• Natural Product Sciences
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• 제9권2호
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• pp.112-116
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• 2003

The antitumor and immunostimulating activities of Acanthopanax sessiliflorus fruits were investigated. Polysaccharide isolated from this plant, when administered consecutively for 9 days at 50 and 100 mg/kg i.p. in mice, caused a significant increase in the life span and a significant decrease in the tumor weight and volume in mice inoculated with Sarcoma-180 tumor cells. Polysaccharide was also demonstrated to exhibit phagocytosis-enhancing activity as measured by the carbon clearance in mice. Polysaccharide, when administered i.p. at 50 and 100 mg/kg/day for 3 consecutive days, exhibited a significant RCtr/RCc [the rate of regression coefficient of the animals teated (RCtr) to that of the control (RCc)], being 1.44 (PI = 1), 1.52 (PI = 2) which was approximately the same with that of enhancement of phagocytosis, its potency as expressed by the regression coefficient ratio of zymosan (RCtr/RCc = 1.55, PI = 2), a typical phagocytosis enhancer. Polysaccharide also caused a significant increase in the acid phosphatase activity representing lysosomal enzymes in macrophages at 1-100 ig/ml in vitro in compliance with in vivo results. These results suggest that the antitumor activity of polysaccharide might be related to the immunostimulating function.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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• pp.185-185
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• 1998

As part of our continuing attempts to evaluate biologically active compounds from fruiting bodies of cultivated fungus of Paecilomyces japonicus Yasuda, we conducted series of experiments on various fractions and compounds isolated by systematic fractionations. Our main efforts were concentrated on searching for compounds showing antitumor activities, which were tested on mice carrying Sarcoma-180 ascitic tumor. The antitumor activity was assessed by the life spans after these mice were administered Lp. with test compounds for consecutive 20 days. One of two pure compounds, which we have isolated to date, demonstrated significant prolongation of life span. ( Mean Survival Time: 30.3 days compared to that of control: 23.6 days). Structural analysis showed that this compound corresponds to D-mannitol. On the other hand, Ergosterol, another isolated pure compound didn't show efficient antitumor activity. We also obtained water-soluble fractions containing protein-bound polysaccharides and n-butantol fractions, which showed strong antitumor activities, 35.4(150%) and 32.1(136.0%) days of MST, respectively. In SRB assay, however, the test materials didn't show any toxic effects, but the level of acid phosphatase increased significantly when they were applied in cultured macrophage in vitro. Therefore, we concluded that antitumour activities might be attributed to immunostimulating rather than cytotoxic effects. Further experiments are underway to purify and structurally characterize new antitumour compounds from the active fractions.

• 한국균학회지
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• 제24권1호통권76호
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• pp.17-24
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• 1996

목재부후성 담자균류의 배양 균사체의 생물활성을 조사하기 위하여 항균활성, 식물생장조절활성, 항암활성 및 그들이 생산하는 효소활성을 검정한 결과 Coriozus versicolor 5129와 C. pubescens 5131 균주는 그람양성세균에, Lenzites betulina 8029 균주는 그람음성세균에 저지 효과를 나타내었으며 L. betulina 8085 균주는 세균과 진균에 저지 효과를 나타내어 광범위한 항균 spectrum을 보였다. 대부분의 균주가 0.8ml/ml 농도 처리시 배추 및 무의 발아 및 생장을 억제하였으며, 특히 Fomitopsis pinicolor 8059와 Fomitella fraxinea 8084 균주의 경우 생육을 장하게 억제하였다. 그러나, Bjerkandera adusta 8054 균주는 0.4 및 0.2ml/ml농도에서 배추 및 무의 생육을 촉진하였다. 몇종의 목재부후균 다당체를 추출하여 암세포를 이식한 ICR mouse에 투여한 결과 거의 전 균주가 항종양 작용을 나타내었으나 버섯종류 간에 큰 차이를 보였고 그중 L. betulina 8029와 미분류된 8058 균주는 효과가 비교적 높았다. 목재부후균의 세룰로스와 리그닌 분해력은 거의 전 공시균주에서 나타났고 종류간에 역가가 다양하여 강력한 분해균의 선발 가능성을 보였다.

• Journal of Pharmaceutical Investigation
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• 제22권3호
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• pp.185-196
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• 1992

To assess its suitability as a prodrug of 5-fluorouracil (5-FU), 1-glycyloxymethyl-5-FU HCl (GFU), a 5-fluorouracil derivative having a glycyloxymethyl group at the N-l position was synthetized. Its physicochemical properties and hydrolysis kinetics, in aqueous solution of pH $1{\sim}10$ and in the presence of human plasma or rat liver homogenate were studied. Its acute toxicity and antitumor activity against sarcoma 180 were also examined, GFU showed higher lipid/water partition coefficient than 5-FU. The calculated $pK_{\alpha}$ values of 5-FU and GFU were 8.02 and 7,20, respectively. The decomposition rates of GFU in aqueous solution showed a pH-dependence over the pH range used, which could be ascribed to solvent catalysed hydrolysis reaction at pH lower than 4,16 and to specific hydroxide ion hydrolysis reaction at pH higher than 4,16, The half-life of GFU was 6,9 min in 80% human plasma solution and less than 3 min in rat liver homogenate at $37^{\circ}C$, The $LD_{50}$ value of 5-FU was 240 mg/kg while that of GFU was 440.6 mg/kg (226 mg as 5-FU). Both of 5FU and GFU showed a strong antitumor activity, Therapeutic ratios of 5-FU and GFU were 3.07 and 3.55, respectively.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 1999년도 The 6th International Symposium on the Development of Anti-Cancer Resource from Plants
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• pp.1-45
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• 1999

To date many kinds of compounds have been obtained from plants kingdom as antineoplastic and anti-cancerous agents. However, there is no special type of compounds for ncancer therapy. Various types of substances are effective for various types of cancers and tumors: for instance, alkaloids, lignans, terpenes and steroids etc. Curcumol obtained from Curcuma aromatica was tested and noticed to be effective against cancer of the uterine cervix clinically Oridonin isolated from Rabdosia ssp.is now investigated for clinical trials in China. Moreover, camptothecine isolated from Camptotheca acuminata is also antineoplastic alkaloid, but is very toxic. Chemical modification has been tried to decrease its toxicity. This compound is now using as clinical agent. Harringtonin was investigated as an anticancerous drug in China. Taxol, a compound with a taxane ring isolated from the bark of Taxus brevifolia, has been demonstrated to have substantial anticancer activity in patients with solid tumors refractory standard chemotherapy. Supply of this drug has severely limited full exploration of its antineoplastic potential. Some efforts are continued in National Cancer Institute NCI) Washington for surveying various Taxus species for optimal taxol content, improvement in semi-synthesis from baccatin III, improvement in method of extraction, and development of alternative renewable resources. Further, there are many compounds which have been reported as antineoplastic agents. On the other hand, we have screened on higher plants collected in Japan, China, Korea, Southeast Asia and South America for antineoplastic activity, which has been done using Sarcoma 180 ascites in mice, P388 Iymphocytic leukemia in mice, Chinese hamster lung V-79 cells, P388 cells and nasopharynx carcinoma (KB) cells in our laboratory, as primary screening. In this meeting, I will present on antitumor and cytotoxic substances of the higher plants (Rubia cordifolia, Ailanfhus Vilmoriniana, Aster tataricus, Taxus cuspidata var. nana, Cephalotaxus harringtonia var drupacea, etc.) selected from above screening tests.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 2000년도 The 7th International Symposium
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• pp.64-65
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• 2000

Cancer is a general term subjected to a series of malignant tumor diseases which may affect many different parts of the human body. These cancer diseases are characterized by a rapid and uncontrolled formation of abnormal cells in the body. Cancer chemotherapeutic agents can often provide the prolongation of life and occasionally cures. To date many kinds of compounds have been obtained from plants kingdom as anti-neoplastic and anti-cancerous agents. However, there is no special type of compounds for cancer therapy. In our laboratory, anti-tumor and cytotoxic screenings on higher plants collected in Japan, China, Korea, Southeast Asia and South America have been done by using Sarcoma 180 ascites in mice, P388 lymphocytic leukemia in mice, Chinese hamster lung V-79 cells, P388 cells and nasopharynx carcinoma (KB) cells. The family, Simaroubaceae consists of about 20 genera and 120 species, mainly shrubs and trees, distributed in tropical and subtropical country. Simaroubaceae is classified as RUTALES, together with Rutaceae, Burseraceae, Meliaceae, Malpighiaceae and Polygalaceae. The members differ from the Rutaceae in not containing oil glands. Bitter principles are a characteristic of the family, Simaroubaceae. The genera include Quassia (Simarouba) (40 spp.), Picrasma (Aeschrion) (6 spp.), Brucea (10 spp.), Soulamea (10 spp.), Ailanthus (10 spp.) and Perriera (1 spp.) etc.. Surinam quassia derived from Quassia amara growing in Guianas, north Brazil and Venezuela is used in traditional medicines for stomachic, anti-amoebic, anti-malarial and anti-anaemic properties. Also, various parts of a number of plants of the family Simaroubaceae have been used in traditional medicine for the treatment of a variety oi diseases including cancer, amoebic, dysentery and malaria. Then, the research has established that it is the quassinoid content of these plants that is responsible for above activities. In this meeting, I will present on anti-tumor and anti-malarial activities and their active principles of Simaroubaceae plants, Eurycoma longifolia, Ailanthus vilmoriniana, Simaba cedron and Brucea mullis which have been studied in our laboratory.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 2000년도 제7차 국제 심포지움(생약자원개발에 관한연구) 및 추계정기 학술발표회 초록집
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• pp.11-13
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• 2000

Cancer is a general term subjected to a series of malignant tumor diseases which may affect many different parts of the human body. These cancer diseases are characterized by a rapid and uncontrolled formation of abnormal cells in the body. Cancer chemotherapeutic agents can often provide the prolongation of life and occasionally cures. To date many kinds of compounds have been obtained from plants kingdom as anti-neoplastic and anti-cancerous agents. However, there is no special type of compounds for cancer therapy. In our laboratory, anti-tumor and cytotoxic screenings on higher plants collected in Japan, China, Korea, Southeast Asia and South America have been done by using Sarcoma 180 ascites in mice, P388 lymphocytic leukemia in mice, Chinese hamster lung V-79 cells, P388 cells and nasopharynx carcinoma (KB) cells. The family, Simaroubaceae consists of about 20 genera and 120 species, mainly shrubs and trees, distributed in tropical and subtropical country. Simaroubaceae IS classified as RUTALES, together with Rutaceae, Burseraceae, Meliaceae, Malpighiaceae and Polygalaceae. The members differ from the Rutaceae in not containing oil glands. Bitter principles are a characteristic of the family, Simaroubaceae. The genera include Quassia (Simarouba) (40 spp.), Picrasma (Aeschrion) (6 spp.), Brucea (10 spp.), Soulamea (10 spp.), Ailanthus (10 spp.) and Perriera (1 spp.) etc.. Surinam quassia derived from Quassia amara growing in Guianas, north Brazil and Venezuela is used in traditional medicines for stomachic, anti-amoebic, anti-malarial and anti-anaemic properties. Also, various parts of a number of plants of the family Simaroubaceae have been used in traditional medicine for the treatment of a variety of diseases including cancer, amoebic, dysentery and malaria. Then, the research has established that it is the quassinoid content of these plants that is responsible for above activities. In this meeting, I will present on anti-tumor and anti-malarial activities and their active principles of Simaroubaceae plants, Eurycoma longifolia, Ailanthus vilmoriniana, Simaba cedron and Brucea mollis which have been studied in our laboratory.

• 동아시아식생활학회지
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• 제18권3호
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• pp.302-310
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• 2008

In this study, potato kimchi was prepared by applying heat to raw potatoes, and then the physico-chemical properties and anti-cancer effects of the kimchi were analyzed. The texture results indicated the potato kimchi had very good hardness and springiness attributes. During th late storage period, total vitamin C content of the kimchi slowly increased. In addition, the potato kimchi had non-volatile organic acid changes that promoted early aging; however, after the complete aging period, it was comparatively similar to other types of kimchi. Using the methanol extracts of various kimchi samples, the potato kimchi(solid 100%) showed the highest anti-carcinogenic effects in terms of anti-tumor activity in tumor bearing Balb/c mice with sarcoma-180 cells. In addition, the effects of the methanol extracts on hepatic glutathione S-transferase content were $289.76\;{\mu}mol/mg$ protein/min, $250.97\;{\mu}mol/mg$ protein/min, $251.20\;{\mu}mol/mg$ protein/min, $219.53\;{\mu}mol/mg$ protein/min, $183.79\;{\mu}mol/mg$ protein/min, for control kimchi, mul kimchi, and two potato kimchis [(solid 100%) and(solid 60%+kimchi juice 40%)], respectively. The in vivo anti-cancer effects of the potato kimchi were investigated using AGS human gastric adenocarcionoma cells and HT-29 human colon adenocarcionoma cells. Overall, an MTT assay revealed that the methanol extract of the potato kimchi showed the highest anti-carcinogenic effects.

• Archives of Pharmacal Research
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• 제16권4호
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• pp.336-338
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• 1993

The immunomodulating activity of Kp, an antitumor protein-polysacchanide preparation from the shake-cultured mycelia of Phellinus linteus, was investigated in ICR mice subcutaneously implanted wit $1\times10^6$ cells of sarcoma 180. The mice were intraperitoneally administered with Kp at a does of 100 mg/kg once daily for five consecutive days starting from 24 hrs after the tumor implantation. Ten days after the last injection, the mice were immunized with $1\times10^7$ or $4\times10^8$ sheep red blood cells (SRBC) and five days later, the antibody-forming immune response were assessed by direct hemolytic plaque assay. To an immunization does of $1\times10^7$ SRBC, the Kp-treated mice elicied a successful humoral immune response despite the turmor-burden and produced $259\times10^3$ plaque-forming cells (PFC)/spleen, while the corresponding tumor-bearing control mice showed virtually no reponse $(2.0\times10^3$ PFC/spleen) (the stimulation index=129.5). However, to an immunization dose of $4\times10^8$ SRBC, both of the control mice and Kp-treated mice showed almost the same level of strong humoral immune response. From these data it is clear that Kp effectively restores the humoral immune response of the turmor-bearing ICR mice.

• 한국균학회지
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• 제11권4호
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• pp.151-157
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• 1983

To find antitumor components in Korean basidiomycetes, the carpophores of Armillariella mellea which were collected in Gyeong Gi Province were extracted with distilled water at $90{\sim}100^{\circ}C$ for eight hours. The hot water extract was concentrated under reduced pressure, mixed with three-fold volumes of ethanol and allowed to stand at $4^{\circ}C$ overnight. The precipitate was centrifugated and lyophilized to yield a protein-polysaccharide fraction. It was examined for antitumor activity against sarcoma 180 implanted in ICR mice. The fraction showed 75.7%, 83.9%, and 94.1% of tumor inhibition ratios at the doses of 10, 20 and 50 mg/kg/day, respectively. The chemical analysis of the fraction showed that it contained a polysaccharide(41.3%) and a protein (35.0%). The hydrolyzates of the polysaccharide moiety contained fucose (4.5%), xylose (1.1%), galactose (17.4%), glucose (55.4%), mannose(19.4%), and one unknown monosaccharide. The protein moiety contained seventeen amino acids. The protein-polysaccharide from A. mellea was administered, i.p., to mice and caused an influx of polymorphonuclear leukocytes (PMN) at $5{\sim}24$ hours which was followed by an accumulation of macrophages and disappearance of the PMN at $48{\sim}72$ hours.