Structure-Activity Relationship

Publication Title: 
Medicinal Chemistry (Shariqah (United Arab Emirates))

Non-steroidal anti-inflammatory drugs (NSAIDs) and cyclooxygenase-2 (COX-2) specific inhibitors are anti-inflammatory agents that have also shown to be useful in anticancer therapy. The effects of chebulagic acid (CA), a benzopyran tannin from Terminalia chebula having COX-2/5-LOX dual inhibitory properties, on the sensitivity of doxorubicin (Dox) in human hepatocellular carcinoma cell line HepG2 were studied in the present investigation. CA increased the accumulation of Dox in a concentration dependant manner and also enhanced the cytotoxicity of Dox in HepG2 cells by 20 folds.

Author(s): 
Achari, Chandrani
Reddy, Gorla V.
Reddy, T. C. M.
Reddanna, Pallu
Publication Title: 
Journal of Enzyme Inhibition and Medicinal Chemistry

Terminalia chebula fruit extracts were prepared sequentially with hexane, ethyl acetate, methanol and methanol-water (70:30) and tested for their ?-glucosidase inhibitory and antioxidant potential. The study resulted in the formulation of an extract with high ?-glucosidase inhibitory potential (IC(50) 0.19 ± 0.03 µg mL(-1)) enriched with hydrolysable tannins.

Author(s): 
Sasidharan, Indu
Sundaresan, A.
Nisha, V. M.
Kirishna, Mahesh S.
Raghu, K. G.
Jayamurthy, P.
Publication Title: 
Computational Biology and Chemistry

Drug resistant tuberculosis has threatened all the advances that have been made in TB control at the global stage in the last few decades. DNA gyrase enzymes are an excellent target for antibacterial drug discovery as they are involved in essential functions like DNA replication. Here we report, a successful application of high throughput virtual screening (HTVS) to identify an inhibitor of Mycobacterium DNA gyrase targeting the wild type and the most prevalent three double mutants of quinolone resistant DNA gyrase namely A90V+D94G, A74S+D94G and A90V+S91P.

Author(s): 
Patel, Kunal
Tyagi, Chetna
Goyal, Sukriti
Jamal, Salma
Wahi, Divya
Jain, Ritu
Bharadvaja, Navneeta
Grover, Abhinav
Publication Title: 
Bioorganic & Medicinal Chemistry Letters

Three new polyhydroxytriterpenoid derivatives, 23-O-neochebuloylarjungenin 28-O-?-d-glycopyranosyl ester (1), 23-O-4'-epi-neochebuloylarjungenin (2), and 23-O-galloylpinfaenoic acid 28-O-?-d-glucopyranosyl ester (17) were isolated from the fruits of Terminalia chebula Retz. along with fourteen known ones. Their structures were elucidated by 1D and 2D NMR spectroscopic data and acid hydrolysis.

Author(s): 
Lee, Dong Young
Yang, Heejung
Kim, Hyun Woo
Sung, Sang Hyun
Publication Title: 
International Journal of Radiation Biology

PURPOSE: Telomeres are specialized DNA-protein complexes found at the ends of eukaryotic chromosomes. In normal somatic cells these become shorter with each cell division and appear to control their replicative lifespan. However almost all tumours show activation of the enzyme telomerase, a specialised reverse transcriptase/DNA polymerase, that can add new telomeric repeats to the ends of chromosomes and this appears to be a key factor in the cell immortalization process.

Author(s): 
Laughton, C. A.
Grindon, C.
Girard, P.
Nikjoo, H.
Publication Title: 
Handbook of Experimental Pharmacology

Members of the sirtuin family including the founding protein Sir2 in Saccharomyces cerevisiae have been linked to lifespan extension in simple organisms. This finding prompted evaluation of the role of Sir2 orthologues in many aging-associated conditions including neurodegeneration, type II diabetes and cancer.

Author(s): 
Mahajan, Sumit S.
Leko, Vid
Simon, Julian A.
Bedalov, Antonio
Publication Title: 
Journal of Medicinal Chemistry

With the aim of up-regulating antitumor efficacy and down-regulating adverse effects, three types of aromatic imide and diimides were designed to couple with different polyamines. The in vitro assays revealed that two naphthalene diimide-polyamine conjugates could inhibit the growth of multiple cancer cell lines more potently than amonafide. 9f, the most potent compound, was verified to efficiently induce apoptosis via a ROS mediated mitochondrial pathway in a preliminary mechanistic study.

Author(s): 
Wang, Yuxia
Zhang, Xingbo
Zhao, Jin
Xie, Songqiang
Wang, Chaojie
Publication Title: 
Expert Opinion on Therapeutic Patents

INTRODUCTION: Reversible acetylation is a key post-translational modification of target proteins. Sirtuin deacetylases represent the homolog of the yeast silent information regulator (SIR2). Although seven sirtuins have been found in mammals, all sirtuin activators described to date act through SIRT1.

Author(s): 
Villalba, JosÈ M.
de Cabo, Rafael
Alcain, Francisco J.
Publication Title: 
Molecular and Cellular Biology

Telomerase is a cellular reverse transcriptase that uses part of its integral RNA (called TER) as the template to synthesize telomeric DNA repeats. Vertebrate TERs are thought to share a conserved, highly structured core domain that includes the templating sequence and a pseudoknot, but not all features of the predicted core structure have been verified directly or shown to affect telomerase enzymatic activity. Here, we report a systematic mutational analysis of the core domain (residues 1 to 210) of human telomerase RNA (hTER).

Author(s): 
Ly, Hinh
Blackburn, Elizabeth H.
Parslow, Tristram G.
Publication Title: 
Perspectives on Developmental Neurobiology

Cerebellar granule cells isolated from postnatal day 7 rat pups are ideal for studying epigenetic events associated with the regulation of neuronal gene expression. These cultures contain from 90 to 95% glutamatergic granule cells and express mRNAs encoding a variety of ionotropic and metabotropic glutamate receptors as well as virtually all of the GABAA-receptor subunit mRNAs to different extents. A unique feature of this culture system is that the neurons undergo time-dependent maturation changes in vitro that mimic many of the characteristics of these receptors occurring in vivo.

Author(s): 
Grayson, D. R.
Zhu, W.
Harris, B. T.
Vicini, S.
Zheng, T.

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