郭綜合醫院蘇士銘醫師 1

淫羊藿 一 名稱二 來源三 生產地四 性味五 活性成分或主要化學成分六 傳統用途七 中醫藥用途八 藥理作用九 用法及劑量十 不良反應、副作用及注意事項 參考

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名稱 拉丁名稱 : Herbra Epimedii 英文名稱 : Epimedium 拉丁學名 : Epimedium brevicornum Maxim 中文名稱 : 仙靈脾 / 淫羊藿 漢語拼音 : Xian Ling Pi/ Yin Yang Huo

來源為小蘗科植物箭葉淫羊藿或淫羊藿等的枝葉。 [1]

生產地 差不多分佈在中國各地，主要生長在高山地帶。 [2]

性味 性溫、味甘甜 [1]

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活性成分或主要化學成分 [3]

淫羊藿 苯 葉麻酸 鞣酸油酸 維生素 E棕櫚酸 黃酮固醇

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傳統用途 由於其益氣靜心功效，淫羊藿常被用來舒緩壓力及疲勞。中國民間醫師常以紅酒加入淫羊藿 (100g-200g ，臨床劑量 10 倍 ) 和烏賊煎劑來治療因負擔過度而導致的疲勞及體弱。 [5]

淫羊藿能治療疲勞及心神恍惚的機制是給腦部供應足夠血液。 [6]

淫羊藿是春藥酒常含的成分之一，淫羊藿葉煎劑作春藥用途更是歷史由久。

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中醫藥用途 1

.補腎、壯陽及補氣。

2.治腎陽虛所致的陽痿、肝硬化、遺精、遺尿、尿頻、

腰膝痠痛、不孕等。 3

.歸肝、腎經。

4.

健筋骨、袪風濕：治療風濕痹痛、四肢麻木或拘攣，風濕所致筋骨痿年次，小兒麻痹。

5.袪痰止咳平喘：治久咳、哮喘( 包括老年哮喘 ) ，以陽

虛者為宜。 6

.還常用於治療冠心病、高血壓、神經衰弱等。

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【概述】本品又名仙靈脾、羊藿、羊角風、羊藿葉。微小檗科植物淫羊藿 Epimedium brevicornum Maxim. 箭葉淫羊藿 Epimedium sagittatum （ Sieb. et Zucc. ） Maxim. 柔毛淫羊藿 Epimedium pubescens Maxim. 巫山淫羊藿 Epimedium wushanese T. S. Ying 或朝鮮淫羊藿 Epimedium koreanum Nakai 的地上部分。主產於陜西、遼寧、山西、湖北、四川等地。夏、秋季採收，割取莖葉，除去粗梗及雜質，曬乾或陰乾。淫羊藿為小檗科植物淫羊藿、箭葉淫羊藿、柔毛淫羊藿或朝鮮淫羊藿的乾燥地上部分。功能補腎陽、強筋骨、袪風濕。用於陽痿遺精、痿軟、風濕、痹痛、麻木拘攣，更年期高血壓等症。臨床應用一般需經淨制、切制、羊脂油炙後入藥。現代研究結果表明，本品主含淫羊藿 苷、藿羊淫次苷、藿羊淫新苷、蜡醇、三 十一烷、植物甾醇、有機酸、脂肪酸、生物鹼、揮發油等成分。具有增強內分泌系統的分泌功能、激素樣作用、促進蛋白質合成、調節細胞代謝、增強免疫功能、抗衰老、抗心肌缺氧、降壓、抗血小板聚集、抗炎、抗菌、抗病毒、袪痰、鎮咳、降糖及性激素樣作用等藥理作用。

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【藥性】味辛、甘，性溫。歸肝、腎經。 【功效】補腎壯陽，強筋健骨，袪風除濕。【應用】 1. 用於腎陽虛衰所致的陽痿遺精，宮寒不孕，尿頻失禁，久咳虛喘。治陽痿、遺精，可單味浸酒服，或配肉蓯蓉、巴戟天、仙茅等同用；治虛冷不孕，可配蛇床子、鎖陽等同用；治尿頻失禁，或小便餘瀝不盡，多配覆盆子、金櫻子、桑螵蛸等同用；治腎虛喘咳，多配補骨脂、胡桃肉等同用 (5) 。 2. 用於風寒濕痹，腰膝酸軟。治風濕久痹，腰膝冷痛，可浸酒飲；或配威靈仙、肉桂等煎服。如肝腎虧虛而致腰膝酸軟，常配杜仲、狗脊等同用。此外，可治虛寒胃痛，常配高良薑同用 (5) 。

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3 . 淫羊藿可以促進骨細胞增生和分化，降低骨質疏鬆症的發生率 (6,7,8,9,10,14) 。促進鈣質小腸吸收 (12) 。 4 . 淫羊藿萃取物可以放鬆兔子海綿體的肌肉，未來可以應用此策略而用來治療陰莖勃起障礙 (11) 。 5 . 淫羊藿萃取物可以使雄性大白鼠陰莖勃起 (13) 。【用法用量】內服：煎湯， 3 -9g ；或入丸、散；或浸酒、鰲膏 (4,5) 。 【使用注意】陰虛而相火易動者禁服 (4,5) 。

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Reference:

1 . 呂俠卿，中藥鑑別大全（ 2002 ），中華人民共和國湖南科學技術出版社。 (Simple Chinese)

2 . 江蘇新醫學院，中藥大辭典（ 1999 ），上海科學技術出版社。 (Simple Chinese)

3 . 張繼、陳德昌、林惠蓉、張文光，中國中藥材真偽鑑別圖典（ 1 ）（ 2004 ），廣東科技出版社（ Simple Chinese ）

4 . 中華人民共和國國家藥典委員會，中華人民共和國藥典ㄧ部 (2005) ，化學工業出版社 (Simple Chinese)

5 . 原思通，醫用中藥飲片學（ 2001 ），中華人民共和國人民衛生出版社。 (Simple Chinese)

6 . Meng FH , Li YB , Xiong ZL , Jiang ZM , Li FM .(2005) Osteoblastic proliferative activity of Epimedium brevicornum Maxim. Phytomedicine. 2005 Mar;12(3):189-93.

7 . Yin XX , Chen ZQ , Dang GT , Ma QJ , Liu ZJ .(2005) Effects of Epimedium pubescens icariine on proliferation and differentiation of human osteoblasts. Zhongguo Zhong Yao Za Zhi. 2005 Feb;30(4):289-91.

8 . Chen KM , Ge BF , Ma HP , Zheng RL .(2004) The serum of rats administered flavonoid extract from Epimedium sagittatum but not the extract itself enhances the development of rat calvarial osteoblast-like cells in vitro. Pharmazie. 2004 Jan;59(1):61-4.

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Reference: 9 . Li J , Yu S , Li T , Pang S .(2002) In vitro study of the effects of Epimedium on oste

oclastic bone resorption in various oral mineralized tissues. Zhonghua Kou Qiang Yi Xue Za Zhi. 2002 Sep;37(5):391-4.

10 . Jiang YN , Mo HY , Chen JM .(2002) Effects of epimedium total flavonoids phytosomes on preventing and treating bone-loss of ovariectomized rats. Zhongguo Zhong Yao Za Zhi. 2002 Mar;27(3):221-4.

11 . Chiu JH, Chen KK, Chien TM, Chiou WF, Chen CC, Wang JY, Lui WY, Wu CW.(2006) Epimedium brevicornum Maxim extract relaxes rabbit corpus cavernosum through multitargets on nitric oxide/cyclic guanosine monophosphate signaling pathway. Int J Impot Res. 2006 Jul-Aug;18(4):335-42. Epub 2006 Jan 5.

12 . Zhang G, Qin L, Hung WY, Shi YY, Leung PC, Yeung HY, Leung KS.(2006) Flavonoids derived from herbal Epimedium Brevicornum Maxim prevent OVX-induced osteoporosis in rats independent of its enhancement in intestinal calcium absorption.Bone. 2006 Jun;38(6):818-25. Epub 2006 Jan 18.

 13 . Chen KK, Chiu JH.(2006) Effect of Epimedium brevicornum Maxim extract on elicitation of penile erection in the rat.Urology. 2006 Mar;67(3):631-5.

14 . Zhang G, Qin L, Hung WY, Shi YY, Leung PC, Yeung HY, Leung KS.(2006) Flavonoids derived from herbal Epimedium brevicornum Maxim prevent OVX-induced osteoporosis in rats independent of its enhancement in intestinal calcium absorption.Bone. 2006 Jun;38(6):818-25.

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藥理作用 1. 對性功能的影響  動物實驗 增加小鼠性器官體積及血睪丸酮含量 雄性小鼠給淫羊藿提取物或煎劑後，前列腺、精囊和提肛肌的重量增加 [7] ，

血漿睪丸酮含量升高、睪丸組織增生、睪丸分泌增加。 [8] 淫羊藿 能促進睪丸間質細胞睪丸酮的基礎分泌和 cAMP 的

生成。 [9] 雌性大鼠給淫羊藿煎劑後，垂體前葉、卵巢和子宮的重量明顯增加，卵巢 HCG/LH 受體特異結合力明顯提高。 [10]   臨床研究 改善陽痿 用淫羊藿及菟絲子治療陽痿 52 例，配合按摩及煎水坐浴，總有效率為 92% 。 [11-12]用一配方含淫羊藿、枸杞子、冬蟲夏草、白芍和懷牛膝治療療陽痿 28例，總有效率為 86% 。 [13]

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藥理作用 1. 對性功能的影響

恢復男子性功能 用淫羊藿、仙茅、刺五加治療男子性功能下降 32例，顯效 21例，改善 7例。 [14] 

減低外陰白斑的症狀 取淫羊藿研末，以魚肝油軟膏適量調勻，塗於患處，患者療效顯著。 [15] 

改善經間出血 用淫羊藿治療 12例，每例療效均滿意。 [16]

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2. 對心血管系統的影響

動物實驗 增強心肌收縮力體外及體內實驗証明，淫羊藿煎劑能增加蟾蜍心肌細胞收縮力。用戊巴比妥鈉造成蟾蜍人工心衰後，注入淫羊藿煎劑，可使心肌張恢復。家兔靜脈注射淫羊藿煎劑，心肌張力增加。 [17]    增加心輸出量 家兔靜脈注射淫羊藿煎膏 ( 1g 生藥 /kg) 或淫羊藿 (1mg/kg) ，前者心輸出量增加，後者心輸出量下降。 [18]    增加冠脈流量淫羊藿煎劑及淫羊藿提取物分別對離體豚鼠及家兔心冠脈流量有增加作用。 [19-20] 麻醉犬靜脈注射淫羊藿水浸膏片中提取的非氨基酸或淫羊藿水溶液，可使冠脈流量明顯增加。 [21-22〕淫羊藿注射劑亦能增加豚鼠冠脈流量，對抗垂體後葉素所致的冠脈流量減少。 [23]   心肌缺血的保護作用淫羊藿煎劑、淫羊藿水溶液及淫羊藿非氨基酸提取物對大鼠心肌缺血均有保護作用。 [21,22,24]   降血壓淫羊藿煎劑給家兔、大鼠及貓靜脈注射，均呈降壓作用。 [7] 腎型高血壓大鼠灌服淫羊藿提取物，血壓明顯下降，但停藥後血壓回升。 [25]    

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2. 對心血管系統的影響

促進血小板聚集離體及在體實驗証明，淫羊藿煎劑及淫羊藿多糖可促進血小板聚集及降低紅血細胞壓積。 [26] 降膽固醇及甘油三脂實驗性高脂血症家兔灌胃淫羊藿煎劑， β- 脂蛋白、總膽固醇及甘油三脂水平下降。 [27]   

臨床研究 減輕心絞痛症狀在兩項獨立的臨床研究中，冠心病患者分別經過淫羊藿片及淫羊藿浸膏片治療後，大部分患者心電圖有明顯改善，心絞痛情況也得到改善。 [28-29]在另一項臨床研究，冠心病患者給肌肉注射淫羊藿注射液，患者心電圖得到改善，大部份有心絞痛、胸悶、心悸和氣短者，情況得到一定改善。[30]   高血壓者血壓用淫羊藿浸膏片治療高血壓 115例，有效率達 78% ，血壓下降幅度為 10.7kPa/5.33kPa (80/40mm Hg) 。 [31]

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3. 對免疫系統的影響

提高 / 恢復巨噬紅胞吞噬功能小鼠皮下注射淫羊藿多糖或淫羊藿黃酮，使巨噬細胞吞噬率提高。 [33]對抗淋巴細胞血清造成的免疫功能低下小鼠，淫羊藿能使其巨噬細胞吞噬炭粒的能力恢復到正常水平。 [36]   刺激 IL-2 產生淫羊藿多糖在較低濃度時 (100μg/ml and 1000μg/ml) ，可增強人體淋巴細胞產生的 IL-2 的活性。相反，在較高濃度時 (2500μg/ml and 5000μg/ml) ，淫羊藿多糖對 IL-2 的產生有抑制作用。 [37]   增加骨髓細胞的 DNA 生成及細胞繁殖淫羊藿煎劑能顯著提高陽虛小鼠骨髓細胞的繁殖 (72%) 及 DNA 生成。 [25]   

臨床研究 減輕白細胞減少症的症狀 有氣虛症狀的白細胞減少症患者 22例，服用淫羊藿沖劑 (15g/包 ) ，第 1週每日 3包，第 2週起每日 2包，共治療 30-45日， 22例中堅持服藥者 14例，其中治癒 3例，有效 5例，無效 2例。 [38]   改善維持性血液透析患者生存質量用淫羊藿對透析患者進行治療 4個月，患者感染發生率有下降趨勢，外周血淋巴細胞個素 2 的活性明顯增強，體力、睡眠、食欲和男性患者的性功能有所改善。 [39]

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3. 對免疫系統的影響 動物實驗 增加抗體生成 小鼠皮下注射淫羊藿總黃酮、淫羊藿多糖及淫羊藿 ，可使綿羊紅細胞 (SRBC) 和免疫小鼠血溶血素抗體水平或脾臟抗體生成增加。 [32-34]   調節淋巴細胞的繁殖小鼠分別皮下注射淫羊藿總黃酮或淫羊藿多糖，每日一次，連續給藥七日，均可顯著促進淋巴細胞轉化。 [32-33]淫羊藿多糖能使小鼠淋巴細胞對植物血凝素 (PHA)刺激增加。 [32]50% 淫羊藿乙醇提取液可明顯抑制絲分裂原誘發的小鼠淋巴細胞增生反應。其抑制反應隨藥物濃度增加而加強。給環璘酸洗胺超適劑量免疫小鼠皮下注射淫羊藿多糖，可促進超適劑量環璘胺誘導的 Ts 細胞產生，增強對受體鼠抗體生成的抑制。相反，當環璘胺超適劑免疫小鼠皮下注射淫羊藿 ， Ts 細胞產生減弱，使受體鼠抗體生成水平升高。 [34]給醋酸強的松龍造成陽虛模型的小鼠灌胃淫羊藿煎劑，可明顯增加淋巴細胞的 3H-TdR 摻入及轉化，紅細胞溶血素及血凝抗體滴度。 [35]給抗淋巴細胞血清造成的免疫功能低下小鼠灌胃淫羊藿煎劑，可使免疫功能低下小鼠脾臟淋巴細胞數量、脾空斑形成細胞反應恢復到正常水平。[36]  

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4. 對呼吸系統的影響

動物實驗 抗哮喘作用一項用貓作模型的實驗發現，淫羊藿提取物能完全抑制由電流刺激回歸喉神經而引起的咳嗽。在另一項以豚鼠作實驗模型的研究顯示，淫羊藿能舒緩組胺引導的哮喘。 [25]   

臨床研究 治療慢性氣管炎用單味淫羊藿丸治療 1066例，總有效率為 74.6% 。 [40]

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5. 抗病毒作用 動物實驗 抗菌及抗毒作淫羊藿對白色葡萄球菌、金黃色葡萄球菌、奈氏卡他球菌、肺炎雙球菌、流感嗜血桿菌、脊髓灰白質炎病毒、 ECHO 病毒 6 、 9型及柯薩奇病毒 A9 、 B4 、B5 型等均有抑制作用。 [7,25,41]   

臨床研究 對治療病毒性心肌炎較維生素Ｃ有效用淫羊藿浸膏片，每次 7-10片，每日 3 次，同時用維生素 C3g 加入 10%葡萄糖溶液 500ml內靜脈滴注，共治療 36例，與單用維生素 C 治療的 25例比較，前者顯效率為 69.44% ，後者為 40% 。 [43]

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6. 其他6. 其他 在動物中的抗氧化作用淫羊藿水提液對大鼠心、肝、腦和腎勻漿過氧化脂質的生成有顯著的抑制作用。 [44]給急性衰老小鼠模型灌胃淫羊藿黃酮，能顯著恢復小鼠 T 和 B淋巴細胞增殖反應，明顯提高小鼠肝臟總超氧化物歧化下霨 (SOD)的活性，減少肝組織過氧化脂質的形成，減少心、肝等組織的脂褐素形成。 [45] 其他研究顯示，淫羊藿具兒茶酚胺抗拮作用。 在動物中的降血糖作用正常大鼠或實驗性高血糖大鼠灌胃淫羊藿提取物，有降血糖作用。[25,46]   配合其他中藥去治療神經衰弱分別用 3% 淫羊藿煎劑離子透入法、淫羊藿提取物、淫羊藿黃酮及淫羊藿治療 104 、 138 、 61 及 29例，總有效率為 85.6%, 89.9%, 93.4% 及 89.6% ，患者的失眠情況也有改善。 [47-48]

郭綜合醫院蘇士銘醫師 22

用法及劑量用法及劑量 煎劑： 6-15g ，可一次增至。 [4]

不良反應、副作用及注意事項 若長期服用，可導致頭暈、嘔吐、口乾、口渴及、流鼻血等不良反應。小鼠被灌服大劑量時可引起呼吸停止及反射亢進，甚至痙攣。 [49]

陰虛內熱者不適合服食淫羊藿。 [50]

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參考資料1.A pharmaco-metabonomic study on the therapeutic basis and metabolic effects of Epimedium brevicornum Maxim. on hydrocortisone-induced rat using UPLC-MS. (eng; includes abstract) By Li F, Biomedical Chromatography: BMC [Biomed Chromatogr], 2007 Apr; Vol. 21 (4), pp. 397-405; 2.Effects of icariin on hypothalamic-pituitary-adrenal axis action and cytokine levels in stressed Sprague-Dawley rats. (eng; includes abstract) By Pan Y, Biological & Pharmaceutical Bulletin [Biol Pharm Bull], 2006 Dec; Vol. 29 (12), pp. 2399-403;3.Epimedium brevicornum Maxim extract relaxes rabbit corpus cavernosum through multitargets on nitric oxide/cyclic guanosine monophosphate signaling pathway. (eng; includes abstract) By Chiu JH, International Journal Of Impotence Research [Int J Impot Res], 2006 Jul-Aug; Vol. 18 (4), pp. 335-42; 4.Flavonoids derived from herbal Epimedium Brevicornum Maxim prevent OVX-induced osteoporosis in rats independent of its enhancement in intestinal calcium absorption. (eng; includes abstract) By Zhang G, Bone [Bone], 2006 Jun; Vol. 38 (6), pp. 818-25; PMID: 164138405.Effect of Epimedium brevicornum Maxim extract on elicitation of penile erection in the rat. (eng; includes abstract) By Chen KK, Urology [Urology], 2006 Mar; Vol. 67 (3), pp. 631-5;

郭綜合醫院蘇士銘醫師 24

參考資料6.Osteoblastic proliferative activity of Epimedium brevicornum Maxim. (eng; includes abstract) By Meng FH, Phytomedicine: International Journal Of Phytotherapy And Phytopharmacology [Phytomedicine], 2005 Mar; Vol. 12 (3), pp. 189-93; 7.On-line concentration by field-enhanced sample injection with reverse migrating micelles in micellar electrokinetic capillary chromatography for the analysis of flavonoids in Epimedium brevicornum Maxim. (eng; includes abstract) By Wang S, Journal Of Chromatography. A [J Chromatogr A], 2003 Oct 31; Vol. 1017 (1-2), pp. 27-34;8.Effects of herbal preparation Equiguard on hormone-responsive and hormone-refractory prostate carcinoma cells: mechanistic studies. (eng; includes abstract) By Hsieh TC, International Journal Of Oncology [Int J Oncol], 2002 Apr; Vol. 20 (4), pp. 681-9;9.[Chemical constituents from the aerial part of Epimedium brevicornum Maxim.] (chi; includes abstract) By Gao B, Zhongguo Zhong Yao Za Zhi = Zhongguo Zhongyao Zazhi = China Journal Of Chinese Materia Medica [Zhongguo Zhong Yao Za Zhi], 1996 May; Vol. 21 (5), pp. 290-2, 319; 10.[Determination of the content of icariine in four Chinese patent medicines containing Epimedium brevicornum Maxim] (chi; includes abstract) By Li Z, Hua Xi Yi Ke Da Xue Xue Bao = Journal Of West China University Of Medical Sciences = Huaxi Yike Daxue Xuebao / [Bian Ji Zhe, Hua Xi Yi Ke Da Xue Xue Bao Bian Wei Hui] [Hua Xi Yi Ke Da Xue Xue Bao], 1995 Mar; Vol. 26 (1), pp. 66-9;11.Determination of total flavonoids in Epimedium brevicornum maxim by differential pulse polarography. (eng; includes abstract) By Xu LX, Yao Xue Xue Bao = Acta Pharmaceutica Sinica [Yao Xue Xue Bao], 1989; Vol. 24 (8), pp. 606-10;

郭綜合醫院蘇士銘醫師 25

A pharmaco-metabonomic study on the therapeutic basis and metabolic effects of Epimedium brevicornum Maxim. on hydrocortisone-induced rat using UPLC-MS

Li F; Lu X; Liu H; Liu M; Xiong [Biomed Chromatogr] 2007 Apr; Vol. 21 (4), pp. 397-405.

Epimedium brevicornum Maxim. (EbM)treated rats with a pathologic condition similar to the 'kidney deficiency syndromes' in traditional Chinese medicine and its therapeutic basis. UPLC-MS technique was used for the development of chemical profile of EbM. and endogenous metabolite profiles of rats pre- and post-hydrocortisone interfered and treated with this herbal medicine. The comparison among profiles was performed with a statistical technique, principle component analysis (PCA). Significant difference in endogenous metabolite profiles was observed in the intervention rats and the abnormality of metabolism recovered towards the normal level after administration withEbM extract. Four active constituents of. were found into the blood circulation of kidney-deficient rats and two of their metabolites in the urine. This work suggests that the metabonomic approach is a potentially powerful tool to explore the therapeutic basis and to clarify the possible action mechanism of traditional Chinese medicine.

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Effects of icariin on hypothalamic-pituitary-adrenal axis action and cytokine levels in stressed Sprague-Dawley rats.

Pan Y; Zhang WY; Xia X; Kong [Biol Pharm Bull] 2006; 29 (12), 2399-403.

Icariin is one of the major active flavonoids constituents of Epimedium brevicornum MAXIM (Berberidaceae). Icariin and E. brevicornum have a wide range of pharmacological activities. Abnormality in the hypothalamic-pituitary-adrenal (HPA) axis is considered to be a key neurobilogical factor in major depression, and cytokines have a close relationship with the activation of the HPA axis. In the present study, the aim was to determine whether icariin possesses an antidepressant-like activity, and to explore the effects of icariin on the HPA axis and cytokine levels in chronic mild stress (CMS) model of depression in Sprague-Dawley rats. Icariin significantly increased the sucros

e intake of CMS-treated rats from week 3. 不但增加 (CRF) and cortisol 而且降低 IL-6 and TNF-alpha It not only attenuated the CMS-induced increases in serum corticotropin-releasing factor (CRF) and cortisol levels, but also reversed the abnormal levels of serum interleukin-6 (IL-6) and tumor-necrosis-factor alpha (TNF-alpha) to the normal in the stressed rats. These results suggested that icariin possessed an antidepressant-like property that was at least in part mediated by neuroendocrine and immune systems.

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Epimedium brevicornum Maxim extract relaxes rabbit corpus cavernosum through multitargets on nitric oxide/cyclic guanosine monophosphate signaling pathway.

邱文慧 Chiu JH; Chen KK; Chien TM; Chiou WF; Chen CC; Wang JY; Lui WY; Wu.

[Int J Impot Res] 2006 Jul-Aug; Vol. 18 (4), pp. 335-42.

Epimedium brevicornum Maxim (EbM) has been reputed to have sexual stimulation effects on males. The study is aimed to test the hypothesis that EbM extracts relaxed the corpus cavernosum (CC) smooth muscle through activation of multitargets on nitric oxide (NO)/cyclic guanosine monophosphate (cGMP) signaling pathway. Water extract of EbM and its subfraction (EP-20) were prepared and standardized by high-performance liquid chromatography. Isolated rabbit CC strips were mounted in organ baths and isometric tension was recorded in the presence or absence of specific inhibitors related to NO/cGMP signaling such as L-N(G)-nitro-arginine methyl ester (L-NAME), 1H-[1,2,4]oxadiazolo-[4,3-a] quinoxalin-1-one (ODQ, a guanylyl cyclase inhibitor) or phosphodiesterase 5 (PDE 5) inhibitors. cGMP level was determined in EP-20-treated CC strips. The results showed that EP-20 enriched the content of L-arginine in the process of purification and relaxed the CC smooth muscle precontracted with phenylephrine (PE, 1 microM) in a concentration-dependent manner. Besides, EP-20 increased the amount of cGMP production in rabbit CC tissues. Coincubation with EP-20 and L-NAME or ODQ significantly decreased EP-20-induced relaxation whereas EP-20 increased sodium nitroprusside-induced relaxation in PE-precontracted CC strips. Besides, EP-20 increased the potency and the duration of the relaxation effects caused by electrical field stimulation. Finally, EP-20 could potentiate PDE 5 inhibitors in relaxation of PE-precontracted CC strips. We concluded that extract of EbM relax the CC smooth muscle through multitargets in NO/cGMP/PDE 5 pathway and might bring into perspective the treatment strategy for those patients with erectile dysfunction

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Epimedium brevicornum Maxim extract relaxes rabbit corpus cavernosum through multitargets on nitric oxide/cyclic guanosine monophosphate signaling pathway.

邱文慧 Chiu JH; Chen KK; Chien TM; Chiou WF; Chen CC; Wang JY; Lui WY; Wu.

[Int J Impot Res] 2006 Jul-Aug; Vol. 18 (4), pp. 335-42.

Epimedium brevicornum Maxim (EbM) has been reputed to have sexual stimulation effects on males.淫羊藿在男性性刺激頗有好名本文主要目標是The study is aimed to test the hypothesis that EbM extracts relaxed the corpus cavernosum (CC) smooth muscle through activation of multitargets on nitric oxide (NO)/cyclic guanosine monophosphate (cGMP) signaling pathway. Water extract of EbM and its subfraction (EP-20) were prepared and standardized by high-performance liquid chromatography. Isolated rabbit CC strips were mounted in organ baths and isometric tension was recorded in the presence or absence of specific inhibitors related to NO/cGMP signaling such as L-N(G)-nitro-arginine methyl ester (L-NAME), 1H-[1,2,4]oxadiazolo-[4,3-a] quinoxalin-1-one (ODQ, a guanylyl cyclase inhibitor) or phosphodiesterase 5 (PDE 5) inhibitors. cGMP level was determined in EP-20-treated CC strips. The results showed that EP-20 enriched the content of L-arginine in the process of purification and relaxed the CC smooth muscle precontracted with phenylephrine (PE, 1 microM) in a concentration-dependent manner. Besides, EP-20 increased the amount of cGMP production in rabbit CC tissues. Coincubation with EP-20 and L-NAME or ODQ significantly decreased EP-20-induced relaxation whereas EP-20 increased sodium nitroprusside-induced relaxation in PE-precontracted CC strips. Besides, EP-20 increased the potency and the duration of the relaxation effects caused by electrical field stimulation. Finally, EP-20 could potentiate PDE 5 inhibitors in relaxation of PE-precontracted CC strips. We concluded that extract of EbM relax the CC smooth muscle through multitargets in NO/cGMP/PDE 5 pathway and might bring into perspective the treatment strategy for those patients with erectile dysfunction

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Chen KK, Chiu JH, Chang LS. The effect of Epimedium brevicornum Maxim extract on clitoral intracavernous pressure in the rabbit. Program and abstracts of the 21st Annual Congress of the European Association of Urology; April 5-8, 2006; Paris,France. Abstract 20.

Researchers from Taipei, Taiwan, focused on the traditional Chinese medication Epimedium brevicornum Maxim (EbM) as a frequently used oral agent to treat erectile dysfunction (ED).[1] Pilot studies with intracavernosal administration of EbM in the rat elicited penile erections. Nitric oxide (NO) is hypothesized to be involved in EbM extract-induced penile erections. Since the clitoris is from the same embryologic origin as the penis, the investigators theorized that EbM might have an effect on clitoral intracavernosal pressure (ICP). Using a 26-gauge needle, 300 micrograms (mcg)/0.2 mL and 3000 mcg/0.2 mL of EbM and saline controls were administered intracavernosally to female New Zealand white rabbits. There were significant dose-response effects of the different doses of EbM compared with placebo: clitoral ICP increased from resting 8-10.3 ± 2.3 mm Hg to 46-63.2 ± 5.7 mm Hg for 46-100 minutes with EbM, and no effect was observed with the saline vehicle. The authors suggest that this agent may show promise in treating female sexual dysfunction (FSD). Most authorities, however, do not foresee any intracavernosal application for EbM, with topical cream or gel being the only acceptable local modality for future clinical use in women with FSD.

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淫羊藿水抽提物舒張離體大白兔胸主動脈之活性研究 錢祖明，陳建志，邱文慧 INDUCTION OF VASORELAXATION IN ISOLATED RABBIT AORTA BY EPIMEDIUM BREVICORNUM MAXIM LEAF EXTRACTS Tsu-Ming Chien, Chien-Chih Chen and Wen-Fei Chiou (全文 pdf)

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陰道高潮比陰蒂高潮重要A German group presented the results of a study that looked at the significance of NO in the control of human vaginal tissues.[2] The authors suggested that the NO-cGMP signaling system in the vaginal tissues is not primarily acting through smooth muscle relaxation and vaginal tumescence. Using vaginal tissues obtained from 15 pre- and postmenopausal women, the researchers evaluated the function of different NO-releasing drugs to counter endothelin (ET)-1 induced tension. They observed increased NO activity localized predominantly to the nerve trunks and arterioles traversing these vaginal sections in subepithelial locations. This introduces a new concept in the study of FSD, ie, that the NO-cGMP pathway might be primarily responsible for vaginal perfusion and neurotransmission and may serve, to a minor extent, as a mechanism for vaginal smooth muscle relaxation. Women who develop clitoral tumescence alone do not necessarily enjoy a better sexual experience. This finding may help explain the lack of benefit witnessed in the early sildenafil trials for the treatment of FSD.Development of effective pharmaceutical agents for the treatment of FSD will undoubtedly surpass the success of PDE 5 inhibitor agents many fold.

Uckert S, Richter K, Nuser V, et al. Significance of the nitric oxide (NO) pathway in the control of human vaginal tissue: a functional and immunohistochemical study. Program and abstracts of the 21st Annual Congress of the European Association of Urology; April 5-8, 2006; Paris, France. Abstract 22.

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Effect of Illicit (非法的被禁止的 )Drug Use on Sexual Function

Cocaine is recognized to possess intense aphrodisiac effects initially, but most long-term male users develop ED. The peripheral mechanisms involved in chronic cocaine use have not been elucidated. Investigators sought to understand the cellular and molecular mechanisms for impaired erectile function due to binge飲酒做樂 cocaine administration in a rat model.[3] Adult male Sprague-Dawley rats were divided into 2 groups: Group 1, the control group, received vehicle (saline), and group 2 received intraperitoneal binge cocaine injections (30 mg/kg for 3 times a day on 3 consecutive days per week for 3 weeks). After triple-binge cocaine or saline injections, both groups underwent an in vivo, neurogenic-mediated erectile response protocol. Plasma levels of ET-1 were assessed using enzyme-linked immunoabsorbent assay. Using Western blot analysis, penile ET-A and -B receptors (ETAR and ETBR) and endothelial nitric oxide synthase (eNOS) protein expression were monitored. Myeloperoxidase (MPO) activity was quantitated using the calorimetric tetra-methyl benzidine method. This study demonstrated that chronic cocaine use in rats caused impaired erectile function in vivo. The mechanisms responsible include increased plasma ET-1 levels, increased ETAR expression, decreased eNOS expression and NO production, and increased activity of tissue MPO. This animal study demonstrates that binge cocaine administration does significantly reduce erectile function.

1. Kendirci M, Pradhan L, Trost L, et al. The mechanisms for diminished erectile function in an animal model of binge cocaine use. Program and abstracts of the 21st Annual Congress of the European Association of Urology; April 5-8, 2006; Paris, France. Abstract 9.

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Effect of Illicit (非法的被禁止的 )Drug Use on Sexual Function

In a related clinical study from Italy, La Pera and colleagues[4] postulated that premature ejaculation (PE) and other sexual disorders might be important risk factors leading to substance abuse and subsequent addiction. The researchers interviewed 86 former heroin addicts and administered extensive questionnaires to elicit detailed histories. They reported that 31.4% of participants used heroin to improve sexual performance, mainly PE. Another 26.7% used drugs as a relief for other sexual problems.While this concept of drug addiction resulting from sexual dysfunctions is controversial, these studies suggest that such issues be taken into account while gathering the clinical history.

1. La Pera G, Cardieri A, Marianantoni Z, Peris F, et al. To what extent is heroin used to relieve premature ejaculation and other sexual disorders? Program and abstracts of the 21st Annual Congress of the European Association of Urology; April 5-8, 2006; Paris, France. Abstract 175.

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Flavonoids derived from herbal Epimedium Brevicornum Maxim prevent OVX-induced osteoporosis in rats independent of its enhancement in intestinal calcium absorption.

Zhang G; Qin L; Hung WY; Shi YY; Leung PC; Yeung HY; Leung Hong Kong, [Bone] 2006 Jun; Vol. 38 (6), pp. 818-25.

AIM: Factorial design was used to test our hypothesis whether a group of flavonoids (FE) derived from herbal Epimedium Brevicornum Maxim exerted its preventive effects on estrogen-deficiency-induced osteoporosis mainly through an enhancement in intestinal calcium absorption.. CONCLUSION: The present study suggested that FE inhibited bone resorption, stimulated bone formation, and accordingly prevented osteoporosis without hyperplastic effect on uterus in the OVX rat model, which was however independent of an enhancement in intestinal calcium absorption

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Effect of Epimedium brevicornum Maxim extract on elicitation of penile erection in the rat.

Chen KK; Chiu JH [Urology] 2006 Mar; Vol. 67 (3), pp. 631-5.

OBJECTIVES: To investigate the effect and mechanism of a Chinese medicine (Epimedium brevicornum Maxim [EbM]) on elicitation of penile erection in the rat. METHODS: Adult male Sprague-Dawley rats were used. The penile intracavernous pressure (ICP) was monitored. Intracavernous administration of different doses (30, 100, 300, 1000, 3000, 6500, and 10,000 microg/0.1 mL) of EbM extract and saline 0.1 mL was done. Intracavernous NG-nitro-L-arginine methyl ester (L-NAME) (120 microg) was administered, followed by EbM extract 300 microg 10 minutes later. EbM extract (20, 10, and 10 microg) was stereotaxically delivered into the intracerebral ventricle, paraventricular nucleus of the hypothalamus, and hippocampus, respectively. RESULTS: After intracavernous administration of 30 or 100 microg EbM extract, no significant change in ICP was noted. All other doses (300 to 10,000 microg) of EbM extract elicited a significant increase in ICP, with the greatest peak at 99.7 +/- 0.3 mm Hg (resting 7.8 +/- 1.0 mm Hg) after application of 6500 microg EbM extract. No change in ICP occurred with administration of L-NAME followed by EbM extract. Furthermore, intracavernous saline or administration of EbM extract into the intracerebral ventricle, paraventricular nucleus of the hypothalamus, or hippocampus was ineffective in inducing a significant change in ICP. CONCLUSIONS: These results suggest that intracavernous administration of EbM extract may elicit penile erection in the rat. Nitric oxide may be involved in this penile erection-inducing effect. No central neural effect of EbM extract may exist in the elicitation of penile erection

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Osteoblastic proliferative activity of Epimedium brevicornum Maxim.

Meng FH; Li YB; Xiong ZL; Jiang ZM; Li [Phytomedicine] 2005 Mar; Vol. 12 (3), pp. 189-93.

The effect of the extracts of Epimedium brevicornum Maxim. was investigated on proliferative activity in vitro. The osteoblast-like UMR106 cells was employed as an osteoblast model. The EtOH extract and the n-butanol fraction from the crude extract were found to show proliferation stimulating activity. Three flavonoid compounds (icariin, epimedin B and epimedin C) were isolated from this fraction by activity-guided assay, and the effects on cell proliferation were studied. Icariin produced the most significant promoting effect on the proliferation in osteoblast-like UMR106 cells. The results suggested that E. brevicornum Maxim. extracts might have potential activity against osteoporosis, and flavonoids such as icariin might be the active constituents stimulating osteoblasts.

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On-line concentration by field-enhanced sample injection with reverse migrating micelles in micellar electrokinetic capillary chromatography for the analysis of flavonoids in Epimedium brevicornum Maxim.

Wang S; Wu Y; Ju Y; Chen X; Zheng W; Hu Z [J Chromatogr A] 2003 Oct 31; Vol. 1017 (1-2), pp. 27-34.

A simple and sensitive micellar electrokinetic capillary chromatography (MEKC) method was developed for the separation and determination of six flavonoids in Epimedium brevicornum Maxim. Field-enhanced sample injection with reverse migrating micelles (FESI-RMM) was used for on-line concentration of the flavonoids. An electrolyte containing 20 mM H3PO4, 100 mM SDS, 20% acetonitrile and 2% 2-propanol (pH 2.0) was chosen as the electrophoretic buffer. By optimizing the stacking conditions, about 40-360-fold improvement in the detection sensitivity was obtained for the flavonoids.

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Chemical constituents from the aerial part of Epimedium brevicornum Maxim.]

Gao B; Yu J; Xiao China Journal Of Chinese Materia Medica [Zhongguo Zhong Yao Za Zhi] 1996 May; Vol. 21 (5), pp. 290-2, 319.

Six flavonoids were isolated from the aerial part of Epimedium brevicornum and identified as

baohuo side I,

baohuoside II

2"' O-rhamnosyl icariside II,

sagittatoside B,,

ikarisoside F and

ikarisoside C

by means of UV, IR, 1H-NMR, 13C-NMR and FAB-MS spectral analysis, they were isolated from this plant for the first time.

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[Determination of the content of icariine in four Chinese patent medicines containing Epimedium brevicornum Maxim]

Li Z; Liu S; Qian G; Li PJournal Of West China University Of Medical Sciences = [Hua Xi Yi Ke Da Xue Xue Bao] 1995 Mar; Vol. 26 (1), pp. 66-9.

A new HPLC method has been developed for analysis of Icariine in four Chinese patent medicines. The symmetric peak of Icariine and good resolution were gotten, when ODS was used as analytical column (30 degrees C) MeOH-KH2PO4 (pH = 2.7, adjusted with H3PO4) (57:43) as a mobile phase; the detective wavelength was 268 nm. The contents of Icariine in Bushen-qiangshen-wan, Guiling-ji, Zhuang-gu-guanjie-wan and Qianliening-chongji were 0.105, 0.0995, 0.0566 and 0.313% respectively.

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Taxonomic, genetic, chemical and estrogenic

characteristics of Epimedium species.

Singapore. Shen P; Guo BL; Gong Y; Hong DY; Hong Y; Yong [Phytochemistry] 2007 May; Vol. 68 (10), pp. 1448-58.

To understand the factors contributing to estrogenic properties of extracts from the genus Epimedium L. (Berberidaceae), we performed taxonomic, genetic and chemical characterization on 37 specimens from 18 species and related these to estrogen receptor (ERalpha and ERbeta) bioactivity, as measured by reporter genes in stable human cells. Strikingly, a genetic cluster comprising six rare Epimedium species exhibited strongest ERalpha and ERbeta activity, and this bioactivity was positively correlated with content of trace flavonoid aglycones (kaempferol, apigenin, quercetin, luteolin and breviflavone B). In contrast, there was no association between estrogenic activity and the major flavonol glycoside constituents (icariin and epimedin A-C). Although they exhibited equally strong ERalpha and ERbeta activity, E. koreanum can be clearly differentiated from E. pubescens and E. brevicornum by genetic distance and its significantly lower content of epimedin C. Our morphologic, genetic, chemical and bioactivity profiling provide the basis for the production of extracts with reproducible estrogenic properties. Such reproducibility will be critical for the standardization of Epimedium-based products

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Neuroprotective effects of icaritin against beta amyloid-induced neurotoxicity in primary cultured rat neuronal cells via estrogen-dependent pathway.

Wang Z; Zhang X; Wang H; Qi L; Lou [Neuroscience] 2007 Mar 30; Vol. 145 (3), pp. 911-22..

Beta-amyloid protein (Abeta) is the hallmark of pathogenic neurotoxins which contribute greatly to Alzheimer's disease (AD)-associated cascade including severe neuronal loss. In present study, icaritin, an active natural ingredient from a Chinese plant, Epimedium sagittatum maxim, was investigated to assess its neuroprotective effect against the toxicity induced with Abeta(25-35) in primary cultured rat cortical neuronal cells as well as the underlying mechanisms. Abeta(25-35) induced neuronal toxicity, characterized by decreased cell viability, lactate dehydrogenase (LDH) release, and neuronal DNA condensation, which is associated with both the loss of membrane potential and the alteration of the expression of Bcl-2 family proteins. The phenotype alternation induced by Abeta(25-35) could be reversed by icaritin. Furthermore, the neuroprotective effects of icaritin mentioned above were estrogen receptor dependent due to the blocking action induced by estrogen receptor antagonist ICI 182,780 and well matched binding affinity with estrogen receptor by a receptor-ligand docking experiment. mitogen-activated protein kinase/extracellular signal-regulated kinase kinase inhibitor PD98059 weakened the protective effects, which implied mitogen-activated protein kinase/extracellular signal-regulated kinase pathway may also be involved in and partly contributed to the neuroprotective effects of icaritin

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Chinese herbal ingredients are effective immune stimulators for chickens infected with the Newcastle disease virus

Kong XF; Hu YL; Yin YL; Wu GY; Rui R; Wang DY; Yang [Poult Sci] 2006 Dec; Vol. 85 (12), pp. 2169-

4 Chinese herbal ingredients (CHI) were Astragalus polysaccharide (APS), Isatis root polysaccharide (IRPS), Propolis polysaccharide, and Epimedium flavone at various concentrations. Two hundred 14-d-old male White Roman chickens were randomly divided into 10 groups. On the basis of the in vivo doses used, Propolis polysaccharide and Epimedium flavone were more potent than APS and IRPS in promoting the humoral immune response in the young birds (P < 0.05). Collectively, these findings suggest that appropriate doses of CHI can be used as novel, effective immune stimulators for chickens.

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