• Title/Summary/Keyword: In vitro screening

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The Experimental Study on the Effect of Herbal Exrtacts on Hair Growth and Acnes (복분자(覆盆子), 석창포(石菖蒲), 상침자 및 숙지황(熟地黃)이 모발성장(毛髮成長)과 면포에 미치는 실험적(實驗的) 연구(硏究))

  • Oh, Young-Sun;Roh, Sek-Seun;Oh, Min-Suck
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.19 no.3 s.31
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    • pp.34-54
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    • 2006
  • The effects of four extracts of medicinal herbs, Rubus coreanum, Acorus calamus, Morus alba and Rehmannia glutinosa on hair growth activity and acnes control were investigated. In the course of screening natural extracts for hair growth, we found that the extract of dried root of Rubus coreanum has the hair growth promoting effect. After topical application of these extracts to the back of C57BL/6 mice, the earlier conversion of telogen-to-anagen phase was induced. The growth of dermal papilla cells and mouse vibrissae hair follicle cultured in vitro, however, was not affected by treatment of these extracts. Furthermore these extracts do not possesspotent inhibitory effect on $5{\alpha}-reductase$ I and II activity and anti-bacterial effect on Escherichia coli , Propionibacterium acnes, Pityrosporum ovale, Staphylococcus aureus, Staphylococcus epidemidis, and Candida albicans. RT-PCR analysis showed that these extracts did notinduce mRNA levels of growth factors such as insulin-like growth factor-I, keratinocyte growth factor, hepatocyte growth factor and vascular endothelial growth factor in dermal papilla cells. These results suggest that Rubus coreanum has hair growth promoting effect. However, the effects of these materials on the hair growth promotion are not mediated through inhibition of $5{\alpha}-reductase$ I and II activity, stimulation of hair follicle cells and expression of growth factors in the dermal papilla cells.

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Toxicity Assessment of Gas Phase in Cigarette Smoke Using Cell-free Assay

  • Park, Chul-Hoon;Sahn, Hyung-Ok;Shin, Han-Jae;Lee, Hyeong-Seok;Min, Yaung-Keun;Hyun, Hak-Chul
    • Journal of the Korean Society of Tobacco Science
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    • v.29 no.2
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    • pp.110-117
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    • 2007
  • In vitro toxicity tests such as cytotoxicity, mutagenicity and genotoxicity assay are useful for evaluating the relative toxicity of smoke or smoke condensates obtained from different cigarette configurations. A major disadvantage of these tests is relatively time-consuming, complicated and expensive. Recently, a cell-free glutathione consumption assay (GCA) as a rapid and simple screening method for the toxicity assessment of smoke has been reported by Cahours et al. (CORESTA, 2006). This study was carried out to assess the GCA application capable of predicting the toxicity of gas/vapor phase (GVP) of cigarette smoke and to identify individual compounds responsible for the glutathione (GSH) consumption in smoke. Each GVPs from 2R4F, standard cigarette, carbon filter cigarette (ExC) and new carbon filter cigarette (ExN), test cigarettes were collected by automatic smoking machine and evaluated the relative toxicity by GCA and neutral red uptake (NRU) assay. Toxic compounds existed in smoke were also chosen, relative toxicities of these compounds were screened by using two methods and compared individually. The overall order of toxicity by GCA was 2R4F > ExC > ExN, which was consistent with the result of Neutral Red Uptake assay. The levels of carbonyl compounds of ExN were lower than those of 2R4F and ExC, indicating that GSH consumption was associated with carbonyl compound yields. A major toxicant under current study is acrolein, which contributed to more than half of the GSH consumption. Collectively, the toxicity of GVP determined by GCA method may be mainly attributed to acrolein.

Insights into the in vitro germicidal activities of Acalypha indica

  • Rahman, Md. Shahedur;Hossain, Riad;Saikot, Forhad Karim;Rahman, Shaikh Mizanur;Saha, Subbroto Kumar;Hong, Jongki;Kim, Ki-Hyun
    • Analytical Science and Technology
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    • v.30 no.1
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    • pp.26-31
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    • 2017
  • Background and purpose: This study was carried out to learn more about the potential prophylactic or antibacterial activity of the plant Acalypha indica against selective pathogenic bacteria. Experimental: The test organisms were Sarcina lutea IFO 3232, Bacillus subtilis IFO 3026, Pseudomonas denitrificans, Escherichia coli IFO 3007, Klebsiella pneumoniae ATTC 10031, Xanthomonas campestris IAM 1671, and Proteus vulgaris. Leaf, stem, and bud powder of Acalypha indica were dissolved in various solvents, and the extracts were tested for antimicrobial activity through the disc diffusion method. GC-MS profiling was performed to characterize active chemical compounds in the essential oil of Acalypha indica. Results: The ethanol extract showed the highest activity against all bacteria, while the petroleum ether extract yielded the highest zone of inhibition against Proteus vulgaris ($11.83{\pm}1.75mm$). The minimum inhibitory concentration (MIC) of the ethyl acetate extract against Bacillus subtilis was 16 µg/mL. Phytochemical screening by GC-MS revealed a total of 12 bioactive compounds. Conclusion: Extracts of Acalypha indica may be useful in formulating and synthesizing new antibacterial drugs.

Pyridoxatin, an Inhibitor of Gelatinase A with Cytotoxic Activity

  • Lee, Ho-Jae;Chung, Myung-Chul;Lee, Choong-Hwan;Chun, Hyo-Kon;Kim, Hwan-Mook;Kho, Yung-Hee
    • Journal of Microbiology and Biotechnology
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    • v.6 no.6
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    • pp.445-450
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    • 1996
  • Gelatinase A is a member of the matrix metalloproteinases that play an important role in cancer invasion and metastasis. In the course of screening gelatinase A inhibitors from microbial sources, a fungal strain PT-262 showed a strong inhibitory activity. The strain was identified as Chaunopycnis alba on the basis of its morphological characteristics. The inhibitor was isolated from acetone extract of mycelial cake by sequential chromatographies on MCI-gel, Sephadex LH-20, and a reverse-phase HPLC column. The purified inhibitor was identified as pyridoxatin by its physico-chemical properties and spectroscopic analysis. Pyridoxatin is not a peptide analog and has cyclic hydroxamic acid moiety. It inhibited activated gelatinase A with an $IC_{50}$ value of 15.2 ${\mu}M$ using fluorescent synthetic peptide. It also had a strong cytotoxicity against human cancer cell lines in vitro. Furthermore, this compound inhibited DNA synthesis with an $IC_{50}$ value of 2.92 ${\mu}M$ in PC-3 prostate cancer cells by [$^3H$]thymidine incorporation assay.

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Regulation of signal transducer and activator of transcription 3 activation by dual-specificity phosphatase 3

  • Kim, Ba Reum;Ha, Jain;Kang, Eunjeong;Cho, Sayeon
    • BMB Reports
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    • v.53 no.6
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    • pp.335-340
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    • 2020
  • Since cancer is the leading cause of death worldwide, there is an urgent need to understand the mechanisms underlying cancer progression and the development of cancer inhibitors. Signal transducer and activator of transcription 3 (STAT3) is a major transcription factor that regulates the proliferation and survival of various cancer cells. Here, dual-specificity phosphatase 3 (DUSP3) was identified as a regulator of STAT3 based on an interaction screening performed using the protein tyrosine phosphatase library. DUSP3 interacted with the C-terminal domain of STAT3 and dephosphorylated p-Y705 of STAT3. In vitro dephosphorylation assay revealed that DUSP3 directly dephosphorylated p-STAT3. The suppressive effects of DUSP3 on STAT3 were evaluated by a decreased STAT3-specific promoter activity, which in turn reduced the expression of the downstream target genes of STAT3. In summary, DUSP3 downregulated the transcriptional activity of STAT3 via dephosphorylation at Y705 and also suppressed the migratory activity of cancer cells. This study demonstrated that DUSP3 inhibits interleukin 6 (IL-6)/STAT3 signaling and is expected to regulate cancer development. Novel functions of DUSP3 discovered in IL-6/STAT3 signaling regulation would help expand the understanding of cancer development mechanisms.

Screening of Antioxidants and Antimicrobial activity in native plants (국내 자생 식물의 항산화 및 항미생물 활성 탐색)

  • Rim, Yo-Sup;Park, Young-Min;Park, Moon-Su;Kim, Kil-Yong;Kim, Myong-Jo;Choi, Yong-Hwa
    • Korean Journal of Medicinal Crop Science
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    • v.8 no.4
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    • pp.342-350
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    • 2000
  • This study was carried out to screen antioxidative by in vitro bioassay method from 89 Korean natural sources extracted by 100% MeOH. Antioxidant activity test was used the DPPH method. MeOH extracts from Castanea crenata and Ulmus davidiana var. japonica showed high antioxidant activity by $5.8{\mu}g\;(RC_{50})$ and $12.2{\mu}g\;(RC_{50})$, respectively, among 13 plants exhibiting the activity. The extracts from Platycarya strobilacea, Lindera erythrocarpa, Chrysanthemum boreale, Rumex crispus and Viburnum awabuki also showed over 90% antimicrobial activity, according to in vivo bioassay method.

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Anti-inflammatory Activity of Medicinal Plant Extracts (약용식물자원 추출물의 항염증활성)

  • Lee, Seung-Eun;Lee, Jeong-Hoon;Kim, Jin-Kyung;Kim, Geum-Sook;Kim, Young-Ok;Soe, Jin-Sook;Choi, Je-Hun;Lee, Eun-Suk;Noh, Hyung-Jun;Kim, Seung-Yu
    • Korean Journal of Medicinal Crop Science
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    • v.19 no.4
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    • pp.217-226
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    • 2011
  • The study was conducted to investigate candidate materials as anti-inflammation agent from plant resources. Activities of 33 plant parts extracts with the final concentration of 5${\mu}g/ml$ were evaluated on the several inflammation-related markers such as the release of proinflammatoty cytokine [tumor necrosis factor-alpha (TNF-${\alpha}$) & interleukin-6 (IL-6)], nitric oxide (NO), the expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and inhibitor of nuclear factor kappa-B alpha ($I{\kappa}-B{\alpha}$) in lipopolysaccharide (LPS)-treated RAW 264.7 cells. The extracts in the final concentration of 10 ${\mu}g/ml$ were also screened on peroxynitrite (ONOO$^-$) scavenging activity. Eleven extracts selected from the screening assay were verified on the inhibition activity on peroxynitrite and total reactive species oxygen (ROS) in the several concentrations. As results, Alpinia officinarum Hance (rhizome), Inula britannica var. chinensis Regel (flower), Ulmus arvifolia Jacq (trunk peel) and Aster scaber Thunb. (aerial part) showed comparatively potent anti-inflammatory activities in vitro cells or chemical level systems, and then these four plant parts should be studied on the antiinflammatory mechanism by further studies.

The Regulatory Effects of Low-Dose Ionizing Radiation on Ikaros-Autotaxin Interaction (저선량 방사선에 의한 Ikaros-Autotaxin 상호작용 조절 효과)

  • Kang, Hana;Cho, Seong-Jun;Kim, Sung Jin;Nam, Seon Young;Yang, Kwang Hee
    • Journal of Radiation Industry
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    • v.10 no.1
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    • pp.7-12
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    • 2016
  • Ikaros, a transcription factor containing zinc-finger motif, has known as a critical regulator of hematopoiesis in immune system. Ikaros protein modulates the transcription of target genes via binding to the regulatory elements of the genes promoters. However the regulatory function of Ikaros in other organelle except nuclear remains to be determined. This study explored radiation-induced modulatory function of Ikaros in cytoplasm. The results showed that Ikaros protein lost its DNA binding ability after LDIR (low-dose ionizing radiation) exposure. Cell fractionation and Western blot analysis showed that Ikaros protein was translocated into cytoplasm from nuclear by LDIR. This was confirmed by immunofluorescence assay. We identified Autotaxin as a novel protein which potentially interacts with Ikaros through in vitro protein-binding screening. Co-immunoprecipitation assay revealed that Ikaros and Autotaxin are able to bind each other. Autotaxin is a crucial enzyme generating lysophosphatidic acid (LPA), a phospholipid mediator, which has potential regulatory effects on immune cell growth and motility. Our results indicate that LDIR potentially regulates immune system via protein-protein interaction of Ikaros and Autotaxin.

The Cytotoxicity of 1,3-diphenylpropenone derivatives (1,3-diphenylpropenone 유도체의 세포독성)

  • Yu, Seong-Jae;Kwon, Byung-Mok;Lee, Chong-Ock;Choi, Sang-Un;Sung, Nack-Do
    • Applied Biological Chemistry
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    • v.42 no.1
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    • pp.68-72
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    • 1999
  • The cytotoxicity of 1,3-diphenylpropenone derivatives known to inhibit the farnesyl protein transferase (FPTase) was examined against various established tumor cell line, A549 (lung cancer), SKMEL-2 (uterine cancer), HCT-15 (skin cancer), SKOV-3 (brain cancer) and XF-498 (colon cancer) of the 1,3-diphenylpropenone derivatives showing farnesyl protein transferase (FPTase) inhibition activity. And the structure-activity relationship (SAR) between structure of 1,3-diphenylpropenone derivatives as substrate and cytotoxicity was investigated by Free-Wilson analysis as well as Hansch method with tumor cell lines. From the result of Free-Wilson analyses, X-substituents on the benzoyl group have a more important role than Y-substituents on the styryl group. The 2,4-dichloro substituent, 15 and 2,4-dimethyl substituent, 16 showed the highest cytotoxicity (average pI_(50)=5.0). Particulary, the cytotoxicity of X-substituents increased with electronic effect $({\sigma})$ due to weak electron withdrawing group with optimum value $({\sigma}_{opt}=0.22{\sim}0.29})$ whereas that of Y-substituent resulted from various factors such as logP, $B_1$ and R constant.

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In vitro screening of elastase, collagenase, hyaluronidase, and tyrosinase inhibitory and antioxidant activities of 22 halophyte plant extracts for novel cosmeceuticals

  • Jiratchayamaethasakul, Chanipa;Ding, Yuling;Hwang, Ouibo;Im, Seung-Tae;Jang, Yebin;Myung, Seung-Won;Lee, Jeong Min;Kim, Hyun-Soo;Ko, Seok-Chun;Lee, Seung-Hong
    • Fisheries and Aquatic Sciences
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    • v.23 no.3
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    • pp.6.1-6.9
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    • 2020
  • Background: Halophyte plant (HPs), a salt-resistant flora, has been reported to provide several health benefits, but the knowledge of its cosmeceutical potential is still ambiguous. Here, 70% ethanol extracts of 22 HPs collected from along the coast of South Korea were investigated for their potentials of antioxidant, anti-aging, and whitening properties for use as materials in novel cosmeceuticals. Methods: Antioxidant activities were determined by DPPH (1,1-diphenyl-2-pricrylhydrazyl) free radical and hydrogen peroxide scavenging assays, and skin aging-related enzyme activities (anti-elastase, anti-collagenase, anti-hyaluronidase, and anti-tyrosinase) were evaluated by using the spectrophotometric method. Results: Among the 22 HPs, we found that Ischaemum antephoroides f. coreana and Atriplex gmelinii extracts presented the strongest scavenging effects against DPPH free radical and hydrogen peroxide, respectively. Our finding additionally suggested that Salicornia europaea extract might provide a major source of anti-elastase and anti-hyaluronidase; meanwhile, Rosa rugosa extract showed the highest anti-collagenase effect. Furthermore, the highest tyrosinase inhibitory activity was possessed by Spartina anglica extract. Conclusion: These findings may suggest that halophyte plants showing biological activities may be potent inhibitors of tyrosinase, elastase, collagenase, and hyaluronidase and could be useful for application in cosmeceuticals.