• 대한한의학방제학회지
• /
• 제7권1호
• /
• pp.167-181
• /
• 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).

• 약학회지
• /
• 제50권4호
• /
• pp.254-262
• /
• 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.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
• /
• pp.233.3-234
• /
• 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)

• 한국식품위생안전성학회지
• /
• 제11권4호
• /
• pp.299-306
• /
• 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.

• 약학회지
• /
• 제42권2호
• /
• pp.159-164
• /
• 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
• /
• 제49권1호
• /
• pp.17-23
• /
• 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.

• 약학회지
• /
• 제40권5호
• /
• pp.608-615
• /
• 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.

• 한국잠사곤충학회지
• /
• 제9권
• /
• pp.67-87
• /
• 1969

1. 본 조사는 현재 우리나라에 보존되어 있는 계통을 전부 수집하여 Virus병에 대한 저항성을 계통별로 조사함으로써 잠견생산에 막대한 피해를 주는 Virus병에 대하여 저항성이 강한 계통을 선발하는 동시에 선발된 결과는 앞으로 저항성품종 육성제료로 삼고저 하였다. 2. 가잠의 핵형다각체 Virus병에 대하여 저항성이 강한 계통은 N$_4$, N$_{6}$, N$_{46}$, $C_{85}$, E$_{111}$로써 log ED$_{50}$ 값이 0.799~1.611 범위내에 있으며 강한 계통으로서는 N$_{10}$, $C_{62}$, N$_{70}$, N$_{79}$, $C_{106}$이고 log ED$_{50}$의 값은 5.159~7.258 범위내에 있다(표 4참조) 그러고 일본계통이 가장 강하여 log ED$_{50}$이 3.770이 3.770이고 중국계통의 log ED$_{50}$은 3.564로서 다음이고 가주계통의 log ED$_{50}$이 3.381로서 가장 강한 계통으로 나타났다. 감염율의 회귀방정식의 방향계수는 0.1~0.6범위로서 우리나라 보존계통의 저항성의 균일성이 비교적 작을 경향을 다타냈다. ra계통별 저항성의 유전현상에 대한 해명과 품질육성을 위한 구체적인 응용방법에 관한 구명은 차후의 숙제로 남게 되었다. 3. 잠체의 수분 및 회분과 Virus병에 대한 저항성과는 상관관계가 없었고(표 8참조) 다만 감잠비율(보통 사육법에 의하여 조사된 것)과는 고도의 상관관계가 있다. 즉 4면 기잠에서는 수분 및 회분과는 관계가 없었고 3면 기잠에서는 수분은 +0.326 회분은 +0.326으로서 고도의 유의성을 나타냈고 1면과 2면의 회분에서는 각각 +0.520과 ＋386으로서 고도의 유의성을 나타냈으나 수분에서는 유의성이 없었다(표7 참조). 4. 교배조간에 있어서는 기호 205가 모든 형질에 있어서 가장 우수하였다. 특히 204는 강건성이 매우 좋았으나 견질에 있어서 대조구보다 약간 떨어진다. 기호 212는 견질을 약간 떨어지고 감잠비율은 보통이나 수견량이 공시품종중 가장 많았다(표 11). 5. 종합적으로 기술하면 Virus에 대한 저항성이 강한 상기 몇 계통은 강건성 품종？성을 위한 기초자료가 될것이며 계속 여러 계통외 특성을 조사하여 특성 보존을 위한 품종보존의 완벽을 기하여야겠다.다.

• Archives of Pharmacal Research
• /
• 제19권3호
• /
• pp.197-200
• /
• 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
• /
• 제20권6호
• /
• pp.586-589
• /
• 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.