8-Isocyanoamphilecta-11(20),15-diene, a new antimalarial isonitrile diterpene from the sponge Ciocalapata sp.

2009 ◽  
Vol 87 (5) ◽  
pp. 612-618 ◽  
Author(s):  
Chatchai Wattanapiromsakul ◽  
Naphatson Chanthathamrongsiri ◽  
Somchai Bussarawit ◽  
Supreeya Yuenyongsawad ◽  
Anuchit Plubrukarn ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Cell Lines ◽  
Nmr Spectra ◽  
Human Fibroblasts ◽  
Fibroblast Cell ◽  
The Other ◽  
Ergosterol Peroxide ◽  
Other Hand ◽  
Mcf 7 ◽  
Fibroblast Cell Lines

A new isonitrile diterpene of the amphilectane family, 8-isocyanoamphilecta-11(20),15-diene (4), was isolated from the sponge Ciocalapata sp., along with three known isonitriles, 8,15-diisocyano-11(20)-amphilectene (1), 7-isocyanoamphilecta-11(20),15-diene (2), and 8-isocyanoamphilecta-11(20),14-diene (3), and two steroidal peroxides, ergosterol peroxide (5) and 5α,9α-epidioxy-8α,14α-epoxy-(22E)-ergosta-6,22-dien-3β-ol (6). The structure of the new isonitrile was elucidated spectroscopically. In addition, anomalous multiplicities in the NMR spectra of some isolated isonitriles were observed and are reported here. The four isonitriles were strongly active against Plasmodium falciparum K1 with IC50 in a range of 0.09–1.07 μmol/L. Except for 1, which was cytotoxic against both MCF-7 and fibroblast cell lines, the other three diterpenes showed no significant cytotoxicity against either targeted cell lines. On the other hand, the steroidal peroxides 5 and 6, which were less active in the antimalarial bioassay (IC50 values of 6.28 and 7.13 µmol/L, respectively), were strongly cytotoxic against MCF-7 (IC50 values of 0.025 and 0.003 µmol/L, respectively), with very little toxicity against human fibroblasts.

Anti-proliferative Effect of Chickpea Extract on Hela, MCF-7, Saos and Fibroblast Cell Lines

2017 ◽  
Vol 15 (1) ◽  
pp. 1-9 ◽  
Author(s):  
Ladan Barari ◽  
Zeinab Abedian ◽  
Asadollah Asadi ◽  
Fatemeh Elmi ◽  
Maryam Elmi
Keyword(s):  
Cell Lines ◽  
Fibroblast Cell ◽  
Proliferative Effect ◽  
Mcf 7 ◽  
Fibroblast Cell Lines

scholarly journals Biosynthesis of the first component of complement by human fibroblasts

1977 ◽  
Vol 167 (3) ◽  
pp. 647-660 ◽  
Author(s):  
Kenneth B. M. Reid ◽  
Ellen Solomon
Keyword(s):  
Human Serum ◽  
Cell Lines ◽  
De Novo ◽  
Culture Media ◽  
Human Fibroblasts ◽  
Sodium Dodecyl ◽  
Fibroblast Cell ◽  
Haemolytic Activity ◽  
Fibroblast Cell Lines

1. Haemolytic activity corresponding to that of the first component of complement (C1) was synthesized and secreted by all nine human fibroblast cell lines examined. No activity was found in the culture media of a variety of other human cell lines. 2. The component-C1 haemolytic activity secreted by the fibroblast lines behaved in an identical manner, in most respects, with that of the component-C1 haemolytic activity of human serum. The component-C1 haemolytic activity secreted by fibroblasts, however, was less susceptible to inhibition by rabbit fragment F(ab′)2 anti-(human subcomponent C1q) than was the component-C1 haemolytic activity of human serum. 3. Biosynthesis of fibroblast component-C1 haemolytic activity was inhibited by the presence of cycloheximide and regained on its removal. 4. Incorporation of radioactivity into proteins secreted by the fibroblasts and release of component-C1 haemolytic activity by the fibroblasts both increased in a linear manner until several days after the cultures had reached a state of confluent growth. 5. Radioactivity was incorporated into subcomponents C1q, C1r and C1s, as judged by the formation of specific immunoprecipitates and by absorption with immune aggregates. 6. The immunoprecipitates formed by using antisera against subcomponents C1r and C1s were run on polyacrylamide gels in sodium dodecyl sulphate, and this provided convincing physiochemical evidence for the biosynthesis of these subcomponents de novo. 7. The results obtained with immunoprecipitates formed by using anti-(subcomponent C1q) suggest that subcomponent C1q may be synthesized and secreted by fibroblast cell lines in vitro, in a form with a higher molecular weight than that of subcomponent C1q which is isolated by conventional techniques of protein fractionation from fresh serum.

New Ferrocene Compounds as Selective Cyclooxygenase (COX-2) Inhibitors: Design, Synthesis, Cytotoxicity and Enzyme-inhibitory Activity

2018 ◽  
Vol 18 (2) ◽  
pp. 295-301 ◽  
Author(s):  
Shabnam Farzaneh ◽  
Elnaz Zeinalzadeh ◽  
Bahram Daraei ◽  
Soraya Shahhosseini ◽  
Afshin Zarghi
Keyword(s):  
Cell Lines ◽  
Inhibitory Activity ◽  
Fibroblast Cell ◽  
Breast Cancer Cell Lines ◽  
Ferrocene Derivatives ◽  
Cox 2 ◽  
Cytotoxicity Effects ◽  
Cox 2 Inhibitors ◽  
Mcf 7

Background: Due to the astonishing properties of ferrocene and its derivatives, it has a broad application in diverse areas. Numerous ferrocene derivatives demonstrated anti-proliferative activity. Also COX-2, as a key isoenzyme for production of prostaglandins, is frequently overexpressed in various cancers. It is now recognized that COX-2 over expression promotes tumorigenic functions which can be suppressed by COX-2 inhibitors, a phenomenon useful for the preventing of tumor progression. The combination of COX-2 inhibitors with other anti-cancer or cancer prevention drugs may reduce their side effects in future cancer prevention and treatment. Objective: Owing to high anticancer potential of ferrocene derivatives and considerable COX-2 inhibitory and cytotoxicity effects of our previously synthesized chalcones, we decided to incorporate the ferrocenyl moiety into appropriate COX-2 inhibitor chalcone based scaffold, to evaluate COX-2 inhibitory activity as well as anticancer activities. Methods: Chalcones were synthesized via clasien-schmidt condensation of methylsulfonyl aldehyde and acetyl ferrocene. Further different amines with solvent free and ultra sound condition were reacted with chalcones to have different 1-ferrocenyl-3-amino carbonyl compounds. Docking study was carried out with Auto Dock vina software. All the newly-synthesized compounds were evaluated for their cyclooxygenase-2 (COX-2) inhibitory activity using chemiluminescent enzyme assays as well as cytotoxicity activity against MCF-7 and T47D and fibroblast cell lines by MTT assay. Results: In vitro COX-1/COX-2 inhibition studies demonstrated that all compounds were selective inhibitors of the COX-2 isozyme with IC50 values in the highly potent 0.05-0.12 µM range, and COX-2 selectivity indexes (SI) in the 148.3-313.7 range. These results indicated that either potency or selectivity of COX-2 inhibitory activity was affected by the nature and size of the substituents on C-3 of propane-1-one. Also anti-proliferative and toxicity activities of synthesized compounds against breast cancer cell lines MCF-7 and T47D and fibroblast cell lines showed that the synthesized compounds had mild to moderate cytotoxicity against MCT7 and T47D breast cancer cell lines at 10 µM concentration. In vitro COX-1/COX-2 inhibition studies and anticancer activity against MCF-7, identified 1-ferrocenyl-3-(4-methylsulfonylphenyl) propen-1-one as a potent compound (IC50 COX-2 = 0.05 µM, MCF-7: % inhibition (at concentration of 10 µM) = 32.7%), and also 1-ferrocenyl-3- (propan-1-amine)-3-(4-methylsulfonylphenyl) propan-1-one showed the most selectivity on COX-2 inhibition (selectivity index= 313.7). Conclusion: A novel group of ferrocene compounds, possessing a methyl sulfonyl COX-2 pharmacophore were synthesized to investigate the effect of different substituents on selectivity and potency of COX-2 inhibitory activity and their cytotoxicity effects. This study indicates that 1-ferrocenyl-3-amino carbonyl compounds having ferrocene motif and methyl sulfonyl COX-2 pharmacophore is a suitable scaffold to design COX-2 inhibitors and anti-cancer agents.

17O and 13C NMR spectra of some geminal diacetates

1988 ◽  
Vol 53 (3) ◽  
pp. 588-592 ◽  
Author(s):  
Antonín Lyčka ◽  
Josef Jirman ◽  
Jaroslav Holeček
Keyword(s):  
13C Nmr ◽  
Nmr Spectra ◽  
Chemical Shifts ◽  
The Other ◽  
13C Nmr Spectra ◽  
Other Hand ◽  
Carboxylic Esters ◽  
C Nmr ◽  
Oxygen Atoms

The 17O and 13C NMR spectra of eight geminal diacetates RCH(O(CO)CH3)2 derived from simple aldehydes have been measured. In contrast to the dicarboxylates R1R2E(O(CO)R3)2, where E = Si, Ge, or Sn, whose 17O NMR spectra only contain a single signal, and, on the other hand, in accordance with organic carboxylic esters, the 17O NMR spectra of the compound group studied always exhibit two well-resolved signals with the chemical shifts δ(17O) in the regions of 183-219 ppm and 369-381 ppm for the oxygen atoms in the groups C-O and C=O, respectively.

scholarly journals Biocompatibility Analyses of Al2O3-Treated Titanium Plates Tested with Osteocyte and Fibroblast Cell Lines

Biomedicines ◽  
2017 ◽  
Vol 5 (4) ◽  
pp. 32 ◽  
Author(s):  
Alberto Smargiassi ◽  
Jessika Bertacchini ◽  
Marta Checchi ◽  
Francesco Cavani ◽  
Marzia Ferretti ◽  
...  
Keyword(s):  
Cell Lines ◽  
Fibroblast Cell ◽  
Fibroblast Cell Lines
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