Bevacizumab: Review of Development, Pharmacology, and Application to Brain Tumors

Newton, Herbert B.

doi:10.4137/cmt.s2042

Cited by 4 publications

(3 citation statements)

References 115 publications

(194 reference statements)

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“…Due to its therapeutic efficacy and increasing use in clinical oncology [1,3,7], the understanding of the in vivo behaviour and physiological mechanism of action, as well as of the toxic and chemotherapeutic adverse side effects of BEVA is of utmost importance.…”

Section: Introductionmentioning

confidence: 99%

In situ dsDNA-bevacizumab anticancer monoclonal antibody interaction electrochemical evaluation

Tomé

Marques

Diculescu

et al. 2015

Analytica Chimica Acta

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Section: Introductionmentioning

confidence: 99%

In situ dsDNA-bevacizumab anticancer monoclonal antibody interaction electrochemical evaluation

Tomé

Marques

Diculescu

et al. 2015

Analytica Chimica Acta

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“…But, there are some clinical problems of u n c o r r e c t e d p r o o f angiogenesis inhibitors in patients (i.e. thromboembolic disorders, intracranial hemorrhagia, and bowel perforation) 6 . Other problems are the occurrence of toxicities such as bleeding, fatigue, hypertension, perforation in gastrointestinal tract 7,8 .…”

Section: Introductionmentioning

confidence: 99%

Ferulic Acid Prevents Angiogenesis Through Cyclooxygenase-2 and Vascular Endothelial Growth Factor in the Chick Embryo Chorioallantoic Membrane Model

Ekowati¹,

Hamid²,

Diyah³

et al. 2020

tjps

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INTRODUCTION: This study designed to verify the antiangiogenic activity of ferulic acid (FA) and its potency to inhibit COX-2 and VEGF expression on CAM model. Moreover besides, we verified its mechanism of action by docking the molecule on COX-2, tyrosine kinase and VEGF-2 proteins in silico METHODS: Anti-angiogenesis assay of FA at the doses of 30, 60 and 90 μg were performed using CAM of chicken eggs with nine-day old which were stimulated by 60 ng basic fibroblast growth factor (b-FGF). Celecoxib 60 μg was used as reference drug. The inhibitory activity on VEGF and COX-2 expressions were conducted by immunohistochemistry assay (IHC). Molecular docking of FA were accomplished by Molegro Virtual Docker program ver. 5.5. on COX-2 enzyme (PDB ID 1CX2), tyrosine kinase receptor (PDB ID 1XKK) and VEGF-2 receptor (PDB ID 4ASD). RESULTS: FA at doses 30, 60, 90 μg significantly prevented angiogenesis on CAM model (p<0.05), which were represented as inhibitory activities against endothelial cell of blood vessels (42.6-70.7%) and neovascularization (43.0-86.6%). Inhibitory activities of FA against VEGF expression were stronger than its action on COX-2 expression. Molecular docking on VEGF-2 receptor result in RS value of FA was -73,844 kcal/mol, and celecoxib was -94.557 kcal/mol. RS value on tyrosine kinase of FA was -84.954 kcal/mol, while celecoxib was -93.163 kcal/mol. Docking on COX-2 receptor denoted RS value of FA was -73,416 kcal/mol, while celecoxib was -118,107 kcal/mol. DISCUSSION AND CONCLUSION: Reduction of VEGF-2 & COX-2 expression due to treatment with FA at dose range 30-90 μg seem to be related to angiogenesis inhibition, which is presented by two parameters, namely inhibition of neovascularization and endothelial cell growth in blood vessels It was concluded that FA is promising anti-angiogenic therapeutic agent especially at early stage, and this activity can be resulted from inhibitory action on COX-2 and VEGF-2 proteins.

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“…Unfortunately, bevacizumab also causes thromboembolic disorders, fatigue, intracranial hemorrhage, proteinuria, hypertension, and bowel perforation. [3,8,9].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Thiourea Derivatives From M-Methoxycinnamic Acid as Antiangiogenic Candidate

et al. 2019

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Microwave-assisted nucleophilic acyl substitution was employed to obtain thiourea derivatives (3a, 3b, 3c) from m-methoxycinnamic acid (1). This synthesis method successfully yielded 60-70% reaction product. In vivo anti-angiogenic evaluation was conducted by chick chorioallantoic membrane model, by which each of the derivative at dose 30, 60, and 90 µg induced by bFGF and compared to celecoxib 60 µg as positive control. It was found that all of the synthesized compound at the tested dose were able to inhibit neovascularization and formation of endothelial cell of new blood vessels by 51-75%. In silico analysis predicted that the anti-angiogenesis mechanism of all the synthesized compounds is through the inhibition of EGFR kinase and COX-2. N atom acts as hydrogen bonding acceptor by residue Gly526 of COX-2. While thiourea moieties of 3a-c have hydrophobic interaction by residues Ser530, Tyr385, and Leu352. In addition, the carbonyl group of thiourea of compound 3a-c inhibit EGFR kinase through the interaction with lys745. The pKCSM data revealed that 3a-c absorbed in intestine by 89-92%, and acut toxicity in rat category 4, suggesting that the compounds show good absorption, and low toxicity. In conclusion, this study successfully synthesized thiourea derivatives, which have anti-angiogenesis activity, tested by CAM model.

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Bevacizumab: Review of Development, Pharmacology, and Application to Brain Tumors

Cited by 4 publications

References 115 publications

In situ dsDNA-bevacizumab anticancer monoclonal antibody interaction electrochemical evaluation

In situ dsDNA-bevacizumab anticancer monoclonal antibody interaction electrochemical evaluation

Ferulic Acid Prevents Angiogenesis Through Cyclooxygenase-2 and Vascular Endothelial Growth Factor in the Chick Embryo Chorioallantoic Membrane Model

Synthesis of Thiourea Derivatives From M-Methoxycinnamic Acid as Antiangiogenic Candidate

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