• Title/Summary/Keyword: $LD_{50}$values

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CHEMOSENSITIVITY TEST OF HUMAN OSTEOSARCOMA AND EPIDERMOID CARCINOMAS USING MTT ASSAY (MTT법을 이용한 사람 골육종과 상피암 세포주들에 대한 항암제 감수성 검사)

  • Park, Sung-Oh;Shin, Hyo-Keun;Kim, Oh-Whan
    • Maxillofacial Plastic and Reconstructive Surgery
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    • v.13 no.4
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    • pp.391-404
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    • 1991
  • Three anticncer agents which are different in time or dosage dependence as well as in phase specificity, namely mitomycin and adriamycin from natural products, and widely different cancer cell lines_Four epidermoid carcinomas originated from larynx, cervix, skin and gut were used toghether with one osteosarcoma as the target cell of single and combined administration of anticancer drugs. Semiautomated tetrazolium dye assay(MTT) appears to offer an attractive option for chemosensitivity of head and neck cancers since it is a simple, valid and inexpensive method of assessing chemosensitivity for large samples in a short time. The results obtained form this study were as follows. 1. Good correlations were obtained with the results of the MTT test and those of $^3H$ thymidine uptake assay. 2. $LD_{50}$ values of HIST and St.Ca. which showed relatively high doubling time on adriamycin were $30{\mu}g/ml$ and $15{\mu}g/ml$ while those of HeLa, Hep-2 and KHOS/NP were $2.1{\mu}g/ml$, $4.8{\mu}g/ml$, and $6.8{\mu}g/ml$ respectively. 3. The $LD_{50}$ value of 5-FU on five cancer cells were very high ranging from 15mg/ml to almost indefinite number, which means 5-FU is very resistant to epidermoid carcinomas or osteosarcoma examined in this study. 4. Mitomycin was relatively effective showing 80% cancer killing effect on HeLa, 70% on St. Ca. and 50% on Hep-2 at the high concentrations used. 5. Adriamycin was the most effective showing 90% cancer cell killing effect on KHOS/NP, 98% on HeLa, 80% both on Hep-2 and St. Ca. The least susceptible cancer cells toward adriamycin was HIST having only 55% cell killing effect at the high cincentration. 6. Combined therapy of adriamycin and 5-FU was more effective than single administration in all the cases examined. Most effective synergism was observed on St. Ca. at the low concentration, showing 21 times higher than each single administration.

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Assessment of free-radical-scavenging and antibacterial activities, and brine shrimp toxicity of Scutellaria pinnatifida (Lamiaceae)

  • Sauvage, Severine;Samson, Emilie;Granger, Melanie;Majumdar, Anisha;Nigam, Poonam;Nahar, Lutfun;Celik, Sezgin;Sarker, Satyajit D.
    • Advances in Traditional Medicine
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    • v.10 no.4
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    • pp.304-309
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    • 2010
  • Scutellaria pinnatifida A. Hamilt. (Lamiaceae) is an endemic Turkish herb. This plant is also endemic to Iran, and grows abundantly in other central and western Asian countries. Several species of the Scutellaria are known for their traditional uses in the treatment of hypertension, arteriosclerosis, inflammatory diseases, hepatitis, allergy, cancer and diarrhoea. Free-radical-scavenging property, antibacterial activity and brine shrimp toxicity of the n-hexane, dichloromethane (DCM) and methanol (MeOH) extracts of S. pinnatifida were assessed using the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) assay, the resazurin microtitre plate based assay, and the brine shrimp lethality assay, respectively. The DCM and MeOH extracts exhibited free-radical-scavenging property, with the $RC_{50}$ values of 0.362 and 0.127 mg/ml, respectively. Among the solid-phase extraction fractions of the MeOH extract, the 50% aqueous-MeOH fraction showed the highest level of free-radicalscavenging activity ($RC_{50}$ = 0.039 mg/ml). While the DCM extract showed low level of antibacterial activity against Bacillus subtilis and ampicillin-resistant Escherichia coli, the MeOH extract was active against B. cereus, B. subtilis, E. coli and ampicillin-resistant E. coli. However, the minimum inhibitory concentrations (MIC) of the MeOH extract against these bacterial strains were >10 mg/ml. None of the extracts showed any significant toxicity towards brine shrimps ($LD_{50}$ = > 1.00 mg/ml).

Intravenous Single Dose and Four-week Repented Dose Toxicity Study of YHB216, a Recombinant Human Erythropoietin, in Beagle Dogs (YHB216의 비글개에서 정맥내 단회 및 4주 반복투여독성시험)

  • 노용우;장호송;지형진;정은용;신지순;강민정;안경규;최연식;이종욱
    • Biomolecules & Therapeutics
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    • v.10 no.1
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    • pp.59-69
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    • 2002
  • Recently, recombinant human erythropoietin (rHu-EPO) has been used to treat various types of anemia. YHB216 is a new rHu-EPO developed by Yuhan Research Institute. In this study, we investigated the single dose and 4-week repeated dose toxicity of YHB216 in Beagle dogs. In the single dose toxicity study, YHB216 was administered intravenously at single dose levels of 0 and 25,000 IU/kg to dogs (2 dogs/sex/group). There were no treament-related changes in survivals, clinical signs, body weight gain, hematological values, blood chemical values, and necropsy finding during experimental period. In the repeated dose toxicity study, YHB216 was administered intravenously to dogs for 4 weeks at the dose levels of 0, 100, 500, and 2,500IU/kg (3 dogs/sex/group). There were no toxicologically significant changes in clinical signs, body weights, food and water consumptions, ophthalmoscopy, urinalysis and blood chemistry. There were increased values of red blood cell, hemoglobin, and hematocrit at all treated groups. Spleen revealed increased weight and extramedullary hematopoiesis at 500 IU/kg or more. These changes are all considered to be Pharmacology-related effects and were recovered after 4-week recovery period. From these results, it is concluded that LD50 value was above 25,000 IU/kg in the single dose toxicity study of YHB216 in dogs and the no observed adverse effect level (NOAEL) was 100 IU/kg day in the repeated dose toxicity study of YHB216 in dogs.

Inhibition of Developmental Processes by Flavone in Caenorhabditis elegans and Its Application to the Pinewood Nematode, Bursaphelenchus xylophilus

  • Lee, Yong-Uk;Kawasaki, Ichiro;Lim, Yoongho;Oh, Wan-Suk;Paik, Young-Ki;Shim, Yhong-Hee
    • Molecules and Cells
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    • v.26 no.2
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    • pp.171-174
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    • 2008
  • Flavone (2-phenyl chromone) is a well-known plant flavonoid, but its bioactivity has been little explored. Treatment of Caenorhabditis elegans or C. brissage with flavones induced embryonic and larval lethality that was pronounced in early larval stages. This anti-nematodal effect was also observed in the pinewood nematode, B. xylophilus. $LD_{50}$ values were approximately $100{\mu}M$ for both B. xylophilus and C. elegans. Our results indicate that flavone is an active nematicidal compound that should be further investigated with the aim of developing a potent drug against B. xylophilus.

Isolation of Torilin from Torilis japonica Fruit and Its Analgesic and Anti-inflammatory Activities (사상자 중 Torilin의 분리 및 진통소염작용)

  • Cho, Sung-Ig;Kang, Sam-Sik;Kim, Kyung-Ran;Kim, Tae-Hee;Lee, Eun-Bang
    • Korean Journal of Pharmacognosy
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    • v.30 no.2
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    • pp.137-144
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    • 1999
  • Torilin was isolated from haxane fraction of Torilis Fructus extract. Torilin produced inhibition of the acetic acid-induced and phenylquinone-induced writhing syndrome at the oral doses of 30 and 90 mg/kg in mice. It also increased the pain threshold at the oral doses of 30, 90 and 270 mg/kg in the tail pressure method and the Randall-Selitto method. However, it did not show a hypothermic action at the oral doses of 30 and 90 mg/kg in mice. The compound exhibited strong anticarrageenan activity at the oral doses of 90 and 270 mg/kg in rats, and had inhibitory effect on the vascular permeability at the oral doses of 30 and 90 mg/kg in mice. It also showed potent inhibition of leucocyte emigration in CMC-pouch at the doses of 3 and 9 mg/rat, sc. The acute toxicity of torilin was very weak: the $LD_{50}$ values were more than 5000 mg/kg, po and 2000 mg/kg, ip in mice. From the above mentioned results, it was suggested that torilin had potent analgesic and anti-inflammatory activities.

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Acute oral and subcutaneous toxicity of Aloewhite in Mice

  • Kim, Hyung-Sik;Ahn, Mi-Young;Kwack, Seung-Jun;Kim, Kyu-Bong;Lee, Seung-Ki;Chun, Sun-Ah;Lim, So-Young;Park, Hyun-Sun;Hong, Che-Young
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1996.04a
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    • pp.251-251
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    • 1996
  • -Acute oral and subcutaneous toxicity of Aloewhite(30% aloesine) were carried out in ICR mice. In this study, we daily examined number of deaths, clinical signs, body weights, and pathological examinations for 14 days after single oral and subcutaneous administration of Aloewhite with different dose levels. Aloewhite did not show any remarkable toxic effect in mice. These results suggest that oral and subcutaneous LD$\sub$50/ values in mice were over 6.8g/kg and 10g/kg, respectively.

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Acaricidal Components of Medicinal Plant Oils Against Dermatophagoides farinae and Dermatophagoides pteronyssinus

  • Cho, Jang-Hee;Sung, Bo-Kyung;Lim, Mi-Youn;Kim, Hyeon-Jin;Lee, Sang-Guei;Lee, Hoi-Seon
    • Journal of Microbiology and Biotechnology
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    • v.14 no.3
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    • pp.631-634
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    • 2004
  • The oils of Acorus gramineus, Cinnamomum sieboldii, Eugenia aromatica, and Inula helenium were tested for their acaricidal activity against Dermatophagoides farinae and D. pteronyssinus. Responses varied according to dose and mite species. As compared to the oils, the oil most toxic to D. farinae and D. pteronyssinus was E. aromatica, followed by C. sieboldii, A. gramineus, and I. helenium. On the basis of $LD_{50}$ values of the oils in A. gramineus, C. sieboldii, and E. aromatica, the compound most toxic against D. farinae and D. pteronyssinus was eugenol congeners (isoeugenol>eugenol>acetyleugenol) followed by benzyl benzoate, salicylaldehyde, safro1, DEET, cinnamyl alcohol, and 3-carene. As a naturally occurring acaricide, these oils and eugenol congeners could be useful as new acaricidal agents against Dermatophagoides spp.

Identification of Virulence Factors in Vibrio vulnificus by Comparative Transcriptomic Analyses between Clinical and Environmental Isolates Using cDNA Microarray

  • Kim, In-Hwang;Kim, Byung-Soo;Lee, Kyung-Shin;Kim, Ik-Joong;Son, Jee-Soo;Kim, Kun-Soo
    • Journal of Microbiology and Biotechnology
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    • v.21 no.12
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    • pp.1228-1235
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    • 2011
  • We compared the gene expression among four clinical and five environmental V. vulnificus isolates, using a cDNA microarray containing 131 genes possibly associated with pathogenicity, transport, signal transduction, and gene regulations in the pathogen. cDNAs from total RNAs of these isolates were hybridized into the cDNA microarray using the cDNA of the wild-type strain MO6-24/O as a reference. We focused on selecting differentially expressed (DE) genes between clinical and environmental isolates using a modified t-statistic. We could detect two statistically significant DE genes between virulent isolates and less-virulent isolates with a marginal statistical significance (p-value of 0.008). These were genes putatively encoding pilin and adenlyate cylase. Real time-PCR confirmed that these two selected genes transcribed in significantly higher levels in virulent isolates than in less-virulent isolates. Mutants with lesions in the gene encoding pilin showed significantly higher $LD_{50}$ values than that of wild type.

Acute and Subacute Toxicity Studies of Water Soluble Dimethyl Dimethoxy Biphenylate Derivative in Rats (수용성 DDB유도체의 주사제 개발을 위한 급성독성 및 아급성독성시험연구)

  • 김준규;박창원;이윤숙;김정구;이치호;조대현
    • Toxicological Research
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    • v.13 no.4
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    • pp.423-433
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    • 1997
  • The acute and subacute toxicity of water soluble dimethyl dimethoxy biphenylate derivative (new DDB), hepatitis therapeutics, were investigated in SD rats. In the acute toxicity study, body weights and clinical signs were observed for 7 days after the intravenous injection of new DDB at doses of 140, 182, 236, 307 and 400 mg/kg(r=1.3). Death. Severe convulsion, tremor and decrease motor activity were observed in almost treated groups (except the 140 mg/kg treated group). Changes of body weight in treated groups were not significantly different from control group. Autopsy of survived animals revealed no abnormal gross findings related to new DDB. As a results, the $LD_{50}$ values of new DDB were 244.1 mg/kg for male and 232.5 mg/kg for female. In subacute toxicity study, body weights and clinical signs were observed after intravenous injection of new DDB at doses of 57, 75 and 100 mg/kg/day for 28 days. Death, decrease motor activity and tremor were observed above 75 mg/kg treated groups. Statistically significant changes were observed in hematological and biochemical parameters of new DDB-treated groups; however, these changes were within normal range and had no relationship with dosage. Several abnormal findings were observed in microscopic examination of tissue; however, these findings were not caused by new DDB but environmental factor. The no toxic dose level of new DDB were estimated to be 57 mg/kg/day in this study.

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The Acute Toxicity of Novel Platinum(II) Complexes

  • Roh, Young-Soo;Lee, Kyung-Tae;Jung, Sae-Young;Jung, Jee-Chang;Chang, Sung-Goo;Park, Byung-Gi;Cho, Dae-Hyun;Kim, Jun-Gyou
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1995.04a
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    • pp.120-120
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    • 1995
  • This study was conducted to examine novel Pt(II) complexes, (KHPC-002; [Pt(trans-1-dach) (DPPE)]. 2NO$_3$, KHPC-005;[Pt(cis-1-dach)(DPPP)]. 2NO$_3$ and KHPC-006; [Pt(cis-1-dach) (DPPE)]. 2NO$_3$) for their acute toxicities and toxicological profiles in preclinical studies. In male and female mice given a single intraperitoneal administration of KHPC-002, KHPC-005 and LHPC-006, we determined that LD$\_$50/ values of pt(II) complexes were 295.5mg/kg(M), 350.4mg/kg(F);KHPC-002, 158.7mg/kg(M), 157.7mg/kg(F); KHPC-005, 574.8mg/kg(M), 596.5 mg/kg (F); KHPC-006, respectively. In gross and histopathological examination on dead animals, no abnormal changes were observed in any organs.

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