• Archives of Pharmacal Research
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• v.20 no.3
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• pp.264-268
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• 1997

In order to study the structure-activity relationship of 7, 8-dimethoxy-2-methyl-3-(4, 5-methylenedioxy-2-vinylphenyl)isoquinoline-1(2H) -one (2), which has exhibited significant antitumor activity, chemical modifications of 2 were performed to yield the corresponding products (3-7). Further systematic uses of an efficient procedure for the synthesis of 3-arylisoquinoline derivatives produced the substituted compounds (9a-9g), which were tested for in vitro antitumor activity against five different human cancer cell lines.

• Journal of the Korean Society of Food Science and Nutrition
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• v.29 no.2
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• pp.235-240
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• 2000

Inhibitory effects of cockle extracts on carcinogen-induced cytotoxicity in C3H/10T1/2 cells were studied. Soup (62$\mu\textrm{g}$/mL), solubility (28$\mu\textrm{g}$/mL) and liposolubility (9 $\mu\textrm{g}$/mL) of the cockle inhibited 3-methyl-cholanthrene(MCA)-induced cytotoxicity in C3H/10T1/2 cells by 53 and 94%, respectively. These results suggest that the extracts cockle might have anticarcinogen-induced cytotoxicity of C3H/10T1/2 cells. The effects of cockle extracts on the immune response related to its antitumor activity in vitro and in vivo were investigated. The cockle extracts showed a direct cytotoxic effect on sarcoma-180 cells, tumor cells in vitro. Soup (0.49 mg/mL), solubility (0.11 mg/mL) and liposolubiliy (0.05 mg/mL) of the cockle markedly decreased the total numbers of sarcoma-180 cells, but not their viability. The phagocytic acitivity of peritoneal macrophage of mice was significantly augmented by these extracts of the cockle compared with that of control in vivo. These extracts also raised the phagocuytic index, indicating that the number of phagocytize dmicrobes per macrophage increased. Thus, cockle extracts might show a antitumor activity by enhancing the phagocytic cell activities.

• Archives of Pharmacal Research
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• v.21 no.2
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• pp.157-163
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• 1998

Several aniline mustard analogues were obtained by introducing N,N-bis(2-chloroethyl)amino moiety to phenyl ring of A10 analogues in order to increase reactivity of A10 analogs and selectivity into DNA. The in vitro antitumor activity of synthesized compounds was evaluated using five different solid tumor cell lines by SRB method. Aniline mustard analogues exhibited more potent antitumor activity than A10 analogs. Especially, m-aniline mustard of benzoyl analogue displayed remarkable antitumor activity.

• Biomolecules & Therapeutics
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• v.3 no.3
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• pp.217-222
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• 1995

Several acyclonucleoside analogues of pyrimidine base and N$^1$-derivatives of 5-fluorouracil have been synthesized and evaluated for their biological effects. When tested with in vitro Lekemia L1210 cells, the 5-fluorouracil derivatives exhibited slightly higher antitumor activity than the parent 5-fluorouracil. When tested against Herpes Simplex Virus type 1 and type 2 cultured in the Vero cell, the 5-fluorouracil derivatives showed weak antiviral activity.

• YAKHAK HOEJI
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• v.46 no.3
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• pp.213-218
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• 2002

In the previous report, we described the in vivo antitumor activity of PJ-4, a protein-polysaccharide fraction prepared from the culture filtrate of an insect-born fungus, Paecilomyces tenuipes DGUM 32001. In the present study, we elucidated the immunomodulating activity of PJ-4 on the BALB/c mouse splenic lymphocytes using flow cytometrical techniques. As a result, PJ-4 was found to stimulate the lymphocytes not only to form lymphoblasts but also to express CD25 (IL-2 receptor $\alpha$ chain) molecule, which is well known as a T cell activation marker. More interestingly, its T cell stimulatory activity was more strongly exerted on CD8$^{+}$ T cells than on CD4$^{+}$ T cells. All these data suggest that PJ-4 exerts its antitumor activity at least partly through stimulation of T cells which play major roles in the cell-mediated immune system.tem.

• Journal of Pharmaceutical Investigation
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• v.24 no.4
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• pp.245-250
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• 1994

An attempt was made to develop new water-soluble antitumor Pt(ll) complexes containing ethylenediamine, and their structures were determined by infrared spectroscopy, $^{13}C$ nuclear magnetic resonance and elemental analysis. Their antitumor activities in vitro against L-1210, p-388 leukemia cells and M-14 melanoma cells were investigated and acceptable antitumor activity was found as compared with cisplatin.

• Macromolecular Research
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• v.16 no.6
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• pp.510-516
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• 2008

New antitumor active polymers, poly(methacryloyl-2-oxy-1,2,3-propanetricarboxylic acid-co-exo-3,6-epoxy-l,2,3,6-tetrahydrophthalic acid) [poly(MTCA-co-ETAc)], poly(methacryloyl-2-oxy-l,2,3-propanetricarboxylic acid-co-hydrogen ethyl-exo-3,6-epoxy-l,2,3,6-tetrahydrophthalate) [poly(MTCA-co-HEET)], and poly(methacryloyl-2-oxy-l,2,3-propanetricarboxylic acid-co-a-ethoxy-exo-3,6-epoxy-1,2,3,6-tetrahydrophthaloyl-5-fluorouracil) [poly(MTCA-co-EETFU)] were synthesized and characterized. Their antitumor activity, inhibition of DNA replication and antiangiogenesis were examined. The structures of the polymers were identified by FT-IR, $^1H$ and $^{13}C$-NMR spectroscopy. The number average molecular weights of the fractionated polymers determined by GPC ranged from 9,400 to 14,900, and polydispersity indices were less than 1.7. The in vitro cytotoxicity of these polymers was determined and their antitumor activity was evaluated. The $IC_{50}$ values (the drug concentration at inhibition of 50% tumor growth) indicated that the synthesized polymers were much better inhibitors of cancer cells and showed lower cytotoxicity than the free 5-FU. The in vivo antitumor activity of the conjugates was examined using mice bearing the sarcoma 180 tumor cell line. The life spans (TIC) of the mice treated with the conjugates were higher than those treated with the free 5-FU. In addition, the synthesized conjugates showed excellent antiangiogenic activity based on an embryo chorioallantoic membrane assay.

• YAKHAK HOEJI
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• v.38 no.2
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• pp.158-165
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• 1994

A protein-polysaccaride fraction Kp(53.9% polysaccharide, 14.2% protein) was separated from the shake-cultured mycelia of a basidiomycetous fungus, Phellinus linteus, and its antitumor activity against sarcoma 180 in ICR mice was investigated. When administered after the tumor implantation, Kp exerted antitumor activity by inhibiting the growth of the sarcoma 180 solid tumor by 71.5% and increasing the life span of the sarcoma 180 ascitic mice by 51.5% at 100 mg/kg. In pretreatment tests, in which Kp was administered once daily for 9 days before the tumor implantation, Kp inhibited the growth of the solid and ascites form of sarcoma 180, respectively, by 35.4% and by 80.3% at 100 mg/kg. However, Kp showed no in vitro cytotoxic activity against a murine leukemia L1210 and a human gastric tumor SNU.1 upto the concentration of $200\;{\mu}g/ml$. From these results, it is clear that the antitumor activity of Kp is exerted through its immunomodulating activity on the host's immune system.

• YAKHAK HOEJI
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• v.45 no.1
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• pp.64-70
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• 2001

Protein-polysaccharide fractions, PJ-3 and PJ-4, were prepared from mycelial culture filtrate of an insect-born fungus, Paecilomyces japonica DGUM 32001, and subjected to a flow cytometrical analysis for their vivo antitumor and immunomodulating activity in ICR mice. When i.p. injected once daily for semen days at 100 mg/kg, PJ-4 exerted a strong antitumor activity showing the growth inhibition ratio of 85.1% against i.p. implanted sarcoma 180 cells, while PJ-3 showed only a weak activity. Moreover, PJ-4 signiscantly increased the expression level of CD25 (IL-2R $\alpha$-chain) as well as forward scatter (FSC) values of splenic CD8$^{8}$ T cells. It is also noteworthy that PJ-4 strongly induced the peritoneal exudate cells in the same experiment. In an in vitro study, PJ-4 slightly inhibited the growth of sarcoma 180 cells at the concentration of 50$\mu$g/ml or higher. These results strongly suggest that PJ-4 might exert its antitumor activity through immunostimulation as well as direct inhibitory activity on the tumor cells.

• Biomolecules & Therapeutics
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• v.8 no.3
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• pp.235-240
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• 2000

Antitumor effect of LC43, a protein-bound ploysaccharide (M.W. 43 kDa) that was purified from intergeneric protoplast fusant of Lentinus edodes and Coriolus versicolor, was elucidated against mouse sarcoma 180 cell in vitro and in vivo. By injecting LC43 into ICR mice bearing solid or ascitic sarcoma 180, tumor regression and survival rates were investigated. To examine the effects of LC43 on immunopotentiation activity. immunoorgan weight, B cell differentiation, T cell activity and macrophage activation were determined. LC43 showed antitumor effects against both solid tumor and ascitic tumor of sarcoma 180. It did not change significantly the immunoorgan weight but potentiated immune responses such as B cell differentiation and the release of superoxide anion from macrophages. These results suggest that the protein-bound polysaccharide of LC43 exhibited antitumor activities through the activation of immune-related cells and acted as an immunmodulator.