scholarly journals Synthesis and In Vitro Antitumor Activity of Novel Bivalent β-Carboline-3-carboxylic Acid Derivatives with DNA as a Potential Target

2018 ◽  
Vol 19 (10) ◽  
pp. 3179 ◽  
Author(s):  
Hongling Gu ◽  
Na Li ◽  
Jiangkun Dai ◽  
Yaxi Xi ◽  
Shijun Wang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Apoptosis ◽  
Docking Studies ◽  
In Vitro Cytotoxicity ◽  
Dependent Manner ◽  
Cycle Arrest ◽  
Dna Binding Affinity ◽  
Dose Dependent ◽  
Mcf 7

A series of novel bivalent β-carboline derivatives were designed and synthesized, and in vitro cytotoxicity, cell apoptosis, and DNA-binding affinity were evaluated. The cytotoxic results demonstrated that most bivalent β-carboline derivatives exhibited stronger cytotoxicity than the corresponding monomer against the five selected tumor cell lines (A549, SGC-7901, Hela, SMMC-7721, and MCF-7), indicating that the dimerization at the C3 position could enhance the antitumor activity of β-carbolines. Among the derivatives tested, 4B, 6i, 4D, and 6u displayed considerable cytotoxicity against A549 cell line. Furthermore, 4B, 6i, 4D, and 6u induced cell apoptosis in a dose-dependent manner, and caused cell cycle arrest at the S and G2/M phases. Moreover, the levels of cytochrome C in mitochondria, and the expressions of bcl-2 protein, decreased after treatment with β-carbolines, which indicated that 6i and 6u could induce mitochondria-mediated apoptosis. In addition, the results of UV-visible spectral, thermal denaturation, and molecular docking studies revealed that 4B, 6i, 4D, and 6u could bind to DNA mainly by intercalation.

Study on the antitumor activity and mechanism of novel targeted nanodrugs based on miRNA in cervical cancer

2020 ◽  
Vol 10 (8) ◽  
pp. 1218-1223
Author(s):  
Xinping Chen ◽  
Zhichao Ma ◽  
Juan Zhu ◽  
Weihua Xu ◽  
Junjie Hu ◽  
...  
Keyword(s):  
Gene Expression ◽  
Flow Cytometry ◽  
Antitumor Activity ◽  
A549 Cell ◽  
Cell Apoptosis ◽  
Caspase 3 ◽  
A549 Cells ◽  
Dependent Manner ◽  
Double Staining ◽  
Dose Dependent

The aim of this study was to investigate the effect of different concentrations of novel targeted nanodrugs based on miRNA on the antitumor activity and mechanism in cervical carcinoma A549 cells. The MTT method was used to determine the effect of different concentrations of novel targeted nanodrugs based on miRNA on A549 cell proliferation, and annexin V FITC/PI double staining flow cytometry was performed to analyze the effect of these nanodrugs on A549 cell apoptosis. Western blotting was performed to observe the effect of these nanodrugs on the expression of Bax, Bcl-2, and caspase-3-related genes involved in A549 cell apoptosis. Compared with the control group, the novel targeted nanodrugs based on miRNA significantly inhibited the proliferation of A549 cells in a time- and dose-dependent manner. Results of double staining flow cytometry demonstrated that these nanodrugs could increase the apoptotic rate of A549 cells in a dose-dependent manner 48 h later. Western blotting revealed that these nanodrugs could upregulate the expression of Bax and caspase3 genes and downregulate the expression of Bcl-2 gene. Nanodrugs display an obvious antitumor activity in vitro, and the underlying mechanism may be associated with the upregulation of Bax and caspase-3 gene expression and the downregulation of Bcl-2 gene expression.

scholarly journals Solid Polymeric Nanoparticles of Albendazole: Synthesis, Physico-Chemical Characterization and Biological Activity

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 5130 ◽  
Author(s):  
Roxana Racoviceanu ◽  
Cristina Trandafirescu ◽  
Mirela Voicu ◽  
Roxana Ghiulai ◽  
Florin Borcan ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Antitumor Activity ◽  
Benzimidazole Derivative ◽  
Chemical Characterization ◽  
Breast Cancer Cell Lines ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Encapsulation Process ◽  
Mcf 7

Albendazole is a benzimidazole derivative with documented antitumor activity and low toxicity to healthy cells. The major disadvantage in terms of clinical use is its low aqueous solubility which limits its bioavailability. Albendazole was incorporated into stable and homogeneous polyurethane structures with the aim of obtaining an improved drug delivery system model. Spectral and thermal analysis was used to investigate the encapsulation process and confirmed the presence of albendazole inside the nanoparticles. The in vitro anticancer properties of albendazole encapsulated in polyurethane structures versus the un-encapsulated compound were tested on two breast cancer cell lines, MCF-7 and MDA-MB-231, in terms of cellular viability and apoptosis induction. The study showed that the encapsulation process enhanced the antitumor activity of albendazole on the MCF-7 and MDA-MB-23 breast cancer lines. The cytotoxic activity manifested in a concentration-dependent manner and was accompanied by changes in cell morphology and nuclear fragmentation.

scholarly journals A Novel Formulation of Cisplatin with γ-Polyglutamic Acid and Chitosan Reduces Its Adverse Renal Effects: An In Vitro and In Vivo Animal Study

Polymers ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1803
Author(s):  
Masao Sasai ◽  
Kazuma Sakura ◽  
Takayuki Matsuda ◽  
Hiroshi Uyama
Keyword(s):  
Renal Damage ◽  
Chemotherapeutic Agent ◽  
In Vitro Cytotoxicity ◽  
Dependent Manner ◽  
Polyglutamic Acid ◽  
Ph Dependent ◽  
Dose Dependent ◽  
Target Effects

Cisplatin (cis-diamminedichloroplatinum (II); CDDP) is a key chemotherapeutic agent but causes renal damage and other off-target effects. Here, we describe the pharmacological and biochemical characteristics of a novel formulation of CDDP complexed with γ-polyglutamic acid (γ-PGA) and chitosan (CS), γ-PGA/CDDP-CS, developed by complexing CDDP with γ-PGA, then adding CS (15 kDa; 10 mol%/γ-PGA). We analyzed tumor cytotoxicity in vitro, as well as blood kinetics, acute toxicity, and antitumor efficacy in vivo in BALB/cAJcl mice. γ-PGA/CDDP-CS showed pH-dependent release in vitro over 12 days (9.1% CDDP released at pH 7.4; 49.9% at pH 5.5). It showed in vitro cytotoxicity in a dose-dependent manner similar to that of uncomplexed CDDP. In a mesothelioma-bearing mouse model, a 15 mg/kg dose of CDDP inhibited tumor growth regardless of the type of formulation, complexed or uncomplexed; however, all mice in the uncomplexed CDDP group died within 13 days. γ-PGA/CDDP-CS was as effective as free CDDP in vivo but much less toxic.

scholarly journals Grape Seed Procyanidins Inhibit the Growth of Breast Cancer MCF-7 Cells by Down-Regulating the EGFR/VEGF/MMP9 Pathway

2021 ◽  
Vol 16 (2) ◽  
pp. 1934578X2199169
Author(s):  
Fan-ting Kong ◽  
Chen-xi He ◽  
Fan-lei Kong ◽  
Su-fen Han ◽  
Xiang-shun Kong ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Growth Factor ◽  
Cell Apoptosis ◽  
Growth Factor Receptor ◽  
Grape Seed ◽  
Dependent Manner ◽  
Flow Cytometric Data ◽  
Mcf 7

Breast cancer is the most common invasive cancer in women and the second leading cause of cancer death in women. However, it is not clear about its effective treatments. As a potential anticancer agent, grape seed procyanidins (GSPs) have been shown to inhibit the proliferation of various cancer cells in vitro and in vivo. In this study, it was shown that GSPs significantly inhibit MCF-7 cell proliferation in a concentration/time-dependent manner. The flow cytometric data clearly demonstrated that GSPs cause cell cycle arrest in the G2/M phase, followed by cell apoptosis. Moreover, it also confirmed that growth inhibition mediated by treatment with GSPs is related to the induction of apoptosis due to p53 elevation, purportedly by inhibition of the epidermal growth factor receptor (EGFR)/vascular endothelial growth factor (VEGF)/matrix metalloproteinase 9 (MMP9) pathway. Taken together, these findings suggest that GSPs inhibit MCF-7 cells proliferation and induce cell apoptosis by suppressing EGFR/VEGF/MMP9 pathway.

scholarly journals Synthesis and Biological Activities of 2-Substituted Benzimidazole-Metal Complexes

1970 ◽  
Vol 8 (2) ◽  
pp. 131-140 ◽  
Author(s):  
Md Afzal Azam ◽  
BRP Kumar ◽  
R Mazumdar ◽  
B Suresh
Keyword(s):  
Antitumor Activity ◽  
Metal Complexes ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
In Vitro Cytotoxicity ◽  
Bidentate Ligands ◽  
Vis Spectroscopy ◽  
Mcf 7

A series of copper(II) and cobalt(II) coordination compounds with 2-substituted benzimidazole derived monodentate and bidentate ligands have been prepared and characterized by microanalysis, IR and UV-Vis spectroscopy. Synthesized metal complexes have been screened for their in vitro antioxidant and antitumor activity. The complex 4a showed significant nitric oxide free radical scavenging activity (IC50 65μg/ml), while 3i and 3g showed potent superoxide dismutase activity with IC50 of 0.26 and 0.28 μM respectively. In vitro cytotoxicity study with human breast MCF-7 and CNS SF 268 cancer cell lines showed that the most active 2-benzyl-1H-benzimidazole Cu(II) complex 3a inhibited the growth of cancer cells at 20 μM concentration. Keywords: Cu(II) complexes; Co(II) complexes; Benzimidazoles; Antitumor activity. DOI: 10.3329/dujps.v8i2.6027 Dhaka Univ. J. Pharm. Sci. 8(2): 131-140, 2009 (December)

scholarly journals In VitroandIn VivoEvaluation of Polyherbal Formulation against Russell’s Viper and Cobra Venom and Screening of Bioactive Components by Docking Studies

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
G. Sakthivel ◽  
Amitabha Dey ◽  
Kh. Nongalleima ◽  
Murthy Chavali ◽  
R. S. Rimal Isaac ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Natural Antioxidants ◽  
Docking Studies ◽  
Cobra Venom ◽  
Type I ◽  
Dependent Manner ◽  
Russell’S Viper ◽  
Dose Dependent

The present study emphasizes to reveal the antivenom activity ofAristolochia bracteolataLam.,Tylophora indica(Burm.f.) Merrill, andLeucas aspera S.which were evaluated against venoms ofDaboia russelli russelli(Russell’s viper) andNaja naja(Indian cobra). The aqueous extracts of leaves and roots of the above-mentioned plants and their polyherbal (1 : 1 : 1) formulation at a dose of 200 mg/kg showed protection against envenomed mice with LD50doses of 0.44 mg/kg and 0.28 mg/kg against Russell’s viper and cobra venom, respectively. Inin vitroantioxidant activities sample extracts showed free radical scavenging effects in dose dependent manner. Computational drug design and docking studies were carried out to predict the neutralizing principles of type I phospholipase A2(PLA2) from Indian common krait venom. This confirmed that aristolochic acid and leucasin can neutralize type I PLA2enzyme. Results suggest that these plants could serve as a source of natural antioxidants and common antidote for snake bite. However, further studies are needed to identify the lead molecule responsible for antidote activity.

scholarly journals Rosiglitazone Suppresses the Growth and Invasiveness of SGC-7901 Gastric Cancer Cells and Angiogenesis In Vitro via PPARγ Dependent and Independent Mechanisms

PPAR Research ◽  
2008 ◽  
Vol 2008 ◽  
pp. 1-9 ◽  
Author(s):  
Qing He ◽  
Ruiping Pang ◽  
Xin Song ◽  
Jie Chen ◽  
Huixin Chen ◽  
...  
Keyword(s):  
Gastric Cancer ◽  
Cancer Cells ◽  
Dependent Manner ◽  
Gastric Cancer Cells ◽  
Independent Manner ◽  
Cycle Arrest ◽  
G1 Cell Cycle Arrest ◽  
Induced Apoptosis ◽  
Dose Dependent

Although thiazolidinediones (TZDs) were found to be ligands for peroxisome proliferators-activated receptorγ (PPARγ), the mechanism by which TZDs exert their anticancer effect remains unclear. Furthermore, the effect of TZDs on metastatic and angiogenesis potential of cancer cells is unknown. Our results in this paper show that rosiglitazone inhibited SGC-7901 gastric cancer cells growth, caused G1 cell cycle arrest and induced apoptosis in a dose-dependent manner. The effects of rosiglitazone on SGC-7901 cancer cells were completely reversed by treatment with PPARγ antagonist GW9662. Rosiglitazone inhibited SGC-7901 cell migration, invasiveness, and the expression of MMP-2 in dose-dependent manner via PPARγ-independent manner. Rosiglitazone reduced the VEGF induced angiogenesis of HUVEC in dose-dependent manner through PPARγ-dependent pathway. Moreover, rosiglitazone did not affect the expression of VEGF by SGC-7901 cells. Our results demonstrated that by PPARγ ligand, rosiglitazone inhibited growth and invasiveness of SGC-7901 gastric cancer cells and angiogenesis in vitro via PPARγ-dependent or -independent pathway.

Synthesis and antitumor activities of piperazine- and cyclen-conjugated dehydroabietylamine derivatives

2015 ◽  
Vol 21 (4) ◽  
pp. 233-237 ◽  
Author(s):  
Xinbin Yang ◽  
Xiaolin Qin ◽  
Qin Wang ◽  
Yu Huang
Keyword(s):  
Positive Control ◽  
Dependent Manner ◽  
Antitumor Activities ◽  
H Nmr ◽  
Flow Cytometric ◽  
Dependent Inhibition ◽  
Dose Dependent Inhibition ◽  
Dose Dependent ◽  
Mcf 7

AbstractA series of piperazine- and cyclen-conjugated dehydroabietylamine derivatives were synthesized and characterized by 1H NMR, 13C NMR, and HRMS. The in vitro antitumor activities of conjugates 10–13 against MCF-7 and HepG-2 tumor cell lines were evaluated using CCK-8 assay. The results show that the synthesized compounds cause a dose-dependent inhibition of cell proliferation and display different antitumor activities with the IC50 values ranging from 23.56 to 78.92 μm. Moreover, the antitumor activity of conjugate 10 against the MCF-7 cell line is superior to that of the positive control 5-fluorouracil. In addition, flow cytometric assay revealed that the representative conjugate 10 could induce apoptosis in MCF-7 tumor cells in a dose-dependent manner.

Methotrexate-gelonin conjugate – an inhibitor of MCF-7 cells expressing the dihydrofolate receptor

2014 ◽  
Vol 395 (12) ◽  
pp. 1461-1466 ◽  
Author(s):  
Mohamed Badr ◽  
Christian Kopp ◽  
Sandra Theison ◽  
Jennifer Meyer ◽  
Wolfgang E. Trommer
Keyword(s):  
Dna Damage ◽  
Oxidative Dna Damage ◽  
Type I ◽  
Dependent Manner ◽  
Alkaline Comet Assay ◽  
Ribosome Inactivating Protein ◽  
Dose Dependent ◽  
Potential Tool ◽  
Mcf 7

Abstract An immunotoxin composed of gelonin, a basic ribosome-inactivating protein, type I of 30 kDa, isolated from the seeds of the Indian plant Gelonium multiflorum and methotrexate (MTX) has been studied as a potential tool of gelonin delivery into the cytoplasm of MTX-responsive cells. On the average, about five molecules of methotrexate were chemically coupled to gelonin via an N-hydroxysuccinimide ester of the drug. The MTX-gelonin conjugate was able to reduce the viability of MCF-7 cells in a dose-dependent manner with ID50 of 10 nm, whereas gelonin or MTX alone showed none or very little effects. Besides its ribosome-inactivating activity, which is about ten-fold lower in an in vitro translation assay (IC50 of 50.5 ng/ml as compared to 4.6 ng/ml), the conjugate also significantly induced direct and oxidative DNA damage as shown by the alkaline comet assay. Hence, MTX-gelonin conjugates are promising candidates for the treatment of MTX-responsive cancers.

scholarly journals In Vitro Cytotoxicity and Morphological Assessments of GO-ZnO against the MCF-7 Cells: Determination of Singlet Oxygen by Chemical Trapping

Nanomaterials ◽  
2018 ◽  
Vol 8 (7) ◽  
pp. 539 ◽  
Author(s):  
Fozia Shaheen ◽  
Muhammad Aziz ◽  
Mahvish Fatima ◽  
Muhammad Khan ◽  
Faisal Ahmed ◽  
...  
Keyword(s):  
Chemical Properties ◽  
In Vitro Cytotoxicity ◽  
Dependent Manner ◽  
X Ray Diffraction ◽  
X Ray ◽  
Vis Spectroscopy ◽  
Potential Applicability ◽  
Mcf 7

Graphene-based materials have attracted considerable interest owing to their distinctive characteristics, such as their biocompatibility in terms of both their physical and intrinsic chemical properties. The use of nanomaterials with graphene as a biocompatible agent has increased due to an uptick in dedication from biomedical investigators. Here, GO-ZnO was characterized by X-ray diffraction (XRD), field emission scanning electron microscopy (FESEM), ultraviolet-visible (UV-Vis) spectroscopy, energy dispersive X-ray analysis (EDAX), and Raman spectroscopy for structural, morphological, and elemental analysis. The toxic extent of GO-ZnO was noted by a methyl-thiazole-tetrazolium (MTT), while cellular morphology was observed towards the MCF-7 cells using an inverted microscope at magnification 40×. The cytotoxic effect of GO-ZnO investigated the cell viability reduction in a dose-dependent manner, as well as prompted the cell demise/destruction in an apoptotic way. Moreover, statistical analysis was performed on the experimental outcomes, with p-values < 0.05 kept as significant to elucidate the results. The generation of reactive oxygen species (ROS) demonstrated the potential applicability of graphene in tumor treatment. These key results attest to the efficacy of GO-ZnO nanocomposites as a substantial candidate for breast malignancy treatment.

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