• Herbal Formula Science
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• v.7 no.1
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• pp.167-181
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• 1999

Rhizoma Arisaematis, Lignum Akebiae, Rhizoma Zedoariae, Cortex Eucommiae, Folium Perillae, Radix Sophorae Subprostratae, Radixi, Radix Ledeboutriellae, Rhizoma Atractylodis, Herba Ephedrae, Radix Puerariae and Radi Aconitx Bupleuri have been used in Korea for many centuries as a treatment for various disease. The purpose of the present study is to determine the effect of several herbs on norepinephrine(NE) induced blood vessel contraction in rabbits and pigs. Rabbit(2 kg, male) were killed by $CO_2$ exposure and a segment (8-10mm) of each rabbit was cut into equal segments and mounted in a tissue bath. Contractile force was measured with force displacement transducers under 2-3 g loading tension. The dose of norepinephrine(NE) which evoked 50% of maximal response $(ED_{50})$ was obtained from cumulative dose response curves for NE $(10^{-6}{\sim}10^{-3}M)$. Contractions evoked by NE $(ED_{50})$ were inhibited significantly by Rhizoma Arisaematis, Lignum Akebiae, Rhizoma Zedoariae, Cortex Eucommiae, Folium Perillae, Radix Sophorae Subprostratae and Herba Ephedrae in abdominal aorta. Contractions evoked by NE $(ED_{50})$ were inhibited significantly be Lignum Akebiae, Rhizoma Zedoariae, Cortex Eucommiae, Herba Ephedrae, Radix Puerariae and Radix Bupleuri in femoral artery. Contractions evoked by NE $(ED_{50})$ were inhibited significantly by Radix Sophorae Subprostratae, Radix Aconiti and Herba Ephedrae in renal artery. These results indicate that each herb can relax NE induced contraction of rabbit and pig blood vessel selectively, and that this relaxation relates to Gui-Gyung(歸經).

• YAKHAK HOEJI
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• v.50 no.4
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• pp.254-262
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• 2006

This study had been done for the investigation of the effect of Vitis vinifera extract(V), Schisandra chinensis extract (S), Taraxacum officinale extract (T), Gardenia jasminoides extract (G), Angelica acutiloba extract (A) and Paeonia japonica extract (P), and their mixtures on the antioxidant and ethanol oxidation system which was induced by Lieber-DeCarli ethanol liquid diet. Male Sprague-Dawley rats were randomly divided into eight groups: ethanol diet (ED), normal diet (ND), ED+V (100 mg/kg/day), ED+S, ED+T, ED+G, ED+A and ED+P (300 mg/kg/day). We studied the effect on alcohol dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH) after herbal extracts administration for 6 weeks in rats induced by Lieber-DeCarli ethanol liquid diet. The differences in ADH and ALDH activity of the rats treated with herbal extracts and ED group were not significant. Phase I enzyme activity was found to be significantly higher in the ED+V than the ED group. Phase II enzymes (glutathione-S-transferase, phenol sulfatransferase) activities were found to be higher in the herbal extracts than the ED group. Herbal extracts not only reduced ethanol-induced elevation of level malondialdehyde but also protected against ethanol-induced decrease of reduced glutathione, gluthione reducatse, glutathione peroxidase, catalase and superoxide dismutase activities. Therefore, they can be utilized as a health functional food or new drug candidate for fatty liver and hepatotoxicity which was induced by chronic alcohol consumption.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.233.3-234
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• 2002

SB31, an extract of Pulsatilla koreana, has been tried as an antitumor agent by traditional medicine pratitioner in Korea for the past 30 years, SB31 was evaluated for cytotoxic and antitumor activity against a variety of cancer cell lines. The SB31 exhibited 5-6 fold less cytotoxic activity against normal mononuclear cells (ED$\sub$50/. 1.1 mg/$m\ell$) than against cancer cell lines (ED$\sub$50/ 0.14-0.19mg/$m\ell$). (omitted)

• Journal of Food Hygiene and Safety
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• v.11 no.4
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• pp.299-306
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• 1996

6-[(N-3,4-Dibromophenyl)amino]-7-chloro-5,8-quinolinedione(FCK13) was tested for antifungal activities. The MIC values were determined by the two-fold dilution method. The therapeutic potential of RCK13 had been assessed in comparison with ketoconazole and fluconazole against systemic infections with candida albicans in normal mice. RCK13 had ED50,0.80$\pm$0.21 mg/kg but ketoconazole had ED50, 8.00$\pm$0.73 mg/kg respectively. And administered RCK13 at the ED50 for 14 days improved survival rates as well as ketoconazole. Acute oral toxicity studies of RCK13 were carried out in ICR mice of both sexes. These acute oral toxicities of RCK13 were low and LD50 values were over 2,850 mg/kg in ICR mice. The genotoxicities of RCK13 had been evaluated. RCK13 was negative in Ames test with Salmonella typhimurium and chromosomal aberration test in CHL cells. The clastogenicity was tested on the RCK13 with in vivo mouse micronucleus assay. RCK13 did not show any clastogenic effect in mouse peripheral blood and was negative in mouse micronucleus assay. These results indicate that RCK13 has no genotoxic potential under these experimental conditions.

• YAKHAK HOEJI
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• v.42 no.2
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• pp.159-164
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• 1998

The secondary hydroxy group at side chain of shikonin structure was selectively acylated with various haloacetic acids in presence of dicyclohexylcarbodiimide and 4-dimethylamin opyridine to produce haloacetylshikonin derivatives. The cytotoxicity of monohaloacetylshikonin derivatives against L1210 cells increased in the following order; monochloroacetylshikonin ($ED_{50}$, 0.142${\mu}$g/ml) > monobromoacetylshikonin ($ED_{50}$. 0.158${\mu}$g/ml) > monoiodoacetylshikonin ($ED_{50}$, 0.173${\mu}$g/ml). Introduction of larger halogen atoms decreased the cytotoxic activity, presumably due to steric hinderance. The cytotoxicity of chloroacetylshikonin derivatives was dependent on the number of chlorine atom, thus increasing in the following order; trichloroacetylshikonin (0.032${\mu}$g/ml) > dichloroacetylshikonin (0.059${\mu}$g/ml) > monochloroacetylshikonin ($ED_{50}$, 0.142${\mu}$g/ml). Thus, the electron withdrawing effect seems to be important for the cytotoxicity of chloroacetylshikonin derivatives. Consistent with the above, dichloroacetylshikonin (T/C. 182%) and trifluoroacetylshikonin (195%) showed higher T/C values than monochloroacetyl-(T/C, 122%), monobromoacetyl-(T/C, 154%) and monoiodoacetylshikonin (T/C, 117%) derivatives. Haloacetylshikonin derivatives showing lower cytoxic activities against L1210 cells exhibited lower T/C values. It seems that there is a relationship between the cytoxicity of haloacetylshikonin and their antitumor activity.

• Parasites, Hosts and Diseases
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• v.49 no.1
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• pp.17-23
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• 2011

The aim of this study was to assess the cytotoxic effects of various concentrations of miltefosine on Leishmania major (MRHO/IR/75/ER) and L. tropica (MHOM/IR/02/Mash10) promastigotes and to observe the programmed cell death features. The colorimetric MTT assay was used to find L. major and L. tropica viability and the obtained results were expressed as 50% inhibitory concentration (IC50). Also, 50% effective doses (ED50) for L. major and L. tropica amastigotes were also determined, Annexin-V FLUOS staining was performed to study the cell death properties of miltefosine using FAGS analysis. Qualitative analysis of the total genomic DNA fragmentation was performed by agarose gel electrophoresis. Furthermore, to observe changes in cell morphology, promastigotes were examined using light microscopy. In both strains of L. major and L. tropica, miltefosine induced dose-dependent death with features of apoptosis, including cell shrinkage, DNA laddering, and externalization of phosphatidylserine. The IC50 was achieved at 22 ${\mu}M$ and 11 ${\mu}M$ for L. major and L. tropica after 48 hr of incubation, respectively. ED50 of L. major and L. tropica amastigotes were 5.7 ${\mu}M$ and 4.2 ${\mu}M$, respectively. Our results indicate that miltefosine induces apoptosis of the causative agent of cutaneous leishmaniasis in a dose-dependent manner. Interestingly, L. major did not display any apoptotic changes when it was exposed to miltefosine in concentrations sufficient to kill L. tropica.

• YAKHAK HOEJI
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• v.40 no.5
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• pp.608-615
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• 1996

6-[(N-3,4-Difluorophenyl)amino]-7-chloro-5,8-quinolinedione(RCK4) was tested for antifungal activities, against systemic infections with Candida albicans in normal mice. The therapeutic potential of RCK4 had been assessed in comparison with ketoconazole and fluconazole. RCK4 had $ED_{50},\;0.30{\pm}0.14$ but ketoconazole and fluconazole had $ED_{50},\;8.00{\pm}0.73,\;10.00{\pm} 0.43mg/kg$ respectively. Intraperitoneally administered RCK3 at the $ED_{50}$ for 7 days and 14 days reduced Candida albicans colony count in the kidneys and liver as well as ketoconazole and fluconazole at these $ED_{50}$. And administered RCK4 at the $ED_{50}$ for 14 days improved survival rates as well as ketoconazole. Acute oral toxicity studies of RCK4 were carried out in ICR mice of both sexes. These acute oral toxicities of RCK4 were low and $LD_{50}$ values were over 2,850mg/kg in ICR mice. The genotoxicities of RCK4 had been evaluated. RCK4 was negative in Ames test with Salmonella typhimurium and chromosomal aberration test in CHL cells. The clastogenicity was tested on the RCK4 with in vivo mouse micronucleus assay. RCK4 did not show any clastogenic effect in mouse peripheral blood and was negative in mouse micronucleus assay. These results indicate that RCK4 has no genotoxic potential under these experimental conditions.

• Journal of Sericultural and Entomological Science
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• v.9
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• pp.67-87
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• 1969

1. Objectives and Importance. Many silkworms have been damaged by nuclear polyhedrosis virus diseases thoughout the country every year causing a decease in cocoon production by approximately ten per cent per year. The damage caused by the infections virus has occured in spite of complete disinfection. In this respect, it is well known it is impossible, at the present time, to protect the silkworm from these virus infections through chemical and physical control methods. Therefore, this author has attempted to solve this urgent problem from the view point of heredity and breeding, discovering the different resistances and heritabilities among 120 stains collected from throughout the country, and selecting the ones with highest resistance for the basic materials in the silkworm breeding. 2. Results of work 1) The strains with strong resistance to the nuclear polyhedrosis virus diseases are N$_4$, N$\sub$15/, N$\sub$48/, C$\sub$55/ and Em. the log ED$\sub$50/ values of them vary between 0.799 and 1.611. The susceptible strains are N$\sub$20/, C$\sub$62/, N$\sub$76/, N$\sub$79/ and C$\sub$108/, the log ED$\sub$50/ values of them vary between 5.159 and 7.258. (Reference Table 4) The Japanese strain with a log ED$\sub$50/, value of 3.770 is the strongest, followed by the Chinese strain with a log ED$\sub$50/ value of 3.564. The weakest is the European strain with a log ED$\sub$50/ value of 3.3381. The direction coefficient of the regression equation of the susceptibility varies between 0.1 and 0.6, the uniformness of the resistance of the preserved strains of this country is comparatively low. The hereditary henomena of the resistance of each strain and the conerete method of its application for silkworm breeding main the subjects for later studies. 2) The content of water and ash in silkworm has not been correlated with the capability for resistance to the virus diseases(Reference. Table 8). but it is very significantly correlated with mortality rate (in common reaning). In the case of the silkworms which have just completed the fourth moulting the content of water and ash is not related to the mortality rate. In the case of the silkworms which have just completed the third moulting, however, the water( +0.326) and ash (+0.362) registered a high significance. The ash content in the first ($\div$0.520) and second ($\div$0.386) moults is highly significant but water content in both cases is not significant (Reference Table 7). 3) The No. 205 strain proved to be the best in character among the various F$_1$ hybrids. No. 204 was very good in strength but a little lower in cocoon character than the control. No. 212 was a little low in coccon character and mortality was average, but the cocoon harvest was the best among all the varieties offered for (Reference Table 9). 4), In short, the above mentioned strains which are known to have strong resistance to the virus disease are expected to provide basic data for breeding strong varieties. It is proposed that continued research should be conducted on the characteristics of various strains for a satisfactory preservation of various characteristics.research should be conducted on the characteristics of various strains for a satisfactory preservation of various characteristics.

• Archives of Pharmacal Research
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• v.19 no.3
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• pp.197-200
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• 1996

6-[(N-2,3-Dichlorophenyl)aminol-7-chloro-5,8-quinolinedione (RCK1 1) was tested for in vivo antifungal activities in the treatment of systemic infection with Canclicla albicans in normal mice compared with ketoconazole. The therapeutic potential of RCK11 had been assessed by evaluating their activities (survival rates) against systemic infections in normal mice. $ED_{50}$ of intraperitoneally administered RCK11 was $0.10\pm0.01 mg/kg$ but that of ketoconazole had $8.00\pm0.73 mg/kg$ respectively. When RCK11 was administered intravenously at the $ED_{50}$(0.10 mg/kg), the colony counts of Canoliola albicans in the liver after 7 days and 14 days were reduced as likely as ketoconazole at the $ED_{50}$ (8.00 mg/kg), and the better survival rates than ketoconazole were achieved after 14 days. The results suggest that RCK11 may be a potent antifungal agent.

• Archives of Pharmacal Research
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• v.20 no.6
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• pp.586-589
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• 1997

Antifungal activities of 6-[(N-4-bromophenyl)amino]-7-chloro-5,8-quinolinedione (RCK7) were tested. The MIC values of RCK7 were determined for antifungal suceptibility, in vitro against Aspergillus niger, Cryptococcus neoformans and Trichophyton mentagrophyte by standard agar streak method. In vitro, RCK7 showed more potent antifungal activity than fluconazole and ketoconazole. Also, RCK7 was tested for in vivo antifungal activity in the treatment of systemic infection with Candida albicans in normal mice. The therapeutic potential of RCK7 had been assessed by evaluating their survival rate against systemic infections compared with that of ketoconazole. $ED_{50}$ of intraperitoneally administered RCK7 ws $2.05{\pm}0.30mg/kg$ but that of ketoconazole was $8.00{\pm}0.73 mg/kg$, respectively. When RCK7 was administered intravenously at the $ED_{50}$(2.05 mg/kg). the colony counts of Candida albicans in the liver after 7 days and 14 days were reduced as likely as ketoconazole at the $ED_{50}(8.00 mg/kg)$, and the better survival rates than ketoconazole's were achieved after 14 days. The results suggest that RCK7 may be a potent antifungal agent.