Benign prostatic hyperplasia (BPH) is a chronic male disease characterized by the enlarged prostate. Celtis chosenianaNakai (C. choseniana) is medicinally used to alleviate pain, gastric disease, and lung abscess. In this study, the effect of C. choseniana extract on BPH was investigated using testosterone-induced rats. Sprague Dawley rats were divided into five groups: control, BPH (testosterone 5 mg·kg^-1), Fina (finasteride 2 mg·kg^-1), and C. choseniana (50 and 100 mg·kg^-1). After four weeks of TP treatment with finasteride or C. choseniana, prostate weights and DHT levels were measured. In addition, the prostates were histopathologically examined and measured for protein kinase B (Akt)/nuclear factor-κB (NF-κB)/AR signaling, proliferation, apoptosis, and autophagy. Prostate weight and epithelial thickness were reduced in the C. choseniana groups compared with that in the BPH group. The extract of C. choseniana acted as a 5α reductase inhibitor, reducing DHT levels in the prostate. Furthermore, the extract of C. choseniana blocked the activation of p-Akt, nuclear NF-κB activation and reduced the expression of AR and PSA compared with BPH. Moreover, the expression of Bax, PARP-1, and p53 increased, while the expression of bcl-2 decreased. The present study demonstrated that C. choseniana extract alleviated testosterone-induced BPH by suppressing 5α reductase and Akt/NF-κB activation, reducing AR signaling and inducing apoptosis and autophagy in the prostate. These results suggested that C. choseniana probably contain potential herbal agents to alleviate BPH.
Animals ; Cholestenone 5 alpha-Reductase/metabolism* ; Finasteride/adverse effects* ; Male ; NF-kappa B/genetics* ; Plant Extracts/therapeutic use* ; Prostatic Hyperplasia/drug therapy* ; Proto-Oncogene Proteins c-akt/genetics* ; Rats ; Rats, Sprague-Dawley ; Receptors, Androgen/metabolism* ; Testosterone ; Ulmaceae/metabolism*

The lignans in Urtica cannabina were isolated by preparative HPLC, silica, and ODS column chromatographies, and identified by NMR and HR-MS. The inhibitory activities on 5α-reductase were evaluated in vitro. As a result, ten secolignans,(2R,4S)-2,4-bis(3-methoxyl-4-hydroxyphenyl)-3-butoxypropanol(1), 3,4-trans-3-hydroxymethyl-4-[bis(3,4-dimethoxyphenyl)methyl] butyrolactone(2), 3,4-trans-3-hydroxymethyl-4-[(3,4-dimethoxyphenyl)(3-methoxyl-4-hydroxyphenyl)methyl] butyrolactone(3), 3,4-trans-3-hydroxymethyl-4-[bis(3-methoxyl-4-hydroxyphenyl)methyl] butyrolactone(trans urticol, 4), 3,4-trans-3-hydroxymethyl-4-[bis(3,4-dimethoxyphenyl)methyl] butyrolactone-3-O-β-D-glucopyranoside(5), 3,4-trans-3-hydroxymethyl-4-[(3,4-dimethoxyphenyl)(3-methoxyl-4-hydroxyphenyl)methyl]butyrolactone-3-O-β-D-glucopyranoside(6), 3,4-trans-3-hydroxymethyl-4-[bis(3-methoxyl-4-hydroxyphenyl)methyl]butyrolactone-3-O-β-D-glucopyranoside(trans-urticol-7-O-β-D-glucopyranoside, 7), cycloolivil-4-O-β-D-glucopyranoside(8), isolariciresinol-4'-O-β-D-glucopyranoside(9), and olivil-4'-O-β-D-glucopyranoside(10), together with a polyphenol [α-viniferin(11)], were isolated from U. cannabina for the first time. Compound 1 was a new lignan. Compound 7 was potent in inhibiting 5α-reductase.
5-alpha Reductase Inhibitors ; Cholestenone 5 alpha-Reductase/pharmacology* ; Chromatography, High Pressure Liquid ; Lignans/pharmacology* ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Urticaceae/enzymology*

BACKGROUND: Androgenic alopecia (AGA) is the most common type of hair loss. It is likely inherited genetically and is promoted by dihydrotestosterone. 5α-reductase has been proven a good target through finasteride use. However, the pathogenesis of AGA cannot be fully explained based only on dihydrotestosterone levels. OBJECTIVE: To identify similar hairloss inhibition activity of RE-ORGA with mode of action other than finasteride. METHODS: We prepared RE-ORGA from Korean herb mixtures. We performed MTT assays for cytotoxicity, Cell Counting Kit-8 assays for cell proliferation, and western blot to identify expression levels of 5α-reductase and Bax. RNA-sequencing was performed for the expression patterns of genes in dihydrotestosterone-activated pathways. Anti-inflammatory activity was also assessed by the expression levels of tumor necrosis factor-alpha (TNF-α) and interleukin 6. RESULTS: REORGA could promote the proliferation of human dermal papilla cells and showed low cytotoxicity. It also inhibited the expression of 5α-reductases and Bax in the cells. RNA-sequencing results verified that the mRNA expressions of SRD5A1, Bax, transforming growth factor-beta 1 (TGF-β1), and TGF-β1 induced transcript 1 (TGFβ1I1) were decreased, whereas expression of protein tyrosine kinase 2 beta (PTK2β) was more elevated. REORGA also showed anti-inflammatory activity through decreased mRNA levels of TNF-α. CONCLUSION: Transcriptionally, up-regulation of PTK2β and concomitant down-regulation of TGFβ1I1 imply that RE-ORGA can modulate androgen receptor sensitivity, decreasing the expression of 5α-reductase type II and Bax together with TGF-β1 transcripts; RE-ORGA also showed partial anti-inflammatory activity. Overall, RE-ORGA is expected to alleviate hair loss by regulating 5α-reductase activity and the receptor's androgen sensitivity.
Alopecia ; Blotting, Western ; Cell Count ; Cell Proliferation ; Cholestenone 5 alpha-Reductase ; Dihydrotestosterone ; Down-Regulation ; Finasteride ; Hair ; Humans ; Interleukin-6 ; Protein-Tyrosine Kinases ; Receptors, Androgen ; RNA, Messenger ; Tumor Necrosis Factor-alpha ; Up-Regulation

Objective: To explore the effects of Kudzu Root plus Cinnamon Granules (KR+C) on prostatic hyperplasia (PH) in mice. METHODS: Sixty 4-week-old Kunming male mice were randomly divided into six groups: blank control, PH model, high-, medium- and low-dose KR+C, and finasteride control. All the mice except those in the blank control group were subcutaneously injected with testosterone propionate (5 mg / ［kg·d］) at 7 days after surgical castration. The animals of different groups were treated intragastrically with different doses of KR+C, finasteride, and normal saline respectively for 3 weeks and then sacrificed for weighing of the prostate, calculation of the prostatic index, observation of the morphological changes in the prostate after HE staining, determination of the expressions of FGF2, Ki67 and TGF-β1 by immunohistochemistry, detection of 5α-reductase activity by ELISA, and measurement of the apoptosis index of the prostatic cells by TUNEL. RESULTS: Compared with the model controls, the mice of the other groups showed significantly reduced prostatic volume (P <0.05), prostatic index (P <0.05), expressions of FGF2, Ki67 and TGF-β1, and activity of 5 α-reductase (P <0.05), but remarkably increased apoptosis index of the prostatic cells (P <0.05). However, no statistically significant differences were observed in the above parameters between the finasteride control and the three KR+C groups (P>0.05). CONCLUSIONS KR+C can reduce the prostatic volume of PH mice by decreasing the activity of 5α- reductase, inhibiting the expressions of FGF2, Ki67 and TGF-β1, and promoting the apoptosis of prostatic cells.
Animals ; Apoptosis ; Cholestenone 5 alpha-Reductase ; metabolism ; Cinnamomum zeylanicum ; chemistry ; Fibroblast Growth Factor 2 ; metabolism ; Finasteride ; therapeutic use ; In Situ Nick-End Labeling ; Ki-67 Antigen ; metabolism ; Male ; Mice ; Organ Size ; Phytotherapy ; methods ; Plant Roots ; chemistry ; Prostate ; pathology ; Prostatic Hyperplasia ; drug therapy ; metabolism ; pathology ; Pueraria ; chemistry ; Random Allocation ; Testosterone Propionate ; administration & dosage ; Transforming Growth Factor beta1 ; metabolism ; Urological Agents ; therapeutic use

BACKGROUND: Dutasteride is an inhibitor of both types I and II 5 alpha-reductase and was approved in Korea in April 2004. This post-marketing surveillance was to assess the safety of dutasteride in Korean patients with benign prostate hyperplasia in real life and to elucidate the risk factors related adverse events. METHODS: From December 2004 to January 2010, 3,977 patients were enrolled by 184 urologists. According to post-marketing surveillance regulation, patients were enrolled consecutively. Patients administered dutasteride at least once were included in safety assessment. The incidences of any adverse events and serious adverse events were evaluated. Multiple logistic regression method was used to identify risk factors related to adverse events. RESULTS: The safety assessment included 3,870 patients with the mean age of 67.3 years. The incidence of adverse events was 3.8 %. The most frequent adverse event was impotence (75 cases, 1.9 %), libido decrease (49 cases, 1.3 %), ejaculation disorder (30 cases, 0.8 %), and gynecomastia (5 cases, 0.1 %). The incidence of unexpected adverse events was 0.5 % and cerebral infarction, lung cancer, pulmonary embolism, and diarrhea were reported as serious adverse events. CONCLUSION: In this survey, impotence was the most frequently reported adverse events. Dutasteride was well tolerated in Korean patients with benign prostate hyperplasia. These results updated the safety information and would provide important additional information for prescribers.
Azasteroids ; Cerebral Infarction ; Cholestenone 5 alpha-Reductase ; Diarrhea ; Drug Toxicity ; Dutasteride ; Ejaculation ; Erectile Dysfunction ; Gynecomastia ; Humans ; Hyperplasia ; Incidence ; Korea ; Libido ; Logistic Models ; Lung Neoplasms ; Male ; Prostate ; Pulmonary Embolism ; Risk Factors

Prostate cancer can be prevented more easily than other types of cancers, thanks to the following reasons: The presence of precursor lesions, longer doulbling time of cancerous cells, high incidence and prevalence, and susceptibility to chemo-preventive agents such as 5 alpha reductase inhibitor (5ARI). The following risk factors may increase the incidence of prostate cancer: age (older than 50), family history of prostate cancer, race (African-American), hormones (testosterone, dehydrotestosterone), and diet high in dairy foods and calcium. The following protective factors may decrease the risk of prostate cancer: Lycopene, Soy, Green tea, Vit. D, and taking Finasteride or Dutasteride. The following have not been proven to prevent prostate cancer: Selenium, vitamin E, retinoid, and multivitamins. However, their effectiveness is still under investigation. Avoiding risk factors such as smoking, being overweight and lack of exercise may help prevent cancers. Increasing protective factors such as quitting smoking, eating a healthy diet and exercising may also help prevent cancers. Some clinical studies are conducted on polyphenon E for high grade PIN, Vitamin D, fish oil, green tea, and aspirin for prostate cancer prevention. Prostate cancer is an attractive and appropriate target for cancer prevention because of its incidence, prevalence and disease-related mortality. In addition to changing life style with healthy food and reducing dairy and calcium intake, taking certain drugs (5ARI) may prevent cancer development.
Aspirin ; Azasteroids ; Calcium ; Carotenoids ; Catechin ; Cholestenone 5 alpha-Reductase ; Continental Population Groups ; Diet ; Dutasteride ; Eating ; Finasteride ; Humans ; Incidence ; Life Style ; Overweight ; Prevalence ; Prostate ; Prostatic Neoplasms ; Risk Factors ; Selenium ; Smoke ; Smoking ; Tea ; Vitamin D ; Vitamin E ; Vitamins

PURPOSE: In Korea, there was no specific guidelines for the management of benign prostatic hyperplasia (BPH). We reviewed the practice patterns of Korean urologists in the management of BPH and aimed to describe the need to develop specific guidelines. MATERIALS AND METHODS: A probability sample was taken from the Korean Urological Association Registry of Physicians, and a structured questionnaire, that explored practice patterns in the management of BPH, was mailed to a random sample of 251 Korean urologists. RESULTS: For the initial evaluation of BPH, most urologists routinely performed prostatic specific antigen (PSA) (96.4%), digital rectal exam (94.4%), international prostate symptom score (IPSS) (83.2%) and transrectal ultrasound (79.2%). Symptom assessment (36.4%) followed by transrectal ultrasound of prostate (TRUS) (20.0%) was considered as the most important diagnostic examination affecting the decision about individual treatment options. Almost all urologists (92.2%) chose medical treatment as the first-line treatment option for uncomplicated BPH with moderate symptoms. Of the respondents, 57.2% had prescribed alpha blocker and 41.6% alpha blocker plus 5-alpha reductase inhibitors as the medical treatment option for BPH. The prescription of 5-ARIs was dependent on the size of the prostate and the severity of symptoms. CONCLUSION: The results of our current survey provide useful insight into variations in the clinical practice of Korean urologists. They also indicate the need to develop further practical guidelines based on solid clinical data and to ensure that these guidelines are widely promoted and accepted by the urological community.
Adrenergic alpha-Antagonists/therapeutic use ; Cholestenone 5 alpha-Reductase/antagonists & inhibitors ; Data Collection ; Humans ; Korea ; Male ; Prostatic Hyperplasia/*diagnosis/*drug therapy ; Urology/statistics & numerical data

PURPOSE: The optimal interval at which to repeat prostate-specific antigen (PSA) measurement is controversial. We evaluated the probability of the serum PSA value increasing above specific cutoff values (4.0 ng/ml, 3.0 ng/ml, and 2.5 ng/ml) on annual follow-up visits in men with a lower baseline PSA than each cutoff value. MATERIALS AND METHODS: Between 2002 and 2006, a total of 14,459 men aged 40 to 79 years who underwent serum PSA determinations at least twice during health examinations at 11 medical centers were enrolled in this study. To reduce probable bias, we excluded men with pyuria, those with a baseline or follow-up PSA level of 10.0 ng/ml or more, and those with a history of medication with 5 alpha-reductase inhibitors. Serum PSA underwent logarithmic conversion to work out the normal distribution. The cumulative rate of freedom from increase in PSA above 4.0 ng/ml, 3.0 ng/ml, and 2.5 ng/ml was estimated with the Kaplan-Meier method according to baseline PSA range and age. The significance level was 1%. RESULTS: The rate of increase in PSA was lower in men who had a baseline PSA value in the low range and whose age was in the 40s or 50s. However, the cumulative rate of freedom from increase in PSA decreased as the PSA cutoff value was lowered. The optimal screening interval for men in their 40s and 50s whose baseline serum PSA level was 1.0 ng/ml or lower was 3 years when the significance level for PSA rising above 4.0 ng/ml was 1%. It was 2 years and 1 year, respectively, when the cutoff value was lowered to 3.0 ng/ml or 2.5 ng/ml. An annual PSA screening interval was recommended in men older than their 60s. CONCLUSIONS: The PSA test interval should be individualized according to baseline PSA, age, and PSA cutoff value.
Aged ; Bias (Epidemiology) ; Cholestenone 5 alpha-Reductase ; Follow-Up Studies ; Freedom ; Humans ; Male ; Mass Screening ; Prostate-Specific Antigen ; Pyuria

PURPOSE: We evaluated the pathologic characteristics and prognosis of pathologic T0 (pT0) prostate cancer (PC). MATERIALS AND METHODS: Of 1,196 consecutive men who underwent radical prostatectomy (RP) between January 1992 and November 2008, 34 patients (mean age, 68.8+/-7.9 years; range, 48-85) had pT0 PC. They were categorized into 4 groups according to neoadjuvant hormone therapy (NHT) and diagnostic methods. The initial PSA, 5 alpha-reductase inhibitor (5alphaRI), Gleason score of prostatic needle biopsy (PNB) or transurethral resection of the prostate (TURP), clinical stage, and presence of high-grade prostatic intraepithelial neoplasia were evaluated. Clinical and biochemical progression were also evaluated. RESULTS: 34 patients were categorized into 4 groups (Group I: 9 without NHT, diagnosed by PNB [1.1%]; Group II: 8 without NHT, diagnosed by TURP [11.3%]; Group III: 16 with NHT, diagnosed by PNB [5.5%]; Group IV: 1 with NHT, diagnosed by TURP [3.8%]). Group I had serum prostate-specific antigen (PSA)<15.0 ng/ml, one positive biopsy core, and a Gleason score< or =7. Group II had serum PSA<10.1 ng/ml, chips involved with cancer<10.0%, and a Gleason score< or =6. There were more patients taking 5alphaRI and high-grade PIN among patients without NHT. None of patients with pathologic pT0 PC had clinical or biochemical progression during follow-up, except 3 patients with NHT (mean, 22 months; range, 2-105 months). CONCLUSIONS: Patients without NHT had more favorable clinical and pathologic results. In our study, except for 3 patients with NHT, all patients had undetectable PSA levels after RP. We need more time for follow-up to conclude whether the prognosis of pT0 PC is favorable.
Biopsy ; Biopsy, Needle ; Cholestenone 5 alpha-Reductase ; Follow-Up Studies ; Humans ; Male ; Neoplasm Grading ; Prognosis ; Prostate ; Prostate-Specific Antigen ; Prostatectomy ; Prostatic Intraepithelial Neoplasia ; Prostatic Neoplasms ; Transurethral Resection of Prostate

5 alpha-reductase deficiency is a rare autosomal recessive disorder caused by mutations in the SRD5A2-gene, resulting in absent or diminished dihydrotestosterone (DHT) formation and, hence, in an underdevelopment of the external genitalia in patients with 46,XY karyotype. Recently we experienced a 17 years old patient with chief complaint of primary amenorrhea, who showed 46,XY karyotype, enlarged clitoris, virilization, undeveloped breast and palpable bilateral inguinal mass. We diagnosed it as 5 alpha?reductase deficiency and removed the bilateral gonads, so we report it with brief review of literature.
46, XY Disorders of Sex Development ; Adolescent ; Amenorrhea ; Breast ; Cholestenone 5 alpha-Reductase* ; Clitoris ; Dihydrotestosterone ; Female ; Genitalia ; Gonads ; Humans ; Karyotype ; Virilism