• Archives of Pharmacal Research
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• v.24 no.3
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• pp.190-193
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• 2001

Various analogues of 5,8-dimethoxy-1,4-naphthoquinone (DMNQ) such as 2- or 6-(1-hydroxyiminoalkyl)-DMNQs were prepared and evaluated for the antitumor action. (1 -Hydroxyiminoalkyl)-DMNQs derivatives expressed greater antitumor action than (1-hydroxyalkyl) - or acyl-DMNQ derivatives. Moreover, 6-(1-hydroxyiminoalkyl)-DMNQ derivatives expressed higher antitumor action than 2-substituted ones, suggestive of a steric effect. Some of 6-(1-propyloxyalkyl)-DMNQ derivatives with an alkyl group of butyl to octyl moiety showed T/C values of >400%

• Archives of Pharmacal Research
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• v.24 no.1
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• pp.35-38
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• 2001

Various analogues of 5,8-dimethoxy-1,4-naphthoquinone (DMNQ) such as 2- or 6-(1-hydro-xyiminoalkyl)-DMNQs were prepared and evaluated for the antitumor action. (1-Hydroxyiminoalkyl)-DMNQ derivatives expressed greater antitumor action than (1 -hydroxyalkyl)- or acyl-DMNQ derivatives. Moreover, 6-(1-hydroxyiminoalkyl)-DMNQ derivatives expressed higher anti-tumor action than 2-sudstituted ones, suggestive of a steric effect. Some of 6-(1-propyloxyalkyl)-DMNQ derivatives with an alkyl group of butyl to octyl moiety showed T/C values of > 400 %.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.56-61
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• 1998

For the screening of bioactive natural products, the benzene or methanol extracts from 93 medicinal plants of Korea were prepared, and tested for the cytotoxicity against L1210 cells and for the antitumor action (Bae et al., 1992 and 1996). Of 93 extracts tested, 6 samples showed a cytotoxicity in both benzene and methanol extract, 39 samples in benzene and 13 samples in methanol extract. The benzene extract of the root of Scutellaria indica L., Sophora fIavescens Solander ex Aiton, Carpesium abrotanoides L., Gymnaster koraiensis (Nakai) Kitamura, Pyrola japonica Klenze, and Forsythiae Fructus showed a potent cytotoxic activity. This observation led to isolate active cytotoxic components, some of which demonstrated some antitumor action. In addition, the structure-activity relationship was discussed.

• Archives of Pharmacal Research
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• v.5 no.2
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• pp.39-43
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• 1982

A protein-polysaccharide fraction was prepared from the carpophores of Laetiporus sulphureus. This fraction suppressed growth of sarcoma 180 in A-strain mice when administered i. p. To investigate the mechanism of antitumor action of this fraction, plaque assay was conducted by administrating i. p. to the mise at a dose level of 50mg/kg for five days. Ten days later, the mice were immunized with 1 * 10$^{7}$ sheep red blooc cells. The number of hemolytic plaque forming cells was significantly greater than that of the control mice. Three monosaccharides and fifteen amino acids were identified in the protein-polysaccharide fraction.

• Journal of Life Science
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• v.7 no.2
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• pp.149-159
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• 1997

Chitin, a linked polysaccharide composed of 2-acetamido-2-deoxy-$\beta$-D-glucopytanose residues, is distributed widely in nature. It has been utilized on various application field due to the development of chitin derivatives such as chitosan, partial deacetylated chitin, carboxylmethyl chitin, sulfated chitin, and so on. Chitin and chitosan have been recently interested in antitumor and antimicrobial activities, because of a powerful tumor inhibitory effect against experimental mouse tumors. Especially, the oligosaccharides obtained by partial degradation of them exhibited a remarkable antitumor effect against sarcoma 180, MM 48 and Meth Asolid tumors and antimetastatic effect against Lewis lung carcinoma in mice. This review describes on antitumor effects of chitin, chitosan and their oligosaccharides by their mechanism of action involving enhancement of immunological system.

• Journal of Ginseng Research
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• v.47 no.1
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• pp.9-22
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• 2023

As a famous herbal medicine in China and Asia, ginseng (Panax ginseng C. A. Meyer) is also known as the "King of All Herbs" and has long been used in medicine and healthcare. In addition to the obvious biological activities of ginsenosides, ginseng polysaccharides (GPs) exhibit excellent antitumor, antioxidant stress, and immunomodulatory effects. In particular, GPs can exert an antitumor effect and is a potential immunomodulator. However, due to the complexity and diversity in the structures and components of GPs, their specific physicochemical properties, and underlying mechanisms remain unclear. In this article, we have summarized the factors influencing the antitumor activity of GPs and their mechanism of action, including the stimulation of the immune system, regulation of the gut microbiota, and direct action on tumor cells

• Archives of Pharmacal Research
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• v.20 no.4
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• pp.368-371
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• 1997

In an effort to increase of the antitumor activity of 2(S)-$2^{I}$,$5^{I}$-trihydroxy-7, 8-dimethoxyflavanone isolated from Scutellaria indica, we synthesized its analogues, II, III and IV. They showed potent cytotoxicity in vitro against cancer cell lines, L1210, K562 and A549. On the basis of $ED_50$ values against the cancer cell lines, III exhibited about 2-7 times stronger activity than I against various cell lines. We tested the antitumor activity of the analogues against Sarcoma 180 cells in vivo and evaluated the structure-activity relationship. The antitumor activity appeared to be related to the hydrogen bond between carbonyl group at C-4 and hydroxyl group at C-5, in contrast to cytotoxic action.

• Journal of Haehwa Medicine
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• v.4 no.1
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• pp.211-223
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• 1995

The antitumor effect of 柴胡(Bupleuri Radix : BP), 茵陳(Artemisiae capillaris Herba; ACH) 및 蒲公英(Taraxaci Herba; TH) and 蒲公英 EE層(Ethyl ether layer of TH; EETH) on human hepatocytes such as Hep G2, PLC and Hep 3B, and synergistic action with the anticancer drugs, that is, mitomycin(MMC), cisplatin(CPT) and 5-fluorouracil(5-FU) were studied by the method of MTT. The results were obtained as follows: 1. $IC_{50}$ against Hep G2, PLC and Hep 3B was $15.5{\mu}g/ml$, $25.4{\mu}g/ml$ and 31.25 in MMC, $92.5{\mu}g/ml$, $50.2{\mu}g/ml$ and $62.5{\mu}g/ml$ in CPT and $125{\mu}g/ml$ in 5-FU respectively. 2. Cytotoxic effect on Hep G2 was obvious in BP-treated group, synergistic action was most effective in TH-treated group or with MMC. 3. Cytotoxic effect on Hep 3B was obvious in ACH-treated group, synergistic action was most effective in ACH-treated group or with MMC. 4. Cytotoxic effect on PLC was obvious in ACH-treated group, synergistic action was most effective in TH-treated group or with MMC. From above results it was concluded that ACH showed the best antitumor effect against PLC and Hep 3B, BP aganst Hep G2 and also synergistic effect was most effective with MMC, which indicates that it is necessary to seperate the antitumor substances in ACH.

• YAKHAK HOEJI
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• v.31 no.2
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• pp.70-81
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• 1987

To elucidate action mechanism of lyophyllan A, an antitumor polysaccharide of Lyophyllum decastes, its immunological activities were examined. Lyophyllan A increased significantly the weights of spleen and liver of mice. Lyophyllan A also restored the decreased thymic weight in tumor-bearing mice. It did not show any direct cytotoxicity against tumor cells, but showed immunopotentiating activities by increasing the number of the plaques in hemolytic plaque assays. Lyophyllan A increased the number of peritoneal exudate cells (PEC) and inhibited the growth of sarcoma 180 mixed with PEC. Moreover the macrophages from lyophyllan A-treated mice exhibited a strong cytotoxic activity towards L5178Y target cells.

• YAKHAK HOEJI
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• v.42 no.3
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• pp.274-274
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• 1998

Aclarubicin(ACL)-entrapped freeze dried liposomes were prepared using Microfludizer to attain a sustained release at targeted organs in a prolonged time so that it can reduce th e side effect and maximize the therapeutic effect. The freeze-dried liposomes were evaluated for pharmacokinetics, antitumor activity against Sarcoma 180, cytotoxicity against L1210 and A549 tumor cells, spleen toxicity and myelosuppressive action. The AUC0->8hr values were 122+/-42, 382+/-140, 419+/-171, 835+/-206 and 443+/-309mcg min/ml for free ACL. ACL-liposome formulation I, II, III and IV, respectively. Cytotoidcity of ACL-entrapped liposomes against L1210 and A549 tumor cells was 2-4 times higher than that of free aclarubicin. ACL-liposome formulation I(PC/CHOL/TA) showed the most potent antitumor activity against Sarcoma 180 in mice. The loss of body weight was much smaller with ACL-entrapped liposomes than free ACL after I.p. injection at a dose of 2 mg/kg/day. Compared to free ACL, ACL-entrapped liposomes expressed a lower and delayed spleen toxicity up to 5th day after I.v. administration. Myelosupperssion seemed to be lower with ACL-entrapped liposome of PC/PC-hydrate/CHOL/TA (formulation III) than free aclarubicin.