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    Types of Reactions of Biotransformations of Xenobiotics in A Liver?

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    jimmy
    The document discusses biotransformation of xenobiotics and endogenous toxins in the liver. It covers 3 key points: 1. It describes the two phases of biotransformation - phase I involving oxidation, reduction, and hydrolysis reactions mediated by cytochrome P450. Phase II involves conjugation reactions like acetylation and methylation that make the compounds more hydrophilic and easier to excrete. 2. It explains the role of microsomal oxidation in phase I, mediated by cytochrome P450 enzymes in the smooth endoplasmic reticulum. It also lists inducers and non-inducers of these monooxygenase enzymes. 3. The role

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    Types of Reactions of Biotransformations of Xenobiotics in A Liver?

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    jimmy
    83 views3 pages
    The document discusses biotransformation of xenobiotics and endogenous toxins in the liver. It covers 3 key points: 1. It describes the two phases of biotransformation - phase I involving oxidation, reduction, and hydrolysis reactions mediated by cytochrome P450. Phase II involves conjugation reactions like acetylation and methylation that make the compounds more hydrophilic and easier to excrete. 2. It explains the role of microsomal oxidation in phase I, mediated by cytochrome P450 enzymes in the smooth endoplasmic reticulum. It also lists inducers and non-inducers of these monooxygenase enzymes. 3. The role

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    The document discusses biotransformation of xenobiotics and endogenous toxins in the liver. It covers 3 key points: 1. It describes the two phases of biotransformation - phase I involving oxidation, reduction, and hydrolysis reactions mediated by cytochrome P450. Phase II involves conjugation reactions like acetylation and methylation that make the compounds more hydrophilic and easier to excrete. 2. It explains the role of microsomal oxidation in phase I, mediated by cytochrome P450 enzymes in the smooth endoplasmic reticulum. It also lists inducers and non-inducers of these monooxygenase enzymes. 3. The role

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    83 views3 pages

    Types of Reactions of Biotransformations of Xenobiotics in A Liver?

    Uploaded by

    jimmy
    The document discusses biotransformation of xenobiotics and endogenous toxins in the liver. It covers 3 key points: 1. It describes the two phases of biotransformation - phase I involving oxidation, reduction, and hydrolysis reactions mediated by cytochrome P450. Phase II involves conjugation reactions like acetylation and methylation that make the compounds more hydrophilic and easier to excrete. 2. It explains the role of microsomal oxidation in phase I, mediated by cytochrome P450 enzymes in the smooth endoplasmic reticulum. It also lists inducers and non-inducers of these monooxygenase enzymes. 3. The role

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    Biochemistry

    Biotransformation of xenobiotics and endogenous toxins in the liver: microsomaloxidation,


    cytochromeР-450.

    Xenobiotic is a chemical substance found within an organism that is not naturally produced or expected
    to be present within the organism. It can also cover substances that are present in much higher
    concentrations than are usual

    1. Types of reactions of biotransformations of xenobiotics in a liver?

    Phases of biotransformation

    Enzyme Phase I Phase II Phase II


    Types of Hydrolysis Conjugation – Conjugated
    reaction Oxidation by cytochrome P40 attachment of an metabolites are
    Reduction ionized group to the excreted through
    drug e.g. Acetyl, Methyl, urine or feces via
    Glutathione. bile
    Increase in small Large
    hydrophilicity
    General Exposes functional group Polar compound added
    mechanism to functional group
    Consequence May result in metabolic activation. Drug inactivated
    Note the drug still active Facilitates excretion
    Example Oxidized to salicylic acid Its conjugated with Excreted in the
    Aspirin glycine or glucuronic urine
    acid forming a range of
    ionized metabolites

    2. Reactions of microsomal oxidation; inductors and aninductors of microsomal monooxygenases?

    The microsomal ethanol oxidizing system (MEOS) is an alternate pathway of ethanol metabolism that
    occurs in the smooth endoplasmic reticulum in the oxidation of ethanol to acetaldehyde.

    The MEOS pathway converts ethanol to acetaldehyde by way of a redox reaction. In this reaction,
    ethanol is oxidized (losing two hydrogens) and O2 is reduced (by accepting hydrogen) to form H2O.
    NADPH is used as donor of hydrogen, forming NADP+. This process consumes ATP and dissipates heat

    Microsomal Enzymes Non-Microsomal Enzymes


    Smooth endoplasmic reticulum of cells of liver, Cytoplasm, mitochondria of hepatic and other
    kidney, lungs and skin tissue
    Nonspecific Inducible Non Inducible
    PHASE 1: most oxidation and reduction, some PHASE 1: most hydrolysis and some oxidation &
    hydrolysis reduction
    PHASE 2: only glucuronide conjugation PHASE 2: all except glucuronide conjugation
    Cytochrome P450 Mono amine oxidase, alcohol dehydrogenase

    3. Reactions of conjugation in the hepatocytes: biochemical mechanisms, functions.

    4. The role of cytochrome Р-450 in biotransformation of xenobiotics?

    Cytochrome P450 is a family of enzymes involved in

    1. Drug metabolism
    2. Bio activation
    3. Breakdown of xenobiotics – hence turns drugs into soluble molecules so that it can be secreted
    out properly

    Active site of Cytochrome P450 has a heme center i.e. iron with a porphyrin ring surrounding it where
    the iron is bound to the 4 nitrogen atoms and the thiol of the cysteine residue

    5. Clinical significance of liver functions’ evaluating (indican’s and hypuric acid qualitative reactions)?

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