• 한국식품영양학회지
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• 제25권4호
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• pp.888-896
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• 2012

Considering the dearth of information regarding the medicinal properties of Luffa cylindrica, we assessed the antioxidative, antimutagenic and hyperplasia inhibitory activity of cancer cells from Luffa cylindrica extracts by employing biological and biochemical assays. Ethanol extracts of Luffa cylindrica inhibited MDA-BSA (malondialdehyde-bovine serum albumin) conjugation reaction ($66.38{\pm}2.65$), DPPH (1,1-diphenyl-2-picryl-hydrazyl) radical production ($60.13{\pm}0.42$) and lipid peroxidation ($56.04{\pm}3.24$). In this study, Luffa cylindrica is believed to exert possible antioxidative effects. The direct and indirect antimutagenic effects of the ethanol extracts of Luffa cylindrica were examined by the Ames test using Salmonella typimurium TA98 and TA100. The inhibitory effects on indirect and direct mutagenicity shows an weak tendency, particularly in direct mutagenicity mediated by 2-nitrofluorene in Salmonella typimurium TA98 ($5.82{\pm}5.74$) and in indirect mutagenicity mediated by 2-anthramine in Salmonella typimurium TA100 ($5.76{\pm}2.15$). The ethanol extracts of Luffa cylindrica on cancer cell hyperplasia inhibitory activity via MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay exerted cytotoxic effects on Hela cells ($55.83{\pm}3.83$) and MCF-7 cells ($33.03{\pm}2.09$), which were used in this study. Based on these results, it believed that the ethanol extracts of Luffa cylindrica have antioxidative capacities as well as hyperplasia inhibitory activity of cancer cells. Furthemore, Luffa cylindrica is a candidate for the prevention and dietetic treatment of chronic diseases and for the development of functional food.

• 약학회지
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• 제54권6호
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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 ($IC_{50}$: $2.4{\times}10^{-7}M$).

• Molecules and Cells
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• 제27권3호
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• pp.345-350
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• 2009

We previously reported that flavone induces embryonic lethality in Caenorhabditis elegans, which appeared to be the result of cell cycle arrest during early embryogenesis. To test this possibility, here we examined whether flavone inhibits the activity of a key cell cycle regulator, CDC-25.1 in C. elegans. A gain-of-function cdc-25.1 mutant, rr31, which exhibits extra cell divisions in intestinal cells, was used to test the inhibitory effects of flavone on CDC-25 activity. Flavone inhibited the extra cell divisions of intestinal cells in rr31, and modifications of flavone reduced the inhibitory effects. The inhibitory effects of flavone on CDC-25.1 were partly, if not completely, due to transcriptional repression.

• Nutrition Research and Practice
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• 제16권4호
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• pp.419-434
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• 2022

BACKGROUND/OBJECTIVES: Benign prostatic hyperplasia (BPH) is the most common prostate disease and one of the most common chronic diseases caused by aging in men. On the other hand, there has been no research on BPH using Abeliophyllum distichum Nakai (A. distichum). Therefore, this study investigated the effects of A. distichum on BPH. MATERIALS/METHODS: A. distichum leaves were extracted with distilled water, 70% ethanol, and 95% hexane as solvents. Subsequently, the inhibitory effects of each A. distichum extract on androgen receptor (AR) signaling were evaluated in vitro. The testosterone-induced BPH model was then used to confirm the efficacy of A. distichum leaves in 70% ethanol extract (ADLE). RESULTS: ADLE had the strongest inhibitory effect on AR signaling. A comparison of the activity of ADLE by harvest time showed that the leaves of A. distichum harvested in autumn had a superior inhibitory effect on AR signaling to those harvested at other times. In the BPH rat model, the administration of ADLE reduced the prostate size and prostate epithelial cell thickness significantly and inhibited AR signaling. Subsequently, the administration of ADLE also reduced the expression of growth factors, thereby inactivating the PI3K/AKT pathway. CONCLUSIONS: An analysis of the efficacy of ADLE to relieve BPH showed that the ethanol extract grown in autumn exhibited the highest inhibitory ability of the androgen-signaling related factors in vitro. ADLE also inhibited the expression of growth factors by inhibiting the expression of the androgen-signaling related factors in vivo. Overall, ADLE is proposed as a functional food that is effective in preventing BPH.

• 한국식품영양과학회지
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• 제43권2호
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• pp.318-322
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• 2014

본 연구에서는 울금(Curcuma longa L.)의 다양한 추출물을 대상으로 5-alpha reductase의 활성 저해 정도를 측정하였다. 5-Alpha reductase는 T에서 활성형 남성호르몬인 DHT로 전환을 담당하며, 전립선비대에서는 혈액에서 DHT 농도가 높다. Rat의 전립선조직 균질액과 5-alpha reductase를 과발현시킨 LNCaP 세포 균질액을 대상으로 측정한 결과, $100{\mu}g/mL$의 농도에서 울금의 열수추출물(CL-HW)과 20% 에탄올추출물(CL-E20)이 5-alpha reductase 활성을 효과적으로 저해하였다. 특히 CL-HW는 $100{\mu}g/mL$의 농도에서 80% 이상의 유의적 억제효과를 보였으며, CL-E20은 $50{\mu}g/mL$의 농도부터 80% 이상의 감소효과를 보였다. 이 같은 결과에서 CL-HW 및 CL-E20은 5-alpha reductase의 억제활성이 있으며, 이는 전립선비대 치료소재로 개발될 수 있는 가능성이 있음을 제안한다.

• 대한본초학회지
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• 제38권2호
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• pp.27-34
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• 2023

Objectives : Currently, the benign prostatic hyperplasia (BPH) is one of the most common urogenital disorder in old men. We were performed to determine the effects of abietic acid (AC), component of pine resin, in benign prostatic hyperplastic Sprague-Dawley rat (SD rat) induced by testosterone injection (IP). Methods : We monitored body weights in SD rat at start and end date of experiment. After end of experiment, the prostate weights were measured in SD rats. Glutamic oxaloacetic transaminase (GOT) and glutamic pyruvic transaminase (GPT) levels was performed in serum. And we determined the 5-alpha reductase Ⅱ activity, testosterone levels, and dihydrotestosterone levels in prostate tissue and serum using ELISA kit. Results : As results, the prostate wights were increased in BPH group compared to normal group and were decreased in fina, AC30, and AC 50 groups, respectively. Serum GOT levels were decreased in AC50 group compared to BPH group. And Serum GPT levels of AC30 and AC50 groups were lower than BPH group. In addition, the 5-alpha reductase Ⅱ activity, testosterone levels, and dihydrotestosterone levels were decreased the fina, AC10, AC30, and AC 50 groups contrast to the BPH group. Furthermore, 5-alpha reductase Ⅱ activity, testosterone levels, and dihydrotestosterone levels were decreased dose dependent in AC groups compared to BPH group. Conclusion : These results suggest that AC could be used as a potential material for the treatment of BPH by decreasing the androgen levels in benign prostatic hyperplasia model rats.

• Natural Product Sciences
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• 제25권3호
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• pp.238-243
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• 2019

In this study, the marker compounds of Curcumae Rhizoma (CR) were simultaneously quantified by high-performance liquid chromatography equipped with a photodiode array detector and the anti-inflammatory effects of CR extract and marker compounds in human benign prostatic hyperplasia epithelial-1 (BPH-1) cell lines were investigated. The marker components (4S,5S)-(+)-germacrone-4,5-epoxide, furanodienone, and germacrone, were separated on Gemini $C_{18}$ columns ($250mm{\times}4.6mm$, $5{\mu}m$) at $40^{\circ}C$ by using a gradient of two mobile phases eluting at 1.0 mL/min. Prostaglandin $E_2$ ($PGE_2$) levels in Human BPH-1 cells were determined with an ELISA kit. The coefficients of determination in a calibration curve of each analyte were all 0.9997. The limits of detection and quantification of the three compounds were $0.10-0.32{\mu}g/mL$ and $0.30-0.98{\mu}g/mL$, respectively. The content of three compounds, (4S,5S)-(+)-germacrone-4,5-epoxide, furanodienone, and germacrone, in the CR sample were found to be 5.79 - 5.92 mg/g, 4.72 - 4.86 mg/g, and 1.06 - 1.09 mg/g, respectively. Regarding pharmacological activity against benign prostatic hyperplasia, CR and its components significantly suppressed $PGE_2$ levels of BPH-1 cells. The established analysis method will help to improve quality assessment of CR samples and related products. In addition, CR and its components exhibit antiinflammatory activity in BPH-1 cells, suggesting the inhibitory efficacy of these compounds against the pathogenesis of BPH.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1997년도 춘계학술대회
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• pp.100-100
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• 1997

To treat peptic ulcer diseases, many potent proton pump inhibitors have been developed for suppressing the gastric acid secretion in clinical patients. However, most of these agents have common irreversible mechanisms against H$\^$+/, K$\^$+/-ATPase which might be the cause of hypergastrinemia and ECL cell hyperplasia. Therefore, the development of new reversible inhibitors is prompted. In this study, we investigated the inhibitory mechanism of a newly synthesized proton pump inhibitor, YJA20379-8 using lyophilized hog gastric microsomes. YJA20379-8 inhibited K$\^$+/-stimulated H$\^$+/K$\^$+/-ATPase activity uncompetitively with respect to K$\^$+/, and in the other hand, showed competitive inhibitory pattern with ATP, respectively. From these data, we suggest that YJA20379-8 may be a proton pump inhibitor with a new inhibitory mechanism.

• 대한한의학회지
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• 제42권4호
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• pp.10-24
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• 2021

Objectives: Yongdamsagan-tang (YST) and Paljung-san (PJS) in traditional medicine and finasteride in modern medicine are used to treat benign prostatic hyperplasia (BPH). In recent, the use of combination herbal remedies with conventional drugs has been increasing. Therefore, we investigated the anti-inflammatory effects of these drugs to treat BPH and the influence of herbal formulas on finasteride metabolism. Methods: The inhibitory effects of the herbal formulas and finasteride on the production of inflammatory mediators and cytokines were determined in lipopolysaccharide (LPS)-treated RAW 264.7 cells. Additionally, the influence of herbal formulas on activities of human drug metabolizing enzymes (DMEs) was assessed using human microsomal enzymes. Results: We observed that YST, PJS and finasteride inhibited the production of nitric oxide (NO), prostaglandin E₂ (PGE₂) and interleukin-6 (IL-6) in RAW 264.7 cells. The half maximal inhibitory concentration (IC₅₀) of YST on PGE₂ production was calculated to be below 25 ㎍/mL. YST inhibited the activity of uridine diphosphate-glucuronosyltransterase (UGT) 1A4 with an IC₅₀ value of 49.35 ㎍/mL. The activities of cytochrome P450 (CYP) 1A2, CYP2B6, CYP2C19, CYP3A4, and UGT1A1 were inhibited by PJS (IC₅₀ < 100 ㎍/mL, each). Although PJS and YST inhibited the activities of CYP3A4 and UGT1A4, respectively, these formulas may not influence the metabolism of finasteride because the IC₅₀ values of herbal formulas on DMEs are too high to affect metabolism. Conclusions: Our results suggest that the combination of finasteride and YST or PJS might not influence their drug metabolism and that the drugs may have synergistic effects against BPH.

• Molecules and Cells
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• 제22권1호
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• pp.104-112
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• 2006

We previously reported that DA-9601, ethanol herbal extract of Artemisia asiatica, inhibited histamine and leukotriene releases in guinea pig lung mast cells activated with specific antigen/antibody reaction. This study aimed to evaluate the inhibitory effect of DA-9601 on the OVA-induced airway inflammation in allergic asthma mouse model. BALB/c mice were sensitized and challenged with OVA. DA-9601 was administered orally 1 h before every local OVA-challenge. OVA-specific serum IgE was measured by ELISA, recruitment of inflammatory cells in BAL fluids and lung tissues by Diff-Quik and H&E staining, respectively, the expressions of CD40, CD40L and VCAM-1 by immunohistochemistry, goblet cell hyperplasia by PAS staining, activities of MMPs by gelatin zymography, expressions of mRNA and proteins of cytokines by RT-PCR and ELISA, activities of MAP kinases by western blot, and activity of NF-${\kappa}B$ by EMSA. DA-9601 reduced IgE level, recruitment of inflammatory cells into the BAL fluid and lung tissues, expressions of CD40, CD40L and VCAM-1 molecules, goblet cell hyperplasia, MMPs activity, expressions of mRNA and productions of various cytokines, activities of MAP kinases and NK-${\kappa}B$ increased from OVA-challenged mice. These data suggest that DA-9601 may be developed as a clinical therapeutic agent in allergic diseases due to suppressing the airway allergic inflammation via regulation of various cellular molecules expressed by MAP kinases/NF-${\kappa}B$ pathway.