• The Korean Journal of Mycology
• /
• v.9 no.2
• /
• pp.49-66
• /
• 1981

The objectives of this investigation were to produce artificially an antitumor constituent by submerged culture of the mycelium of Coriolus versicolor (Fr.) Quel., to characterize the influence of various modifications of the nutrient and culture conditions with respect to the pro­duction, to determine chemical composition of the antitumor constituent, and to examine effects of the constituent on the immune response of mice. Submerged agitation of the mycelium in flasks containing a nutrient solution showed its adequate growth. Especially the mycelial growth in the medium containing glucose and yeast extract was abundant. The addition of cotton seed flour or ginseng waste to the medium increased the yield of mycelial growth and the production of the antitumor constituent. The replacement of glucose with starch also yielded the adequate growth. The antitumor constituent extracted from the mycelium and isolated from the culture filtrate was a protein-bound polysaccharide. The analyses of this constituent by GLC and amino acid autoanalysis showed that it contained four monosaccharides and fifteen amino acids. The protein-free polysaccharide of the constituent was also found to exert greater antitumor activity against sarcoma-180 in mice than the entire constituent. The antitumor constituent was found to potentiate the immune response of mice against sheep red blood cell. The protein-bound polysaccharide exerted more favorable influence on the immunity than the protein-free moiety.

• Korean Journal of Pharmacognosy
• /
• v.15 no.2
• /
• pp.61-73
• /
• 1984

To investigate antitumor component of Lyophyllum decastes, the aqueous extract of its shake-cultured mycelia was subjected to antitumor test against sarcoma 180 cells implanted in ICR mice. The extract showed an inhibition ratio of 65.4% and was found to consist of a polysaccharide moiety and a protein moiety. After purification with DEAE-Sephadex A-50 ion exchange chromatography, Fraction D showed the highest inhibition ratio of 75.7%. The antitumor constituent was examined for immunoaccelerating activity and was found to increase macrophage accumulation in the peritoneal cavity and plaque forming cells of the spleen cells. It was named lyophyllan after the genus name.

• YAKHAK HOEJI
• /
• v.40 no.2
• /
• pp.225-229
• /
• 1996

The cytotoixic effect of Pylorae Herba (Pyrola japonica Klenze) against L1210 and K-562 cells was studied in vitro. The methanolic extract of Pylorae Radix was add ed to the culture of L1210 cells and K-562 cells for the cytotoxic activity and the ED50 values of hexane, ethylacetate, buthanol and water fractions from methanolic extract were determined using MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazoliumbromide) assay. The active constituent isolated by bioassay guided fractionation followed by purification gave rise to a yellow needle crystal and was clarified to be chimaphilline by the comparison with the published data. The average life spans with it were not prolonged significantly on tumor growth in hybrid female mouse (BDF1-KIST) inoculated subcutaneously with P388 cells.

• YAKHAK HOEJI
• /
• v.45 no.4
• /
• pp.328-333
• /
• 2001

Ginsenoside Rh$_2$, a minor glycoside constituent of the red ginseng is known as an unique antitumor compound. Several attempts to prepare it in a large scale including semisynthesis from betulafolientriol, an 3-epimer of 20(S)-protopanaxadiol, has been reported. We have previously reported a synthesis of ginsenoside Rh$_2$from 20(S)-protopanaxadiol obtained by alkaline hydrolysis of total ginsenoside. The regioselective synthesis of this compound was achieved by protection of 12-OH group.

• The Korean Journal of Mycology
• /
• v.16 no.3
• /
• pp.162-174
• /
• 1988

To separate and quantitate antitumor protein-bound polysaccharides of Coriolus versicolor, the constituents were obtained from the submerged culture of the mycelia(C) and from the extract of the carpophores of the wild fungus(N). The polysaccharides were degraded by methanolysis. The neutral monosaccharides were separated and quantitated by HPLC using microbondapak carbohydrate analysis column, refractive index detection and water-acetonitrile acetic acid elution. The analyses of these constituents by HPLC showed that the natural constituent(N) consisted of glucose, xylose and mannose, the average amount being 96.44, 2.16 and 1.73%, respectively. The fermentation constituent(C) consisted of mannose, glucose, xylose and galactose, the average amount being 61.30, 14.00, 12.95, and 11.75%, respectively. The analyses of these constituents by an amino acid analyzer showed that both C and N contained 17 amino acids.

• The Korean Journal of Mycology
• /
• v.11 no.2
• /
• pp.91-95
• /
• 1983

To investigate antitumor constituents of Hydnum repandum, which belongs to edible basidiomycetes, the mycelia separated from the carpophore were shake-cultured and subjected to hot water extraction. The extract was concentrated under vacuum and mixed with a three-fold volume of 95% ethanol to yield precipitates. The water soluble fraction of the precipitates was dialyzed and then lyophilized to yield a water soluble protein-polysaccharide fraction (= WPPF). This exerted antitumor activity against sarcoma 180 implanted in ICR mice. When administered i.p. at the dose level of 20mg/kg once daily for ten consecutive days, it showed an inhibition ratio of 54.3%. WPPF was found to be composed of a polysaccharide moiety (42% of WPPF) and a protein moiety (28% of WPPF) when determined by colorimetric method using anthrone reagent and Folin's phenol reagent. The polysaccharide moiety of WPPF was found to contain glucose (57.4%), mannose(19.3%), galactose (10.8%), xylose (6.8%), and fucose (5.7%), when the methanolysate of WPPF was analysed by GLC method.

• The Korean Journal of Mycology
• /
• v.12 no.4
• /
• pp.129-132
• /
• 1984

To find antitumor constituents in Korean basidiomycetes, the mycelia of Lentinus edodes DMC7, which had shown a good mycelial growth in shakeflasks, were cultured at $27^{\circ}C$ on an orbital shaking incubator at 180 rev/min for 12 days. The medium was composed of glucose (50g/l), yeast extract (9g/l), peptone (9g/l), and seven inorganic salts. A water soluble macromolecular fraction, LF-3, was obtained from the culure filtrate by fractionation with ethanol and dialysis using a Visking tube. When LF-3 was administered i.p. at 50mg/kg/day once daily for 10 consecutive days to female ICR mice which were implanted s.c. with sarcoma 180 $(10^6\;cells/mouse)$, it exerted a highly significant antitumor activity, with the tumor inhibition ratio of 53. 1%.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.16 no.3
• /
• pp.542-546
• /
• 2002

The purpose of this study was to investigate the effect of 2-thioDMNQ-S160, shikonin analogue isolated from Uthospermum Erythrorhizon, on the antitumor activity. In the present study, 2-thioDMNQ-S160 exhibited a significant cytotoxicity against L1210, A549, U937, and 816-BL6 cell lines with IC/sub 50/s of 2.4ug/ml, 2,0ugjml. 4ug/ml and 20 ug/ml, respectively. 2-ThioDMNQ-S160 strongly inhibited adhesion of B16-BL6 cells to gelatin and matrigel coated matrices. Also, 2-ThioDMNQ-S160 exhibited anti-invasive effect of B16-BL6 cells. The T/C% was 123 % in 2-ThioDMNQ-S160 treated group in S-180 bearing ICA mice. These results suggested that 2-thioDMNQ-S160 might be a potent candidate of cancer drug.

• YAKHAK HOEJI
• /
• v.41 no.5
• /
• pp.559-564
• /
• 1997

To find out antitumor active principles from natural resources, we have evaluated various extracts from the leaves of Alnus hirsuta (Betulaceae). The ethylacetate extract of this plant was found to show a significant cytotoxicity against several kinds of cultured human solid tumor cell lines (AGS, A5 49, HCT15, SKOV3, HEP3B) in vitro. Using cytotoxicity-guided chromatographic purification of the ethylacetate extract, cytotoxic constituent:1,7-bis-(4-hydroxyphenyl)-5-(${\beta}$-D-glucopyranosyloxy)-3-heptanone, was isolated and structurally identified by physico-chemical properties and spectroscopic evidences.

• YAKHAK HOEJI
• /
• v.41 no.6
• /
• pp.704-708
• /
• 1997

In our search for bioactive natural products with antitumor activity, we have valuated various extracts of Saururi Herba (Saururaceae), which has been used in traditional medici ne for edema, beriberi, jaundice, turbid urine, carbuncle and furuncle. The hexane extract of the aerial part of this plant was found to show a potent cytotoxicity against several kinds of cultured human solid tumor cell lines (AGS, A549, HCT15, SKOV3, HEP-3B) in vitro. Using cytotoxicity-guided chromatographic separation of the hexane extract, cytotoxic constituent: 10-aminomethyl-3-hydroxy-4-methoxyphenanthrene-carboxylic acid lactam, was isolated and structurally identified by physico-chemical properties and spectroscopic evidences.