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Hirudin is a
naturally occurring peptide in the salivary
glands of medicinal leeches (Hirudo medicinalis)
that has a blood anticoagulant property. This is
fundamental for the leeches’ alimentary habit of
hematophagy, since it keeps the blood flowing
after the initial phlebotomy performed by the
worm on the host’s skin.A key event in the final
stages of blood coagulation is the convertion of
fibrinogen into fibrin by the serine protease
enzyme thrombin.[4] Thrombin is produced from
prothrombin, by the action of an enzyme,
prothrombinase, in the final states of
coagulation. Fibrin is then cross linked by
factor XIII to form a blood clot. The principal
inhibitor of thrombin in normal blood
circulation is antithrombin III.[3] Similar to
antithrombin III, the anticoagulatant activity
of hirudin is based on its ability to inhibit
the pro-coagulant activity of thrombin.Hirudin
is the most potent natural inhibitor of
thrombin. Unlike antithrombin III hirudin binds
to and inhibits only the activity of thrombin
forms with a specific activity against
fibrinogen.[3] Therefore, hirudin prevents or
dissolves the formation of clots and thrombi
(i.e. it has a thrombolytic activity), and has
therapeutic value in blood coagulation
disorders, in the treatment of skin hematomas
and of superficial varicose veins, either as an
injectable or a topical application cream. In
some aspects, hirudin has advantages over more
commonly used anticoagulants and thrombolytics,
such as heparin, as it does not interfere with
the biological activity of other serum proteins
and can also act on complexed thrombin. |