Bradykinin, Kallidin and Kallikrein

ISBN-13: 9783642462245 / Angielski / Miękka / 2012 / 768 str.

Ervin G. Erdos;Anne F. Wilde

Opis

Bradykinin is frequently referred to as an elusive substance; the editor of a comprehensive volume dealing with kinins thus has a difficult task. The com- plexity of the issues calls for a large number of contributors who approach the topics from the various angles that are dictated by the sometimes divergent views of the individuals. The editor saw no reason to prescribe the mode of presentation, which was left to the authors and accounts for the variety of approaches. Contributors from nine countries were asked to participate in the volume. The chapters were organized to present, first, the history of the discoveries and methods of approach to kinin research. Then follows a discussion of the enzymes that release kinins, their substrates, and other enzymes that inactivate the peptides. If the release of kinin is important, then the inhibition of the releasing enzymes is of obvious interest and is described. Since the measurement of kinin- ogen levels in blood has been frequently used as an indicator of kinin liberation, in addition to a separate chapter, kininogens are also mentioned where the functions of kinins are discussed. The conclusions drawn from establishing structure-action relationships for many analogs and the actions of kinins are indicated and summarized.

Spis treści

1: Introduction.- Discovery of the Most Important Kallikreins and Kallikrein Inhibitors.- A. Discovery of Kallikrein from Urine.- B. Discovery of the Kallikrein Inhibitor of Blood Serum.- C. Discovery of F-Substance in Pancreas.- D. Discovery of Kallikrein in Salivary Glands and Saliva.- E. Discovery of Kallikreinogen in Pancreas and Pancreas Secretion and in Other Organs.- F. Discovery of Plasma Kallikrein.- G. Discovery of the Kallikrein Inhibitor of Bovine Organs (Trasylol).- H. Discovery of Kallidin and the Enzymatic Nature of Kallikrein.- J. Detection of Kallidin-Inactivating Enzymes.- References.- The Discovery and Characterization of Bradykinin.- References.- 2: Methods Used in Kinin Research.- The Kinins: Methods of Chemical Synthesis.- A. Methods of Peptide Synthesis.- B. Synthesis of Bradykinin.- C. Synthesis of Kallidin.- D. Synthesis of Methionyl-Lysyl-Bradykinin.- E. Synthesis of Nonmammalian Kinins.- References.- Purification of Mammalian Kallikreins, Kininogens, and Kinins.- A. Introduction.- I. Methodological Considerations.- II. Reporting Purification Results.- III. Possibility of a Unified Approach to the Purification of Kallikrein and Kininogen Homologs and Kinins.- B. Plasma Kallikreins.- I. Hog Serum Kallikrein (Habermann and Klett, 1966).- II. Human Plasma Kallikrein (Webster and Pierce, 1963).- III. Bovine Plasma Prekallikrein (Nagasawa et al., 1968).- C. Pancreatic Kallikreins.- I. Hog Pancreatic Kallikrein (Method 1, Moriya et al., 1965b, 1969).- II. Hog Pancreatic Kallikrein (Method 2, Habermann, 1962).- D. Urinary Kallikreins.- I. Horse Urinary Kallikrein (Prano et al., 1962, 1963).- II. Human Urinary Kallikrein (Moriya et al., 1963).- E. Salivary Kallikreins.- I. Hog Submaxillary Kallikrein (Trautschold, 1965; Roder, 1967).- II. Human Salivary Kallikrein (Moriya et al., 1965a, 1966).- F. Low Molecular Weight Kininogens.- I. Bovine LMW Kininogen (Suzuki et al.).- II. Rabbit LMW Kininogen (Egorova and Paskhina, 1967; Egorova et al., 1969).- III. Human LMW Kininogens I and II (Pierce and Webster, 1966).- G. High Molecular Weight Kininogens.- I. Human HMW Kininogen (Jacobsen and Kriz, 1967).- II. Bovine UMW Kininogen (Yano et al., 1967b).- H. Kinins.- Procedure.- I. Preparation of the Extract.- II. IRC-50 Adsorption.- III. IRC-50 Elution.- IV. Gel Filtration.- V. CM-Cellulose and CM-Sephadex C-25 Chromatography.- VI. P-Cellulose Chromatography.- References.- Assay Methods in the Kinin System.- Kinins.- A. Isolated Smooth Muscle Preparations Used in the Bioassay of Kinins.- I. Guinea Pig Ileum.- II. Rat Uterus.- III. Miscellaneous Preparations.- IV. Superfusion Technique by Vane (1964) and Ferreira and Vane (1967).- B. Vascular Effect of the Kinins and Bioassay.- I. Blood Pressure Recorded from the Carotid Artery.- II. Blood Flow Bioassay Techniques for Vasoactive Substances.- C. Increase of the Capillary Permeability as Bioassay.- D. Radioimmunoassay of Kinins.- E. Assay of Free Kinins in the Blood and Urine.- I. Determination in Blood.- II. Determination in Urine.- Kininogen.- I. Pretreatment of the Plasma Kininogen.- II Kinin Release with Trypsin.- III. Kinin Release with Kallikrein and by Glass Activation.- Kininases.- I. Determination of the Kininase Activity with Kinins as Substrate.- II. Determination of the Kininase Activity with Synthetic Substrates.- III Kininase Units.- Kininogenases.- I. Estimation of Kininogenases by Bioassay.- II. Estimation of the Kininogenases with Synthetic Substrates.- Kininogenase Inhibitors.- References.- 3: Kininogenases.- Plasma Kininogenases and Their Activators.- A. Introduction.- B. Postulated Mechanisms of Intrinsic Plasma Kinin Formation.- I. Early Views on the Origin and Activation of Serum Prekallikrein.- II. The Fibrinolytic System.- III. The Contact System.- IV. The System of Globulin Permeability Factors.- V. The Kininogenase I and Kininogenase II System.- C. Activators.- I. Hageman Factor.- II. Permeability Factor (PF).- III. Plasmin (EC 3.4.4.14).- D. Kininogenases.- I. Plasma Kallikrein (EC 3.4.4.21).- II. Plasmin.- III. Kininogenase II.- IV Kinin-Forming Substance.- E. Differentiation of Kinin-Forming Enzymes and Activators of Plasma.- References.- Kallikreins in Glandular Tissues.- A. Introduction and History.- B. Subcellular Location and Activation of the Glandular Kallikreins.- C. Tissue Concentrations of the Glandular Kallikreins.- D. Purification and Some Properties of the Glandular Kallikreins.- E. The Active Center of the Kallikreins.- F. Species Differences Among the Glandular Kallikreins.- G. Detection and Identification of a Glandular Kallikrein.- References.- Proteolytie Enzymes as Kininogenases.- A. Introduction.- I. Terminology.- II. Kininogenases other than Kallikreins and Snake Venom Enzymes.- B. Chemistry.- I. Trypsin.- II. Pepsin.- III. Clostripain.- IV. Subtilisin BPN’ (Nagarse).- V. Ficin.- VI. Papain.- VII. Streptomyces griseus Protease (Pronase).- VIII. Carboxypeptidase A.- IX. Chymotrypsin.- C Kinin Formation.- I. Demonstration of Kinin-Forming Activity.- II. Nature of Kinin Liberated.- III. Action on the Substrate.- IV. Relative Kinin-Forming Activity.- V. Specificity.- D Kininase Activity.- E. Other Pharmacological Effects.- I. Stimulating Effect on Smooth Muscles.- II. Shock.- III. Pruritus.- References.- Snake Venoms.- A. Bradykinin-Releasing Enzyme in Snake Venom.- B. Purification of Bradykinin-Releasing Enzyme (Kininogenase) from Snake Venom.- C. Dependency of the Kininogenase on the Arginine Esterase in the Venom.- D. The Kinin Liberated by Venom Enzymes and the Properties of Kininogenase in Venoms.- E. Kininases and Bradykinin Potentiators in Snake Venoms.- References.- Kallikrein Inhibitors.- A. Introduction.- B. Kallikrein Blocking Agents.- C Immune Bodies Against Kallikreins.- D. Natural Kallikrein Inhibitors.- I. Units.- II. Methods of Determination.- III. Plant Inhibitors.- IV Inhibitors of Animal and Human Origin.- E. Kallikrein-Destroying Enzymes.- References.- 4: Kininogens.- Kininogens.- A. History and Definition.- B. Estimation.- I. Important Factors.- II. Typical Procedures for Kinin Release.- C. Isolation and Biochemical Properties.- I. Bovine Kininogens.- II. LMW Human Kininogens.- III. Horse Kininogens.- IV. LMW Rabbit Kininogen.- D Kinin Release and Its Relationship to the Structure of Kininogens.- I. Bovine LMW Kininogen.- II. Human Kininogens.- E. Kininogen Level in vivo.- I. General Considerations.- II. Normal Kininogen Values.- III. Variations of Kininogen Level.- References.- 5: Kininases.- Kininases.- A. Blood.- I. Carboxypeptidase N.- II Kininase II.- III. Blood Cells.- B. Other Biological Fluids.- C. Tissues.- D. Purified Proteolytic Enzymes.- I. Use of Carboxypeptidase B in vivo.- II. Fate of Injected Carboxypeptidase B.- E. Snake Venoms.- F. Microorganisms.- G. Fate of Kinins in Circulation.- H Inhibitors of Kininases.- Inhibition in vivo.- J. Activities of Kininases in Various Conditions.- K. Conversion of Kinins.- References.- 6: Kinins.- Section A: Physiological and Pharmacological Actions.- Structure-Activity Relationships of Kinins.- A. Modified Functional Groups.- B. Replacement of One or More Amino Acids.- C. Shortening of the Peptide Chain.- D. C-Terminal Lengthening of the Peptide Chain or Inserting Amino Acids.- E. N-Terminal Shortening and C-Terminal Lengthening of the Peptide Chain.- F. N-Terminal Lengthening of the Peptide Chain (Kallidin Analogues).- G. N-Terminal Lengthening of the Peptide Chain with More than One Amino Acid.- H. Bradykinin Analogs with Prolonged and Differentiated Activities.- J. Bradykinin Analogs with Inhibitory Activity.- K Summary.- References.- Effect of Kallikrein on the Cardiovascular System.- A. In vitro Responses of Isolated Vasculature.- B. Vascular Reactions in the Skin.- C. Vascular Reactions in Skeletal Muscle.- D. Behavior of Coronary Vessels.- E Kallikrein Activity in the Cerebral and Ocular Circulation.- F. Pulmonary Vessels.- G. Changes in the Heart and in the Greater Circulation.- I. Heart Rate.- II. Mean Blood Pressure.- III. Pulse Pressure.- H. Overall Effects.- J. Brief Remarks Concerning Therapeutic Applications.- References.- The Effect of the Kinins on the Cardiovascular System.- A. General Effects on the Cardiovascular System.- Summary.- B Effects on Transvascular Movement of Water.- Summary.- References.- Effects of Bradykinin on the Kidney and Gastrointestinal Organs.- A. Kidney.- B. Gastrointestinal Organs.- References.- The Physiological Role of Glandular Kallikreins.- A. Early Ideas.- B Kinins as Mediators of Functional Vasodilatation in Glands.- I. Cat Submandibular Salivary Gland.- II. Cat Pancreas.- III. Sweat Glands in Human Skin.- C. Criteria for the Theory.- D. Arguments Against the Theory.- I. Arguments Based on Presence or Absence of Kallikreins.- II. Arguments Based on “Perfectionist” View of Humoral Transmitter Theory.- III. Arguments Based on Attempts to Deplete the Substrate or Enzyme.- E. New Evidence for the Theory, in a Gland with a Blood Supply.- F. Other Possible Physiological Roles for Kinins.- References.- Vasodilatation in the Submaxillary Gland of the Cat, Rabbit, and Sheep.- A. Introduction.- B. Experiments on the Cat.- C. Experiments on the Rabbit.- D. Experiments on the Sheep.- E. Discussion.- References.- Kinins and Ventilation of the Lungs.- A. Introduction.- B. Responses of Lungs to Kinins.- I. Tracheobronchial Muscle in vitro.- II. Isolated Lungs.- III. Artificially Ventilated Preparations in vivo.- IV. Action of Antagonism of Kinins in Other Preparations.- V. Spontaneously Breathing Preparations.- VI. The Release of Catecholamines.- C. The Role of Kinins in Airway Function.- D. Summary and Conclusion.- References.- The Effect of Bradykinin and Kallidin on Smooth Muscle.- A. Actions of Kinins on Smooth Muscle in vitro.- B. Action of Kinins on Smooth Muscle in vivo.- C. Mode of Action of Kinins on Smooth Muscle.- D. Antagonists of Kinins on Smooth Muscle.- E. Potentiators of Kinins on Smooth Muscle.- References.- Effect of Bradykinin on the Central Nervous System.- References.- Section B: Pathological Role.- Pain.- A. Introduction.- The Paravascular Sensory Nerve Endings as the Chemoreceptors for Pain.- B. Pain Induced by Kinins. Experimental Methods. Quality of Pain.- I. The Cantharidin Blister Area in Man (CBA).- II. The Pain Experience with Bradykinin Applied to Man by Other Techniques.- III. Other Findings with CBA.- IV. Bradykinin-Induced Pain in Animals.- C. Structure-Action Relationships.- I. Bradykinin Analogs.- 1. Action in Man.- 2. Action in Animals.- II. Bradykinin Compared with Other Peptides.- 1. Action in Man.- 2. Action in Animals.- III. General Discussion.- D. Characteristics of Pain Induced by Bradykinin.- I. Tachyphylaxis.- II. Sensitization of Tissues.- E. Proteolytic Enzymes.- F. Antagonisms.- Acetylsalicylic Acid, Morphine and Other Drugs.- G. Discussion.- References.- Bradykinin and Intracranial Circulation in Man.- A. Introduction.- B Kinin and Kininogen in the Carotid and Internal Jugular Vein.- C. The Action of Bradykinin on Cerebral Circulation.- D. Pharmacodynamics of Intracranial Circulation.- I. Method.- II. Intracranial Vasodilatation by Bradykinin.- III. Intracranial Vasodilatation by Kininogenases (Trypsin, Kallikrein).- E. Action of Bradykinin Given by Spinal Injection.- F. Pathophysiologic Implications.- I. Bradykinin, Cranial Vasodilatation and Febrile Headache.- II. Migraine and Other “Medical” Headache.- III. Subarachnoid Hemorrhage.- IV. Experimental Kinin Release and Clearance in the CSF in vivo.- V. Cerebral Stroke.- References.- Kinins in Inflammation and Tissue Injury.- A. Actions of Kinins.- I. Vasodilatation.- II. Vascular Permeability.- III. Lymph Flow.- IV. Pain.- V. Accumulation of Leukocytes.- B. Evidence for Components of the Kinin-Forming System at the Site of Injury.- C. Local Conditions in Injury which Favor Kinin Actions.- D. Anti-Inflammatory Agents and Kinins.- References.- Immunochemistry of Bradykinin and Immunologic Activation of the Kinin System.- A. Immunochemistry.- I. Preparation of Bradykinin Immunogens.- II. Immunization and Assessment of Specific Antibody Response to Bradykinin.- III. Consideration of Methods of Quantifying Bradykinin by Immunoassay.- IV Immunochemical Determination of the Conformation of Bradykinin.- V. Relationship Between Antibody Combining Site and Biologic Receptor Site.- VI. Immunologic Interrelationships Between Bradykinin and Kininogen.- B Immunologic Activation of the Kinin System.- I. In vivo.- II. In vitro.- References.- Addenda.- Evaluation of the Role of Kinins in Experimental, Pathological, and Clinical Conditions; the Therapeutic Use of Kallikrein Inhibitor.- A. Introduction.- I. Therapeutic Application of Various Proteinase Inhibitors.- II. Arguments for the Therapeutic Use of Trasylol.- B. Pancreatitis.- I. Tissue Necrosis.- II. Local Disturbance of Blood Circulation and Disorder of Cardiovascular System.- III. Imbalance of Blood Coagulation System.- IV. The Therapeutic Effects of Trasylol.- V. The Problem of Trasylol Application in Clinical Pancreatitis.- C. Shock.- Therapy of Shock Based on the Possible Role of Kinins.- D. Carcinoid and Kallikrein-Kirin System.- E. Blood Coagulation and Fibrinolysis.- F. Various Applications.- G. Hereditary Inhibitor Deficiency.- References.- 7: Urinary Kinins.- Urinary Kinins and Colostrokinin.- A. Urinary Kinins.- B. Colostrokinin.- References.- 8: Non-Mammalian Kinins.- Discovery of Non-Mammalian Kinins.- References.- Kinins of Non-Mammalian Origin.- A Kinins in Insect Venoms.- B Kinins in Amphibian Skin.- C. Avian Kinins.- D. Evolution of the Kinin System.- Conclusion.- References.- 9: Summary of Literature Published in Various Languages.- Summary of the Literature Published in Czechoslovakian, Polish, and Russian Journals.- A. Synthesis of Bradykinin.- B Kininogenases, Kininogen.- C. Kinins.- I. Bradykinin Analogs.- II. Effects on Smooth Muscle.- III. Effects on Nervous System.- IV. Cardiovascular Effects; Pain, Inflammation.- D. Carboxypeptidase N.- E. Reviews.- References.- A Summary of Literature Published in French.- A. Identification of Kinins and Their Precursors.- B. Pharmacological Actions of Kinin-Forming Agents and Enzymes.- C. Pharmacological Actions of the Kinins.- I. The Cardiovascular System.- II. Respiration.- III. Vascular Permeability and Local Actions.- IV. Action on the Ileum.- V. Action on Milk Ejection.- D. Catabolism and Antagonists.- E. Physiological Role of the Kininogen-Kinin System.- F. Physiopathological Role.- References.- Summary of Literature Published in Italian.- A. Metabolism.- B. Pharmacology.- C. Pathology.- D. Therapy.- References.- Summary of Literature Published in Japanese.- References.- Summary of Literature Published in Spanish and Portuguese.- A. 1938 to 1954.- I. Discovery, Purification, and Chemical Nature of Bradykinin.- II Kinin-Forming Activity of Fibrinolysin.- III. Bradykinin: Mechanism of Action.- IV. The First Thesis on Bradykinin.- V. First Observations from Other Brazilian Laboratories.- B. 1954 to 1960.- I. Polistes Kinin; Purified Bradykinin.- II. Bradykinin Liberation from Blood Plasma.- III. Oxytoxic Activity of Bradykinin; Effects on Central Nervous System.- IV. Thermic Edema.- V. Kininogenase in Urine.- VI Kinin in Peptone Shock.- VII Kinin Activity in Normal Human Urine.- VIII. Substance V.- IX. Horse Urinary Kallikrein; Substance U; Vasoactive Peptides.- C. 1961 to 1966.- I. Pressor Action of Bradykinin.- II. Kininogen.- III Kinin System.- IV. Neurokinin.- V. Pharmacological Activity of Aqueous Humor.- VI Bilikinin.- VII. Kininogen and Shock.- VIII. Plasma Kininogen in Several Conditions, Including Pregnancy.- IX. Kininogenase in Kidney Subcellular Particles.- X. Oxytoxic Substance in Urine.- XI. Peptone Shock.- XII. Other Kinin Effects.- XIII. Venom Kinins.- XIV. Liberation of Bradykinin by Milk and Polysaccharide Sulfuric Esters.- XV. Horse Urinary Kallikrein.- XVI. Effect of Nagarse on Angiotensin.- XVII. Potentiation of Kinin Effects.- XVIII. Inhibition of Kinin Effects.- D. 1967 and 1968.- I Kinin Effects.- II Kinin Liberation.- III. Thermic Shock.- IV. Oxytoxic Factor in Rat Saliva and Pancreatic Juice.- V. Kininase Activity in Brain.- VI Kallikreins.- VII Kinin System in Bothrops Plasma.- VIII. Kininogen Formation.- References.- Author Index.