• 약학회지
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• 제42권5호
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• pp.494-499
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• 1998

As part of a drug discovery program to discover more effective platinum-based anticancer drugs, a series of platinum complexes of 1,2-bis(diphenylphosphino)ethane(1,2-diaminopro pane)platinum(II)dinitrate (KHPC-070) has been evaluated in vitro against various tumor cell lines and normal kidney cells. The structure of this new compound was determined by elemental analysis, infrared spectroscopy (IR) and $^{13}carbon$ nuclear magnetic resonance (NMR). With the use of nine tumor cell lines, KHPC-070 exhibited a comparable cytotoxic to cisplatin. The cytotoxicity of KHPC-070 in normal cells was quite less than that of cisplatin using 3-(4.5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) and [$^3H$]-thymidine uptake tests in rabbit renal proximal tubular cells and human renal cortical cells. Based on these results, KHPC-070 is considered to have more selective cytotoxicity toward cancer cells than normal human/rabbit kidney cells.

• 약학회지
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• 제36권4호
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• pp.326-333
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• 1992

A new series of methotrexate analogues was prepared in which the ${\beta}-position$ of the glutamic acid moiety is substituted by the aryl groups. The glutamic acid moiety was modified in order to enhance the lipophilic property. Reaction of N-acetylglicine ester[1] with ethyl 3-arylacrylate derivatives[2] produced trans-3-aryl-2-carboxy-5-pyrrolidone derivatives[3], which were hydrolyzed to give ${\beta}-aryl-glutamic$ acid derivatives[4]. The compounds[4] were treated with the p-aminobenzoic acid moiety and then with the pteridine ring moiety to give ${\beta}-arylmethotrexate$ derivatives[6,7]. These compounds were tested for antibacterial activity against Streptococcus faecium and for antitumor activity against murine leukemias and against human tumor cell lines in vitro. Several compounds showed significant antibacterial activity.

• 한국자원식물학회지
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• 제31권4호
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• pp.342-354
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• 2018

Suaeda japonica is a halophytic plant that lives in mudflat at intertidal zone of western and southern coastal areas of Korea. The seawater-living plants showed a purple color during their whole life. In contrast, freshwater-living plants displayed a green color in leaves. When seawater-living plants were transferred to potting soil, the purple color was gradually changed to green in the leaves. The extracted purple pigment compound exhibited typical characteristics of betacyanin that were represented by water solubility, pH- and temperature-dependent color changes, sensitivity to light, UV-Vis spectra, and gel electrophoretic migration pattern. The LC-MS analysis of the extracted pigment compound showed the presence of two major protonated molecular ions ($[M+H]^+$) at m/z 651.1 and m/z 827.1. Antioxidant activity of the pigment compound was determined using stable free radical DPPH assay. It was found to have an antioxidant activity that is linearly increased in proportion to the reaction time for up to 30 min, and the activity was comparable to that of control BHA at 9.0 mg/ml. The anticancer activity against several tumor cell lines was also examined following the MTT assay. The significant growth inhibitory effect was observed on two tumor cell lines, SW-156 (human kidney carcinoma) and HEC-1B (human endometrial adenocarcinoma). Probably, the pigment compound may function as an osmolyte to uphold halotolerant physiological processes in saline environment.

• Molecules and Cells
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• 제28권6호
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• pp.521-527
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• 2009

Previously, we have reported tissue- and stage-specific expression of miR-372 in human embryonic stem cells and so far, not many reports speculate the function of this microRNA (miRNA). In this study, we screened various human cancer cell lines including gastric cancer cell lines and found first time that miR-372 is expressed only in AGS human gastric adenocarcinoma cell line. Inhibition of miR-372 using antisense miR-372 oligonucleotide (AS-miR-372) suppressed proliferation, arrested the cell cycle at G2/M phase, and increased apoptosis of AGS cells. Furthermore, AS-miR-372 treatment increased expression of LATS2, while over-expression of miR-372 decreased luciferase reporter activity driven by the 3' untranslated region (3' UTR) of LATS2 mRNA. Over-expression of LATS2 induced changes in AGS cells similar to those in AGS cells treated with AS-miR-372. Taken together, these findings demonstrate an oncogenic role for miR-372 in controlling cell growth, cell cycle, and apoptosis through down-regulation of a tumor suppressor gene, LATS2.

• Molecules and Cells
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• 제26권5호
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• pp.514-516
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• 2008

The cancer stem cell hypothesis posits that tumor growth is driven by a rare subpopulation of cells, designated cancer stem cells (CSC). Studies supporting this theory are based in large part on xenotransplantation experiments wherein human cancer cells are grown in immunocompromised mice and only CSC, often constituting less than 1% of the malignancy, generate tumors. Herein, we show that all colonies derived from randomly chosen single cells in mouse lung and breast cancer cell lines form tumors following allografting histocompatible mice. Our study suggests that the majority of malignant cells rather than CSC can sustain tumors and that the cancer stem cell theory must be reevaluated.

• Archives of Pharmacal Research
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• 제28권3호
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• pp.280-284
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• 2005

The chromatographic separation of the MeOH extract from the aerial parts of Syneilesis palmata led to the isolation of a new sesquiterpene glycoside 4, together with four known compounds. Their structures were characterized to be 4$\beta$,5$\beta$-epoxy-caryophill-8,(15)-ene (1), 3$\beta$­hydroxy-gultin-5-ene (2), 4$\alpha$,5$\beta$-dihydroxy-caryophill-8,(15)-ene (3), (-)-oplopan-4-one-10-$\alpha$-O­$\beta$-D-glucose (4) and 3-hexenyl-1-O-$\beta$-D-glucopyranose (5), based on spectroscopic and chemical methods. Compound 2 showed moderate cytotoxicity against five human tumor cell lines in vitro with its EDso values ranging from 5.90-1 0.83 $\mu$g/mL.

• Biomolecules & Therapeutics
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• 제23권5호
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• pp.428-433
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• 2015

Acetylshikonin, a natural naphthoquinone derivative compound, has been used for treatment of inflammation and cancer. In the present study, we have investigated whether acetylshikonin could regulate the NF-${\kappa}B$ signaling pathway, thereby leading to suppression of tumorigenesis. We observed that acetylshikonin significantly reduced proliferation of several cancer cell lines, including human pancreatic PANC-1 cancer cells. In addition, acetylshikonin inhibited phorbol 12-myristate 13-acetate (PMA) or tumor necrosis-${\alpha}$ (TNF-${\alpha}$)-induced NF-${\kappa}B$ reporter activity. Proteome cytokine array and real-time RT-PCR results illustrated that acetylshikonin inhibition of PMA-induced production of cytokines was mediated at the transcriptional level and it was associated with suppression of NF-${\kappa}B$ activity and matrix metalloprotenases. Finally, we observed that an exposure of acetylshikonin significantly inhibited the anchorage-independent growth of PANC-1 cells. Together, our results indicate that acetylshikonin could serve as a promising therapeutic agent for future treatment of pancreatic cancer.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.190.1-190.1
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• 2003

A bioassay-guided fractionation of the stem bark extract of Eucommia ulmoides Oliver (Eucommiaceae) led to the isolation of three iridoid constituents, genipin (1), geniposide (3), geniposidic acid (4) as well as (${\pm}$)-guaiacylglycerol (2) and fatty acid mixtures as active ingredients of the extract responsible for the antitumoral property. The EtOAc soluble part and BuOH soluble part of the extract demonstrated a significant inhibition on the proliferation of cultured human tumor cells such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system) and HCT-15 (colon) in vitro, whereas the remaining water soluble part exhibited a poor inhibition. (omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.202.2-202.2
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• 2003

A bioassay-guided fractionation of the whole extract of Viscum album (a parasitic plant : Loranthaceae) led to the isolation of two triterpenoidal components, oleanolic acid (1), ${\beta}$-amyrin acetate (2), homoflavoyadorinin B (3) as well as large quantity of free fatty acid mixtures as active ingredients of the extract responsible for the antitumoral property. The EtOAc soluble part and BuOH soluble part of the extract demonstrated a significant inhibition on the proliferation of cultured human tumor cells such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system) and HCT-15 (colon) in vitro, whereas the remaining water soluble part exhibited a poor inhibition. (omitted)

• 대한수의학회지
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• 제33권4호
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• pp.701-710
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• 1993

The pine needles, Pinus densiflow Sieb. et Zucc., which is a feed for goats showing a low incidence rate of cancer were evaluated to confirm the potent anticancer effects, with or without several conventional anticancer drugs. The pine needles collected from Mt. Buk-Han located near Seoul were extracted with 95% methanol and methand and concentrated. From the methanol extract, SOM-A, was extracted dichlormethane and SOM-B was extracted with ethyl acetate. SOM-C was extracted with distilled water. These extracts were tested for their antitumor activities in vitro and in vivo. Among them, SOM-A and SOM-C exhibited potent antitumor activities described as belows. 1. The cytotoxic effects of SOM-A and SOM-C were examined against in vitro cultured murine and humman tumor cells. SOM-A showed strong cytotoxicity against human tumor cell lines and SOM-C showed strong cytotoxicity against murine tumor cell lines tested. 2. The antitumor effects of SOM-A and SOM-C were examined against P388 and L1210 of mouse ascitic tumors. The highest mean survival time(MST) ration was 151%(P388) for SOM-C(90mg/kg). 3. To compare the antitumor effects of SOM-A, SOM-B, and SOM-C against solid tumors, S-180 and Ehrlich carcinoma were implanted subcutaneously to mice on Day O. The drugs were given intraperitoneally to mice once a day on Days 1-20, and the tumor weights were measured on Day 21. SOM-A showed inhibition of tumor growth more than 50% in the experiment on S-180 and Ehrlich, and SOM-C also markedly inhibited tumor growth. However, SOM-B had no effect. 4. SOM-C combined with ${\alpha}$-interferon and SOM-C combined with Mitomycin-C enhanced the antitumor activities against murine ascitic tumors P388 leukemia.