Evaluation of Cytotoxic Effect of Punica granatum L. var spinosa extracts on Malignant Cell Line MCF-7 in vitro

Breast cancer is the most common cancer among women and in order to create alternative treatments different types of in vivo and in vitro studies have used various plant-based therapeutic agents. Humic acid (HA) induces apoptosis and has various pharmacological properties including anti-inflammatory and anti-proliferative effects. In our study, we examined the cytotoxic effects of HA at concentrations of 5, 10, 20, 50 and 100 μg/mL in human breast adenocarcinoma MCF-7 cell line for 24 and 48 h. By using MTT method, it has been found out that HA 100 g/mL had cytotoxic effect on human breast adenocarcinoma MCF-7 cell line at both 24 and 48 h; also found out that the effective dose of HA at the same time (24 and 48 h) was 50 μg/mL. The results of our study will shed light on the development of alternative therapeutic approaches in the treatment of cancer by evaluating the cytotoxic effect of HA.

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Effect of bioactive compounds in ginger extract on cancer cell lines In vitro.

Journal of Biotechnology Research Center ◽

10.24126/jobrc.2012.6.2.219 ◽

2012 ◽

Vol 6 (2) ◽

pp. 34-41

Author(s):

Mohammed S. Mohammed Al-Zobaidi ◽

Muayad S. Shawkat ◽

Abd Al-Amer N. Galoob

Keyword(s):

Cell Line ◽

Cell Lines ◽

Exposure Time ◽

Crude Extract ◽

Cytotoxic Effect ◽

Ethanolic Extract ◽

Malignant Cell ◽

Mammary Adenocarcinoma ◽

Ginger Extract

his study was designed to detect the active compounds found in ethanolic crude extract of Zingeber officinale rhizome. Chemical detection of extract appeared that the ethanolic extract contain flavonoid, saponin, glycosids, phenols, resins, volatile oils, tannins, terpins and steroids while alkaloids and cumarines gave negative results. Different concentrations were prepared from ethanolic extract starting from (1-1000) µg/ml to evaluate the cytotoxic effect of ethanolic extract on two malignant cell lines, human laryngeal carcinoma (HEP-2) cell line and murine mammary adenocarcinoma (AMN-3) cell line, exposure periods of cell lines were measured at (24, 48, 72)hr in a microtitration plate under complete sterile conditions. Results showed that, Ethanolic crude extract exhibited time-dependent cytotoxic effect of all concentrations after exposure for 24hr on cancer and transformed cells lines, and the 100 µg/ml gave the highest inhibition rate for AMN-3 86.2% after 24hr of exposure time and the cytotoxic effect of the extract started at lowest concentrations on HEP-2 cell line after 48hr of exposure reached which the best concentration 600 µg/ml gave the highest inhibition cell growth 73.4% after 48hr of exposure time.

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Phytochemical and Cytotoxicity Evaluation of Lagerstroemia speciosa (L.) Leaves Extract by MCF-7 Cell Line and Brine Shrimp Lethality Bioassay

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.10.1.6 ◽

2020 ◽

Vol 10 (01) ◽

pp. 40-44

Author(s):

ABM Helal Uddin ◽

Abul Kalam Azad

Keyword(s):

Cell Line ◽

Brine Shrimp ◽

Cytotoxic Effect ◽

Potassium Dichromate ◽

Positive Control ◽

Phytochemical Screening ◽

Brine Shrimp Lethality ◽

Lagerstroemia Speciosa ◽

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This study aimed to investigate the cytotoxicity of Lagerstroemia speciosa (L.) leaves crude extract. It has been reported to show various bioactivities. The phytochemical screening of the extract has been carried qualitatively. The cytotoxic effect was determined through in vitro MTT assay of MCF-7 cell line, and brine shrimp lethality bioassay. The presence or absence of alkaloid, carbohydrate, glycoside, saponin, terpene, steroid, phenol, and flavonoid in the extract was determined through the qualitative tests. The extract showed cell viability of 100% (1.95–3.9 μL/mL), 96% (1.95 μL/mL), ≈ 95% (3.9–15.62 μL/mL) and 88% (250 μL/mL) while the mortality of brine shrimp nauplii was from 5% to 10% (7.8 – 125 μL/mL) respectively. For both assays, DMSO of 1 and 0.1% were used as vehicle controls, while the potassium dichromate as the positive control for the brine shrimp only. These results proved the leaves extract to be non-toxic.

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Antioxidant and cytotoxic activity of mono- and bissalicylic acid derivatives

Acta periodica technologica ◽

10.2298/apt1445173d ◽

2014 ◽

pp. 173-189 ◽

Cited By ~ 2

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 ◽

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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.

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

Current Topics in Medicinal Chemistry ◽

10.2174/1568026618666180917100640 ◽

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.

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

Current Organic Synthesis ◽

10.2174/1570179417666191220100614 ◽

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.

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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

Medicinal Chemistry ◽

10.2174/1573406415666190425153717 ◽

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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