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Neuroprotective Compounds Isolated from Lysimachia christinae

  • Gahee Ryu;Choong Je Ma
    • Natural Product Sciences
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    • v.29 no.1
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    • pp.10-16
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    • 2023
  • We previously reported that dried Lysimachia christinae whole plant extract exerted significant neuroprotective activity. In this study, we tried to isolate neuroprotective compounds of L. christinae. We evaluated the neuroprotective activity of the four fractions (hexane, chloroform, ethyl acetate, and n-butanol fractions) of methanol extract. Among them, ethyl acetate and n-butanol fractions showed most potent neuroprotective activity against glutamate excitotoxicity. Nine compounds were isolated from ethyl acetate and n-butanol fractions of L. christinae extract and identified as cynaroside (1), (3,4,5,6-tetrahydroxytetrahydro-2H-pyran-2-yl)methyl-3-hydroxy-2-octyldopentaconta-23,33-dienoate (2), androst-16-ene-3,6-diol (3), 2-hydroxy-24-propoxytetracos-4-enoic acid (4), 2-hydroxy-24-methoxytetracos-4-enoic acid (5), 12-(stearoyloxy)octadec-9-enoic acid (6), β-sitosterol (7), (E)-4-(3,4-dimethoxyphenyl)but-3-en-1-yl palmitate (8) and (1S,2S,3R,4R)-4-(((2S,3R,4R,5R,6S)-2-(((2R,3R,4S,5R,6R)-2-(3,4-dimethoxyphenethoxy)-3,5-dihydroxy-6-(hydroxymethyl) tetrahydro-2H-pyran-4-yl)oxy)-4,5-dihydroxy-6-methyltetrahydro-2H-pyran-3-yl)oxy)cyclohexane-1,2,3-triol (9) by spectroscopic data such as UV, IR, NMR, Mass spectroscopy. Their neuroprotective activity was evaluated by MTT assay. Cynaroside (1) and androst-16-ene-3,6-diol (3) had significant neuroprotective activity against glutamate-injured HT22 cells. The neuroprotective efficacy of cynaroside (1) and androst-16-ene-3,6-diol (3) was related to their anti-oxidative activity.

Nutrient Utilization, Body Composition and Lactation Performance of First Lactation Bali Cows (Bos sondaicus) on Grass-Legume Based Diets

  • Sukarini, I.A.M.;Sastradipradja, D.;Sutardi, T.;Mahardika, IG.;Budiarta, IG.A.
    • Asian-Australasian Journal of Animal Sciences
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    • v.13 no.12
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    • pp.1681-1690
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    • 2000
  • A study on energy and protein utilization, and milk production of Bali cows on grass-legume diets was carried out using 12 first lactation cows (initial BW $263.79{\pm}21.66kg$) during a period of 16 weeks starting immediately post calving. The animals were randomly allotted into 4 dietary treatment groups R1, R2, R3 and R4, receiving from the last 2 months of pregnancy onwards, graded improved rations based on a mixture of locally available grass and legume feed ad libitum. R1 contained on a DM basis 70% elephant grass (PP, Penisetum purpureum) plus 30% Gliricidia sepia leaves (GS), R2 was 30% PP plus 55% GS supplemented with 15% Hibiscus tilliactus leaves (HT, defaunating effect), R3 and R4 were 22.5% PP+41.25% GS+11.25% HT+25% concentrate, where R3 was not and R4 supplemented with zinc di-acetate. TDN, CP and zinc contents of the diets were 58.2%, 12.05% and 18.3 mg/kg respectively for R1, 65.05%, 16.9% and 25.6 mg/kg respectively for R2, 66.03%, 16.71% and 29.02 mg/kg respectively for R3 and 66.03%, 16.71% and 60.47 mg/kg respectively for R4. Milk production and body weight were monitored throughout the experimental period. In vivo body composition by the urea space technique validated by the body density method and supported by carcass data was estimated at the start and termination of the experiment. Nutrient balance and rumen performance characteristics were measured during a balance trial of 7 days during the 3rd and 4th week of the lactation period. Results indicated that quality of ration caused improvement of ruminal total VFA concentration, increments being 52 to 65% for R2, R3 and R4 above R1, with increments of acetate being less (31 to 48%) and propionate being proportionally more in comparison to total VFA increments. Similarly, ammonia concentrations increased to 5.24 to 7.07 mM, equivalent to 7.34 to 9.90 mg $NH_3-N/100ml$ rumen fluid. Results also indicated that feed quality did not affect DE and ME intakes, and heat production (HP), but increased GE, UE, energy in milk and total retained energy (RE total) in body tissues and milk. Intake-, digestible- and catabolized-protein, and retained-protein in body tissues and milk (Rprot) were all elevated increasing the quality of ration. Similar results were obtained for milk yield and components with mean values reaching 2.085 kg/d (R4) versus 0.92 kg/d (R1) for milk yield, and 170.22 g/d (R4) vs 71.69 g/d (R1), 105.74 g/d (R4) vs 45.35 g/d (R1), 101.34 g/d (R4) vs 46.36 g/d (R1) for milk-fat, -protein, and -lactose, respectively. Relatively high yields of milk production was maintained longer for R4 as compared to the other treatment groups. There were no significant effects on body mass and components due to lactation. From the relationship $RE_{total}$ (MJ/d)=12.79-0.373 ME (MJ/d); (r=0.73), it was found that $ME_{m}=0.53MJ/kgW^{0.75}.d$. Requirement of energy to support the production of milk, ranging from 0.5 to 3.0 kg/d, follows the equation: Milk Prod. ($Q_{mp}$, kg/d)=[-2.48+4.31 ME($MJ/kg^{0.75}.d$)]; (r=0.6) or $Q_{mp}$=-3.4+[0.08($ME-RE_{body\;tissue}$)]MJ/d]; (r=0.94). The requirement for protein intake for maintenance ($IP_m$) equals $6.19 g/kg^{0.75}.d$ derived from the relationship RP=-47.4+0.12 IP; (r=0.74, n=9). Equation for protein requirement for lactation is $Q_{nl}$=[($Q_{mp}$)(% protein in milk)($I_{mp}$)]/100, where $Q_{nl}$ is g protein required for lactation, $Q_{mp}$ is daily milk yield, Bali cow's milk-protein content av. 5.04%, and $I_{mp}$ is metabolic increment for milk production ($ME_{lakt}/ME_{m}=1.46$).

Preparation of $^{125}I-Iodotyraminehemisuccinyltaxol\;(^{125}ITHT)$ for Competitive Taxol Radioimmunoassay (Taxol 방사면역측정을 위한 $^{125}I-Iodotyraminehemisuccinyltaxol\;(^{125}ITHT)$의 제조)

  • Lee, Tae-Sup;Awh, Ok-Doo;Choi, Tae-Hyun;Kim, Hyun-Suk;Hong, Jun-Pyo;Lee, Eun-Sook;Choi, Chang-Woon;Lim, Sang-Moo
    • The Korean Journal of Nuclear Medicine
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    • v.36 no.2
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    • pp.121-132
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    • 2002
  • Purpose : Taxol(Paclitaxel), an antineoplastic agent, has been used in the treatment of ovarian and breast cancers. The determination of optimal Taxol concentrations in human serum was required for enhancing therapeutic effect and maintaining the appropriate Taxol level in blood. This study was aimed to synthesizeradiolabeled Taxol derivatives as radiotracer in competitive radioimmunoassay for monitoring Taxol concentrations in blood and to determine the usefulness of its derivatives. Materials and Methods : Hemisucdcinyltaxol(HT) was synthesized by esterification of Taxol with succinic anhydride. Tyraminehemisuccinyltaxol(THT) was synthesized by coupling of HT with tyramine using isobutylchlormate as coupling agent and purified by HPLC. By using chloramine-T($5.25mg/ml,\;10{\mu}{\ell}$) as oxidant agent, THT($4mg/ml,\;30{\mu}{\ell}$) was labeled wity $^{125}I\;(37MBq,\;1mCi)$. To estimate the stability of purified THT, $^{125}I-iodotyraminehemisuccinyltaxol(^125}ITHT)$ was dissolved in 80% acetonitrile aqueous solution, and the solution was incubated at $4^{\circ}C\;and\;37^{\circ}C$ for 7 days. At various time intervals, the stability of THT and $^{125}ITHT$ was monitored. The titer of Taxol monoclonal antibody, 3G5A7, was determined by competitive radioimmunoassay using $^{125}ITHT$ as a labeled antigen. A standard dose-response curve was demonstated by Taxol competitive radioimmunoassay. Resulls : HT and THT were synthesized with 79.9% and 19.5% yield, respectively. The labeling yield of $^{125}ITHT$ was 93%. After 7 days, the chemical purity of THT was 96.5% at $4^{\circ}C$, and 97.5% at $37^{\circ}C$. After 3 days, $^{125}ITHT$ was stable with 94.7% at $4^{\circ}C$ and 93.4% at $37^{\circ}C$. After 7 days, fadiochemical purity was diminished to 88.1% at $37^{\circ}C$. The titer of Taxol monoclonal antibody, 3G5A7, was determined to 1:256. A standard dose-response curve demonstated good collinearity ($R^2=0.971$) as Taxol concentration-dependent manner. Conclusion : Competitive radioimmunoassay using $^{125}I-iodotyraminehemisuccinytaxol$ as radiotracer could be used to monitor for concentration of Taxol in the human serum.

Antihypertensive activity of Zingiber officinale and Korean ginseng in experimentally induced hypertension in rats

  • Mohan, M;Balaraman, R;Kasture, SB
    • Advances in Traditional Medicine
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    • v.7 no.3
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    • pp.261-273
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    • 2007
  • We investigated the antihypertensive effect of Pet ether extract (PE) of ginger rhizome; its toluene fraction (TF) and Korean ginseng extract (KGE) in deoxycorticosterone acetate (DOCA) - salt induced and fructose induced hypertensive rats. In DOCA model, DOCA (25 mg/kg, once a week; s.c) was administered in uninephrectomised animals for 4 w. PE (50 mg/kg/day; p.o), TF (10 mg/kg/day; p.o) and KGE (30 mg/kg/day; p.o) were evaluated for their antihypertensive effect. In the fructose model, drinking water was replaced with fructose (10%) for five weeks to induce hypertension. PE (50 mg/kg/day; p.o) and KGE (30 mg/kg/day; p.o) were assessed for its antihypertensive effect in fructose model. After completion of the treatment schedule, vascular reactivity to various agonists like 5-HT, noradrenaline, adrenaline, phenylbiguanide and acetylcholine were recorded in rats of both the models. A cumulative dose response curve (CDRC) of 5-HT was carried out in isolated rat fundus strip of the fructose induced hypertensive rats. Chronic administration of PE (50 mg/kg/day; p.o), TF (10 mg/kg/day; p.o), and KGE (30 mg/kg/day; p.o) significantly reduced the blood pressure in DOCA salt whereas PE (50 mg/kg/day; p.o) and KGE (30 mg/kg/day; p.o) reduced the blood pressure in fructose induced hypertensive rats. Treatment with PE (50 mg/kg/day; p.o) and KGE (30 mg/kg/day; p.o) in fructose model for five weeks shifted the CDRC towards the right on rat fundus. The mechanism of action may partly involve the serotonergic antagonistic property.

Synthesis of 1,6-Disubstituted 4,5,6,7-Tetrahydropyrazolo[3,4-c]pyridin-7-one Derivatives and Evaluation of Their Anticancer Activity

  • Devegowda, Vani Nelamane;Seo, Seon-Hee;Pae, Ae Nim;Nam, Ghil-Soo;Choi, Kyung-Il
    • Bulletin of the Korean Chemical Society
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    • v.33 no.2
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    • pp.647-650
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    • 2012
  • Promising anticancer compounds of the type 1,6-disubstituted 4,5,6,7-tetrahydropyrazolo[3,4-c]pyridin-7-ones were identified. The target compounds were readily synthesized in a large scale via a sequence of reactions starting from the commercially available primary amines. Their in vitro anti-proliferative activity has been evaluated on prostate (DU-145), colon (HT-29 and HCT-116) and melanoma (A375P) human cancer cell lines. The relationships between the structure and the anticancer activity, covering all tested cancer cell lines, revealed that the compound 5c with 2,4-dimethylphenyl substituent at $R^2$ was the most potent with the $IC_{50}$ values in the range as low as 0.16 to $0.40{\mu}M$.

Experimental Studies of the Blood Gas Transport during Normothermic Hemodilution Perfusion (상온하 혈액희석 체외순환에 있어서 혈액 GAS 동태에 관한 실험적 연구)

  • 박희철
    • Journal of Chest Surgery
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    • v.13 no.2
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    • pp.85-91
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    • 1980
  • Extracorporeal circulation by hemodilution technique has been currently used with its clinical safety and good peripheral tissue perfusion in open heart surgery. There is no doubt that $O_{2}$ carrying capacity of the blood is disturbed by decreased hemoglobin level resulting from hemodilution of the circulating blood. From the view point of the blood gas exchange, these experimental studies were undertaken to determined the sate limit of hemodilution in the condition of cardiopulmonary bypass with a constant perfusion flow rate. Twelve adult mongrel dogs weighing 10 to 13 Kg. were anesthetized with pentobarbital and then respiration was controlled with Harvard volume respirator using room air. The cardiopulmonary by pass was performed by use of Sarns heart lung machine (console 5000, 5 head and 2 roller pumps) and Travenol pediatric bubble oxygenator. The perfusion rate during bypass was maintained at a constant rate of 80 ml/min/Kg of body weight. The ratio of oxygen gas flow to blood flow was kept in 3 to 1 constantly. International hemodilution was attained by serial blood withdrawals and immediate infusion of equal volumes of diluants composed of Ringer's lactate, 5% dextrose in water and 25% mannitol solution, proportionally 60%, 30%, and 10%. Arterial and venous blood samples were obtained between 15 and 20 minutes following each hemodilution. Hematocrits and hemoglobin values, $PO_{2}$, $PCO_{2}$ and pH were measured. Oxygen and carbon dioxide contents oxygen consumption and carbon dioxide elimination were calculated groups according to different hematocrit values and the correlations were evaluated. Result were as follows. 1. the arterial $O_{2}$ tension and $O_{2}$ saturation were maintained at the physiological level irrespective of the hematocrit value. 2. The venous $O_{2}$ tension and $O_{2}$ saturation showed a tendency to decline with the decrease in hematocrit value and positive correlation between them (r = +0.49, r = +0.76), The mean values of venous $O_{2}$ tension and $O_{2}$ saturation, however, were not decreased when the hematocrit levels were lower than 20%. 3. The arterial $O_{2}$ content declined lineally in proportion to the fall of hematocrit level with a positive correlation between them (r = +0.95). 4. The venous $O_{2}$ contents were decreased gradually as the hematocrit value decreased with positive correlation between them ( r =+0.89). The trend of diminution of venous $O_{2}$ content, however, was became low according to progressive decrease of hematocrit level. 5. Systemic oxygen consumption was in higher range than $O_{2}$ requirement of basal metabolism when the hematocrit value was above 20%, but abruptly decreased when the hematocrit value became to below 20%. 6. The arterial $CO_{2}$ tension and $CO_{2}$ content showed trend of increasing with progressive decrease of hematocrit value but exhibited a rather broad range and there was no relationship between those value and the hematocrit value. 7. The venous $CO_{2}$ tension and $CO_{2}$ content have also no correlation with change of Ht. value but related directly to those value of arterial blood with positive correlation between them (r = +0.78, r = +0.95_. 8. A-V difference of $CO_{2}$ content and $CO_{2}$ elimination wasnot significantly influenced by Ht. value. From the results, we obtained that feasible limit in inteneional hemodilution is above the hematocrit value of 20% under the given experimental condition.

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Anxiolytic effect of chronic ginseng treatment using elevated T-maze in mice

  • Mohan, M;Kasture, SB;Balaraman, R
    • Advances in Traditional Medicine
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    • v.7 no.1
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    • pp.41-45
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    • 2007
  • The roots of the plant Korean ginseng have been extensively used in the traditional Chinese herbal medicine. The effects of chronic administration of Korean ginseng extract (KGE) were investigated on two different anxiety models: the elevated T-maze (for inhibitory avoidance and escape measurements) and the open field test (OFT). Diazepam (1 mg/kg), KGE (10, 30 and 100 mg/kg) were administered orally for 15 days. On the 14th day, mice were previously exposed for 30 min to one of the open arms of the T-maze, 24 h before the test. On 15th day, mice had two exposures to the enclosed and open arm of the elevated T-maze followed by exposure to the open field apparatus. The number of line crossings in the apparatus was used to assess locomotor changes. Cumulative Concentration Response Curve of 5-HT was plotted using rat fundus which were pre-treated in a similar way. Treatment with Diazepam (1 mg/kg) and KGE (10, 30 and 100 mg/kg) significantly (P < 0.05) impaired inhibitory avoidance performance but did not impair escape latency. In OFT, diazepam facilitated locomotion as compared to vehicle and other treatment groups. KGE at any of the selected doses did not impair locomotion. Concentration response curve of 5-HT was shifted towards the right with suppression of maxima in rats treated with KGE. The results suggest that KGE exerts anxiolytic like behaviour in a specific subset of defensive behaviour, particularly those related to generalized anxiety disorder.

ABTS Radical Scavenging and Anti-Tumor Effects of Tricholoma matsutake Sing. (Pine Mushroom) (송이(Tricholoma matsutake Sing.)의 ABTS Radical 소거능과 암세포 생장 억제효능의 검색)

  • Kim, Young-Eon;Yang, Ji-Won;Lee, Chang-Ho;Kwon, Eun-Kyung
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.5
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    • pp.555-560
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    • 2009
  • Pine mushroom (Tricholoma matsutake Sing.) is an expensive and highly prized delicacy in Korean and Japanese cuisines with its unique flavor and functional properties. The pine mushroom juice (PMJ) was investigated for its antioxidant and anti-tumor activities with ABTS radical scavenging method and MTT assay. The phenolic contents in pine mushroom juice ranged from 1.19 to 54.99 GAEs mg/100 mL at the concentrations of $1{\sim}50\;mg/mL$. The ABTS radical scavenging activities of pine mushroom juice were 7.0%, 81.7% and 91.8% at the concentrations of 1, 10 and 50 mg/mL, respectively. The $IC_{50}$ values of pine mushroom juice were 605.9, 788.4, 583.6 and $232.5{\mu}g/mL$ on the cytotoxicities against AGS, HeLa, HepG2 and HT-29, respectively, and PMJ showed the strongest growth inhibitory activity against HT-29 cell. These results suggested therapeutic potential for pine mushroom juice as an anti-oxidant and anti-tumor agent.

Hematological Characterietic of Bastard halibut according to Cultured experiment of Mari-floating netcage- I On the Hematological conditions (넙치의 해상(海上)가두리 사육시험(飼育試驗)에 따른 혈액학적(血液學的) 연구(硏究)-I 혈액성상(血液性狀)에 대(對)하여)

  • Sim, Doo-Saing;Jeon, Im-Gi;Jung, Sung-Hee
    • Journal of fish pathology
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    • v.3 no.1
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    • pp.27-38
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    • 1990
  • Hematological conditions were measured to the cultured bastard halibut classified by control group and establishments of mari-floating netcages from April 7, 1990 to May 24, 1990. The RBC, Hb, HT, MCHC, MCH and MCV values were $289{\pm}61{\times}10/^4/mm^3$, $4.8{\pm}0.9g/dl$, $22{\pm}6%$, $22.7{\pm}4.0%$, $16.9{\pm}3.3pg$ and $77{\pm}19{\mu}m^3$ respectively in the hematological conditions of control group. Relation between Hb and Ht was represented highly positive(r=0.805, p<0.01>, and relation between MCV and MCH was represented positive (r=0.696, p<.0.05) in the control group. In the variation of hematological conditions classified by experimental group, RBC of PVC group was returned $293{\pm}57{\times}10/mm^3$ on the 21th after locomotion to mari-floating netcages. RBC of netron group was also returned as control level on the 21th after locomotion, showed stabilization. Hb of PVC and netron group was low in the range of variation, was represented $3.9{\pm}9.6g/dl$ on the 45th after locomotion. The group that was also satabilizied variation of Ht were PVC, netron group. According to the results of hematological conditions classified by establishment of mari-floating netcages, the experiment group that were stabilized variation were in order of PVC, netron and pole-PVC group. But the other groups were extended the range of variation.

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Arm Span-Height Relationship for Prediction of Spirometric Values in Korean Adult Women (우리나라 성인여성에서 정상 폐활량 예측을 위한 양팔벌린 손끝길이와 신장과의 관계)

  • Koh, Won-Jung;Ju, Young-Su;Kim, Tae-Yub;Park, Jae-Sung;Yu, Seung-Do;Choi, Kwaung-Soo;Paek, Do-Myung;Han, Sung-Koo;Shim, Young-Soo
    • Tuberculosis and Respiratory Diseases
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    • v.46 no.6
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    • pp.786-794
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    • 1999
  • Back ground : Arm span measurements provide a practical substitute for standing height to predict normal spirometric values in subjects unable to stand or those with a skeletal deformity such as kyphoscoliosis. The relationship between arm span and height has previously been reported as either a fixed ratio unaffected by age or as a regression equation in which the ratio varies as a function of age. The fixed ratio or regression equation is known to be specific for sex and race. Methods : We studied the relationship between standing height, arm span, and age in 381 Korean adult female subjects (ages 20 to 69 yrs) sampled in a general population. Results : The mean ratio for arm span to height is 1.004. Multiple linear analysis found arm span and age to be predictive of standing height (p=0.0001, $r^2$=0.76). We performed the analysis of the difference between the predicted height using either fixed ratio or regression equation and actual height. At the extremes of arm span and age, the ratio method either underestimated(at smaller arm span or younger age) or overestimated(at larger arm span or older age) as compared with actual height (p=0.0001). Conclusion : This results indicate that the estimated height using the fixed ratio method provides a less acceptable method of estimating height for the prediction of lung volumes in the Korean adult women when compared with the regression equations, especially at the extremes of stature or age.

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