• Title/Summary/Keyword: active agent

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Ginseng saponins and the treatment of osteoporosis: mini literature review

  • Siddiqi, Muhammad Hanif;Siddiqi, Muhammad Zubair;Ahn, Sungeun;Kang, Sera;Kim, Yeon-Ju;Sathishkumar, Natarajan;Yang, Dong-Uk;Yang, Deok-Chun
    • Journal of Ginseng Research
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    • v.37 no.3
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    • pp.261-268
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    • 2013
  • The ginseng plant (Panax ginseng Meyer) has a large number of active ingredients including steroidal saponins with a dammarane skeleton as well as protopanaxadiol and protopanaxatriol, commonly known as ginsenosides, which have antioxidant, anticancer, antidiabetic, anti-adipocyte, and sexual enhancing effects. Though several discoveries have demonstrated that ginseng saponins (ginsenosides) as the most important therapeutic agent for the treatment of osteoporosis, yet the molecular mechanism of its active metabolites is unknown. In this review, we summarize the evidence supporting the therapeutic properties of ginsenosides both in vivo and in vitro, with an emphasis on the different molecular agents comprising receptor activator of nuclear factor kappa-B ligand, receptor activator of nuclear factor kappa-B, and matrix metallopeptidase-9, as well as the bone morphogenetic protein-2 and Smad signaling pathways.

Effect of imidazole receptor active agents on porcine myometrial contractility (돼지의 자궁근 수축성에 대한 몇가지 imidazole receptor active agents의 효과)

  • Shin, Dong-ho;Nah, Seung-youl;Kim, Jae-ha
    • Korean Journal of Veterinary Research
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    • v.37 no.2
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    • pp.331-338
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    • 1997
  • 최근 동물의 진통 및 진정을 목적으로 널리 사용되고 있는 imidazole 유도체인 clonidine, medetomidine, etomidate 등의 약물과 xylazine의 효과를 발정정지기의 척출 돼지 자궁근에서 검토하였다. Clonidine($10^{-8}{\sim}10^{-6}M$)이나 medetomidine($10^{-8}{\sim}10^{-6}M$)은 xylazine과 비슷한 정도로 용량의존적인 자궁근의 수축을 일으켰다. Clonidine, medetomidine, xylazine 등의 $EC_{50}$는 각각 24.7nM, 19.9nM, 45.1nM이었다. 그러나 etomidate는 $10^{-6}M$ 미만의 농도에서 반응이 거의 없었으며, $10^{-6}M$ 이상에서 수축반응을 일으켰다. 이들 agonists의 효과는 yohimbine($10^{-8}{\sim}10^{-6}M$), idazoxan($10^{-7}{\sim}10^{-5}M$), tolazoline($10^{-7}{\sim}10^{-5}M$) 등의 ${\alpha}_2-adrenoceptor$ antagonists에 의해서 차단되었으나, ${\alpha}_1-adrenoceptor$ antagonist인 prazosin ($10^{-6}M$)에 의해서는 차단되지 않았다. 또한 $Ca^{2+}-free$ medium이나 verapamil($10^{-5}M$)의 전처치에 의해서 이들 agonist의 효과가 완전히 차단되었다. 결론적으로 발정정지기의 돼지 자궁근에서 clonidine, medetomidine, etomidate, xylazine 등은 ${\alpha}_2-adrenoceptors$의 흥분을 통해 자궁근의 수축을 일으키며, 이 효과는 voltage-dependent $Ca^{2+}$ channels을 통한 extracellular $Ca^{2+}$ influx의 증가에 의한 것으로 추론하였다.

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Isolation of Biosurfactant-Producing P. aeruginosa Mi-7 and the Biosurfactant Production (Biosurfactant를 생산하는 P. aeruginosa. KK-7의 분리 및 Biosurfactant의 생산)

  • 강상모;김대원;김혜자
    • Microbiology and Biotechnology Letters
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    • v.22 no.1
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    • pp.92-98
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    • 1994
  • The bacteria which secrete surface-active agent and decrease the surface tension of culture broth were isolated from soil samples. Among them, biosurfactant producing strain KK-7 was selected and emulsification was also detected. The KK-7 produced biosurfactant not only lipid but also glucose by using carbon source. Taxonomical characterization tests have demostrated the strain KK-7 to be Pseudomonas aeruginosa. The media composition of the P. aeruginosa KK-7 for the biosurfactant production was 1% glucose, 0.5% tryptone, 0.2% yeast extract, 0.15% potas sium phosphate mono-dibasic, 0.05% MgSO$_{4}$, initial pH 8.5, at 30$\circ $C for 2 days. In this condition, the concentration of biosurfactant was reached CMC 5 in the culture broth. Surface active material was produced maximum at stationary8 phase, but emulsification power was higher at log phase than stationary phase. It was considered that P. aeruginosa KK-7 produced biosurfactant more than one type having defferent properties and each maximum production time was different. The minimun surface tension of biosurfactant in 50 mM Tris buffer (pH8.0) was 28 dyn/cm, and CMC was 1 g/L.

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Isolation of 1',3'-Dilinolenoyl-2'-Linoleoylglycerol with Tyrosinase Inhibitory Activity from Flammulina velutipes

  • Jang, Se-Gul;Jeon, Kyung-Su;Lee, Eun-Hee;Kong, Won-Sik;Cho, Jae-Yong
    • Journal of Microbiology and Biotechnology
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    • v.19 no.7
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    • pp.681-684
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    • 2009
  • This study was carried out to evaluate the inhibitory effect of Flammulina velutipes extracts on tyrosinase activity and to identify its biologically active component. The ethyl acetate and n-butanol extracts showed potent tyrosinase inhibitory activities. Subsequently, fractions of the n-butanol extract showed only a partial tyrosinase inhibitory activity. The most active compound of tyrosinase inhibitory activity was identified from the ethyl acetate extract as 1',3'-dilinolenoyl-2'-linoleoylglycerol (LnLLn) by comparing its mass, $^1H-$, and $^{13}C-NMR$spectral data with those previously reported in the literature. LnLLn showed tyrosinase inhibitory activity with an $IC_{50}$value of 16.1 ${\mu}g/ml$. These results suggest that the ethyl acetate extract of F. velutipes could be applicable for the development of a new whitening agent.

Antiproliferative effect of Schisandrae Fructus extract on PC-3 human prostate cancer cells (오미자(五味子) 추출물의 인간 전립선암 세포주 PC-3에 대한 성장 억제 효과)

  • Moon, Jung-Min;Seok, Ga-Hyeong;Cho, Su-In
    • The Korea Journal of Herbology
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    • v.27 no.4
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    • pp.17-23
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    • 2012
  • Objectives : Schisandrae Fructus (SF) has traditionally been used to balance level of body fluid and to strengthen kidney function. It has been reported that the SF extract has antioxidant, hepatoprotective, neuroprotective and anticancer effects. This study investigated an antiproliferative effect of SF extract on PC-3 human prostate cancer cells and analyzed active ingredients of SF extract qualitatively and quantitatively. Methods : We examined the antiproliferative effect of SF extract with MTT assay, DAPI staining and annexin-V/7-AAD double staining. The active ingredients of SF extract were identified by using HPTLC and HPLC/DAD system. Results : SF-chloroform fraction inhibited growth of PC-3 cells and changed the morphology of nucleus in a dose dependent manner. A dose-dependent apoptotic cell death was also measured by flow cytometry analysis. It was analyzed that SF-chloroform fraction contained more schizandrin than other fractions by using HPTLC and HPLC/DAD system. Conclusions : These results suggest that SF extract and schizandrin may be a potential chemotherapeutic agent for the control of PC-3 human prostate cancer cells.

Eugenol suppresses inducible cyclooxygenase-2(COX-2) expressionin lipopolysaccharide-stimulated mouse macrophage cells.

  • Kim, Sun-Suk;Oh, O-Jin;Min, Hye-Young;Lee, Youngm-Kim;Lee, Sang-Kook
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2001.11a
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    • pp.86-86
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    • 2001
  • Based on the potential inhibitors of cyclooxygenase-2 (COX-2) as anti-inflammatory or cancer chemopreventive agents, we have evaluated the active principles of COX-2 inhibition from natural products. The methanol extract of the cortex of Eugenia caryoplyllata (Myrtaceae) showed the potent inhibition of prostaglandin E$_2$(PGE$_2$) production in lipopolysaccharide (LPS)-activated RAW 264.7 cells (98.3% inhibition at the test concentration of 10 $\mu\textrm{g}$/$m\ell$) Further, hexane-soluble layer was the most active partition compared to ethyl acetate, n-butanol, and water -soluble parts. By bioassay-guided fractionation of hexane-soluble layer, eugenol was isolated and exhibited a significant suppression of PGE$_2$ production (IC$\_$50/=0.06$\mu\textrm{g}$/$m\ell$). In addition, eugenol suppressed the COX-2 gene expression in LPS-stimulated mouse macrop-hage cells. Therfore, eugenol might be a plausible lead candidate for further developing the COX-2 inhibitor as an anti-inflammatory or cancer chemopreventive agent.

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The Combined Anti-apoptotic Effect from Tamiflu and Pinoresinol of Forsythia fructus Extract Against Influenza Virus Infection (연교 추출물 Pinoresinol와 Tamiflu의 병용효과로부터 Influenza Virus 감염에 의한 세포사멸 억제효과)

  • Kim, Sang-Tae;Kim, Jang-Soo;Choe, Young-Uung;Kim, Young-Kyoon
    • Korean Journal of Pharmacognosy
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    • v.42 no.1
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    • pp.9-14
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    • 2011
  • The fruit body of Forsythiae Fructus (Oleaceae), a common Korean medical herb, is widely used in the treatment of cold and inflammation. In order to elucidate the action mechanism and the active principles from the plant against anti-influenza virus, the influenza virus hemagglutinin (HA) and neuraminidase (NA) gene RT-PCR and Viral Screening & Identification (VSI) assay were conducted, and the activity against viral replication was also investigated. Consequently, one active constituent, namely pinoresinol showed the in vitro antiviral principle using a cytopathic effect (CPE) reduction method, indicating pinoresinol possessed anti-influenza viral activity. Furthermore, combination of pinoresinol and Tamiflu exhibited higher activities than Tamiflu alone against influenza virus (H3N2) infection. The results suggested that combination of pinoresinol with Tamiflu could be a better candidate for an ant-H3N2 viral agent in the treatment of the influenza.

Characterization of Antibiotic Substance Produced by Serratia plymuthica A21-4 and the Biological Control Activity against Pepper Phytophthora Blight

  • Shen, Shun-Shan;Piao, Feng-Zhi;Lee, Byong-Won;Park, Chang-Seuk
    • The Plant Pathology Journal
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    • v.23 no.3
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    • pp.180-186
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    • 2007
  • The biocontrol agent, Serratia plymuthica A21-4, has been developed for controlling pepper Phytophthora blight. Serratia plymuthica A21-4 strongly inhibits the mycelial growth, zoospore formation, and cyst germination of Phytophthora capsici in vitro. The application of a cell suspension of strain A21-4 to pepper plants in pot experiments and in greenhouse successfully controlled the disease. The bacteria produced a potent antifungal substance which was a key factor in the suppression of Phytophthora capsici. The most active chemical com-pound was isolated and purified by antifungal activity-guided fractionation. The chemical structure was identified as a chlorinated macrolide $(C_{23}H_{31}O_8Cl)$ by spectroscopic (UV, IR, MS, and NMR) data, and was named macrocyclic lactone A21-4. The active compound significantly inhibited the formation of zoosporangia and zoospore and germination of cyst of P. capsici at concentrations lower than $0.0625{\mu}g/ml$. The effective concentrations of the macrocyclic lactone A21-4 for $ED_{50}$ of mycelial growth inhibition were $0.25{\mu}g/ml,\;0.25{\mu}g/ml,\;0.30{\mu}g/ml \;and\;0.75{\mu}g/ml$ against P. capsici, Pythium ultimum, Sclerotinia sclerotiorum and Botrytis cinerea, respectively.

Study on the development of preventive agent of dental caries from biological active materials Development of disc PAHA for an artificial tooth and preventive effect on dental caries from plant extracts (생물학적 활성물질에서 치아우식 예방제 개발에 관한 연구 I. 인조치아 disc PAHA의 제조 및 식물추출물들의 치아우식 예방효과)

  • 이기용;조효상윤정원허태련
    • KSBB Journal
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    • v.8 no.2
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    • pp.126-132
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    • 1993
  • The objective of this study was to develop an artificial dentin for easy handle and accurate observation of the mechanism on dental caries and to screen biologically active materials from the extracts of traditional plants and fruits for prevention of early dental cares. In order to produce disc PAHA (artificial dentin), the powdered hydroxylapatite was immobilized in a 20% polyacrylamide gel. The characteristics of disc PAHA was very similar to the surface, figure and lattice of human enamel. After decalcification in 0.1M citric acid based on observation with SEM. The critical point of decalcification of disc PAHA by acids was found to be pH 5.0-5.5, which was hi agreement with human enamel. The degree of decalcification from disc PAHA in 0.1M citric acid solution was sixfold higher than that of human enamel. This result suggested that disc PAHA would be useful as a substitute of human enamel for in vitro experiment. The extracts of garlic and Flower Apple A, B seemed to inhibit growth of S. mutans. Especially, when the 300$\mu\ell$ of its extracts added to the medium to incubate S. mutans, F. apple B showed strongly an inhibitory effect in both the growth of S. mutans and the synthesis of insoluble glucan.

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Characterization of a Novel Carbohydrase from Lipomyces starkeyi KSM 22 for Dental Application

  • KIM, DOMAN;SU-JIN RYU;SOO-JIN HEO;DO-WON KIM;HO-SANG KIM
    • Journal of Microbiology and Biotechnology
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    • v.9 no.3
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    • pp.260-264
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    • 1999
  • The combined activities of dextranase and amylase(DXAMase) from Lipomyces starkeyi KSM 22 produced from starch fermentation inhibited or prevented dental plaque formation. The activities were stable in commercial mouthwash products; DXAMase activity retained over 93% of original activity after 6 months at 23℃. We examined the effects of enzyme inhibitors and active ingredients in mouthwash on DXAMase activity. The DXAMase was stable with 0.29%(w/v) EDTA, 20% (v/v) ethanol, 0.05% (w/v) fluoride, and 0.05% (w/v) SDS. Among the active ingredients of mouthwash, sodium benzoate (up to 1 %, w/v) had no inhibitory effect on either dextranase or amylase activity. In the case of cetylpyridinium chloride, the addition of 0.05% (w/v) inhibited 6% of dextranase activity and 13% of amylase activity. Propylene glycol (up to 1%, w/v) showed no inhibitory effect on either enzyme activity. DXAMase (5 IU/㎖) in mouthwash could remove pre-formed films of glucan-bound S. mutans cells. The addition of 0.1 IU/㎖ DXAMase in mouthwash prevented the formation of insoluble-glucan. These in vitro properties of L. starkeyi KSM 22 DXAMase are desirable for its application as a dental plaque control agent.

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