Insecticidal and growth inhibitory activity of essential oils of Boenninghausenia albiflora and Teucrium quadrifarium against Spilarctia obliqua

Background: Clove and lemon basil are widely used in Indonesian culinary and known for their antimicrobial properties. This study was designed to identify the chemical constituents of single clove and lemon basil Essential Oils (EOs) as well as determine the potential of the combinations of both EO for preserving chicken meats. Methods: The compositions of clove and lemon basil EOs were evaluated with Gas Chromatography-Mass Spectrometer. Three different concentration ratios of the combination of clove and lemon basil EOs (2:0.2, 1:1, and 0.1:2% v/v) were prepared along with single clove and lemon basil EOs in a concentration of 1% v/v. Their potential preservation effect was evaluated by observing the reduction of the microbial growth on the meats by evaluating Optical Density (OD) of cultured bacterial suspensions during 15 days of refrigerated storage. Statistical analyses were conducted by SPSS Statistics v. 20. Results: The major constituents of clove EO were eugenol, β-caryophyllene, and αhumulene, while those of lemon basil were estragol, linalool, E-citral, and Z-citral. Both treatment groups and storage time affected significantly on ODs of the samples. Combination of these two EOs, particularly at the optimum ratio of 1:1%, showed the best microbial inhibitory activity, and delayed the sensorial changes of the meats for 12 days. Conclusion: The combinations of cloves and lemon basil EOs showed a better microbial growth inhibitory activity and preservation potential than those of the single use. This meat preservation effects might be related to the presence of high fractions of oxygenated compounds, mainly eugenol, Z-citral, and E-citral in both clove and lemon basil EOs.

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Modifications on the Tetrahydroquinoline Scaffold Targeting a Phenylalanine Cluster on GPER as Antiproliferative Compounds against Renal, Liver and Pancreatic Cancer Cells

Pharmaceuticals ◽

10.3390/ph14010049 ◽

2021 ◽

Vol 14 (1) ◽

pp. 49

Author(s):

David Méndez-Luna ◽

Loreley Araceli Morelos-Garnica ◽

Juan Benjamín García-Vázquez ◽

Martiniano Bello ◽

Itzia Irene Padilla-Martínez ◽

...

Keyword(s):

Binding Site ◽

Cell Lines ◽

Cancer Cell ◽

Inhibitory Activity ◽

In Silico ◽

Cancer Cell Lines ◽

Pancreatic Cancer Cells ◽

Growth Inhibitory ◽

Growth Inhibitory Activity ◽

New Compounds

The implementation of chemo- and bioinformatics tools is a crucial step in the design of structure-based drugs, enabling the identification of more specific and effective molecules against cancer without side effects. In this study, three new compounds were designed and synthesized with suitable absorption, distribution, metabolism, excretion and toxicity (ADME-tox) properties and high affinity for the G protein-coupled estrogen receptor (GPER) binding site by in silico methods, which correlated with the growth inhibitory activity tested in a cluster of cancer cell lines. Docking and molecular dynamics (MD) simulations accompanied by a molecular mechanics/generalized Born surface area (MMGBSA) approach yielded the binding modes and energetic features of the proposed compounds on GPER. These in silico studies showed that the compounds reached the GPER binding site, establishing interactions with a phenylalanine cluster (F206, F208 and F278) required for GPER molecular recognition of its agonist and antagonist ligands. Finally, a 3-(4,5-dimethylthiazol-2-yl)2,5-diphenyltetrazolium bromide (MTT) assay showed growth inhibitory activity of compounds 4, 5 and 7 in three different cancer cell lines—MIA Paca-2, RCC4-VA and Hep G2—at micromolar concentrations. These new molecules with specific chemical modifications of the GPER pharmacophore open up the possibility of generating new compounds capable of reaching the GPER binding site with potential growth inhibitory activities against nonconventional GPER cell models.

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Indole-3-carbinol inhibits the proliferation of colorectal carcinoma LoVo cells through activation of the apoptotic signaling pathway

Human & Experimental Toxicology ◽

10.1177/09603271211021475 ◽

2021 ◽

pp. 096032712110214

Author(s):

JY Lee ◽

HM Lim ◽

CM Lee ◽

S-H Park ◽

MJ Nam

Keyword(s):

Colorectal Carcinoma ◽

Cancer Cells ◽

Inhibitory Activity ◽

Annexin V ◽

Fluorescein Isothiocyanate ◽

Cell Counting ◽

Terminal Deoxynucleotidyl Transferase ◽

Growth Inhibitory ◽

Growth Inhibitory Activity ◽

Lovo Cells

Indole-3-carbinol (I3C) is a phytochemical that exhibits growth-inhibitory activity against various cancer cells. However, there are limited studies on the effects of I3C on colon cancer cells. In this study, the growth-inhibitory activity of I3C against the human colorectal carcinoma cell line (LoVo) was examined. The results of the 3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide, colony formation, and cell counting assays revealed that I3C suppressed the proliferation of LoVo cells. Microscopy and wound-healing analyses revealed that I3C affected the morphology and inhibited the migration of LoVo cells, respectively. I3C induced apoptosis and DNA fragmentation as evidenced by the results of fluorescein isothiocyanate-conjugated annexin V staining and terminal deoxynucleotidyl transferase-mediated dUTP-biotin nick-end labeling assay, respectively. Additionally, I3C arrested the cell cycle at the G0/G1 phase and enhanced the reactive oxygen species levels. Western blotting analysis revealed that treatment with I3C resulted in the activation of apoptotic proteins, such as poly(ADP-ribose) polymerase, caspase-3, caspase-7, caspase-9, Bax, Bim, and p53 in LoVo cells. These results indicate that I3C induces apoptosis in LoVo cells by upregulating p53, leading to the activation of Bax and caspases. Taken together, I3C exerts cytotoxic effects on LoVo cells by activating apoptosis.

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