• YAKHAK HOEJI
• /
• v.32 no.1
• /
• pp.80-85
• /
• 1988

QSAR of Salicylic acid derivatives, as anti-inflammatory agent, classified into Group I (not-having-5-phenyl ones) and Group II (having-5-phenyl ones) were investigated by quantum chemical calculations. The results are below: not significant statistically for both of Group I and Group II, but significant for each Group. $potency=-8.46X_{5}+1.639\;n=5\;r=0.77\;se=0.31\;for\;Group\;I.$ $({\pm}4.05)\;({\pm}0.5)$ where $X_5$ means charge of carbon atom bonded to hydroxyl radical. $potency=0.16X_{19}+7427.38HO-6629.85X_{15}+4977.40X_{10}+351.51X_5+3378.84$ $({\pm}0.17)\;({\pm}10.18)\;({\pm}11.70)\;({\pm}33.78)\;({\pm}4.41)\;({\pm}13.13)$ n=7 r=0.99 se=0.019 for Group II. where $X_{19}$ and $X_{15}$ stand for charges of the para carbon and the first carbon atoms in phenyl radical, respectively and $X_{10}$, charge of carboxylic carbon atom, HO, HOMO energy. It seems to be possible to qualitatively predict potency of drug by Pearson's HSAB theory. It means that drug should possess low LUMO energy and high HOMO energy.

• The Research Journal of the Costume Culture
• /
• v.12 no.1
• /
• pp.28-40
• /
• 2004

The purpose of this study was (1) to identify the experimental bias which could appear person perception as results of development methods (2) to find out the most desirable method in developments of stimulus. The research was a quasi experiment and the subjects were 358 male and female undergraduate students by convenient sampling. The experimental instruments consisted of a set of stimulus and semantic differential scales of 7-point bi-polar adjectives. The collected data were analyzed by Principle Component Analysis, ANOVA(analysis of variance), Scheffe's multiple range test. The independent variables were developing methods of stimulus(live person, photography of real person, 2 kinds of black and white line drawing, 2 kinds of color drawing). The results were as follows. First, five factors which were potency, sociality, appearance, evaluation, activity impressional dimensions emerged to account for the methods of development of stimulus. Second, the methods of development of stimulus had significant effects on potency, sociality, appearance, activity factors. In sociality factors, the impression of photographic stimulus was the closest to the live person's impression. However in the appearance and activity impressions, significant difference existed between live person and other developing stimulus. In the potency impression, black and white line-drawing gave the highest impressional bias. In the sociability and appearance impressions, color-drawing stimulus gave the highest impressional bias. Result: On conclusion the developments of stimulus can effect on stimulus person's impressions and these effects can produce experimental biases, the photographic stimulus gave the least impressional bias. The study shows that photography of real person will produce minimize measurement error.

• Journal of Pharmaceutical Investigation
• /
• v.30 no.2
• /
• pp.127-131
• /
• 2000

Previously, we have reported an antitumor efficacy of liposomal N-(phosphon-acetyl)-L-aspartic acid (or PALA) in C-26 tumor bearing Balb/c mice, where PALA in liposome was administered one day after tumor inoculation. In this report, we have investigated the therapeutic potency of liposomal formulation of PALA, which was administered eight days after tumor inoculation in the same C-26 tumor bearing mice. The C-26 murine colon tumor inoculated mice were randomized for the in vivo therapy and the survival was measured after a single intraperitoneal injection of the drug. When the therapy was initiated eight days after tumor inoculation, DSPC-PALA at 150 mg/kg resulted in a significant increase in median survival time (MST) of 56% over the control group which received MES/HEPES buffer alone. However, none of the free PALA and DSPG-PALA liposome doses caused a statistically significant increase in MST over control group at the 95% confidence level. At 750 mg/kg dose, free PALA caused a marginally significant improvement in MST by 34%, but both 375 mg/kg and 150 mg/kg doses of free PALA caused only a 2% and a 4% increase in MST, respectively. These results show that PALA in neutrally charged liposome can exhibit considerably greater potency than free PALA in established C-26 tumor bearing mice.

• Journal of the Korean Society of Clothing and Textiles
• /
• v.27 no.5
• /
• pp.496-504
• /
• 2003

The purpose of this study was (1) to identify the experimental bias which could appear person perception as results of presentation methods (2) to find out the most desirable method in presentation of stimulus. The research was a quasi experiment and the subjects were 773 male and female undergraduate students. The experimental instruments consisted of a set of stimulus and semantic differential scales of 7- point hi-polar adjectives. The collected data were analyzed by Factor Analysis, ANOVA(analysis of variance), Scheffe＇s multiple range test. The independent variables were presentation orders and presentation time of stimulus. The results were as follows: First, five factors which were potency, sociality, appearance, evaluation, activity impression dimensions emerged to account for the methods of development of stimulus. Second, the presentation order of stimulus in the combination of four stimuli sets had significant effects on the 3 impressional factors(sociality, appearance, evaluation). The presentation order of stimuli in the combination of eight stimuli set had significant effects on the 3 impressional factors(potency, sociality, appearance) and the presentation order of stimuli in the combination of eight stimuli set showed a significant effect on memorization of stimulus and the results support the recency effect. Third, the presentation time of stimuli had significant effects on the 2 impressional factors(potency, activity). 30 seconds presentation as well as free duration time resulted less experimental bias than 3 seconds presentation.

• Archives of Pharmacal Research
• /
• v.20 no.6
• /
• pp.579-585
• /
• 1997

To gain further insight into the mechanism of action of antiestrogens, we examined the interaction of antiestrogen with the estrogen receptor system and with estrogen- noncompetable antiestrogen binding sites. In addition to binding directly to the estrogen receptor, antiestrogens can be found associated with binding sites that are distinct from the estrogen receptor. In contrast to the restriction of estrogen receptors to estrogen target cells, such as those of uterus and mammary glands, antiestrogen binding sites are present in equal amounts in estrogen receptor-positive and -negative human breast cancer cell lines, such as MCF-7, T47D, and MDA-MB-231 that differ markedly in their sensitivity to antiestrogens. In order to gain greater insight into the role of these antiestrogen binding sites in the action of antiestrogens, we have examined the biopotency of different antiestrogens for the antiestrogen binding sites and that is CI628 > tamoxifen > trans-hydroxy tamoxifen > CI628M > H1285 > LY117018. This order of affinities does not parallel the affinity of these compounds for the estrogen receptor nor the potency of these compounds as antiestrogens. Indeed, compounds with high affinity for the estrogen receptor and greatest antiestrogenic potency have low affinities for these antiestrogen binding sites. Antiestrogenic potency correlates best with estrogen receptor affinity and not with affinity for antiestrogen binding sites. In summary, our findings suggested that interaction with the estrogen receptor is most likely the mechanism through which antiestrogens evoke their growth inhibitory effects.

• Journal of Pharmacopuncture
• /
• v.11 no.1
• /
• pp.99-107
• /
• 2008

Objectives : This experimental study was performed to investigate the effect of herbal eye drops(Sean-tang, Jinpi-san, Tangpo-san, Copitdis Rhizoma) on Staphylococcus aureus keratitis. Methods : After administering various herbal eye drops on Staphylococcus aureus, I measured MIC and the size of inhibition zone. MIC was measured by dropping from 20 to $50{\mu}{\ell}$ according to density. Anti-bacterial potency was measured by the size of inhibition zone with change of volume under 2 days culture condition. Also continuous antibacterial potency of herbal eye drops was measured by the size of inhibition zone according to 2 days and 6 days culture each under the $50{\mu}{\ell}$condition. Results : 1. MIC on Staphylococcus aureus in Sean-tang, Jinpi-san and Tangpo-san was 100%, $20{\mu}{\ell}$. 2. MIC on Staphylococcus aureus in Coptidis rhizoma was 10%, $30{\mu}{\ell}$. 3. MIC on Staphylococcus aureus in Cravit was 0.1%, $50{\mu}{\ell}$. 4. Under the 2 days culture condition, the size of inhibition zone on Staphylococcus aureus by volume for Sean-tang was 12.0mm in $50{\mu}{\ell}$, Jinpi-san was 19.0mm in $50{\mu}{\ell}$, Tangpo-san was 15.0mm in $50{\mu}{\ell}$, Coptidis rhizoma was 32.7 mm in $50{\mu}{\ell}$ and Cravit was 31mm in $50{\mu}{\ell}$, Coptidis rhizoma showed the highest anti-bacterial potency. 5. Under the $50{\mu}{\ell}$ condition, the size of inhibition zone on Staphylococcus aureus by 2 and 6 culture days for Sean-tang was 12.0mm, Jinpi-san was 19.0mm, Tangpo-san was 15.0mm, Coptidis rhizoma was 32.7mm and Cravit was 31.0 mm, which showed sameness anti-bacterial potency in 2 days and 6 days. Conclusions : The present author think that the herbal eye drops can be used to cure Staphylococcus aureus keratitis and if further study is performed, the use of the herbal eye drops will be valuable and beneficial in the clinical medicines.

• Asian Pacific Journal of Cancer Prevention
• /
• v.16 no.14
• /
• pp.5635-5641
• /
• 2015

Background: Cirrhosis is regarded as a possible end stage of many liver diseases, including viral infection. It occurs when healthy liver tissue becomes damaged and is replaced by scar tissue and finally may lead to hepatocellular carcinoma. Interferons (IFNs)are two general categories, type I and II. Type I includes one beta interferon and over 20 different alpha interferons. Alpha interferons are very similar in how they work, interacting with other proteins on cells like receptors. The main objective of this study was to compare Mx gene productivity post different cell line treatment with imported and Egyptian biosimilar locally produced IFNs, as well as the efficacy of those tested IFNs. Also, an assessment was made of sensitivity of different cell lines as alternatives to that recommended for evaluation of antiviral activity. Materials and Methods: Different cell lines (Vero, MDBK and Wish) were employed to evaluate cytotoxicity using the MTT assay. Antiviral activity was evaluated compared with standard IFN against VSV, Indiana strain -156, on tested rh-IFNs (imported; innovated and Egyptian biosimilar locally produced IFNs) in the pre-treated cell lines previously mentioned. The virus was propagated in the Wish cell line as recommended. Finally we estimated up-regulation of the Mx gene as a biomarker. Results: Data recorded revealed that test IFNs were safe in test cell lines. Viability was around 100%. Locally tested interferon did not realize the international potency limits, while the imported one was accepted compared with the standard IFN. These results were the same either using infectivity titer reduction assay or crystal violet staining of residual non- infected cells. Mx protein production was cell type related and confirmed by the detected Mx gene expressed in imported and locally produced IFN pre-treated cell lines. The expression of the gene was arranged in the order of Vero> wish > MDBK for the imported IFN, while for the Egyptian biosimillar locally produced one it was MDBK> Vero> wish. With regard to the antiviral activity there was a significant difference of imported IFN potency compared with the locally produced IFN (P<0.05), the IFN potential (antiviral activity) was not cell line related and showed non-significant difference for each separate product. Conclusions: Vero cells can be used as an alternative cell line for evaluation of IFN potency in case of unavailable USP recommended cell lines. Alternative potency evaluation assay could be used and proved significant difference in IFN potency in case of local and imported agents. Evaluation of antiviral activity could be used in parallel to viral infectivity reduction assay for better accuracy. Mx gene can be used as a marker for IFN potential.

• The Journal of Internal Korean Medicine
• /
• v.36 no.2
• /
• pp.165-179
• /
• 2015

Objectives: This experiment investigated the antimicrobial activity of Hwangryunheadok-tang and extracts of Scutellariae radix , Phellodendri cortex , Coptis rhizome , and Gardenia jasminoides against Salmonella typhimurium . Methods: After spreading S. typhimurium on a bacterial culture medium plate, antimicrobial activity was tested by dripping diluted Hwangryunheadok-tang or extracts of Scutellariae radix , Phellodendri cortex , Coptis rhizome , or Gardenia jasminoides (80 μl, diluted 100, 50, 10, and 1%) onto the plate, followed by culture for 16 to 72 hours. The minimal inhibitory concentration (MIC) was tested by dripping the minimum dilution that showed antimicrobial activity (80, 60, 40, and 20 μl) and measuring the density. The antimicrobial activity of Hwangryunheadok-tang and four extracts showed continuous antibacterial activity against S. typhimurium throughout the experiment. Result: 1. S. typhimurium . (Standard Microorganism, ATCC) 1) The Hwangryunheadok-tang and extracts of Scutellariae radix , Phellodendri cortex , and Coptis rhizome showed antibacterial activity in the undiluted solutions and in 50% dilutions. Gardenia jasminoides extract showed potency only in the undiluted solution. The antimicrobial potency of the undiluted solution was increased when the volume of inoculation was increased, but no difference was noted when the culture time was extended. All the extracts showed antimicrobial potency against S. typhimurium . 2. S. typhimurium isolated from diarrhea patients 1) When compared to the standard microorganism experiment on S. typhimurium , the MICs of the five extracts were increased. However, whereas the antimicrobial potency of doxycycline was lost entirely against bacteria isolated from patients with diarrhea, the antimicrobial potency of all the extracts was diminished but did not disappear. 2) The antimicrobial activity of Hwangryunheadok-tang and four extracts was continuous even when the culture time was extended to 16, 24, and 72 hours. Conclusions: The Hwangryunheadok-tang and four kinds of extracts have antimicrobial activity against S. typhimurium . Comparison of a standard microorganism with S. typhimurium isolated from diarrhea patients showed that the antimicrobial activity of all the extracts was better than that of antibiotics. Further studies should focus on the value and benefits of Hwangryunheadok-tang , and the four kinds of extracts as clinical treatments.

• Korean Journal of Veterinary Research
• /
• v.33 no.3
• /
• pp.547-554
• /
• 1993

This study was carried out to investigate the best condition for in vitro and in vivo culture after freezing and thawing of nuclear transplant 2 cell embryos. When nuclear transplant embryos were submitted to electrofusion, the significantly higher fusion rates of 2 cell donor nuclei were achieved at the electric field strength of DC 1.5 kV/cm for 100 and $150{\mu}sec$, DC 2.0 kV/cm for 100 and $150{\mu}sec$ than DC 1.0 kV/cm for 100 and $150{\mu}sec$(p<0.01). The significantly higher fusion rates of 4 cell donor nuclei were achievecl at DC 2.0 kV/cm for 100 and $150{\mu}sec$ than DC 1.0 kV/cm for 100 and $150{\mu}sec$(p<0.01). The fusion rates in 8 cell donor nuclei were 94.2~99.3%. The developmental potency to blastocyst in 2 cell donor nuclei was significantly higher in DC 2.0 kV/cm for $150{\mu}sec$ treated group(p<0.01). The significantly higher developmental potency to blastocyst in 4 cell donor nuclei were achieved at the electric field strength of DC 2.0 kV/cm for $150{\mu}sec$ than DC 1.5 kV/cm for 100 and $150{\mu}sec$, DC 2.0 kV/cm for $100{\mu}sec$ treated group(p<0.01). The develop mental potency to blastocyst in 8 cell donor nuclei was significantly higher in DC 2.0 kV/cm for $100{\mu}sec$ treated group(p<0.01). The developmental potency to blastocyst after nuclear transplantation was significantly higher in 2 cell donor nuclei than in 8 cell donor nuclei(p<0.01). When the recovered embryos in normal morphology were cultured in vitro, there were no significant differences in the developmental potency to blastocyst between the freezing methods and the concentrations of cryoprotectant(p<0.01). The production rates of offspring after transfer of nuclear transplant embryos to recipient mouse were no significant difference in 2, 4 and 8 cell donor nuclei.

• Bulletin of the Korean Chemical Society
• /
• v.33 no.9
• /
• pp.2991-2998
• /
• 2012

A series of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was synthesized and their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 9, 11, 12, 14, and 17-21 showed superior potency against A375P to Sorafenib. Over the NCI-60 cancer cell line panel, compound 14 possessing a methoxy group, amide linker, and 4-chloro-3-(trifluoromethyl)phenyl terminal ring showed the highest potency and broad-spectrum anticancer activity. Compound 13 showed high selectivity towards leukemia subpanel over other cancer types.