Design, synthesis and in vitro biological evaluation of non-redox inhibitors of leukotriene biosynthesis on the basis of medicinal plant derived lead compounds:
Gespeichert in:
| 1. Verfasser: | |
|---|---|
| Format: | Buch |
| Sprache: | English |
| Veröffentlicht: |
1999
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| Schlagworte: | |
| Online-Zugang: | Inhaltsverzeichnis |
| Beschreibung: | Regensburg, Univ., Diss., 1999 |
| Beschreibung: | 247 S. Ill., graph. Darst. |
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| adam_text | V- DESIGN, SYNTHESIS AND IN VITRO BIOLOGICAL EVALUATION OF NON- REDOX
INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS ON THE BASIS OF MEDICINAL PLANT
DERIVED LEAD COMPOUNDS DISSERTATION IN FULFILMENT OF THE REQUIREMENTS
FOR THE DEGREE DOKTOR DER NATURWISSENSCHAFTEN (DR. RER. NAT.) OF THE
NATURWISSENSCHAFTLICHE FAKULTST IV CHEMIE UND PHARMAZIE OF THE
UNIVERSITY OF REGENSBURG PRESENTED BY SUNIL KUMAR K. C. FROM KATHMANDU,
NEPAL 1999 CONTENTS: I INTRODUCTION: CHEMICAL, BIOCHEMICAL AND
PHARMACOLOGICAL ASPECTS OF LEUKOTRIENES 1 DISCOVERY AND CHEMICAL
CHARACTERIZATION OF LEUKOTRIENES 1 2 BIOSYNTHESIS OF LEUKOTRIENES 2 3
LIPOXYGENASES 5 4 PHARMACOLOGY AND PATHOPHYSIOLOGY OF LEUKOTRIENES 8 5
INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS 9 5.1 ANTIOXIDANTS AND FREE
RADICAL SCAVENGERS 9 5.2 IRON CHELATORS 10 5.3 FLAP BINDING INHIBITORS
11 5.4 SUBSTRATE AND PRODUCT ANALOGS 12 5.5 STRUCTURALLY UNRELATED
COMPOUNDS 12 6 PURPOSE AND PROSPECTS OF THE PRESENT WORK 13 T NATURAL
PRODUCT CHEMISTRY: EXTRACTION, ISOLATION AND STRUCTURE ELUCIDATION OF
CHEMICAL CONSTITUENTS FROM MEDICINAL PLANTS 1 INTRODUCTION 14 2
ETHNOBOTANICAL SURVEY, PLANT COLLECTION AND EXTRACTION 15 3 ISOLATION
AND STRUCTURE ELUCIDATION 17 3.1 CHEMICAL CONSTITUENTS OF ZANTHOXYLUM
NEPALENSIS 17 3.2 CHEMICAL CONSTITUENTS OF ZANTHOXYLUM ARMATUM 21 3.3
CHEMICAL CONSTITUENTS OF PARMELIA NEPALENSIS 23 3.4 CHEMICAL
CONSTITUENTS OF MAHONIA NEPALENSIS 26 3.5 CHEMICAL CONSTITUENTS OF
PARMELIA TINCTORWN 32 3.6 CHEMICAL CONSTITUENTS OF SOLARIUM NIGRUM 34 4
HPLC ANALYSIS OF BIOLOGICALLY ACTIVE EXTRACTS 36 4.1 HPLC PROFILE OF
HYOSCYAMUS NIGER 38 4.2 HPLC PROFILE OF CITRULLUS COLOCYNTHIS... 39 4.3
HPLC PROFILES OF SOME COMMON LICHEN SPECIES ; 40 SYNTHESIS: DESIGN,
SYNTHESIS AND CHARACTERIZATION OF NOVEL DERIVATIVES OF DIFFRACTAIC,
BARBATIC AND OBTUSATIC ACID 1 INTRODUCTION 41 2 GENERAL SYNTHETIC
STRATEGY 42 3 SYNTHESIS AND CHARACTERIZATION OF NOVEL DERIVATIVES OF
DIFFRACTAIC ACID 45 4 SYNTHESIS AND CHARACTERIZATION OF NOVEL
DERIVATIVES OF BARBATIC ACID 51 5 SYNTHESIS AND CHARACTERIZATION OF
NOVEL DERIVATIVES OF OBTUSATIC ACID 54 6 SYNTHESIS AND CHARACTERIZATION
OF NOVEL DERIVATIVES OF METHYLOBTUSATIC ACID 56 ) BIOCHEMICAL PART: IN
VITRO BIOLOGICAL EVALUATION OF MEDICINAL PLANT EXTRACTS, THEIR
CONSTITUENTS AND NOVEL DERIVATIVES OF ACTIVE PRINCIPLES 1 INTRODUCTION
58 2 EVALUATION OF LEUKOTRIENE BIOSYNTHESIS INHIBITION 58 2.1
INTRODUCTION 58 2.2 TEST SYSTEM 59 2.3 INHIBITION OF LEUKOTRIENE
BIOSYNTHESIS BY MEDICINAL PLANT EXTRACTS 60 2.4 INHIBITION OF
LEUKOTRIENE BIOSYNTHESIS BY CHEMICAL CONSTITUENTS ISOLATED FROM ACTIVE
PLANT EXTRACTS 63 2.5 INHIBITION OF LEUKOTRIENE BIOSYNTHESIS BY NOVEL
DERIVATIVES OF DIFFRACTAIC ACID... 66 2.6 INHIBITION OF LEUKOTRIENE
BIOSYNTHESIS BY NOVEL DERIVATIVES OF BARBATIC ACID 70 2.7 INHIBITION OF
LEUKOTRIENE BIOSYNTHESIS BY NOVEL DERIVATIVES OF OBTUSATIC ACID 73 2.8
INHIBITION OF LEUKOTRIENE BIOSYNTHESIS BY NOVEL DERIVATIVES OF
METHYLOBTUSATIC ACID 77 3 EVALUATION OF REDOX PROPERTIES 79 3.1
INTRODUCTION 79 3.2 TEST SYSTEMS 80 3.2.1 LIPID PEROXIDATION IN
BIOLOGICAL MEMBRANE 80 3.2.2 DEOXYRIBOSE DEGRADATION 84 3.2.3 RADICAL
SCAVENGING ACTIVITY 86 3.3 REDOX PROPERTIES OF MEDICINAL PLANT EXTRACTS
87 3.4 REDOX PROPERTIES OF CHEMICAL CONSTITUENTS ISOLATED FROM ACTIVE
EXTRACTS 90 3.5 REDOX PROPERTIES OF NOVEL DERIVATIVES OF DIFFRACTAIC
ACID 93 3.6 REDOX PROPERTIES OF NOVEL DERIVATIVES OF BARBATIC ACID 95
3.7 REDOX PROPERTIES OF NOVEL DERIVATIVES OF OBTUSATIC AND
METHYLOBTUSATIC ACID.... 97 4 ANTIPROLIFERATIVE ACTIVITY AGAINST HACAT
CELL 100 4.1 INTRODUCTION 100 4.2 TEST SYSTEMS 100 4.2.1
ANTIPROLIFERATIVE ACTIVITY 100 4.2.2 ASSAY TO MEASURE LDH IN THE CULTURE
MEDIUM 102 4.3 ANTIPROLIFERATIVE AND CYTOTOXIC ACTIVITY OF MEDICINAL
PLANT EXTRACTS 103 4.4 ANTIPROLIFERATIVE AND CYTOTOXIC ACTIVITY OF
CHEMICAL CONSTITUENTS ISOLATED FROM ACTIVE EXTRACTS 107 4.5
ANTIPROLIFERATIVE AND CYTOTOXIC ACTIVITY OF BARBATIC AND DIFFRACTAIC
ACID DERIVATIVES 110 E SUMMARY 113 F ZUSAMMENFASSUNG 117 G EXPERIMENTAL
PART 1 STANDARD EXPERIMENTAL CONDITIONS 121 2 ISOLATION 124 2.1 CHEMICAL
CONSTITUENTS OF ZANTHOXYLUM NEPALENSIS 124 2.2 CHEMICAL CONSTITUENTS OF
ZANTHOXYLUM ARMATUM 126 2.3 CHEMICAL CONSTITUENTS OF PARMELIA NEPALENSIS
128 2.4 CHEMICAL CONSTITUENTS OF MAHONIA NEPALENSIS 132 2.5 CHEMICAL
CONSTITUENTS OF PARMELIA TINCTORUM 136 2.6 CHEMICAL CONSTITUENTS OF
SOLATIUM NIGRUM 137 3 SYNTHETIC METHODS AND ANALYTICAL DATA 139 3.1
SYNTHESIS OF DIFFRACTAIC ACID ANALOGS 139 3.2 SYNTHESIS OF BARBATIC ACID
ANALOGS 166 3.3 SYNTHESIS OF OBTUSATIC ACID ANALOGS 185 3.4 SYNTHESIS OF
METHYLOBTUSATIC ACID ANALOGS 204 4 5-LIPOXYGENASE ASSAY IN BOVINE
POLYMORPHONUCLEAR LEUKOCYTES 221 4.1 REAGENTS AND MATERIALS 221 4.2
ISOLATION OF GRANULOCYTES 222 4.3 CELL COUNTING 223 4.4 DETERMINATION OF
CELL VIABILITY 223 4.5 INCUBATION PROCEDURE AND DETERMINATION OF
LIPOXYGENASE PRODUCTS 224 4.6 CALCULATION OF IC50 VALUES 225 5 ASSAY OF
LIPID PEROXIDATION IN BOVINE BRAIN PHOSPHOLIPID LIPOSOMES 226 5.1
REAGENTS AND MATERIALS 226 5.2 ISOLATION OF PHOSPHOLIPIDS FROM BOVINE
BRAIN 227 5.3 PREPARATION OF LIPOSOMES FROM PHOSPHOLIPIDS 227 5.4 ASSAY
OF LIPID PEROXIDATION AND CALCULATION OF IC50 VALUES 227 6 DEOXYRIBOSE
DEGRADATION 229 6.1 REAGENTS AND MATERIALS 229 6.2 DETERMINATION OF
HYDROXYL RADICAL GENERATING CAPACITY BY MEASURING DEOXYRIBOSE
DEGRADATION 229 7 DETERMINATION OF REDUCING ACTIVITY AGAINST DPPH 230
7.1 REAGENTS AND MATERIALS 230 7.2 DETERMINATION OF THE RATE CONSTANT OF
THE REACTION WITH DPPH 231 8 ANTIPROLIFERATIVE ACTIVITY AGAINST THE
GROWTH OF HUMAN KERATINOCYTES 231 8.1 REAGENTS AND MATERIALS 231 8.2
CELL CULTURE AND DETERMINATION OF CELL GROWTH 232 9 ASSAY OF LACTATE
DEHYDROGENASE RELEASE 233 9.1 REAGENTS AND MATERIALS 233 9.2 LDH ASSAY
233 H REFERENCES 235 INDEX: I STRUCTURE OVERVIEW
|
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| spelling | Sunil Kumar, K. C. Verfasser (DE-588)121805921 aut Design, synthesis and in vitro biological evaluation of non-redox inhibitors of leukotriene biosynthesis on the basis of medicinal plant derived lead compounds presented by Sunil Kumar K. C. 1999 247 S. Ill., graph. Darst. txt rdacontent n rdamedia nc rdacarrier Regensburg, Univ., Diss., 1999 Pflanzeninhaltsstoff (DE-588)4139067-2 gnd rswk-swf Heilpflanzen (DE-588)4024076-9 gnd rswk-swf Leukotriene (DE-588)4198723-8 gnd rswk-swf Inhibitor (DE-588)4027007-5 gnd rswk-swf Biosynthese (DE-588)4006902-3 gnd rswk-swf (DE-588)4113937-9 Hochschulschrift gnd-content Leukotriene (DE-588)4198723-8 s Biosynthese (DE-588)4006902-3 s Inhibitor (DE-588)4027007-5 s Heilpflanzen (DE-588)4024076-9 s Pflanzeninhaltsstoff (DE-588)4139067-2 s DE-604 GBV Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=008722048&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Sunil Kumar, K. C. Design, synthesis and in vitro biological evaluation of non-redox inhibitors of leukotriene biosynthesis on the basis of medicinal plant derived lead compounds Pflanzeninhaltsstoff (DE-588)4139067-2 gnd Heilpflanzen (DE-588)4024076-9 gnd Leukotriene (DE-588)4198723-8 gnd Inhibitor (DE-588)4027007-5 gnd Biosynthese (DE-588)4006902-3 gnd |
| subject_GND | (DE-588)4139067-2 (DE-588)4024076-9 (DE-588)4198723-8 (DE-588)4027007-5 (DE-588)4006902-3 (DE-588)4113937-9 |
| title | Design, synthesis and in vitro biological evaluation of non-redox inhibitors of leukotriene biosynthesis on the basis of medicinal plant derived lead compounds |
| title_auth | Design, synthesis and in vitro biological evaluation of non-redox inhibitors of leukotriene biosynthesis on the basis of medicinal plant derived lead compounds |
| title_exact_search | Design, synthesis and in vitro biological evaluation of non-redox inhibitors of leukotriene biosynthesis on the basis of medicinal plant derived lead compounds |
| title_full | Design, synthesis and in vitro biological evaluation of non-redox inhibitors of leukotriene biosynthesis on the basis of medicinal plant derived lead compounds presented by Sunil Kumar K. C. |
| title_fullStr | Design, synthesis and in vitro biological evaluation of non-redox inhibitors of leukotriene biosynthesis on the basis of medicinal plant derived lead compounds presented by Sunil Kumar K. C. |
| title_full_unstemmed | Design, synthesis and in vitro biological evaluation of non-redox inhibitors of leukotriene biosynthesis on the basis of medicinal plant derived lead compounds presented by Sunil Kumar K. C. |
| title_short | Design, synthesis and in vitro biological evaluation of non-redox inhibitors of leukotriene biosynthesis on the basis of medicinal plant derived lead compounds |
| title_sort | design synthesis and in vitro biological evaluation of non redox inhibitors of leukotriene biosynthesis on the basis of medicinal plant derived lead compounds |
| topic | Pflanzeninhaltsstoff (DE-588)4139067-2 gnd Heilpflanzen (DE-588)4024076-9 gnd Leukotriene (DE-588)4198723-8 gnd Inhibitor (DE-588)4027007-5 gnd Biosynthese (DE-588)4006902-3 gnd |
| topic_facet | Pflanzeninhaltsstoff Heilpflanzen Leukotriene Inhibitor Biosynthese Hochschulschrift |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=008722048&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
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