madman
Super Moderator
Abstract
Background: Androgen deficiency affects men in adulthood, causing several harmful effects at the reproductive and behavioral levels. Since aromatase is an enzyme that catalyzes the conversion of androgens to estrogens, and it is responsible for an adequate balance of both sex hormones in males and females, the administration of molecules acting as down modulators may contribute to restore an abnormal enzymatic activity. A prospective pilot study was carried out to investigate the effect of D-chiro-inositol, a putative aromatase downmodulator, on serum levels of testosterone, estradiol, estrone, dehydroepiandrosterone, and epiandrosterone from a group of adult male volunteers. Glucose, insulin, follicle-stimulating hormone, luteinizing hormone, inhibin B, Dchiro-inositol, and Myo-inositol serum levels were also measured.
Results: Male volunteers were selected according to age and body mass index. Subjects with altered glycemia and/or hormonal status, due to advanced age or abnormal weight, were enrolled in the study. Each of the 10 volunteers enrolled took oral D-chiro-inositol (1 g/day) for 1 month. Serum assays of selected markers were performed at baseline (control) and after treatment. D-chiro-inositol administration was associated with reduced serum levels of estrone (− 85.0%) and estradiol (− 14.4%), and increased serum levels of testosterone (+ 23.4%) and dehydroepiandrosterone (+ 13.8%). In addition, epiandrosterone levels were higher (+39%) after treatment. On the other hand, follicle-stimulating hormone, luteinizing hormone, and inhibin B did not change. A trend toward a decrease of glycemia, insulinemia, and Homeostatic Model Assessment index was observed after D-chiro-inositol treatment, although differences did not reach statistical significance. D-chiro-inositol treatment did not cause any noticeable adverse effect.
Conclusions: Increased androgens and decreased estrogens seem to confirm that D-chiro-inositol acts as an aromatase down-modulator, but with a still unknown mechanism of action. This pilot study opens up new perspectives of research and therapeutic applications for D-chiro-inositol at different dosages and lengths of treatment.
Introduction
Testosterone (T) and Estradiol (E2) are essential in male physiology. Both hormones participate in the development of sexual characteristics during adolescence and contribute to general health in adulthood [1–6]. The biosynthesis of T and its conversion to E2 involve enzymatic processes that maintain the delicate balance between the two hormones. Hence, adequate regulation of the participating enzymes is of primary importance. In particular, the enzyme aromatase catalyzes the peripheral conversion of androgens to estrogens. Aromatase, also known as estrogen synthetase (gene CYP19A1), is widely expressed in several tissues and organs of the human body, including testis, granulosa of ovarian follicles, placenta, skin fibroblasts, prostate, adipose tissue, bones, breast, brain [7]. Furthermore, it was found also in vascular smooth muscle cells [8], skeletal muscles [9], liver [10], and gastric mucosa [11]. In particular, the adipose tissue that is very rich in aromatase content [12], produces a considerable amount of circulating estrogens [13].
Alterations in the aromatase activity lead to a hormonal imbalance. In fact, excessive aromatase activity results in reduced levels of T and increased concentration of estrogens [7, 14].
*Estrogens, androgens, and aromatase expression are fundamental in men, just like in women
Conclusions
The preliminary results presented in this report demonstrate, for the first time, that a daily oral administration of 1 g DCI can improve the sexual hormone profile in adult men. As a result of DCI treatment, E1 significantly and E2 not significantly decreased, whereas T, DHEAS, and Epia increased, resulting in an increased T/E2 ratio. The most dramatic change was the significant reduction of E1 serum levels, which may relate to a direct hypoglycemic activity previously observed for DCI. Altogether, these findings lead the authors to propose that DCI may act as a down-regulator of the aromatase activity. Additional studies with a larger cohort of patients are required to confirm our findings, but also to evaluate the effects on prostate and sperm parameters and to understand the underlying molecular mechanisms involved in DCI activities. A relevant aspect to highlight is the safety profile of DCI, which represents a great advantage with respect to aromatase inhibitors.
The complex activities exerted by DCI offer promising opportunities. DCI may be administered at different dosages and lengths of treatment to treat in men mood disorders or reduced libido associated with low testosterone levels, hypogonadotropic hypogonadism, overweight, or obesity.
Background: Androgen deficiency affects men in adulthood, causing several harmful effects at the reproductive and behavioral levels. Since aromatase is an enzyme that catalyzes the conversion of androgens to estrogens, and it is responsible for an adequate balance of both sex hormones in males and females, the administration of molecules acting as down modulators may contribute to restore an abnormal enzymatic activity. A prospective pilot study was carried out to investigate the effect of D-chiro-inositol, a putative aromatase downmodulator, on serum levels of testosterone, estradiol, estrone, dehydroepiandrosterone, and epiandrosterone from a group of adult male volunteers. Glucose, insulin, follicle-stimulating hormone, luteinizing hormone, inhibin B, Dchiro-inositol, and Myo-inositol serum levels were also measured.
Results: Male volunteers were selected according to age and body mass index. Subjects with altered glycemia and/or hormonal status, due to advanced age or abnormal weight, were enrolled in the study. Each of the 10 volunteers enrolled took oral D-chiro-inositol (1 g/day) for 1 month. Serum assays of selected markers were performed at baseline (control) and after treatment. D-chiro-inositol administration was associated with reduced serum levels of estrone (− 85.0%) and estradiol (− 14.4%), and increased serum levels of testosterone (+ 23.4%) and dehydroepiandrosterone (+ 13.8%). In addition, epiandrosterone levels were higher (+39%) after treatment. On the other hand, follicle-stimulating hormone, luteinizing hormone, and inhibin B did not change. A trend toward a decrease of glycemia, insulinemia, and Homeostatic Model Assessment index was observed after D-chiro-inositol treatment, although differences did not reach statistical significance. D-chiro-inositol treatment did not cause any noticeable adverse effect.
Conclusions: Increased androgens and decreased estrogens seem to confirm that D-chiro-inositol acts as an aromatase down-modulator, but with a still unknown mechanism of action. This pilot study opens up new perspectives of research and therapeutic applications for D-chiro-inositol at different dosages and lengths of treatment.
Introduction
Testosterone (T) and Estradiol (E2) are essential in male physiology. Both hormones participate in the development of sexual characteristics during adolescence and contribute to general health in adulthood [1–6]. The biosynthesis of T and its conversion to E2 involve enzymatic processes that maintain the delicate balance between the two hormones. Hence, adequate regulation of the participating enzymes is of primary importance. In particular, the enzyme aromatase catalyzes the peripheral conversion of androgens to estrogens. Aromatase, also known as estrogen synthetase (gene CYP19A1), is widely expressed in several tissues and organs of the human body, including testis, granulosa of ovarian follicles, placenta, skin fibroblasts, prostate, adipose tissue, bones, breast, brain [7]. Furthermore, it was found also in vascular smooth muscle cells [8], skeletal muscles [9], liver [10], and gastric mucosa [11]. In particular, the adipose tissue that is very rich in aromatase content [12], produces a considerable amount of circulating estrogens [13].
Alterations in the aromatase activity lead to a hormonal imbalance. In fact, excessive aromatase activity results in reduced levels of T and increased concentration of estrogens [7, 14].
*Estrogens, androgens, and aromatase expression are fundamental in men, just like in women
Conclusions
The preliminary results presented in this report demonstrate, for the first time, that a daily oral administration of 1 g DCI can improve the sexual hormone profile in adult men. As a result of DCI treatment, E1 significantly and E2 not significantly decreased, whereas T, DHEAS, and Epia increased, resulting in an increased T/E2 ratio. The most dramatic change was the significant reduction of E1 serum levels, which may relate to a direct hypoglycemic activity previously observed for DCI. Altogether, these findings lead the authors to propose that DCI may act as a down-regulator of the aromatase activity. Additional studies with a larger cohort of patients are required to confirm our findings, but also to evaluate the effects on prostate and sperm parameters and to understand the underlying molecular mechanisms involved in DCI activities. A relevant aspect to highlight is the safety profile of DCI, which represents a great advantage with respect to aromatase inhibitors.
The complex activities exerted by DCI offer promising opportunities. DCI may be administered at different dosages and lengths of treatment to treat in men mood disorders or reduced libido associated with low testosterone levels, hypogonadotropic hypogonadism, overweight, or obesity.
