• Title/Summary/Keyword: 3D IC

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Evaluation of the antimalarial activity of SAM13-2HCl with morpholine amide (SKM13 derivative) against antimalarial drug-resistant Plasmodium falciparum and Plasmodium berghei infected ICR mice

  • Hyelee Hong;Kwonmo Moon;Thuy-Tien Thi Trinh;Tae-Hui Eom;Hyun Park;Hak Sung Kim;Seon-Ju Yeo
    • Parasites, Hosts and Diseases
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    • v.62 no.1
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    • pp.42-52
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    • 2024
  • Antimalarial drugs are an urgently need and crucial tool in the campaign against malaria, which can threaten public health. In this study, we examined the cytotoxicity of the 9 antimalarial compounds chemically synthesized using SKM13-2HCl. Except for SKM13-2HCl, the 5 newly synthesized compounds had a 50% cytotoxic concentration (CC50) >100 μM, indicating that they would be less cytotoxic than SKM13-2HCl. Among the 5 compounds, only SAM13-2HCl outperformed SKM13-2HCl for antimalarial activity, showing a 3- and 1.3-fold greater selective index (SI) (CC50/IC50) than SKM13-2HCl in vitro against both chloroquine-sensitive (3D7) and chloroquine -resistant (K1) Plasmodium falciparum strains, respectively. Thus, the presence of morpholine amide may help to effectively suppress human-infectious P. falciparum parasites. However, the antimalarial activity of SAM13-2HCl was inferior to that of the SKM13-2HCl template compound in the P. berghei NK65-infected mouse model, possibly because SAM13-2HCl had a lower polarity and less efficient pharmacokinetics than SKM13-2HCl. SAM13-2HCl was more toxic in the rodent model. Consequently, SAM13-2HCl containing morpholine was selected from screening a combination of pharmacologically significant structures as being the most effective in vitro against human-infectious P. falciparum but was less efficient in vivo in a P. berghei-infected animal model when compared with SKM13-2HCl. Therefore, SAM13-2HCl containing morpholine could be considered a promising compound to treat chloroquine-resistant P. falciparum infections, although further optimization is crucial to maintain antimalarial activity while reducing toxicity in animals.

Determination of shear wave velocity profiles in soil deposit from seismic piezo-cone penetration test (탄성파 피에조콘 관입 시험을 통한 국내 퇴적 지반의 전단파 속도 결정)

  • Sun Chung Guk;Jung Gyungja;Jung Jong Hong;Kim Hong-Jong;Cho Sung-Min
    • 한국지구물리탐사학회:학술대회논문집
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    • 2005.09a
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    • pp.125-153
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    • 2005
  • It has been widely known that the seismic piezo-cone penetration test (SCPTU) is one of the most useful techniques for investigating the geotechnical characteristics including dynamic soil properties. As the practical applications in Korea, SCPTU was carried out at two sites in Busan and four sites in Incheon, which are mainly composed of alluvial or marine soil deposits. From the SCPTU waveform data obtained from the testing sites, the first arrival times of shear waves were and the corresponding time differences with depth were determined using the cross-over method, and the shear wave velocity profiles (VS) were derived based on the refracted ray path method based on Snell's law and similar to the trend of cone tip resistance (qt) profiles. In Incheon area, the testing depths of SCPTU were deeper than those of conventional down-hole seismic tests. Moreover, for the application of the conventional CPTU to earthquake engineering practices, the correlations between VS and CPTU data were deduced based on the SCPTU results. For the empirical evaluation of VS for all soils together with clays and sands which are classified unambiguously in this study by the soil behavior type classification Index (IC), the authors suggested the VS-CPTU data correlations expressed as a function of four parameters, qt, fs, $\sigma$, v0 and Bq, determined by multiple statistical regression modeling. Despite the incompatible strain levels of the down-hole seismic test during SCPTU and the conventional CPTU, it is shown that the VS-CPTU data correlations for all soils clays and sands suggested in this study is applicable to the preliminary estimation of VS for the Korean deposits and is more reliable than the previous correlations proposed by other researchers.

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UBVRI CCD PHOTOMETRY OF THE TYPE Ic SUPERNOVA SN 1994I IN M51: THE FIRST TWO MONTHS

  • LEE MYUNG GYOON;KIM EUNHYEUK;KIM SANG CHUL;KIM SEUNG LEE;PARK WON KEE;PYO TAE SOO
    • Journal of The Korean Astronomical Society
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    • v.28 no.1
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    • pp.31-43
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    • 1995
  • We present UBVRI CCD photometry of the Type Ie supernova SN 19941 in M51 which was discovered on April 2, 1994 (UT). UBVRI CCD photometry of SN 1994 I were obtained for the period of the first two months from April 4, 1994, using the Seoul National University Observatory 60 cm telescope. The light curves of SN 19941 show several interesting features: (a) SN 19941 reaches the maximum brightness at B-band on April 8.23 (B = 13.68 mag), at V-band on April 9.10 (V = 12.89 mag), and at I-band on April 10.32 (I = 12.48 mag); (b) The light curves around the maximum brightness are much narrower than those of other types of supernovae; (c) The light curves after the peak decline more steeply than those of other types of supernovae; and (d) The colors get redder from $(V-R){\approx}0.2 mag ((V - I){\approx} 0.3 mag, (B - V){\approx}0.7 mag)$ on April 4 to $(V-R){\approx}0.6 mag ((V-1){\approx}0.9 mag, (B-V){\approx}1.3 mag)$ on April 18. Afterwards (V - R) colors get bluer slightly $(by\~0.005 mag/day)$, while (V-I) colors stay almost constant around $(V-1){\approx}1.0 mag$. The color at the maximum brightness is (B-V)=0.9 mag, which is $\~1$mag redder than the mean color of typical Type la supernovae at the maximum brightness. The light curves of SN 1994I are similar to those of the Type Ie supernova SN 1962L in NGC 1073. Adopting the distance modulus of $(m-M)_0 = 29.2 mag$ and the reddening of E(B - V) = 0.45 mag [Iwamoto et al. 1994, preprint for ApJ], we derive absolute magnitudes at the maximum brightness of SN 1994I, Mv(max) = -17.7 mag and MB(max) = -17.4 mag. This result shows that SN 1994I was $\~2$mag fainter at the maximum brightness compared with typical Type Ia supernovae. A narrower peak and faster decline after the maximum in the light curve of SN 1994I compared with other types of supernovae indicate that the progenitor of SN 1994I might be a lower mass star compared with those of other types of supernovae.

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Quantitative Analsysis of Flavanone Glycosides and Peroxynitrite Scavenging Effect of the Five Oriental Medicinal Drugs (Aurantii nobilis Pericarpium, Citrii unshiu Pericarpium, Citrii unshiu Semen, Aurantii Fructus, Poncirii Fructus) (5종 생약(진피, 청피, 귤핵, 지실, 지각)의 Flavanone Glycoside 함량분석과 Peroxynitrite 소거효과)

  • Nugroho, Agung;Park, Myung-Gon;Jin, Seong-Eun;Choi, Jae-Sue;Park, Hee-Juhn
    • Korean Journal of Pharmacognosy
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    • v.40 no.4
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    • pp.370-375
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    • 2009
  • Overproduction of peroxynitrite ($ONOO^-$) causes a variety of disease such as atherosclerosis, hypercholesterolemia, diabetes mellitus or obesity. Peroxynitrite scavenging activities and HPLC analysis on the five Oriental medicinal drugs belonging to the genus Citrus, Aurantium or Poncirus (Rutaceae family) and HPLC analysis were taken to evaluate flavanone glycosides with peroxynitrite scavenging activity. The $IC_{50}s$ of the five crude drugs were shown as follows: Aurantii nobilis Pericarpium (Jinpi, 18.3 ${\mu}g$/ml), Citrii unshiu Pericarpium (Chungpi, 7.50${\mu}g$/ml), Citrii unshiu Semen (Gyulhaek, >50.0${\mu}g$/ml), Aurantii Fructus (Jigak, 18.3${\mu}g$/ml), and Poncirii Fructus (Jisil, >50.0${\mu}g$/ml) where Korean crude drug's names are noted in the parenthesis. Peroxynitrite scavenging effect of flavanones or their glycosides usually contained in Citrus species were observed as follows: hesperetin (1.89 ${\mu}g$/ml), naringenin (7.77 ${\mu}g$/ml), hesperidin (8.44 ${\mu}g$/ml), poncirin (>50.0 ${\mu}g$/ml)and ponciretin(>50.0 ${\mu}g$/ml). The activities of naringin and poncirin with ${\alpha}$-L-rhamnopyranosyl($1{\rightarrow}2$)-${\beta}$-D-glucopyranosyl moiety were weak. HPLC analytical data revealed that Jinpi (the peels of mature fruits of Citrus unshiu) and Chungpi (the peels of immature fruits of C. unshiu) had high quantities of hesperidin as the value of 142.1${\pm}$0.21 and 104.51${\pm}$1.10 mg/g dried weight, respectively. Poncirin was clearly detected in only Jisil and naringenin and naringin were not observed on the HPLC chromatogram of the five crude drugs.

Identification of PM10 Chemical Characteristics and Sources and Estimation of their Contributions in a Seoul Metropolitan Subway Station (서울시 지하역사에서 PM10의 화학적 특성과 오염원의 확인 및 기여도 추정)

  • Park, Seul-Ba-Sen-Na;Lee, Tae-Jung;Ko, Hyun-Ki;Bae, Sung-Joon;Kim, Shin-Do;Park, Duckshin;Sohn, Jong-Ryeul;Kim, Dong-Sool
    • Journal of Korean Society for Atmospheric Environment
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    • v.29 no.1
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    • pp.74-85
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    • 2013
  • Since the underground transportation system is a closed environment, indoor air quality problems may seriously affect many passengers' health. The purpose of this study was to understand $PM_{10}$ characteristics in the underground air environment and further to quantitatively estimate $PM_{10}$ source contributions in a Seoul Metropolitan subway station. The $PM_{10}$ was intensively collected on various filters with $PM_{10}$ aerosol samplers to obtain sufficient samples for its chemical analysis. Sampling was carried out in the M station on the Line-4 from April 21 to 28, July 13 to 21, and October 11 to 19 in the year of 2010 and January 11 to 17 in the year of 2011. The aerosol filter samples were then analyzed for metals, water soluble ions, and carbon components. The 29 chemical species (OC1, OC2, OC3, OC4, CC, PC, EC, Ag, Al, Ba, Cd, Cr, Cu, Fe, Mn, Ni, Pb, Si, Ti, V, Zn, $Cl^-$, $NO_3{^-}$, $SO_4{^{2-}}$, $Na^+$, $NH_4{^+}$, $K^+$, $Mg^{2+}$, $Ca^{2+}$) were analyzed by using ICP-AES, IC, and TOR after proper pretreatments of each sample filter. Based on the chemical information, positive matrix factorization (PMF) model was applied to identify the $PM_{10}$ sources and then six sources such as biomass burning, outdoor, vehicle, soil and road dust, secondary aerosol, ferrous, and brakewear related source were classified. The contributions rate of their sources in tunnel are 4.0%, 5.8%, 1.6%, 17.9%, 13.8% and 56.9% in order.

A Microcomputer-Based Data Acquisition System (Microcomputer를 이용(利用)한 Data Acquisition System에 관(關)한 연구(硏究))

  • Kim, Ki Dae;Kim, Soung Rai
    • Journal of Biosystems Engineering
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    • v.7 no.2
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    • pp.18-29
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    • 1983
  • A low cost and versatile data acquisition system for the field and laboratory use was developed by using a single board microcomputer. Data acquisition system based on a Z80 microprocessor was built, tested and modified to obtain the present functional system. The microcomputer developed consists of 6 kB ROM, 5 kB RAM, 6-seven segment LED display, 16-Hex. key and 8 command key board. And it interfaces with an 8 channel, 12 bits A/D converter, a microprinter, EPROM programmer for 2716, and RS232C interface to transfer data between the system and HP3000 mini-computer manufactured by Hewlett Packard Co., A software package was also developed, tested, and modified for the system. This package included drivers for the AID converter, LED display, key board, microprinter, EPROM programmer, and RS232c interface. All of these programs were written in 280 assembler language and converted to machine codes using a cross assembler by HP3000 computer to the system during modifying stage by data transferring unit of this system, then the machine language wrote to the EPROM by this EPROM programmer. The results are summarized as follows: 1. Measuring program developed was able to control the measuring intervals, No. of channels used, and No. of data, where the maximum measuring speed was 58.8 microsec. 2. Calibration of the system was performed with triangle wave generated by a function generator. The results of calibration agreed well to the test results. 3. The measured data was able to be written into EPROM, then the EPROM data was compared with original data. It took only 75 sec. for the developed program to write the data of 2 kB the EPROM. 4. For the slow speed measurements, microprinter instead of EPROM programmer proved to be useful. It took about 15 min. for microprinter to write the data of 2 kB. 5. Modified data transferring unit was very effective in communicating between the system and HP3000 computer. The required time for data transferring was only 1~2 min. 6. By using DC/DC converting devices such as 78-series, 79-series. and TL497 IC, this system was modified to convert the only one input power sources to the various powers. The available power sources of the system was DC 7~25 V and 1.8 A.

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Inhibitory Effects of Ethanolic Extracts from Aster glehni on Xanthine Oxidase and Content Determination of Bioactive Components Using HPLC-UV (섬쑥부쟁이 에탄올 추출물의 잔틴산화효소 저해 효능 및 HPLC-UV를 이용한 유효성분의 함량 분석)

  • Kang, Dong Hyeon;Han, Eun Hye;Jin, Changbae;Kim, Hyoung Ja
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.45 no.11
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    • pp.1610-1616
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    • 2016
  • This study aimed to establish an optimal extraction process and high performance liquid chromatography-ultraviolet (HPLC-UV) analytical method for determination of 3,5-dicaffeoylquinic acid (3,5-DCQA) as a part of materials standardization for the development of a xanthine oxidase inhibitor as a health functional food. The quantitative determination method of 3,5-DCQA as a marker compound was optimized by HPLC analysis using a Luna RP-18 column, and the correlation coefficient for the calibration curve showed good linearity of more than 0.9999 using a gradient eluent of water (1% acetic acid) and methanol as the mobile phase at a flow rate of 1.0 mL/min and a detection wavelength of 320 nm. The HPLC-UV method was applied successfully to quantification of the marker compound (3,5-DCQA) in Aster glehni extracts after validation of the method with linearity, accuracy, and precision. Ethanolic extracts of A. glehni (AGEs) were evaluated by reflux extraction at 70 and $80^{\circ}C$ with 30, 50, 70, and 80% ethanol for 3, 4, 5, and 6 h, respectively. Among AGEs, 70% AGE at $70^{\circ}C$ showed the highest content of 3,5-DCQA of $52.59{\pm}3.45mg/100g$ A. glehni. Furthermore, AGEs were analyzed for their inhibitory activities on uric acid production by the xanthine/xanthine oxidase system. The 70% AGE at $70^{\circ}C$ showed the most potent inhibitory activity with $IC_{50}$ values of $77.01{\pm}3.13{\sim}89.96{\pm}3.08{\mu}g/mL$. The results suggest that standardization of 3,5-DCQA in AGEs using HPLC-UV analysis would be an acceptable method for the development of health functional foods.

Changes in the constituents and UV-photoprotective activity of Astragalus membranaceus caused by roasting (황기의 볶음 조건에 따른 성분 및 자외선 광보호 활성 변화)

  • Park, Jeong-Yong;Lee, Ji Yeon;Kim, Hyung Don;Jang, Gwi Yeong;Seo, Kyung Hye
    • Journal of Nutrition and Health
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    • v.52 no.5
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    • pp.413-421
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    • 2019
  • Purpose: Astragalus membranaceus (AM) is an important traditional medicinal herb. Pharmacological research has indicated that AM has various physiological activities such as antioxidant, anti-inflammatory, immunoregulatory, anticancer, hypolipidemic, antihyperglycemic, and hepatoprotective activities. The bioactive substances responsible for the physiological activities in AM, including many antioxidant substances, change during the roasting process. This study investigated and compared the changes in the antioxidant constituents of AM caused by roasting. Methods: DPPH (1,1-diphenyl-2-picryl hydrazyl) and $ABTS^+$ (2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt) radical scavenging activities and their total phenolic content (TPC) were measured. High-performance liquid chromatography (HPLC) analysis was performed to confirm any changes in the isoflavonoids of roasted AM (R-AM),. The cell viability of UVB-induced HDF (Human dermal fibroblast) cells treated with AM and R-AM extracts was investigated. The comet assay was used to examine the inhibitory effects of R-AM extracts on DNA damage caused by oxidative stress. Results: The DPPH and $ABTS^+$ radical scavenging activities were $564.6{\pm}20.9$ and $108.2{\pm}3.1$ ($IC_{50}$ value) respectively, from the 2R-AM. The total phenol content was $47.80{\pm}1.40mg$ GAE/g from the 1R-AM. The values of calycosin and formononetin, which are the known isoflavonoid constituents of AM, were $778.58{\pm}2.72$ and $726.80{\pm}3.45{\mu}g/g$ respectively, from the 2R-AM. Treatment of the HDF cells with R-AM ($50{\sim}200{\mu}g/mL$) did not affect the cell viability. Furthermore, the R-AM extracts effectively protected against UVB-induced DNA damage. Conclusion: The findings of this study indicate that R-AM increases its isoflavonoid constituents and protects against UVB-induced DNA damage in HDF cells.

Analysis of Immunomodulating Gene Expression by cDNA Microarray in $\beta$-Glucan-treated Murine Macrophage

  • Sung, Su-Kyong;Kim, Ha-Won
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2003.11a
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    • pp.98-98
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    • 2003
  • ${\beta}$-(1,3)-D-Glucans have been known to exhibit antitumor and antimicrobial activities. The presence of dectin-1,${\alpha}$, ${\beta}$-glucan receptor of dendritic cell, on macrophage has been controvertial. RT-PCR analysis led to the detection of dectin-1${\alpha}$ and ${\beta}$ in murine macrophage Raw264.7 cell line. Among the various organs of mouse, dectin-1${\alpha}$ and ${\beta}$ were detected in the thymus, lung, spleen, stomach and intestine. To analyze gene expression modulated by ${\beta}$-glucan treated murine Raw264.7 macrophage, total mRNA was applied to cDNA microarray to interrogate the expression of 7,000 known genes. cDNA chip analysis showed that ${\beta}$-glucan of P. osteatus increased gene expressions of immunomodulating genes, membrane antigenic proteins, chemokine ligands, complements, cytokines, various kinases, lectin associated genes and oncogenes in Raw 264.7 cell line. When treated with ${\beta}$-glucan of P. osteatus and LPS, induction of gene expression of TNF-${\alpha}$ and IFN-R1 was confirmed by RT-PCR analysis. Induction of TNF-R type II expression was confirmed by FACS analysis. IL-6 expression was abolished by EDTA in ${\beta}$-glucan and LPS treated Raw264.7 cell line, indicating that ${\beta}$-glucan binds to dectin-l in a Ca$\^$++/ -dependent manner. To increase antitumor efficacy of ${\beta}$-glucan, ginsenoside Rh2 (GRh2) was co-treated with ${\beta}$-glucan in vivo and in vitro tests. IC$\sub$50/ values of GRh2 were 20 and 25 $\mu\textrm{g}$/$m\ell$ in SNU-1 and B16 melanoma F10 cell line, respectively. Co-treatment with ${\beta}$-glucan and GRh2 showed synergistic antitumor activity with cisplatin and mitomycin C both in vitro and in vivo. Single or co-treatment with ${\beta}$-glucan and GRh2 increased tumor bearing mouse life span. Co-treatment with ${\beta}$-glucan and GRh2 showed more increased life span with mitomycin C than that with cisplatin. Antitumor activities were 67% and 72 % by co-injection with ${\beta}$-glucan and GRh2 in the absence or presence of mitomycin C, respectively.

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THE EFFECT OF ACID ETCHING ON GLASS IONOMER CEMENT SURFACES (Glass ionomer cement 표면의 산부식 효과에 관한 연구)

  • Han, Seung-Weon;Park, Sang-Jin;Min, Byung-Soon;Choi, Ho-Young;Choi, Gi-Woon
    • Restorative Dentistry and Endodontics
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    • v.18 no.1
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    • pp.1-26
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    • 1993
  • The purpose of this study was to investigate the effect of acid etching on the surface appearance and fracture toughness of five glass ionomer cements. Five kinds of commercially available glass ionomer cements including chemical curing filling type, chemical curing lining type, chemical curing metal reinforced type, light curing tilling type and light curing lining type were used for this study. The specimens for SEM study were fabricated by treating each glass ionomer cement with either visible light curing or self curing after being inserted into a rubber mold (diameter 4mm, depth 1mm). Some of the specimens were etched with 37% phosphoric acid for 0, 15, 30, 60, go seconds, at 5 minutes, 1 hour and 1 day after mixing of powder and liquid. Unetched ones comprised the control group and the others were the experimental groups. The surface texture was examined by using scanning electron microscope at 20 kV. (S-2300, Hitachi Co., Japan). The specimens for fracture toughness were fabricated by curing of each glass ionomer cement previously inserted into a metal mold for the single edge notch specimen according to the ASTME399. They were subjected to a three-point bend test after etching for 0, 30, 60, and 90 seconds at 5 minutes-, 1 hour-and 1 day-lapse after the fabrication of the specimens. The plane strain fracture toughness ($K_{IC}$) was determined by three-point bend test which was conducted with cross-head speed of 0.5 mm/min using Instron universal testing machine (Model No. 1122) following seven days storage of the etched specimens under $37^{\circ}C$, 100% humidity condition. Following conclusions were drawn. 1. In unetched control group, crack was present, but the surface was generally smooth. 2. Deterioration of the surface appearance such as serious dissolving of gel matrix and loss of glass particles occured as the etching time was increased beyond 15 s following Immediate etching of chemical curing type of glass ionomer cements. 3. Etching after 1 h, and 1 d reduced surface damage, 15 s, and 30s etch gave rough surface appearance without loss of glass particle of chemical curing type of glass ionomer cements. 4. Light curing type glass ionomer cement was etched by acid, but there was no difference in surface appearances according to various waiting periods. 5. It was found that the value of plane stram fracture toughness of glass ionomer cements was highest in the light curing filling type as $1.79\;MNm^{-1.5}$ followed by the light curing lining type, chemical curing metal reinforced type, chemical curing filling type and chemical curing lining type. 6. The value of plane stram fracture toughness of the chemical curing lining type glass ionomer cement etched after 5 minutes was lower than those of the cement etched after 1 hour or day or unetched (P < 0.05). 7. Light curing glass ionomer cement showed Irregular fractured surface and chemical curing cement showed smooth fractured surface.

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