51 results about "5 alpha reductase" patented technology

This invention relates to compounds, compositions, and methods useful for modulating 5-alpha reductase (SRD5A-1, SRD5A-2) and androgen receptor (AR) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of 5-alpha reductase and androgen receptor (AR) gene expression and / or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (mRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of 5-alpha reductase and androgen receptor (AR) genes.

This invention provides a composition comprising a 5-alpha reductase inhibitor and a class of androgen receptor targeting agents (ARTA), which are selective androgen receptor modulators (SARM). The compositions of this invention are useful for, inter-alia, a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment of polycystic ovarian disease; e) treatment and / or prevention of acute and / or chronic muscular wasting conditions; f) preventing and / or treating dry eye conditions; g) oral androgen replacement therapy; h) decreasing the incidence of, halting or causing a regression of prostate cancer; and / or i) inducing apoptosis in a cancer cell.

This invention relates to compounds, compositions, and methods useful for modulating 5-alpha reductase (SRD5A-1, SRD5A-2) and androgen receptor (AR) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of 5-alpha reductase and androgen receptor (AR) gene expression and / or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of 5-alpha reductase and androgen receptor (AR) genes.

This invention provides for combinations of 5 alpha reductase inhibitors and SERMs. These combinations are useful in: 1) preventing prostate carcinogenesis in a subject; 2) preventing the recurrence of, suppressing, inhibiting or reducing the incidence of prostate carcinogenesis in a subject; 3) treating a subject with prostate cancer; 4) suppressing, inhibiting or reducing the incidence of prostate cancer in a subject; 5) treating a subject with pre-malignant lesions of prostate cancer; 6) suppressing, inhibiting or reducing the incidence of pre-malignant lesions of prostate cancer in a subject; 7) reducing the incidence, inhibiting, suppressing, preventing and / or treating androgen-deprivation induced conditions in men suffering from prostate cancer, such as androgen-deprivation induced osteoporosis, bone fractures, loss of bone mineral density (BMD), hot flashes and / or gynecomastia; and 8) treating polycystic ovarian syndrome and reducing the incidence, inhibiting, suppressing, preventing and / or treating diabetes, cardiovascular disease, breast cancer and endometrial cancer in women suffering from polycystic ovarian syndrome.

The invention provides a new application of lotus plumule, in particular to the application of the lotus plumule, lotus plumule total alkaloid, bisbenzylisoquinoline-(7-0-11')-monoether key alkaloid derivant or analogue in preparing a drug or health care food of 5 alpha-reductase inhibitor. The invention also provides a 5 alpha-reductase inhibitor. The lotus plumule of the invention serves as the 5 alpha-reductase inhibitor and can serve as drug, health care food or food additive. The lotus plumule and the active ingredients thereof of the invention are used for inhibiting 5 alpha-reductase, can reduce prostate gland, can quickly remove the obstruction symptom of benign prostatic hyperplasia, can treat seborrheic alopecia and acne, has specific potency and controllable quality, is safe and provides a new option for clinic.

Disclosed are compositions of benzo(c)quinolizine derivatives and methods for promoting plant and seed growth. The compounds are benzo[c]quinolizine derivatives which exert an inhibiting effect on the 5-alpha-reductase enzymes. The compounds selectively affect the growth of plants, improving morphogenesis and development of commercially useful plants while acting as herbicides to inhibit weed development.

A cosmetic composition for preventing and treating acne, contains cryptotanshinone as an effective component. The cosmetic composition containing cryptotanshinone can be safely used without any side effect on skin, and further, can very effectively control the amount of sebum secretion due to inhibition of 5 alpha-reductase activation, and has superior anti-bacterial and anti-inflammation ability.

Disclosed is a novel synthetic method for isomeric peptides through an appropriate linkage of L-selenomethionine or Se-Methyl-L-selenocysteine with L-glutamic acid. The novel synthetic method produces isomeric peptides of L-selenomethionine or Se-Methyl-L-selenocysteine that exhibit (i) enhanced water solubility; (ii) enhanced rate of dissolution in water; (iii) enhanced bioavailability; (iv) excellent vascular endothelial growth factor promoting activity; (v) excellent anti-5-alpha-reductase activity; (vi) capabilities to prevent / reduce “hair fall” and promote “hair growth”, thereby maintaining a perfect homeostasis for “hair care”. Cosmeceutical and pharmaceutical compositions comprising the isomeric peptides obtained through an appropriate linkage of L-selenomethionine or Se-Methyl-L-selenocysteine with L-glutamic acid are also disclosed. Other dipeptides with several other amino acids and uses thereof are also disclosed.

The invention discloses a plant stock solution having oil controlling and acne removing functions and a preparation method thereof. The plant stock solution is prepared from raw materials in percentage by weight as follows: 5%-10% of 1,3-propylene glycol, 1%-5% of glycerin, 3%-8% of plant extracts, 0.1%-1% of xanthan gum, 0.01%-0.1% of sodium hyaluronate, 0.2%-0.6% of phenoxyethanol, 0.05%-0.35% of ethylhexylglycerin and the balance of deionized water. A spiraea salicifolia extract can effectively inhibit activity of 5 alpha-reductase, inhibit secretion activity of skin glands and prevent excessive oil and acne, and a bacteriostatic component can inhibit bacteria forming acne. A lotus seed extract can effectively decompose pimple and acne and regulate oil secretion; a calendula extract has superhigh healing capacity, can calm skin and has red fading, relieving and repairing effects. The three extracts are used cooperatively to effectively control secretion of sebaceous gland, and the best use effect can be obtained.

Disclosed are (i) a standardized method for the recovery of the polyphenolic contents from the seed coats of Tamarindus indica L. (ii) a standardized polyphenolic extract (10%-90%) from the seed coat of Tamarindus indica L. (standardized Indian date extract) and uses thereof as oral / topical, “skin care” and “hair care” nutra-cosmetic formulations. The standardized Indian Date extract of the present invention exhibits anti-collagenase, anti-elastase, anti-5-alpha-reductase and anti-hyaluronidase activities. The standardized Indian date extract of the present invention is suitable for oral / topical, “skin care” and “hair care” nutra-cosmetic formulations either singly or as “cosmetic blends” with other carefully chosen natural plant actives.

The invention relates to an oil control composition, which is prepared from octanoyl glycine, nicotinamide, inositol, sophorolipid fermentation liquor and a laminaria saccharina extract. The oil control composition prepared from the nicotinamide, the inositol, the octanoyl glycine, the laminaria saccharina extract and the sophorolipid fermentation liquor adjusts oil secretion on the basis of moisture retention, and establishes a three-dimensional balance oil control technology aiming at inhibition for the activity of three target points, i.e., lipase, 5 alpha-reductase and sebum flow regulation.

This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

The invention provides a skin-protecting composition and cosmetics with oil-controlling and pore-shrinking effects. The composition is prepared from Chinese violet extract, rhizoma anemarrhenae extract and rheum officinale extract in a weight ratio of 4:2-4:1-5 based on traditional Chinese medicine raw materials Chinese violet, rhizoma anemarrhenae and rheum officinale. The composition can play a synergetic effect in inhibiting 5 alpha reductase, resisting inflammation, inhibiting grease secretion and shrinking pores, and can be applied to skin-protecting and washing cosmetics, so that a product has the effects of controlling oil and shrinking pores.

The invention relates to application of nymphaea hybrid or a product thereof, and specifically relates to application of nymphaea hybrid to improvement of prostate symptoms. Specifically, the invention discloses the application of a nymphaea hybrid or a product thereof to preparation of medicament or health care product for improving symptoms of prostate. Improvements of the symptoms of prostate involve treatment of prostatic hyperplasia or prevention of prostatitis; the nymphaea hybrid product is a nymphaea hybrid extract or a nymphaea hybrid wine; and the nymphaea hybrid refers to dried flower or fresh flower of nymphaea hybrid. The invention conducts systematic studies on effects of nymphaea hybrid and product thereof on prevention of 5 alpha-reductase related diseases, especially prevention of prostate hyperplasia; and results show that nymphaea hybrid and product thereof have obvious effects on 5 alpha-reductase activity inhibition and prostatic hyperplasia resistance.

The invention relates to a supercritical extraction pollen extractive as well as preparation and application thereof, wherein the extractive has high safety and 5 alpha-reductase inhibitory activity. The supercritical extraction pollen extractive is prepared by the following method: a pollen raw material is weighed, and is added in an extraction kettle; a lid of the extraction kettle is tightened; then the pollen raw material is extracted for 1-3 hours by a supercritical CO2 extraction instrument at the temperature of 30-60 DEG C under the pressure of 200-500 bar; and the supercritical extraction pollen extractive is collected after the extraction is finished; the pollen raw material is selected from papaver rhoeas, schisandra chinensis or corn. The method is adopted to obtain three supercritical extraction pollen extractives with better 5 alpha-reductase inhibitory activity; the source of raw materials is safe; the supercritical extraction process adopted by the method dose not relate to poisonous and harmful organic solvent; and prepared products have lower poison and side effects, have high safety, and bring convenience to develop subsequent health care foods.

An improved method for concentrating / enriching the polyphenolic contents from the dried, unripe fruit rinds of Terminalia belerica is disclosed. The present invention also discloses a light colored, enriched / concentrated (85%-100%) polyphenolic extract from the dried, unripe fruit rinds of Terminalia belerica which, by virtue of its excellent skin lightening, anti-aging, anti-inflammatory, anti-oxidant, UV protective, anti-microbial, sebum control, anti-acne and safety properties shows tremendous nutra-cosmetic potential as topical / oral “skin care” and “hair care” formulations. Additionally, the oral nutra-cosmetic formulations containing the light colored, enriched / concentrated (85%-100%), polyphenolic extract from the dried, unripe fruit rinds of Terminalia belerica, in view of their excellent 5-alpha-reductase activity, provide a natural therapeutic alternative to the problems of Benign prostatic hyperplasia (BPH), prostate cancer, and prostatitis.

The invention provides a method for improving hair biology, e.g., hair growth. The method comprises administering to a subject a monoamine oxidase inhibitor and a vasodilator, a zinc salt of a carboxylic acid, a xanthine compound, pyrithione or a salt thereof, saponin, tritapene, crataegolic acid, celastrol, asiatic acid, an inhibitor of 5-alpha-reductase, 1,4-methyl-4-azasteroid, an androgen receptor antagonist, azelaic acid or a derivate thereof, cyclosporin, triiodothyronine, diazoxide, retinoic acid, a prostaglandin analog, aminexil, carnitine tartrate, apigenin, procapil, or adenosine, in an amount effective to achieve a desired effect. The invention further provides a method of reducing or delaying the appearance of an age-related skin imperfection. The method comprises administering to the subject a composition comprising an MAO inhibitor. A kit for improving hair growth also is provided.

The invention discloses a plant stock solution having oil controlling and acne removing functions and a preparation method thereof. The plant stock solution is prepared from raw materials in percentage by weight as follows: 5%-10% of 1,3-propylene glycol, 1%-5% of glycerin, 3%-8% of plant extracts, 0.1%-1% of xanthan gum, 0.01%-0.1% of sodium hyaluronate, 0.2%-0.6% of phenoxyethanol, 0.05%-0.35% of ethylhexylglycerin and the balance of deionized water. A spiraea salicifolia extract can effectively inhibit activity of 5 alpha-reductase, inhibit secretion activity of skin glands and prevent excessive oil and acne, and a bacteriostatic component can inhibit bacteria forming acne. A lotus seed extract can effectively decompose pimple and acne and regulate oil secretion; a calendula extract has superhigh healing capacity, can calm skin and has red fading, relieving and repairing effects. The three extracts are used cooperatively to effectively control secretion of sebaceous gland, and the best use effect can be obtained.

The invention discloses novel endocrine treatment phytochemicals which affect androgenic status. The method for treatment of 5-alpha-reductase responsive diseases using four novel 5-alpha-reductase inhibitor compounds; leucoanthocyanidin, glabrene, glabridin, and alpha-terpineol is disclosed. Glabridin does not interfere with normal testosterone to androgen receptor binding.

The invention belongs to the field of food, and in particular relates to a composition with an effect of preventing alopecia and a preparation method thereof. The composition consists of a preparation for oral administration and a preparation for external application, wherein the preparation for oral administration is prepared from the following components: notoginsenoside, dodder extract, mulberry bark extract, medium-chain fatty acid glyceride, phospholipid, vitamin E and rapeseed oil; and the preparation for external application is prepared from the following components: peppermint oil, notoginsenoside, safflower extract, ginger extract, ethanol and water. The composition achieves the purposes of preventing and / or treating alopecia through inhibiting male hormone, strengthening functions of the hair follicles, moisturizing the scalp, inhibiting the activity of 5-alpha reductase and improving sebum secretion.

The invention discloses multiple-effect acne removing gelatin. Aqueous gelatin which is salubrious in skin sense is selected as a substrate, Chinese herbal medicine compounding liquid screened by a scientific method is added to be used as an acne removing functional composition, the DPPH. free radical suppression ratio, the hyaluronidase suppression ratio and the teststerone conversion ratio are determined, staphylococcus aureus restraining experiment is performed, and the acne removing efficacy of the product namely the multiple-effect acne removing gelatin is comprehensively evaluated in four respects of resisting oxidation, resisting inflammation, restraining the activity of 5 alpha-reductase and restraining bacteria. The acne removing gelatin disclosed by the invention is refreshing intexture, good in skin sense, free from fat, ethanol and essence, mild and non-irritating, has good effects of restraining bacteria, resisting inflammation and resisting oxidation, can alleviate skinfat secretion, can effectively relieve symptoms of acne, can alleviate the discomfort of acne patients, and can achieve the purpose of removing acne safely. The preparation method of the product namely the acne removing gelatin is simple, large-scale production is easy, and the acne removing gelatin has great market prospects.

The invention discloses a method for screening an acne-removing compound containing coptis chinensis, cortex phellodendri, radix scutellariae and rheum officinale. Based on a traditional acne-removingformula of rheum officinale, radix scutellariae and cortex phellodendri, traditional Chinese herbal medicinal aqueous extracts of coptis chinensis, cortex phellodendri, radix scutellariae and rheum officinale are selected as acne-removing effective ingredients, a four-factor three-level orthogonal testing method is adopted for compounding, the DPPH cleaning capability, hyaluronidase inhibitability, 5 alpha-reductase activity inhibitability and staphylococcus aureus inhibitability of each compound are analyzed by a modern testing method, and scientific analysis and comparison are performed from the four aspects to determine an optimized compounding proportion, and a scientific accordance is provided to the influence of dosage of four traditional Chinese herbal medicinal materials on the compound acne-removing effect. The coptis chinensis, cortex phellodendri, radix scutellariae and rheum officinale are natural materials, accord with the concept of safe skin protection of modern people,and have more advantages in application in comparison with acne-removing medicines and acne-removing cosmetics on the market. The method is modern application of an ancient formula and provides relatively good technical support to researches and development of compound acne-removing products containing coptis chinensis, cortex phellodendri, radix scutellariae and rheum officinale.

The invention provides a 5 alpha-reductase mutant. The 5 alpha-reductase mutant is obtained through site-specific mutation and reconstruction of 5 alpha-reductase, a genetic engineering bacterium of the 5 alpha-reductase mutant is constructed and applied to high-efficiency catalysis of 5 alpha-AD production, in the 5 alpha-reductase subjected to site-specific mutation and reconstruction, 187th tyrosine is mutated into phenylalanine, 5 alpha-reductase mutant recombinant plasmids are electrically transferred into mycobacterium neoaurum to be subjected to heterologous expression, then enzymatic activity and production efficiency are determined, the inventor finds that the enzyme activity of a mycobacterium neoaurum genetic engineering bacterium of the 5 alpha-reductase mutant is increased by2.3 times, the catalysis efficiency is improved by 22.8%, and the 5 alpha-AD production is increased to 1.78g / L from the original 1.45g / L; and when the 5 alpha-reductase mutant is used as a key enzymefor production of an important sterides medicine intermediate, the bioconversion efficiency and the yield of products can be obviously improved.

The invention relates to a medicine compound for preventing alopecia, in particular to a multiple-target-point traditional Chinese medicine compound for restraining the seborrhoeic alopecia. The traditional Chinese medicine compound is prepared from angelica extract, shrubby sophora extract, astragalus extract, scutellaria baicalensis extract, blackberry lily extract, stephania terandra extract, notopterygium root extract, garden sorrel extract, subprostrate sophora root extract and sophora fruit extract. Each type of extract accounts for 0.1-99.1% of the traditional Chinese medicine compound in weight. The traditional Chinese medicine compound can control the multiple target points of 5 alpha-reductase activity, AR expression, scalp hair microbial infection and the like at the same time and treat the seborrhoeic alopecia effectively, and is low in stimulation on the human body and low in toxicity.

The invention discloses a composition to prevent and treat hair loss, comprising Chinese herb 5-alpha reductase inhibitor, an antibacterial agent and a hair loss preventive, wherein the Chinese herb 5-alpha reductase inhibitor includes one or more of nutmeg extract, biochanin, root extract of red ginseng, and Cuscuta reflexa extract. After being applied to cosmetics, the composition enables the scalp to be healthier and effectively prevents and treats hair loss through the route of inhibiting and killing bacteria, inhibiting 5-alpha reductase and promoting hair growth.

The invention discloses a traditional Chinese medicinal anti-hair loss and hair growth liquid composition for men. The traditional Chinese medicinal anti-hair loss and hair growth liquid composition is prepared from the following traditional Chinese medicinal raw materials in parts by weight: 100-120 parts of white peony roots, 80-100 parts of semen cuscutae, 100-120 parts of moutan bark, 100-120 parts of red peony roots, 160-180 parts of rosemary leaves, 120-140 parts of melon leaves, 140-160 parts of poria with hostwood and 180-200 parts of mint leaves. The components are mixed by using 60% ethyl alcohol at the ratio of traditional Chinese medicines to the ethyl alcohol of 1:5, and are soaked at a room temperature for 5d; and a soak solution is filtered through a 200mesh stainless steel screen and then mixed to prepare a traditional Chinese medicinal anti-hair loss and hair growth liquid for the men. According to the traditional Chinese medicinal anti-hair loss and hair growth liquid for the men, the cutaneous penetration efficiency is improved through cooperation of inhibition 5-alpha-reductase and a plant penetration enhancer, the dihydrotestosterone level is reduced, the damage of male sex hormone to hair follicles is blocked, pathological cells are repaired, and meanwhile, oil secretion is balanced, the problems such as greasy hair, pruritus capitis and abnormal loss can be quickly solved and normal growth of the hair can be gradually restored.

Methods and systems are described for prediction of a patient's response to a drug for treating androgenetic skin disorders such as alopecia, acne, and hirsutism. For a given drug such as anti-androgens and 5-alpha-reductase inhibitors, and a given dosage, the likely responsiveness of that drug and dosage may be determined, for example, by generating a set of patient scores based on a patient profile, including genetic sample information, and comparing that scores to a set of reference information.

The invention provides a crocus sativus extract-containing hair loss preventing and nourishing essence spray and a preparation method thereof. The crocus sativus extract-containing hair loss preventing and nourishing essence spray is composed of 12 Chinese herbal components achieving different hair nourishing effects to comprehensively solve existing common hair problems. Also, the crocus sativusextract-containing hair loss preventing and nourishing essence spray can inhibit 5 alpha-reductase, protect hair follicles, achieve bacteriostatic and antipruritic effects, prevent hair loss, restore,care and smooth hair, improve scalp microcirculation and meanwhile achieve antagonism against AR (androgen) receptors. The crocus sativus extract-containing hair loss preventing and nourishing essence spray achieves bacteriostatic effects through the plant bacteriostatic agent of Leucidal liquid SF, which is mild and non-irritating and meanwhile achieve scalp moisturizing effects. Besides, as a spray, the crocus sativus extract-containing hair loss preventing and nourishing essence spray is convenient to use and saves washing and accordingly can provide the scalp with nutrients for a long term.

This invention provides for combinations of 5 alpha reductase inhibitors and SERMs. These combinations are useful in: 1) preventing prostate carcinogenesis in a subject;2) preventing the recurrence of, suppressing, inhibiting or reducing the incidence of prostate carcinogenesis in a subject; 3) treating a subject with prostate cancer; 4) suppressing, inhibiting or reducing the incidence of prostate cancer in a subject; 5) treating a subject with pre-malignant lesions of prostate cancer; 6) suppressing, inhibiting or reducing the incidence of pre-malignant lesions of prostate cancer in a subject; 7) reducing the incidence, inhibiting, suppressing, preventing and / or treating androgen-deprivation induced conditions in men suffering from prostate cancer, such as androgen-deprivation induced osteoporosis, bone fractures, loss of bone mineral density (BMD), hot flashes and / or gynecomastia.; and 8) treating polycystic ovarian syndrome and reducing the incidence, inhibiting, suppressing, preventing and / or treating diabetes, cardiovascular disease, breast cancer and endometrial cancer in women suffering from polycystic ovarian syndrome.