Melittin

UniProtKB accession:  P01501

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UniProtKB description:  Melittin: Main toxin of bee venom with strong antimicrobial activity and hemolytic activity (PubMed:5794226, PubMed:5139482, PubMed:4057243, PubMed:24512991). It has enhancing effects on bee venom phospholipase A2 activity (PubMed:4371280). This amphipathic toxin binds to negatively charged membrane surface and forms pore by inserting into lipid bilayers inducing the leakage of ions and molecules and the enhancement of permeability that ultimately leads to cell lysis (PubMed:6830776, PubMed:4057243, PubMed:3666135). It acts as a voltage-gated pore with higher selectivity for anions over cations (PubMed:6269667). The ion conductance has been shown to be voltage-dependent (PubMed:7061434). Self-association of melittin in membranes is promoted by high ionic strength, but not by the presence of negatively charged lipids (PubMed:3443079). In vivo, intradermal injection into healthy human volunteers produce sharp pain sensation and an inflammatory response (PubMed:26983715). It produces pain by activating primary nociceptor cells directly and indirectly due to its ability to activate plasma membrane phospholipase A2 and its pore-forming activity (PubMed:26983715). In the context of inflammation and cancer tests, is highly cytotoxic to normal cells, highly induces calcium signaling and almost completely prevents cAMP production (PubMed:36548715). In addition, prevents LPS-induced nitric oxid (NO) synthesis but does not affect the IP3 signaling and pro-inflammatory activation of endothelial cells (PubMed:36548715). Also shows significant antiproliferative activity on the breast cancer cell line MDA-MB-231 (PubMed:36548715).