Abstract 1006: Structural peculiarities of flavonoids influence anti-angiogenic, cytotoxic and antioxidant effects: experimental and insilico analysis

Abstract

Structural diversity of flavonoids and biological activities has remained an important discourse in the mainstream of flavonoid research. In the present studies different class of flavonoids such as flavones, flavanones and flavanolols were evaluated for their antiangiogenic, cytotoxic and antioxidant activities. The anti-angiogenic activity was evaluated using in vivo chorioallantoic membrane model (CAM), antioxidant potential and kinetics of free radical scavenging activity was determined using DPPH (2, 2-diphenyl-1-picryl hydrazine) and superoxide anion radical (SOR) scavenging assays, while cytotoxicity against selected cancer cell lines was carried out using MTT cell viability assay. The physicochemical properties/quantum chemical discriptors of the selected flavonoids were calculated using BioMed CAChe 6.1.10 drug. The selected flavonoids were docked in silico onto the proangiogenic peptides such as vascular endothelial growth factor (VEGF), hypoxia inducible factor (HIF-1α), and vascular endothelial growth factor receptor-2 (VEGFR2) and others from human origin. The results of the present investigation are discussed in the mainstream of structure activity relationship which may be useful in translating flavonoids as therapeutic molecules targeting angiogenesis. References 1. Gacche R. N. Shegokar Harshala, Gond Dhananjay , A. D. Jadhav and Ghole Vikram. (2010). Effect of Hydroxyl Substitution of Flavone on Antiangiogenic and Free Radical Scavenging Activities: A Structure Activity Relationship Studies Using Computational Tools. European J. Pharmaceutical Science 39, 37-44. 2. Gacche R. N. Shegokar Harshala, Gond Dhananjay , Zhenzhou Yang, A. D. Jadhav (2011). Evaluation of selected flavonoids as antiangiogenic, anticancer and radical scavenging agents: an experimental and in silico analysis. Cell Biochemistry and Biophysics 61, 651-663. DOI 10.1007/s12013-011-9252-z. 3. Gacche RN and Meshram RJ (2013) Targeting Tumor Micro-environment for Design and Development of Novel Anti-angiogenic Agents Arresting Tumor Growth. Progress in Biophysics & Molecular Biology 113 (2013) 333-354. Note: This abstract was not presented at the meeting. Citation Format: Raju N. Gacche, Harshala D. Shegokar, Dhananjay S. Gond, Rohan J. Meshram. Structural peculiarities of flavonoids influence anti-angiogenic, cytotoxic and antioxidant effects: experimental and insilico analysis. [abstract]. In: Proceedings of the 105th Annual Meeting of the American Association for Cancer Research; 2014 Apr 5-9; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2014;74(19 Suppl):Abstract nr 1006. doi:10.1158/1538-7445.AM2014-1006

Purple Sweet Potato Color Attenuates Kidney Damage by Blocking VEGFR2/ROS/NLRP3 Signaling in High-Fat Diet-Treated Mice

“…Recently, Shan et al have found that PSPC relieves kidney damage by inhibiting NLRP3-induced inflammation [8]. In addition, various flavonoids have been shown to inhibit VEGFR2 expression and its downstream signaling in the pathological angiogenesis of tumors and diabetic retinopathy [17, 18]. Given our preliminary evidence showing that VEGFR2 stimulated ROS overproduction, the current study aims at investigating whether PSPC alleviates kidney injury by downregulating VEGFR2-mediated oxidation stress and inflammation and further explaining the pathological mechanism underlying kidney damage in HFD-treated mice.…”