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(12) Patent Application Publication (10) Pub. No.: US 2008/0261896 A1 Tanaka Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2008/0261896 A1 Tanaka Et Al US 20080261896A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2008/0261896 A1 Tanaka et al. (43) Pub. Date: Oct. 23, 2008 (54) TESTOSTERONE GENERATING AND Publication Classification METABOLIZING ENHANCER (51) Int. Cl. (75) Inventors: Junji Tanaka, Aichi-pref (JP); A63L/70 (2006.01) Hiroshi Shi-Moda, Aichi-pref (JP); A6IP3/00 (2006.01) Shao-Jie Shan, Aichi-pref (JP); (52) U.S. Cl. .......................................................... S14/25 Hiromichi Murai, Aichi-pref (JP) (57) ABSTRACT Correspondence Address: A testosterone generating and metabolizing enhancer is pro BACON & THOMAS, PLLC posed in the invention, which increases concentrations of 625 SLATERS LANE, FOURTH FLOOR testosterone in both seminal vesicle and bloodstream, and ALEXANDRIA, VA 22314-1176 (US) may further promote the gene expression of metabolizing testosterone into 5C.-reductase of dihydrotestosterone. The (73) Assignee: Sinphar Pharmaceutical Co., testosterone generating and metabolizing enhancer of the Ltd., I Lan (TW) invention is characterized in that an effective component (21) Appl. No.: 12/081,147 thereof may be phenylethanoid glycosides; said phenyletha noid glycosides may comprise at least one of echinacoside (22) Filed: Apr. 11, 2008 and acteoside, or may comprise both echinacoside and acteo side, more preferably. The testosterone generating and (30) Foreign Application Priority Data metabolizing enhancer of the invention may be applied in medicines, Substances for external uses on skin, and foods Apr. 11, 2007 (JP) ................................. 2007-103561 and beverages for mammals (including humans); as well as an May 12, 2007 (JP) ................................. 2007-127458 animal feed for mammals. Patent Application Publication Oct. 23, 2008 Sheet 1 of 4 US 2008/0261896 A1 &&&&&&&&&&&&&&&&&& aaaaaaaaaaaaaaaaaaaaaaaaassessssssssssssss v.v.a. assassasssssssssssssssss'ssssssssss Patent Application Publication Oct. 23, 2008 Sheet 2 of 4 US 2008/0261896 A1 (400 mg/kg) Fig. 3 couº&un (400 mg/kg) Fig. 4 Patent Application Publication Oct. 23, 2008 Sheet 3 of 4 US 2008/0261896 A1 5a-reductase 4. 2 Control Extract of C. tubulosa (400 mg/kg) Fig. 5 Patent Application Publication Oct. 23, 2008 Sheet 4 of 4 US 2008/0261896 A1 9(31H audioisoisºmoipá?aisos US 2008/0261896 A1 Oct. 23, 2008 TESTOSTERONE GENERATING AND enhancer, which may enhance the gene expression of test METABOLIZING ENHANCER osterone generation, and consequently increase testosterone concentration in the seminal vesicle and the bloodstream. FIELD OF THE INVENTION Additionally, another objective of the invention is to propose 0001. The invention relates to a testosterone generating a testosterone metabolizing enhancer, which may enhance the and metabolizing enhancer having novel components, and gene expression of 5C-reductase (which allows testosterone more particularly to a testosterone generating and metaboliz to be metabolized into dihydrotestosterone), thereby promot ingenhancer that may be applied in medicines, Substances for ing the metabolism of testosterone into dihydrotestosterone. external uses on skin, and foods for mammals including humans. Means for Solving the Problems 0010. In order to solve the aforesaid problems, the inven DESCRIPTION OF PRIOR ART tion proposes: 0002 Traditionally, it has been known that fresh stems of 0011 (1) A testosterone generating enhancer comprising herbs of the Cistanche family are effective for treating infer phenylethanoid glycosides as effective components. tility, impotence, and constipation (please refer to Patent Cita 0012 (2) The testosterone generating enhancer of (1), tion 1). Moreover, preparations made from the fresh stems of characterized in that said phenylethanoid glycosides of the the perennial herbs may be used to nutritionally Supplement testosterone generating enhancer comprise at least one of the bloodstream and the kidneys. These perennial herbs have echinacoside and acteoside. been widely cultivated in the northwestern region of China, 0013 (3) The testosterone generating enhancer of (2), and are known as 'ginseng from the deserts'. Among the characterized in that said phenylethanoid glycosides of the cultivated herbs of the Cistanche family, the holoparasitic testosterone generating enhancer comprise both echinaco herb Cistanche tubulosa (Schrenk.) Wight is the most widely side and acteoside. cultivated. 0014 (4) A testosterone generating enhancer comprising 0003 Previously, Japanese researchers have systemati extracts from plants of the Cistanche family as effective cally studied the chemical compositions and pharmaceutical components. properties of the herbs of the Cistanche family, and found that 00.15 (5) The testosterone generating enhancer of (4), phenylethanoid glycosides are the main active components of characterized in that said extracts comprise phenyletha these perennial herbs (for example, refer to Non-patent Cita noid glycosides as effective components. tion 1-3). The active components may serve as effective anti 0016 (6) The testosterone generating enhancer of (5), oxidants, metabolizing enhancers, memory enhancers, and characterized in that said phenylethanoid glycosides of the sexual drive enhancers. Many researchers have further stud extracts comprise at least one of echinacoside and acteo ied the medicinal properties of phenylethanoid glycosides. side. 0004 Patent Citation 1: Japanese Publication Number 0017 (7) The testosterone generating enhancer of (6), 2004-250449 characterized in that said phenylethanoid glycosides of the 0005. Non-patent Citation 1: Sato T, et al. Yakugaku extracts comprise both echinacoside and acteoside. Zasshi, 1985, 105(12): 1131 0018 (8) A testosterone metabolizing enhancer compris 0006 Non-patent Citation 2: Jimenez, C., et al. Nat. Prod. ing phenylethanoid glycosides as effective components. Rep., 1994, 11 (6): 591 0019 (9) The testosterone metabolizing enhancer of (8), 0007 Non-patent Citation 3: Cometa F., et al. Fitoterapia, characterized in that said phenylethanoid glycosides of the 1993, 64 (3): 195 testosterone metabolizing enhancer comprise at least one 0008. Non-patent Citation 4: Deng Min et al. Acta Phar of echinacoside and acteoside. macoeSin, 2004, 25(10): 1276-128 0020 (10) The testosterone metabolizing enhancer of (9), characterized in that said phenylethanoid glycosides of the SUMMARY OF THE INVENTION testosterone metabolizing enhancer comprise both echina coside and acteoside. Problems to be Solved 0021 (11) A testosterone metabolizing enhancer compris 0009 Basing on the aforesaid studies, the inventor of the ing extracts from plants of the Cistanche family as effective invention had carried out relevant tests, in which rats were fed components. phenylethanoid glycosides and extracts from herbs of the 0022 (12) The testosterone metabolizing enhancer of Cistanche family comprising phenylethanoid glycosides, and (11), characterized in that said extracts comprise phenyle the resulted showed that testosterone concentration in the thanoid glycosides as effective components. seminal vesicles of the rats was increased. In addition, it was 0023 (13) The testosterone metabolizing enhancer of found that after feeding mice the aforesaid Substances, test (12), characterized in that said phenylethanoid glycosides osterone concentration in the bloodstream of the mice was of the extracts comprise at least one of echinacoside and also increased, which indicated that phenylethanoid glyco acteoside. sides and extracts from herbs of the Cistanche family com 0024 (14) The testosterone metabolizing enhancer of prising phenylethanoid glycosides may promote the gene (13), characterized in that said phenylethanoid glycosides expression of turning cholesterol into the enzymes of test of the extracts comprise both echinacoside and acteoside. osterone, as well as promoting the gene expression of synthe 0025 (15) A medicine applicable to mammals including sizing 5C-reductase (which allows testosterone to be metabo humans, and the medicine may comprise any of the test lized into dihydrotestosterone); the results formed the basis osterone generating enhancers described in (1) to (7), or for the present invention. In other words, a major objective of any of the testosterone metabolizing enhancers described the invention is to propose a testosterone generating in (8) to (14) as effective components. US 2008/0261896 A1 Oct. 23, 2008 0026 (16) A substance for external uses on skin applicable to mammals including humans, and the Substance for external uses on skin may comprise any of the testosterone Formula (1) generating enhancers described in (1) to (7), or any of the testosterone metabolizing enhancers described in (8) to (14) as effective components. 0027 (17) A food or beverage, and the food or beverage may comprise any of the testosterone generating enhancers described in (1) to (7), or any of the testosterone metabo lizing enhancers described in (8) to (14) as effective com ponents. 0028 (18) An animal feed for mammals, which may com prise any of the testosterone generating enhancers 0037. The phenylethanoid glycosides are not limited to the described in (1) to (7), or any of the testosterone metabo aforesaid scope, and may also include components like lizing enhancers described in (8) to (14) as effective com echinacoside, acteoside, 2'-acetylacteoside, campneoside I. ponents. campneoside II, cistantubuloside A, cistantubuloside B1, cistantubuloside B2, cistantubuloside C1, cistantubuloside DESCRIPTION OF THE ACCOMPANYING C2, crenatoside, decaffeoylacteoside,
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