In vitro and in vivo studies on stilbene analogs as potential treatment agents for colon cancer.

European Journal of Medicinal Chemistry
Shiby PaulAgnes M Rimando

Abstract

Based on the potential of resveratrol as a colon cancer chemopreventive agent, a set of 26 stilbenes were synthesized and tested against the colon cancer cell lines HT-29 and Caco-2. (Z)-4-(3,5-Dimethoxystyryl)aniline (4), (Z)-methyl-4-(3,5-dimethoxystyryl)benzoate (6), and (Z)-1,3-dimethoxy-5-(4-methoxystyryl)benzene (10) showed strong inhibitory activity in vitro. In vivo studies using HT-29 xenografts in immunodeficient mice were conducted with 4, 6 and 10, together with their corresponding trans isomers (3, 5, and 9, respectively), at the dose of 10 mg/kg body weight. Tumor volume was significantly lowered in 3-, 4-, and 9-treated groups. The cis- and trans-amino analogs (4 and 3, respectively) had similar effect on tumor growth, a 40% decrease compared to the control. Analysis of the serum revealed that 4 isomerized to 3, which may explain their similar effects in SCID mice. Stilbenes 5, 6, 9, and 10 retained their configurations in the serum. Stilbenes 6 and 10 lacked tumor-suppressive effect in SCID mice; the serum levels of these analogs were low (18.8 and 15.5 ng/mL, respectively). Stilbene 9, while weakly active in vitro demonstrated good activity in vivo, was found at higher levels in the serum (69.9 ng/mL) compared ...Continue Reading

Citations

Jul 3, 2013·Current Colorectal Cancer Reports·Bharat AggarwalSushovan Guha
Dec 7, 2011·Critical Reviews in Clinical Laboratory Sciences·Miguel AsensiJosé M Estrela
Apr 14, 2015·Seminars in Cancer Biology·Stephanie C CaseyDean W Felsher
Nov 20, 2014·Journal of Enzyme Inhibition and Medicinal Chemistry·Fahad S AldawsariCarlos A Velázquez-Martínez
Jun 6, 2015·Toxicology and Applied Pharmacology·Maria-Christina ScherzbergSandra Ulrich-Rückert
Jul 28, 2015·Annals of the New York Academy of Sciences·Avinash KumarAnait S Levenson
May 30, 2015·Chemistry Central Journal·Vishal C BirarElizabeth L Ostler
Feb 28, 2015·Investigational New Drugs·Fahad S Aldawsari, Carlos A Velázquez-Martínez
Mar 8, 2017·ChemMedChem·Barbara De FilippisRosa Amoroso
Mar 29, 2012·Chemistry : a European Journal·Xiao-Yan CaoBo Zhou
Jul 1, 2014·Journal of Nutritional Science and Vitaminology·Takakazu MitaniRyoichi Yamaji
Apr 22, 2017·Molecular Diversity·Zulfiqar Ali KhanSohail Anjum Shahzad
Jul 12, 2017·Genetics and Molecular Biology·Cassia Suemi MizunoRaquel Alves Dos Santos

❮ Previous
Next ❯

Related Concepts

Related Feeds

Cell Checkpoints & Regulators

Cell cycle checkpoints are a series of complex checkpoint mechanisms that detect DNA abnormalities and ensure that DNA replication and repair are complete before cell division. They are primarily regulated by cyclins, cyclin-dependent kinases, and the anaphase-promoting complex/cyclosome. Here is the latest research.

Aminoglycosides

Aminoglycoside is a medicinal and bacteriologic category of traditional Gram-negative antibacterial medications that inhibit protein synthesis and contain as a portion of the molecule an amino-modified glycoside. Discover the latest research on aminoglycoside here.

Aminoglycosides (ASM)

Aminoglycoside is a medicinal and bacteriologic category of traditional Gram-negative antibacterial medications that inhibit protein synthesis and contain as a portion of the molecule an amino-modified glycoside. Discover the latest research on aminoglycoside here.

Cell Cycle Pathways

Cell cycle is a complex process regulated by several signal transduction pathways and enzymes. Here is the latest research on regulation of cell cycle and cell cycle pathways.

Bioinformatics in Biomedicine

Bioinformatics in biomedicine incorporates computer science, biology, chemistry, medicine, mathematics and statistics. Discover the latest research on bioinformatics in biomedicine here.