Bergamot derivative compounds affect on F1FO-ATPase and the mitochondrial permeability transition

The albedo and pulp of bergamot are rich sources of fibers and polyphenols [1].Bergamot fiber (BF) confers a beneficial effect on the gut microbiota and can beconsidered prebiotics. The bergamot polyphenolic fraction (BPF) is used in the form ofnutraceuticals with countless beneficial properties such as anticancer, antiviral and anti-inflammatory, antioxidant, cardioprotective, and lipid-lowering [2]. The F1FO-ATPase isconsidered the leading candidate responsible for the mitochondrial permeability transitionpore (mPTP) formation when the natural cofactor Mg2+ is replaced with Ca2+ [3]. Wetested BF, BPF or a mixture of both on swine heart mitochondria to evaluate the effect onmitochondrial bioenergetics. The F1FO-ATPase activity, dependent on the naturalcofactor Mg2+ increased by 15%, whereas the enzyme activity in the presence of Ca2+was inhibited by 10% with 100 μg/mL BPF. Conversely, BF did not affect the Mg2+- orCa2+-activated F1FO-ATPase. mPTP formation, measured as calcium retentioncapacity, was inhibited with BPF or BF. The correlation index (CI) will be calculated toevaluate the pharmacological interaction between BPF and BF to define synergism (CI <1), antagonism (CI > 1) or additive (CI = 1) effect.