scholarly journals Antiproliferative Activity of Hamigerone and Radicinol Isolated fromBipolaris papendorfii

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Periyasamy Giridharan ◽  
Shilpa A. Verekar ◽  
Akash R. Gohil ◽  
Prabhu Dutt Mishra ◽  
Amit Khanna ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Cancer Cells ◽  
High Throughput ◽  
Antiproliferative Activity ◽  
High Throughput Screening ◽  
Spectroscopic Data ◽  
Caspase 3 ◽  
Tumor Suppressor Protein ◽  
Natural Form ◽  
Tumor Suppressor Protein P53

Secondary metabolites from fungi organisms have extensive past and present use in the treatment of many diseases and serve as compounds of interest both in their natural form and as templates for synthetic modification. Through high throughput screening (HTS) and bioassay-guided isolation, we isolated two bioactive compounds hamigerone (1) and radicinol (2). These compounds were isolated from fungusBipolaris papendorfii, isolated from the rice fields of Dera, Himachal Pradesh, India. The structures of the compounds were established on the basis of spectroscopic data, namely, NMR (1H,13C, mass, and UV). Both compounds were found to be antiproliferative against different cancer cells. Furthermore we have also noted that both compounds showed increase in apoptosis by favorably modulating both tumor suppressor protein (p53) and antiapoptic protein (BCL-2), and in turn increase caspase-3 expression in cancer cells. This is the first report of these compounds from fungusBipolaris papendorfiiand their anticancer activity.

scholarly journals Sensitive ADAR editing reporter in cancer cells enables high-throughput screening of small molecule libraries

2018 ◽  
Vol 47 (4) ◽  
pp. e22-e22 ◽  
Author(s):  
Kajsa Fritzell ◽  
Li-Di Xu ◽  
Magdalena Otrocka ◽  
Claes Andréasson ◽  
Marie Öhman
Keyword(s):  
Cancer Cells ◽  
Small Molecule ◽  
High Throughput ◽  
High Throughput Screening ◽  
Small Molecule Libraries ◽  
Adar Editing

High throughput screening to identify new compounds with proapoptotic activity in resistant lung cancer cells

2015 ◽  
Vol 32 (3) ◽  
pp. 324
Author(s):  
P. Gilson ◽  
L. Vanwonterghem ◽  
F. Mahuteau ◽  
S. Piguel ◽  
J.L. Coll ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
High Throughput ◽  
High Throughput Screening ◽  
Lung Cancer Cells ◽  
New Compounds

Inhibitor or promoter? The performance of polysaccharides from Ganoderma lucidum on human tumor cells with different p53 statuses

2016 ◽  
Vol 7 (4) ◽  
pp. 1872-1875 ◽  
Author(s):  
Jue Zhang ◽  
Jun-ming Chen ◽  
Xiao-xia Wang ◽  
Yong-mei Xia ◽  
Steve W. Cui ◽  
...  
Keyword(s):  
Cell Growth ◽  
Tumor Suppressor ◽  
Cancer Cells ◽  
Tumor Cells ◽  
Ganoderma Lucidum ◽  
Human Tumor ◽  
Tumor Suppressor Protein ◽  
Human Tumor Cells ◽  
Cancer Cell Growth ◽  
Tumor Suppressor Protein P53

GLPs inhibit cancer cell growth when the tumor suppressor protein p53 is functional but often stimulate cancer cells when p53 is absent.

scholarly journals Phytochemicals potently inhibit migration of metastatic breast cancer cells

2015 ◽  
Vol 7 (7) ◽  
pp. 792-800 ◽  
Author(s):  
Stephanie Lemmo Ham ◽  
Samila Nasrollahi ◽  
Kush N. Shah ◽  
Andrew Soltisz ◽  
Sailaja Paruchuri ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Metastatic Breast Cancer ◽  
Cancer Cells ◽  
High Throughput ◽  
High Throughput Screening ◽  
Breast Cancer Cells ◽  
Metastatic Breast ◽  
Natural Compounds ◽  
Screening Technology

A high throughput screening technology enables identifying natural compounds, phytochemicals, that potently inhibit migration of metastatic breast cancer cells.

scholarly journals Momordica charantia (Indian and Chinese Bitter Melon) Extracts Inducing Apoptosis in Human Lung Cancer Cell Line A549 via ROS-Mediated Mitochodria Injury

2019 ◽  
Vol 2019 ◽  
pp. 1-9 ◽  
Author(s):  
Siroshini Thiagarajan ◽  
Daryl J. Arapoc ◽  
Nurul Husna Shafie ◽  
Yong Yoke Keong ◽  
Hasnah Bahari ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
Antiproliferative Activity ◽  
Caspase 3 ◽  
Human Lung ◽  
Momordica Charantia ◽  
Lung Cancer Cells ◽  
Human Lung Cancer ◽  
Bitter Melon ◽  
Human Lung Cancer Cells

Lung cancer is the leading cause of cancer related deaths worldwide with about 40% occurring in developing countries. The two varieties of Momordica charantia, which are Chinese and Indian bitter melon, have been subjected to antiproliferative activity in human non-small cell lung cells A549. The A549 cells were treated with hot and cold aqueous extraction for both the bitter melon varieties, and the antiproliferative activity was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The apoptotic mechanism of action on A549 human lung cancer cells was evaluated first morphologically using Hoechst 33358, and cytoskeleton staining using Filamentous-actin (F-actin) cytoskeleton FICT and DAPI followed by caspase-3/7, reactive oxygen species (ROS), and p53 activity. Chinese hot aqueous extraction (CHA) exhibited potent antiproliferative activity against A549 human lung cancer cells. The morphological analysis of mitochondria destruction and the derangement of cytoskeleton showed apoptosis-inducing activity. CHA increased the caspase-3/7 activity by 1.6-fold and the ROS activity by 5-fold. Flow cytometric analysis revealed 34.5% of apoptotic cells significantly (p<0.05) compared to cisplatin-treated A549 human cancer cells. CHA is suggested to induce apoptosis due to their rich bioactive chemical constituents. These findings suggest that the antiproliferative effect of CHA was due to apoptosis via ROS-mediated mitochondria injury.

scholarly journals High-Throughput Fluorescence Assay for Small-Molecule Inhibitors of Autophagins/Atg4

2011 ◽  
Vol 16 (2) ◽  
pp. 174-182 ◽  
Author(s):  
Chih-Wen Shu ◽  
Charitha Madiraju ◽  
Dayong Zhai ◽  
Kate Welsh ◽  
Paul Diaz ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Caspase 3 ◽  
Bioactive Molecules ◽  
Dependent Manner ◽  
Chemical Libraries ◽  
Evolutionarily Conserved ◽  
Identification And Characterization

Autophagy is an evolutionarily conserved process for catabolizing damaged proteins and organelles in a lysosome-dependent manner. Dysregulation of autophagy may cause various diseases, such as cancer and neurodegeneration. However, the relevance of autophagy to diseases remains controversial because of the limited availability of chemical modulators. Herein, the authors developed a fluorescence-based assay for measuring activity of the autophagy protease, autophagin-1(Atg4B). The assay employs a novel reporter substrate of Atg4B composed of a natural substrate (LC3B) fused to an assayable enzyme (PLA2) that becomes active upon cleavage by this cysteine protease. A high-throughput screening (HTS) assay was validated with excellent Z′ factor (>0.7), remaining robust for more than 5 h and suitable for screening of large chemical libraries. The HTS assay was validated by performing pilot screens with 2 small collections of compounds enriched in bioactive molecules ( n = 1280 for Lopac™ and 2000 for Spectrum™ library), yielding confirmed hit rates of 0.23% and 0.70%, respectively. As counterscreens, PLA2 and caspase-3 assays were employed to eliminate nonspecific inhibitors. In conclusion, the LC3B-PLA2 reporter assay provides a platform for compound library screening for identification and characterization of Atg4B-specific inhibitors that may be useful as tools for interrogating the role of autophagy in disease models.

scholarly journals High-Throughput Identification of Inhibitors of Human Mitochondrial Peptide Deformylase

2007 ◽  
Vol 12 (4) ◽  
pp. 521-535 ◽  
Author(s):  
Christophe Antczak ◽  
David Shum ◽  
Sindy Escobar ◽  
Bhramdeo Bassit ◽  
Earl Kim ◽  
...  
Keyword(s):  
High Throughput ◽  
Antiproliferative Activity ◽  
High Throughput Screening ◽  
Peptide Deformylase ◽  
Chemical Libraries ◽  
New Class ◽  
Cytotoxicity Studies ◽  
Antiproliferative Agent ◽  
And Performance

The human mitochondrial peptide deformylase (HsPDF) provides a potential new target for broadly acting antiproliferative agents. To identify novel nonpeptidomimetic and nonhydroxamic acid—based inhibitors of HsPDF, the authors have developed a high-throughput screening (HTS) strategy using a fluorescence polarization (FP)—based binding assay as the primary assay for screening chemical libraries, followed by an enzymatic-based assay to confirm hits, prior to characterization of their antiproliferative activity against established tumor cell lines. The authors present the results and performance of the established strategy tested in a pilot screen of 2880 compounds and the identification of the 1st inhibitors. Two common scaffolds were identified within the hits. Furthermore, cytotoxicity studies revealed that most of the confirmed hits have antiproliferative activity. These findings demonstrate that the designed strategy can identify novel functional inhibitors and provide a powerful alternative to the use of functional assays in HTS and support the hypothesis that HsPDF inhibitors may constitute a new class of antiproliferative agent. ( Journal of Biomolecular Screening 2007:521-535)

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