• Archives of Pharmacal Research
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• v.27 no.8
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• pp.829-833
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• 2004

The bioactivity-guided fractionation of the methylene chloride extract of the sclerotium of Poria cocos led to the isolation of (S)-(＋)-turmerone (1), ergosterol peroxide (2), polyporenic acid C (3), dehydropachymic acid (4), pachymic acid (5), and tumulosic acid (6). Compounds 4-6 exhibited moderate cytotoxicities, with $IC_{50}$ values of 20.5, 29.1, and $10.4{\;}\mu\textrm{m}$, respectively, against a human colon carcinoma cell line. However, 3-6 not only showed inhibitory activities as potent as etoposide used as a positive control on DNA topoisomerase II (36.1, 36.2, 43.9 and 66.7％ inhibition at a concentration of $20{\;}\mu\textrm{m}$, respectively), but also inhibition of DNA topoisomerase I (55.8, 60.7, 43.5, and 83.3％ inhibition at a concentration of $100{\;}\mu\textrm{m}$, respec-tively).

• Bulletin of the Korean Chemical Society
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• v.29 no.10
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• pp.1988-1992
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• 2008

A series of new derivatives on the ring A of luotonin A were prepared by Friedländer condensation of 6,7,8,10- tetrahydropyrrolo[2,1-b]quinazoline-6,10-dione and suitably substituted 2-aminobenzaldehydes and 2- aminoacetophenones. Their inhibitory activities on topoisomerases and cytotoxicities against selected human cancer cell lines were evaluated. Among the compounds tested, 8-fluoroluotonin A showed similar inhibitory activity on topoisomerase I comparable to camptothecin while luotonin A and 9-hydroxyluotonin A showed 1.37 and 0.94 times stronger inhibitory activity, respectively, on topoisomerase II compared to etoposide. Some derivatives of luotonin A showed moderate cytotoxicity. The possible relationship between the inhibitory activity on Topo II and the cytotoxicity of luotonin A and its analogues, thus, cannot be ruled out.

• BMB Reports
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• v.40 no.6
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• pp.959-965
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• 2007

Two isolectins (KML-IIU and the KML-IIL) were individually isolated from the previously reported Korean mistletoe lectin, KML-C, by using an immunoaffinity column. Molecular weights of the KML-IIU and the KML-IIL were 64 kDa and 60 kDa respectively. Both of the lectins were composed of heterogeneous A and B subunits linked with a disulfide bond, and showed the same carbohydrate-binding specificities for Gal and GalNAc. However, they are different not only in biophysical properties (glycosylation and amino acid compositions) but also bioactivities (cell killing and cytokine induction). The KML-IIL showed 17-145 times stronger in cytotoxicities to various human and mouse cancer cell lines than the KML-IIU. The KML-IIL also induced TNF-$\alpha$ secretion from mouse peritoneal macrophages 4.5 times better than the KML-IIU. The results demonstrated isolectins in Korean mistletoe were varied in bioactivities and the KML-IIL may be developed as an anti-cancer agent.

• The Journal of Pediatrics of Korean Medicine
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• v.19 no.1
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• pp.11-23
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• 2005

Objectives : In the present study, the authors intended to investigate whether two oriental medical prescriptions named chwiyeon-tang and chihyosan-gamibang significantly affect much release from cultured hamster tracheal surface epithelial HTSE cells. Methods : Confluent HTSE cells were metabolically radiolabeled with 3H-glucosamine for 24 hrs and chased for 30 min in the presence of chwiyeon-tang or chihyosan-gamibang to assess the effect of each agent on 3H-mucin release. Possible cytotoxicities of each agent were assessed by measuring lactate dehydrogenase LDH release. Also, the effect of chwiyeon-tang and chihyosan-gamibang on contractility of isolated tracheal smooth muscle were investigated. Results : (1) Chwiyeon-tang significantly inhibited mucin release from cultured HTSE cells, with significant cytotoxicity ; (2) Chihyosan-gamibang significantly stimulated mucin release from cultured HTSE cells, with minute cytotoxicity ; (3) Chwiyeon-tang and Chihyosan-gamibang did not affect contractility of isolated tracheal smooth muscle. Conclusions : We suggest that the effects of Chwiyeon-tang and Chihyosan-gamibang with their components should be further investigated and it is of great value to find, from oriental medical prescriptions, noel agents which might regulate mucin secretion from airway goblet cells.

• Archives of Pharmacal Research
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• v.14 no.3
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• pp.207-216
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• 1991

Pseudixus japonicus agglutinin (PJA) was isolated. And its characteristics were compared with those of concanavalin A (Con A). PJA is a glycopritein composed of 49.3% carbohydrate and 50.7% protein which had relatively high percentages of glutamic acid, aspartic acid and phenylalanine residues. The hemagglutinating activity of PJA was approximately one-eighth of that of Con A when tested with mouse crythrocytes. PJA failed to simulate the proliferation or transformation of human and mouse lymphocytes in contratst to Con A. PJA and Con A showed cytotoxicities against SNU-1 (human stomach cancer cells), SNU-CI (human colon cancer cells) and mouse Sarcoma 180 cells when tested by 3-(4, 5-dimethyl thiazol-2-yl)2. 5-diphenyl tetrazolium bromide (MIT) colorimetric assay. The antitumor activity of the lectin in vivo was also tested in Sarcoma 180 bearing mice. There was no significant difference in prologation of lifc span of the mice after the treatment with PJA and Con A for 10 consecutive days.

• YAKHAK HOEJI
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• v.40 no.6
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• pp.697-704
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• 1996

Quinolone derivatives, SJ5b (ethyl 5,12-dihydro-5-dihydro-5-oxobenzoxazolo[3,2-a]quinoline-6-carboxylate) and SQ7b (3-fluoro-2-(4-methylpiperazin-1-yl)-5.12-dihydro-5-oxobenzoxa zolo[3,2-a]quinoloine carboxylic acid) showed in vitro cytotoxicities against various tumor cell lines. SJ5b and SQ7b completely inhibited the DNA relaxation activities of human placental topoisomerase II at the concentration of 15.63 and 1.95 ${\mu}$g/ml, respectively. However, unlike etoposide which stabilize the topoisomerase II-DNA complex, SQ7b did not cause topoisomerase II-mediated DNA cleavage and SJ5b weakly stabilized the topoisomerase II-DNA cleavable complex. Through both experiments. DNA relaxation assay by the increment of topoisomerase II concentration and DNA unwinding assay, it was shown that SJ5b and SQ7b did not interact with topoisomerase II itself but bound to DNA. Therefore, it was concluded that DNA binding of SJ5b and SQ7b caused the inhibition of topoisomerase II related to DNA relaxation but no or very weak stabilization of topoisomerase II-DNA cleavable complex. In addition, SJ5b and SQ7b prevented whole cell nucleic acid syntheses in HL60 cells.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.27 no.1
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• pp.43-52
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• 2001

Living systems constantly suffer from atmospheric reactive oxygen species and also produce inevitably them by the course of metabolism. Therefore, antioxidants play important roles in protecting the systems from various diseased caused by them. In this study, we investigated various tinged autumnal leaves as antioxidant sources. Among the, the red leaf extracts of Acer Palmatum THUNBERG.(Aceraceae: maple tree) and Prunus Donarioum Sieb. Var. spontanea Makino(Rosaceae : cherry trees) showed the highest anti-oxidativities. The major antioxidants in their red leaves were isolated and identified as vitexin from maple leaves and isoscutellarein-4'-O-$\beta$-glucopyranoside from cherry leaves. Finally, we evaluated the efficacy of skin care products containing the extracts by human use study. As a result, the tinged leaves of maple and cherry trees were evaluated as good antioxidant sources on the bases of antioxidativities, cytotoxicities, cell proliferation effects and human use study.

• Korean Journal of Pharmacognosy
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• v.26 no.4
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• pp.344-348
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• 1995

Preliminary screening test of modulators for multidrug resistance with 400 medicinal plants was carried out by using human multidrug resistance cell line, KB-V1. Among active medicinal plants, the unripe fruits of Evodia officinalis showed a potent modulating activity of MDR. From MeOH extract of this plant, we isolated two indole alkaloids, rutaecarpine (1) and evodiamine (2), by repeated silicagel column chromatography. Rutaecarpine increased the cytotoxicities of vinblastine and taxol against multidrug resistance cells, but evodiamine showed no modulating activity in spite of its potent cytotoxic activities.

• Restorative Dentistry and Endodontics
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• v.14 no.1
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• pp.25-40
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• 1989

This study was conducted to evaluate the influence of 5 microfilled composite resin to fibroblast cultivated from human pulp (age 13). Each composite resin was manually mixed and filled in cylinder. Resin filled cylinders were placed in dishes (35mm in diameter) containing 3 ml of ${\alpha}$-MEM. Filters (pore size 0.22 ${\mu}m$) to simulate dentin were also placed between the bottom of cylinder and the dish floor. Then stored in 5% $CO_2$ containing incubator for 1 and 2 weeks at the temperature 36.6 C. The results analysed after 1 and 2 weeks were as follows: 1. Experimental group except group 2, 2 weeks incubation cases showed the cytotoxicity compared to the control group in cell count. 2. After 2 week-incubation of group 1 and group 4, cell count was more decreased than 1 week cases and cytotoxicity seemed to be constantly influenced to the cell multiplication. 3. The cell growth rate of 1 week incubation in group 3 and group 5 was similar to the control group and recognized the cytotoxicities of these groups were mild. 4. The cell multiplication rate of 2 week incubation cases in group 2 was greater than control group.

• The Journal of Pediatrics of Korean Medicine
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• v.20 no.1
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• pp.93-107
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• 2006

Objective : To investigate the effectiveness of two oriental medical prescriptions named Sigoungcheongpyetang(SCPT) and Tonggyutanggamibang(TGT) for mucin release from cultured hamster tracheal surface epithelial(HTSE) cells. Method : Confluent HTSE cells were metabolically radiolabeled with $^{3}H-glucosamine$ for 24hrs and chased for 30 min in the presence of SCPT or TGT to assess the effect of each agent $^{3}H-mucin$ release. Possible cytotoxicities of each agent were assessed by measuring lactate dehy drogenase(LDH) release. Also, the effects of SCPT and TGT on contrectility of isolated tracheal smooth muscle were investigated. Results : (1) SCPT and TGT significantly increased mucin release from cultured HTSE cells, with significantly cytotoxicity ; SCPT did not affect contractility of isolated tracheal smooth muscle and TGT inhibited Ach-induced contraction of isolated tracheal smooth muscle. Conclusion : We suggest that the effects of SCPT and TGT with their components should be further investigated and it is of great value to find, from oriental medical prescriptions, novel agents which might regulate mucin secretion from airway goblet cells.