• 약학회지
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• 제40권5호
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• pp.599-607
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• 1996

Acetylarsonate was prepared for testing antitumor and immunological effects. It showed cytotoxicity directly on Sarcoma 180. L1210 and MOLT-4 by MTT assay. It did not seemed to trigger the mitosis of human lymphocytes in culture, but that showed the cytotoxicity with higher dose. The rosette formation and spleen weight of mouse which acetylarsonate was administered to for 2 weeks were increased. Furthermore, peripheral helper T- and cytotoxic/suppressor T-lymphocytes were increased in acetylarsonate-injected-mice significantly when it was estimated with simultaneous 2 color analysis using anti Lyt2-FITC and L3T4-PE monoclonal antibody by Flow cytometer.

• Toxicological Research
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• 제4권2호
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• pp.95-105
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• 1988

The effects of polyacetylenes on living membrances, rat erythrocyte and murine leukemic L1210 cell as well as artificial lipid bilayer were determined to investigate the cytotoxic mechanism of polyacetylenes against cancer cell lines. As results, panaxydol and panaxynol caused erythrocyte hemolysis dose-dependently while panaxytriol had no lysis. For liposomes composed of phosphatidyl choline (PC) and phosphatidic acid(PA), all three polyacetylenes supressed the osmotic behavior at the same degree.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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• pp.73-73
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• 1993

As part of a research program to develope 3rd generation anti tumor platinum complexes, a series of platinum complexes which have 4, 5-bis-(aminomethyl)- 1, 3-dioxolane derivatives as bidenate amine ligands, represented by the general structual formula was prepared. The R$_1$ and/or R$_2$ substituents in this series of platinum complexes can be hydrogen. alkyl, of jointly formed cyclohexane. Two Xs can be a bidenate leaving ligand such as 1, 1-cyclobutanedicarboxylate, malonate, dimethylmalonate, ethylmalonate, glycolate, L-lactate, or N-methyliminodiacetate. From based on the pharmacological and toxicological studies, we have chosen SKI 2053R, cis-malonato[(4R, 5R)-4, 5-bis(aminomethyl)-2-isopropyl-1, 3-dioxolane] platinum(II) complex (NSC D644591) as a candidate for clinical evaluation. The antitumor activity of a new anti tumor platinum complex, cis-malonato [(4R, 5R)-4, 5-bis(aminomethyl)-2-isopropyl-1, 3-dioxolane] platinum(II) (SKI 2053R, NSC D644591), was compared with those of cisplatin and carboplatin using murine tumors. We evaluated three platinum complexes against L1210/CPR, a subline of L1210 leukemia resistant to cisplatin for their abilities to overcome tumor resistance to cisplatin. The in vitro cytotoxicity of SKI 2053R to L1210 cell line was 2.5-fold less potent thann that of cisplatin, and was 10-fold more cytotoxic than that of carboplatin. SKI 2053R retained similar cytotoxic effect and anti tumor activity to L1210/CPR cell line, like the cytotoxicity of SKI 2053R to L1210 cell line, while either cisplatin or carboplatin had not property to overcome the acquired cisplatin-resistance. SKI 2053R exhibited greater or comparable antitumor activity than cisplatin or carboplatin in murine tumor models.

• 한방안이비인후피부과학회지
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• 제18권1호
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• pp.82-93
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• 2005

Objective: This Study was to investigate effects of Neasookseul-Tang on the anti-cancer, proliferation of immunocytes and nitric oxide(NO) production of peritoneal macrophages. Methods: We used Neasookseul-Tang extract(NOT) with freeze-dried, 8wks-old male mice(balb/c, ICR) and cancer cell lines(L1210, sarcoma-180) for this Study. The proliferation of cells was tested using a colorimetric tetrazoliun assay(MTT assay). Results: 1. NOT was significantly showed cytotoxicity on the L1210 and Sarcoma-180 cell lines. 2. NOT was significantly increased proliferation of thymocytes and splenocytes in vitro. 3. NOT was significantly decreased proliferation of L1210 cells in L1210 cells transplanted mice. 4. NOT was significantly increased proliferation of thymocytes and splenocytes in L1210 cells transplanted mice. 5. NOT was significantly increased NO production from peritoneal macrophages in L1210 cells transplanted mice. 6. NOT was significantly inhibited body weight and tumor weight in Sarcoma-180 cells transplanted mice. 7. NOT was significantly increased in the mean survival days in Sarcoma-180 cells transplanted mice. Conclusions: The present author thought that NOT had action of anti-cancer by accelerating immuno-function.

• Biomolecules & Therapeutics
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• 제5권2호
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• pp.215-221
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• 1997

In an effort to screen new selective antitumor agents from the broth of soil microorganism, cytotoxicity oriented screening was performed against tumor cells and 3 compounds (Compound 1, 2 and 3) were isolated from Sreptomyces parvullus ISP 5048 and their chemical structures were determined. Among these compounds, Compound 2 showed the highest cytotoxicity against P388Dl and L1210. While the $IC_{50}$/ values of compound 2 against P388Dl and L1210 were 0.073$\mu$g/ml and 0.07$\mu$g/ml, respectively, and the $IC_{50}$/ value of Compound 3 was 0.17$\mu$g/ml against human lung cancer cells, A549, the cytotoxicity of Compound 2 and 3 against normal cell line, Vero E6 cell was about 4- and 8-fold lower than that of adriamycin. Based on the chemical analysis data, Compound 3 was octacosamicine A, a known antibiotic, which was reported by Dobasih et al. (1988). Taken together the results demonstrated that Compound 2 and Compound 3 has the possibility to be developed as antitumor agent because of its potent cytotoxicity as well as high selectivity against various cancer cell lines.

• 한방안이비인후피부과학회지
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• 제18권1호
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• pp.104-115
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• 2005

Sunjeonhwadok-Tang was a drug that treated carbuncle and cellulitis. So, the purpose of this study was to investigate effects of Sunjeonhwadok-Tang on the proliferation of cancer calls and immunocytes focusing around combined effects of anticarcinogen. We used Sunjeonhwadok-Tang extract(SHT) with freeze-dried, 8wks-old male balb/c mice and cancer cell lines(L1210, Sarcoma-180) for this Study. The proliferation of cells was tested using a colorimetric tetrazoliun assay(MTT assay). The results : 1. SHT was significantly showed cytotoxicity on the L1210 cell lines. 2. SHT was significantly increased proliferation of thymocytes and splenocytes in vitro. 3. In combined effects of SHT and vincristine(0.005 mg/kg), SHT was significantly inhibited proliferation of L1210 cell lines, but was not inhibited proliferation of Sarcoma-180 cell lines compared with positive control group. 4. In combined effects of SHT and vincristine(0.005 mg/kg), SHT was significantly increased proliferation of thymocytes and splenocytes compared with positive control group. 5. In combined effects of SHT and vincristine, SHT was significantly increased proliferation of thymocytes and splenocytes in normal mice. 6. In combined effects of SHT and vincristine, SHT was significantly inhibited proliferation of L1210 cells in L1210 cells transplanted mice 7. In combined effects of SHT and vincristine, SHT was significantly increased proliferation of L1210 cell in L1210 cells transplanted mice. The present author thought that SHT had action of anti-cancer and immuno-activity, and in combined effects of vincristine, SHT had recoverable effects on damage by anticarcinogen.

• 약학회지
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• 제32권2호
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• pp.125-128
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• 1988

Geranylation of some synthetic and natural flavones have yielded cytotoxic products against L1210 coll; 5,2´-dihydroxy-6,7,8-trimethoxy-6´-geranyloxyflavone 4$(8.5{\mu}g/ml)$, 5,6-dihydroxy-7-gerenyloxyflavone 9$(2.3{\mu}g/ml)$. 2 has showed the same range of cytotoxicity as the starting material, 5,2´-dihydroxy-6,7,8-trimethoxy-6´-benzyloxyflavone$(17.0{\mu}g/ml)$. The cytotoxicity of 4 was lower than its starting substance, 5,2´,6´-trihydroxy-6,7,8-trimethoxyflavone $(4.5{\mu}g/ml)$. On geranylating 5,6,7-trihydroxyflavone(baicalein, $15.0{\mu}g/ml$) the cytotoxic activity has been strongly potentiated($2.3{\mu}g/ml$ of 9). The presence of at least a free hydroxy group in B-ring of Skullkapflavone II-type flavones. was essential for a high activity. A larger RD-group than methoxy in the B-ring has weakened the activity. The cytotoxicities of baicalein series could not be correlated to their structures.

• 한국식품영양과학회지
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• 제33권6호
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• pp.1074-1077
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• 2004

저령의 에틸아세테이트 추출물에서 4개의 분획을 제조한 후 백혈병 세포인 K-562, L-1210, HL-60와 U-937 세포의 세포생존 억제효능을 관찰하였다. Fr. 2는 L-1210, HL-60 세포 억제효능이 미비하였고, Fr. 3은 4종의 백혈병 세포주에 대하여 세포생존 억제효능이 있었다. 이 효능은 L-1210 세포에 대하여 가장 강하게 나타났다. 세포사멸 작용을 증명하는 DNA분절 현상을 L-1210 세포에서 관찰하였을 때, fr. 3을 30 $\mu\textrm{g}$/mL, 100 $\mu\textrm{g}$/mL로 처리한 군에서 만 DNA분절 현상이 관찰되었다. Fr. 3에 대한 DNA합성 억제능을 [$^3$H]thymidine incorporation test로 관찰하였을 때 50 $\mu\textrm{g}$/mL, 100 $\mu\textrm{g}$/mL로 처리한 군에서만 [$^3$H]thymidine incorporation이 저하되었다. 결론적으로 저령에는 백혈병세포인 L-1210과 HL-60의 세포생존 억제성분이 포함되어 있으며, 억제작용은 L-1210에 가장 뚜렷이 나타내었다. Fr. 3은 L-1210 세포에 대하여 DNA 합성능을 저해시켰고, Fr. 3가 L-1210 세포에 대하여 세포생존 억제작용을 나타내는 것은 계획된 세포사멸현상인 apoptosis에 의한 것으로 사료된다. 따라서 fr. 3에 대한 성분 연구가 요구되어진다.

• Archives of Pharmacal Research
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• 제20권4호
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• pp.368-371
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• 1997

In an effort to increase of the antitumor activity of 2(S)-$2^{I}$,$5^{I}$-trihydroxy-7, 8-dimethoxyflavanone isolated from Scutellaria indica, we synthesized its analogues, II, III and IV. They showed potent cytotoxicity in vitro against cancer cell lines, L1210, K562 and A549. On the basis of $ED_50$ values against the cancer cell lines, III exhibited about 2-7 times stronger activity than I against various cell lines. We tested the antitumor activity of the analogues against Sarcoma 180 cells in vivo and evaluated the structure-activity relationship. The antitumor activity appeared to be related to the hydrogen bond between carbonyl group at C-4 and hydroxyl group at C-5, in contrast to cytotoxic action.

• Archives of Pharmacal Research
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• 제9권2호
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• pp.115-117
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• 1986

Some coumarins were sythesized for the screening of their cytotoxic activities against L1210 cell. Of the conmarins sythesized, 6, 7-dihydroxycoumarin (esculetin) and 7, 8-dihydroxycoumain (dephnetin) as coumarins with dioxygenated A-ring, and 6-acetoxy-5, 7-dimethoxycoumarin and5, 7-dimethoxy-6-hydroxycoumarin as trioxygenated ones, show considerable cytotoxic activities, ED 50 being 4. 3, 8. 8, 17.2 and 5.5 $\mu$g/ml in the same other as the substances. THe extent oxygenation of the A-ring and the positions of the oxygen functions eventually play an important role for the cytotoxic activity.