Radhakrishnan Narayanaswamy1, Majumder Shymatak2, Suvro Chatterjee2, Lam Kok Wai3, Gnanamani Arumugam4. 1. Microbiology Division, Central Leather Research Institute (CLRI), Chennai, India. ; Laboratory of Natural Products, Institute of Bioscience (IBS), Universiti Putra Malaysia (UPM), Serdang, Selangor, Malaysia. 2. Vascular Biology Laboratory, AU-KBC Research Centre, Anna University, Chennai, India. 3. Faculty of Pharmacy, Universiti Kebangsaan Malaysia (UKM), Jalan Raja Muda Abdul Aziz, Kuala Lumpur, Malaysia. 4. Microbiology Division, Central Leather Research Institute (CLRI), Chennai, India.
Abstract
PURPOSE: In recent year's anti-angiogenesis agents have been recognized as effective drugs for the treatment of solid tumors, this prompted us to conduct the present study. METHODS: The anti-angiogenic activity of dimeric form of embelin (vilangin) was evaluated using endothelial cell (in vitro) and chorioallantoic membrane (CAM) egg yolk angiogenesis model (in vivo) and in addition the docking behaviour of human nitric oxide synthases (NOS) with four different ligands was evaluated along with their putative binding sites using Discovery Studio Version 3.1 (in silico) compared with the parent compound (embelin). RESULTS: Vilangin exhibits 50% cytotoxic at 92 ± 1 µg/ml concentration level with reference to ECV 304 endothelial cells. Both vilangin and embelin, showed inhibitory effects on wound healing, single cell migration, nitric oxide production, and endothelial ring formation at 0.1 and 1.0 µg/ml concentration level. Similarly, CAM assay also showed inhibitory effect of vilangin and embelin with respect their reduction in length, size and junctions of blood capillaries compared to untreated egg yolk. Docking studies and binding free energy calculations revealed that vilangin has maximum interaction energy (-74.6 kcal/mol) as compared to the other investigated ligands. CONCLUSION: The results suggest that both vilangin and embelin attenuates angiogenesis in similar manner.
PURPOSE: In recent year's anti-angiogenesis agents have been recognized as effective drugs for the treatment of solid tumors, this prompted us to conduct the present study. METHODS: The anti-angiogenic activity of dimeric form of embelin (vilangin) was evaluated using endothelial cell (in vitro) and chorioallantoic membrane (CAM) egg yolk angiogenesis model (in vivo) and in addition the docking behaviour of humannitric oxide synthases (NOS) with four different ligands was evaluated along with their putative binding sites using Discovery Studio Version 3.1 (in silico) compared with the parent compound (embelin). RESULTS:Vilangin exhibits 50% cytotoxic at 92 ± 1 µg/ml concentration level with reference to ECV 304 endothelial cells. Both vilangin and embelin, showed inhibitory effects on wound healing, single cell migration, nitric oxide production, and endothelial ring formation at 0.1 and 1.0 µg/ml concentration level. Similarly, CAM assay also showed inhibitory effect of vilangin and embelin with respect their reduction in length, size and junctions of blood capillaries compared to untreated egg yolk. Docking studies and binding free energy calculations revealed that vilangin has maximum interaction energy (-74.6 kcal/mol) as compared to the other investigated ligands. CONCLUSION: The results suggest that both vilangin and embelin attenuates angiogenesis in similar manner.
Authors: M Niwa; N Nakamura; K Kitajima; M Ueda; Y Tsutsumishita; S Futaki; Y Takaishi Journal: Biochem Biophys Res Commun Date: 1997-10-20 Impact factor: 3.575
Authors: Radhakrishnan Narayana Swamy; A Gnanamani; Sangeetha Shanmugasamy; Ramesh Kumar Gopal; Asit Baran Mandal Journal: BMC Res Notes Date: 2011-10-12
Authors: Kurt Schmidt; Jens Martens-Lobenhoffer; Andreas Meinitzer; Wolfgang F Graier; Christina M Torres; Richard C Venema; Bernd Mayer Journal: Nitric Oxide Date: 2010-02-06 Impact factor: 4.427