• Archives of Pharmacal Research
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• 제19권1호
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• pp.77-78
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• 1996

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 1993년도 천연항암자원의 개발에 관한 국제학술회의
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• pp.14-20
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• 1993

We in anticancer drug development from natural resources have conceived and used a wide variety of experimental screening systems to support our efforts during the past 20 tears. Screens have been devided to address targets at the molecular, biochemical and cellular levels, both in vivo and in vitro. Screens have been essential for the experimental evaluation of the products from natural sources. In this congress, antitumor screening methods for deveol[ment of new drugs from natural sources and evaluation of their crude drugs are discussed.

• 약학회지
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• 제14권3_4호
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• pp.51-53
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• 1970

Alcohol extracts of six plant namely Coix agrestis L$_{OUREIRO}$, Chloranthus Japonicus (Siebi) N$_{AKAI}$, Ajuga Spectabilis N$_{AKAI}$, Juglans mandsuria Max., Cirsium Macki var Ussuriense $K_{ITA}$ and Sasamorpha Purpurascense (Hack) N$_{AKAI}$ were subjected to the screening tests for anti-tumor activities against SN-36 Leukemia, Sarcoma 180 and Ehrlich ascites carcinoma. Of the six extracts, Ajuga Spectabilis N$_{AKAI}$ and Coix agrestis L$_{OUREIRO}$ were found to be potential in survival effect of tumor transplanted mice.

• 생약학회지
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• 제13권2호
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• pp.62-69
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• 1982

Fiftythree species(35 families and 52 genera)of Korean medicinal plants which have been frequently used in oriental herb prescriptions or have been used as folklorics were evaluated on their short term acute toxicity and potential antitumor activities against P-388 murine lymphocytic leukemia model in vivo. Among these plants Acorus gramineus (Araceae), Agrimonia pilosa (Rosaceae), Aralia elata (Araliaceae), Dryopteris crassirhizoma (Aspidiaceae), Syringa reticulata (Oleaceae) and Calystegia japonica (Convolvulaceae) exhibited potent acute toxicity resulting from severe weight loss and death. Agrimonia pilosa (Rosaceae) showed about 33% of increased life span in comparison with that of control group mouse, but others exhibited no significant antitumor activities.

• Archives of Pharmacal Research
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• 제18권6호
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• pp.462-463
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• 1995

• Journal of Ginseng Research
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• 제46권6호
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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.

• 동의생리병리학회지
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• 제19권2호
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• pp.441-445
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• 2005

Tripterygium regelii has been used as an oriental medicine, especially antiparasitic, anti-inflammatory and detoxifying agents in East asia. During our research to develop new antitumor agents from natural products, MeOH ext. and CH2Cl2 ext. of Tripterygium regelii showed the potent antitumor activity. In order to purify active compounds from Tripterygium regelii, activity-guided fractionation was carried out. Silica gel and RP-18 column chromatography for the active fraction led to the isolation of two compounds and their antitumor activities were studied. Those two compounds didn't show potent antitumor activity against human tumor cell lines. The structure of two compounds were determined by $^1H-NMR$, $^{13}C-NMR$, DEPT, $^1H-^{13}C$ COSY and IR spectrum. Compound I and Compound II were turned out to be Celastrol, and ${\beta}-sitosteryl-3-o-{\beta}-D-glucopyranoside$ respectively.

• Natural Product Sciences
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• 제26권2호
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• pp.109-117
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• 2020

The canonical Wnt/β-catenin signaling pathways play an important role in the embryonic development, cell proliferation, differentiation, and adhesion. Therefore, the abnormal activation and repression have been associated with uncontrolled homeostasis in human tissues. In particular, the activation of Wnt signaling is highly correlated with a diverse of diseases including cancer. On this regard, a strategy for targeting Wnt/β-catenin signaling has been employed in the discovery and development of antitumor agents. Herein, the evolution of Wnt signaling and the Wnt inhibitors derived from natural products were briefly summarized in the drug discovery of anticancer agents.

• 생약학회지
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• 제13권2호
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• pp.55-61
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• 1982

Thirtyfour species of Korean medicinal plants which have been frequently used in oriental herb prescriptions were evaluated on their cytotoxicity and potential antitumor activities against AC glioma(9 ASK) in vitro. Dose of $100{\mu}g/ml$ of plant extracts appeared to exhibit slight cytotoxicity. Seven plant extracts, Aralia continentalis(Araliaceae), Lycium chinensis(Solanaceae), Epimedium koreanum(Berberidaceae), Platyodon grandiflorium(Campanulaceae), Pleuropterus multiflorus(Polygonaceae), Rheum undulatun(Polygonaceae) and Scutellaria baicalensis(Laminaceae), exhibited significant reversal$(51{\sim}90%)$ of astrocyte formation into original neuroglial cells' morphology through the prescreen tests.

• Archives of Pharmacal Research
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• 제17권5호
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• pp.337-342
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• 1994

Carbohydrate analysis is important in studying structure and activity of complex polysaccharides. New analytical method was applied to get an information on the composition of polysaccharides showing antitumor activity. Monosaccharides were labeled with 7-amino-1, 3-naph-thalenedisulfonic acid (7-AGA) by reductive amination and separated by HPLC. Five kinds of polysaccharides from Basidiomycetes were hydrolyzed and analyzed in combination with electrophresis and HPLC. At the same time, alditol acetate derivatives were prepared and analyzed by gas chromatography. Two different techniques using different derivatization methods showed very similar results. The monosaccharides from Coriolus versicolor and Cordyceps militaris were glucose and galactose. Phellinus linteus composed of glucose, glactose, mannose, arabinose and fucose. The HPLC method with fluorescence detector was very sensitive compared to other methods.