• Korean Journal of Clinical Laboratory Science
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• v.39 no.3
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• pp.190-195
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• 2007

In the present study, the author investigated to the cytotoxocity in cultured rat hepatocytes of Viscum album lectin. The cytotoxcity effect in Viscum album lectin on the activity of LDH was also investigated. Viscum album lectin significantly increased LDH leakage into medium of hepatocytes treated or untreated with $CCl_4$ (p<0.001). However, Viscum album lectin significantly increased LDH leakage from $CCl_4$-induced hepatocyte (p<0.001). There was a significant increase in LDH levels relative to the control group. Histological observation basically supported the result obtained from LDH assay. The livers of rats challenged with $CCl_4$ produced a marked increased cytoplasmic vacuoles and inflammatory cells in number, while the number of necrotic cells and swollen hepatocytes did not change significnatly. Rats administered DMSO alone did not alter the normal hepatic architecture. Histological observation of liver section in rat treated 72 hrs with either Viscum album lectin $CCl_4$-induced liver damage showed number of cytoplasmic vaculoe and necrotic cell. The number of inflammatory cell increased markedly. This results suggest to the conclusion that Viscum album lectin has a effect of hepatotoxicity activator.

• Archives of Pharmacal Research
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• v.26 no.6
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• pp.446-448
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• 2003

Cystocin belongs to the class of nucleoside antibiotics from Streptomyces sp. GCA0001. Cystocin showed good activity against Gram-positive bacteria, but showed less activity against the Gram-negative bacteria. Cystocin exhibited about two to four folds higher activity than puromycin. Especially, cystocin shows relatively strong activity against Streptococcus strains. Cystocin shows quite potent antitumor activity against all of the cells tested showing $IC_{50}$ values of 0.10 to 0.14 $\mu$ g/mL. This in vitro result indicates that the cytotoxocity of cystocin is two ten folds more active than puromycin s.

• Archives of Pharmacal Research
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• v.20 no.2
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• pp.155-157
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• 1997

An attempt to estabilish the relationship between anti-cell adhesive action of phenylacetylshikonin analogues and their cytotoxicity against A549 cells was done. In the one hour incubation with A549 cells,${\alpha}$-methoxyphenylacetyl-(9), ${\alpha}$-acetoxyphenylacetyl-(13), 3,4-methylenedioxyphenylacetyl-(15) and 4-(N,N-dimethylamino)-phenylacetylshikonin (17) analogues showed a high anti-cell adhesive activity $(IC_100; value, 4-8{\mu}g/ml)$, while halophenylacetyl- and dimethoxy- or trimethoxyphenylacetyl analogues expressed no activity at $40{\mu}g/ml$, indicating that the presence of a bulky group at $ C^I-{\alpha}$ and a polar group at C-4 of phenylacetyl moiety may be important. A similar structure activity relationship exists for the 48 hr cytotoxocity $(ED_{50})$ of phenylacetylshikonin analogues in A 549 cells, but not in either K562 or L1210 cells. Furthermore, the difference between $IC_{100}$ values for anti-cell adhesive activity and$ED_{50}$ values for cytotoxicity of potent compound in A549 cells was not so great (1.5 to 3 times). Based on these observations, it is proposed that the anti-cell adhesive action of phenylacetylshikonins might be responsible for their cytotoxicity in A549 cells.

• Journal of the Korean Society of Food Science and Nutrition
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• v.29 no.5
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• pp.875-880
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• 2000

Reactive oxygen species are produced under diabetic conditions and possibly cause various forms of tissue damage in patients with diabetes mellitus. The aim of this study was to examine the effects of high glucose on the alloxan-induced beta cell injury. The insulinoma (RINm5F) cells were clutured either with high glucose (22.2 mM) or normoglucose (5.6 mM) in RPMI 1460 media for 3 days. The SOD activities were determined by spectrophotometric assay and nitroblue tetrazolium (NBT) stain. The effects of high glucose on the cytotoxicity of alloxan were also investigated in RINm5F cells and the cells viability were determined by 3-(4,5-dimethylthiazolyl)-2,5-diphenyltetrazolium bromide (MTT) methods. Results showed that the CuZn-SOD activity was decreased but Mn-SOD activity was increased significantly in RINm5F cells cultured with high glucose (22.2 mM) media. The cytotoxicity of alloxan was increased by high glucose compared with normoglucose in RINm5F cells. Diethyl-dithiocarbarmate (DDC), as inhibitor of CuZn-SOC, also potentiate the alloxan-induced cytotoxocity in RINm5F cells. These results suggest that, in RINm5F cells, short term culture with high glucose media decreases Cu-Zn-SOD activity and the decreased activity of CuZn-SOD many one of the causative factors of beta-cell injury induced by high glucose.

• Natural Product Sciences
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• v.13 no.1
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• pp.33-39
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• 2007

Eleven polyhydroxyursane triterpenoids (PHUTs) were tested to determine their cytoprotective, immunosuppressive and anti-inflammatory effects. To compare the bioactivities of $19{\alpha}$-hydroxyursane-type triterpenoids {23-hydroxytormentic acid (6), its methyl ester (7), tormentic acid (8), niga-ichigoside $F_1$ (9),euscaphic acid (10) and kaji-ichigoside $F_1$ (11)} of the Rosaceae crude drugs (Rubi Fructus and Rosa rugosae Radix) with PHUTs possessing no $19{\alpha}-hydroxyl$ of Centella asiatica (Umbelliferae), the four PHUTs, asiaticoside (1), madecassoside (2), asiatic acid (3), and madecassic acid (4) were isolated from C. asiatica and 23-hydroxyursolic acid (5) from Cussonia bancoensis. Cytoprotective effects were assessed by measuring cell viabilities against cisplatin-induced cytotoxocity in $LLC-PK_1$, cells (proximal tubule, pig kidney) to determine whether these agents have protective effects against nephrotoxicity caused by cisplatin. The inhibitory effect of 11 PHUTS on nitric oxide (NO) and prostaglandin $E_2\;(PGE_2)$ were evaluated by measuring nitrite accumulation in lipopolysaccharide (LPS)-induced macrophage RAW 264.7 cells, and their anti-inflammatory effects were tested in 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema model. Six MHUTs (compounds 1, 2, 4, 6, 10, and 11) exhibited higher cell viabilities during cisplatin-induced cytotoxicity testing even at a concentration of $200\;{\mu}g/ml$ than cisplatin only-treated group, suggesting that ese compounds have the potentcytoprotective efffcts. Compounds 1 and 3 of the C. asiatica and niga-ichigoside $F_1$ exhibited no inhibitory effect on NO and/or $PGE_2$ production whereas other PHUTs produced mild to significant NO and/or $PGE_2$ production.The four compounds (2, 5, 9, and 10) potently inhibited mouse ear edema induced by TPA whereas two compounds (1 and 3) had no activity in this test. These results suggest that many PHUTs are potentchemopreventives. Structure-activity relationship (SAR) was also discussed in each assay with regard to the significant role of OHs at the position of 2, 3, 6, 19, and 23 and to the glycoside linkage at the 28-carboxyl.