Pharmacodynamics and pharmacokinetics of inositol(s) in health and disease

Abstract

Besides being a structural element, myo-inositol exerts unexpected functions, mostly unknown. However, several reports indicate that inositol plays a key role during phenotypic transitions and developmental phases. Furthermore, dysfunctions in the regulation of inositol metabolism have been implicated in several chronic diseases. Clinical trials using inositol in pharmacological doses provide amazing results in the management of gynecological diseases, respiratory stress syndrome, Alzheimer's disease, metabolic syndrome, and cancer, for which conventional treatments are disappointing. However, despite the widespread studies carried out to identify inositol-based effects, no comprehensive understanding of inositol-based mechanisms has been achieved. An integrated metabolomics-genomic study to identify the cellular fate of therapeutically administered myo-inositol and its genomic/enzymatic targets is urgently warranted.

Inositol and antioxidant supplementation: Safety and efficacy in pregnancy

“…Inositol (cyclohexanehexol), a cyclic carbohydrate with six hydroxyl groups, was originally isolated in 1850 from muscle extracts by Scherer and named Myo‐inositol (Myo), from the Greek word meaning “muscle.” Myo can be obtained through biosynthetic mechanisms and from dietary sources. Although Myo was initially considered as an essential nutrient belonging to the vitamin B family, it has been observed that the liver and the kidneys are able to produce up to 4 g/day of inositol.…”

“…Myo is only one of the nine possible structural isomers of inositol, as other naturally occurring stereoisomers have been found: scyllo‐, muco‐, epi‐, neo‐, allo‐, cis‐, d ‐chiro‐, and l ‐chiro‐inositol . In vivo Myo can be converted into DCI in tissues expressing the specific epimerase .…”

Myo‐inositol and D‐chiro‐inositol (40:1) reverse histological and functional features of polycystic ovary syndrome in a mouse model

“…MyoIns/DCIns formulation that contained the minimal amount of DCIns was less effective than the 40:1 ratio in terms of both ovarian structure and clinical outcome.Results herein reported with various MyoIns/DCIns ratios deserve further discussion regarding the specific functions of the two isomers. Although the intracellular inositol pool in the whole body is almost totally represented by MyoIns, the balance in the MyoIns/DCIns ratio, which is maintained by activity of a nicotinamide adenine dinucleotide (NAD), NADH-dependent epimerase that converts MyoIns into DCIns(Bizzarri, Fuso, Dinicola, Cucina, & Bevilacqua, 2016b), is strictly tissue-dependent and reflects specific tissue-related functions. Indeed, MyoIns and DCIns have different physiological roles since the former increases cellular glucose uptake,…”

Looking at the Link between Diet and PCOS Onset and Management

“…Inositol and its derivatives cover a very wide range of physiological activities. The most important molecule is Myo-Inositol (MI), which plays a key function as essential constituent of membrane-incorporated phosphatidylinositol, as well as contributing, per se or conjugated to phosphate, to ion channel permeability, metabolic homeostasis, mRNA export and translation, cytoskeleton remodelling, stress response, just to cite a few [1]. MI and D-chiro-Inositol (DCI), both stereoisomers of inositol, are capable of exerting an insulin-sensitizing effect leading to a reduction of insulin levels in blood, function as insulin second messengers and mediate different insulin actions.…”