• 대한한방내과학회지
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• 제27권4호
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• pp.895-904
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• 2006

Objectives : In the present study, the author intended to investigate whether two oriental medical prescriptions named Socheongryongtang-ga-seoggo (SCTS) and Prescription D (P-D) significantly affect mucin release from cultured hamster tracheal surface epithelial (HTSE) cells. Materials and Methods : Confluent HTSE cells were metabolically radiolabeled with 3H-glucosamine for 24 hrs and chased for 30 min in the presence of SCTS or P-D 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 effects of SCTS and P-D on contractility of isolated tracheal smooth muscle were investigated. Results : SCTS did not affect mucin release from cultured HTSE cells, without cytotoxicity. However, P-D significantly increased mucin release from cultured HTSE cells. with significant cytotoxicity. SCTS inhibited Ach-induced contraction of isolated tracheal smooth muscle. P-D also inhibited Ach-induced contraction of isolated tracheal smooth muscle. Conclusions : The author suggests that the effects of SCTS and P-D with their components should be further investigated and it is valuable to find, from oriental medical prescriptions, novel agents which might regulate mucin secretion from airway goblet cells.

• Biomolecules & Therapeutics
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• 제10권3호
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• pp.156-164
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• 2002

In the present study, we tried to investigate whether polymerized basic amino acid e.g. poly-L-lysine (PLL) which has the degree of polymerization under 50mer significantly affects the physiological and stimulated mucin release from cultured hamster tracheal surface epithelial cells. Confluent primary hamster tracheal surface epithelial (HTSE) cells were metabolically radiolabeled with $^3{H}$-glucosamine for 24 hr and chased for 30 min in the presence of either PLLs or adenosine triphosphate (ATP) and PLL to assess the effects on basic or ATP-stimulated $^3{H}$-mucin release. Possible cytotoxicities of PLLs were assessed by measuring lactate dehydrogenase (LDH) release from HTSE cel1s during treatment. The results were as follows: PLLs significantly inhibited basic mucin release from cultured HTSE cells in a dose-dependent manner from the range of 46mer to 14mer; PLL 46mer significantly inhibited the stimulated mucin release by ATP from cultured HTSE cells; there was no significant release of LDH from cultured HTSE cells during treatment. We conclude that PLLs inhibit both physiological and stimulated mucin release from airway epithelial cells without significant cytotoxicity and PLL lost its activity under the range of 14mer. This finding suggests that polymer of basic amino acid like PLL might function as a regulator for hypersecretion of mucus manifested in various respiratory diseases.

• 약학회지
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• 제48권1호
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• pp.93-98
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• 2004

The purpose of this study was to evaluate the effect of pharbitidis seed extract (PE) on antioxidant enzymes. The cytotoxicities of PE were measured by 3- (4,5-dimethlthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay; The change of superoxide dismutase (SOD), glutathione peroxidase (GPx), and catalase (CAT) activity assay were measured. The SOD activities by PE-treated groups were lower than control group's one. In the co-treated with hydrogen peroxide ($H_2O$$_2$) group, SOD activity was higher than $H_2O$$_2$ treated group's activity In the case of GPx, GPx activities were increased in both PE-treated and co-treated with $H_2O$$_2$ group. In the case of CAT $H_2O$$_2$ treated group's activityies were very increased. The CAT activities by PE-treated groups were lower than control group's one, but the activity of co-treated group with H $_2$O$_2$ was higher than that of control group's one. These results suggest that PE has antioxidant activity.

• Biomolecules & Therapeutics
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• 제9권4호
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• pp.263-269
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• 2001

In this study, we tried to investigate whether poly-L-arginine (PLA) (MW 10,800) significantly affect mucin release from cultured hamster airway goblet cells and the mucosubstances of hypersecretory air-way goblet cells of rats. Confluent primary hamster tracheal surface epithelial (HTSE) cells were metabolically radiolabeled with $^3$H-glucosamine for 24 hr and chased for 30 min in the presence of varying concentrations of PLA to assess the effects on $^3$H-mucin release. Possible cytotoxicities of PLA were assessed by measuring both Lactate Dehydrogenate (LDH) release and by checking the possible changes on the morphology of HTSE cells during treatment. For in vivo experiment, hyperplasia of rat airway goblet cells and increase in intraepithelial mucosubstances were induced by exposing rats to SO$_2$ for 3 weeks and varying concentrations of PLA were administered inhalationally to assess the effects on the mucosubstances of airway goblet cells of rats. The results were as follows : (1) PLA significantly inhibited mucin release from cultured HTSE cells in a dose-dependent manner; (2) there was no significant release of LDH and no significant change on the morphology of cultured HTSE cells during treatment; (3) PLA also affected the intraepithelial mucosubstances of hypersecretory rats and restored them to the levels of control animals. We conclude that PLA inhibit mucin release from airway goblet cells without significant cytotoxicity and possibly normalize the hypersecretion of airway mucosubstances in vivo. This finding suggests that PLA might function as an airway mucoregulative agent.

• 한국식품위생안전성학회지
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• 제11권1호
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• pp.71-75
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• 1996

In order to study the antitumoral effect of Selaginella tamariscina extracts, the cytotoxicities to human histiocytic leukemia cells (U937) and lymphocyte were measured by MTT method. The water extract of Selaginella tamariscina was partitioned into chloroform (CHCl3), ethylacetate (EtAc), n-butanol (BuOH) and water (H2O), successively. CHCl3, EtAc and BuOH fractions of Selaginella tamariscina showed the cytotoxicity to the U937 cells but they had effect on the cytotoxicity of lymphocyte under the same conditions. The tumor-specific cytotoxicity of Selaginella tamariscina fractions migh have been attributed to their genotoxic effect on actively proliferating cells. The expression of p53 tumor suppressor gene was then evaluated by northern blotting. The increased expression of p53 was induced by Selaginella tamariscina fraction V but no expression of p53 was induced by CHCl3, EtAc, and BuOH fractions of Selaginella tamariscina water extract (fraction V) should be required for the cytotoxcity on U937 and the other fractions of Selaginella tamariscina mediated the U937 disruption.

• Archives of Pharmacal Research
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• 제23권2호
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• pp.155-158
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• 2000

Bioassay-guided fractionation of Crataegus pinnatifida (Rosaceae) gave two cytotoxic ursane-type triterpenes which were identified as uvaol (1) and ursolic acid (2) by physicochemical and spectroscopic methods. 3-Oxo-ursolic acid (3) was synthesized from ursolic acid (2) by Jones method. The cytotoxic activities of these compounds were tested against murine L1210 and human cancer cell lines (A549, SK-OV-3, SK-MEL-2, XF498, and HCT15) in vitro. Compounds 1 and 2 showed moderate cytotoxicities against L1210, whereas they showed weak activities against human cancer cell lines. However compound 3 exhibited potent cytotoxic activities both in murine and in human cancer cell lines.

• Restorative Dentistry and Endodontics
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• 제22권2호
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• pp.575-595
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• 1997

Replacement resorption is followed by the delayed replantation of an avulsed tooth. Currently no effective treatment is substantiated for replacement resorption. The purpose of this study was to investigate the effect of stannous fluoride, bisphosphonate (etidronate disodium) and gallium nitrate, which have been shown to reduce dentin resorption, on human dentin. Osteoclasts were collected from tibeas of chick embryo. The cells were well agitated to prevent adhesion and seeded onto the sliced human dentin wafers which had been soaked in either culture media (control), or several different concentrations of stannous fluoride, etidronate disodium (l-hydroxyethylidene -1,1-bisphosphonate disodium), and gallium nitrate. Resorption was measured by counting the number of resorptive pit produced by the cells. Results are as follows. Stannous fluoride and etidronate disodium showed statistically significant reduction of dentin resorption(p<0.05) but the effect of stannous fluoride seemed to be its high cytotoxicity. Etidronate disodium did not show cytotoxicities in all experimented concentrations. Gallium nitrate did not show differences in resorption either between different concentrations or from the control group.

• Archives of Pharmacal Research
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• 제19권6호
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• pp.535-542
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• 1996

Seven isoazamitosene derivatives, mitomycin analogues, were synthesized and tested for cytotoxicities against leukemia and gastric cancer cell lines. Preparation of a pyrrolo[1, 2-a]benzimidazole (3) (azamitosene ring system) was completed by utilizing the Lewis acid-catalized cyclization, with .omicron.-chloronitrotoluene as the starting material. Nitration of 3 produced a mixtue of two isomers (5-nitro isomer (4) and 7-nitro isomer (5)) in product ratio of 36 : 52. 4 was directly converted into quinone (7) by reduction and Fremy oxidaton. Finally, quinone derivatives (8, 9, 10, and 11) were synthesized by 1, 4-addition of 7 with cyclic secondary amines. From above-mentioned 5, 8-nitro compound (15) was prepared in 4 steps. At pH 3, Fremy oxidation of 15 produced quinone (16), whereas iminoquinone derivatives (17a and 17b) at pH 7. Isoazamitosene derivatives (8, 9, 10, and 11), containing cyclic amino groups at the 7-position, showed potent cytotoxicity on P388, SNU-1, and KHH tumor cell lines. Among them, 8 had stronger cytotoxicity against SNU-1 cell line than mitomycin and adriamycin. Considering these results, isoazamitosene derivatives may had unique cytotoxicity profiles. However, isoiminoazamitosene derivatives (17a and 17b) revealed very weak cytotoxicity.

• 약학회지
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• 제47권6호
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• pp.432-437
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• 2003

It has been known that quercetin, a bioflavonoid widely distributed in fruits and vegetables as dietary-derived flavonoid and exert significant multiple biological effects such as antioxidant and anti-inflammatory, anti-tumor effects. In addition, it has been shown to have a chemoprotective role in cancer, though complex effects on signal transduction involved in cell proliferation and angiogenesis. The present study investigated whether quercetin can enhance antioxidant enzyme activity (glutathione peroxidase: GPx, superoxide dismutase: SOD, catalase: CAT) and regulate the reactive oxygen species (ROS) generation in the presence of vitamin E, L-ascorbic acid, reduced glutathione (GSH) on B16F10 murine melanoma cells. After 48h treatment of cells with quercetin in the presence of vitamin E, L-ascorbic acid, GSH, we measured the cytotoxicities by MTT assay. The cells exhibited a dose-dependent inhibition in their proliferation in the presence of vitamin E, L-ascorbic acid, GSH respectively. We also investigated the effects of antioxidant enzyme activity and ROS generation. The antioxidant enzyme activity of quercetin in the presence of vitamin E was stronger than GSH, L-ascorbic acid, the same treatments decreased ROS generation in B16F10 murine melanoma cells. Taken together, these result demonstrate that the antioxidant effect of quercetin can enhanced in the presence of vitamin E and it might plays an important role in anti-oxidative effects.

• 생약학회지
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• 제28권4호
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• pp.174-178
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• 1997

Methanol extracts from 450 plants were screened for muttidrug-resistance reversing activity using drug sensitive KB-3-1 and multidrug-resistant KB-Vl cells. Among them, the extracts of Cynanchum wilfordii, Torilis japonica, Celastrus orbiculatus, Melia toosendan and Teminialia chebula strongly potentiated vinblastine cytotoxicity in KB-Vl cells. But their cytotoxicities to both sensitive KB-3-1 and resistant KB-Vl cells were in the same order of magnitude. These results indicate that the above samples would contain the active principles which do not exert their ativity solely by cytotoxicity.