Metal Toxicity Cellular Injuries • Diverse – Many mechanisms – Different biol levels • Changes in activities – Mostly direct – Key bio molecules – Biochem pathways.

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Transcript Metal Toxicity Cellular Injuries • Diverse – Many mechanisms – Different biol levels • Changes in activities – Mostly direct – Key bio molecules – Biochem pathways.

Metal Toxicity
Cellular Injuries
• Diverse
– Many mechanisms
– Different biol levels
• Changes in activities
– Mostly direct
– Key bio molecules
– Biochem pathways
Metals of Concern
• Lead (Pb)
• Mercury (Hg)
• Cadmium (Cd)
• Arsenic (As)
• Chromium (Cr)
• Zinc (Zn)
• Copper (Cu)
• Book notes last 3
essential nutrients for
animals, humans
• Water soluble
• Readily absorbed
• Bind proteins,
enzymes, nucleic acids
in cells
Metals Chemistry
• Most are electron acceptors
• Preferential reaction w/ -SH grps
– Also –COOH, -PO4-2
Metals Chemistry
• Most interactions w/ proteins, enzymes
– BUT in vitro data
– Not all competitive mol’s present
– Also metal mol’s may compete for binding
sites
• May displace essential metal cofactors
Lead (Pb)
• Routes of ingestion
– Lung
• Industry
• Wind (soil, vegetation)
• Gasoline engines
– Oral
• Food (vegetation (soils), pottery glaze, paint)
• Water (incl lead shot)
Pb Toxicity to Plants, Animals
• From air, soil, lead shot
• Dependent on species
– Ex: barley sensitive
– Ex: goldfish insensitive
• May inhibit seed germination
• Paralyzes bird gizzard  starvation, death
• Impt: ingestion by animals further up food chain
Toxicity to Humans
• Adult intake threshold ~ 500 mg/d
– Children half
• 5-15% ingested dose abs’d (15-25 mg/d)
• 20-40% inhaled dose abs’d (~8 mg/d)
• Unleaded gasoline decr’d intake
Lead Poisoning in Humans
• Nausea, anorexia
• Anemia
• Renal tubular
dysfunction
• Crosses placenta
– Miscarriage
• Crosses bbb
– Behavioral dysfunction
• Joint pain
– Convulsions
• Deposits in bone
– Delirium
– Equilib bone 
blood
– Encephalopathy
Pb Toxicity within Cells
• Not fully known
• Highly reactive to –SH grps
–  Mercaptide
• R—S—Pb—S—R
– Can inactivate enz’s, other prot’s
• Book ex: adenyl cylase (brain transmission)
• Book ex: aminotransferase (aa metab)
• Similar to Ca, competes
– At presyn receptor
• Now decr’d Ca avail
– Bone
• Interacts w/ nucleic acids
– Decr’s protein synth
• Decr’d binding tRNA to ribosomes
– OR may incr prot synth
Nucleus
• As, Pb, Hg, Se
• Produce
intranuclear
inclusion bodies
• BUT mechanisms
varied/complex
Nucleus
• Ex: Pb best studied
– Renal tubule DNA, RNA, prot syntheses stim’d
– So biochem changes in nuclear structure,
function
– Karyomegaly
– Can  renal adenocarcinoma w/ high dose
• Ex: Methyl-Hg, Cd inhibit nucleic acid
synth w/ acute exposure
• Interacts w/ Zn, Fe  inhib’n d-
aminolevulinic acid dehydratase and
ferrochelatase
–  Decr’d heme synth
–  Decr’d rbc’s
– Book p. 224
Cadmium (Cd)
• Routes of exposure
– Lung
• Highest concent’s – industrialized cities, near
smelters
• Tobacco smoke (more impt)
– 1.5-2.0 mg/cigarette; 70% found in smoke
• Routes of exposure – cont’d
– Oral
• Water
– From industrial, mining wastes
• Soils
– From sewage sludge appl’d to agri fields; phosphate
fertilizers
• Food – largest exposure source
– Accum’d from plants (soil), fish (water)
Cd Toxicity to Plants
• Accum’d by all plants
– Soil pH, species impt
– Stunts growth, photosynth; inhibits seed
germination
Cd Toxicity to Humans
• Toxicity @ 250-300 mg/day
• Pulmonary exposure not as impt to burden
– Except tobacco smoke
– BUT more dangerous route (direct)
• Greater percentage dose abs’d (25-40%)
• Drinking water not as impt to burden
– 20-30 mg/day
• Food most impt
– 35-90 mg/day
– Based on 5-10% abs’n
– Low prot in diet  incr’d abs’n, incr’d toxicity
• Binds albumin in blood, taken up by liver
– Binds metallothionein, then  blood 
kidney, bone, muscle
• Embryotoxic
High Affinity Metal Binding
Proteins
• In cytosol
• Intracellular “sinks”
– Hold toxic metals away from
• Sensitive organelles
• Metabolic sites
– Overwhelmed w/ very high metal exposure
High Affinity Metal Binding
Proteins
• Metallotheionine most impt
– Low MW
– Mammalian, nonmammamlian
– Cd, Zn, Hg, Ag, Cu, bismuth
• Also impt to regulating availability of
metals in cell
– Nuclear inclusion bodies
– Lysosomes
Example: Cd in Mammals
• Ingestion through lungs, g.i. 
• Blood, binds high MW proteins,
transported 
• Liver
– Cd induces synth MT
• Impt to availability of Cd in cell
– If high Cd dose, released back to blood as CdMT
• Kidney
– Cd-MT taken up by prox tubule cells
– Damage if lysosomes cleave complex  free Cd
• Hepatic cyt P450
– Acute Cd  decr’d cyt P450 content, activities
– Chronic Cd not same
• MT has time to be induced
• Can bind Cd
• MT can sequester from sensitive cell structures
– Other physio factors probably involved
But…
• Other metal binding proteins
• Some metals don’t induce synth of metal
binding prot’s
Lysosomes
• Renal tubules
• Cd+2, Hg (as Hg+2 or
methyl-Hg)
– Inhibit normal function
–  cell injury
• Indirect effect due to
dysfunction of other
damaged organelles
Cd Toxicity within Cells
• Energy prod’n
– Chloroplast photophosph’n
– Mitochondria ATP synth, NADH ox’n, electron
transport
• Enzyme inhib’n
– Book ex: alkaline phosphatase, myosin
ATPases
– Binds –SH grps
– Competes w/, displaces Zn
• Binds –SH grps in other impt cell prot’s
– Cell membr
– Mitochondria
• Uncouples oxidative phosph’n
• Antimetabolite
– Competes w/ other metals (Zn, Cu, Se, Fe)
Mitochondria
• Major intracell target
of many metals
– Rapid transport metals
across mitoch membr’s
– Has high metab
activity
– Sensitive to disruption
Mitochondria
• Membranes
– Highly sensitive to metals toxicity
– Alterations in marker enz activities found
– Ex: As, Pb, methyl-Hg
• Affect respiration
– Direct effect on enzymes
• Binding to cofactors
– Indirect effect on enzymes
• Perturbation of membr’s (site of activity)
Cd Poisoning in Humans
• Emphysema
• Liver dysfunction
• Pneuomonitis
• Kidney damage
• GI disturbances
–  Anemia
• Vomiting
–  Proteinuria
• Hypertension
Mercury (Hg)
• Routes of exposure
– Lung
• Little in atmosphere harmful to health
• BUT vapor diffuses through alveolar membr 
brain quickly, directly
– Oral
• Little in drinking water harmful to health
• Food – largest exposure source
• FDA guideline: accum’n <0.5 mg/day
Hg Toxicity to Plants, Animals
• In plants toxicity dependent on species
– Impairs germination, growth
• Fish may accum Hg > FDA guideline
– In tissue, as methylmercury (CH3Hg)
– Ingested via water through gills + food chain
• May be as CH3Hg or Hg
– Age, rate of exposure less impt than metabolic rate of
indiv fish
• Incr’d T  incr’d metab  greater Hg in tissue in summer
• Toxicity to fish incr’d w/ incr’d T
Hg Toxicity to Humans
• Critical intake 300 mg Hg as CH3Hg
• Almost all CH3Hg in diet from fish, meat
– Book: Japanese Hg, CH3Hg discharges  11
mg Hg/g fish
• Fetal, newborn brains very sensitive to
toxicity
• Tissue susceptibility related to form’n Hg+2
ion
Hg Poisoning
• Chronic
– Salivation, loss
appetite
– Anemia
– Tissue irritation,
gingivitis
• Mercuric chloride
– Precipitates all prot’s
– Vomiting
– Severe thirst
– Nausea
– Nutrional disturbances
– Severe GI irritation
– Renal damage
– Loss fluids, electrolytes
– Neurotoxicity
Hg Toxicity within Cells
• Inhib’n enzymes
– Selective affinity to –SH grps
– R—SH + CH3Hg  R—S—Hg—CH3 + H+
• Incr’s permeability Na+, K+
– Inhibits active transport mech’s
– Disrupts fluid/electrolyte balance
• Affects chromosomes, mitosis 
mutagenesis
Protection against Hg Toxicity
• Metallothionein
– Kidney damage when metallothionein
saturated
• Se
– Mech unknown, but Se binds cysteine more
tightly than Hg
• Vitamin E
– Mech unknown
Cellular Injuries
• Dependent on individual physiological
factors
– Developmental stage
– Sex
– Nutritional status
– Toxicant dose
– Toxicant combination
Organelles/Structures Effected by
Various Metals
• Nucleus
• Lysosomes
• Mitochondrion
• Cell membrane
• Endoplasmic Reticulum
Cell Membrane
• Movement into cell dependent on
– Lipophilicity
– Metal binding to protein  endocytosis
– Chem similarity of metal to nutrient
– Ex: As
• Metals may enter
membr by
– Passive diffusion
– Binding cell membr,
then endocytosis
• Ex: Pb
• Hg+2, Cr+6(chromate) strong oxidizers
– Acute high dose effects membranes
– Not seen w/ chronic low dose
• Some membr’s adapt to chronic dosage
– Exceptions to metals trend
• Most don’t directly damage cell membrane
• Most are intracellular toxicants
Endoplasmic Reticulum
• Co, Cd, Sn, CH3Hg, In
• Metabolic enz’s inhib’d
– Cyt P450 and non-cyt
P450
• Ex: In disrupts e.r.
structure
– Alters microsomal enz
activities