Nattokinase

The pharmacological effects and mechanisms of action of nattokinase mainly include the following five aspects: fibrinolytic/antithrombotic effect, anti-atherosclerotic/lipid-lowering effect, antihypertensive effect, antiplatelet/anticoagulant effect, and neuroprotective effect. The fibrinolytic/antithrombotic effect is due to the excellent fibrinolytic effect of nattokinase, which can degrade fibrin and release tissue plasminogen activator (t-PA) to exert a promoting effect on the formation of plasmin. The blood pressure-lowering effect of nattokinase can be achieved by inhibiting angiotensin-converting enzyme (ACE) activity to produce its antihypertensive effect. In addition, nattokinase can degrade amyloid fibrils under neutral pH and normal body temperature, which suggests that nattokinase may be used as a potential therapeutic agent for amyloid-related diseases such as Alzheimer's disease (AD).

Fig. 1 Microparticle digestion and nattokinase adsorption in the intestine. (Zhang X.; et al. 2020)

The oral administration of nattokinase would make it easy for clinical treatment, but the efficacy is largely not achieved, and the thrombolytic activity of nattokinase may be inactivated in the gastric acid. Zhang et al. developed a functional oral delivery system for nattokinase. The chitosan microparticle served as the delivery carrier and was prepared to load nattokinase by genipin cross-linking, followed by coating a protective casein shell with transglutaminase (TG) crosslinking. in vitro and in vivo experiments show that the core-shell carrier with two-layer coating could protect the loaded nattokinase from being degraded in the gastric fluid and then release the loaded protein in a controlled manner in the intestinal tract, thus maintaining the bioactivity and prolonging the therapeutic efficacy of nattokinase.

Fig. 2 Pharmacologic actions of nattokinase as related to cardiovascular health and disease. (Chen H.; et al. 2018)