Lentini Guglielmo, Querqui Alessandro, Monti Noemi, Bizzarri Mariano
Department of Experimental Medicine, Space Biomedicine Laboratory, University Sapienza, Rome, Italy.
Drug Des Devel Ther. 2025 May 21;19:4183-4199. doi: 10.2147/DDDT.S524718. eCollection 2025.
This Expert Opinion covers recent updates in the use of Inositol in polycystic ovary syndrome (PCOS), highlighting the specific effects triggered upon ovarian steroidogenesis.
An impressive body of evidence, obtained from molecular, animal and clinical studies, demonstrated the striking association between PCOS and the metabolism of myo-Inositol (myo-Ins) and its isomer D-Chiro-Inositol (DCI). Early investigations focused primarily on the metabolic consequences of inositol in modulating insulin transduction. However, recent advances disclosed that Inositols trigger direct effects on steroidogenesis. High DCI levels exacerbate androgen synthesis, and downregulate aromatase expression. Myo-Ins modulates insulin effects too, but exerts opposite actions on steroidogenesis, by increasing aromatase and FSH receptor expression. Clinical studies demonstrated myo-Ins efficacy, suggesting that an appropriate ratio in between myo-Ins/DCI (40:1) improves the reproductive function in PCOS women, even in absence of insulin resistance.
Inositol-based treatments in PCOS are gaining momentum, demonstrating safety and efficacy greater than those obtained with other pharmacological agents. The efficacy depends not only on the modulation of insulin sensitivity but also on the direct, steroidogenic effects upon the ovaries. Adequate adsorption of Inositol is a critical issue, and the association of α-Lactalbumin can significantly overcome this problem. However, if a treatment based on inositol could be equally effective on different phenotypes of PCOS needs a specific assessment.
本专家意见涵盖了多囊卵巢综合征(PCOS)中肌醇使用的最新进展,重点介绍了对卵巢类固醇生成产生的特定影响。
从分子、动物和临床研究中获得的大量令人瞩目的证据表明,PCOS与肌醇(myo-Ins)及其异构体D-手性肌醇(DCI)的代谢之间存在显著关联。早期研究主要集中在肌醇调节胰岛素转导的代谢后果上。然而,最近的进展表明,肌醇对类固醇生成有直接影响。高DCI水平会加剧雄激素合成,并下调芳香化酶表达。肌醇也调节胰岛素作用,但对类固醇生成发挥相反作用,通过增加芳香化酶和促卵泡激素(FSH)受体表达。临床研究证明了肌醇的疗效,表明即使在没有胰岛素抵抗的情况下,肌醇/ DCI之间的适当比例(40:1)也能改善PCOS女性的生殖功能。
PCOS中基于肌醇的治疗正在兴起,显示出比其他药物更高的安全性和疗效。疗效不仅取决于胰岛素敏感性的调节,还取决于对卵巢的直接类固醇生成作用。肌醇的充分吸收是一个关键问题,而α-乳白蛋白的联合使用可以显著克服这一问题。然而,基于肌醇的治疗对PCOS的不同表型是否同样有效需要进行具体评估。