• Journal of Ginseng Research
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• v.29 no.4
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• pp.176-181
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• 2005

Our previous reports demonstrated that ip. administration of Korean red ginseng acidic polysaccharide (RGAP) exerts antitumor activity In mice. The present study was carried out to compare the effects of ip. and p.o. routes of administration of RGAP on either normal or tumor-bearing BALB/c mice. RGAP was administered either ip. or p.o. at doses of 100, 300, 500, 1000 mg/kg for 1 or 5 weeks. Peritoneal macrophages from mice treated with RGAP p.o. at a dose of 300 mg/kg either for 1 or 5 weeks did not exhibit growth inhibition activity toward WEHI-I64 tumor cells. However, administration of RGAP at a dose of 600 mg/kg for both 1 and 5 weeks increased the antitumor activity of macrophages. Oral administration of RGAP (600 mg/kg) for 5 weeks and ip. administration of RGAP (300 mg/kg) for 1 week resulted in antitumor activities of $40\%$ and $45\%$, respectively, indicating that the effect of i.p. injection is more potent 2 and 5 times than that of p.o. one in terms of dose and duration, respectively. Tumor inhibition rates of RGAP at doses of 300, 500, 1000 mg/kg in mice transplanted with B16-F10 melanoma were 4.4, 12.0, and $45.4\%$, respectively, meaning that p.o. dose higher than 500 mg/kg possess marked antitumor activity. The results above suggests that p.o. administration of RGAP also show antitumor activity in vivo depending on the dose.

• Archives of Pharmacal Research
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• v.22 no.6
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• pp.592-607
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• 1999

2-(1-Aryl-1-hydroxymethyl)-and 2-aroyl-DHAQ derivatives (DHAQ, 1,4-dihydroxy-,10-anthraquinone), and 2-(1-aryl-1-hydroxymethyl)-ATO derivatives (ATO, anthraceneactivity (T/C 125~128%), though their cytotoxicity was not further improved compared to that of 2-(1-aryl-1-dydroxymethyl)-1,4-dihydroxy-9,10-anthraquinones. They manifested no correlation between the cytotoxicity and the antitumor activity. In case of 2-[1-hydroxy-1-(4-propylphenyl)-methyl]-ATO, the most bioactive one in viv-1,4,9,10-tetraone) were synthesized and their antitumor activities were determined. 2-(1-Aryl-1-hydroxymethyl)-DHAQ derivatives showed a stronger cytotoxicity compared to the series of 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinone derivatives. It was suggested that the presence of aryl group at the side chain accelerated the bioreductive activation leading to cell death. 2-Aroyl-DHAQ derivatives, despite their higher electrophilicity, revealed smaller cytotoxicity and antitumor activity (expressed by T/C value) than 2-(1-aryl-1-hydroxymethyl)-DHAQ derivatives. Thus, no consistent relationship between the electronic effect on aromatic side chain and the cytotoxicity was observed. ATO series exhibited a higher antitumor o among the same series, it showed an $ED_{50}$ value of 10.2 mg/mL and a T/C value of 218%. It is assumed that the anthrancene1,4,9,10-tetraones after uptake into cellular tissues might be transformed to a cytotoxic metabolite(s).

• Korean Journal of Pharmacognosy
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• v.28 no.4
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• pp.264-270
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• 1997

This Study was carried out develop antitumor effect of the n-butanol soluble of fraction of Perilla frutescens on human skin melanoma cells. The antitumor activity of various fractions obtained form n-butanol soluble fraction of Perilla frutescens was evaluated in human skin melanoma cells. The antitumor activity of the n-butanol soluble fraction in human skin melanoma cells was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay, neutral red (NR) assay and sulforhordamine B protein (SRB) assay of colorimetic assay methods. The light microscopic study was carried out to observe morphological changes of cultured human skin melanoma cells. These results were obtained follows; The fractions 5 and 6 of the n-butanol soluble fraction of P frutescens were shown significant antitumor activities. The number of human skin melanoma cells were decreased and tend to form cell cluster by treatment with actions 5 and 7 of the n-butanol soluble fraction of P. frutescens. The fraction 6 of the the n-butanol soluble fraction showed the highest antitumor activity on P. frutescens. These results suggest that the fraction 6 of the n-butanol soluble fraction of P. frutescens may be a valuable choice for the studies on the treatment of human skin tumors.

• Korean Journal of Pharmacognosy
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• v.31 no.1
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• pp.7-15
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• 2000

Glycyrrhizae Radix aqua-acupuncture solution (GRAS) and Glycyrrhizae Radix water-extracted solution (GRWS) were prepared and tested for organ toxicities, antitumor activities, and immunomodulatory effects. The organ-toxicity of GRAS to male ICR mice was studied by the measurements of glutamic oxaloacetic transaminase (GOT), glutamic pyruvate transaminase (GPT), lactate dehydrogenase (LDH), and alkaline phosphatase (ALP-s) activities after injection of GRAS for 7 days. The activities of GOT, GPT, LDH, ALP-s were decreased with GRAS. It was shown to possess considerable toxicity toward various tumor cell lines. Concentration of GRAS at 1.5g/ml and 3g/ml resulted in more than 80% inhibition of growth in Ehrlich ascites tumor cells (EATC), Hepa1c1c7, and HeLa cells. Toxicity of GRAS to A549 revealed that 68% inhibition of growth. GRWS at the concentration of 3g/ml showed more than 80% inhibition of growth with EATC, Hepalclc7, A549 and HeLa. In morphological study, the number of cells were decreased, and the shape of cells was round-form in EATC, Hepalclc7, A549 and HeLa cells with GRAS. Administration of GRAS inhibited the growth of EATC in vivo. Mice given EATC at 1.5g/ml or 0.3g/ml GRAS had 16.7% to 50% survival after 21 days. GRAS increased the proliferation of T and B cells and the cytolytic activity of purified T cell. The biosyntheses of nucleic acid and protein of EATC, Hepalclc7, A549 and HeLa cells were inhibited by GRAS.

• Journal of Marine Bioscience and Biotechnology
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• v.1 no.3
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• pp.144-155
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• 2006

This report reviews the literatures on chemical constituents of marine sponges of the genus Spongosorites and also highlights our own research. Specific biological activities of the metabolites from these sponges include: cytotoxic, antitumor, antibacterial, antifungal, antiviral, anti-inflammatory, and other pharmacological activities.

• Journal of Food Hygiene and Safety
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• v.23 no.2
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• pp.149-156
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• 2008

This study was carried out to investigate the anti oxidative and antitumor activities of medicinal plants for the purpose of developing a functional food. The methanol extracts of Agrimonia pilosa was fractionated with five solvents and examined anti oxidative activities and enzyme inhibitory activities in addition to growth inhibitory activity of human cancer cell. The contents of total phenol compounds in EtOAc and BuOH fraction were 39.89% and 39.56%, respectively. Strong electron donating abilities(>90%) were shown in these fractions and its abilities were 92.90% ($500\;{\mu}g/ml$), 94.47% ($1000\;{\mu}g/ml$) in EtOAc fraction and 93.77% ($500\;{\mu}g/ml$), 92.90% ($1000\;{\mu}g/ml$) in BuOH fraction, respectively. These fractions exhibited more than 50% nitrite scavenging ability and potent inhibition activities to XOase activity (93.06%, 91.73%) at concentration of $1000\;{\mu}g/ml$. In antitumor activity test, hexane fraction showed the strongest growth inhibition activity against HT-29, SNU-1 and HeLa cells. Inhibition levels were 51.50, 90.09% in HT-29, 88.19, 95.11 % in SNU-1 and 42.66, 96.40% in HeLa at the concentration of 50, $100\;{\mu}g/ml$, respectively.

• Journal of Acupuncture Research
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• v.17 no.1
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• pp.129-142
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• 2000

Gamdutang aqua-acupuncture solution(GAS), Gamdutang water-extracted solution(GWS) and Degamdutang aqua-acupuncture solution(DGAS) were prepared and tested for potential antitumor activities. It was used three biomarkers (quinone reductase, omithine decarboxylase, glutathione) to test chemopreventive potentials of GAS, GWS, DGAS. GAS was potent inducer of quinone reductase activity in Hepalclc7 murine hepatoma cells in culture, whereas GWS is less potent. GAS, GWS and DGAS were significantly induced quinone reductase activity in cultured rat normal liver cell, Ac2F. Glutathione levels were increased about 1.8-fold with GAS, 1.0-1.1 fold with GWS, DGAS in cultured murine hepatoma hepaiclc7 cells. In addition glutathione s-transferase levels were increased with GAS, GWS and DGAS. The effects of GAS, GWS and DGAS were tested on the growth of Acanthamoeba castellanii. Proliferation of Acanthamoeba castellanii was inhibited by GAS, GWS and DGAS at concentradons of $1{\times}$ and $5{\times}$. These results suggest that GAS has chemopreventive potential by inducing quinone reductase and quinone reductase activities, inhibition of ornithine decarboxylase activity, and increasing glutathione levels.

• The Journal of Internal Korean Medicine
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• v.21 no.3
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• pp.425-432
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• 2000

Objective : It is well known that Gagamsojeokbackchool-san show antitumor effects and its activities are result from enhancement of immune function, we investigated the antitumor effects of Sambonggangyongbaneo-tang and its mechanism. Methods : We measured change of body weight, weight of immune organs (Spleen, Thymus), Liver, Kidney, tumor weight, cytotoxicity for investigation of antitumor effects of Sambonggangyongbaneo-tang. Results : 1. The body weight of mouse has no significant difference between control and sample groups. 2. The weights of immune organs (Spleen and Thymus) decreased significantly in sample groups. The weights of Liver and Kidney have no significant difference. 3. The tumor weights in mouse decreased significantly in sample groups and showed dose-dependent effect. 4. Cell viability of Sarcoma 180 has no significant difference in sample groups. 5. HeLa cell viability has no significant difference in low concentration, but it decreased significantly in high concentration. Conclusions : According to the above results, it could be suggested that Sambonggangyongbaneo-tang has prominant antitumor effects and cytotoxicity.

• BMB Reports
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• v.31 no.6
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• pp.560-564
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• 1998

Echinomycin-7 is an echinomycin derivative, Smethylated sulfonium perchlorate of echinomycin. We studied the in vitro cytotoxicity and in vivo antitumor activity of echinomycin-7 against P388 leukemia cells and compared the results with echinomycin. With respect to the cytotoxic effects, echinomycin-7 had cell line-dependent $IC_{50}$ values while echinomycin had similar values to several tumor cell lines. Also, in vivo antitumor activities were observed in tumor-bearing mice treated with both agents, which showed that echinomycin-7 had a broad therapeutic dose range. We also observed the apoptosis on leukemia cells treated with echinomycin-7 which exihibited the ladder pattern of DNA on electrophoresis. In addition to apoptosis, echinomycin-7 arrested $G_1/S$ phases of the cell cycle at the same time. We then examined the signaling pathway of echinomycin-7-induced apoptosis and showed that ERK of the MAP kinase family was activated and translocated into the nucleus by echinomycin-7 stimulation. This study suggests that echinomycin-7 acts as an antitumor agent through in vitro cytotoxicity and has in vivo antitumor activity against leukemia cells, and that the echinomycin-7- induced apoptosis might involve signal transduction via MAP kinases.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.159-160
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• 1998

Results of chemistry and biological activity of many years indicate that plants belonging to the Isodon genus are rich in ent-kaurane diterpenoids, which have been revealed to possess biological activities such as antitumor, antibacterial and antiinflammatory effects. In continuation of our research on diterpenoids in medicinal plants of this genus, the acetone extract from the leaves of I. xerophilus, which is a plant native to Yunnan province of China, showed potent antitumor activity against K562. After partition, the most active EtOAc part was studied. Four new diterpenoids named xerophilusin A(l), B(2), C(3), D(4), and eight known compounds including macrocalin B(5) and rabdorosthomin A(6) were isolated, whose structures were elucidated through a series of one- and two-dimensional NMR techniques(DEPT, COSY, HMQC, HMBC and ROESY experiments). Among them, compound 1, 2 and 5 had two unique epoxy units formed by two ether bridges from C-20 to C-7, C-14. Up to now, there are four compounds having such an peculiar structure besides these three compounds. Compound 3 and 4 were two of the few examples possessing $1{\beta}$ substitutes. All the diterpenoid compounds were subjected to the antitumor screening. It is interesting that only xerophilusin A(l), B(2) and macrocalin(5) exhibited significant antitumor activity against K562 by the method of MTT($IC_{50}$ were listed in Table 1.). The results inspired us to infer that the unique ether bridges from C-20 to C-7, C-14 possibly played an important role in the antitumor activity.