Neuroprotective, antioxidant and antiproliferative activity of grapefruit IntegroPectin on SH-SY5Y cells

Abstract

Tested in vitro on SH-SY5Y neuroblastoma cells, grapefruit IntegroPectin is a powerful neuro-protective, antioxidant and antiproliferative agent. The strong antioxidant properties of grape-fruit IntegroPectin, and its ability to preserve mitochondrial membrane potential and mor-phology, severely impaired in neurodegenerative disorders, make this new biopolymer highly soluble in water an attractive therapeutic agent for oxidative stress-associated brain disorders. Similarly, the ability of this new citrus pectin rich in naringin, linalool, linalool oxide and lim-onene adsorbed at the outer surface to inhibit cell proliferation or even kill, at high doses, neo-plastic cells, coupled to its excellent health and safety profile, opens up new therapeutic strate-gies in cancer research. In order to take full advantage of its vast therapeutic and preventive po-tential, detailed studies of molecular mechanism involved in the antiproliferative and neuro-protective of IntegroPectin are urgently needed.

Flavonoids in Lemon and Grapefruit IntegroPectin**

“…Numerous new biomedical applications of citrus IntegroPectin are anticipated, including likely use in the prevention and treatment of microbial infections and neurodegenerative disease. Preliminary evidence of synergy seems to emerge via the combined broad scope bioactivity of the i) citrus flavonoids identified in this study, ii) terpenes and other volatile compounds adsorbed at their surface, [3] and the unique molecular structure of these new pectins isolated after freeze‐drying the cavitation‐based aqueous extract [4–6] . The results of further ongoing biological and structural investigations will be reported in due course.…”

“…Along with the unique molecular structure of these new pectins, with very low degree of esterification and high amount of RG−I “hairy” region, [6] these results shed further light on the high bactericidal, antioxidant, antiproliferative and mitoprotective activity of grapefruit IntegroPectin, [4,5] and the neuro‐ and mitoprotective action of lemon IntegroPectin [6] . In the former case, the IntegroPectin polymer chains rich in RG−I regions act as carriers of adsorbed naringin, α‐terpineol and linalool, [3] which are powerful antibacterial agents particularly against Gram‐positive bacteria, permeating the hydrophobic S. aureus cell membrane, [31] with subsequent likely hydrolysis of naringin into highly antimicrobial naringenin [22]…”

“…The neuro‐ and mitoprotective action of lemon IntegroPectin, in its turn, might therefore be due to the combined neuroprotective, antioxidant and anti‐inflammatory action of eriocitrin in synergy with hesperidin and with α‐terpineol and terpinen‐4‐ol neuroprotective species abundant in the newly obtained citrus pectin [3] . Again, the physiological effects of these small biomolecules would act in combination with the RG−I enriched structure of lemon IntegroPectin polysaccharide favoring interaction with the cancer cells studied, [5] including human pulmonary cells [1] . The latter RG−I side‐chains, indeed, play a central role in enhancing the anti‐cancer, immunomodulatory, anti‐hyperlipidemic, and anti‐hyperglycemic activity [32] .…”

“…Further reporting the broad‐scope bactericidal activity of grapefruit IntegroPectin against Gram‐positive and Gram‐negative bacteria, and suggesting also the bacterial inactivation mechanism, [4] we noted that the analysis of the flavonoids and terpenes present in the new IntegroPectin was necessary en route to develop new applications of these new pectic polymers. Indeed, along with the aforementioned pronounced antibacterial activity, [2,3] grapefruit IntegroPectin was recently shown to exert high in vitro neuroprotective, mitoprotective and antiproliferative activity towards neuronal model cells [5] . Lemon IntegroPectin, in its turn, shows exceptionally high in vitro neuro‐ and mitoprotective activity towards the same human neuron model cells [6] …”