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*

Prostate cancer is one of the most common visceral malignancies in human. In recent years, its incidence has dramatically increased in China. 5 alpha-reductase inhibitors can block the biological effects of dihydrotestosterone by restraining the transformation from testosterone to dihydrotestosterone, and therefore can be used for the chemoprevention of prostate cancer. Two large clinical trials on the chemoprevention of prostate cancer (the Prostate Cancer Prevention Trial and the Reduction by Dutasteride of Prostate Cancer Events) were completed in 2003 and 2008, respectively, bringing the global interests on this topic. However, the interpretations of these two trials and the possible recommendations on clinical applications remain controversial.
5-alpha Reductase Inhibitors ; therapeutic use ; Chemoprevention ; Humans ; Male ; Prostatic Neoplasms ; prevention & control

OBJEVTIVETo synthesize phenoxybutyric acid derivatives as 5α-reductase inhibitors and test their biological activities in vitro.

METHODSEight analogues as nonsteroidal 5α-reductase inhibitors were designed and synthesized by substitution reaction of 6-(4-phenyl-piperazine-1-yl)-3(2H)-pyridazinone with phenoxybutyric acid derivatives.

RESULTS AND CONCLUSIONThe structures of the compounds were characterized by 1H-NMR and MS. Biological evaluation indicated that 7 out of the 8 compounds exhibited moderate 5α-reductase inhibitory activities, especially the compounds A1 and A7 with inhibition rates reaching 12.50% and 19.64% at the concentration of 3.3 × 10⁻⁵ mol/L, respectively.

Benign prostatic hyperplasia (BPH) is a common disease in older men. At present, 5alpha reductase inhibitor-based medication, preferred by most BPH patients as the first-choice therapy, is taking place of traditional transurethral resection of the prostate. This article presents an update of the researches on the treatment of BPH with dutasteride--a novel 5 alpha-reductase inhibitor.
5-alpha Reductase Inhibitors ; therapeutic use ; Azasteroids ; therapeutic use ; Dutasteride ; Humans ; Male ; Prostatic Hyperplasia ; drug therapy

5-alpha reductase inhibitors decrease the level of dihydrotestosterone (DHT) by inhibiting 5-alpha reductase. Trials on 5-alpha reductase inhibitors in prostate cancer prevention showed that they could significantly decrease the incidence of prostate cancer, but meanwhile increase high-grade cases as well. Recent studies demonstrated that 5-alpha reductase inhibitors could reduce not only the prostate volume but also the volume of Gleason grade 3 prostate cancer, which made easier the detection of higher-grade prostate cancer in the second biopsy. 5-alpha reductase inhibitors could also increase the sensitivity of prostate biopsy in detecting prostate cancer, particularly that of a higher grade. The evidence we have obtained leads to the conclusion that 5-alpha reductase inhibitors do not increase the incidence of high-grade prostate cancer, but on the contrary help its earlier detection.
5-alpha Reductase Inhibitors ; therapeutic use ; Humans ; Male ; Prostatic Neoplasms ; prevention & control

PURPOSE: To compare and analyze the therapeutic effects and changes in the prostate-specific antigen (PSA) level with treatment with finasteride or dutasteride for benign prostatic hyperplasia (BPH) for 1 year. MATERIALS AND METHODS: We retrospectively investigated patients who suffered from BPH for 1 year between January 2005 and December 2008. For treatment groups, we divided the patients into two groups: one was treated with alfuzosin and finasteride and the other was treated with alfuzosin and dutasteride. At the beginning of treatment, the patients underwent transrectal ultrasonography and measurement of urine flow rate, residual urine volume, PSA, and International Prostate Symptom Score (IPSS). Patients with diseases affecting urinary function were excluded. We not only analyzed the data at the time of initial treatment, but also after 1 year of treatment. A total of 219 patients were able to be evaluated for 1 year. RESULTS: Both finasteride and dutasteride reduced PSA and prostate volume significantly. The comparison between groups showed a more significant reduction of PSA (p=0.020) and prostate volume (p=0.052) in the dutasteride group. Other parameters did not differ significantly between the groups. CONCLUSIONS: 5-alpha Reductase inhibitors for BPH treatment reduced PSA and prostate volume significantly when the patients were treated for 1 year. Administration of dutasteride is considered to be more effective in reducing PSA and prostate volume. Therefore, dutasteride should not be considered equivalent to finasteride in the reduction rate of PSA. The intensity of dutasteride must be reevaluated in comparison with finasteride.
5-alpha Reductase Inhibitors ; Azasteroids ; Finasteride ; Humans ; Prostate ; Prostate-Specific Antigen ; Prostatic Hyperplasia ; Quinazolines ; Retrospective Studies ; Dutasteride

PURPOSE: To evaluate the effect of preoperative 5-alpha reductase inhibitor (ARI) administration on the operative results of photoselective vaporization of prostate with 120W GreenLight HPS laser. MATERIALS AND METHODS: Data were collected from 98 benign prostatic hyperplasia (BPH) patients who underwent transurethral electrovaporization of prostate by 120W Greenlight HPS laser between Jan. 2010 and Dec. 2010. We compared the time of operation, the energy required in lasering, postoperative maximum uroflow velocity, change in residual urine volume and complications between 5-ARI administrating group and control group. RESULTS: 56 patients administrated 5-ARI at least 3 months before surgery. 30 and 26 patients administrated finasteride and dutasteride, respectively. Mean follow up period was 4.1+/-1.8 months. Mean age of the subjects and mean prostate volume were not different. Mean change of postoperative hemoglobin, lasing time and energy required in lasering were greater in 5-ARI administrating group. There were 3 and 1 cases of acute urinary retension in 5-ARI administrating group and control group, respectively. CONCLUSIONS: The mean change of hemoglobin and mean energy required in lasering were greater and mean lasing time was longer in the patients who administrated 5-ARI before photoselective vaporization of prostate by 120W Greenlight HPS laser. Further investigation and extensive study will be needed to confirm these results.
5-alpha Reductase Inhibitors ; Azasteroids ; Finasteride ; Follow-Up Studies ; Hemoglobins ; Humans ; Oxidoreductases ; Prostate ; Prostatic Hyperplasia ; Transurethral Resection of Prostate ; Volatilization ; Dutasteride

PURPOSE: Many patients with benign prostatic hyperplasia (BPH) have storage symptoms. The aim of this study was to evaluate the effects of treatment with a 5-alpha reductase inhibitor (5ARI) on storage symptoms in patients with BPH. METHODS: This study was conducted in 738 patients with lower urinary tract symptoms secondary to BPH. Patients with a prostate volume of higher than 30 mL on the transrectal ultrasound were classified into two groups: group A, in which an alpha blocker was solely administered for at least 12 months, and group B, in which a combination treatment regimen of an alpha blocker plus 5ARI was used. This was followed by an analysis of the changes in parameters such as the total International Prostate Symptom Score (IPSS), voiding symptom subscore, and storage symptom subscore between the two groups. In addition, we examined whether there was a significant difference between the two groups in the degree of change in storage symptoms between before and after the pharmacological treatment. RESULTS: Of the 738 men, 331 had a prostate volume > or =30 mL, including 150 patients in group A and 181 patients in group B. Total IPSS, the voiding symptom subscore, and the storage symptom subscore were significantly lower after treatment than before treatment in both groups (P<0.05). A comparison of the degree of change between before and after treatment, however, showed no significant differences in the storage symptom subscore between the two groups (P>0.05). CONCLUSIONS: Alpha blocker and 5ARI combination treatment is effective for patients with BPH including storage symptoms. However, 5ARI does not exert a significant effect on storage symptoms in BPH patients.
5-alpha Reductase Inhibitors ; Humans ; Lower Urinary Tract Symptoms ; Male ; Oxidoreductases ; Prostate ; Prostatic Hyperplasia ; Urinary Bladder, Overactive

PURPOSE: To assess changes in lower urinary tract symptoms (LUTS), prostate volume, and serum prostate-specific antigen (PSA) after discontinuation of 5-alpha reductase inhibitor (5ARI) combination therapy in patients with benign prostatic hyperplasia (BPH). MATERIALS AND METHODS: From December 2003 to December 2012, data were collected retrospectively from 81 men more than 40 years of age with moderate to severe BPH symptoms (International Prostate Symptom Score [IPSS]> or =8). The men were classified into group 1 (n=42) and group 2 (n=39) according to the use of 5ARI therapy. A combination of dutasteride 0.5 mg with tamsulosin 0.2 mg was given daily to all patients for 1 year. For the next 1 year, group 1 (n=42) received the combination therapy and group 2 (n=39) received tamsulosin 0.2 mg monotherapy only. The IPSS, prostate volume, and PSA level were measured at baseline and at 12 and 24 months according to the use of dutasteride. RESULTS: Discontinuation of dutasteride led to significant deterioration of LUTS, increased prostate volume, and increased PSA level. The repeated-measures analysis of variance showed that the changes in IPSS, prostate volume, and PSA level over time also differed significantly between groups 1 and 2 (p<0.001). CONCLUSIONS: Withdrawal of 5ARI during combination therapy resulted in prostate regrowth and deterioration of LUTS. The PSA level is also affected by the use of 5ARI. Therefore, regular check-up of the IPSS and PSA level may be helpful for all patients who either continue or discontinue the use of 5ARI.
5-alpha Reductase Inhibitors ; Humans ; Lower Urinary Tract Symptoms ; Male ; Oxidoreductases* ; Prostate ; Prostate-Specific Antigen ; Prostatic Hyperplasia* ; Retrospective Studies

PURPOSE: To compare the clinical therapeutic efficacy of finasteride and dutasteride as 5-alpha reductase inhibitor (5-ARI) in the medical treatment of benign prostate hyperplasia. MATERIALS AND METHODS: From July 2007 to July 2010, 354 benign prostatic hyperplasia patients with combination medication : alpha blocker plus 5-ARI were enrolled. These patients were classified into a finasteride medication group (F group) and dutasteride medication group (D group) retrospectively. We initially measured the total prostate volume (TPV), prostate specific antigen (PSA), International Prostate Symptom Score (IPSS), quality of life score (QoL), maximal flow rate (Qmax), and post-void residual urine (PVR). After at least twelve months of medication, we rechecked these clinical parameters and during medication, side effects related to medication were also recorded. RESULTS: The F group (n=129) and D group (n=225) showed no differences in baseline characteristics for age, TPV, IPSS, QoL scores, or PSA. After medication, decreases in TPV were relatively higher in the D group than the F group (28.2% vs 20.5%). In addition, the decrease in PSA (43.6% vs 39.2%) and IPSS score (4.6 vs 3.5) were also higher in the D group. There were no significant differences in QoL score, Qmax, PVR change, or side effects between the two groups. CONCLUSIONS: Dutasteride showed greater efficacy in reduction of TPV and PSA and in symptomatic improvement by IPSS score than finasteride. More large scale studies about the differences on clinical efficacy of finasteride and dutasteride are needed.
5-alpha Reductase Inhibitors ; Azasteroids ; Finasteride ; Humans ; Oxidoreductases ; Prostate ; Prostate-Specific Antigen ; Prostatic Hyperplasia ; Quality of Life ; Retrospective Studies ; Dutasteride