• Mycobiology
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• 제46권4호
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• pp.448-451
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• 2018

Fungal perylenequinones have photodynamic activity and are promising photosensitizers for photodynamic therapy (PDT). Here, we investigated the bactericidal and antitumor activities of phleichrome from the fungal perylenequinone family in vitro. Photodynamic bactericidal activity of phleichrome was analyzed by agar-well diffusion method under dark and illuminated conditions. The photodynamic antitumor activity of phleichrome was analyzed in MCF-7, HeLa, SW480, and HepG2 human cancer cell lines using in vitro cytotoxicity assays. Photodynamic bactericidal activities against Gram-negative and Gram-positive bacteria were species-specific. Antitumor activity against all tumor cell lines increased under the illuminated condition. Depending on the results of the analyses, Phleichrome has potential for further drug development related to its antibacterial and antitumor activities.

• Journal of Nutrition and Health
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• 제26권4호
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• pp.379-389
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• 1993

Several studies have shown that extracts from yellow-green vegetables reveal antitumor activities. In the present study we investigated the effect of phytol in order to elucidate the immunological mechanism of antitumor activity of this substance. The results obtained from the experiment as follows: 1) Phytol showed cytotoxic effect on sarcoma 180 cells in vitro. 2) When phytol was injected into the peritoneal cavity of mice transplanted with sarcoma 180 cells, the average survival time (24.0 days) tended to increase as compared with the nontreated control (19.2 days). 3) When sarcoma 180 cells were injected subcutaneously into the right groin of mice, and then phytol was injected into the peritoneal cavity, the tumor inhibition ratio was 33%. 4) The natural killer(NK) cell activity was significantly augmented by phytol in vitro and in vivo. Similar augmentations of NK cell activity were obtained with culture supernatants of phytol exposed spleen cells and peripheral blood mononuiclear cells. 5) Phytol on the macrophage from peritoneal cavity showed a higher effectiveness in vivo than in vitro. These results indicate that phytol shows the inhibitory effect for growth of sarcoma 180 cells in vitro, also it can augment macrophage and NK cell activities in vivo.

• 약학회지
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• 제44권5호
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• pp.463-469
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• 2000

Protein-polysaccharide fractions separated from nine Korean wild mushrooms were subjected to an in vitro screening test for lymphoblastogenic activity. Of these, PPLP, the protein-polysaccharide fraction of Lycoperdon pedicellatum, showed the most potent activity and were further investigated for its antitumor activity. When intraperitoneally injected into ICR mice once daily for six days at a dose of 30 mg/kg, PPLP strongly inhibited the growth of sarcoma 180 tumor cells, showing the inhibition ratio of 97.6%. PPLP also showed in vitro inhibitory activity on sarcoma 180 or leukemia L1210 at the concentration of 500 $\mu\textrm{g}$/$m\ell$ or higher. These results strongly suggest that PPLP might exert its antitumor activity through immunostimulation as well as inhibitory activity on the tumor cells.

• 약학회지
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• 제49권1호
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• pp.60-67
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• 2005

Nonclassical aminobenz[cd]indole antifolates 4, 5 and 6, in which the glutamic acid moiety of the classical antifolates is substituted by 2-phenylglycinamide or 3-aminobenzamide, were synthesized and their in vitro antitumor activity was evaluated. The purpose of this substitution is that the lipophilicity is enhanced due to the aromatic ring of the target compounds for the passive transport through lipid membrane of cells while the hydrogen bonding of the amide is retained in the active site of the enzyme, thymidylate synthase, where the glutamate is originally present. The target compounds were highly cytotoxic against tumor cell lines of murine and human origin with micromolar to nanomolar $IC_{50}$ values. Most effective was compound 4 ($N^6-methyl-N^6$-[4-[(${\alpha}$(S)-aminocarbonylbenzyl) aminocarbonyl]benzyl]-2,6-diaminobenz[cd]indole)with $IC_{50}$ of 2 nM against SW480, human colon adenocarcinoma cell line, which is 650-fold more potent than the reference compound 3.

• Archives of Pharmacal Research
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• 제25권4호
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• pp.457-462
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• 2002

Oregonin, a diarylheptanoid derivative from Alnus hirsuta Turcz, Betulaceae, was evaluated for its antitumor activity. Oregonin, known to have an antitumor function, and is a novel immunomodulator, which may augment macrophage activity. MTT assays and NO production tests were performed in order to investigate the cytotoxicity of oregonin in tumor cells and to examine its influence on macrophage in detail. In this study, the tumoricidal activity was also evaluated by a MTT assay. The cytotoxicity measurements in the oregon in-treated group both in vitro and in vivo showed a significant difference from that of the control group. In vivo, oregonin significantly increased NO production in a dose-dependent manner, and in vitro, the thioglycolate-induced inflammatory macrophages increased NO production in a dose-dependent manner after incubation. These results suggest that oregonin reacts with both the inflammatory and non-inflammatory macrophages in a similar way.

• Biomolecules & Therapeutics
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• 제9권3호
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• pp.143-155
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• 2001

Many attention has been focused on developing new chemotherapeutic agents for a treatment of cancer from natural products. From Carpesium divaricatum S. et Z. (Compositae), various monoterpenoid compounds were isolated and exhibited mild antitumor activity against human tumor cell lines. These facts prompted us to explore the structure-activity relationship of these compounds. The synthesis of monoterpenoid compound was accomplished by Fries rearrangement, Grignard reaction, elimination, allylic oxidation, esterification and epoxidation as key steps. The results of in vitro cytotoxicity (A549, SK-OV-3, SK-MEL-2, XF498, HCT15) of the synthesised compounds are as follows: First of all, epoxide moiety is prerequisite for cytotoxic activity in diester compound. Any kind of compounds with olefin or diol moiety instead of epoxide ring exhibited poor or mild cytotoxic activity respectively. Of o-acetoxy and isobutoxy epoxy esters, p-sub-stituted phenylacetate compounds exhibited high cytotoxic activities against SK-MEL-2 and HCT15.

• 약학회지
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• 제50권4호
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• pp.278-286
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• 2006

Classical dihydropyrrole[3,4-f]quinazoline antifolates 7,8 and 9, in which the tricyclic ring is structurally similar to the pteridine ring of $CH_2-THF(1)$, the cofactor of thymidylate synthase (TS), were synthesized, and their in vitro antitumor activity was evaluated by measuring the cell growth inhibitory activity against cancer cell lines. The target compounds were cytotoxic against CCRF-CEM, human T-cell acute lymphoblastic leukemia, with the cell growth inhibitory activity $(IC_{50})$ of $0.8{\sim}8.3\;{\mu}M$. Among the three compounds, 3-amino analog 7 was 10- and 3.5-fold more cytotoxic compared to the 3-methyl analogs 8 and 9, and its cytotoxicity was similar to that of the reference compound with the $IC_{50}$ value of $0.83\;{\mu}M$. This result was supposed as the consequence of the fact that dihydropyrroloquinazolinone ring with amino group was able to bind well in the active site of TS. In the case of 3-methyl analogs, analog 9, which has two-carbon bridge between the dihydropyrroloquinazolinone ring and benzoyl-L-glutamic acid, was 3-times more potent in cytotoxicity than analog 8 which has one-carbon bridge, and this result indicates that the distance and conformational orientation of the benzoyl-L-glutamic acid moiety with respect to the tricyclic ring may also be a crucial determinant of cell growth inhibitory activity.

• 동의생리병리학회지
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• 제19권4호
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• pp.1011-1015
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• 2005

Antitumor and anti-metastatic effects of mineral powder(MP) were studied. In the present study, MP did not exhibit the any cytotoxic activity against leukemic cells such as L1210 and U937 tumor cell lines in vitro. Also, MP did not exhibit the any cytotoxic activity against solid cells such as A549 and B16-BL6 tumor cell lines in vitro. However, in vivo, MP exhibit a significant antitumor activity in BDF1 mice bearing Lewis lung carcinoma cells(LLC) with inhibition rates of 46 and $23\%$ at 200 and 100 mg/kg/day, respectively. Furthermore, in pulmonary colonization assay, MP exhibit the inhibitory effect of tumor metastasis. From these results, it was concluded that MP had antitumor and anti-metastatic activity suggesting its application for the prevention and treatment of cancer.

• Asian Pacific Journal of Cancer Prevention
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• 제15권3호
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• pp.1163-1169
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• 2014

Astragalus, a commonly used traditional Chinese medicine, has exhibited antitumor actions in patients. In this study, in vitro and in vivo antitumor effects of astragalus and synergistic antitumor efficacy in combination with pterostilbene were investigated. Melanoma cells were treated with pterostilbene (Pt), graduated doses of astragalus injection (AI), or these in combination. Cell viability was measured using a MTT assay. Released nucleosomes and caspase activity were measured using enzyme-linked immunosorbent assay. Growth inhibition in vitro and in vivo was also assessed. Analysis of variance and t tests were used for statistical analysis. Significant reduction (p<0.05) in cellular proliferation were observed with AI and AI-Pt in a time- and concentration-dependent manner. Apoptosis and caspase-3/7 activity were significantly increased by AI and AI-Pt treatment (p<0.05). In vivo, AI inhibited melanoma tumor growth, with inhibition rates ranging from 36.5 to 62.3%, by inducing apoptosis via up-regulation Bax expression and the Bax/Bcl-2 ratio and down-regulating Bcl-2 expression. AI significantly inhibits the growth of melanoma in vitro and in vivo by inducing apoptosis. These data suggest that combined treatment of astragalus with pterostilbene enhances antitumor efficacy.

• 약학회지
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• 제49권1호
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• pp.68-73
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• 2005

Epi-xanthatin analogs containing hydrophilic substituents such as carboxylic acid, alcohol, morpholine, amino acid, and glucose derivatives were synthesized and their in vitro cytotoxicity and in vivo antitumor activity were evaluated. The target compounds were generally cytotoxic against tumor cell lines of human origin with $ED_{50}$ values of $0.1{\sim}30{\mu}g/ml$, except the highly hydrophilic analog 6 containing aspartic acid. Contrary to the potent cytotoxicity weakly hydrophilic analogs 2 and 8 were not active in vivo, or even toxic to the test animals. As a result, hydrophilic analog of epi-xanthatin did not show in vitro cytotoxicity and hydrophobic analogs did not show in vivo antitumor activity, thus it is presumed that amphiphilic analogs or those with medium hydrophilicity would exhibit the antitumor potency in vivo.