• 한국임상약학회지
• /
• 제21권1호
• /
• pp.1-5
• /
• 2011

Purpose: 본 연구는 토끼의 음경해면체 조직에 대한 인진쑥의 에탄올 추출물과 그 성분 중의 하나인 scoparone의 효능을 평가하고자 하였다. Methods: 체중이 2.5-3.0 Kg의 New Zealand백색 가토를 사용하여 음경 전체를 골반골로부터 분리하여 요도를 제거한 후 백막을 보유한 음경해면체를 2 mL organ chamber 관류모형에 연결하고, $10^{-5}M$의 phenylephrine을 관류하여 음경해면체를 수축시킨 후 0.1, 0.5, 1, 2 mg/mL의 에탄올 추출물 또는 $10^{-7}$, $10^{-6}$, $10^{-5}$, $10^{-4}M$의 scoparone을 녹인 용액으로 관류시켜 음경의 장력 변화를 측정하였다. 기존의 발기부전 치료제로 사용되는 실데나필에 대한 인진쑥과의 상호작용을 검토하기 위하여$10^{-6}M$의 scoparone과 $10^{-8}M$의 실데나필을 병용 사용 시 음경해면체 조직에 대한 효과도 함께 검토하였다. Results: 인진쑥의 에탄올 추출물은 phenylephrine으로 전처리하여 수축시킨 음경해면체 평활근을 농도 의존적으로 효과적으로 이완시켰으며 scoparone도 음경해면체 조직에 대한 이완작용 또한 농도 의존적으로 강한 효과를 나타내었다. 실데나필로 전처리한 음경해면체 조직에 대한 scoparone의 효과는 scoparone만을 단독으로 관류시킨 조직에서의 효과보다 강하게 나타났으며 실데나필과 scoparone의 병용사용은 실데나필의 효능을 2배 이상 증가시켰다. Conclusions: Scoparone은 실데나필의 음경해면체평활근 작용을 증가시킴으로써 실데나필에 완전히 반응하지 않는 환자들의 발기부전 치료효과 향상에 유용할 것으로 전망된다.

• Mycobiology
• /
• 제48권2호
• /
• pp.153-156
• /
• 2020

Calvatia nipponica, a puffball mushroom (Agaricaceae), is thought to be an aphrodisiac, as this mushroom is traditionally known to improve sexual function in males. As part of the systematic study to determine the bioactive secondary metabolites from C. nipponica responsible for aphrodisiac effects, chemical analysis of methanol (MeOH) extracts of the fruiting bodies of C. nipponica resulted in the isolation of two major compounds: N,N-dimethyl-anthranilic acid (1) and (7Z,10Z)-7,10-octadecadienoic acid methyl ester (2). Compounds 1 and 2 were evaluated for cumulative dose-dependent relaxation responses to precontracted penile corpus smooth muscle (PCCSM). Results show that compounds 1 and 2 exhibited a maximum relaxation effect of 20.33 ± 2.18% and 24.63 ± 3.60%, respectively. These findings indicate that compounds 1 and 2, major components of C. nipponica, could potentially be used to treat erectile dysfunction, functioning as natural aphrodisiacs.

• Archives of Pharmacal Research
• /
• 제25권6호
• /
• pp.873-878
• /
• 2002

OA-8159, a new Phosphodiesterase (PDE) 5 inhibitor, has exhibited potent erectogenic potential in a penile erection test in rats and anesthetized dogs. In this study, we investigated the mechanism of its erectogenic activity by measuring the activity of OA-8159 against a various PDE isozymes and assessing cGMP and cAMP formation in a rabbit corpus cavernosum in vitro. DA-8159 inhibited the PDE 5 activity in rabbit and human platelets, which the $IC_{50}$ was 5.84$\pm$1.70 nM and 8.25$\pm$2.90 nM, respectively. The $IC_{50}$ of DA-8159 on PDE 1, PDE2, PDE 3 and PDE 6 were 870$\pm$57.4 nM, $101\pm$5 $\mu$M, 52.0$\pm$3.53 $\mu$M and 53.3$\pm$2.47 nM, respectively. This suggests that DA-8159 is a potent, highly selective, competitive inhibitor of PDE 5-catalyzed cGMP hydrolysis. The rates of cGMP hydrolysis catalyzed by human platelets-derived PDE 5 as a function of the cGMP concentration (5~100 nM) and two-fixed DA-8159 concentration (11.3 and 18.8 nM) were investigated in order to characterize the mode of PDE 5 inhibition by DA-8159. DA-8159 increased the apparent 4K_{m}$ value for cGMP hydrolysis but had no effect on the apparent $V_{max}$, indicating a competitive mode of inhibition. DA-8159 increased the cGMP concentrations in the rabbit corpus cavernosum dose dependently. In the presence of sodium nitroprusside (SNP), DA-8159 significantly sti\mulated the accu\mulation of cGMP when compared to the control level. This indicated that the enhancement of a penile erection by DA-8159 involved the relaxation of the cavernosal smooth \muscle by NO-sti\mulated cGMP accu\mulation. In conclusion, DA-8159 is a selective inhibitor of PDE 5-catalyzed cGMP hydrolysis and the enhancement of a penile erection by DA-8159 is mediated by the relaxation of the cavernosal smooth \muscle by the NO-sti\mulated cGMP accu\mulation.

• Journal of Ginseng Research
• /
• 제20권3호
• /
• pp.339-343
• /
• 1996

The effect of ginseng on the reactivity of penile corpus cavernosal smooth muscle strips of rabbits was investigated to support the clinical application of ginseng for the treatment of erectile dysfunction. New Zealand white rabbits were randomly divided into two groups, normal diet group (n=9) and ginseng saponin diet group (n=5). Then, each group was fed normal diet and Korean red ginseng saponin diet (50 mg/kg/day) for 10 weeks. We measured concentration dependent relaxation of corporal smooth muscle to acetylcholine (10-8 M to 10-4M) in organ chamber. The degree of relaxation was expressed as percentage of maximal relaxation obtained by papaverine (10-4M). Dose dependent relaxation of corpus cavernosal smooth muscle to acetylcholine, at the concentration of 10-8 M to 10-4M by half log increment, was 4.06$\pm$0.00, 4.30$\pm$1.30, 5.32$\pm$0.68, 11.64$\pm$1.74, 16.24$\pm$1.61, 23.33$\pm$ 2.29, 26.45$\pm$2.25, 30.43$\pm$2.40 and 33.41 $\pm$2.48 (%), respectively in normal diet group and 9. 83$\pm$4.15, 20.60$\pm$4.62, 24.1815.12, 35.75$\pm$5.71, 43.35$\pm$6.11, 51.30$\pm$6.22, 56.33$\pm$6.22, 54.30$\pm$4.17 and 51.98$\pm$3.92 (Vc), respectively in ginseng group. These data suggest that ginseng enhances ondothelium-dependent acetylcholine-induced relaxation of penile corpus cal.ernosal smooth muscle in rabbits.

• Nutrition Research and Practice
• /
• 제12권4호
• /
• pp.291-297
• /
• 2018

BACKGROUND/OBJECTIVES: This study evaluated the effects and molecular mechanisms of the Schisandra chinensis fruit extract (SC) and its major compound gomisin A (GA), on the contractility of rabbit penile corpus cavernosum smooth muscle (PCCSM). MATERIALS/METHODS: PCCSM was exposed to SC or GA after appropriate pretreatment with nitric oxide synthase (NOS) blocker, guanylate cyclase blocker, adenylyl cyclase blocker or protein kinase A blocker. Subsequently, we evaluated the cyclic nucleotide in the perfusate by radioimmunoassay, protein expression level of neuronal NOS (nNOS) and endothelial NOS (eNOS) by western blot, and the interaction of SC or GA with udenafil and rolipram. RESULTS: Both SC and GA induce PCCSM relaxations in a concentration-dependent manner. Pretreatment with NOS blocker, guanylate cyclase blocker, adenylyl cyclase blocker or protein kinase A blocker result in significantly decreased relaxation. SC and GA also induce the levels of cyclic nucleotide in the perfusate in a concentration-dependent manner. Perfusion with GA also showed significantly higher levels of eNOS protein. Furthermore, the udenafil and rolipram induced relaxations of PCCSM were enhanced after exposure to SC and GA. Our results indicate that SC and GA induce the relaxation of PCCSM via the nitric oxide (NO)-cGMP and cAMP signaling pathways. CONCLUSIONS: The SC and GA are potential alternative treatments for men who want to consume natural products to ameliorate erectile function, or who do not respond to the commercially available medicines.

• Journal of Yeungnam Medical Science
• /
• 제23권1호
• /
• pp.52-61
• /
• 2006

이상의 결과를 종합하면, 인삼 총사포닌은 본 실험의 조건에서 배뇨개선 효과가 있으며 이에 관여하는 총사포닌의 주 효능은 근위부요도를 이완시킴으로써 이루어지는 것으로 생각된다. 그리고 인삼 총사포닌은 혈류역동학적으로 안전하게 음경해면체 평활근을 이완시켜 음경발기를 유발시키는 것으로 생각된다.

• Natural Product Sciences
• /
• 제22권1호
• /
• pp.46-52
• /
• 2016

Erectile dysfunction (ED) is a highly prevalent disorder that affects millions of men and considered to be an early symptom of atherosclerosis and a precursor of various systemic vascular disorders. The aim of the present study was to prepare ginsenoside Re enriched fraction (GS-F3K1, ginsenoside Re 10%, w/w) from ginseng berries flesh and to investigate the enhanced activities of GS-F3K1 on alcohol-induced ED. GS-F3K1 was prepared by the continuous liquid and solid separating centrifugation and circulatory ultrafiltration from ginseng berries flesh. GS-F3K1 was administered for 5 weeks in ethanol-induced ED rat by oral administration of 20% ethanol. To investigate the effects of GS-F3K1 on ED model, the levels of nitrite expression, cyclic guanosine monophosphate (cGMP) and erectile response of the penile corpus cavernosum of rat were measured. The erectile response of the corpus cavernosum was restored after GS-F3K1 administration, to a level similar to the normal group. The level of nitrite and cGMP expression in the corpus cavernosum of GS-F3K1-administered male rats was increased significantly compared to positive control group. GS-F3K1 from ginseng berries should effectively restore ethanol-induced ED in male rats and could be developed as a new functional food for the elderly men.

• 생약학회지
• /
• 제37권2호통권145호
• /
• pp.85-91
• /
• 2006

The present study was undertaken to evaluate the effect of evening primrose oil (EPO) on the male sexual functions. EPO (daily 0.5 ml/mouse) was orally intubated for 28 consecutive days to experimental ICR mice, and same vol. of vehicle to control mice. On the 14th and 28th experimental day, the testis weight, number of complete intromissions and mating, serum testosterone and cGMP levels, prostaglandin leveIs of penile corpus cavernosum smooth muscle cells, and NO-productive activity of endothelial cells were determined. The weight of body and testis, the number of complete intromissions during the 3hour period were somewhat increased in EPO treated mice than those of control. The number of sperm-positive females and testosterone level in serum were increased in experimental groups. The serum cGMP level was significantly increased but the NO production of ionomycin-stimulated HUVEC cells was not affected when EPO was added into cultures. These results suggest that oral administration of EPO enhanced the sexual functions of male mice, and EPO could be developed as a tonic improving sexual functions.

• Journal of Ginseng Research
• /
• 제40권4호
• /
• pp.334-343
• /
• 2016

Background: Progressed tissue culture techniques have allowed us to easily obtain mass products of tissue-cultured mountain ginseng over 100 yr old (TCMG-100). We investigated the effects of TCMG-100 extract on erectile function using in vitro and in vivo studies. Methods: To examine the relaxation effects and mechanisms of action of TCMG-100 on rabbit cavernosal strips evaluated in an organ bath. To investigate the long-term treatment effect of TCMG-100, 8-wk administration was performed. After administration of TCMG-100, intracavernosal pressure, cyclic guanosine monophosphate and nitric oxide (NO) levels of cavernosal tissue, serum testosterone level, histological observation of collagen fiber, endothelium, smooth muscle cell, and transforming growth factor-${\beta}1$ were investigated. Results: TCMG-100 extract displayed dose-dependent relaxation effects on precontracted rabbit corporal smooth muscle. The TCMG-100-induced relaxation was significantly reduced by removing the endothelium, and treatment with an NO synthase inhibitor or NO scavenger. Eight weeks of TCMG-100 administration increased intracavernosal pressure in a rat model. The levels of cyclic guanosine monophosphate and NO in the corpus callosum and serum testosterone level were also increased by TCMG-100 treatment. Furthermore, histological evaluation of collagen, smooth muscle, and endothelium showed increases in endothelium and smooth muscle, and a decrease in transforming growth factor-${\beta}1$ expression. Conclusion: These relaxation effects on corporal smooth muscle and increased erectile function suggest that TCMG-100 might be used as an alternative herbal medicine to improve erectile function.

• 동의생리병리학회지
• /
• 제20권1호
• /
• pp.174-180
• /
• 2006

We examine the effect of Geiji-Bokryung-Hwan(GBH) on erectile function in a rat model of hypercholesterolemic erectile dysfunction. GBH, a drug preparation consisting of five herbs of Cinnamomi Ramulus (Geiji), Poria Cocos (Bokryun), Mountan Cortex Radicis (Mokdanpi), Paeoniae Radix (Jakyak), and Persicae Semen (Doin) is a traditional Korean herbal medicine that is widely used in the treatment of atherosclerosis-related disorders. In this study, 3-month-old Sprague-Dawley rats were used. The 6 rats control animals were fed a normal diet and the other 18 rats were fed 1% cholesterol diet for 3 months. After 1 months, GBH was added to the drinking water of the treatment group of 12 rats but not the cholesterol only group of 6 rats. Of the 12 rats 6 received 30 mg/kg per day (group 1) and 6 received 60 mg/kg per day (group 2) of GBH. At 3 months erectile function was evaluated with cavernous nerve electrostimulation in all animals. Penile tissues were collected for electron microscopy, and to perform Western blot for endothelial nitric oxide synthase (eNOS), neuronal nitric oxide synthase (nNOS), basic fibroblast growth factor (bFGF) and caveolin-1. Systemic arterial pressure was not significantly different between the animals that were fed the 1% cholesterol diet and the controls. Conversely erectile function was not impaired in the herbal medicine treated rats. Electron microscopy showed many caveolae with fingerlike processes in the cavernous smooth muscle and endothelial cell membranes in control and treated rats but not in the cholesterol only group of rats. Western blot showed differences among groups in protein expression for eNOS, nNOS, caveolin-1 and bFGF protein expression in penile tissue. Increased eNOS and nNOS protein expressions dy high cholesterol diet were significantly decreased in group 1 and group 2. Interestingly, caveolin-1 and bFGF protein expression was significantly higher in groups 1 and 2 than in the cholesterol only and control groups.