scholarly journals A New Antimicrobial and Anticancer Peptide Producing by the Marine Deep Sediment Strain “Paenibacillus profundus” sp. nov. Sl 79

2013 ◽  
Vol 8 (3) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Nataliya I. Kalinovskaya ◽  
Lyudmila A. Romanenko ◽  
Anatoly I. Kalinovsky ◽  
Pavel S. Dmitrenok ◽  
Sergey A. Dyshlovoy
Keyword(s):  
Amino Acids ◽  
Staphylococcus Epidermidis ◽  
Inhibitory Activity ◽  
2D Nmr ◽  
Colony Growth ◽  
Anticancer Peptide ◽  
Deep Sea Sediment ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Nmr Techniques

A new linear glyceryl acid derived heptapeptide (1), together with known isocoumarin antibiotic, Y-05460M-A (2), were isolated from the culture of the deep sea sediment strain Sl 79 classified as “ Paenibacillus profundus” sp. nov. Their structures were determined by 1D- and 2D- NMR techniques and ESI-MS/MS experiments. HPLC analysis of the Marfey derivatives in comparison to their analogs of authentic amino acids revealed that all amino acids in peptide 1, with an exception of Val, have the D-configuration. The compound 1 showed inhibitory activity against Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, Enterococcus faecium as well as cytotoxic and moderate colony growth inhibitory activity against SK-MEL-28 cell line.

scholarly journals Structure and Absolute Configuration of a Diterpenoid from Castanea mollissima

2010 ◽  
Vol 5 (1) ◽  
pp. 1934578X1000500
Author(s):  
Hui-Yuan Gao ◽  
Xiao-Bo Wang ◽  
Rong-Gang Xi ◽  
Bo-Hang Sun ◽  
Jian Huang ◽  
...  
Keyword(s):  
Spectral Analysis ◽  
Enzymatic Hydrolysis ◽  
Tumor Cells ◽  
Absolute Configuration ◽  
Inhibitory Activity ◽  
2D Nmr ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Castanea Mollissima ◽  
Hydrolysis Of

From the nuts of Castanea mollissima Blume, a new kauranoid diterpene glycoside, named mollioside (1), was isolated. Its structure was established as (4R, 5S, 6R, 8R, 9S, 10S, 13R, 16R) 17-O-β-D-glucopyranoside, ent-6,7-epoxy-6α-hydroxyl-6,7-secokaur-19-oic acid, 6, 19-lactone-16β, 17-diol on the basis of HR-FAB-MS, 1D, 2D-NMR and CD spectral analysis. The aglycone (1a, named mollissin), also as a new compound, was obtained after enzymatic hydrolysis of 1. Both compounds exhibited significant growth inhibitory activity on HeLa tumor cells, but no activity on A375-S2.

scholarly journals Two New Aromadendrane Sesquiterpenes from the Stem Bark of Alafia multiflora

2014 ◽  
Vol 9 (12) ◽  
pp. 1934578X1400901
Author(s):  
Alembert T. Tchinda ◽  
David E. Tsala ◽  
Nnanga Nga ◽  
Ewa Cieckiewicz ◽  
Robert Kiss ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
2D Nmr ◽  
Stem Bark ◽  
Dioic Acid ◽  
Murine Melanoma ◽  
Spectroscopic Analyses ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Weak Growth

Two new aromadendrane sesquiterpenoids (1β,4β,5β,6α,7α,11 S)-aromadendr-9-en-13,14-dioic acid (1) and (1β,4β,5β,6α,7α,11 S)-13-oxoaromadendr-9-en-14-oic acid (2) have been isolated from the stem bark of Alafia multiflora along with β-sitosterol and β-sitosterol glucoside. Their structures were established on the basis of spectroscopic analyses, including 1D and 2D NMR experiments (1H-1H COSY, NOESY, HSQC, HMBC). Compound 1 showed a weak growth inhibitory activity against the murine melanoma line B16F10 MTT.

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

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.

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

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.

scholarly journals Structural Determinants of Heparin's Growth Inhibitory Activity

1989 ◽  
Vol 264 (3) ◽  
pp. 1534-1542
Author(s):  
T C Wright ◽  
J J Castellot ◽  
M Petitou ◽  
J C Lormeau ◽  
J Choay ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Structural Determinants ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity

Spontaneous immortalisation of Schwann cells in culture: short-term cultured Schwann cells secrete growth inhibitory activity

Development ◽  
1991 ◽  
Vol 112 (1) ◽  
pp. 33-42
Author(s):  
P.A. Eccleston ◽  
R. Mirsky ◽  
K.R. Jessen
Keyword(s):  
Growth Factor ◽  
Schwann Cell ◽  
Dna Synthesis ◽  
Schwann Cells ◽  
Inhibitory Activity ◽  
Short Term ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Cultured Schwann Cells

In the developing peripheral nerve, Schwann cells proliferate rapidly and then become quiescent, an essential step in control of Schwann cell differentiation. Cell proliferation is controlled by growth factors that can exert positive or inhibitory influences on DNA synthesis. It has been well established that neonatal Schwann cells divide very slowly in culture when separated from neurons but here we show that when culture was continued for several months some cells began to proliferate rapidly and non-clonal lines of immortalised Schwann cells were established which could be passaged for over two years. These cells had a similar molecular phenotype to short-term cultured Schwann cells, except that they expressed intracellular and cell surface fibronectin. The difference in proliferation rates between short- and long-term cultured Schwann cells appeared to be due in part to the secretion by short-term cultured Schwann cells of growth inhibitory activity since DNA synthesis of long-term, immortalised Schwann cells was inhibited by conditioned medium from short-term cultures. This conditioned medium also inhibited DNA synthesis in short-term Schwann cells stimulated to divide by glial growth factor or elevation of intracellular cAMP. The growth inhibitory activity was not detected in the medium of long-term immortalised Schwann cells, epineurial fibroblasts, a Schwannoma (33B), astrocytes or a fibroblast-like cell-line (3T3) and it did not inhibit serum-induced DNA synthesis in epineurial fibroblasts, 33B cells or 3T3 cells. The activity was apparently distinct from transforming growth factor-beta, activin, IL6, epidermal growth factor, atrial natriuretic peptide and gamma-interferon and was heat and acid stable, resistant to collagenase and destroyed by trypsin treatment. We raise the possibility that loss of an inhibitory autocrine loop may contribute to the rapid proliferation of long-term cultured Schwann cells and that an autocrine growth inhibitor may have a role in the cessation of Schwann cell division that precedes differentiation in peripheral nerve development.

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