Apitoxin
Encyclopedia
Apitoxin, or honey bee
Honey bee
Honey bees are a subset of bees in the genus Apis, primarily distinguished by the production and storage of honey and the construction of perennial, colonial nests out of wax. Honey bees are the only extant members of the tribe Apini, all in the genus Apis...

 venom
Venom
Venom is the general term referring to any variety of toxins used by certain types of animals that inject it into their victims by the means of a bite or a sting...

, is a bitter colorless liquid. The active portion of the venom is a complex mixture of protein
Protein
Proteins are biochemical compounds consisting of one or more polypeptides typically folded into a globular or fibrous form, facilitating a biological function. A polypeptide is a single linear polymer chain of amino acids bonded together by peptide bonds between the carboxyl and amino groups of...

s, which causes local inflammation and acts as an anticoagulant
Anticoagulant
An anticoagulant is a substance that prevents coagulation of blood. A group of pharmaceuticals called anticoagulants can be used in vivo as a medication for thrombotic disorders. Some anticoagulants are used in medical equipment, such as test tubes, blood transfusion bags, and renal dialysis...

. The venom is produced in the abdomen of worker bee
Worker bee
A Worker bee is any female eusocial bee that lacks the full reproductive capacity of the colony's queen bee; under most circumstances, this is correlated to an increase in certain non-reproductive activities relative to a queen, as well...

s from a mixture of acidic and basic secretions. Apitoxin is acidic (pH
PH
In chemistry, pH is a measure of the acidity or basicity of an aqueous solution. Pure water is said to be neutral, with a pH close to 7.0 at . Solutions with a pH less than 7 are said to be acidic and solutions with a pH greater than 7 are basic or alkaline...

 4.5 to 5.5). A honeybee can inject 0.1 mg of venom via its stinger. Apitoxin is similar to nettle
Nettle
Nettles constitute between 24 and 39 species of flowering plants of the genus Urtica in the family Urticaceae, with a cosmopolitan though mainly temperate distribution. They are mostly herbaceous perennial plants, but some are annual and a few are shrubby...

 toxin
Toxin
A toxin is a poisonous substance produced within living cells or organisms; man-made substances created by artificial processes are thus excluded...

. It is estimated that 1% of the population is allergic to bee stings. Apitoxin can be deactivated with ethanol
Ethanol
Ethanol, also called ethyl alcohol, pure alcohol, grain alcohol, or drinking alcohol, is a volatile, flammable, colorless liquid. It is a psychoactive drug and one of the oldest recreational drugs. Best known as the type of alcohol found in alcoholic beverages, it is also used in thermometers, as a...

.

Bee venom therapy is used by some as a treatment for rheumatism
Rheumatism
Rheumatism or rheumatic disorder is a non-specific term for medical problems affecting the joints and connective tissue. The study of, and therapeutic interventions in, such disorders is called rheumatology.-Terminology:...

 and joint diseases due to its anticoagulant
Anticoagulant
An anticoagulant is a substance that prevents coagulation of blood. A group of pharmaceuticals called anticoagulants can be used in vivo as a medication for thrombotic disorders. Some anticoagulants are used in medical equipment, such as test tubes, blood transfusion bags, and renal dialysis...

 and anti-inflammatory
Anti-inflammatory
Anti-inflammatory refers to the property of a substance or treatment that reduces inflammation. Anti-inflammatory drugs make up about half of analgesics, remedying pain by reducing inflammation as opposed to opioids, which affect the central nervous system....

 properties. It is also used to desensitize people allergic to insect stings. Bee venom therapy can also be delivered in the form of Bee Venom Balm although this may be less potent than using live bee stings.

Components of Apitoxin

The main component is melittin
Melittin
Melittin is the principal active component of apitoxin and is a powerful stimulator of phospholipase A2. Melittin is a peptide consisting of 26 amino acids with the sequence GIGAVLKVLTTGLPALISWIKRKRQQ.-Biological effects:...

 comprising 52% of venom peptides. Melittin is a strong anti-inflammatory agent and induces the production of cortisol
Cortisol
Cortisol is a steroid hormone, more specifically a glucocorticoid, produced by the adrenal gland. It is released in response to stress and a low level of blood glucocorticoids. Its primary functions are to increase blood sugar through gluconeogenesis; suppress the immune system; and aid in fat,...

 in the body.
  • Apamin
    Apamin
    Apamin is an 18 amino acid peptide neurotoxin found in apitoxin . It selectively blocks SK channels, a type of Ca2+-activated K+ channel expressed in the central nervous system and smooth muscle...

     increases cortisol production in the adrenal gland
    Adrenal gland
    In mammals, the adrenal glands are endocrine glands that sit atop the kidneys; in humans, the right suprarenal gland is triangular shaped, while the left suprarenal gland is semilunar shaped...

    . Apamin is a mild neurotoxin
    Neurotoxin
    A neurotoxin is a toxin that acts specifically on nerve cells , usually by interacting with membrane proteins such as ion channels. Some sources are more general, and define the effect of neurotoxins as occurring at nerve tissue...

    .

  • Adolapin, comprising 2-5% of the peptides, acts as an anti-inflammatory and analgesic
    Analgesic
    An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....

     because it blocks cyclooxygenase
    Cyclooxygenase
    Cyclooxygenase is an enzyme that is responsible for formation of important biological mediators called prostanoids, including prostaglandins, prostacyclin and thromboxane. Pharmacological inhibition of COX can provide relief from the symptoms of inflammation and pain...

    .

  • Phospholipase
    Phospholipase
    A phospholipase is an enzyme that hydrolyzes phospholipids into fatty acids and other lipophilic substances. There are four major classes, termed A, B, C and D, distinguished by the type of reaction which they catalyze:*Phospholipase A...

     A2 comprises 10-12% of peptides and it is the most destructive component of apitoxin. It is an enzyme
    Enzyme
    Enzymes are proteins that catalyze chemical reactions. In enzymatic reactions, the molecules at the beginning of the process, called substrates, are converted into different molecules, called products. Almost all chemical reactions in a biological cell need enzymes in order to occur at rates...

     which degrades the phospholipid
    Phospholipid
    Phospholipids are a class of lipids that are a major component of all cell membranes as they can form lipid bilayers. Most phospholipids contain a diglyceride, a phosphate group, and a simple organic molecule such as choline; one exception to this rule is sphingomyelin, which is derived from...

    s which cellular membranes are made of. It also causes decreased blood pressure
    Blood pressure
    Blood pressure is the pressure exerted by circulating blood upon the walls of blood vessels, and is one of the principal vital signs. When used without further specification, "blood pressure" usually refers to the arterial pressure of the systemic circulation. During each heartbeat, BP varies...

     and inhibits blood coagulation. Phospholipase A2 activates arachidonic acid
    Arachidonic acid
    Arachidonic acid is a polyunsaturated omega-6 fatty acid 20:4.It is the counterpart to the saturated arachidic acid found in peanut oil, Arachidonic acid (AA, sometimes ARA) is a polyunsaturated omega-6 fatty acid 20:4(ω-6).It is the counterpart to the saturated arachidic acid found in peanut oil,...

     which is metabolized in the cyclooxygenase
    Cyclooxygenase
    Cyclooxygenase is an enzyme that is responsible for formation of important biological mediators called prostanoids, including prostaglandins, prostacyclin and thromboxane. Pharmacological inhibition of COX can provide relief from the symptoms of inflammation and pain...

    -cycle to form prostaglandin
    Prostaglandin
    A prostaglandin is any member of a group of lipid compounds that are derived enzymatically from fatty acids and have important functions in the animal body. Every prostaglandin contains 20 carbon atoms, including a 5-carbon ring....

    s. Prostaglandins regulate the body's inflammatory response. The toxin from wasp
    Wasp
    The term wasp is typically defined as any insect of the order Hymenoptera and suborder Apocrita that is neither a bee nor an ant. Almost every pest insect species has at least one wasp species that preys upon it or parasitizes it, making wasps critically important in natural control of their...

    s contains phospholipase A1.

  • Hyaluronidase
    Hyaluronidase
    The hyaluronidases are a family of enzymes that degrade hyaluronic acid.In humans, there are six associated genes, including HYAL1, HYAL2, HYAL3, and PH-20/SPAM1.-Use as a drug:...

     comprising 1-3% of peptides dilates the capillaries
    Capillary
    Capillaries are the smallest of a body's blood vessels and are parts of the microcirculation. They are only 1 cell thick. These microvessels, measuring 5-10 μm in diameter, connect arterioles and venules, and enable the exchange of water, oxygen, carbon dioxide, and many other nutrient and waste...

     causing the spread of inflammation.

  • Histamine
    Histamine
    Histamine is an organic nitrogen compound involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter. Histamine triggers the inflammatory response. As part of an immune response to foreign pathogens, histamine is produced by...

     comprising 0.5-2% and is involved in the allergic response.

  • Dopamine
    Dopamine
    Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...

     and noradrenaline which comprise 1-2% increase pulse rate.

  • Protease-inhibitors
    Protease
    A protease is any enzyme that conducts proteolysis, that is, begins protein catabolism by hydrolysis of the peptide bonds that link amino acids together in the polypeptide chain forming the protein....

    comprise 2% and act as anti-inflammatory agents and stop bleeding.
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