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Title of Thesis

Talat Makhmoor
Institute/University/Department Details
H.E.J. Research Institute of Chemistry/ University of Karachi
Number of Pages
Keywords (Extracted from title, table of contents and abstract of thesis)
antioxidant activity, synthetic compounds, xanthine oxidase inhibitors, bilirubins, transaminases, cytotoxicity assay, antioxidants, fungal cultures,

This dissertation describes studies on antioxidant activities of a number of chemical compounds, natural in origin or synthesized in the laboratory. As a result of this study, a total of eighty four compounds were identified as antioxidants. Out of these eighteen new and twelve known phytochemicals were isolated from different medicinally important plants and fungal cultures, while fifty four synthetic chemical constituents, belonging to six different classes of compounds, were identified as antioxidants. Modification of the structures of parent chemical constituents of each class of synthetic compounds resulted in enhancement of antioxidant activity. The antioxidant activities of these compounds were determined through their radical scavenging and xanthine oxidase inhibition potential using three assays. First, all the compounds were checked for radical scavenging activity in an in vitro method, i.e. DPPH radical scavenging assay. Compounds which showed radical scavenging activity in DPPH radical scavenging assay were further studied for their superoxide anion scavenging potential using NADH/PMS/O2 assay. The compounds which were checked for radical scavenging activity were also assayed for xanthine oxidase inhibition. Based on the bioassay results, structure-activity relationship (SAR) studies on different classes of antiradical and xanthine oxidase inhibitors were conducted. The six most active xanthine oxidase inhibitors were also studied for their kinetic behavior. In vivo studies using CC4-induced liver toxicity assay in rat model on the selected twenty eight compounds of synthetic and natural origins, were also carried out. From these different classes of compounds, the most active compounds were subjected to in vivo studies. Subsequently, these compounds were also checked for their Cytotoxicity using a Sensitive in vitro Cytotoxicity assay on human neutrophils.-------------------------------------------------------------------------------------------------------------------

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3011.79 KB
S. No. Chapter Title of the Chapters Page Size (KB)
1 0 Contents
233.88 KB
2 1 Introduction 1-28
382.28 KB
  1.1 General Introduction 1
  1.2 Reactive Oxygen Species( Ros ) 2
  1.3 Antioxidants 11
  1.4 Aims Of The Present Study 27-28
3 2 In Vitro Antioxidants Studies On Natural Products 29-63
581.43 KB
  2.1 Standard Antioxidants 29-31
  2.2 Triterpendoids 32-36
  2.3 Cinnamic Acid Derivatives 37-42
  2.4 Phenylethanoid Glycosides 42-47
  2.5 Coumarins 45
  2.6 Aurone, Ferulic Acid And Salireposide Derivatives 54-57
  2.7 Stibene Glycosides 57-59
  2.8 Ellagic Acid Derivatives 60-61
  2.9 Proposed Mechanism Of Action Of Antiradical Compounds 62-63
4 3 In Vitro Antioxidant Studies On Synthetic Compounds 64-107
774.97 KB
  3.1 Acyl Hydrazides 64-73
  3.2 Oxadiazole Thione Derivatives 74-84
  3.3 Triazole Thione Derivatives 90-94
  3.4 Coumarin Derivatives 95-102
  3.5 Benzothiazepine Derivatives 103-107
5 4 Kinetics Studies On Some Xanthine Oxidase Inhibitors 108-114
72.56 KB
  4.1 Kinetic Studies On Cinnamic Acid Derivative And Stibenes
  4.2 Kinetic Studies On 1,3,4-Oxadizole-2-(3-H)- Thione Derivatives
6 5 In Vivo Studies On Natural/ Synthetic Antioxidants 115-142
408.5 KB
  5.1 Effect Of Saline And Cci 4 On Transaminases And Bilirubins 115
  5.2 Effects Of Natural Antioxidant On Transaminases And Bilirubins 116-123
  5.3 Effect Of Synthetic Antioxidants On Transaminases And Bilirubins 114
7 6 Cytotoxicity Studies 143-149
86.83 KB
  6.1 Cytotoxicity Study On Natural Antioxidants 143-144
  6.2 Cytotoxicity Study On Synthetic Antioxidants 145-149
8 7 Conclusion 150-153
35.88 KB
9 8 Experimental 154-169
160.41 KB
  8.1 Materials 154
  8.2 In Vitro Assays 155-156
  8.3 In Vivo Assay 163-166
  8.4 Cytotoxicity Assay 167-169
10 9 Bibliography 170-192
282.29 KB
11 10 Appendix 193-201
255.94 KB