• Title/Summary/Keyword: LD50

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A Study on the Correlationship among QSAR Parameters and Toxicity Data of Amine- and Nitrocompounds (아민 및 니트로화합물에 대한 QSAR의 물리화학적 매개변수 및 독성과의 상관관계)

  • 김재현;김애경
    • Environmental Analysis Health and Toxicology
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    • v.14 no.1_2
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    • pp.45-54
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    • 1999
  • Quantitative strucrure-activity relationships between the toxicity (LD$\_$50/) and molecular properties of amine and nitro compounds were tested. The all 19 compounds showed low correlations below 0.500 to their LD$\_$50/ values. When amine or nitro compounds were taken separately, the correlation between the calculated chemphysico parameters and LD$\_$50/ were also poor (r$^2$=0.4911, 3967 repectively). The overall relationships among the QSAR parameters were investigated. Molecular weight shows a high correlation with total surface area (r$^2$=0.9287); 0.9090 for zero-order connectivity and second-order connectivity : 0.8784 for bioconcentration factor and second-order connectivity. When amine compounds were taken to perform the statistical treatment, the relationships between parameters were as follows: 0.8436 for volume-negentropy; 0.8925 for volume-bioconcentration factor; 0.9929 for zero-order connectivity-Kow; zero-order connectivity-bioconcentration factor; 0.9141 for zero-order connectivity-solubility; 0.9718 for solubility-bioconcentration factor; 0.9894 for solubility-bioconcentration factor and 0.9319 for Kow-bioconcentration factor. On the other hand, nitro compounds showed different relationships as follows: 0.8952 for volume-I/O character; 0.9520 for volume-total surface area: 0.9351 for volume-molecular weight; 0.9351 for volume-MW; 0.9961 for Kow-Koc; 0.8455 for Kow-bioconcentration factor; 0.8879 for Koc-bioconcentration factor; 0.9987 for MW-total surface area respectively.

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Acute Oral Toxicity Studies of WHS-1 and WHS-2 in Rats (경구용 복합제 WHS-1,2의 급성독성시험 연구)

  • 조대현;황세진;이원용;이주영;윤형중;문병우
    • Biomolecules & Therapeutics
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    • v.1 no.2
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    • pp.275-279
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    • 1993
  • Single oral administration to SD rats of both sexes were performed to investigate the acute toxicity of two new cough and cold remedies, WHS-1 and WHS-2. WHS-1 is composed of acetaminophen, chlorpheniramine maleate, cloperastine hydrochloride, dl-methylephedrine hydrochloride, caffein anhydrous, thiamine hydrochloride, riboflavin and serratiopeptidase. WHS-2 is composed of similar formula except that thiamine hydrochloride and riboflavin is not added. The results were as follows. $LD_{50}$ values of WHS-1 were 4295.5 mg/kg for males and 4606.3 mg/kg for females, and $LD_{50}$ values of WHS-2 were 3236.7 mg/kg for males and 4360.5 mg/kg for females. Death occurred within 2~3 hours after administration at doses up to 2900 mg/kg in WHS-1 and 2500 mg/kg in WHS-2, the main cause of deaths seemed to be respiratory disturbance. General symptoms included decreased motor activity, salivation and loss of consciousness which were commonly observed in all dead animals treated with WHS-1 and WHS-2. No significant gross finding and body weight changes were observed at any dose level in the groups treated with WHS-1 and WHS-2.

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Experimental Studies of quantitative evaluation using HPLC and safety of Bee Venom Acupuncture (봉독침의 봉독함량분석과 LD50 및 조직학적 소견 관찰)

  • Jang, Seong-Bong;Kwon, Ki-Rok
    • Journal of Pharmacopuncture
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    • v.9 no.1
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    • pp.155-165
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    • 2006
  • Objectives : This study was conducted to carry out quantitative evaluation and safety of Bee Venom Acupuncture. Methods : Content analysis was done using HPLC, measurement of $LD_{50}$, and histological observations were made on the skin and muscles. Results : 1. According to HPLC analysis, each BVA-1 contained approximately $0.36{\mu}g$, and BVA-2 contained approximately $0.54{\mu}g$. But the volume of coating was so minute, slight difference exists between each needle. 2. LD50 of mouse with BVA-1 was 16 counts and this is equivalent to 640 needles/kg, making Bee Venom Acupuncture safe treatment apparatus. 3. Regardless of the number of needles, there was no sign of blood stasis or inflammation detected on the skin and muscle tissues. Conclusion : Above results indicate that the Bee Venom Acupuncture can complement shortcomings of syringe usage as a part of Oriental medicine treatment, but extensive researches should be done for further verification.

Acute Toxicity of Enrofloxacin-Colistin Combinations after a Single Oral and Intravenous Administration in ICR Mice (ICR계 마우스에서 Enrofloxacin과 Colistin 복합체의 단회 경구 및 정맥투여시 급성독성)

  • Kim, Min-Kyu;Park, Seung-Chun;Yun, Hyo-In;Oh, Tae-Kwang;Choi, Yang-Woong
    • Toxicological Research
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    • v.14 no.3
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    • pp.385-391
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    • 1998
  • The study was carried out to evaluate the acute toxicity of enrofloxacin-colistin combination via a single oral(p.o.)and intravenous(i.v.) administration in ICR mice. All procedures of the test were performed by the established regulation of Korean National Institute of Safety Research (1994. 4.14). The maximal dose of oral and intravenous routes was 5,000mg/kg and 90mg/kg, consisting with each 6 groups including control of male and female, respectively. As the results, $LD_{50}$m}'s of the combinations showed 3,075mg/kg (f)and 2,564mg/kg(m) after oral administrations, together with 48mg/kg(f) and 40mg/kg(m) after intravenous administration. These facts indicated that acute toxicitiy of enrofloxacin-colistin combination were different depending on the administration routes and sexes in ICR mice. In conclusion, the route of enrofloxacin-colistin combination must not choose as i.v. route administration in terms of acute toxicity based on $LD_{50}$.

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Single Oral Dose Toxicity Study of Pinelliae Rhizoma Aqueous Extract in ICR Mice

  • Lim, Young-Kwon;Park, Ji-Ha;Seo, Bu-Il;Roh, Seong-Soo;Ku, Sae-Kwang
    • Toxicological Research
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    • v.25 no.3
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    • pp.147-157
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    • 2009
  • This study was conducted to obtain acute information of the oral dose toxicity of lyophilized water extract of Pinelliae Rhizoma, a dried tuber of Pinellia ternata (PR) in male and female mice. In order to calculated 50% lethal dose (LD$_{50}$) and approximate lethal dose (ALD), test material was once orally administered to male and female ICR mice at dose levels of 2000, 1000, 500, 250, 125 and 0 (vehicle control) ml/kg (body weight). The mortality and changes in body weight, clinical signs, gross observation, organ weight and histopathology of principle organs were monitored 14 days after treatment with PR extract. We could not find any mortalities, clinical signs, changes in the body and organ weights, gross and histopathological findings except for dose-dependent increases in the hepatic fatty change frequencies detected in PR extract 2000 and 1000mg/kg treated in both male and female mice. The results obtained in this study suggest that LD$_{50}$ and approximate LD in mice after single oral dose of PR extracts were considered over 2000 mg/kg in both and female male mice, but more than 1000mg/kg of PR extracts treatment could induce slight hepatotoxicity the fatty changes in mice.

Pesticidal Constituents Derived from Piperaceae Fruits

  • Lee, Hoi-Seon
    • Journal of Applied Biological Chemistry
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    • v.48 no.2
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    • pp.65-74
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    • 2005
  • Fungicidal, insecticidal, and mosquito larvicidal activities of piperidine alkaloids, pipernonaline and piperoctadecalidine, and isobutylamide alkaloids, pellitorine, guineensine, pipercide, and retrofractaminde A, derived from Piperaceae fruits were studied. Pipernonaline and piperoctadecalidine showed potent fungicidal activities against Puccinia recondita with 91 and 80% control values at 500 ppm. Against Phytophthora infestans, pipernonaline showed strong fungicidal activity with 91 and 80% control values at 1,000 and 500 ppm. $LD_{50}$ values of pipernonaline and piperoctadecalidine against Plutella xylostella were 125 and 95.5 ppm, respectively, and that of piperoctadecalidine against Tetranychus urticae was 246 ppm. Against larvae of Aedes aegypti and Culex pipiens pallens, $LD_{50}$ values of pipernonaline were 0.35 and 0.21 ppm, respectively. Highest larvicidal activities of pipercide and retrofractamide A were found against A. aegypti, A. togoi, and C. pipiens pallens. $LD_{50}$ values of pipercide and retrofractamide A were 0.10 and 0.039 ppm against A. aegypti, 0.26 and 0.01 ppm against A. togoi, and 0.004 and 0.028 ppm against C. pipiens pallens, respectively. Based upon these results and earlier findings, bioactive components derived from Piperaceae fruits may be valuable for development of useful lead product of possibly safer fungicidal, insecticidal, and mosquito larvicidal agents.

Studies on X-Ray Sterilization of House Fly (I) (X-선 조사에 의한 집파리의 불임유기에 관하여 (I))

  • Chung K. H.;Ryu J.;Kwon S. H.
    • Korean journal of applied entomology
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    • v.13 no.2 s.19
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    • pp.89-92
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    • 1974
  • This experiment was carried out to investigate the X-ray sterilization of house fly, Musca domestica when 3-5 days old pupae were irradiated. The results obtained were summerized as follows; 1) Sub-lethal dosage (LD50) for tile pupal mortality were 12.2-13.1 kRad. 2) Sterile dosage (SD90) showed 3. 1kRad in male and such low dosage appears adequate as a sterile dosage. 3) The mortality of male flies was significantly higher than in female at the doses of 4 and 5 kRad.

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Toxicity Test of Public Health Insecticides Against the Smoky-Brown Cockroach, Periplaneta fuliginosa, Serville in Korea (韓國産 먹바퀴에 대한 防疫用殺蟲劑의 毒性調査)

  • Koo, Sung Hoi;Shim, Jae Chul
    • Journal of Environmental Health Sciences
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    • v.10 no.1
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    • pp.47-54
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    • 1984
  • The toxicity value of 13 kinds of public health insecticides against the adult female cockroach, Periplaneta fuliginosa, Setville in Korea were evaluated by the topical application method of insecticides. The results obtained were summarized as follows 1. S-biolline showed the most strong susceptibility with LD$_{50}$ of 1.9${\mu}g$ per cockroach (1,100 mg) out of 13 kinds of insecticides and other synthetic pyrethroides insecticides (bio-resmethrin 2.8${\mu}g$/cockroach, permethrin 4.3 ${\mu}g$/cockroach) showed some degree of susceptibility to the smoky brown cockroach. 2. Fenitrothion showed 2.5 $\mu$g per cockroach which was the most strong susceptibility out of 8 kinds of organophosphorus and most of them were good susceptibile but there was clear evidence for developed resistance against malathion with LD$_{50}$ of 80.5 {$\mu}g$ per cockroach (1,100 mg). 3. Lindane showed some degree of susceptibility with LD$_{50}$ of 13.9 {$\mu}g$ per cockroach (1,100 mg) but DDT showed the most strong resistance to the smoky brown cockroach out of 13 kinds of insecticides tested.

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Toxicity of Aceporol 330 in Mice as Novel Solubilizer of Paclitaxel

  • Kim, Yeo-Woon;Chung, Kyu-Nung;Kang, Hoon-Suk;Sheen, Yhun-Yhong
    • Biomolecules & Therapeutics
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    • v.16 no.1
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    • pp.40-45
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    • 2008
  • The objective of this study was to investigate the single dose and 2-week repeated dose toxicity of Aceporol 330 in ICR mice following single intravenous administration and to compare its toxicity with a commercially available solubilizer of paclitaxel, Cremophor EL. In single dose toxicity test, $LD_{50}$ of Aceporol 330 in mice was estimated to be greater than maximum applicable dose, 4 ml/kg. However, $LD_{50}$ of Cremophor EL in male mice was determined to be 4 ml/kg. Maximum tolerated dose (MTD) of males and females in Aceporol 330-treated group and MTD of females in Cremophor EL-treated group were 3 ml/kg. MTD of males in Cremophor EL-treated group was less than 3 ml/kg. Characteristic toxic symptoms, and hematological and blood chemical changes were not observed after single dose and repeated dose of Aceporol 330 or Cremophor EL. No histopathological abnormalities were found in organs of all animal groups. Based on the linear pharmacokinetic property of paclitaxel and the higher $LD_{50}$ in mice, Aceporol 330 has a potential for use as a safer solubilizer for paclitaxel than Cremophor EL.

The Effect of Dilution with 10% Dextrose Solution on the Potency of Botulinum Toxin A

  • Ham, Jong Wook;Kwon, Jeong-Seung;Cho, Eunae Sandra;Choi, Jong Hoon
    • Journal of Oral Medicine and Pain
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    • v.44 no.1
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    • pp.11-15
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    • 2019
  • Purpose: The aim of this study was to compare the potency-stabilizing effects of two different diluents of botulinum toxin A (10% dextrose solution and 0.9% saline). Methods: A mouse lethality bioassay was undertaken. Ninety mice were divided into experimental and control groups which received varying dosages in subgroups of 10. The experimental group was injected with botulinum toxin A diluted with 10% dextrose solution and the control group was injected with botulinum toxin A diluted with 0.9% saline. A 72 hours after intraperitoneal injection, the number of dead mice was counted to confirm median lethal dose ($LD_{50}$) of each group. Results: The value of $LD_{50}$ in the experimental group was approximately 0.131 mL (1.31 U) and the value of $LD_{50}$ in the control group was approximately 0.107 mL (1.07 U). The potency preservation rate of the experimental group was estimated to be 93.5% and that of the control group was estimated to be 76.3%. Conclusions: Dilution with 10% dextrose solution displayed less potency loss than 0.9% saline.