• YAKHAK HOEJI
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• v.44 no.6
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• pp.601-606
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• 2000

Recently, studies on missile antitumor drugs, which selectively act on tumor cell and display drug effects, have been performed. These missile antitumor drugs which can increase drug effects and decrease side effects, are ideal medication method. Lectin has been reported as tumor cell specific binding protein and tannin as antitumor substance. In this study, we studied inhibition of melanoma metastasis by lectin-conjugated ellagitannin and used praecoxin A as ellagitannin source. Mouse melanoma cell, B16-F10, was injected into the sole of forefoot of C57BL/6 mouse, and after administration with drug, the number of pulmonary tumor colony was counted. The administration of praecoxin A, lectin-praecoxin A mixiture, and lectin-conjugated praecoxin A was started after amputation of established tumor foci at right forefoot of mice and continued for 3 weeks with i.p. injection of one of those drugs A every 24 hours. Lectin-praecoxin A mixture, and lectin-conjugated praecoxin A significantly reduced the number of spontaneous pulmonary metastasis. Exposure to 5 mg/kg of lectin-praecoxin A mixiture and lectin-conjugated praecoxin A produced a statistically significant 38.3%, 41.8% reduction in the number of remaining pulmonary metastasis. These results suggest that metastasis inhibition by lectin-praecoxin A mixiture and lectin-conjugated praecoxin A are better than that of praecoxin A.

• 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.

• Journal of Pharmaceutical Investigation
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• v.31 no.3
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• pp.197-200
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• 2001

Lectin-conjugated ellagitannin (LET), a newly introduced melanoma-specific antitumor agent which has been synthesized by conjugation of wheat germ agglutinin as a lectin with praecoxin A as an ellagitannin, was encapsulated into sterically stabilized liposomes (SSL). Modified Folin phenol method was established for the quantitation of LET contents in liposomal formulations protein employing the standard calibration curve with bovine serum albumin. After removal of phospholipid by organic solvent extraction, which interferes the specific selectivity of the Folin-Ciocalteu reagent with the protein, recovery of LET was $94.5{\pm}2.3%$ and the encapsulation efficiency was revealed as $37.8{\pm}5.9%$ for 2.5 mg/ml LET solution.

• YAKHAK HOEJI
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• v.46 no.3
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• pp.197-202
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• 2002

Lectin-conjugated praecoxin A, which has developed as a missile antitumor drug, is the one that has conjugated with wheat germ agglutinin (WGA), a kind of carbohydrate-binding protein (lectin) especially bound to melanoma. Praecoxin A is a kind of tannin extracted and purified from plants. Beside this direct antitumor effect as tannins, we have examined an activation of macrophage by lectin-conjugated praecoxin A. We also confirmed the gene expression of IL-1 $\beta$, both in vitro and in vivo. We added 1, 10, 100 $\mu\textrm{g}$/mι of lectin-conjugated praecoxin A, 10 $\mu\textrm{g}$/mι of lectin, 10 $\mu\textrm{g}$/mι of praecoxin A to normal murine macrophage and analyzed the extracted total RNAs by RT-PCR after 4, 8, 12, 24 hours. Our data demonstrated that lectin-conjugated praecoxin A increased IL-1$\beta$, mRNA expression in a dose dependent manner. However, the effectiveness of lectin-conjugated praecoxin A was not superior to lectin and praecoxin A.

• Proceedings of the PSK Conference
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• 2000.10a
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• pp.179.2-179.2
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• 2000

• Proceedings of the PSK Conference
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• 2000.10a
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• pp.180.1-180.1
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• 2000

• Proceedings of the PSK Conference
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• 2000.10a
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• pp.278.1-278.1
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• 2000

• Proceedings of the PSK Conference
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• 2001.04a
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• pp.233.1-233.1
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• 2001

• Proceedings of the PSK Conference
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• 2001.04a
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• pp.167.1-167.1
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• 2001