[Natural 5α-reductase inhibitors in treatment of benign prostatic hyperplasia].

Benign prostatic hyperplasia(BPH) is a common disease of the male urinary system, and its incidence rate in China is increasing. However, the mechanism underlying the pathogenesis of BPH remains unclear. Some studies demonstrated that the incidence of BPH was related to the change in the levels of steroid hormones. Too high content of dihydrotestosterone(DHT) in the body may cause BPH and other related diseases. Testosterone(T) is converted to DHT by 5α-reductase(SRD5A). By inhibiting the activity of this enzyme, the production of DHT can be reduced, and then the incidence of BPH can be lowered. Therefore, it has drawn great attention to screen and discover safer and more effective 5α-reductase inhibitors from natural medicines to treat prostatic hyperplasia without affecting the physiological function of men. This review summarizes the characteristics and tissue distribution of 5α-reductase, the discovery of 5α-reductase inhibitors in traditional Chinese medicine and natural medicines, 5α-reductase inhibitors commonly used in clinical practice and their side effects, as well as the animal models of prostatic hyperplasia and common detection indicators, aiming to provide a reference for more in-depth understanding and research about BPH and development of drugs.

The extract of Celtis choseniana Nakai alleviates testosterone-induced benign prostatic hyperplasia through inhibiting 5α reductase type 2 and the Akt/NF-κB/AR pathway / 中国天然药物

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.

Effects of Kudzu Root plus Cinnamon Granules on prostatic hyperplasia in mice / 中华男科学杂志

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).@*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.

Prevention of Prostate Cancer

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.

Pathologic Characteristics and Prognosis of Pathologic T0 Prostate Cancer

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.

The Antihyperplastic Effect of Oral Catechin Ingestion in a Rat Model of Benign Prostatic Hyperplasia / 대한비뇨기과학회지

PURPOSE: Benign prostatic hyperplasia (BPH) is one of the common diseases in elderly men. Recently, the old-aged population has increased, with the interest in the clinical importance of BPH ever growing. Catechin, an extract of green tea, has the effect of the 5-alpha reductase inhibitor. Typically, BPH has been shown to be influenced by 5-alpha reductase. Therefore, the relationship between BPH and catechin was evaluated. MATERIALS AND METHODS: An experimental prostatic hyperplasia was induced in male Wistar rats by the administration of testosterone propionate, 3mg/kg sc, for 4 weeks. The Wistar rats were divided into four experimental groups: the control, BPH-induced, oral finasteride ingestion and oral catechin ingestion groups. After 4 weeks, the prostates were removed, and analyzed for their prostatic weight and histological examination. RESULTS: The prostate weights were measured in each group, and found to be 330.0+/-40.7, 970.0+/-1.1, 358.0+/-39.9 and 415.0+/-45.3mg in the control, BPH-induced, oral finasteride ingestion and oral catechin ingestion groups, respectively. The oral finasteride and catechin ingestion groups showed statistically significant decreases in their prostatic weights compared with the BPH-induced group (p0.05). Histologically injected testosterone lead to prostatic hyperplasia in rats, but oral catechin ingestion decreased this change. CONCLUSIONS: These results suggest that catechin may be effective in BPH, and the consumption of green tea may be effective in preventing BPH.

Effect of selective 5alpha-reductase inhibitor or/and testosterone undecanoate on the reproductive function of male rats / 中华男科学杂志

<p><b>OBJECTIVE</b>To investigate whether 5alpha-reductase inhibitor and dihydrotestosterone (DHT) play a role in spermatogenesis in male rats.</p><p><b>METHODS</b>Thirty-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.</p><p><b>RESULTS</b>(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.</p><p><b>CONCLUSION</b>High 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.</p>

Promoting Effect of a Mixture of 8 Herbal Extracts (SPELA 707) on Hair Growth

In Korean folk medicine, several herbs, Glycyrrhizae Radix, Persicae Semen, Salviae Radix, Angelicae Gigantis Radix, Zanthoxyli Fructus, Ginseng Radix Alba, Cnidii Rhizoma, and Carthami Flos, are known to enhance blood circulation and have wound healing or anti-inflammatory effects. These pharmacological actions prompted us to investigate whether these herbs might stimulate hair growth. Thus, using a mixture of their extracts called SPELA 707, we investigated their effects and found that SPELA 707 possessed significant hair cycle converting activity from the telogen phase to the anagen phase in C3H mice. Furthermore, we found that SPELA 707 enhanced the hair density in subjects with hair loss and also promoted the conversion of hair into the anagen phase in subjects with androgenetic alopecia. In addition, hair growth promotion effect of SPELA 707 occurred through inhibition of steroid 5 alpha-reductase activity, which is known to block hair growth. Taken together, these results suggest that SPELA 707 has a potential to be used for the treatment of hair loss.