Roseff Scott, Montenegro Marta
South Florida Institute for Reproductive Medicine, Boca Raton, FL 33428, USA.
South Florida Institute for Reproductive Medicine, Miami, FL 33143, USA.
Int J Endocrinol. 2020 Mar 27;2020:6461254. doi: 10.1155/2020/6461254. eCollection 2020.
The aim of this paper is to critically analyze the composition of many inositol-based products currently used to treat Polycystic Ovary Syndrome (PCOS). Several different combinations of myo-inositol and D-chiro-inositol, with and without additional compounds such as micro- and macroelements, vitamins, and alpha-lipoic acid, have been formulated over the years. Such therapeutic proposals do not take various features of inositol stereoisomers into consideration. As an example, it is important to know that D-chiro-inositol treatment may be beneficial when administered in low doses, yet the progressive increase of its dosage results in the loss of its advantageous effects on the reproductive performance of women and a deterioration in the quality of blastocysts created via in vitro fertilization (IVF). In addition, we have to consider that the intestinal absorption of myo-inositol is reduced by the simultaneous administration of D-chiro-inositol since the two stereoisomers compete with each other for the same transporter that has similar affinity for each of them. A decrease in myo-inositol absorption is also found when it is coadministered with inhibitors of sugar intestinal absorption and/or types of sugars such as sorbitol, maltodextrin, and sucralose. The combination of these may require higher amounts of myo-inositol in order to reach a therapeutic dosage compared to inositol administration alone, a particularly important fact when physicians strive to obtain a specific plasma level of the stereoisomer. Finally, we must point out that D-chiro-inositol was found to be an aromatase inhibitor which increases androgens and may have harmful consequences for women. Therefore, the inositol supplements used in PCOS treatment must be carefully defined. Clinical evidence has demonstrated that the 40 : 1 ratio between myo-inositol and D-chiro-inositol is the optimal combination to restore ovulation in PCOS women. Therefore, it is quite surprising to find that inositol-based treatments for PCOS seem to be randomly chosen and are often combined with useless or even counterproductive molecules, all of which can weaken myo-inositol's efficacy. Such treatments clearly lack therapeutic rationale.
本文旨在批判性地分析目前用于治疗多囊卵巢综合征(PCOS)的多种基于肌醇的产品的成分。多年来,已经配制了多种不同组合的肌醇和D-手性肌醇,其中有些含有微量元素、宏量元素、维生素和α-硫辛酸等附加化合物,有些则没有。这些治疗方案没有考虑肌醇立体异构体的各种特性。例如,重要的是要知道,低剂量使用D-手性肌醇治疗可能有益,但随着剂量的逐渐增加,其对女性生殖性能的有利影响会丧失,并且通过体外受精(IVF)产生的囊胚质量会下降。此外,我们必须考虑到,由于两种立体异构体竞争相同的转运体,且该转运体对它们各自具有相似的亲和力,所以同时服用D-手性肌醇会降低肌醇的肠道吸收。当肌醇与糖肠道吸收抑制剂和/或山梨醇、麦芽糊精和三氯蔗糖等糖类同时给药时,也会发现肌醇吸收减少。与单独服用肌醇相比,这些物质的组合可能需要更高剂量的肌醇才能达到治疗剂量,这在医生努力获得特定立体异构体血浆水平时是一个特别重要的事实。最后,我们必须指出,D-手性肌醇被发现是一种芳香化酶抑制剂,会增加雄激素,可能对女性产生有害后果。因此,用于PCOS治疗的肌醇补充剂必须仔细界定。临床证据表明,肌醇与D-手性肌醇的40:1比例是恢复PCOS女性排卵的最佳组合。因此,令人惊讶的是,用于PCOS的基于肌醇的治疗方法似乎是随机选择的,并且经常与无用甚至适得其反的分子组合,所有这些都会削弱肌醇的疗效。此类治疗显然缺乏治疗依据。