• 대한수의학회지
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• 제38권3호
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• pp.589-594
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• 1998

The in vitro screening tests against the in vitro cultivated $L_3$ of Ascaris suum (in vitro $L_3$), which were cultivated from the embryonated egg to third-stage larva on 7 days in culture(DIC) and the in vivo rat's lung-derived $L_3$ of Ascaris suum (in vivo $L_3$), which were recovered from the lungs of rat on 7 days after infection, carried out in order to compare the anthelmintic efficacy of in vitro $L_3$ and that of in vivo $L_3$ in RPMI medium 1640 with 5% bovine calf serum. And also a screening test of efficacy against adult worms of Trichuris suis performed. The efficacies of screening tests were as follows : 1. The screening efficacies of abamectin and ivermectin against the in vitro $L_3$ were all 100% at the 10ppm concentration in RPMI medium 1640 on 5 DIC. 2. The screening efficacies of abamectin and ivermectin against the in vivo $L_3$ were all 100% at the 20ppm on 5 DIC or at 40ppm on 3 DIC. 3. The screening efficacies of abamectin and ivermectin against the adult worms of Trichuris suis were all 100% at 20ppm on 4 DIC. And therefore, the in vitro cultivated $L_3$ of Ascaris suum were used in the screening test as well as the in vivo rat's lung-derived $L_3$ of Ascaris suum. And also the adult worms such as Trichuris suis and filaroids which is small size and difficult to cultivate to vitro, were used in the screening test in vitro.

• 대한화학회지
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• 제52권5호
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• pp.495-502
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• 2008

• 농약과학회지
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• 제3권3호
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• pp.37-44
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• 1999

In vivo와 in vitro 생물검정법에서의 활성관계를 조사하고 또한 보다 효율적인 in vitro 검정법을 개발하기 위하여 작용기구가 다른 두 계열 살균제 즉 sulphamide계 (dichlofluanid와 tolylfluanid)와 dicarboximide계 살균제 (iprodione, vinclozolin 및 procymidone)을 시험약제로 하여 본 실험을 수행하였다. Dichlofluanid, tolylfluanid, iprodione, vinclozolin procymidone의 토마토 유묘에서의 병 방제효과는 유사하였다. 그러나 이들 살균제에 대해 in vitro 생물검정법으로 항균활성을 비교한 결과, sulphamide계 살균제는 포자발아 억제실험에서 높은 활성을 나타낸 반면에, dicarboximide계 살균제는 균사생장 억제실험에서 항균활성이 더 우수하였다. 그러므로 in vivo 병 방제효과가 유사하더라도 작용기구가 다르면 in vitro 생물검정법에서의 항균활성은 다르게 나타남을 알 수 있었다. 또한 포자현탁액을 넣은 96-well microtiter plate에 약제를 처리하고 3시간 배양 후 배양액을 제거하고 다시 새 배지를 넣어 배양한 후 생장억제를 조사한 실험 (microtiter plate method I, MPM I)에서는 살균제들의 포자발아 억제실험과 유사한 경향의 활성을 보였다. 96-well microtiter plate에서 포자현탁액을 6시간 동안 배양하여 포자를 발아시킨 후에 약제를 처리한 실험(microtiter plate method II, MPM II)에서의 항균활성은 균사생장 억제효과와 일치하는 경향을 보였다. 따라서 기존의 in vitro 항균활성 실험보다 편리하고 효율적인 MPM I과 II 방법은 각각 포자발아와 균사생장 억제실험을 대신할 수 있으리라 생각되었다.

• 대한화장품학회지
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• 제34권3호
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• pp.183-188
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• 2008

미백제를 선발하기 위해 주로 사용하는 현재의 방법은 in vitro 타이로시네이즈 활성 및 항산화능을 측정하는 것이다. 이 결과에 기초하여 다음 단계인 멜라노사이트에서의 멜라닌 생성량을 측정한다. 세포 내의 멜라닌 생성량 측정 법은 시간, 인력 및 숙련도가 요구된다. 따라서 초기 선발 방법의 신뢰성이 중요하다. 200개 중국시료 중 측정범위 내에서 세포독성이 없는 34개를 대상으로 세포 내 멜라닌량, 타이로시네이즈 활성, 항산화능의 상관관계를 조사하였다. 조사결과 직선의 상판관계를 확인할 수 없었다. 이 결과는 현재 선발방법의 한계 및 새로운 방법이 필요함을 보여주었다.

• Toxicological Research
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• 제16권2호
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• pp.109-116
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• 2000

The purposes of our study were to optimize the conditions of the screening and testing methods for endocrine disruptors, to characterize these assays using several compounds with well-defined endocrine activity, and to compare the sensitivity between these assays currently undergoing validation. Two in vitro test systems, MCF-7 cells proliferation (E-screen assay) and competitive binding to estrogen receptors (ER) were selected to evaluate the estrogenic effects. 17$\beta$-Estradiol (E2) and diethylstilbestrol (DES) were used as a positive control in vitro test. Also, E2 and ethinyl estradiol (EE) were used as a positive control in vivo uterotrophic assay. In in vitro test, E2 and DES showed a strong estrogenic response at concentration of 1.0 nM. In uterotrophic assay, E2 (0.3 $\mu\textrm{g}$/kg) and EE (0.3 $\mu\textrm{g}$/kg) produced a significant increase in uterus and vagina weight in both immature and ovariectomized rats. Although we did not com-pared the specificity between in vivo and in vitro assays, these assay systems may serve as a good tool for endocrine disruptors screening methods. Our data indicate that these assay systems exhibit some difference in their sensitivity to the same estrogenic compounds. Therefore, as a first rapid screening assay for estrogenic activity qf unknown chemicals, at least two assay systems should probably be carried out with a view of high sensitivity and standardization conditions. Also, a careful validation tests are necessary to obtain a reasonable degree of reproducibility.

• Toxicological Research
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• 제35권4호
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• pp.343-351
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• 2019

Many in vitro developmental toxicity assays have been proposed over several decades. Since the late 1980s, we have made intermittent attempts to introduce in vitro assays as screening tests for developmental toxicity of inhouse candidate products. Two cell-based assays which were developed two decades apart were intensively studied. One was an assay of inhibitory effects on mouse ascites tumor cell attachment to a concanavalin A-coated plastic sheet surface (MOT assay), which we studied in the early days of assay development. The other was an assay of inhibitory effects on the differentiation of mouse embryonic stem cell to beating heart cells (EST assay), which we assessed more recently. We evaluated the suitability of the assays for screening in-house candidates. The concordance rates with in vivo developmental toxicity were at the 60% level. The EST assay classified chemicals that inhibited cell proliferation as embryo-toxic. Both assays had a significant false positive rate. The assays were generally considered unsuitable for screening the developmental toxicity of our candidate compounds. Recent test systems adopt advanced technologies. Despite such evolution of materials and methods, the concordance rates of the EST and MOT systems were similar. This may suggest that the fundamental predictivity of in vitro developmental toxicity assays has remained basically unchanged for decades. To improve their predictivity, in vitro developmental toxicity assays should be strictly based on elucidated pathogenetic mechanisms of developmental toxicity.

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
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• pp.266.2-266.2
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• 2000

• 생약학회지
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• 제26권1호
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• pp.51-56
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• 1995

To devise an in vitro screening method for antihepatotoxic activity, $CCl_4-induced$ cytotoxicities in primary cultures rat hepatocytes were examined. When rat hepatocytes were intoxicated with 0.5, 1.0 or 1.5 mM $CCl_4$ for 1.5, 3 or 19hr, in order of LDH>GOT>GPT release form hepatocytes was increased in a dose-dependent manner. Treatment with 1.5 mM $CCl_4$ for 1.5 hr showed maximum increase in activity of LDH, GOT or GPT released in the medium compared with the control. At this experimental condition, well known antihepatotoxic substances, glycyrrhizin and silybin markedly inhibited $CCl_4-induced$ cytotoxicities. These results demonstrated that the screening method using $CCl_4-induced$ injury in primary cultured rat hepatocytes might be suitable in vitro assay for antihepatotoxic activity.

• 한국자원식물학회지
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• 제5권2호
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• pp.95-103
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• 1992

Present anticancer drugs in the clinical side have not showed a conclusive effect of the chemotherapy for cancer patients. In order to find much more efficient antitumor agents fromnatural resources, various screening methods vivo and in vitro have been developed by manyresearchers. The intention of this paper is to provide an outline of some background on the tumorsystem in drug development of natural products, to review some screening programs for theevaluation of antitumor activity and to introduce the practical procedures of some antitumorscreening methods in vivo and in vitro. At the end of this paper, the current literatures related toantitumor natural products from higher plants at our laboratory are described.Key words'anticancer drugs, screening methods.

• Archives of Pharmacal Research
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• 제22권2호
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• pp.137-142
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• 1999

Anti-ulcer activity of newly synthesized acylquinoline derivatives was investigated. For the in vitro screening, the effects of compounds on gastric $H^{+}/K^{+}$ ATPase isolated from hog and rabbit were examined. Among them, AU-090, AU-091, AU-254, AU-413 and AU-466 exhibited good in vitro activity on both enzymes. To correlate the in vitro activity with in vivo action, the effects of the compounds on the basal gastric acid secretion were studied. Some derivatives showed considerable anti-secretory activities, and AU-413 was selected for further studies. AU-413 protected gastric damage induced by either ethanol or NaOH dose dependently when given orally. $ED_{50}$ values of 12 mg/kg, p.o. (ethanol) and 41 mg/kg, p.o. (NaOH) were obtained. In addition, histamine-stimulated gastric secretion was reduced upon AU-413 administration. Taken together, newly synthesized acylquinoline derivatives, especially AU-413, is worthy of further investigation to be developed as an anti-ulcer agent.