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Substances and agents for positively influencing collagenRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Live Hair Or Scalp Treating Compositions (nontherapeutic), Plant Extract Of Undetermined ConstitutionSubstances and agents for positively influencing collagen description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070148123, Substances and agents for positively influencing collagen. Brief Patent Description - Full Patent Description - Patent Application Claims
BRIEF DESCRIPTION OF THE DRAWINGS [0001] FIG. 1 shows a micrograph of a skin biopsy taken from a 43 year old women prior to treatment with the cream lotion described in Example 3; [0002] FIG. 2 shows a micrograph of a skin biopsy taken from the 43 year old women after 16 weeks of treatment with the cream lotion described in Example 3; [0003] FIG. 3 is a photograph showing the stretched strias in the region of thighs and buttock of a 25 year old women before treatment with the gel described in Example 4; and [0004] FIG. 4 is a photograph showing the region of the thighs and buttock of the 25 year old women after 10 weeks of treatment with the gel described in Example 4. DESCRIPTION [0005] The present invention relates to the use of substances and agents, which positively influence the peripheric-local, tissue- or organ-cell specific generation of sexual hormones, and to the therapeutic or prophylactic applications related thereto. The present invention particularly relates to the use of such substances and agents for positively influencing collagen. For this purpose, applications for collagen-containing parts of the body are contemplated, such as skin, tendons, fasciae, ligaments, cartilages, bones, dentine, arteries and veins, urinary vessels and other vessel walls. Extremely useful possibilities follow therefrom for the prophylaxis and therapy of various diseases. "Positive influencing" in the terms of the invention means essentially a stabilization, an increase and/or a restoration of collagens or collagen fibres. [0006] As to the background of the invention, the context of the peripheric local, tissue- or organ-cell specific production of sexual hormones will be described in the following. [0007] Testosterone is the essence of the male sexual hormones. Its effects are exhibited via the so-called androgen receptor. Like all steroid hormones, testosterone acts together with its transcriptional factor (Roy 1995), which regulates the transcription. Androgen receptors change their structure upon binding of androgen and move to the cell nucleus towards the corresponding genes, the expressions of which are influenced by androgens. Testosterone itself does not bind particularly strong to the androgen receptor, but first has to be slightly chemically modified within the cell. The enzyme 5-alpha-reductase removes the single double-bond in the steroid hormone molecule, and dihydrotestosterone (DH) is made, which has a tenfold higher affinity to the androgen receptor than testosterone (Grino, 1990). Dihydrotestosterone may also be made from 5-alpha-dihydroandrostendione, which itself was made from androstendione by means of 5-alpha-reductase. This route strongly predominates e.g. in the genital skin of men and women (Stanczyk 1990). [0008] Thus, this conversion, which occurs not before the target organ, i.e. in the periphery, strongly enhances the testosterone-derived effect. For example, in the skin, the effect comprises the promotion of hair growth (except for the scalp) and the increase of the activity of the sebaceous glands. Only cells which have both 5-alpha-reductase-activity and androgen receptors, are allowed to be correspondingly stimulated by testosterone in physiological amounts. The testosterone merely originates from the testicle and, at a minor proportion, also from the adrenal gland. The testosterone level of men is 280 to 1100 nano grams/milli liter and of women 15 to 70 nano grams/milli liters (estradiol: up to 0.45 nano grams/milli liter), resp. [0009] Not only for dihydrotestosterone, but also for testosterone itself, there is an intracellular synthesis route in the periphery (Labrie 1995). Testosterone produced there, however, is not delivered to the blood stream, but acts within the cell where it was made after its conversion into DHT within the same cell. The precursor of the testosterone produced in the periphery is released from the adrenal gland into the blood. The precursor is dehydroepiandrosterone (DHEA), which is present in the blood in micro molar concentrations. Dehydroepiandrosterone is converted into another molecule within the cell, where it has been invaded easily through the cell membrane by simple diffusion. To this end, the 3-beta-hydroxyl group is converted into a keto group, and the double-bond of ring B is transferred into ring A (3-betahydroxysteroid-dehydrogenase/isomerase, 3-beta HSD). Androstendione is produced thereby, from which it is only a little step to testosterone (conversion of the keto group at C-17 into a hydroxyl group by means of 17-betahydroxysteroid-dehydrogenase). This testosterone is then, within the same or other cells, converted into the potent androgen DHT. Using the precursor which is present in the blood at a relatively high concentration, the cells which have the above-mentioned two enzymes therefore can themselves produce, further modify or release testosterone to the environment, where it is contacted with cells which have 5-alpha-reductase and therefore can make DHT. [0010] The extent of conversion of DHEA into androstendione in the peripheral tissue depends from the DHEA level on the one hand, but also from the activity of 3-beta-HSD on the other hand. The latter is probably stimulated by the luteotropic hormone (LH) not only in the testicle, but also in the peripheral tissue (Venencie 1999). [0011] Particular structures in the brain can sensitize testosterone concentrations. When these sensitize them as being too low, a demand is directed to the pituitary gland to the effect that LH is more released. Because of this, the production of androstendione or testosterone in the corresponding peripheral tissue, such as e.g. skin, is also stimulated. If 5-alpha-reductase is present, the androgen effects are then more exerted. [0012] In women, the brain determines the concentration of estrogens instead of that of androgens. A decrease of them also leads, via LH release, to an enhancement of the peripheric conversion of DHEA into androstendione in the correspondingly established tissue. Besides testosterone, androstendione may also be converted into estrone. The enzyme which is responsible therefor is aromatase, which is not as much ubiquitous as the testosterone producing enzyme 17-beta-HSD. Aromatase is also present in the skin (Thiboutot, 1998, Theintz, 1989, Milevich 1988, Svenstrup 1990, Milevich 1990, Dijkstra 1987), but also in other tissue- or organ-specific cells. Estrone is only a weakly effective estrogen and therefore, like testosterone, must be first converted to an active hormone in the target cell in order to fully display its effects. This is done by 17-beta-HSD, which converts estrone in the much more active estradiol. The mechanism of action of estradiol on the cellular level corresponds to that of DHT. It acts via intracellular hormone receptors, which selectively activate as transcription factors the corresponding genes. However, estradiol may also be made intracellularily from androstendione not only via estrone, but also via testosterone, which can also be converted into an estrogen by means of aromatase. This time, it is converted directly into an active estrogen, estradiol. Within a particular target cell, testosterone may also be converted into a highly active androgen or a highly active estrogen by means of a single enzymatic catalytic step, resp., depending on which enzyme is more active. Therefore, in order to provide hormone effects from estrogens or androgens in the peripheral tissue, the organism needs neither ovaries nor testicles, but only an adrenal gland (Labrie 1995, Labrie 1997). Therefore, both men and women can produce in corresponding tissues both estradiol and testosterone. Since the production of highly active hormones and their effects may occur within the same cell, we speak of "intracrinology" (Labrie 1991). [0013] Since aromatase is distributed less ubiquitary than 17-beta-HSD, it is possible that steroids which have to be aromatized have been produced in other cells than estrone or estradiol. Accordingly, the theca cells in the ovary are specialized for the production of androgenic estrogen precursors, and estradiol is produced from them in the adjacent granulosa cells (Tamaoka 1987, Roberts 1990). This is reasonable, because in this case only those cells, the growth of which is connected to the growth of the follicle, release estradiol into the blood, the concentration of which indicates the size of the follicle to the brain. At a specific concentration of estradiol in the blood, ovulation occurs. This is caused by a sudden increase of the concentration of FSH in the blood which is effected by the excess of a specific threshold concentration of estradiol in the blood. The direct production of estrogens from DHEA takes place strongly during pregnancy in the placenta. The essential precursor is the sulfate form, DHEA-S. DHEA-S does not derive from the adrenal gland of the pregnant, but from that of the fetus (Gips 1980). If the delivery or the conversion is ineffective, a diagnostically distinctive decrease of particular degeneration products of estrogens (17-keto-steroids) occur in the urine. If the sulfatase which releases DHEA is missing (in-born ichthyose, which occurs only in boys) , there is no increase of the estrogen concentration within the blood of the mother. The extragonadale sexual hormone production in the skin apparently plays a role already within the fetus. A further condition, under which a normal spontaneous birth occurs in spite of hardly present estrogens in the mother blood, is the inborn deficiency of aromatase. The placenta does not convert any more androgens into estrogens, and a moustache even grows in the mother. This may be based on a stimulation of the extragonadale sexual hormone production within the skin of the mother, which results from human choriongonadotropin (hCG). This increased production is apparently responsible for the effect that at those locations, where estradiol is necessary for a normal birth, this production also results from the precursors. The estrogens which are mainly produced by the placenta are biologically quite ineffective. Their increased production is apparently based both on a high concentration of fetal precursors in the funiculus blood and on the stimulus of aromatase by means of the pregnancy-hormone hCG, the beta-chain of which is almost identical with that of FSH and therefore also displays identical biological effects. In the pregnant woman, the peripheral production of sexual steroids is also enhanced in the organs which have LH/hCG-receptors (or possibly receptors for another messenger agent). Certainly, the skin belongs to such organs (Venencie 1999, You 2000). [0014] The object of the invention is to favourably influence the extragonadal sexual hormone production in order that therapeutic effects are enabled through the peripheric-local, tissue- or organ-cell specific presence or absence of sexual hormones. [0015] According to the present invention, it was surprisingly found that collagen can be positively influenced in the collagen-containing body parts concerned by using a substance which is capable of inhibiting the production and/or the effect of estrogens. After the application of the substance or a composition containing this substance, the collagen is stabilized, increased and/or restorated in the collagen-containing body parts. [0016] With this concept, the present invention follows a fundamentally new approach. The central issue of this concept is a targeted intervention in the peripheric-local, tissue- or organ-cell specific production of sexual hormones by means of sub-stances which are particularly suitable therefor, that is essentially those substances which inhibit the production and/or the effect of estrogens. Since aromatase was found to be a key enzyme in this context, aromatase inhibitors serve as particularly suitable substances of the invention for being used according to the present invention. The concurrent or additional inhibition of the production of dihydrotestosterone may also be preferably effective, particularly when applied to the skin. To this end, preferably 5-alpha-reductase inhibitors, but also alpha-receptor blockers are contemplated. [0017] It was surprisingly found that said substance(s) or the composition containing this (these) substance(s) exhibit as a consequence of their action a positive influence on the collagen, particularly on the content of the collagen fibres within the collagen containing body region such as the skin, thereby rendering these body region more tight or firm. By means of biopsies it was found that the proportion of collagen fibres increased. It is considered that--in fundamental contrast to the natural influence via the estrogen level in the blood as well as in contrast to the known estrogen replacement therapy (HRT) --a positive influence on the collagen can be achieved at the specific target location when the local extragonadal estrogen production and/or the local effect of estrogens is reduced or inhibited by using the specific substance or the composition containing this substance according to the use of the present invention. [0018] In a further aspect of the invention it was found that negative influencing factors, which may disadvantageously affect the content and stability of collagens, can be compensated at least partially by using the substance or the composition containing this substance, and harmful effects on the human body can be ameliorated thereby. As such negative influencing factors, there were identified particularly the increased release of LH, the production of vitamin D as a result of an exposure to sun illumination, and the excessive presence or the administration of glucocorticoids. [0019] As a result of the concept of the invention as mentioned above, significant implications and useful cosmetic and therapeutic uses are provided which are exemplified in further detail below. For the medical applications, the suitable substances can be used, together with the pharmaceutically acceptable additives which are typical for the respective mode of application, for the production of an agent or a pharmaceutical formulation and can be applied in the therapeutic uses. [0020] The term "estrogens" shall be construed to mean all natural, female sexual hormones which have estrogen-like effects, such as estradiol, estrone and estrol. [0021] As substances which are inhibitory in terms of production and/or effect of estrogens, particularly two classes of substances which will be described in further detail in the following are contemplated. [0022] On the one hand, these are anti-estrogens, i.e. substances which block estrogen receptors and therefore inhibit the effect of estrogen as antagonists. Continue reading about Substances and agents for positively influencing collagen... Full patent description for Substances and agents for positively influencing collagen Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Substances and agents for positively influencing collagen patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. 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