Bee Venom: An Updating Review of Its Bioactive Molecules and Its Health Applications

Abstract

Bee venom (BV) is usually associated with pain since, when humans are stung by bees, local inflammation and even an allergic reaction can be produced. BV has been traditionally used in ancient medicine and in acupuncture. It consists of a mixture of substances, principally of proteins and peptides, including enzymes as well as other types of molecules in a very low concentration. Melittin and phospholipase A2 (PLA2) are the most abundant and studied compounds of BV. Literature of the main biological activities exerted by BV shows that most studies focuses on the comprehension and test of anti-inflammatory effects and its mechanisms of action. Other properties such as antioxidant, antimicrobial, neuroprotective or antitumor effects have also been assessed, both in vitro and in vivo. Moreover, human trials are necessary to confirm those clinical applications. However, notwithstanding the therapeutic potential of BV, there are certain problems regarding its safety and the possible appearance of adverse effects. On this perspective, new approaches have been developed to avoid these complications. This manuscript is aimed at reviewing the actual knowledge on BV components and its associated biological activities as well as the latest advances on this subject.

Keywords: bee venom; biological properties; enzymes; health applications; peptides.

Figure 1

Scheme and process flow of typical bee venom collection by means of using an electroshock trap. Bees are submitted to an electric current, and consequently they eject the venom, which is collected on a glass plate and then transferred to bottles for further processing.

Figure 2

Action mechanism of anti-inflammatory effects of melittin. Melittin inhibits the routes of TLR2, TLR4, CD4, NEMO and PDGFRβ and therefore, inhibits the action of pro-inflammatory genes. This process results in lower levels of pro-inflammatory molecules and the reduction of inflammation. Abbreviations: TLR2, Toll-Like Receptors 2; CD4, Cluster of Differentiation 4; NEMO, nuclear factor kappa-β essential modulator; PDGFRβ, platelet-derived growth factor receptor β;

Figure 3

Different effects of Mast Cell-Degranulating (MCD) peptide when it is present in low or high concentration. In a low concentration, MCD induces mast cell degranulation and the release of histamine, resulting in inflammation processes. In a high concentration, MCD inhibits mast cell degranulation and therefore, exerts anti-inflammatory effects.

Figure 4

Double behavior of PLA2. This enzyme has the ability of acting as enzyme or as a ligand. As an enzyme, it causes membrane disruption and can exert antimicrobial and cytotoxic effects. As a ligand, it produces cellular signals and modulate immune response.