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Bio-Pharmacological Screening on Liver-Protective and Anti-Hepatocarcinoma Activities of Vietnam Natural Products Minh Quan Pham

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Bio-Pharmacological Screening on Liver-Protective and Anti-Hepatocarcinoma Activities of Vietnam Natural Products Minh Quan Pham Bio-pharmacological screening on liver-protective and anti-hepatocarcinoma activities of Vietnam natural products Minh Quan Pham To cite this version: Minh Quan Pham. Bio-pharmacological screening on liver-protective and anti-hepatocarcinoma ac- tivities of Vietnam natural products. Pharmacology. Université Paul Sabatier - Toulouse III, 2016. English. NNT : 2016TOU30042. tel-01473865 HAL Id: tel-01473865 https://tel.archives-ouvertes.fr/tel-01473865 Submitted on 22 Feb 2017 HAL is a multi-disciplinary open access L’archive ouverte pluridisciplinaire HAL, est archive for the deposit and dissemination of sci- destinée au dépôt et à la diffusion de documents entific research documents, whether they are pub- scientifiques de niveau recherche, publiés ou non, lished or not. The documents may come from émanant des établissements d’enseignement et de teaching and research institutions in France or recherche français ou étrangers, des laboratoires abroad, or from public or private research centers. publics ou privés. THTHESEESE`` En vue de l’obtention du DOCTORAT DE L’UNIVERSITE´ DE TOULOUSE D´elivr´e par : l’Universit´eToulouse 3 Paul Sabatier (UT3 Paul Sabatier) Pr´esent´ee et soutenue le 30/05/2016 par : Minh Quan PHAM Bio-pharmacological screening on liver-protective and anti-hepatocarcinoma activities of Vietnam natural products JURY M. Etienne CHATELUT, Professeur, Universit´ePaul Sabatier, Toulouse Pr´esident du Jury M. Lars Petter JORDHEIM, MCU-HDR, INSERM U1052 - CNRS 5286, Lyon Rapporteur M. Georges MASSIOT, Directeur de Recherche, URCA, Reims Rapporteur M. Bruno DAVID, Docteur es-Sciences, Institut de Recherche Pierre FABRE Examinateur M. Quoc Long PHAM, Professeur, INPC-VAST, Vietnam Examinateur M. Jean Edouard GAIRIN, Professeur, Universit´ePaul Sabatier, Toulouse Directeur de th`ese Ecole´ doctorale et sp´ecialit´e : BSB : Pharmacologie Unit´e de Recherche : PHARMA DEV, IRD - Universit´ePaul Sabatier (UMR 152) Directeur de Th`ese : Pr. Jean Edouard GAIRIN THTHESEESE`` En vue de l’obtention du DOCTORAT DE L’UNIVERSITE´ DE TOULOUSE D´elivr´e par : l’Universit´eToulouse 3 Paul Sabatier (UT3 Paul Sabatier) Pr´esent´ee et soutenue le 30/05/2016 par : Minh Quan PHAM Bio-pharmacological screening on liver-protective and anti-hepatocarcinoma activities of Vietnam natural products JURY M. Etienne CHATELUT, Professeur, Universit´ePaul Sabatier, Toulouse Pr´esident du Jury M. Lars Petter JORDHEIM, MCU-HDR, INSERM U1052 - CNRS 5286, Lyon Rapporteur M. Georges MASSIOT, Directeur de Recherche, URCA, Reims Rapporteur M. Bruno DAVID, Docteur es-Sciences, Institut de Recherche Pierre FABRE Examinateur M. Quoc Long PHAM, Professeur, INPC-VAST, Vietnam Examinateur M. Jean Edouard GAIRIN, Professeur, Universit´ePaul Sabatier, Toulouse Directeur de th`ese Ecole´ doctorale et sp´ecialit´e : BSB : Pharmacologie Unit´e de Recherche : PHARMA DEV, IRD - Universit´ePaul Sabatier (UMR 152) Directeur de Th`ese : Pr. Jean Edouard GAIRIN You beat cancer by how you live, why you live, and in the manner in which you live Stuart Scott 1 2 Acknowledgements Foremost, it is a genuine pleasure to express my deep sense of thanks and gratitude to my supervisor Prof. Jean Edouard GAIRIN for the continuous support of my Ph.D study and research, for his patience, motivation, enthusiasm and immense knowledge. His guidance helped me in all the time of research and writing of this thesis. I could not have imagined having a better advisor and mentor for my Ph.D life in France. I would like to express my thank to Dr. MASSIOT Georges, Dr. JORDHEIM Lars Petter for their time and effort in checking this manuscript, their comments are very helpful for me. In addition, it is my fortunate to have Prof. Etienne CHATELUT and Dr. Bruno DAVID participate in my thesis committee. My sincere thank also goes to Stéphanie CAZE-SUBRA and Camille GIRONDE for their help during my beginning days in the laboratory, for your encouragement, discussions and all the fun we have had in the last three years. I thank to all the staff in the team “Cytométrie et Tri Cellulaire” at UMR INSERM 1043- CNRS UMR 5282: Fatima-Ezzahra L’FAQIHI-OLIVE, Valérie DUPLAN-ECHE and especially Anne-Laure ISCACHE for offering me the chance to do experiment in your laboratory. This work would not have been possible without their help. A grateful thank to: Lucie PALOQUE, Sandra BOURGEADE-DELMAS, Haouaria BELKHELFA, Pierre PÉRIO, Laure-Estelle CASSAGNES, Franck MARIE-SAINTE, Laïla HADDIOUI, Sokhna KEITA, Prof. Annick BARRE, Prof. Pierre ROUGÉ and my other labmates for their kind help and encouragement throughout my study period. Thanks to all my friends in AEVTL and UEVF organization for being an important part of my life and all the memorable experiences we have shared together during my life in France. It is my privilege to thank my girlfriend Mrs. Dao for being with me in the last two years. Without your love, constant support and encouragement, I could not have achieved these successes, both in my study and in social life. 3 Last but not least, I would like to thank my family: my parents, my younger sister and everybody for their unconditional love, caring, patients and understanding in every step of my life. I deeply thank you for everything ! 4 Table of Contents A - Introduction ...................................................................................................................... 13 B - Bibliographic Review ....................................................................................................... 17 1. Cancer and Hepatocellular Carcinoma ............................................................................ 19 1.1. Cancer ........................................................................................................................... 19 1.1.1. Overview of cancer ............................................................................................. 19 1.1.2. Aetiologies of Cancer ......................................................................................... 21 1.1.3. Mechanisms of cancer development ................................................................... 24 1.2. Hepatocellular Carcinoma (HCC) ................................................................................ 26 1.2.1. Overview of Hepatocellular Carcinoma ............................................................. 26 1.2.2. Aetiologies of Hepatocelluler Carcinoma .......................................................... 28 1.2.3. Pathogenesis of HCC development .................................................................... 29 1.3. Treatment against cancer .............................................................................................. 31 2. Natural products as sources of anticancer agents ........................................................... 34 2.1. The origin of medicine .................................................................................................. 34 2.2. The origin of cancer drugs ............................................................................................ 36 2.3. Overview of anticancer agents worldwide .................................................................... 37 2.3.1. Anticancer agents from plant .............................................................................. 37 2.3.2. Anticancer agents from marine organisms ......................................................... 40 2.3.3. Anticancer agents from microbial sources ......................................................... 43 2.4. Vision of the development of natural-derived anticancer agents ................................. 44 3. Vietnamese natural products as sources of anticancer agents ....................................... 46 3.1. Potential of Vietnamese plant sources .......................................................................... 46 3.2. Potential of Vietnamese marine sources ....................................................................... 47 3.3. Potential of Vietnamese microbial sources ................................................................... 48 5 4. Targeting mortalin – p53 interactions as an anti-cancer strategy ................................. 49 5. Overview of virtual screening in drug discovery ............................................................. 50 C - Thesis Objectives .............................................................................................................. 55 D - Materials and Methods .................................................................................................... 59 1. Plant Material ..................................................................................................................... 61 1.1. Natural compounds from medicinal plants of Vietnam ................................................ 61 1.2. Natural compounds from virtual screening .................................................................. 61 2. Virtual Screening ................................................................................................................ 61 2.1. Database of Vietnamese natural compounds ................................................................ 61 2.2. Protein preparation ........................................................................................................ 64 2.2.1. Primary Mortalin protein model – PDB ID: 3N8E ............................................. 65 2.2.2. Secondary Mortalin protein model – PDB ID: 4KBO ........................................ 65 2.2.3. Primary p53 protein model
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