1.Change in hair growth-related gene expression profile in human isolated hair follicles induced by 5-alpha reductase inhibitors - dutasteride and finasteride - in the presence of testosterone.
Toshiki HATANAKA ; Zrinka LULIC ; Tim MEFO ; Cath BOOTH ; Elliott HARRISON ; Gary ONG
Singapore medical journal 2022;63(9):552-558
2.Effects of competitive and noncompetitive 5α-reductase inhibitors on serum and intra-prostatic androgens in beagle dogs.
Xiao-feng ZHAO ; Yong YANG ; Wei WANG ; Zhi QIU ; Peng ZHANG ; Biao WANG
Chinese Medical Journal 2013;126(4):711-715
BACKGROUND5α-Reductase inhibitors (5α-RI) act by inhibiting the conversion of testosterone to dihydrotestosterone (DHT), thereby preventing DHT induced benign prostatic hyperplasia. The existing 5α-RIs can be classified into two types: competitive and noncompetitive. Currently, limited evidence is available concerning the effect differences between the two types of 5α-RI on androgens. The purpose of this study was to assess the effects of competitive and noncompetitive 5α-RIs on serum and intra-prostatic androgens in beagle dogs.
METHODSTwenty beagles with spontaneous benign prostatic hyperplasia were randomly allocated into two groups: epristeride group (n = 10) in which beagles were treated with epristeride at 1 mg/kg once a day for 3 months, and finasteride group (n = 10) in which beagles were treated with finasteride at 1 mg/kg once a day for 3 months. The levels of intra-prostatic testosterone and DHT were measured before treatment and on day one after three months medication. Serum levels of testosterone and DHT were measured at the same time points. Changes in androgen levels before and after treatment were analyzed, and comparisons were made within each treatment group and between treatment groups.
RESULTSAfter 3-month treatment, serum and intra-prostatic DHT levels all decreased significantly in both the epristeride and finasteride groups. The change of DHT in serum was significantly higher in the finasteride group (-14% and -43% in epristeride and finasteride groups respectively, with P < 0.001); however there was no significant difference in the changes of intra-prostatic DHT between the two groups (-47% and -51% in epristeride and finasteride groups, respectively, P = 0.304). The decreases in DHT levels were accompanied by reciprocal increases in serum and intra-prostatic testosterone levels. Changes of testosterone were significantly higher in finasteride group both in serum (20% and 42% in epristeride and finasteride groups, respectively, P < 0.001) and in prostate tissue (18% and 29% in epristeride and finasteride groups, respectively, P = 0.004).
CONCLUSIONSTwo types of 5α-RI have similar effects in reducing DHT in prostate tissue in beagles. Competitive 5α-RI may reduce serum DHT to a greater scale, and significantly increase testosterone in beagle serum and prostate.
5-alpha Reductase Inhibitors ; pharmacology ; Androgens ; blood ; metabolism ; Androstadienes ; pharmacology ; Animals ; Dihydrotestosterone ; blood ; metabolism ; Dogs ; Finasteride ; pharmacology ; Male ; Prostate ; drug effects ; metabolism
3.Effect of large-dosage of 5alpha-reductase inhibitors on the spermatogenesis of male rats.
Xiao-dong WANG ; Yue JIA ; Yu-gui CUI ; Xing-hai WANG ; Jian-sun TONG ; Ding-zhi MA ; Rui-fen CAI ; Fu-song DI
National Journal of Andrology 2005;11(9):652-654
OBJECTIVETo identify the role of 5alpha-reductase in the spermatogenesis of male rats by studying the effect of two 5alpha-reductase inhibitors, Epristeride and Finasteride, on the spermatogenesis in male Sprague-Dawley (SD) rats.
METHODSChanges in the weight of the testis, serum testosterone and dihydrotestosterone levels, epididymal sperm count, and reproductive function were observed and analyzed after the two 5alpha-reductase inhibitors were administered to male SD rats orally.
RESULTSThe experiment showed that in comparison with control animals, both the two 5alpha-reductase inhibitors: 1. suppressed the development of the prostate and reduced the weight of the testis in the experimental groups (P < 0.05); 2. decreased the serum level of dihydrotestosterone and enhanced testosterone; 3. inhibited epididymal sperm count and productive function.
CONCLUSIONHigh dosages of the 5alpha-reductase inhibitor, Epristeride, can suppress the development of the prostate and reduce the weight of the testis, decrease dihydrotestosterone, and inhibit spermatogenesis and productive function in male rats.
5-alpha Reductase Inhibitors ; Androstadienes ; pharmacology ; Animals ; Dose-Response Relationship, Drug ; Finasteride ; pharmacology ; Male ; Rats ; Rats, Sprague-Dawley ; Spermatogenesis ; drug effects
4.Effect of androgen deprivation on penile ultrastructure.
Zhou-Jun SHEN ; Xie-Lai ZHOU ; Ying-Li LU ; Zhao-Dian CHEN
Asian Journal of Andrology 2003;5(1):33-36
AIMTo investigate the ultrastructural changes of penile corpus cavernosum and tunica albuginea in rats treated with castration or finasteride.
METHODSEighteen male Sprague-Dawley rats of nine weeks old were randomly divided into three groups with 6 rats each. Group A served as the control, Group B was castrated and Group C, treated with finasteride. Four weeks later, rats were anesthetized and blood samples obtained for the determination of serum testosterone (T) and dihydrotestosterone (DHT) levels; penile tissues were taken for scanning electron microscopy.
RESULTSThe T, free T and DHT levels in Group B and the DHT level in Group C were significantly lower than those in Group A (P<0.05). The tunica albuginea was significantly thinner in Group B than that in Group A (P<0.05), but there was no significant difference between Group C and Group A (P>0.05). Elastic fibers in the tunica albuginea of Group A were very rich and arranged regularly and undulatedly, but in Group B, most of the elastic fibers were replaced by collagenous fibers. In Group C, the tunica albuginea was mainly composed of thick and irregular-arranged collagenous fibers. In Group A, there were abundant smooth muscle fibers in the trabeculae of corpus cavernosum, but they were much less in Group C and scarce or even disappeared in Group B. In Groups B and C, the diminished/disappeared smooth muscle fibers were replaced by irregularly arranged collagenous fibers.
CONCLUSIONIn rats, androgen is essential for maintaining the normal structure of penile tunica albuginea and corpus cavernosum.
Animals ; Dihydrotestosterone ; blood ; Enzyme Inhibitors ; pharmacology ; Finasteride ; pharmacology ; Male ; Microscopy, Electron, Scanning ; Orchiectomy ; Penis ; pathology ; ultrastructure ; Rats ; Rats, Sprague-Dawley ; Testosterone ; blood ; deficiency
5.Effect of selective 5alpha-reductase inhibitor or/and testosterone undecanoate on the reproductive function of male rats.
Yue JIA ; Yu-gui CUE ; Xiao-dong WANG ; Xing-hai WANG ; Jian-sun TONG ; Ding-zhi MA ; Rui-fen CAI ; Fu-song DI
National Journal of Andrology 2005;11(1):38-41
OBJECTIVETo investigate whether 5alpha-reductase inhibitor and dihydrotestosterone (DHT) play a role in spermatogenesis in male rats.
METHODSThirty-two male rats were divided into 4 groups (Groups C, T, F and FT). Group C received plant oil injection and oral starch perfusion, Group T testosterone undecanoate (TU, 20 mg/kg) injection and oral starch perfusion, Group F plant oil injection and oral Finasteride perfusion, and Group FT TU (20 mg/kg) injection and oral Finasteride perfusion. Data on serum T and DHT, sperm count, sperm mobility and reproductive function were collected and analysed.
RESULTS(1) 5alpha-reductase inhibitor, Finasteride and TU reduced the weight of the testis and epididymis in the experiment groups compared with the negative control (Group C), but TU increased the weight of the prostate while Finasteride decreased it compared with the positive control (Group T). TU combined with Finasteride could counteract the effect of the weight increase of the prostate, but not that of the testis. (2) Finasteride, or Finasteride combined with TU, reduced the DHT but increased the testosterone level in comparison with the control group. (3) Both Finasteride and TU could inhibit epididymal sperm count and reproductive function compared with the control, but the effect was less significant in Group FT than in Group F.
CONCLUSIONHigh dosages of 5alpha-reductase inhibitor, Finasteride, can suppress male reproductive function, but the inhibiting effect could be counteracted by administration of 5alpha-reductase inhibitor along with TU.
Animals ; Cholestenone 5 alpha-Reductase ; antagonists & inhibitors ; Dihydrotestosterone ; pharmacology ; Dose-Response Relationship, Drug ; Finasteride ; pharmacology ; Male ; Organ Size ; Prostate ; drug effects ; pathology ; Rats ; Rats, Sprague-Dawley ; Spermatogenesis ; drug effects ; Testis ; drug effects ; pathology ; Testosterone ; analogs & derivatives ; pharmacology
6.Effect of two different extracts of red maca in male rats with testosterone-induced prostatic hyperplasia.
Gustavo F GONZALES ; Vanessa VASQUEZ ; Daniella RODRIGUEZ ; Carmen MALDONADO ; Juliet MORMONTOY ; Jimmy PORTELLA ; Monica PAJUELO ; León VILLEGAS ; Manuel GASCO
Asian Journal of Andrology 2007;9(2):245-251
AIMTo determine the effect of two different extracts of red maca in male rats.
METHODSProstatic hyperplasia was induced in male rats with testosterone enanthate (TE). The study comprised six groups: one control group (group 1), one group treated with TE (group 2), two groups treated with TE and aqueous extract of red maca (groups 3 and 4), one group treated with hydroalcoholic extract of red maca (group 5) and one group treated with finasteride (0.1 mg, group 6). Differences in the aqueous extract dependent on the length of time of boiling, whether for 2 or 3 hours, for groups 3 and 4 was assessed. Extracts of red maca contained 0.1 mg of benzylglucosinolate. Thereafter, a dose-response effect of different doses of benzylglucosinolates (0.02-0.08 mg) in red maca extracts was assessed.
RESULTSProstate weight was similar in rats treated with freeze-dried aqueous extract of red maca prepared after 2 and 3 hours of boiling. Freeze-dried aqueous extract of red maca, hydroalcoholic extract of red maca and finasteride reduced prostate weight in rats with prostatic hyperplasia. No difference was observed between the data obtained from aqueous extract or hydroalcoholic extract of red maca. A dose dependent reduction of prostate weight was observed with the increase of the dose of benzylglucosinolates in red maca extracts.
CONCLUSIONThe present study showed that hydroalcoholic or aqueous extract of red maca containing 0.1 mg of benzylglucosinolate can reduce prostate size in male rats in which prostatic hyperplasia had been induced by TE.
Alcohols ; Animals ; Finasteride ; therapeutic use ; Lepidium ; Male ; Organ Size ; drug effects ; Plant Extracts ; therapeutic use ; Prostate ; drug effects ; pathology ; Prostatic Hyperplasia ; chemically induced ; drug therapy ; pathology ; Rats ; Testosterone ; analogs & derivatives ; Thiocyanates ; analysis ; pharmacology ; Thioglucosides ; analysis ; pharmacology ; Water
7.Finasteride inhibits microvascular density and VEGF expression in the seminal vesicle of rats.
Shuai SUN ; Yong-Chuan WANG ; Kai GUO ; Jing DU ; Hai-Jun ZHOU ; An-Ji REN
National Journal of Andrology 2018;24(5):387-392
ObjectiveTo investigate the effect of finasteride on the microvascular density (MVD) and the expression of the vascular endothelial growth factor (VEGF) in the seminal vesicle of rats.
METHODSForty male SD rats were randomly and equally divided into groups A, B, C and D, those in groups A and B fed with normal saline as the control and those in C and D with finasteride at 40 mg per kg of the body weight per day, A and C for 14 days and B and D for 28 days. Then the seminal vesicles of the animals were harvested for HE staining, measurement of MVD, determination of the expressions of CD34 and VEGF by immunohistochemistry, and observation of histomorphological changes in the seminal vesicle.
RESULTSThe expressions of CD34 in groups C and D were decreased by 6.7% and 15.8% as compared with those in A and B (P<0.01), and that in group D decreased by 9.3% in comparison with that in C (P<0.01). The expression indexes of VEGF in groups C and D were decreased by 6.9% and 14.1% as compared with those in A and B (P<0.01), and that in group D decreased by 9.0% in comparison with that in C (P<0.01).
CONCLUSIONSFinasteride can inhibit the expression of VEGF in the seminal vesicle tissue of the rat and hence suppress the angiogenesis of microvessels of the seminal vesicle.
Angiogenesis Inhibitors ; pharmacology ; Animals ; Antigens, CD34 ; metabolism ; Finasteride ; pharmacology ; Immunohistochemistry ; Male ; Neovascularization, Physiologic ; drug effects ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Seminal Vesicles ; blood supply ; drug effects ; metabolism ; Vascular Endothelial Growth Factor A ; metabolism
8.Effects of Xialiqi Capsules on the expressions of PCNA and caspase-3 in rats withbenign prostatic hyperplasia.
Hong-Cai CAI ; Le-Bin SONG ; Guo-Wei ZHANG ; Xing-Rong QING ; Dun-Sheng MO ; Wei LIU ; Xu-Xin ZHAN ; Yu-Feng HUANG ; Xue-Jun SHANG
National Journal of Andrology 2017;23(8):728-733
Objective:
To explore the effects of Xialiqi Capsules(XLQ) on the expressions of the proliferating cell nuclear antigen (PCNA) and caspase-3 in the prostate tissue of the BPH rat model.
METHODS:
Fifty male SD ratswereequally randomized into groups A (sham operation control), B (BPH model control), C (high-dose XLQ), D (low-dose XLQ), and E (finasteridecontrol) andthe BPH modelswere established by subcutaneous injection of testosterone propionate at 0.5 mg per kilogram of the body weight per day for 30 days after castration. After modeling, the animals in groups A and B were treated intragastricallywith normal saline, while those in C, D, and E with XLQ at 1.20 and 0.61 g per kilogram of the body weight per day or finasterideat 0.8 mg per kilogram of the body weight per day, respectively, all for 30 days. Then,the bilateral prostates were harvestedfrom the rats for calculation of the prostatic index (prostate wet weight/ body weight) and determination of the expressions of PCNA and caspase-3 in the prostate tissue by immunohistochemistry and immunofluorescence staining, respectively.
RESULTS:
The prostate wet weight and prostate index were significantly increased in group B as compared with group A, ([1326±60] vs[471±17] g, P<0.01; [2.89±0.18] vs [1.06±0.06] mg/g, P<0.01), but decreased in groups C ([914±36] g;[2.02±0.08] mg/g), D ([1 099±46]g;[2.39±0.11] mg/g), and E ([817±53] g;[1.83±0.10] mg/g)in comparison with B (P<0.01), with statistically significant differences among groups C, D, and E(P<0.01) and most significantly in E.The PCNA level in the prostate tissue wasremarkably higher in group B than in A, but lower in groups C, D and E than in B. The expression of caspase-3 was down-regulatedin group B as compared with A, but up-regulated in groups C, D and E in comparison with B, most significantly in E.
CONCLUSIONS
Xialiqi Capsules can effectively reduce the prostate wet weight and prostatic index of in rats with BPH by inhibiting the level of PCNA and promoting the expression of caspase-3.
Animals
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Capsules
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Caspase 3
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metabolism
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Drugs, Chinese Herbal
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administration & dosage
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pharmacology
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Finasteride
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administration & dosage
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pharmacology
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Male
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Orchiectomy
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Organ Size
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drug effects
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Proliferating Cell Nuclear Antigen
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metabolism
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Prostate
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drug effects
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metabolism
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pathology
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Prostatic Hyperplasia
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drug therapy
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metabolism
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pathology
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Random Allocation
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Rats
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Rats, Sprague-Dawley
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Urological Agents
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administration & dosage
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pharmacology