• YAKHAK HOEJI
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• v.44 no.6
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• pp.607-612
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• 2000

Generally, antitumor drugs have strong toxicity and result in damage in normal cells. Previously, lectin has been reported as a tumor cell specific binding protein and tannin as an antitumor substance. In this study, we investigated antitumor activity of lectin-conjugated ellagitannin and used praecoxin A as an ellagitannin source. We injected mouse melanoma cell, B16-F10, on right the femoral region of C57BL/6 mouse. After 10 hours later, first treatment with praecoxin A, lectin-praecoxin A mixiture and lectin-conjugated praecoxin A was carried and followed by injection i.m. every 48 hours. Praecoxin A extended the life of mice up to 14.8% in comparison with the negative control group at 5 mg/kg dose. The life extending ratio of Lectin-praecoxin A mixture was 26.1% at 5 mg/kg dose, and the life extending ratio of lectin-conjugated praecoxin A was 28.7% at 5 mg/kg dose. On the basis of these findings, we suggest that antitumor activities of lectin-praecoxin A mixiture and lectin-conjugated praecoxin A on survival are better than that of praecoxin A.

• Toxicological Research
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• v.13 no.4
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• pp.311-316
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• 1997

This study was carried out to develop antitumor effect of the n-butanol soluble fraction of Perilla frutescens on (KB cells) human oral epitheloid carcinoma cells. The cytotoxictty of methanollc extract of Perilla frutescens on KB cells was evaluated by 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide(MTT) assay. The antitumor activity of various fractions obtained from n-butanol soluble fraction of Perilla frutescens was evaluated in human oral epithelold carcinoma cells. The antitumor acavity of the n-butanol soluble fraction on human oral epitheloid carcinoma cells was evaluated by MTT assay of colorimetric method. The light microscopic study was carried out to observe morphological changes of cultured human oral epitheloid carcinoma cells. These results were obtained as follows; 1. The fractions 1,2 and 3 of the n-butanol soluble fraction of Perilla frutescens were shown significant antitumor activities. 2. The number of human oral epitheloid carcinoma cells were decreased and tend to form cell cluster by treatment with fractions 1,2,3 and 4 of the n-butanol soluble fraction of Perilla frutescens. 3. The fraction 1 of the n-butanol soluble fraction of Perllla frutescens showed the highest antitumor activity on Perilla frutescens. It has been selected as a lead fraction for further examinations.

• Korean Journal of Pharmacognosy
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• v.39 no.3
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• pp.237-240
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• 2008

C-22 is one of health food made in Han Kook Shin Yak. For studying its antitumor activity, the 50% ethanol extract from C-22 was tested on BDF1 mice bearing LLC tumor cell by Teruhiro’s method. The samples were intraperitoneally injected to mice once a day with a daily dose of 50, 100, and 200 mg/kg for 14 consecutive days. Taxol was used as positive control with a dose of 50 mg/kg. As a result, the C-22's extracts dose dependently inhibited the tumor volume with the IRTV values of 28.7, 46.7, 58.9% and the IRTW values of 28.1, 46.0, 57.8% in 50, 100, and 200 mg/kg, respectively, while the Taxol showed antitumor activity with IRTV and IRTW values of 68.5 and 67.3% in 50 mg/kg. No loss of body weight was observed at any samples. This data suggested that the C-22's antitumor activity was enough to use as a cancer chemopreventive agent, and it will be used for preventing cancer as health food.

• Archives of Pharmacal Research
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• v.18 no.6
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• pp.396-401
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• 1995

As a part of trials to develop the antitumor agent from tannins isolated from plants, the antitumor activity of peduculagin, an ellagitannin, isolated from Alnus hirsuta var. microphylla was examined in vitro and in vivo. In vitro, the cytotoxicity was determined by 0.4% typanblue dye exclusion method. peduculagin showed the dose-dependent cytotoxicity against human chronic myelogenous leukemia (K-562), human promyelocytic leukemia (HL-60), mouse lymphoid neoplasm (P388), mouse lymphocytic leukemia (L1210) and mouse sarcoma 180(S180) cell lines. $ED_{50}\; values\; (ED_{50})$ of each cell line were 5.30, 0.92, 2.78, 9.35 and $1.38 \mug/ml$ respectively. The most sensitive cell line was HL-60. In vivo, pedunculagin was administered to ICR mouse with the doses of 50 and $100{\;}{\mu}g/ml$intraperitoneally once at 20 days before S180 inoculation. peduculagin showed the antitumor activity and its T/C ratio (%) was 120.82% in the group of both concentrations.

• Microbiology and Biotechnology Letters
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• v.23 no.3
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• pp.329-336
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• 1995

For the development of new antitumor antibiotics produced by microorganisms, Streptomyces sp. YBE-316 was isolated from soil. The productivity of the antitumor antibiotic from Streptomyces sp. YBE-316 gradually increased after 60 hours, and was maximum after 100 hours after inoculation in growth medium (2.0% sucrose, 1.0% soybean meal, 0.1% K$_{2}$HPO$_{4}$, pH 7.0) at 30$\circ$C, 150 rpm, 5 NL/min by 30 l jar fermentor. This antitumor antibiotic was present only in mycelium, and stable in pH 5.0-10.0 for 20 minutes at 100$\circ$C. Antitumor and antibiotic activities were maintained at neutral pH, and heat stability was low. This antitumor antibiotic was soluble in methanol and ethanol, and insoluble in water, ethyl acetate, chloroform, and n-hexane. This antitumor antibiotic was sequentially purified by acetone extraction from mycelium, butanol extraction, and silica gel column chromatography. Antitumor activity was low against most tested cell lines, but antibiotic activity was high and low against yeasts and bacteria, respectivelv. The visualization test showed that this antitumor antibiotic had higher hydroxyl, ketone, amino, carboxyl groups, and sugar(s) in its structure. Instrumental analyses showed that this antitumor antibiotic was a pentaene in polyene class antibiotics. In pentaene class antibiotics, this was considered as an eurocidin or capacidin type antibiotics. The molecular weight of this antitumor antibiotic was higher than 683.0 daltons, and this antitumor antibiotic might be glycosylated by other sugar(s), instead of mycosamine or perosamine, an amino sugar.

• YAKHAK HOEJI
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• v.44 no.4
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• pp.347-353
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• 2000

To examine influence of artificial digestive juice on the antitumor activity of Ganoderma lucidum-A(GL-A), protein-bound polysaccharide from Ganoderma lucidum, we compared the digested protein-bound polysaccharide with undigested one both on immunopotentiating activity and influence of digestive juices. Protein-bound polysaccharide GL-B was obtained by digesting the antitumor component GL-A with artificial digestive Juices in vitro. When GL-A was administered orally to sarcoma 180 tumor-bearing ICR mice, the life prolonging effect was exhibited in a dose dependent manner Not only GL-A but GL-B increased the production of colony forming unit (CFU) to 10- and 8-fold of that of the control, respectively. Both of the protein-bound polysaccharides also showed the secretion of nitric oxide in RAW 264.7 cell lines to 3.5-and 3.7-fold of that of the control, respectively: GL-A activated components of the alternative complement pathway, whereas GL-B did not. In humoral immunity GL-A increased the activity of alkaline phosphatase in differentiated B cells to 3 times and GL-B to 4 times of that of the control. These results showed that the artificial digestive juices had no influence on the antitumor activity of the protein-bound polysaccharide from Ganoderma lucidum and that its immunomodulating activity retained after treatment with artificial digestive juice. And this provides a basis of the protein-bound polysaccharide of Ganoderma lucidum as an peroral anticancer drug.

• Journal of Ginseng Research
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• v.46 no.6
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• pp.738-749
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• 2022

Background: Ginseng possesses antitumor effects, and ginsenosides are considered to be one of its main active chemical components. Ginsenosides can further be hydrolyzed to generate secondary saponins, and 20(R)-panaxotriol is an important sapogenin of ginsenosides. We aimed to synthesize a new ginsengenin derivative from 20(R)-panaxotriol and investigate its antitumor activity in vivo and in vitro. Methods: Here, 20(R)-panaxotriol was selected as a precursor and was modified into its derivatives. The new products were characterized by ¹H-NMR, ¹³C-NMR and HR-MS and evaluated by molecular docking, MTT, luciferase reporter assay, western blotting, immunofluorescent staining, colony formation assay, EdU labeling and immunofluorescence, apoptosis assay, cells migration assay, transwell assay and in vivo antitumor activity assay. Results: The derivative with the best antitumor activity was identified as 6,12-dihydroxy-4,4,8,10,14-pentamethyl-17-(2,6,6-trimethyltetrahydro-2H-pyran-2-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl(tert-butoxycarbonyl)glycinate (A11). The focus of this research was on the antitumor activity of the derivatives. The efficacy of the derivative A11 (IC₅₀ < 0.3 µM) was more than 100 times higher than that of 20(R)- panaxotriol (IC₅₀ > 30 µM). In addition, A11 inhibited the protein expression and nuclear accumulation of the hypoxia-inducible factor HIF-1α in HeLa cells under hypoxic conditions in a dose-dependent manner. Moreover, A11 dose-dependently inhibited the proliferation, migration, and invasion of HeLa cells, while promoting their apoptosis. Notably, the inhibition by A11 was more significant than that by 20(R)-panaxotriol (p < 0.01) in vivo. Conclusion: To our knowledge, this is the first study to report the production of derivative A11 from 20(R)-panaxotriol and its superior antitumor activity compared to its precursor. Moreover, derivative A11 can be used to further study and develop novel antitumor drugs.

• Journal of Microbiology and Biotechnology
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• v.12 no.3
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• pp.503-507
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• 2002

Chitosan oligosaccharides (COSs) were prepared and fractionated into three groups of COS [a high molecular weight COS (HMWCOS), medium molecular weight COS (LMWCOS), and low molecular weight COS (LMWCOS)] according to their molecular weight, using an ultrafiltration membrane enzymatic bioreactor designed earlier [8]. Antitumor activity of these COSs was then examined against Sarcoma 180 solid (S180) or Uterine cervix carcinoma No. 14 (Ul4) tumor cell-bearing mice. Among these COSs, MMWCOS with molecular weight range from 1.5 to 5.5 kDa effectively inhibited the growth of both tumor cells in the mice. In addition, the administration of MMWCOS resulted in increased thymus weight among lymphoid organs. The mice treated with MMWCOS showed improved survival rate and larger number of survivors after 40 days of feeding. The most effective of MMWCOS far antitumor activity in the S180- or U14-bearing mice was 20 mg/kg/day or more.

• Archives of Pharmacal Research
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• v.21 no.2
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• pp.193-197
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• 1998

A number of substituted isoquinolin-1-ones, possible bioisosteres of the 5-aryl substituted 2,3-dihydroimidazo[2,$1-a$]isoquinolines, were synthesized and tested for their antitumor activity against five different human tumor cell lines. O-(3-hydroxyporpyl) substituted compound (15) exhibited the best antitumor activity which is 3-5 times better than 5-[$4^1$-(piperidinomethyl)phenyl]-2,3-dihydroimidazo[2,$1-a$]isoquinoline (1).

• Korean Journal of Pharmacognosy
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• v.35 no.3 s.138
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• pp.199-202
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• 2004

A highly potent antitumor sesquiterpene O-naphthoquionone has been isolated from Ulmus davidiana, which has been traditionally used as the folk medicine. The structure of this compound was established on the basis of spectral data obtained from UV, IR, MS, and NMR spectrometry, and determined as mansonone E. This compound showed potent antitumor activity on in vivo assay, hollow fiber and xenograft assay.