Przeciwnowotworowe działanie składników propolisu. Cz. 3. Związki o różnej strukturze chemicznej

2021 ◽  
Vol 22 (1) ◽  
Author(s):  
Elżbieta Hołderna-Kędzia ◽  
Bogdan Kędzia
Keyword(s):  
Antitumor Activity ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Aromatic Acids ◽  
In Vivo Tests ◽  
Artepillin C ◽  
Chemical Groups

The paper reviews the research on the antitumor activity of propolis components belonging to different, previously (Part 1 and 2), not discussed chemical groups. The in vitro (human and animal cancer cell lines) and in vivo tests performed showed differentiated cytotoxic activity of the tested compounds (IC50 from 2 to > 100.0 g/ml), including weak, moderate or strong (IC50 = 4.0 μg/ml). The strongest cytotoxic activity was shown by prenylated aromatic acids (artepillin C), isoflavones (mucronulatol) and prenylated benzophenones (nemorosan and plukenethione). The studies also showed a reduction in the degree of neoplastic metastases to various organs under the influence of the test substances (83.0%), as well as inhibition of neoplastic cells (90%) compared to control cultures.

scholarly journals Design, Synthesis, Molecular Modeling and Antitumor Evaluation of Novel Indolyl-Pyrimidine Derivatives with EGFR Inhibitory Activity

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 1838
Author(s):  
Naglaa M. Ahmed ◽  
Mahmoud M. Youns ◽  
Moustafa K. Soltan ◽  
Ahmed M. Said
Keyword(s):  
Molecular Modeling ◽  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Antitumor Agents ◽  
Cancer Cell Lines ◽  
Normal Cells

Scaffolds hybridization is a well-known drug design strategy for antitumor agents. Herein, series of novel indolyl-pyrimidine hybrids were synthesized and evaluated in vitro and in vivo for their antitumor activity. The in vitro antiproliferative activity of all compounds was obtained against MCF-7, HepG2, and HCT-116 cancer cell lines, as well as against WI38 normal cells using the resazurin assay. Compounds 1–4 showed broad spectrum cytotoxic activity against all these cancer cell lines compared to normal cells. Compound 4g showed potent antiproliferative activity against these cell lines (IC50 = 5.1, 5.02, and 6.6 μM, respectively) comparable to the standard treatment (5-FU and erlotinib). In addition, the most promising group of compounds was further evaluated for their in vivo antitumor efficacy against EAC tumor bearing mice. Notably, compound 4g showed the most potent in vivo antitumor activity. The most active compounds were evaluated for their EGFR inhibitory (range 53–79 %) activity. Compound 4g was found to be the most active compound against EGFR (IC50 = 0.25 µM) showing equipotency as the reference treatment (erlotinib). Molecular modeling study was performed on compound 4g revealed a proper binding of this compound inside the EGFR active site comparable to erlotinib. The data suggest that compound 4g could be used as a potential anticancer agent.

scholarly journals Metabolites Profiling, In Vitro, In Vivo, Computational Pharmacokinetics and Biological Predictions of Aloe perryi Resins Methanolic Extract

Plants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1106
Author(s):  
Rasha Saad Suliman ◽  
Sahar Saleh Alghamdi ◽  
Rizwan Ali ◽  
Dimah A. Aljatli ◽  
Sarah Huwaizi ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Methanolic Extract ◽  
Bioactive Constituents ◽  
Pharmacokinetic Properties ◽  
Anti Inflammatory ◽  
Aloe Perryi

Background: Aloe perryi is a traditional herb that has various biological and pharmacological properties such as anti-inflammatory, laxative, antiviral, antidiabetic, and antitumor effects, which have not been deliberated before. The current investigation aims to evaluate in vitro cytotoxicity against several cancer cell lines in addition to in vivo anti-inflammatory activities of Aloe perryi extract using a rat animal model. Moreover, the pharmacokinetic properties of bioactive constituents and possible biological targets were assessed and evaluated. The methanolic extract of Aloe perryi was prepared by maceration, to tentatively identify the biomolecules of the Aloe perryi extract, analytical LC–QTOF-MS method was employed for Aloe perryi methanolic extract. The cytotoxic activity was examined in six cancer cell lines using Titer-Glo assay and the IC50s were calculated in addition to in silico target predictions and in vivo anti-inflammatory activity assessment. Subsequently, the pharmacokinetics of the identified active components of Aloe perryi were predicted using SwissADME, and target prediction using the Molinspiration webserver. The cytotoxic activity on HL60 and MDA-MB-231 was moderately affected by the Aloe perryi extract with IC50 of 63.81, and 89.85 μg/ml, respectively, with no activity on other cells lines. Moreover, the Aloe perryi extract exhibited a significant increase in wound contraction, hair growth, and complete re-epithelization when compared with the negative control. The pharmacokinetic properties of the bioactive constituents suggested a good pharmaceutical profile for the active compounds and nuclear receptors and enzymes were the two main possible targets for these active compounds. Our results demonstrated the promising activity of Aloe perryi extract with cytotoxic and anti-inflammatory properties, indicating a potential therapeutic utility of this plant in various disease conditions.

Antitumor Activity of Suberoylanilide Hydroxamic Acid against Thyroid Cancer Cell Lines In vitro and In vivo

2006 ◽  
Vol 12 (18) ◽  
pp. 5570-5577 ◽  
Author(s):  
Quang T. Luong ◽  
James O'Kelly ◽  
Glenn D. Braunstein ◽  
Jerome M. Hershman ◽  
H. Phillip Koeffler
Keyword(s):  
Thyroid Cancer ◽  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Hydroxamic Acid ◽  
Suberoylanilide Hydroxamic Acid ◽  
Thyroid Cancer Cell ◽  
Thyroid Cancer Cell Lines

scholarly journals Analgesic, Anti-Inflammatory, Cytotoxic Activity Screening and UPLC-PDA-ESI-MS Metabolites Determination of Bioactive Fractions of Kleinia pendula

Molecules ◽  
2020 ◽  
Vol 25 (2) ◽  
pp. 418 ◽  
Author(s):  
Mohammad Alfaifi ◽  
Abdulrhman Alsayari ◽  
Narasimman Gurusamy ◽  
Justin Louis ◽  
Serag Eldin Elbehairi ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Plant Metabolites ◽  
Esi Ms ◽  
Anti Inflammatory

Kleinia pendula (Forssk.) DC. is a prostrate or pendent dark green succulent herb found in the southwestern mountain regions of Saudi Arabia. The literature survey of the plant reveals a lack of phytochemical and pharmacological studies, although traditional uses have been noted. The objective of the present work was to assess the in vivo analgesic and anti-inflammatory activities, as well as, the in vitro cytotoxic potential of the fractions of Kleinia pendula, and correlate these activities to the plant metabolites. The methanolic extract of Kleinia pendula was subjected to fractionation with n-hexane, ethyl acetate, chloroform, n-butanol, and water. The fractions were screened for their analgesic and anti-inflammatory activities, as well as cytotoxic activity against breast, liver, and colon cancer cell lines. The n-hexane and chloroform fractions of Kleinia pendula showed significant cytotoxic activity against all three cancer cell lines tested. The ethyl acetate and chloroform fractions showed significant analgesic and anti-inflammatory activities. The metabolites in these three active fractions were determined using UPLC-PDA-ESI-MS. Thus, the analgesic and anti-inflammatory activities of the plant were attributed to its phenolic acids (caffeoylquinic acid derivatives, protocatechuic, and chlorogenic acids). While fatty acids and triterpenoids such as (tormentic acid) in the hexane fraction are responsible for the cytotoxic activity; thus, these fractions of Kleinia pendula may be a novel source for the development of new plant-based analgesic, anti-inflammatory, and anticancer drugs.

scholarly journals Synthesis and Evaluation of the Antitumor Activity of (E)-3-((2-(5-(4-chlorophenyl) thiazol-2-yl) hydrazono) methyl) benzene-1,2-diol “In vitro and In vivo Study”

2019 ◽  
pp. 1-16
Author(s):  
Faten Z. Mohamed ◽  
Mohamed S. Elghreeb ◽  
Moustafa S. Abdelhamid ◽  
Hazem A. Elbaz
Keyword(s):  
Antitumor Activity ◽  
Life Span ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cytotoxic Effect ◽  
Ehrlich Ascites Carcinoma ◽  
Ehrlich Ascites ◽  
Liver And Kidney

Background: Thiazole nucleus–containing compounds have an antitumor efficiency against various types of cancer. Purpose: The present study was designed to determine the cytotoxic effect of newly synthesized thiazole derivative (TD1) on human cancer cell lines, in addition to evaluate its antitumor activity against Ehrlich ascites carcinoma (EAC) in mice. Materials and Methods: TD1 was synthesized and investigated for its cytotoxic effect on HCT116 (colon cancer), HepG2 (liver cancer), PC3 (prostate cancer) and MCF7 (breast cancer). The effect of TD1 on cell viability, tumor volume, and percent of increase in life span (% ILS) in Ehrlich–bearing mice was studied. Hematological parameters, liver and kidney function tests were evaluated. The activity of superoxide dismutase (SOD) and catalase (CAT), as well as malondialdehyde (MDA) and reduced glutathione levels were determined in liver and kidney tissues. The expression of P53 in EAC was analyzed by flow cytometry. Results: TD1 demonstrated an inhibitory effect on both cancer cell lines in vitro and Ehrlich ascites cells in vivo. TD1 increased in life span of Ehrlich–bearing mice compared to control. Cell cycle and flow cytometric analysis revealed that TD1 directed Ehrlich cells toward apoptosis by increasing of P53 expression. Conclusion: It was concluded that TD1 have a potent antitumor activity against Ehrlich ascites carcinoma in mice beside a cytotoxic effect on MCF-7, PC3, HepG2 and HCT-116.

scholarly journals Identification of Prostaglandin F2 Receptor Negative Regulator (PTGFRN) as an internalizable target in cancer cells for antibody-drug conjugate development

PLoS ONE ◽  
2021 ◽  
Vol 16 (1) ◽  
pp. e0246197
Author(s):  
Jorge Marquez ◽  
Jianping Dong ◽  
Chun Dong ◽  
Changsheng Tian ◽  
Ginette Serrero
Keyword(s):  
Flow Cytometry ◽  
Western Blot ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Negative Regulator ◽  
Target Validation ◽  
Antibody Drug

Antibody-drug conjugates (ADC) are effective antibody-based therapeutics for hematopoietic and lymphoid tumors. However, there is need to identify new targets for ADCs, particularly for solid tumors and cancers with unmet needs. From a hybridoma library developed against cancer cells, we selected the mouse monoclonal antibody 33B7, which was able to bind to, and internalize, cancer cell lines. This antibody was used for identification of the target by immunoprecipitation and mass spectrometric analysis, followed by target validation. After target validation, 33B7 binding and target positivity were tested by flow cytometry and western blot analysis in several cancer cell lines. The ability of 33B7 conjugated to saporin to inhibit in vitro proliferation of PTFRN positive cell lines was investigated, as well as the 33B7 ADC in vivo effect on tumor growth in athymic mice. All flow cytometry and in vitro internalization assays were analyzed for statistical significance using a Welsh’s T-test. Animal studies were analyzed using Two-Way Analysis of Variance (ANOVA) utilizing post-hoc Bonferroni analysis, and/or Mixed Effects analysis. The 33B7 cell surface target was identified as Prostaglandin F2 Receptor Negative Regulator (PTGFRN), a transmembrane protein in the Tetraspanin family. This target was confirmed by showing that PTGFRN-expressing cells bound and internalized 33B7, compared to PTGFRN negative cells. Cells able to bind 33B7 were PTGFRN-positive by Western blot analysis. In vitro treatment PTGFRN-positive cancer cell lines with the 33B7-saporin ADC inhibited their proliferation in a dose-dependent fashion. 33B7 conjugated to saporin was also able to block tumor growth in vivo in mouse xenografts when compared to a control ADC. These findings show that screening antibody libraries for internalizing antibodies in cancer cell lines is a good approach to identify new cancer targets for ADC development. These results suggest PTGFRN is a possible therapeutic target via antibody-based approach for certain cancers.

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