scholarly journals 10′-Deoxy-10′ α-hydroxyascochlorin, a New Cell Migration Inhibitor and Other Metabolites from Acremonium sp., a Fungal Endophyte in Ephedra trifurca

2013 ◽  
Vol 8 (5) ◽  
pp. 1934578X1300800
Author(s):  
W. M. Anoja P. Wanigesekara ◽  
E. M. Kithsiri Wijeratne ◽  
A. Elizabeth Arnold ◽  
A. A. Leslie Gunatilaka

A new ascochlorin, 10′-deoxy-10′ α-hydroxyascochlorin (1), together with ascofuranone (2), ascochlorin (3), and 4′,5′-dihydro-4′ β-hydroxyascochlorin (4) were isolated from Acremonium sp. LG0808, an endophytic fungal strain occurring in the stem tissue of the medicinal plant, Ephedra trifurca. The structure of 1 was elucidated on the basis of its high-resolution mass spectrometric, and 1D and 2D NMR spectroscopic data. Compounds 1 and 3 inhibited migration of metastatic prostate cancer cells, PC-3M. In addition, 3 exhibited moderately selective cytotoxicity against the NCI-H460 (non-small cell lung cancer) cell line, but its dimethyl ether (6) showed selective activity against PC-3M, MCF-7 (breast cancer), and MDA-MB-231 (metastatic breast cancer) cell lines.

2020 ◽  
Vol 44 (5) ◽  
pp. 2166-2179 ◽  
Author(s):  
Elavarasan Nagaraj ◽  
Prakash Shanmugam ◽  
Kokila Karuppannan ◽  
Thirunavukkarasu Chinnasamy ◽  
Sujatha Venugopal

ZnO/GO nanocomposites were synthesized and their antibacterial activities assessed against various pathogens. They are potential antibacterial materials and significant anticancer activity against the MCF-7 breast cancer cell line compared to the A549 lung cancer cell line.


2019 ◽  
Vol 19 (5) ◽  
pp. 410-423
Author(s):  
Md Rahmat Ali ◽  
Suresh Kumar ◽  
Nishtha Shalmali ◽  
Obaid Afzal ◽  
Sabir Azim ◽  
...  

Introduction: The signalling function of 2-arachidonoylglycerol (2-AG) in endocannabinoid system is delineated by Monoacylglycerol lipase (MAGL). MAGL readdresses the lipid stores in the direction of pro-tumorigenic signalling lipids in cancer cells. Selective as well as potent MAGL inhibitors are limited in number hence their continuous development may lead to a breakthrough invention in the field of MAGL inhibitors. In succession of the above, we have synthesised 2-amino-4- methylthiazole-5-carboxylate derivatives and characterised them by collective use of IR, 1H-NMR, 13C-NMR, Mass spectral data and elemental analysis. </P><P> Methodology: Thirteen compounds (3c-g, 4c, 4e, 4f and 6b-f) inhibited MAGL with IC50 value 0.037- 9.60 &#181;M. Two compounds (3g and 4c) were found to be most potent with IC50 values 0.037 and 0.063&#181;M, respectively. Thirty synthesised compounds were sent to NCI for anticancer screening, out of which nine compounds were selected for one dose anticancer assay. Compounds 3g (NSC:788170) and 4c (NSC:788176)were found to be the most potent during one dose anticancer screening and fulfilled the specified threshold for growth inhibition criteria of NCI and were further selected for full panel five dose assay at 10-fold dilutions of five different concentrations. </P><P> Conclusion: Compound 3g displayed GI50 value 0.865 μM against EKVX (Non-Small Cell Lung Cancer cell line), and 1.20 &#181;M against MDA-MB-468 (Breast Cancer cell Line), while (4c) showed GI50 value 0.34 and 0.96 &#181;M against HOP-92 and EKVX (Non-Small Cell Lung Cancer cell line) and 1.08 &#181;M against MDA-MB-231/ATCC(Breast Cancer cell Line). In addition, molecular docking studies of the said MAGL inhibitors have also been presented in this article.


Author(s):  
Vasanth N ◽  
Melchias G ◽  
Kumaravel P

Objective: To evaluate the potential aspects of biologically synthesized silver nanoparticles mediated by Broussonetia papyrifera against the human pathogens. The same is acknowledged to have high efficiency in the field of Pharmaceutical industry.Methods: The 1Mm of AgNO3 is prepared and mixed with appropriate volume of plant extract and reaction volume was made up to 100 ml. the physical   characterization of AgNPs was done. The anti-microbial activity was done against dread pathogens. Cytotoxic activity of the AgNPs was investigated against breast and lung cancer cell lines.Results: The FESEM and EDAX of the microscopic level showed the particle surface measurements around 44 nm to 50 nm. The XRD investigations are being an evidence for the crystalline structure of the AgNPs with 30 nm. The bacterial pathogen Rhodococcus rhodochrous showed the maximum zone of inhibition (11.8±0.447). The A549 human lung cancer cell line and MCF-7 human breast cancer cell line were tested against the toxicity of AgNPs. The toxicity of AgNPs was valued and corresponding IC50 for Lung cancer (A549) is 12.95± 0.05 µg/mL and Breast cancer (MCF-7) is 10.75± 0.05 µg/mL respectively.Conclusion: The present research denotes that biomolecules derived AgNPs have larger impact as antimicrobials in the biomedical field. Since the aggressive chemicals are not involved AgNPs production, these bio-substances can of alternative medicine to resistant once. The in-vitro experiments exhibits the therapeutic effect of this AgNPs based on the ambient concentration on the process.KEYWORDS: Cancer activity, Antimicrobial agents, Resistance, Silver nanoparticles.


2012 ◽  
Vol 2012 ◽  
pp. 1-9 ◽  
Author(s):  
Harshita Sachdeva ◽  
Diksha Dwivedi

Various Biginelli compounds (dihydropyrimidinones) have been synthesized efficiently and in high yields under mild, solvent-free, and eco-friendly conditions in a one-pot reaction of 1,3-dicarbonyl compounds, aldehydes, and urea/thiourea/acetyl thiourea using lithium-acetate as a novel catalyst without the addition of any proton source. Comparative catalytic efficiency of lithium-acetate and polyphosphoric acid to catalyze Biginelli condensation is also studied under neat conditions. The reaction is carried out in the absence of any solvent and represents an improvement of the classical Biginelli protocol and an advantage in comparison with FeCl3·6H2O, NiCl2·6H2O and CoCl2·6H2O that were used with HCl as a cocatalyst. Compared to classical Biginelli reaction conditions, the present method has advantages of good yields, short reaction times, and experimental simplicity. The obtained products have been identified by spectral (1H NMR and IR) data and their melting points. The prepared compounds are evaluated for anticancer activity against two human cancer cell lines (lung cancer cell line A549 and breast cancer cell line MCF7).


2004 ◽  
Vol 32 (3) ◽  
pp. 987-995 ◽  
Author(s):  
NT Peekhaus ◽  
T Chang ◽  
EC Hayes ◽  
HA Wilkinson ◽  
SW Mitra ◽  
...  

The effects of estrogen receptor (ER) ligands on the stability and transcriptional activity of ERbeta in the breast cancer cell lines MCF-7 and HeLa were examined. We found that ERbeta was degraded in the presence of 17beta-estradiol. Tamoxifen and Faslodex (ICI 182,780) prevented ERbeta receptor destabilization. In contrast to ERalpha, ERbeta degradation was not abolished by inhibitors of the proteasome-mediated protein degradation pathway. Furthermore, single point mutations in helix 12 of the receptor dramatically affected the stability and subsequent transcriptional activation of ERbeta.


2014 ◽  
Vol 25 (1) ◽  
pp. 17-29 ◽  
Author(s):  
Sabrina Schlienger ◽  
Shirley Campbell ◽  
Audrey Claing

Invasion of tumor cells is a key step in metastasis that depends largely on the ability of these cells to degrade the extracellular matrix. Although we have showed that the GTPase ADP-ribosylation factor 1 (ARF1) is overexpressed in highly invasive breast cancer cell lines and that epidermal growth factor stimulation can activate this ARF isoform to regulate migration as well as proliferation, the role of this small GTP-binding protein has not been addressed in the context of invasiveness. Here we report that modulation of ARF1 expression and activity markedly impaired the ability of M.D. Anderson-metastatic breast-231 cells, a prototypical highly invasive breast cancer cell line, to degrade the extracellular matrix by controlling metalloproteinase-9 activity. In addition, we demonstrate that this occurs through inhibition of invadopodia maturation and shedding of membrane-derived microvesicles, the two key structures involved in invasion. To further define the molecular mechanisms by which ARF1 controls invasiveness, we show that ARF1 acts to modulate RhoA and RhoC activity, which in turn affects myosin light-chain (MLC) phosphorylation. Together our findings underscore for the first time a key role for ARF1 in invasion of breast cancer cells and suggest that targeting the ARF/Rho/MLC signaling axis might be a promising strategy to inhibit invasiveness and metastasis.


2020 ◽  
Vol 11 (2) ◽  
pp. 2101-2108
Author(s):  
Mahendran V S ◽  
Sophiya K ◽  
Sruthi Malavika S ◽  
Suganthi B ◽  
Ragul Prasath P ◽  
...  

Cancer is the second leading cause of death globally. Among the group of cancer diseases, breast cancer is the most common type of cancer to affect women. The treatment options that are currently available for this include surgery, radiation therapy and therapy through medication or drugs. But, since all these are harmful and have severe side effects, drugs from natural plant compounds are being developed to act against cancer and its metastatic activity. The aim of this article is to perform in silico studies to identify phytochemicals in Cissus quadrangularis that can act against breast cancer, predict its targets and study its properties using bioinformatic tools and databases. It also involves studying of anticancer and anti-metastatic activity of the plant, Cissus quadrangularis (CQ) in MCF-7 breast cancer cell lines. CQ, a perennial plant of the grape family, has many medicinal benefits including antioxidant and anticancer properties. Alpha-amyrin, a terpenoid, was selected as a potential phytochemical in CQ and its ADME properties were studied using SwissADME. Then, its target was identified as androgen receptor using Swiss Target Prediction. Plant extract of CQ was prepared by ethyl acetate extraction method. Various tests such as MTT assay, Wound healing assay, DNA fragmentation assay, Caspase 7/9 induction detection assay and Annexin V assay were performed to evaluate the anticancer and anti-metastatic activity of CQ extract in MCF-7 cell lines. The results of the tests showed good anticancer and anti-metastasis activity of CQ with an IC50 value of 141.369µg/mL. It can be concluded that CQ has the properties required to act against breast cancer with the dose being directly proportional to the efficiency of CQ on the cancer cells.


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