31 results about "5 α reductase" patented technology

The present invention includes 1) a novel formulation for the treatment of hair loss comprising oleanolic acid (a 5α-reductase inhibitor), apigenin (a vasodilator), and biotinyl-GHK (a cell metabolism stimulant), 2) a novel additive for the treatment of hair loss comprising oleanolic acid, apigenin, biotinyl-GHK and a delivery agent, 3) a personal care, cosmetic, and / or dermopharmaceutical composition comprising oleanolic acid, apigenin, biotinyl-GHK, and at least one additional ingredient, and 4) a method for treating hair loss comprising the administration of oleanolic acid, apigenin, and biotinyl-GHK.

Provided is a screening method for compounds affecting fatty acid biosynthesis, the method comprising: providing a reaction mixture comprising: an acyl carrier moiety or enzymes and precursors sufficient to generate the acyl carrier moiety; a bacterial enzymatic pathway comprising at least two consecutively acting enzymes selected from the group consisting of: malonyl-CoA:ACP transacylase, beta-ketoacyl-ACP synthase III, NADPH dependent beta-ketoacyl-ACP reductase, beta-hydroxylacyl-ACP dehydrase and enoyl-ACP reductase; and substrates and cofactors required for the operation of the enzymes; contacting the reaction mixture with a prospective bioactive agent; conducting a high throughput measurement of the activity of the enzymatic pathway; and determining if the contacting altered the activity of the enzymatic pathway.

The present invention relates to topical compositions comprising 5α-reductase inhibitors. The present invention also includes processes for preparation of such topical compositions and methods of using them.

This invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of benign prostate hyperplasia in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) and / or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of treating a subject suffering from hair loss, comprising the step of administering to the subject a therapeutically effective amount of a 5-α reductase enzyme type 1 and / or type 2 inhibitor, wherein said inhibitor is a selective androgen receptor modulator (SARM) and / or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of inhibiting a 5-α reductase type 1 and / or type 2 enzyme, comprising contacting the enzyme with an effective 5-α reductase inhibitory amount of a selective androgen receptor modulator (SARM) and / or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof, as described herein.

A dietary composition for promoting melanogenesis in hair of a user comprising approximately 5,000 IU per day of catalase, a synergistic core component, 5-α-reductase inhibitors, an antioxidant component, and approximately 200 mg per day of L-tyrosine. Preferably, the synergistic core component comprises copper, vitamin B6, biotin, para-aminobenzoic acid, folic acid, zinc, and pantothenic acid. Further, 5-α-reductase inhibitors preferably comprise Saw palmetto, phytosterols, and nettle root extract. The antioxidant component preferably comprises horsetail, Fo-Ti, chlorophyll, and barley grass.

Disclosed herein are compositions for controlling androgen activity in target organs and cells through the modulation of a 5-α-reductase activity. In certain aspects, these compositions are employed to modulate androgenic activity by inhibiting the formation and availability of active androgen in target cells. As a result, the present invention is directed toward the treatment of a wide variety of conditions including, but not limited to, the treatment of prostatic hyperplasia, prostatic cancer, hirsutism, acne, male pattern baldness, seborrhea, and other diseases related to androgen hyperactivity. Several of these compositions have been shown to effectively decrease body weight, and in some cases, to decrease the weight of an androgen-dependent body organ, such as the prostate and other organs.

The present invention relates to a composition for promoting hair growth. More particularly, the present invention comprises a component for inhibiting 5α-reductase activity, a functional component of cell activity, and an expansion component of peripheral blood vessels. A composition for promoting hair growth of the present invention has a superior effect on hair growth.

The present invention relates to a composition for increasing testosterone physiological levels comprising: a) a sufficient amount of at least one aromatase inhibitor chosen from a flavone substituted with at least one methoxy group at position 3′,4′,5 or 7, any combinations thereof, and any di, tri or tetra combinations thereof; and a flavanone substituted with at least one methoxy group at position 3′,4′,5 or 7, any combinations thereof, and any di, tri or tetra combinations thereof; and b) a sufficient amount of at least one 5α-reductase inhibitor that inhibit testosterone conversion to DHT, such as beta-sitosterols; in association with a pharmaceutically acceptable carrier.

There is provided a hair tonic comprising at least two of an inhibitor against 5α reductase type 2, an inhibitor against transforming growth factor β2, and an inhibitor against caspase-3; a method comprising screening for at least two of inhibition against 5α reductase type 2, inhibition against transforming growth factor β2, and inhibition against caspase-3, or comprising screening for inhibition against caspase-3 and then for apoptosis inhibition, and a hair loss inhibitor having the effect of inhibiting caspase-3, and a hair loss inhibitor having the effect of inhibiting caspase-3 and of inhibiting apoptosis.

New 17α-fluorosteroid compounds of formula (I) are disclosed: wherein R1 denotes H or methyl; R2 and R3 each denote H, Cl or methyl; and either a double bond or a single bond is present between C-6 and C-7 and also C-9 and C-10 of the steroid ring system respectively. These compounds have an activity profile with hybrid character so that they act as inhibitors for 5α-reductase and as high potency gestagens. Pharmaceutical compositions containing them are disclosed. They are suitable for treatment of conditions, which are caused by high levels of androgen in organs and tissues. These new compounds can be used in combination with other hormonal substances, such as estrogens, testosterone and other androgens, as contraceptives and for other applications.

The present invention relates to a composition for topical application for preventing hair loss and stimulating hair growth having a 5α-reductase suppressant and minoxidil. The composition for topical application for preventing hair loss and stimulating hair growth according to the present invention provides equal or superior hair loss prevention and hair growth stimulation effects while using a much smaller dosage than conventional compositions which use oral 5α-reductase inhibitors and minoxidil alone or together.

Provided are uses of lychee skin extract as a 5α-reductase inhibitor: use of lychee skin extract as a 5α-reductase inhibitor in preparation of personal care products having sebum balancing and anti-acne efficacy, and use of lychee skin extract as a 5α-reductase inhibitor in preparation of personal care products having hair loss prevention efficacy.

The present invention includes 1) a novel formulation for the treatment of hair loss comprising oleanolic acid (a 5α-reductase inhibitor), apigenin (a vasodilator), and biotinyl-GHK (a cell metabolism stimulant), 2) a novel additive for the treatment of hair loss comprising oleanolic acid, apigenin, biotinyl-GHK and a delivery agent, 3) a personal care, cosmetic, and / or dermopharmaceutical composition comprising oleanolic acid, apigenin, biotinyl-GHK, and at least one additional ingredient, and 4) a method for treating hair loss comprising the administration of oleanolic acid, apigenin, and biotinyl-GHK.

A method and preparation which uses Argania spinosa is provided for treating acne, seborrhoea, unwanted hair, and having anti-5-α-reductase activity. The useful compositions contain from 0.01 to 25% by weight, based on a dry weight, of an extract of Argania spinosa.

An isolated steroidogenesis modified cell comprising one or more steroid biosynthesis knock down nucleic acid operatively linked to a promoter, wherein the steroid biosynthesis knock down nucleic acid reduces the expression of a gene selected from the group CYP21A2, CYP11A1, CYP17A1, CYP19A1, 3-βHSD1, 3-βHSD2, 17-βHSD1, StAR, HMGR, CYP11B2, CYP11B1, 5α-Reductase 2, SULT1E1, CYP3A4 and UTG1A1, wherein the cell comprises reduced expression of one or more of said genes. The cells are useful for identifying endocrine disruptors. Accordingly, the disclosure includes in a further aspect a screening assay for identifying an endocrine disruptor comprising:a) contacting a cell described herein with a test substance;b) determining a level of at least one steroid or steroidogenic gene mRNA or enzyme activity;wherein a modulation in the level of the at least one steroid or steroidogenic gene mRNA or enzyme activity compared to a control is indicative that the test substance is an endocrine disruptor.

The invention provides the use of an extract of a plant of the genus Elephantorrhiza and at least one compound selected from quercitin-3′-O-glucoside, trans-3-O-galloyl-3,3′,5,5′,7-pentahydroxyflavan, taxifolin-3′-O-glucoside, catechin and epicatechin in the preparation of a medicament for the treatment of benign prostatic hyperplasia (BPH). The mode of action is by a route selected from blocking the conversion of testosterone to dihydrotestosterone by inhibiting the 5α-reductase enzyme or by reducing oxidative stress or both.

With an object of discovering a substance having a testosterone 5α-reductase inhibiting action, a hair papilla cell growth promoting action, a fibroblast growth factor-7 production promoting action, a vascular endothelial growth factor production promoting action or a bone morphogenetic protein-2 production promoting action, and of providing a hair care product having this substance blended therein, and a hair growth tonic, a testosterone 5α-reductase inhibitor, a hair papilla cell growth promoter, a fibroblast growth factor-7 production promoter, a vascular endothelial growth factor production promoter and a bone morphogenetic protein-2 production promoter each having this substance as an active ingredient thereof, a hair care product of the present invention is made to contain corosolic acid therein, and each of a hair growth tonic, a testosterone 5α-reductase inhibitor, a hair papilla cell growth promoter, a fibroblast growth factor-7 production promoter, a vascular endothelial growth factor production promoter and a bone morphogenetic protein-2 production promoter of the present invention is made to contain corosolic acid as an active ingredient thereof.

The human body is mediated by a large number of chemicals and chemical processes where imbalances can result in an abnormal condition that affects part or all of the human body. Amongst these conditions are hair loss and male impotence or erectile dysfunction, both of which can have psychological consequences for the patient and others as they can be tied to relationship difficulties and self-image. 5α-reductase Type II inhibitors prevent DHT production and reduce androgen activity in key tissues such as prostate and scalp. Similarly, an inhibitor of cyclic guanosine monophosphate (cGMP) specific phosphodiesterase type 5 (PDE5) can lead to improved vasodilation and blood flow. It would be beneficial to provide patients with either of these treatments within a topical cream form allowing localized targeted delivery.

The present disclosure relates to an engineered microbe capable of improved productivity of fatty acid or fatty acid derivative. An NAD+-dependent 3-oxoacyl-ACP reductase or NAD+-dependent 3-oxoacyl-CoA reductase replaces or supplements the native NADP+-dependent 3-oxoacyl-ACP reductase so as to utilize the higher availability of NAD+ rather than NADP+ in the cell. Higher production, yield and titer of fatty acids are therefore obtained. Such microbes can be combined with other mutations to further improve yield of fatty acids or fatty acid derivatives.

An isolated steroidogenesis modified cell comprising one or more steroid biosynthesis knock down nucleic acid operatively linked to a promoter, wherein the steroid biosynthesis knock down nucleic acid reduces the expression of a gene selected from the group CYP21A2, CYP11A1, CYP17A1, CYP19A1, 3-βHSD1, 3-βHSD2, 17-βHSD1, StAR, HMGR, CYP11B2, CYP11B1, 5α-Reductase 2, SULT1E1, CYP3A4 and UTG1A1, wherein the cell comprises reduced expression of one or more of said genes. The cells are useful for identifying endocrine disruptors. Accordingly, the disclosure includes in a further aspect a screening assay for identifying an endocrine disruptor comprising:a) contacting a cell described herein with a test substance;b) determining a level of at least one steroid or steroidogenic gene mRNA or enzyme activity;wherein a modulation in the level of the at least one steroid or steroidogenic gene mRNA or enzyme activity compared to a control is indicative that the test substance is an endocrine disruptor.

The present disclosure relates to an engineered microbe capable of improved productivity of fatty acid or fatty acid derivative. An NAD+-dependent 3-oxoacyl-ACP reductase or NAD+-dependent 3-oxoacyl-CoA reductase replaces or supplements the native NADP+-dependent 3-oxoacyl-ACP reductase so as to utilize the higher availability of NAD+ rather than NADP+ in the cell. Higher production, yield and titer of fatty acids are therefore obtained. Such microbes can be combined with other mutations to further improve yield of fatty acids or fatty acid derivatives.

This invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of benign prostate hyperplasia in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) and / or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of treating a subject suffering from hair loss, comprising the step of administering to the subject a therapeutically effective amount of a 5-α reductase enzyme type 1 and / or type 2 inhibitor, wherein said inhibitor is a selective androgen receptor modulator (SARM) and / or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of inhibiting a 5-α reductase type 1 and / or type 2 enzyme, comprising contacting the enzyme with an effective 5-α reductase inhibitory amount of a selective androgen receptor modulator (SARM) and / or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof, as described herein.

A substance having a testosterone 5α-reductase inhibiting action, a hair papilla cell growth promoting action, a fibroblast growth factor-7 production promoting action, a vascular endothelial growth factor production promoting action or a bone morphogenetic protein-2 production promoting action, and a hair care product having this substance blended therein. A hair growth tonic, a testosterone 5α-reductase inhibitor, a hair papilla cell growth promoter, a fibroblast growth factor-7 production promoter, a vascular endothelial growth factor production promoter and a bone morphogenetic protein-2 production promoter each having this substance, such as corosolic acid, as an active ingredient thereof.

Disclosed herein are compositions for controlling androgen activity in target organs and cells through the modulation of a 5-α-reductase activity. In certain aspects, these compositions are employed to modulate androgenic activity by inhibiting the formation and availability of active androgen in target cells. As a result, the present invention is directed toward the treatment of a wide variety of conditions including, but not limited to, the treatment of prostatic hyperplasia, prostatic cancer, hirsutism, acne, male pattern baldness, seborrhea, and other diseases related to androgen hyperactivity. Several of these compositions have been shown to effectively decrease body weight, and in some cases, to decrease the weight of an androgen-dependent body organ, such as the prostate and other organs.

The abietic acid derivatives as anti-tumor agents are derivatives of abietic acid in which the hydroxyl entity (—OH) of the carboxyl entity is replaced by an electronegative substituent, which may be C6H5-O—, C6H5-S—, or C6H5-NH—, and a hydrogen atom on one of the rings is replaced by a hydroxyl (—OH) substituents, the derivatives having the formula:wherein X is O, S, or NH. The derivatives are formed by formation of an intermediate lactone from abietic acid, followed by reaction of the lactone with phenol, thiophenol, or aniline. All of the derivatives exhibited potent 5α-reductase inhibitor activity, both in vitro and in vivo, and anti-tumor activity with regard to two prostate cancer cell lines—LNCaP and PC-3. The intermediate lactones are also derivatives of abietic acid that exhibit anti-tumor activity.

Causes of hair loss have not been completely clarified and still remain unknown in many points. However, it appears that hair loss is partly caused by a mechanism wherein androgenic hormones in the scalp become active via the activation of DHT hormone by 5α-reductase and thus the activity of cells in hair roots is lost.In the present invention, an antibody, said antibody being obtained by inoculating a female bird with 5α-reductase or DHT as an antigen, is administered to the scalp so that the activity of DHT is suppressed and the activity of cells in hair roots is elevated. This antibody can be used in the form of a composition together with other component(s), for example, as a hair tonic together with another hair growth promoter.