In Silico and In Vitro Study of the Bromelain-Phytochemical Complex Inhibition of Phospholipase A2 (Pla2)

Abstract

Phospholipase A2 (Pla2) is an enzyme that induces inflammation, making Pla2 activity an effective approach to reduce inflammation. Therefore, investigating natural compounds for this Pla2 inhibitory activity has important therapeutic potential. The objective of this study was to investigate the potential in bromelain-phytochemical complex inhibitors via a combination of in silico and in vitro methods. Bromelain-amenthoflavone displays antagonistic effects on Pla2. Bromelian-asiaticoside and bromelain-diosgenin displayed synergistic effects at high concentrations of the combined compounds, with inhibition percentages of more than 70% and 90%, respectively, and antagonistic effects at low concentrations. The synergistic effect of the bromelain-asiaticoside and bromelain-diosgenin combinations represents a new application in treating inflammation. These findings not only provide significant quantitative data, but also provide an insight on valuable implications for the combined use of bromelain with asiaticoside and diosgenin in treating inflammation, and may help researchers develop more natural bioactive compounds in daily foods as anti-inflammatory agent.

Role of enzyme-flavonoid therapy in controlling inflammatory pathology of pelvic inflammatory disease

“…26,31 The potent inhibitory action of bromelain on Phospholipase A2, a key enzyme in the induction of arachidonic acid pathway leading to the formation of inflammation mediators, may be responsible for this. 32 In a placebo-controlled crossover randomized clinical trial, bromelain led to a significant shift in the circadian profiles of the Th1 cell mediator IFN-γ and trends in those of the Th2-type cytokine IL-5 and immunosuppressive cytokine interleukin (IL)-10, thus suggesting a general effect on the antigen-specific (T cell) compartment of the human immune system. 33 Bromelain has been shown to proteolytically block the activation of extracellular regulated kinase-2 (ERK-2) in T Cells, thereby inhibiting cytokine production and T cell signaling.…”