Review Article

Scorpion Peptides: Potential Use for New Drug Development

Table 4

Summary of the modus operandi of some scorpion derivatives with potential therapeutic use.

PeptidesOriginBiological effects

Immune diseases
 Charybdotoxin [84, 85]L. quinquestriatus Blockade of shaker potassium channels (Kv1.3.) which suppresses lymphocytes proliferation and IL2 production.
 Parabutoporin [26, 45, 95, 96]P. schlechteri Activation of the Rac receptor coupled to G protein, and inhibiting NADPH/oxidase complex function. The cumulus of these actions enhances exocytosis and chemotaxis and prevents superoxide production.
 Fraction 1 [88]A. australis Stimulating lymphocytes proliferation.
 Total venom [82, 86]
γTsTx (gamma toxin) [89]
T. serrulatus Lymphocytes proliferation enhancement.
Lymphocytes mobilization from the bone marrow.
Pro- and anti-inflammatory factor release (exocytosis).
Platelet-activating factor receptor (PAFR), chemotaxis, and complement stimulation.

Cardiovascular diseases
γTsTx (gamma toxin)[89]T. serrulatus PAFR stimulation (aggregating factor)
 Charybdotoxin [84]L.  quinquestriatus Blockade of voltage and Ca2+-activated potassium channels, decreasing prothrombinase activity and phosphatidylserine exposition (aggregating factor).
 SVAP [74, 77]B. m. Kirsch Increasing PGI2 production/altering pro- and anti inflammatory compounds release, probably from white blood cells.
 Bpps (Bppk12) [10]B. occitanus Inhibiting the downregulation of the bradykinin (vasodilatator) and the angiotensin II (vasoconstrictor) synthesis.
 Hypotensins [87]T.  serrulatus Inhibiting the downregulation of the bradykinin and enhancing NO release.

Neurological diseases
 Various [102]Various Interaction with adrenergic and cholinergic receptors.
 K+ channels blockers [103]Various Blockade of potassium current which prevents symptoms and signs in multiple sclerosis.
 Whole venom [104]
 Bmk AS [105, 106]
B. m. Kirsch Inhibition of the voltage-sensitive sodium channels.

Cancer
 Chlorotoxin [107110]
 rBmKTa (recombinant) [111]
L. q. hebraeus  
B. m. Kirsch
Carrying gene transfecting-nanovecteors to their targeted cancer cells.
blockade of chloride channels responsible for cell motility and metastasis invasion.
 AmmTx3 [112]
 BmTx3[112]
 BeKm-1[112]
A.m. mauritanicus  
Meso. martensi  
Meso. eupus
Blockade of hERGK+ channels involved in tumoral cells activities.
 BmHYA1 [30]B. martensi Modulation of cell cycle, apoptosis and invasion.
Facilitation of drugs biodistribution by acting on MPPs.
Modulation of CD44 surface marker of breast cancer cells.
 PESV [113]Nd Enhances the immune sentinel against tumors.

Osteoporosis
 Whole venom [114] H. bengalensis  Stimulation of osteoclast activity and mineral deposits and modulation the release of osteoporosis regulating factors (antiosteoporosis).
 KTXs [115]Various Blockade of Kv1.3 channels which reduce inflammatory bone resorption.