• Biomedical Science Letters
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• v.24 no.3
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• pp.263-269
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• 2018

This study aims to investigate the biological activities related to hair loss of short anti-oxidant peptides (DK peptides) $5{\alpha}$-reductase inhibition and anti-oxidation. The series of DK peptides were generated amphipathic helical properties using leucines, lysines and tryptophan residues. Cell viability and free radical scavenging activities were performed using 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl-tetrazolium bromide (MTT) and 2, 2-diphenyl-1-picrylhydrazyl (DPPH) assay, respectively. The DK peptides were investigated for inhibitory activity against $5{\alpha}$-reductase. Antioxidant activities were determined by means of, 2, 2-diphenyl-1-picrylhydrazyl (DPPH) assays. All peptides could inhibit $5{\alpha}$-reductase in lipopolysaccharide-stimulated macrophage. In conclusion, DK peptides was suggested as the most attractive ingredients for improving hair loss, because of the high inhibitory against $5{\alpha}$-reductase inhibition.

• Journal of the Korean Society of Food Science and Nutrition
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• v.43 no.2
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• pp.318-322
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• 2014

5-Alpha reductase II, which converts testosterone (T) to dihydrotestosterone (DHT), is a crucial enzyme II in benign prostatic hyperplasia. Inhibitory effects of Curcuma longa L. (CL) extracts on 5-alpha reductase II activity were investigated in rat prostate tissue homogenates as well as LNCaP cells expressing human 5-alpha reductase II. Hot water extract (CL-HW) of Curcuma longa L. significantly inhibited 5-alpha reductase activity by over 80% at a concentration of $100{\mu}g/mL$, whereas 20% ethanol extracts (CL-E20) of Curcuma longa L. exhibited significant inhibitory activity from $50{\mu}g/mL$. These results indicated that Curcuma longa L is a potent 5-alpha reductase II inhibitor for benign prostatic hyperplasia treatment.

• Korean Journal of Pharmacognosy
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• v.31 no.2
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• pp.245-248
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• 2000

As a series of the studies on cultivated Korean rhubarb rhizomes (Rheum undulatum), five stilbene derivatives were screened for inhibitory activity against $5{\alpha}-reductase$. Of these, desoxyrhapontigenin, rhapontigenin, and piceatannol exhibited inhibition, whereas, two other stilbene glycosides, rhaponticin and $piceatannol-3'-O-{\beta}-D-glucopyranoside$ did not show the inhibition.

• Natural Product Sciences
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• v.5 no.2
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• pp.97-103
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• 1999

The enzyme steroid $5{\alpha}-reductase$ is responsible for the conversion of testosterone into the most potent androgen dihydrotestosterone (DHT). In man, this steroid acts on a variety of androgen-responsive target tissues to mediate such diverse endocrine processes as male sexual differentiation in the fetus and prostatic growth in men. Androgen levels in the prostate may influence carcinogenesis in this organ. The use of a $5{\alpha}-reductase$ inhibitor, finasteride, in the chemoprevention of prostate cancer is being evaluated in a clinical trial and have been used successfully for treatment of benign prostatic hyperplasia. Therefore, for the discovery of $5{\alpha}-reductase$ type 2 inhibitors, we have evaluated the inhibitory effects of solvent fractionated extracts of natural products on $5{\alpha}-reductase$ type 2 activity. We have tested approximately 80 kinds of natural products after partition into n-hexane, ethyl acetate and aqueous layers from 100% methanol extracts of plants. The ethyl acetate fractions of Perilla sikokiana $(seed,\;IC_{50}\;:\;6.2\;ug/ml)$, Sophora flavescens $(root,\;IC_{50}\;:\;8.9\;ug/ml)$, and Angelica tenuissima $(root,\;IC_{50}\;:\;11.7\;ug/ml)$ revealed inhibitory effects on $5{\alpha}-reductase$ 2 activity in LNCaP cells. The effective ethyl acetate fractions of Perilla sikokiana, Sophora flavescens, Hydnocarpus anthelmintica, and Angelica tenuissima were subfractionated by column chromatography and tested. The subfractions $F4\;(IC_{50}\;:\;1.1\;ug/ml),\;F5\;(IC_{50}\;:\;2.0\;ug/ml),\;and\;F6\;(IC_{50}\;:\;5.8\;ug/ml)$ of the ethyl acetate fraction of Perilla sikokiana and the subfraction $F8\;(IC_{50}\;:\;5.3\;ug/ml)$ of the ethyl acetate fraction of Sophora flavescens displayed greater inhibition of $5{\alpha}-reductase$ type 2 than did finasteride in LNCaP cells. These active fractions are under the process of further sequential fractionation to find the effective pure compounds against $5{\alpha}-reductase$ 2 activity.

• YAKHAK HOEJI
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• v.54 no.6
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• pp.466-473
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• 2010

A series of $3{\beta}$-substituted 5-androstene-$17{\beta}$-carboxamides were synthesized from analogs of $3{\beta}$-hydroxy-5-androstene-$17{\beta}$-carboxylic acid (1) with tert-butylamine, N,N-diethylamine and 3-aminopyridine and some compounds were epoxidized with mCPBA. A rat prostate testosterone $5{\alpha}$-reductase inhibitory activity of synthesized compounds was assessed by radioimmunoassay using [1,2,6,7-3H]-testosterone as substrate. All synthesized compounds showed lower activity than finasteride and the N-(3-pyridino)-$3{\beta}$-carboxycarbonyloxy-5-androstene-$17{\beta}$-carboxamide (12) showed weak inhibitory activity ($IC_{50}$: $2.4{\times}10^{-7}M$).

• The Journal of Internal Korean Medicine
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• v.30 no.2
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• pp.327-337
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• 2009

Objective : In benign prostatic hyperplasia, dihydrotestosterone acts as a potent cellular androgen and promotes prostate growth. Inhibiting enzyme 5${\alpha}$-reductase, which is involved in the conversion of testosterone to the active form dihydrotestosterone, reduces excessive prostate growth. Recently Scutellaria baicalensis has been related reports about the effect of baicalein on anti-proliferation of the prostate gland. In this study, we investigated the effects of Scutellaria baicalensis on cytopathological alterations and expression of 5${\alpha}$-reductase in the rat model of benign prostatic hyperplasia induced by castration and testosterone treatment. Methods : Sprague-Dawley rat were treated with testosterone after castration for induction of experimental benign prostatic hyperplasia, which is similar to human benign prostatic hyperplasia in histopathological profiles. Scutellaria baicalensis as an experimental specimen, and finasteride as a positive control, were administered orally. The prostates were evaluated by histopathological changes, testosterone levels, and the expression of 5${\alpha}$-reductase genes. Results : While prostates of control rats revealed severe acinar gland atrophy and stromal proliferation, the rats treated with Scutellaria baicalensis showed a diminished range of tissue damage. In the reverse transcription-polymerase chain reaction(RT-PCR) of 5${\alpha}$-reductase genes. Scutellaria baicalensis inhibited the expression of 5${\alpha}$-reductase genes. Conclusions : These findings suggest that Scutellaria baicalensis may protect glandular epithelial cells and also inhibit stromal proliferation in association with the suppression of 5${\alpha}$-reductase. From theses results, we suggest that Scutellaria baicalensis could be a useful remedy agent for treating benign prostatic hyperplasia.

• Korean Journal of Oriental Medicine
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• v.16 no.2
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• pp.131-141
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• 2010

Objective : Benign prostatic hyperplasia(BPH) is one of the most common diseased among elderly men. BPH can be treated with alpha-1 adrenergic blocker or $5{\alpha}$-reductase inhibitor(Finasteride) that reduces serum dihydrotestosterone(DHT). Phellodendri Cortex Ex has been broad studied on its chemical components, pharmacological activity, and clinical effects on anti-inflammation, anti-allergy, anti-tumor, immunity, antibacteria and other bioactivities. In this study, we investigated the therapeutic effects and action mechanism of Phellodendri Cortex Ex with a BPH induced by castration and testosterone treatment. Methods : Sprague-Dawley rats were treated with testosterone after castration for induction of experimental benign prostatic hyperplasia, which is similar to human benign prostatic hyperplasia in histopathological profiles. Phellodendri Cortex as an experimental specimen, and Finasteride as a positive control, were administered orally. The prostates were evaluated by histopathological changes, and the expression of $5{\alpha}$-reductase genes. Results : While prostates of control rats revealed severe acinar gland atrophy and stromal proliferation, the rats treated with Phellodendri Cortex Ex showed a diminished range of the tissue damage. In the reverse transcription-polymerase chain reaction(RT-PCR) of $5{\alpha}$-reductase genes, Phellodendri Cortex inhibited the expression of $5{\alpha}$-reductase genes. Conclusions : These findings suggest that Phellodendri Cortex Ex may protect the glandular epithelial cells and also inhibit stromal proliferation in association with the suppression of $5{\alpha}$-reductase. From these results, we suggest that Phellodendri Cortex Ex could be a useful agent for treating the benign prostatic hyperplasia.

• Journal of Physiology & Pathology in Korean Medicine
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• v.31 no.6
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• pp.356-361
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• 2017

Houttuyniae Herba is widely used as a cosmetic for enhancing hair growth, and study on promoting mouse hair growth has also been reported. However, studies on the effects of the Houttuyniae Herba on dermal papilla (DP) cells, which play an important role in hair growth, are not well known. For this reason, we studied the effect of Houttuyniae Herba on DP cells. The strong antioxidant activity of Houttuyniae Herba was confirmed by ABTS assay. In the MTS assay, cell viability was reduced to 94.5% in DP cells by treatment of 2 mg/ml concentration of Houttuyniae Herb and cytotoxicity was not observed at 1 mg/ml concentration. The mRNA expression levels of Bone morphogenetic pretein (BMP6), fibroblast growth factor 7 (FGF7), FGF10, and ${\beta}$-galactosidase genes, which are involved in hair growth cycle and hair loss induction, were measured by quantitative RT-PCR after Houttuyniae Herbtreatment. Houttuyniae Herb did not significantly affect mRNA expression of BMP6, FGF7, FGF10, and ${\beta}$-catenin, which are important factors for regulating the hair cycle, including type 1 $5{\alpha}$-reductase. However, mRNA expression of type 2 $5{\alpha}$-reductase, the major cause of male hair loss, was significantly reduced to 56.1% by treatment of Houttuyniae Herbtreatment. Taken together, these results suggest that the Houttuyniae Herbtreatment can help to treat lair loss through removing free radicals and suppression of the expression level of type 2 $5{\alpha}$-reductase in DP cells.

• Development and Reproduction
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• v.11 no.3
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• pp.187-193
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• 2007

Ethane 1,2-dimethane sulfonate(EDS), a Leydig cell specific toxicant, has been widely used to create the reversible testosterone withdrawal rat model. Though the maintenance of epididymal structure and function is highly dependent on the testosterone secreted from testis, its derivatives, dihydroxytestosterone(DHT) and estrogen, might have crucial roles. The aim of present study was to monitor the expression patterns of sex steroid receptors, cytochrome P450 aromatase(P450arom) and $5{\alpha}$-reductase in the rat epididymis up to 7 weeks after EDS injection. Adult male rats($350{\sim}400g$) were injected with a single does of EDS(75 mg/kg i.p.) and sacrificed on weeks 0, 1, 2, 3, 4, 5, 6 and 7. The transcriptional activities of the target genes were evaluated by semi-quantitative RT-PCRs. The transcript level of estrogen receptor alpha($ER{\alpha}$) in EDS group was significantly higher than control level on week 1(P<0.01). After week 2, there was no significant difference in $ER{\alpha}$ levels between EDS group and control. The transcript level of estrogen receptor beta($ER{\beta}$) in EDS group was significantly higher than control level on week 1(P<0.05), lowered on weeks 2 and 3(P<0.05 and P<0.01, respectively), fluctuated during weeks 4 and 6, and elevated on week 7(P<0.05). The androgen receptor (AR) message levels increased significantly week 2(P<0.01), then returned to control level on week 3. In contrast, expression of cytochrome P450 aromatase(P450arom) decreased sharply during weeks $1{\sim}3$(P<0.01 on weeks 1 and 2; P<0.05 on week 3), then went back to control level on week 4. The mRNA level of $5{\alpha}$-reductase type 2($5{\alpha}$-RT2) increased significantly on week 4(P<0.01), then returned to control level. The present study indicated that EDS administration could induce reversible alterations in the transcriptional activities of sex steroid hormone receptors and androgenconverting enzymes in rat epididymis. EDS injection model will be useful to clarify the regulation mechanism of mammalian epididymal physiology.

• Journal of Applied Biological Chemistry
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• v.49 no.1
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• pp.24-27
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• 2006

Four ursane-type triterpenoids, 2${\alpha}$,3${\alpha}$,19${\alpha}$-trihydroxy-24-norurs-4(23),12-dien-28-oic acid (1), 4(R),23-epoxy-2${\alpha}$,3${\alpha}$,19${\alpha}$-trihydroxy-24-norurs-12-en-28-oic acid (2), myrianthic acid (3), and tormentic acid (4), and a phenolic compound, ethyl gallate (5), from an EtOAc-soluble extract of the stems of Rumex japonicus, were subjected to in vitro bioassays to evaluate advanced glycation end products (AGEs) and rat lens aldose reductase (RLAR) inhibitory activity. Compounds 1 and 5 exhibited a significant inhibitory activity on AGEs formation with $IC_{50}$ value of 87 ${\mu}M$ and on RLAR with $IC_{50}$ value of 14.3 ${\mu}M$, respectively. Ethyl gallate (5) was isolated for the first time from this plant.