• The Korean Journal of Pesticide Science
• /
• v.16 no.1
• /
• pp.1-10
• /
• 2012

Fungicidal activities against phytopathogenic fungi of diarylthiazole compound of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-(4-fluorophenyl)thiazol-5-yl]-1-methylpiperidine (I) have been determined to be excellent and compound I was used as the leading compounds in this study. Furthermore, the compound was synthesized by reacting them with five functional groups, 4-fluoro-3-methylphenyl, 4-fluoro-3-chlorophenyl, 4-chloro-2-fluorophenyl, 4-bromo-3-methylphenyl and 2,4-dichlorophenyl groups instead of 4-fluorophenyl group. Also, 2-amino-, 2-(N-ethoxycarbonyl)piperidin-4-yl-, and 2-piperidin-4-yl-thiazole were introduced as the leads instead of 2-N-methylpiperidine-4-yl-thiazol of compound I. VIII-1~VIII-5 and XIII-1~XV-5 compounds were newly synthesized and their structures were confirmed by $^1H$-NMR-spectrum. The fungicidal activities of all the synthesized compounds against Phytophthora capsici were examined using the whole plant method. Among the VIII-1~VIII-5 and XIII-1~XV-5 chemicals, XIV-3 showed the most potent antifungal activity in vivo. While the $EC_{50}$ and $EC_{90}$ values of the commercial fungicide dimethomorph and I were $4.26{\pm}0.02$, $14.72{\pm}0.05$ and $1.01{\pm}0.11$, $6.31{\pm}0.09mM$, those of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-(4-chloro-2-fluorophenyl)thiazol-5-yl]-1-methylpiperidine (XIV-3) was $0.98{\pm}0.21$ and $5.85{\pm}0.05mM$. Therefore, XIV-3 can be considered as a viable candidate for the control of plant diseases caused by P. capsici, and further studies will be conducted on the mode of action XIV-3.

• Journal of the Korean Chemical Society
• /
• v.39 no.5
• /
• pp.344-349
• /
• 1995

The crystal and molecular structure of the title compound has been determined from 2568 reflections collected on an automatic CAD4 diffractometer using graphite-monochromated $Mo-K\alpha$ radiation. The crystal is monoclinic system, space group $P2_1$ with unit cell dimensions $a=8.756(8)\AA$, $b=25.757(2)\AA$, $c=8.628(1)\AA$, $\beta=99.15(4)^{\circ}$, V= 1,921(2) ${\AA}^3$, Z=4, $D_C=1.336\;g/cm^3$, ${\mu}=1.54\;cm^{-1}\;and\;T=298^{\circ}K$. The final R factor was 0.051 for 2049 reflections over $3{\sigma}(Fο).$ The crystal has two asymmetric molecules in the unit cell. The arrangement of sulfon group was shown a distorted tetrahedron structure and N(6), N(6') atoms were deviated from the least-squares planes of the thiadiazine rings, respectively. The molecular packings in the unit cell are linked by the two intermolecular hydrogen bonds of N-H---O type and van der Waals forces.

• Applied Microscopy
• /
• v.40 no.4
• /
• pp.245-251
• /
• 2010

In this study, we applied 15% glycolic acid peeling agent and 30% glycolic acid peeling agent to the dorsal skin of mice and analyzed the oil content, moisture content, and pH value of the skin before and after test using cutometer. Ultrastructure for changes in the epidermis of mice were observed under a dermoscope and a scanning electron microscope before and after test. When using 15% glycolic acid peeling agent, the changes of moisture content was measured 74.67 AU for the normal control group and 70.21 AU for the experimental group, the oil content was 13.49 mg/$cm^2$ for the normal control group before test and 8.25 mg/$cm^2$ after test, and the pH value was 6.70 and 5.36 before and after test, respectively. When using 30% glycolic acid peeling agent, the moisture content was measured 74.46 AU for the normal control group before test and 53.50 AU for the experimental group after test, the oil content was 13.82mg/$cm^2$ and 5.70 mg/$cm^2$ before and after test, and the pH value was 6.45 and 4.58 before and after test, respectively. As such, it was found that the changes of moisture and oil content on the skin rely on the concentration of peeling agent and the degree of exfoliation of keratin. The surface of stratum corneum of mice with application of 15% glycolic acid peeling agent was relatively smooth and the exposed cellular surface of keratinocyte had some wrinkles. The surface of stratum corneum of mice with application of 30% glycolic acid peeling agent was smooth. No wrinkles were observed under high-resolution scanning electron microscope.

• Journal of Sericultural and Entomological Science
• /
• v.16 no.1
• /
• pp.21-48
• /
• 1974

The studies were carried out to disclose the physical and chemical properties of sericin fraction obtained from silk cocoon shells and its characteristics of swelling and solubility. The following results were obtained. 1. The physical and chemical properties of sericin fraction. 1) In contrast to the easy water soluble sericin, the hard soluble sericin contains fewer amino acids include of polar side radical while the hard soluble amino acid sach as alanine and leucine were detected. 2) The easy soluble amino acids were found mainly on the outer part of the fibroin, but the hard soluble amino acids were located in the near parts to the fibroin. 3) The swelling and solubility of the sericin could be hardly assayed by the analysis of the amino acid composition, and could be considered to tee closely related to the compound of the sericin crystal and secondary structure. 4) The X-ray patterns of the cocoon filament were ring shape, but they disappeared by the degumming treatment. 5) The sericin of tussah silkworm (A. pernyi), showed stronger circular patterns in the meridian than the regular silkworm (Bombyx mori). 6) There was no pattern difference between Fraction A and B. 7) X-ray diffraction patterns of the Sericin 1, ll and 111 were similar except interference of 8.85A (side chain spacing). 8) The amino acids above 150 in molecular weight such as Cys. Tyr. Phe. His. and Arg. were not found quantitatively by the 60 minutes-hydrolysis (6N-HCI). 9) The X-ray Pattern of 4.6A had a tendency to disappear with hot-water, ether, and alcohol treatment. 10) The partial hydrolysis of sericin showed a cirucular interference (2A) on the meridian. 11) The sericin pellet after hydrolysis was considered to be peptides composed with specific amino acids. 12) The decomposing temperature of Sericin 111 was higher than that of Sericin I and II. 13) Thermogram of the inner portioned sericin of the cocoon shell had double endothermic peaks at 165$^{\circ}C$, and 245$^{\circ}C$, and its decomposing temperature was higher than that of other portioned sericin. 14) The infrared spectroscopic properties among sericin I, II, III and sericin extracted from each layer portion of the cocoon shell were similar. II. The characteristics of seriein swelling and solubility related with silk processing. 1) Fifteen minutes was required to dehydrate the free moisture of cocoon shells with centrifugal force controlled at 13${\times}$10$^4$ dyne/g at 3,000 R.P.M. B) It took 30 minutes for the sericin to show positive reaction with the Folin-Ciocaltue reagent at room temperature. 3) The measurable wave length of the visible radiation was 500-750m${\mu}$, and the highest absorbance was observed at the wave length of 650m${\mu}$. 4) The colorimetric analysis should be conducted at 650mu for low concentration (10$\mu\textrm{g}$/$m\ell$), and at 500m${\mu}$ for the higher concentration to obtain an exact analysis. 5) The absorbing curves of sericin and egg albumin at different wave lengths were similar, but the absorbance of the former was slightly higher than that of the latter. 6) The quantity of the sericin measured by the colorimetric analysis, turned out to be less than by the Kjeldahl method. 7) Both temperature and duration in the cocoon cooking process has much effect on the swelling and solubility of the cocoon shells, but the temperature was more influential than the duration of the treatment. 8) The factorial relation between the temperature and the duration of treatment of the cocoon cooking to check for siricin swelling and solubility showed that the treatment duration should be gradually increased to reach optimum swelling and solubility of sericin with low temperature(70$^{\circ}C$) . High temperature, however, showed more sharp increase. 9) The more increased temperature in the drying of fresh cocoons, the less the sericin swelling and solubility were obtained. 10) In a specific cooking duration, the heavier the cocoon shell is, the less the swelling and solubility were obtained. 11) It was considered that there are differences in swelling or solubility between the filaments of each cocoon layer. 12) Sericin swelling or solubility in the cocoon filament was decreased by the wax extraction.. 13) The ionic surface active agent accelerated the swelling and solubility of the sericin at the range of pH 6-7. 14) In the same conditions as above, the cation agent was absorbed into the sericin. 15) In case of the increase of Ca ang Mg in the reeling water, its pH value drifted toward the acidity. 16) A buffering action was observed between the sericin and the water hardness constituents in the reeling water. 17) The effect of calcium on the swelling and solubility of the sericin was more moderate than that of magnecium. 18) The solute of the water hardness constituents increased the electric conductivity in the reeling water.

• Journal of Life Science
• /
• v.24 no.5
• /
• pp.567-572
• /
• 2014

Extracts of Platycodon grandiflorum have been reported to show anti-inflammatory, antioxidant, anti-metastatic, and hepato-protective effects. This study was designed to evaluate T-cell activation and M1/M2 differential macrophage activation by extracts of P. grandiflorum or P. grandiflorum containing various medicinal herbs. Using real-time RT-PCR, we analyzed expression levels of c-fos, and CD40L (T-cell activation markers) in splenocytes and iNOS, Ym1, and ARG1 in RAW 246.7 cells after treatment of CC (hot water extract of P. grandiflorum), MAEK (hot water extract of P. grandiflorum [82%] and six different plants), and HWAL (hot water extract of P. grandiflorum [7%] and eight different plants. The results showed that MAEK significantly elevated the expression of T-cell activation markers of splenocytes, with the c-fos gene activated more than 10-fold and the CD40L gene activated more than 6-fold. Although CD40L was significantly increased by CC and HWAL, the increase was only about 2-fold. In addition, CC and HWAL did not significantly activate the expression of the c-fos gene. On the other hand, CC elevated the M1 activation marker iNOS, and HWAL elevated the M2 activation marker Ym1 and ARG1 gene expression. In conclusion, MAEK could be used as an immune stimulant because of its ability to activate T cells (elicited c-fos and CD40L gene expression), whereas HWAL could serve as an anti-inflammatory agent because of its differential activation of M2 macrophages.

• Korean Journal of Food Science and Technology
• /
• v.3 no.3
• /
• pp.178-184
• /
• 1971

Samples of refined soybean oil were irradiated with lights from a 20-watt incandescent tungsten lamp, a 20-watt fluorescent daylight type lamp, a 20-watt low-pressure mercury vapor germicidal lamp, and direct sunlight for an experimental period of 147 days. Some samples were stored in a dark room throughout the period as a control. The peroxide values of all samples were measured every week. The induction period of the samples was arbitrarily taken as the time required for the samples to reach a peroxide value of 15. The induction period of the control was estimated at 198 days. Those of the samples irradiated with the incandescent light, the fluorescent light, the ultraviolet light, and the sunlight were estimated at 196, 119, 52 and 6 days, respectively. The sunlight showed by far the strongest prooxidant activity whereas the incandescent light showed the weakest but distinct prooxidant activity. The small temperature differences observed among the various samples throughout the experimental period did not seem to affect the oxidation rates of the irradiated samples in any significant way.

• Journal of Food Hygiene and Safety
• /
• v.16 no.3
• /
• pp.212-220
• /
• 2001

To investigate the modifying effect of Kwao Kreu, Pueraria mirifica (PM), we performed two kind of studies which are the non-surgical medium-term carcinogenicity study and the modulation of gap junctional intercellular communication study. The first study, a non-surgical medium-term carcinogenicity bioassay was done to investigate the modifying effect of Kwao Keru, Pueyaria mirifca (PH), a rejuvenating folk medicine from Thailand, on the male F344 rat liver. Specific pathogen free, male 6-week-old F3444 rats were divided into ten groups. To induce hepatocarcinogenesis, those in all groups were given a single i.p. injection of DEN (200 mg/kg) and were received two i.p. injection of DGA (300 mg/kg) at the ends of weeks 2 and 5. Rats of group 3-6 were given sodium phenobarbital (PB 0.05% in drink). A diet containing 10 mg/kg PM was given to group 2 during the post-initiation phase and to groups 4 and 5 during promotion and initiation phase, respectively. Group 6 was given the experimental diet alone throughout the experiment (8 weeks). Rats of group 7, 8, 9 and 10 were fed 1000 mg/kg PH in the same manner as group 2, 4, 5 and 6. All animals were sacrificed at 8 weeks after DEN administration. Result of the immunohistochemical staining of the glutathione S-transferase placental form (GST-p) indicated that the numbers and areas of the preneoplastic leisions were not significantly changed in all PM treatment group comparing to control group. Also the numbers and areas of GST-p positive foci among group 7, 8, 9 and 10 were not significantly changed in comparing to control group. To study the effect of PM on the modulation of gap junctional intercellular communication, the present study was performed scrape-loading dye transfer (SL/DT) assay in human keratinocytes. The results showed that PM could not modulate GJIC. These results indicate that Pueraria mirifica may have no carcinogenic effects on experimental hepatocarcinogenesis in rats and gap junctional intercellular communication in human keratinocyte.

• Journal of Acupuncture Research
• /
• v.29 no.2
• /
• pp.73-88
• /
• 2012

Objectives : The purpose of this study is to research the effects of acupuncturing $BL_{67}$ and $LI_1$ and determine the mechanism of action of acupuncturing $BL_{67}$ and $LI_1$ by measuring the changes of regional cerebral blood flow(rCBF) and mean arterial blood pressure(MABP) in normal rats and ischemic rats. Method : This study researched the effects of acupuncturing $BL_{67}$ and $LI_1$ on the change of rCBF and MABP. To determine the mechanism of action of acupuncturing $BL_{67}$ and $LI_1$, pretreatment with indomethacine and methylene blue was done. Result : 1. Acupuncturing $BL_{67}$ and $LI_1$ significantly increased rCBF and acupuncturing $BL_{67}$ and $LI_1$ induced increase of rCBF was significantly inhibited by pretreatment with indomethacin(1 mg/kg, i.p.), an inhibitor of cyclooxygenase, and methylene blue(10 ${\mu}g$/kg, i.p.), an inhibitor of guanylate cyclase. 2. Acupuncturing $BL_{67}$ and $LI_1$ decreased MABP and there was no significantly change of decrease of MABP on acupuncturing $BL_{67}$ and $LI_1$ by pretreatment with indomethacin and methylene blue. 3. These result suggested that acupuncturing $BL_{67}$ and $LI_1$ might significantly increase rCBF by dilating arterial diameter and mechanism of acupuncturing $BL_{67}$ and $LI_1$ might be mediated by cyclooxygenase and guanylate cyclase. 4. The rCBF was significantly and stably increased by acupuncturing $BL_{67}$ and $LI_1$ during the period of cerebral reperfusion in cerebral ischemic rats, which contrasted with the rapid and marked increase in the control group. Pretreatment with methylene blue significantly decreased rCBF by acupuncturing $BL_{67}$ and $LI_1$ during the period of ischemic state, increased rCBF during the period of cerebral reperfusion. These results suggested that the mechanism of acupuncturing $BL_{67}$ and $LI_1$ might be mediated by guanylate cyclase. Conclusion : Acupuncturing $BL_{67}$ and $LI_1$ can increase rCBF in normal state, and improve stability of rCBF in ischemic state. In addition, we suggested that mechanisms related with acupuncturing $BL_{67}$ and $LI_1$ was more involved in the guanylate cyclase pathway.

• Korean Journal of Veterinary Research
• /
• v.40 no.3
• /
• pp.471-478
• /
• 2000

The pharmacokinetic properties of KR-V compounds, recently developed as new anti-HIV agents, were studied after i.v. and p.o. administration in rats. The concentrations of the KR-V series were determined in rat plasma using an high-performance liquid chromatography (HPLC)-UV detection system. Of the 19 KR-V compounds investigated in the present study, only KR-V 3, 10, 14, 16 and 18-1 showed oral bioavailability. The plasma concentration-time data could be adequately described by an one-compartment open model. In the i.v. kinetic study (10mg/kg), the CLt of KR-V 3, 10, 14 and 16 (>4L/hr/kg) were significantly higher than that of KR-V 18-1 (1.1 L/hr/kg). The AUC of KR-V 18-1 was greater ($8.97{\mu}g{\cdot}hr/ml$) than that of the other compounds, but the Vd (0.58 L/kg) was lower. In the p.o. kinetic study (50mg/kg), although the t-1/2 of KR-V 18-1 was shorter than that of the other compounds, the AUC ($3.659{\mu}g{\cdot}hr/ml)$ and $C_{max}(1.891{\mu}g/ml$) were markedly higher. In a seperated in vitro experiment, only KR-V 18-1, of the 5 compounds with bioavailibility, exhibits potent activity against HIV-1 mutant strains. Therefore, KR-V 18-1 is expected to become a new potent anti-AIDS drug candidate/lead compound.

• Journal of Nutrition and Health
• /
• v.31 no.9
• /
• pp.1468-1480
• /
• 1998

This study was conducted to investigate the nutritional intake of people in rural areas using 24-hour recall method. Kyungki Yeoju, Kangwon Whengsung, Chungbuk Chungju, Kyungnam Ulju, and Junbuk Jungup were selected for this study. The results were as follows 1) The mean daily energy intake was 2055.7kcal for male, 1703.2kcal for female. Fat intake were 43.0g for male, 32.7g for (female and protein intake was 74.5g for male 61.5g for female. Nutrient intake of Ulju residents were the highest and that of Whengsung and Yeoju residents were the lowest. Nutrient intake decreased significantly in elderly over 70 years. 2) Nutrients consumed below 80% of Korean RDA were Ca, Vit A, riboflavin and Vit E. Ulju residents consumed significantly higher protein, Ca, P compared to other area residents. P, Fe, Vit C intake of adults male were significantly higher than those of elderly over 80 years. Vit A, thiamin and riboflavin consumption of adults female were also significantly higher than those of elderly over 80 years. Ca, Vit A, riboflavin and Vit I were consumed below the Korean RDA in both male and female. 3) Average CPF ratio of energy intake was 69.2 : 14 : 16.8. Energy intake ratio from carbohydrate was significantly lower in Ulju residents compared to Yeoju and Jungup residents. Energy intake ratio from protein was significantly higher in Ulju area than the other areas. Carbohydrate dependency was increased with age, meanwhile fat dependency was decreased with age. 4) The mean adequacy ratio(MAR), an index of overall dietary quality, were significantly different among areas : the highest was 0.81 in Ulju, the lowest was 0.65 in Whengsung. Adults of 20-49 years showed the highest MAR of 0.76 and the lowest MAR was 0.52 in over 80 years group. The indexes of nutritional quality(INQ) was higher in 01;u area than the other areas, and INQ showed the tendency to decrease with increasing age. Especially, there were significant decrease in INQ of all nutrients except Vit A with age. Based on these results, it is evident that people in rural area did not consume enough nutrients. Specially, dietary intake of Vit A, Vit B$_2$, Vit E and Ca were not adequate. (Korean J Nutrition 31(9) : 1468-1480, 1998)