Anticancer activity of food grade nanoemulsions on hepatic cancer cells: a comparative study

Mapping Intimacies ◽

10.21203/rs.3.rs-61937/v1 ◽

2020 ◽

Author(s):

Sayyeda Hira Hassan ◽

Muhammad Rehan Khan

Keyword(s):

Olive Oil ◽

Cell Line ◽

Mtt Assay ◽

Anticancer Agents ◽

Cancer Cell Line ◽

Flax Seed ◽

Anticancer Activities ◽

Ic50 Value ◽

Flax Seeds

Abstract The current study was aimed to prepare stable NEs from plant oils to evaluate their cytotoxic effect on HepG2 cells. Oils form three different samples (flax seeds, cloves and olives) were extracted. NEs from these oils were prepared separately by ultrasonication method. After characterization of stable NEs, they were evaluated for their antioxidant and anticancer activities. Extracted oils and their NEs were applied separately to HepG2 cell line to construct a comparison and MTT assay was used for this purpose. Prepared NEs were found more effective against cancer cell line as compared to their respective oils. MTT assay showed efficacy of NEs in reducing cell viability with IC50 value of 10 µl (flax seed oil), 25 µl (clove oil NE) and 1 µl (olive oil NE), and was safe to normal cells. The results of the current study revealed that NEs prepared from flax seed, clove and olive oil have the potential for further development as anticancer agents.

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Synthesis and Antibacterial / Anticancer Activities of Compounds Containing Pyrazole Ring Linked to Piperazines

Current Bioactive Compounds ◽

10.2174/1573407215666190111124513 ◽

2020 ◽

Vol 16 (4) ◽

pp. 419-431

Author(s):

Kishore K. Valluri ◽

Tejeswara R. Allaka ◽

IV Kasi Viswanath ◽

Nagaraju PVVS

Keyword(s):

Cell Line ◽

Cancer Cell ◽

Anticancer Agents ◽

Cancer Cell Line ◽

Pyrazole Ring ◽

Therapeutic Effects ◽

Anticancer Activities ◽

Human Colon Cancer ◽

Parent Molecule ◽

Wide Range

Background: Many pyrazole piperazine derivatives are known to exhibit a wide range, thus being attractive for the drug design and synthesis of interesting class of widely studied heterocyclic compounds. It is therefore necessary to devote continuing effort for the identification and development of New Chemical Entities (NCEs) as potential antibacterial and anticancer agents to address serious health problems. Methods: A series of new compounds containing pyrazole ring linked to a piperazine hydrochloride moiety were synthesized and screened for their antibacterial activity, cytotoxicity of novel scaffolds are described by variation in therapeutic effects of parent molecule. The structure variants were characterized by using a blend of spectroscopic 1H NMR, 13C NMR, IR, Mass and chromatographic techniques. Results: When tested for in vitro antibacterial and anticancer activities, several of these compounds showed good activities. The target compounds 9b, 9a and 9e exhibited a high degree of anticancer activity against human colon cancer cell line Caco-2 and human breast cancer cell line MDAMB231. Further, 9a, 9b, 9d, and 9h showed better activity towards four medically relevant organisms; Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Klebsiella Species compared to CPF. In the present investigation, cheminfomatics tools Molinspiration, 2003 and MolSoft, 2007 for the prediction of insilico molecular properties and drug likeness for the target compounds 9a-h was evaluated and positive results were observed. Conclusion: Our study revealed that the molecular framework presented here could be a useful template for the identification of novel small molecules as promising antibacterial/ anticancer agents.

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Assessment of the Cytotoxic Activity of Triphala: A Semisolid Traditional Formulation on HepG2 Cancer Cell Line

BioMed Research International ◽

10.1155/2021/6689568 ◽

2021 ◽

Vol 2021 ◽

pp. 1-7

Author(s):

Ali Sahragard ◽

Zohreh Alavi ◽

Zohreh Abolhassanzadeh ◽

Mahmoodreza Moein ◽

Afshin Mohammadi-Bardbori ◽

...

Keyword(s):

Natural Products ◽

Cytotoxic Activity ◽

Cell Line ◽

Cancer Cell ◽

Mtt Assay ◽

Cancer Cell Line ◽

Control Group ◽

Anticancer Activities ◽

Human Liver Cancer Cell ◽

Human Liver Cancer

Cancer chemotherapies may result in resistance, and therefore, contemporary treatments including natural products may find an increasing consideration. As per Persian medicine (PM), many natural products have been used for malignant and chronic diseases. Triphala, with a combination of Terminalia chebula Retz., Terminalia bellirica Retz., Phyllanthus emblica L., and honey, is a multi-ingredient traditional formulation attributed to anticancer activities in PM. This study is aimed at evaluating the cytotoxic activity of this preparation on HepG2, the human liver cancer cell line. Hydroalcoholic extracts were prepared from the formulation and its components. Compared with the control and Cisplatin, the extracts were tested using MTT assay at different concentrations. All concentrations of the preparation, as well as Cisplatin, were effective significantly against HepG2 cells. All extract preparations at multiple concentrations were significantly effective as evidenced by MTT assay when compared to the control group. The IC50 level for Triphala extract was 77.63 ± 4.3 μ g / ml . Based on the results, Triphala and its components have cytotoxic activity on the HepG2 cancer cell line and they can reduce the survival rate significantly.

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Anticancer Evaluation and Docking Study of New Bifunctional Phthalazine Derivatives

Current Organic Synthesis ◽

10.2174/2211556006666170927155809 ◽

2018 ◽

Vol 15 (3) ◽

pp. 414-422 ◽

Cited By ~ 2

Author(s):

Marwa G. El-Gazzar ◽

Hala M. Aly

Keyword(s):

Anticancer Activity ◽

Cell Line ◽

Anticancer Agents ◽

Active Site ◽

Cancer Cell Line ◽

Docking Study ◽

Quinazoline Derivative ◽

Spectroscopic Measurements ◽

Ic50 Value

Aims and Objective: A series of novel phthalazine derivatives was synthesized with versatile, readily accessible electrophilic and nucleophilic reagents. The newly synthesized compounds were confirmed by the results of spectroscopic measurements. Hence, their potential clinical application investigated in particular for cancer treatment. Materials and Methods: The newly synthesized compounds were characterized by spectroscopic measurements and were tested for their in vitro anticancer activity by MTT assay against human liver cancer cell line. Docking study of all the synthesized compounds was performed within the active site of the enzyme VEGFR-2 (Vascular Endothelial Growth Factor Receptor-2). Results: The quinazoline derivative 12 emerged as the most potent compound in this study with an IC50 value of 5.4 µM. Docking study showed that the synthesized compounds were fit in the VEGFR-2 active site almost at the same position of sorafenib and vatalanib with comparable docking scores (-15.20 to -8.92 was kcal/mol). Conclusion: we have synthesized a novel series of phthalazine derivatives and evaluated their potential anticancer activity against HEPG2 cell line. The quinazoline derivative 12 emerged as the most potent compound in this study with an IC50 value of 5.4 µM. The SAR and docking studies pointed out that rigidification of the structure resulted in better activity and better binding within the active site of VEGFR-2 as in compounds 3, 5, 6 and 12. These results introduced new phthalazine derivatives having promising activity which could lead to the development of more potent anticancer agents.

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Synthesis of Spirooxindole-O-Naphthoquinone-Tetrazolo[1,5-a]Pyrimidine Hybrids as Potential Anticancer Agents

Molecules ◽

10.3390/molecules23092330 ◽

2018 ◽

Vol 23 (9) ◽

pp. 2330 ◽

Cited By ~ 10

Author(s):

Liqiang Wu ◽

Yunxia Liu ◽

Yazhen Li

Keyword(s):

Cell Line ◽

Anticancer Agents ◽

Normal Cell ◽

Antitumor Agents ◽

Cancer Cell Line ◽

The Novel ◽

Normal Cell Line ◽

Pharmaceutical Applications ◽

Ic50 Value ◽

High Cytotoxic Activity

A series of novel spirooxindole-O-naphthoquinone-tetrazolo[1,5-a]pyrimidine hybrids were designed, synthesized and evaluated as potent antitumor agents. These hybrids exhibited relatively high cytotoxic activity against cancer cell line HepG2 (IC50 = 2.86–36.34 μM), while normal cell line LO2 was less sensitive to these hybrids (IC50 = 36.37–248.39 μM). On the whole, among all the compounds tested, compound 4e, with a mean IC50 value of 2.86 μM, was the most active. The novel hybrids may find their pharmaceutical applications after further investigations.

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Synthesis of Flavone Derivatives via N-Amination and Evaluation of Their Anticancer Activities

Molecules ◽

10.3390/molecules24152723 ◽

2019 ◽

Vol 24 (15) ◽

pp. 2723 ◽

Cited By ~ 1

Author(s):

Ni Zhang ◽

Jin Yang ◽

Ke Li ◽

Jun Luo ◽

Su Yang ◽

...

Keyword(s):

Cell Line ◽

Biological Activities ◽

Cancer Cell Line ◽

Prostate Cancer Cell Line ◽

Antibacterial Activities ◽

Anticancer Activities ◽

Structure Activity ◽

Ic50 Value ◽

Erythroleukemia Cell ◽

Flavone Derivatives

Seventeen new flavone derivatives substituted at the 4′-OH position were designed, synthesized and evaluated for their anticancer and antibacterial activities. Among them, compounds 3, 4, 6f, 6e, 6b, 6c and 6k demonstrated the most potent antiproliferative activities against a human erythroleukemia cell line (HEL) and a prostate cancer cell line (PC3). The results also showed that the IC50 value of compounds 3, 4, 6f, 6e, 6b, 6c and 6k were close to that of the anticancer drug cisplatin (DDP) and lower than that of apigenin. All of the derivatives did not present antibacterial activities. The structure–activity relationships evaluation showed that the configuration of methyl amino acid might affect their biological activities.

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Novel 7-substituted Fluoroquinolone Citrate Conjugates as Powerful Antibacterial and Anticancer Agents: Synthesis and Molecular Docking Studies

Current Organic Chemistry ◽

10.2174/1877946809666191007125408 ◽

2019 ◽

Vol 23 (18) ◽

pp. 1992-2003

Author(s):

Tejeswara R. Allaka ◽

Jaya S. Anireddy

Keyword(s):

Staphylococcus Aureus ◽

Cell Line ◽

Anticancer Agents ◽

Docking Studies ◽

Significant Activity ◽

Anticancer Activities ◽

Lipinski’S Rule ◽

Ic50 Value ◽

Pharmacokinetic Properties ◽

Lipinski’S Rule Of Five

In this study, the synthesis and evaluation of norfloxacin analogues of dimethyl citrate conjugates were described and their antibacterial and anticancer activities were assessed. The cognate 7-substituted norfloxacin citrate conjugates are active against various strains of bacteria, including MRSA (methicillin-resistant Staphylococcus aureus) with higher activity than ciprofloxacin. Screening results indicated that compound 10 possessed good antibacterial activity against several microorganisms, with MIC values in the range of 0.16-0.35 mg/mL and MBCs in the range of 0.55-0.84 mg/mL. Experiments indicated that 9 demonstrated the most significant activity towards the HCT-15 cell line with IC50 value 8.2 ± 0.139 and against the HT-29 cell line with IC50 8.9 ± 0.122. The title compounds were also evaluated for determining the molecular and pharmacokinetic properties and drug-likeness model scores by using the Molinspiration-2008 and MolSoft-2007 softwares. The region isomeric conjugates followed the Lipinski’s rule of five can be considered as potential antibacterial and anticancer bioavailable oral leads. Compounds 9 and 10 possessed maximum drug-likeness scores. The docking pose interactions of target compounds with the active site of enzyme PDB: 2ZCS of Staphylococcus aureus were estimated by using Autodock 4.2, to calculate the affinity, binding orientation of the ligand with the target protein and to explore the finest conformations. The target compounds, 7, 8, 9, 10, with protein, were loaded separately into Auto dock tools (ADT) and evaluated. The citrate conjugates, 8, 9, showed better docking scores with amino acids Lys17, Ser21, Val268, Lys273 and Arg171, Arg265, Val268, Val273 with the binding energy -5.70, -5.57 kcal/mol and dissociation constant 66.62, 82.13 µM respectively.

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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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Bimetallic Iron–Palladium Catalyst System as a Lewis-Acid for the Synthesis of Novel Pharmacophores Based Indole Scaffold as Anticancer Agents

Molecules ◽

10.3390/molecules26082212 ◽

2021 ◽

Vol 26 (8) ◽

pp. 2212

Author(s):

Mohammad Shahidul Islam ◽

M. Ali ◽

Abdullah Mohammed Al-Majid ◽

Abdullah Saleh Alamary ◽

Saeed Alshahrani ◽

...

Keyword(s):

Prostate Cancer ◽

Cell Line ◽

Cell Lines ◽

Cancer Cell ◽

Anticancer Agents ◽

Palladium Catalyst ◽

Cancer Cell Line ◽

Catalyst System ◽

Mcf 7 ◽

Iron Palladium

The Friedel–Crafts reaction between substituted indoles as nucleophiles with chalcones-based benzofuran and benzothiophene scaffolds was carried out by employing a highly efficient bimetallic iron–palladium catalyst system. This catalytic approach produced the desired bis-heteroaryl products with low catalyst loading, a simple procedure, and with acceptable yield. All synthesized indole scaffolds 3a–3s were initially evaluated for their cytotoxic effect against human fibroblast BJ cell lines and appeared to be non-cytotoxic. All non-cytotoxic compounds 3a–3s were then evaluated for their anticancer activities against cervical cancer HeLa, prostate cancer PC3, and breast cancer MCF-7 cell lines, in comparison to standard drug doxorubicin, with IC50 values 1.9 ± 0.4 µM, 0.9 ± 0.14 µM and 0.79 ± 0.05 µM, respectively, and appeared to be moderate to weak anticancer agents. Fluoro-substituted chalcone moiety-containing compounds, 3b appeared to be the most active member of the series against cervical HeLa (IC50 = 8.2 ± 0.2 µM) and breast MCF-7 cancer cell line (IC50 = 12.3 ± 0.04 µM), whereas 6-fluroindol-4-bromophenyl chalcone-containing compound 3e (IC50 = 7.8 ± 0.4 µM) appeared to be more active against PC3 prostate cancer cell line.

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Synthesis and characterization of a new series of thiadiazole derivatives as potential anticancer agents

Heterocyclic Communications ◽

10.1515/hc-2020-0002 ◽

2020 ◽

Vol 26 (1) ◽

pp. 6-13 ◽

Cited By ~ 1

Author(s):

Ulviye Acar Çevik ◽

Derya Osmaniye ◽

Serkan Levent ◽

Begüm Nurpelin Sağlik ◽

Betül Kaya Çavuşoğlu ◽

...

Keyword(s):

Anticancer Agents ◽

Biological Activities ◽

Cancer Cell Line ◽

Chemotherapeutic Agents ◽

Anticancer Activities ◽

Normal Tissues ◽

H Nmr ◽

Wide Range ◽

Thiadiazole Derivatives ◽

Low Efficiency

AbstractCancer is one of the most common causes of death in the world. Despite the importance of combating cancer in healthcare systems and research centers, toxicity in normal tissues and the low efficiency of anticancer drugs are major problems in chemotherapy. Nowadays the aim of many medical research projects is to discover new safer and more effective anticancer agents. 1,3,4-Thiadiazole compounds are important fragments in medicinal chemistry because of their wide range of biological activities, including anticancer activities. The aim of this study was to determine the capacity of newly synthesized 1,3,4-thiadiazole compounds as chemotherapeutic agents. The structures of the obtained compounds were elucidated using 1H-NMR, 13C-NMR and mass spectrometry. Although the thiadiazole derivatives did not prove to be significantly cytotoxic to the tumour tissue cultures, compound 4i showed activity against the C6 rat brain cancer cell line (IC50 0.097 mM) at the tested concentrations.

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