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 Growth-inhibitory activity of lymphoid cell plasma membranes. II. Partial characterization of the inhibitor.

1984 ◽  
Vol 99 (4) ◽  
pp. 1227-1234 ◽  
Author(s):  
K C Stallcup ◽  
S J Burakoff ◽  
M F Mescher
Keyword(s):  
Tumor Cells ◽  
Inhibitory Activity ◽  
Lymphoid Cell ◽  
Plasma Membranes ◽  
Gel Filtration ◽  
Lymphoid Cells ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Membrane Components ◽  
A Minor

We have shown that plasma membranes from lymphoid cells have inhibitory activity for the growth of normal lymphocytes and lymphoid tumor cells (Stallcup, K. C., A. Dawson, and M. F. Mescher, J. Cell Biol. 99:1221-1226). This growth-inhibitory activity has been found to co-purify with major histocompatibility complex class I antigens (H-2K and D) when these cell surface glycoproteins are isolated from detergent lysates of cells by affinity chromatography on monoclonal antibody columns. When incorporated into liposomes, the affinity-purified H-2 antigens inhibited the growth of both normal lymphocytes and tumor cells at concentrations of 1-3 micrograms/ml. Inhibition was readily reversed upon removal of the liposomes from the cell cultures, even after several days of exposure of cells to the inhibitor. Inhibitory activity was insensitive to protease digestion or heat treatment, indicating that it was not due to the H-2 glycoproteins. This was confirmed by the demonstration that inhibitory activity could be separated from the H-2 protein by gel filtration in the presence of deoxycholate and could be extracted from membranes or H-2 antigen preparations with organic solvents. The results demonstrate that the growth-inhibitory component(s) of the plasma membrane is a minor lipid or lipid-like molecule which retains activity in the absence of other membrane components. The findings reported here and in the preceding article suggest that this novel membrane component may have a role in control of lymphoid cell growth, possibly mediated by cell contacts.

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 Growth inhibitory activity of synthetic mannan derivative against tumor cells in vitro.

1978 ◽  
Vol 26 (1) ◽  
pp. 321-324
Author(s):  
TATSUJI MATSUMOTO ◽  
TAKESHI MIKAMI ◽  
YUICHI SATO ◽  
MASUKO SUZUKI ◽  
SHIGEO SUZUKI
Keyword(s):  
Tumor Cells ◽  
Inhibitory Activity ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity

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.

scholarly journals Massiliamide, a cyclic tetrapeptide with potent tyrosinase inhibitory properties from the Gram-negative bacterium Massilia albidiflava DSM 17472T

2020 ◽  
Author(s):  
Andri Frediansyah ◽  
Jan Straetener ◽  
Heike Brötz-Oesterhelt ◽  
Harald Gross
Keyword(s):  
Absolute Configuration ◽  
Inhibitory Activity ◽  
Liquid Culture ◽  
Spectroscopic Analysis ◽  
2D Nmr ◽  
Negative Bacterium ◽  
Gram Negative ◽  
The Absolute ◽  
Potent Inhibitory Activity ◽  
Cyclic Tetrapeptide

AbstractA cyclic tetrapeptide, designated massiliamide, was isolated from the liquid culture of the Gram-negative bacterium Massilia albidiflava DSM 17472T. The structure was elucidated through extensive spectroscopic analysis, including HR-MS and 1D and 2D NMR experiments. The absolute configuration was determined using the Marfey´s method. Massiliamide showed potent inhibitory activity towards tyrosinase with an IC50 value of 1.15 µM and no cytotoxicity.

scholarly journals Semi-Synthesis of Small Molecules of Aminocarbazoles: Tumor Growth Inhibition and Potential Impact on p53

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1637
Author(s):  
Solida Long ◽  
Joana B. Loureiro ◽  
Carla Carvalho ◽  
Luís Gales ◽  
Lucília Saraiva ◽  
...  
Keyword(s):  
Growth Inhibition ◽  
Small Molecules ◽  
Tumor Cells ◽  
Mutant P53 ◽  
Wild Type ◽  
Naturally Occurring ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Amino Derivatives ◽  
Carbazole Alkaloids

The tumor suppressor p53 is inactivated by mutation in approximately 50% of human cancers. Small molecules that bind and stabilize those mutants may represent effective anticancer drugs. Herein, we report the tumor cell growth inhibitory activity of carbazole alkaloids and amino derivatives, as well as their potential activation of p53. Twelve aminocarbazole alkaloids were semi-synthesized from heptaphylline (1), 7-methoxy heptaphylline (2), and 7-methoxymukonal (3), isolated from Clausena harmandiana, using a reductive amination protocol. Naturally-occurring carbazoles 1–3 and their amino derivatives were evaluated for their potential effect on wild-type and mutant p53 activity using a yeast screening assay and on human tumor cell lines. Naturally-occurring carbazoles 1–3 showed the most potent growth inhibitory effects on wild-type p53-expressing cells, being heptaphylline (1) the most promising in all the investigated cell lines. However, compound 1 also showed growth inhibition against non-tumor cells. Conversely, semi-synthetic aminocarbazole 1d showed an interesting growth inhibitory activity in tumor cells expressing both wild-type and mutant p53, exhibiting low growth inhibition on non-tumor cells. The yeast assay showed a potential reactivation of mutant p53 by heptaphylline derivatives, including compound 1d. The results obtained indicate that carbazole alkaloids may represent a promising starting point to search for new mutp53-reactivating agents with promising applications in cancer therapy.

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.

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