• Title/Summary/Keyword: $HT_7$

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Suppressive effects on the expression of cyclooxygenase-2 and inducible nitric oxide synthase by a natural sesquiterpenoid in lipopolysaccharide-stimulated mouse macrophage cells

  • Min, Hye-Young;Park, Hyen-Joo;Park, Eun-Jung;Lee, Sang-Kook
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2003.11a
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    • pp.101-101
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    • 2003
  • Prostaglandins (PGs) and nitric oxide (NO) produced by inducible cyclooygenase (COX-2) and nitric oxide synthase (iNOS), respectively, have been implicated as important mediators in the process of inflammation and carcinogenesis. On this line, the potential COX-2 or iNOS inhibitors have been considered as anti-inflammatory and cancer chemopreventive agents. In our continuing efforts of searching for novel cancer chemopreventive agents from natural products, we isolated natural sesquiterpenoids as potential COX-2 and iNOS inhibitors in cultured lipopolysaccharide (LPS)-activated mouse macrophage RAW 264.7 cells. Alantolactone, a natural eudesmane-type sesquiterpenoid, exhibited a potent inhibition of COX-2 (IC50 = 0.4 $\mu\textrm{g}$/$m\ell$) and iNOS activity (IC50 = 0.08 $\mu\textrm{g}$/$m\ell$) in the assay system determined by PGE2 and NO accumulation, respectively. The inhibitory potential of alantolactone on the PGE2 and NO production was well coincided with the suppression of COX-2 and iNOS protein and mRNA expression in LPS-induced macrophages. Furthermore, alantolactone inhibited NF-kB but not AP-l binding activity on nuclear extracts evoked by LPS-stimulated macrophage cells, suggesting the possible involvement of NF-kB in the regulation of COX-2 and iNOS expression. In further study with COX-2-expressing human colon HT-29 cells, alantolactone inhibited the cell proliferation, down-regulated COX-2, and inhibited the ERK phosphorylation in the early time. These results suggest that a natural sesquiterpenoid alantolactone might be a potential lead candidate for further developing COX-2 or iNOS inhibitor possessing cancer chemopreventive or anti-inflammatory activity

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Evaluation of the bioequivalence of Sumatriptan in healthy volunteers (이미그란 정 50 mg에 대한 수마트란 정의 생물학적 동등성 평가)

  • Yun, Hwi-Yeol;Baek, In-Hwan;Kwon, Kwang-Il
    • Korean Journal of Clinical Pharmacy
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    • v.15 no.2
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    • pp.160-164
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    • 2005
  • 수마트립탄은 뇌혈관에 분포되어 있는 5-HT1B/1D수용체에 특이적이고 선택적으로 작용하여 뇌혈관 수축 작용을 나타내어 편두통의 치료에 널리 쓰이는 약물이다. 본 연구는 수마트립탄 제제인 이미그란(50 mg tablet, GSK사)을 대조약으로 하여 시험약인 명인 제약의 수마트란 50mg정의 생물학적 동등성 평가를 하기 위해 22명의 건강한 지원자를 모집하였다. 지원자를 두 군으로 나누어 1정씩 투여하였고 $2{\times}2$ 교차시험을 실시하였다. 수마트립탄의 혈장 중의 농도를 정량하기 위하여 발리데이션된 HPLC/FD를 사용하였다. 채혈 시간은 투약 전 및 투약 후 0.5, 1, 1.5, 2, 2.5, 3,4, 5, 7, 9, 12시간에 걸쳐 총 12시점에 걸쳐 시행하였다. 생물학적 동등성을 판정하기 위한 파라미터로 12시간까지의 혈장 중 농도 곡선 하 면적$(AUC_{12hr})$ 최고 혈중 농도$(C_{max})$를 사용하였다. $AUC_{12hr}$의 평균은 $137.87ng{\cdot}ml/hr$(시험약)과 $130.12ng{\cdot}ml/hr$(대조약)으로 나타났다. $C_{max}$의 경우 각 각 29.30 ng/ml(시험약)과 29.25ng/m1(대조약)으로 관찰되었다. $AUC_{12hr}$의 경우 로그변환 한 평균치 차의 90% 신뢰구간이 log0.95-log1.24이었고, $C_{max}$의 경우 log0.90-log1.149로 계산되 어 두 항목 모두 log0.8-log1.25이어야 한다는 식품의 약품 안전청 과 FDA의 기준을 모두 만족시켰다. 이상의 결과를 종합하면 시험약 수마트란 정 50 mg은 대조약 이미그란 정 50 mg에 대하여 생물학적으로 동등한 것으로 판정되었다.

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Apoptosis Induction, Cell Cycle Arrest and in Vitro Anticancer Activity of Gonothalamin in a Cancer Cell Lines

  • Alabsi, Aied M.;Ali, Rola;Ali, Abdul Manaf;Al-Dubai, Sami Abdo Radman;Harun, Hazlan;Kasim, Noor H. Abu;Alsalahi, Abdulsamad
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.10
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    • pp.5131-5136
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    • 2012
  • Cancer is one of the major health problems worldwide and its current treatments have a number of undesired adverse side effects. Natural compounds may reduce these. Currently, a few plant products are being used to treat cancer. In this study, goniothalamin, a natural occurring styryl-lactone extracted from Goniothalamus macrophyllus, was investigated for cytotoxic properties against cervical cancer (HeLa), breast carcinoma (MCF-7) and colon cancer (HT29) cells as well as normal mouse fibroblast (3T3) using MTT assay. Fluorescence microscopy showed that GTN is able to induce apoptosis in HeLa cells in a time dependent manner. Flow cytometry further revealed HeLa cells treated with GTN to be arrested in the S phase. Phosphatidyl serine properties present during apoptosis enable early detection of the apoptosis in the cells. Using annexin V/PI double staining it could be shown that GTN induces early apoptosis on HeLa cells after 24, 48 and 72 h. It could be concluded that goniothalamin showing a promising cytotoxicity effect against several cancer cell lines including cervical cancer cells (HeLa) with apoptosis as the mode of cell death induced on HeLa cells by Goniothalamin was.

Antioxidant and Anticancer Activities of Poria cocos and Machilus thunbergii Fermented with Mycelial Mushrooms (버섯균사체로 발효시킨 복령과 후박의 항산화 및 항암효과)

  • Shon, Mi-Yae
    • Food Industry And Nutrition
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    • v.12 no.2
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    • pp.51-57
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    • 2007
  • 한국산 복령과 후박의 이용성 확대를 위하여 각각 추출물의 ABTS와 DPPH라디칼의 소거능, 환원력의 항산화능 효과 및 인체암 세포주의 항암활성에 대하여 조사하였다. 복령과 후박을 버섯균사체로 발효시킨 한약 추출액의 항산화활성(ABTS와 DPPH 라디칼소거, 환원력)은 시료 추출물의 농도가 증가할수록 비례적으로 증가하였으며, DPPH 라디칼 소거활성은 ABTS보다 비교적 높게 나타났고, 원료후박 추출물($21.16{\sim}24.68%$)은 원료복령 추출물($45.46{\sim}49.63%$)에 비하여 약 2배 이상 높았다. 복령 시료 추출물의 농도별에 따른 환원력은 원료 복령($0.55{\sim}0.63$)에 비하여 동충하초, 팽이버섯 및 큰 느타리 균사체로 발효시킨 시료($0.50{\sim}0.62$)의 흡광도로 서로 비슷한 증가를 나타내었고, 후박 시료 추출물의 농도별에 따른 환원력은 원료 후박 추출물($0.98{\sim}1.06$)이 3가지의 버섯 균사체 발효후박 추출물($0.76{\sim}1.01$)에 비하여 약간 높았다. 자궁경부암세포(HeLa)와 대장암세포(HT-29)는 원료복령과 후박의 추출물이 각각의 발효한약에 비하여 저해활성이 높았다. 간암세포(HepG2)는 $200{\mu}g/assay$ 농도에서 팽이버섯 균사체 발효복령의 추출물이 가장 높았는데, 원료복령과 동충하초 및 큰 느타리에 비하여 각각 1.79, 1.35, 1.03배 높은 저해활성을 나타내었다. 그리고 팽이버섯과 동충하초 균사체를 배양한 발효후박에서 각각 $11.39{\sim}53.92%$, $10.71{\sim}50.21%$ 범위였으며, 원료후박에 비하여 $200{\mu}g/assay$ 농도에서 각각 2.21배, 2.05배 높은 저해활성을 나타내었다. 유방암세포(MCF-7)는 발효복령 추출물의 저해활성이 팽이버섯 균사체($58.35{\sim}72.87%$)에서 가장 높았으며, 큰 느타리버섯($61.04{\sim}67.66%$)과 동충하초($39.74{\sim}66.40%$) 및 원료복령($50.32{\sim}69.24%$)은 서로 비슷하였다.

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Effects of Hair Tonic and Food including Korean Medicinal Herbs on Hair Growth in an Alopecia Model of C57BL/6 Mice (한약재 함유 헤어토닉 및 식품이 C57BL/6 마우스의 탈모 모델에서 모발성장에 미치는 영향)

  • Choi, Hye-Min;Hwang, Su-Jung;Lee, Jin-Sang;Do, Eun-Ju;Kim, Mu-Young;Kim, Mi-Ryeo
    • The Korea Journal of Herbology
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    • v.26 no.1
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    • pp.119-124
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    • 2011
  • Objective : This study was carried out to investigate effect of korean medicinal herbs-included hair tonic (MHT) and food (MF) on hair growth in an alopecia model of C57BL/6 mice. Methods : Six-weeks old mice were given laboratory rodent chow diet for 1 week. Then, we used a depilatory for hair removal on mice. The next day, mice were randomized and separated in 3 groups of 6 mice; normal group (N, vehicle epidermal application+normal diet-treated group), positive control group (C, 3% minoxidil sulfate epidermal application+normal diet-treated group), and the treatment group (T, HT epidermal application+ MF diet-treated group). The hair regrowth was determined by photograph, which was taken at 7, 14 and 21 days. And scoring indices, hair density and hair thickness, were evaluated by Folliscope at same day. In addition, the hair regrowth was analyzed insulin-like growth factor (IGF-1) in the dorsal skin of mice. Results : As a result, not only external appearance but also hair density and hair thickness on dorsal skin were increased more in C, T groups than in N group at 21 days with mixed treatment. Therefore, distinct regrowth pattern is appeared by treatment of herbal tonic and natural food for 21 days. Also, the expressions of IGF-1 on dorsal skin were higher in C, T groups than in N group. Conclusion : These results suggested that this herbal hair tonic and natural food has hair growth promoting activities and may be useful for treatment of bald or alopecia.

An Ecological Analysis of Iron Status of Middle School Students in Seoul (중학생의 철분 영양 상태에 영향을 미치는 생태학적 변인 분석)

  • 최주현
    • Journal of Nutrition and Health
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    • v.30 no.8
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    • pp.960-975
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    • 1997
  • This study was carried out to evaluate the iron nutrition status of 212 middle school students(106 males and 106 females) residing in Seoul(13-14 years old ) using eating patterns and a measurement of anthropometrical determination and hematological indices. Fasting blood samples were taken from all subjects, serum iron (SI) and total iron binding capacity(TIBC) concentrations were measured, and transferrin saturation(TS) levels were calculated. Iron and other nutrient intakes were estimated by a semi-quantitative frequency questionnaire. The level of TS(%) which was calculated with TIBC and SI in females(20.4$\mu\textrm{g}$/dl) was significantly lower(p<0.050 than that of males (27.4$\mu\textrm{g}$/㎗). The prevalence of iron deficiency was found to be 36.7% when defined by TS(%) (<05%). Mean daily intake of total iron in the study subjects was 14mg and heme iron intake was 5.4mg(38.1%) . There was a significant negative correlation between the level of SI and the income level and a positive correlation with the level of TIBC and the income level. TIBC had a positive correlation with the anthropometric variables(Ht, Wt, BMI, RI and PIBW). SI and TS had a negative correlation with body fat percentage. There was a positive correlation between energy intake and TIBC only among females. The logistic regression analysis revealed that income level, body fat percentage , weight and energy intake were major determinants of low SI levels. Among the determinants of abnormal TIBC levels were weight , height, income level and energy intake. Finally , among those of low TS% were iron and energy intake and income level. These observations suggest that physical status, body fat percentage energy and iron intakes and income level are risk factors for iron-deficiency anemia among the middle school students in Seoul.

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Measurement of Body Fat by Impedance Technique (임피던스 방법을 이용한 체지방 측정)

  • Kim, Deok-Won;Song, Chul-Gyu;Hwang, Soo-Kwan
    • Journal of Biomedical Engineering Research
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    • v.13 no.2
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    • pp.133-140
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    • 1992
  • Bioelectrical Impedance method for measuring human body composition is based upon the principle that the electrical conductivity of the fat-free mass (FFM) is far greater than that of the (at. Deter- mination o( impedance was nlade in 30 healthy and obese men aged $40.9{\pm}14.7$yr (mean${\pm}$SD) and 25 healthy and obese women aged $44.0{\pm}10.2$ yr. A commercial impedance body fat analyzer was used with a four electrode arrangement that introduced a painless constant current(ImA at 50 kHz) into the body. Linear relationships were found between impudence values and FFM(r=-0.786) and between weight and FFM(r=0.837). Signigicant increases in the correlation coefficients were ob served when the predicator Hta/z was regressed against FFM(r=0.912) where Ht Is height and Z Is impedance. A linear regression equation, FFM=0.586(Htf/z) +0.317(Weight) -1.674(r=0.977), was found. The correlation coefficient of % body fat between the impedance and infrared methods was 0.898. These data Indicate that the bioelectrical impedance technique is a reliable and valld approach for the estimation of human body composition. This method Is safe, noninvasivr, prouides rapld measure menu, requires little operator skill and subject cooperation, and Os portable. Finally measurement of percent body fat was made possible using both the regression equation and a developed impedance measuring device which measures impedance between wrist and ankle.

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Inhibition of MMP-2 and MMP-9 activities by solvent-partitioned Sargassum horneri extracts

  • Karadeniz, Fatih;Lee, Seul-Gi;Oh, Jung Hwan;Kim, Jung-Ae;Kong, Chang-Suk
    • Fisheries and Aquatic Sciences
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    • v.21 no.6
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    • pp.16.1-16.7
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    • 2018
  • Background: Matrix metalloproteinases (MMPs) are linked with several complications such as metastasis of cancer progression, oxidative stress, and hepatic fibrosis. Brown seaweeds are being extensively studied for their bioactive molecule content against cancer progression. In this context, Sargassum horneri was reported to possess various bioactivities including antiviral, antimicrobial, and anti-inflammatory partly due to its phenolic compound content. Methods: In this study, potential of S. horneri was evaluated through anti-MMP effect in HT1080 fibrosarcoma cells. S. horneri crude extract was fractionated with organic solvents, namely, water ($H_2O$), n-buthanol (n-BuOH), 85% aqueous methanol (85% aq. MeOH), and n-hexane. The non-toxicity of fraction samples (Sargassum horneri solvent-partitioned extracts (SHEs)) was confirmed by cell-viability assay. SHEs were tested for their ability to inhibit MMP enzymatic activity through gelatin digestion evaluation and cell migration assay. Expressions of MMP-2 and MMP-9 and tissue inhibitors of MMP (TIMPs) were evaluated by reverse transcription and Western blotting. Results: All fractions inhibited the enzymatic activities of MMP-2 and MMP-9 according to gelatin zymography. Except $H_2O$ fraction, fractions hindered the cell migration significantly. All tested fractions suppressed both mRNA and protein levels of MMP-2, MMP-9, TIMP-1, and TIMP-2. Conclusion: Overall, current results suggested that S. horneri has potential to be a good source for anti-MMP agents, and further investigations are underway for better understanding of the action mechanism and isolation and elucidation of the bioactive molecules.

Antinociception Effect and Mechanisms of $Campanula$ $Punctata$ Extract in the Mouse

  • Park, Soo-Hyun;Sim, Yun-Beom;Lim, Soon-Sung;Kim, Jin-Kyu;Lee, Jin-Koo;Suh, Hong-Won
    • The Korean Journal of Physiology and Pharmacology
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    • v.14 no.5
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    • pp.285-289
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    • 2010
  • In the present study, the antinociceptive profiles of $Campanula$ $punctata$ extract were examined in ICR mice. The $Campanula$ $punctata$ contain a large dose of saponin. $Campanula$ $punctata$ extract administered orally (200 mg/kg) showed an antinociceptive effect as measured by the tail-flick and hot-plate tests. In addition, $Campanula$ $punctata$ extract attenuated the writhing numbers in the acetic acid-induced writhing test. Furthermore, the cumulative nociceptive response time for intrathecal (i.t.) injection of substance P ($0.7{\mu}g$) was diminished by $Campanula$ $punctata$ extract. Intraperitoneal (i.p.) pretreatment with yohimbine (${\alpha}_2$-adrenergic receptor antagonist) attenuated antinociceptive effect induced by $Campanula$ $punctata$ extract in the writhing test. However, naloxone (opioid receptor antagonist) or methysergide (5-HT serotonergic receptor antagonist) did not affect antinociception induced by $Campanula$ $punctata$ extract in the writhing test. Our results suggest that $Campanula$ $punctata$ extract shows an antinociceptive property in various pain models. Furthermore, this antinociceptive effect of $Campanula$ $punctata$ extract may be mediated by ${\alpha}_2$-adrenergic receptor, but not opioidergic and serotonergic receptors.

The Comparison Between Various Solvents Extracts of Mahaenggamsuk-tang on The Anti-oxidative, Anti-inflammatory and Neuro-protective Effects (마행감석탕 용매별 추출물의 항산화, 항염증 및 뇌세포보호 효과 비교)

  • Lee, Hwan;Han, Yu-Bin;Ko, Wonmin;Kim, Nayeon;Kim, Jungyoung;Lee, Dong-Sung;Woo, Eun-Rhan
    • Korean Journal of Pharmacognosy
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    • v.51 no.3
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    • pp.163-170
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    • 2020
  • Mahaenggamsuk-tang (MHGS) has been widely used in Korea and China for the treatment of various diseases. MHGS was constituted the Ephedrea Herba, Armenicae Semen, Glycyrrhizae Radix and Gypsum Fibrosum. In this study, we have made three different solvents extract as MHGS water extract (MHGS-W), MHGS 50% EtOH extract (MHGS-50E), and MHGS 100% EtOH extract (MHGS-100E). The MHGS-W, MHGS-50E and MHGS-100E showed the discernible difference patterns on HPLC analysis. Furthermore, MHGS-50E and MHGS-100E significantly increased the DPPH and ABTS radical scavenging effects than MHGS-W. In addition, the MHGS-50E and MHGS-100E also inhibited significantly nitric oxide (NO) and prostaglandin E2 (PGE2) production, and inducible nitric oxide synthase (iNOS) cyclooxygenase-2 (COX-2) protein expression in RAW264.7. On the other hand, MHGS-50E and MHGS-W showed remarkable protection on the HT22 cell via heme oxygenase (HO)-1, but MHGS-100E did not show. The results of this study proved that MHGS-50E has greater potential therapeutic uses by exerting antioxidant, anti-inflammatory and neuroprotective effects compared to MHGS-100E, MHGS-W. Our study suggests that the different solvent might be affected the biological activities when make the traditional herbal medicines including MHGS.