ◽  
Russel J. Reiter ◽  
Juan R. Calvo ◽  
David Pozo
Keyword(s):  
Tumor Cell ◽  
Cell Line ◽  
Tumor Cell Line ◽  
Telomerase Activity ◽  
Mcf 7

scholarly journals Synthesis and Bioactivity of β-Carboline Derivatives

2010 ◽  
Vol 5 (10) ◽  
pp. 1934578X1000501
Author(s):  
Shengkun Li ◽  
Bing Yang ◽  
Qianliang Zhang ◽  
Jiwen Zhang ◽  
Junru Wang ◽  
...  
Keyword(s):  
Synthesis Method ◽  
Leaf Disc ◽  
Cytotoxic Activities ◽  
Antibacterial Effects ◽  
Mythimna Separata ◽  
One Pot ◽  
Biochemical Effects ◽  
Third Stage ◽  
Mcf 7

The β-carboline alkaloids possess a wide diversity of important biochemical effects and pharmacological properties. A series of β-carboline derivatives were synthesized from L-tryptophan through the Pictet-Spengler reaction and oxidation of K2Cr2O7 by a sequential one-pot synthesis method. In Vitro antibacterial, insecticidal, and cytotoxic activities of all synthesized compounds were investigated by the tablet diffusion, leaf disc, and MTT methods, respectively. Some of the compounds (1-1, 1-2, 1-3 and 1-12) exhibited obvious antibacterial effects and some (1-3) had significant cytotoxic activities against tumor cells 3LL, MCF-7, BGC-823 and QGY-7701, with IC50 values of 7.79, 5.75, 3.53 and 4.02 μg/mL, respectively. No insecticidal activity against third stage instar larvae of Mythimna separata Walker were observed under the tested concentration.

Synthesis, Characterized and Biological Activities of Chalcone Derivatives

2012 ◽  
Vol 535-537 ◽  
pp. 2540-2543
Author(s):  
Xiao Yang Qiu ◽  
Su Zhi Li ◽  
An Ran Shi ◽  
Qiao Li Yue
Keyword(s):  
Tumor Cell ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Biological Activities ◽  
Tumor Cell Line ◽  
Cytotoxic Activities ◽  
Epidermoid Tumor ◽  
Chalcone Derivatives

A series of 4-nitrochalcones (compounds 1-10) are synthesized and characterized. The products synthesized are evaluated for their cytotoxic activities in vitro. Among the compounds tested, (E)-3-(4-nitrophenyl)-1-(4-nitrophenyl)prop-2-en-1-one (1) showes the favorable in vitro cytotoxic activity against human nasopharyngeal epidermoid tumor cell line KB.

scholarly journals Design, Synthesis, Physicochemical, Drug-likeness Properties of Quercetin Derivatives and Their Effect On MCF-7 Cell Line and Free Radicals

2021 ◽  
Author(s):  
Sulakshana Shankar ◽  
Jaishree Vaijanathappa ◽  
Ashish Wadhwani ◽  
Mahendran Sekar
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Drug Screening ◽  
Synthesis Method ◽  
Oral Drug ◽  
One Pot ◽  
Quercetin Derivatives ◽  
Study Results ◽  
Mcf 7

Abstract In the present study, four novel quercetin derivatives were designed and synthesised by one pot synthesis method using benzoic acid and its derivatives. The synthesised compounds were screened for physicochemical and drug-likeness properties, evaluated for in vitro antioxidant assays such as hydrogen peroxide (H2O2) and 2,2-diphenyl-1-picryl hydrazyl (DPPH), cytotoxicity study on breast cancer cell line MCF-7 and performed molecular docking against the nitric oxide synthase (iNOS) enzyme 4NOS PDB (Protein Data Bank) ID which is expressed in breast cancer. In the screening of physicochemical and drug-likeness properties, QB, QB1 and QB4 are eligible for oral drug screening and other derivatives QB2 and QB3 were not eligible for oral drug screening. Among all, QB-1 showed highest percentage of inhibition and lowest IC50 value in both the assays. The docking results displayed that QB-2 showed highest docking score and exhibited highest cytotoxicity against MCF-7 cell line and the study results conclude that QB1 and QB2 compounds can be further explored to in vivo anticancer activity.

scholarly journals Cytotoxic activities of Methanolic and Chloroform Extract of Cryptocarya Massoy (Oken) Kosterm. Bark on MCF-7 human breast cancer cell line

2018 ◽  
Vol 9 (1) ◽  
pp. 57-62
Author(s):  
Yuli Widiyastuti ◽  
Ika Yanti M. Sholikhah ◽  
Sari Haryanti
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Mtt Assay ◽  
Cancer Cell Line ◽  
Chloroform Extract ◽  
Cytotoxic Activities ◽  
Litsea Cubeba ◽  
Mcf 7

Abstrak Latar Belakang. Krangean [Litsea cubeba (Lour.) Pers.] Adalah salah satu tanaman aromatik purba di Indonesia. Tanaman ini adalah anggota keluarga Lauraceae, tumbuh liar di dataran tinggi Sumatera, Kalimantan, dan pulau Jawa. Aktivitas antikanker tanaman ini belum banyak dieksplorasi. Penelitian ini bertujuan untuk mengetahui kandungan fitokimia dan aktivitas sitotoksik ekstrak buah krangean pada sel kanker manusia secara in vitro. Metode. Kloroform dan metanol digunakan untuk mempererat bubuk buah kering selama 3x24 jam. Senyawa fitokimia utama ditandai dengan KLT (kromatografi lapis tipis). Uji MTT dilakukan untuk mengamati morfologi dan viabilitas kanker serviks HeLa, kanker payudara MCF-7, dan sel HEPG2 hepar. Hasil. Hasil penelitian menunjukkan bahwa karakterisasi KLT ekstrak kloroform dan metanol Litsea cubeba menunjukkan profil yang sama, dengan senyawa utama yang ditemukan adalah terpenoid dan alkaloid. Uji MTT menemukan bahwa kedua ekstrak memiliki penghambatan kuat pada sel HeLa. Ekstrak kloroform menunjukkan aktivitas sitotoksik yang lebih kuat dibandingkan dengan metanol, dengan nilai IC50 masing-masing 33,7 dan 64,8 μg / mL. Kesimpulan. Esktrak kloroform dan ekstrak metanol dari Litsea cubeba memiliki aktivitas yang kuat terhadap sel HeLa dan aktivitas sedang terhadap sel HEPG2 dan MCF-7.  Selanjutnya disarankan untuk dilakukan penelitian lebih lanjut untuk mengathui senyawa aktif L. cubeba (Lour.) Pers. yang memiliki aktivitas antikanker potensial. Kata kunci: Litsea cubeba (Lour.) Pers., sitotoksik, HeLa, MCF-7, HebG2, MTT assay   Abstract Background. Krangean [Litsea cubeba (Lour.) Pers.] is one of ancient aromatic plants in Indonesia. This plant is the member of Lauraceae family, growing wild on the highlands of Sumatera, Kalimantan, and Java island. The anticancer activity of this plant haven’t been explored extensively.This research aimed to investigate phytochemical content and cytotoxic activity of krangean fruits extract on human cancer cell line in vitro. Method. Chloroform and methanol were used to macerate dried fruits powder for 3x24 hours. Major phytochemical compounds was characterized by TLC (thin layer chromatography). MTT assay was done to observe morphology and viability of HeLa cervical cancer, MCF-7 breast cancer, and HepG2 hepar cancer cell line. Result. The results showed that TLC characterization of chloroform and methanolic extracts of Litsea cubeba revealed similar profile, with the major compound found are terpenoid and alkaloid. The MTT assay found that both extracts have strong inhibition on HeLa cell line. Chloroform extract exhibited stronger cytotoxic activities compared to methanol, with the IC50 values of 33,7 and 64,8 μg/mL respectively. While, the both extract have moderate cytotoxic activities to HEPG2 and MCF-7 cancer cell line indicated by IC50value more than 100 mg/mL. Conclusion. Chloroform and methanolic extract of Litsea cubeba have a strong activity againts HeLa cancer cell lines and moderate activity to HEPG2 and MCF-7, thought chloroform extract of Litsea cubeba has stronger effect on cancer cell line viability. It is well recommended for further studies to investigate the active compound of L. cubeba (Lour.) Pers. for potential anticancer activity.   Key words: Litsea cubeba (Lour.) Pers., cytotoxic, HeLa, MCF-7, HebG2, MTT assay

scholarly journals Antioxidant and cytotoxic activity of mono- and bissalicylic acid derivatives

2014 ◽  
pp. 173-189 ◽  
Author(s):  
Evgenija Djurendic ◽  
Marina Savic ◽  
Suzana Jovanovic-Santa ◽  
Marija Sakac ◽  
Vesna Kojic ◽  
...  
Keyword(s):  
Cell Line ◽  
Tumor Cell Line ◽  
Malignant Cell ◽  
Qsar Modeling ◽  
Scavenger Activity ◽  
Alkaline Conditions ◽  
Salicylic Acid Derivatives ◽  
New Compounds ◽  
Mcf 7

A simple synthesis of mono- and bis-salicylic acid derivatives 1-10 by the transesterification of methyl salicylate (methyl 2-hydroxybenzoate) with 3-oxapentane-1,5-diol, 3,6- dioxaoctane-1,8-diol, 3,6,9-trioxaundecane-1,11-diol, propane-1,2-diol or 1-aminopropan- 2-ol in alkaline conditions is reported. All compounds were tested in vitro on three malignant cell lines (MCF-7, MDA-MB-231, PC-3) and one non-tumor cell line (MRC- 5). Strong cytotoxicity against prostate PC-3 cancer cells expressed compounds 3, 4, 6, 9 and 10, all with the IC50 less than 10 ?mol/L, which were 11-27 times higher than the cytotoxicity of antitumor drug doxorubicin. All tested compounds were not toxic against the non-tumor MRC-5 cell line. Antioxidant activity of the synthesized derivatives was also evaluated. Compounds 2, 5 and 8 were better OH radical scavengers than commercial antioxidants BHT and BHA. The synthesized compounds showed satisfactory scavenger activity, which was studied by QSAR modeling. A good correlation between the experimental variables IC50 DPPH and IC50 OH and MTI (molecular topological indices) molecular descriptors and CAA (accessible Connolly solvent surface area) for the new compounds 1, 3, and 5 was observed.

A Novel Triazole Derivative Drug Presenting In Vitro and In Vivo Anticancer Properties

2018 ◽  
Vol 18 (17) ◽  
pp. 1483-1493
Author(s):  
Ricardo Imbroisi Filho ◽  
Daniel T.G. Gonzaga ◽  
Thainá M. Demaria ◽  
João G.B. Leandro ◽  
Dora C.S. Costa ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Hepatic Function ◽  
Anticancer Properties ◽  
Mcf 7

Background: Cancer is a major cause of death worldwide, despite many different drugs available to treat the disease. This high mortality rate is largely due to the complexity of the disease, which results from several genetic and epigenetic changes. Therefore, researchers are constantly searching for novel drugs that can target different and multiple aspects of cancer. Experimental: After a screening, we selected one novel molecule, out of ninety-four triazole derivatives, that strongly affects the viability and proliferation of the human breast cancer cell line MCF-7, with minimal effects on non-cancer cells. The drug, named DAN94, induced a dose-dependent decrease in MCF-7 cells viability, with an IC50 of 3.2 ± 0.2 µM. Additionally, DAN94 interfered with mitochondria metabolism promoting reactive oxygen species production, triggering apoptosis and arresting the cancer cells on G1/G0 phase of cell cycle, inhibiting cell proliferation. These effects are not observed when the drug was tested in the non-cancer cell line MCF10A. Using a mouse model with xenograft tumor implants, the drug preventing tumor growth presented no toxicity for the animal and without altering biochemical markers of hepatic function. Results and Conclusion: The novel drug DAN94 is selective for cancer cells, targeting the mitochondrial metabolism, which culminates in the cancer cell death. In the end, DAN94 has been shown to be a promising drug for controlling breast cancer with minimal undesirable effects.

Synthesis, Docking Study, Cytotoxicity, Antioxidant, and Anti-microbial Activities of Novel 2,4-Disubstituted Thiazoles Based on Phenothiazine

2020 ◽  
Vol 17 (2) ◽  
pp. 151-159
Author(s):  
Tran Nguyen Minh An ◽  
Pham Thai Phuong ◽  
Nguyen Minh Quang ◽  
Nguyen Van Son ◽  
Nguyen Van Cuong ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Antimicrobial Activities ◽  
Significant Activity ◽  
Thiazole Derivatives ◽  
Ligand Interaction ◽  
Ic50 Value ◽  
Mcf 7

: A series of novel 1,3-thiazole derivatives (5a-i) with a modified phenothiazine moiety were synthesized and tested against cancer cell line MCF-7 for their cytotoxicity. Most of them (5a-i) were less cytotoxic or had no activity against MCF-7 cancer cell line. Material and Methods: The IC50 value of compound (4) was 33.84 μM. The compounds (5a-i) were also evaluated for antimicrobial activities, but no significant activity was observed. The antioxidant activity was conducted for target compounds (5a-i). The IC50 value of compound (5b) was 0.151mM. Results: The total amount of energy, ACE (atomic contact energy), energy of receptor (PDB: 5G5J), and ligand interaction of structure (4) were found to be 22.448 Kcal.mol-1 , -247.68, and -91.91 Kcal.mol-1, respectively. The structure (4) is well binded with the receptor because the values of binding energy, steric energy, and the number of hydrogen bondings are -91.91, 22.448 kcal.mol-1, and 2, respectively. It shows that structure (4) has good cytotoxicity with MCF-7 in vitro. Conclusion: The increasing of docking ability of structures (5a-i) with the receptor is presented in increasing order as (5f)>(5e)>(5g)>(5a)>(5b)>(5d)>(5c)>(5i)>(5h). The structure bearing substitution as thiosemicarbazone (4), nitrogen heterocyclic (5f), halogen (5e), and azide (5g) showed good cytotoxicity activity in vitro.

Design, Synthesis and In Vitro Anti-Cancer Evaluation of Novel Derivatives of 2-(2-Methyl-1,5-diaryl-1H-pyrrol-3-yl)-2-oxo-N-(pyridin-3- yl)acetamide

2020 ◽  
Vol 16 (3) ◽  
pp. 340-349
Author(s):  
Ebrahim S. Moghadam ◽  
Farhad Saravani ◽  
Ernest Hamel ◽  
Zahra Shahsavari ◽  
Mohsen Alipour ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Peripheral Neuropathy ◽  
Cell Line ◽  
Normal Cell ◽  
Caspase 3 ◽  
Annexin V ◽  
Normal Cell Line ◽  
Anti Cancer ◽  
Mcf 7

Objective: Several anti-tubulin agents were introduced for the cancer treatment so far. Despite successes in the treatment of cancer, these agents cause toxic side effects, including peripheral neuropathy. Comparing anti-tubulin agents, indibulin seemed to cause minimal peripheral neuropathy, but its poor aqueous solubility and other potential clinical problems have led to its remaining in a preclinical stage. Methods: Herein, indibulin analogues were synthesized and evaluated for their in vitro anti-cancer activity using MTT assay (on the MCF-7, T47-D, MDA-MB231 and NIH-3T3 cell lines), annexin V/PI staining assay, cell cycle analysis, anti-tubulin assay and caspase 3/7 activation assay. Results: One of the compounds, 4a, showed good anti-proliferative activity against MCF-7 cells (IC50: 7.5 μM) and low toxicity on a normal cell line (IC50 > 100 μM). All of the tested compounds showed lower cytotoxicity on normal cell line in comparison to reference compound, indibulin. In the annexin V/PI staining assay, induction of apoptosis in the MCF-7 cell line was observed. Cell cycle analysis illustrated an increasing proportion of cells in the sub-G-1 phase, consistent with an increasing proportion of apoptotic cells. No increase in G2/M cells was observed, consistent with the absence of anti-tubulin activity. A caspase 3/7 assay protocol showed that apoptosis induction by more potent compounds was due to activation of caspase 3. Conclusion: Newly synthesized compounds exerted acceptable anticancer activity and further investigation of current scaffold would be beneficial.

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