Result of Protodioscin (Tribulus terrestris) treatment in ...
Result of Protodioscin (Tribulus terrestris) treatment in males diagnosed with infertility and impotence
K.M. Arsyad
Medical Biology Division of Andrology, University of Sriwijaya, Indonesia (1996)
SUMMARY
Libilov treatment consisting of oral administration of 3 x 1 to 3 x 2 tablets / day for 14 to 60 days was shown to be effective in improving the concentration and quality of spermatozoa in patients with oligozoospermia. Furthermore, the treated men also reported improvement in sexual libido, erection, ejaculation and orgasm. Libilov treatment also resulted in improved spermatogenesis in the Sertoli and germinal cells, and increased the efficiency of testosterone conversion to dihydrotestosterone (DHT). As DHT played an important role in the improvement of red blood cell formation (erythropoiesis) as well as muscle development, this contributed to the sense of physical well-being and improved oxygen circulation in the body. Indirectly, these effects also added to the improvement in sexual functions, including libido, erection, and orgasm.
INTRODUCTION
Protodioscin is the active ingredient found in the extract of the plant Tribulus terrestris L., available under the tradename Libilov™. This herbal plant has been traditionally used in Asian and European countries to treat infertility and impotence (Viktorof et al. 1994). Male fertility is defined as a man's ability to impregnate his spouse or partner, leading to a successful birth within the first twelve months of continuous effort to conceive. In contrast, the inability of the male to achieve conception is defined as male infertility. In primary male infertility, it is the woman's first time trying to conceive. On the other hand, if a man has successfully impregnated the woman in the past, leading to a normal pregnancy, or spontaneous or intentional abortion, but is currently unable to impregnate his wife successfully within one year of effort, then his infertility is characterized as secondary infertility (Rowe et al. 1993).
Generally defined, impotence is a collection of sexual dysfunctions that can be manifested as reduction in sexual drive, desire or libido, penile erection, ejaculation or even the ability to achieve orgasm. As impotence can occur in all sexual response phases, we can classify impotence as follows (Susilo 1994, Adimoelja 1985, Barry and Hodges 1987, Ellenberg 1971):
1. Impotensia libidinis or impotensia concupiciency ( manifests as lowered sexual drive)
2. Impotensia erectionis (the inability to achieve or maintain penis erection for normal sexual intercourse)
3. Impotensia ejaculationis (involves ejaculation dysfunctions, which includes premature, retarded, retrograde, incomplete ejaculations and non-ejaculations)
4. Impotensia satisfactionis / emotionis (manifests as unsatisfactory orgasm or inability to reach orgasm during sexual intercourse)
Here, we review the mechanism of how protodioscin treatment works, as well as the result of Libilov clinical trials on male subjects diagnosed with either impotence or infertility.
CLINICAL ACTION OF PROTODIOSCIN ON THE MALE REPRODUCTIVE SYSTEM
In comparison to currently available treatments for infertility and impotence, protodioscin has been shown to be more efficient, less costly, and more importantly, to carry significantly less risk of unwanted side-effects. The rapid development of Libilov, a non-hormonal and natural herbal preparation of Tribulus terrestris L., was accompanied by intensive clinical and laboratory tests. Based on those tests, we conclude that Libilov provides an effective viable alternative in treating male impotence and infertility.
Chemical and Physical Characteristics of Protodioscin
Protodioscin is the active ingredient of the plant extract of Tribulus terrestris L., and is produced by PT Teguhsindo Lestaritama, Indonesia. Protodioscin is classified as a furostanol saponin, and is present in the extract at no less than 45% of the total weight. The chemical structure of this compound is shown below in Figure 1.
[pic]
Figure 1. The chemical structure of protodioscin, the active ingredient of Tribulus terrestris L. extract.
Protodioscin is physically characterized as a bitter-tasting amorphous powder, with a yellow-brown color. It is soluble in water, slightly soluble in methanol, but not soluble in chloroform.
Gonadal steroid
Three male sex steroids or androgens, namely testosterone, dihydrotestosterone and estradiol, are important for the male reproductive system (Greenspan 1991). From a quantitative perspective, the most important androgen is testosterone. More than 95% of this hormone is produced by Leydig cells, with the rest produced by the adrenal glands. To supplement testosterone, the testes also produces a small amount of potent form of androgen called dihydrotestosterone (DHT), as well as weaker forms such as dehydroepiandrosterone (DHEA) and androstenedione. These cells also secrete a small quantity of estradiol (E), estrone, pregnenolone, and progesterone, and 17-alpha-hydroxyprogesterone. In addition to their production in testes, DHT and E are also produced by the breakdown of androgens in the peripheral circulatory networks. The biosynthetic steps of androgen in the testes is diagrammed in Figure 2. The contribution of testes, adrenal and peripheral networks on the serum level of the male sexual steroids is shown in Table 1.
[pic]
Figure 2. The biosynthetic steps of androgen production in the testes.
|Androgen |Testes Secretion |Adrenal Secretion |Peripheral Conversion |
|Testosterone |95 |< 1 |< 5 |
|Dihydrotestosterone |20 |< 1 |80 |
|Estradiol |20 |< 1 |80 |
|Estrone |2 |< 1 |98 |
|DHEA-Sulphate |< 10 |90 |- |
Table I. The contribution of testes adrenal secretion and peripheral network conversion on the total level of androgens in the bloodstream. Values are in percent.
In the bloodstream, androgen and estrogen are either in free form, or are in a form bound to serum proteins. Although approximately 38% of bound testosterone is bound to albumin, its major binding partner is the Sex Hormone Binding Globulin (SHBG), which associates with more than 60% of bound testosterone. SHBG is different from the Androgen Binding Protein (ABP), which is synthesized by the heart and the Sertoli cells, as SHBG level can be increased by treatment with estrogen or thyroid hormones, or by medical conditions of hyperthyroidism and hepatic cirrhosis. Conversely, treatment with growth hormone, or condition of hypothyroidism, acromegaly or obesity can lower the level of this protein. Approximately 20% of testosterone in the bloodstream is in the unbound or free form. This form of testosterone is free to enter and metabolically affect cells. In addition to the level of the free form, the bioavailability of testosterone is also influenced by the dissociation of testosterone from its binding proteins.
The majority of testosterone is converted in the heart into metabolites such as androsterone and eticholanolone, which are secreted in the urine after they react chemically with glucoronatic or sulfuric acid into 17-keto-steroid. However, since this is not the major source of 17-ketosteroid, simple measurement of this compound in the urine does not provide an accurate picture of testes steroid production. Moreover, this measurement would also not be able to detect the small amount of testosterone that is converted into a specific form of androgen called dihydrotestosterone (DHT) in specific target tissues.
In the majority of target cells, some testosterone is enzymatically converted into DHT by the microsomal enzyme 5-alpha-reductase. Similar to testosterone, DHT is then bound by an intracytoplasmic receptor protein specific for it (becoming DHT-Rc, Figure 3). After the DHT-protein complex formation, the bound hormone is transported into the nucleus (becoming DHT-Rn, Figure 3). There the protein complex undergoes a conformational transformation, which is thought to involve chromatin binding. This results in mRNA syntheses, and subsequently in syntheses of cytoplasmic proteins, which lead to cell growth and other secondary effects mediated by androgens (Figure 3).
[pic]
Figure 3. The mechanism of the androgen's action. Free testosterone is transported into the cell and some is converted to dihydrotestosterone (DHT). Cytoplasmic receptors (Rc) bind these molecules, which are subsequently transported into the nucleus. These protein-hormone complexes (DHT-Rn, T-Rn) activate transcriptions of androgen-sensitive genes, resulting in the production of transcript mRNAs. These mRNAs are transported to the cytoplasm and are translated into proteins responsible for the androgen's action.
The biological effects of androgens in males include the appropriate fetal differentiation of the internal and external tissues which comprise the male genitalia. During puberty, androgens act to stimulate the development of the scrotum, epididymis, vas deferens, seminal vesicles, prostate, and penis tissues development. The functional integrity of these organs also depends on the androgen levels. Furthermore, androgen also induced larynx and muscle developments, which lead to the development of secondary sexual characteristics. The ambi-sexual development of pubic and armpit hair, as well as the male-specific development of facial, chest, abdomen, and back hairs are induced by the stimulation of the sebaceous glands with androgen. Other effects of androgens include stimulation of erythropoiesis, as well as psychological and behavioral changes.
Mechanism of Protodioscin
Protodioscin acts by stimulating the enzyme 5-alpha-reductase, which plays a role in the conversion of testosterone into dihydrotestosterone (Viktorof et al. 1994). In addition, protodioscin also stimulates the hypothalamus secretion of luteinizing hormone (LH), but not of follicle stimulating hormone (FSH). Protodioscin is shown to increase the density of the Leydig, but not that of the Sertoli cells, and to improve the level of spermatogonia and to increase the production of spermatocytes and spermatids without changing the diameter of the seminiferous tubules. Physically, protodioscin treatment results in increased male fertility and sexual functions.
In respect to improving fertility, protodioscin increases the level of spermatogenesis by stimulating the Sertoli and germinal cells, resulting in the increased production of sperms. In this process, protodioscin improves the conversion of testosterone to DHT, which in turn stimulates the production of Androgen Binding Protein (ABP) in the Sertoli cells. Increased ABP production results in increased formation of DHT-ABP complex, which stimulates spermatogenesis in the germinal cells. Another fraction of the DHT-ABP complex is transported to the epididymis, which increases the efficiency of the maturation of spermatozoa into fertile sperms.
In respect to increasing sexual functions, protodioscin works by increasing the conversion of testosterone into the potent DHT(Figure 4). In addition to the increase in sexual drive or libido, DHT also stimulates erythropoiesis or production of red blood cells, and muscle developments, thus contributing to the improvement of blood circulation as well as the oxygen transport systems. Importantly, regular use of protodioscin has also been shown to increase the duration of penile erection and improve ejaculation in males.
[pic]
Figure 4. The mechanism of protodioscin's action. Protodioscin increases the production of serum testosterone and the conversion of testosterone to dihydrotestosterone. Dihydrotestosterone, in turn enhances erythropoiesis and muscle development. More erythropoiesis or production of red blood cell increases the hemoglobin level, which results in better oxygen transport throughout the body, resulting in a more optimal health. Both increased production of testosterone and better health contribute to the increase in sexual functions, especially the increase in sex drive.
Fertility and the Male Sexual Potential
Male fertility is clinically quantified by laboratory analyses of semen. The normal boundaries are determined by the World Health Organization in 1992 as described in Table 2. Male sexual dysfunctions are listed in Table 3.
|Parameter |Value |
|Volume |> 2.0 ml |
|pH |7.2 - 7.8 |
|Sperm concentration |> 20 million sperms / ml |
|Sperm concentration / ejaculate |> 40 million sperms / ejaculate |
|Motility |> 50% progressively motile category (a+b); or |
| |>25% rapid progressively motile (a) |
| |within 60 minutes of ejaculation |
|Morphology |> 30% with normal morphology |
|Vitality |> 70% viability, i.e. without supravital color |
|Leukocyte cells |< 1 million / ml |
|Immune droplet test |Binding to less than 20% of sperms |
|MAR test |Binding to less than 10% of sperms |
|Other tests: | |
|alpha-glucosidase |> 20 mU / ejaculate |
|zinc |< 2.4 µmol /ejaculate |
|citric acid |>52 µmol / ejaculate |
|phosphatase |>200 U / ejaculate |
|fructose |>13 µmol / ejaculate |
Table II. Parameter of semen analyses as determined by the World Health Organization (1992).
|Nomenclature |Definition |
|Normozoospermia |Normal ejaculation based on concentration, mobility and |
| |morphology of sperms |
|Oligozoospermia |Concentration of sperm < 20 million / ml |
|Severe oligozoospermia |Concentration of sperm < 3 million / ml |
|Asthenozoospermia |Mobility < 50% (a+b) or grade a mobility < 30% |
|Teratozoospermia |Normal morphology < 30% |
|Oligoashtenoteratozoospermia |Defects in concentration, mobility and morphology of |
| |sperms |
|Azoospermia |No sperm in ejaculate |
|Aspermia |No ejaculate |
|Hemospermia |Red blood cells in ejaculate |
|Pyospermia |White blood cells in ejaculate at concentration > |
| |1 million / ml |
Table III. Nomenclature of sexual dysfunctions based on semen analyses.
Male infertility can be diagnosed by routine semen analyses or by causative etiology (Comhaire 1991, Adimoelja 1990, Lee 1983, Kolodny et al. 1979). In a routine semen analyses, abnormal semen volume (hypo- or hyperspermia), abnormal sperm concentration such as polyzoospermia ( ................
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