• Archives of Pharmacal Research
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• v.24 no.4
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• pp.323-326
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• 2001

Previous studies have demonstrated that CW252053, a quinazoline antifolate, exhibits potent inhibitory activity against thymidylate synthase (TS) as well as cytotoxic activity against tumor cell lines in vitro. In this studys, we evaluated the in vivo antitumor efficacy of CW252053 in the mouse tumor model. Female B6D2F$_1$ mice were injected with LY3.7. 2C TK-/- (thymidine kinase deficient mouse Iymphoma) cells into the gastrocnemius muscle. Then, CW252053 was administered twice daily by intraperitoneal injection for 10 days, and tumor growth was monitored daily by leg diameter measurement. All animals in the vehicle, 5-FU, and low dose (30mgmg/kg CW252053 treated groups died between days 12 and 23 because of the tumor burden. In contrast, dosing with 60 mg/kg of CW252053 produced a cure rat against tumor growth of 37.5% and a survival rate of 50%. Even more significantly, a higher dose of CW252053 (120 mg/kg) elicited both a 100% cure rate and a 100% survival rate at the termination of the study, confirming that this compound has very potent in vivo antitumor activity against tumor growth. During the experimental period of this study no signs of toxicity were observed even at the high CW252053 dosage rate of 120 mg/kg.

• The Journal of the Korean dental association
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• v.14 no.3
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• pp.297-305
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• 1976

신생의 Balb/C strain 백서20두를 사용하였고, 실험군과 대조군으로 구분하여 실험군에는 5-fluorouracil의 체중 25 mg/kg씩 2회를 복강내주사하였다. 실험군가 대조군에 모두 희생 2시간전에 체중그람당 5μ Ci의 thymidine-H³ (Specific activity는 9.0 Ci/mM 이상)를 복강내 주사하였다. 각군은 5-fluorouracil 최종 주사후 1, 3, 7, 14, 21일 간격으로 희생시키고, 두부를 4% formalin에 고정하였다. 조직을 0.5M EDTA에 탈회하고 parlodion과 paraplast에 이중 매몰을 하여 Parasagittal serial section 을 10μ의 절편을 만든 후 자기방사용표본을 제작하였다. 그 결과는 다음과 같다. 1. 5-fluorouracil이 백서설의 기저세포층의 핵산합성 및 단백합성에 미치는 영향은 실험초일인 제 1일부터 억제하기 시작하여 (80.9%) 제3일 76.9%이고, 제 7일이 가장 극심하고 (66.2%) 그후부터는 다소회복되기 시작하여 제14일이 92/3%이고, 제21일인 98.9%로서 서의 대조군수치에 접근하였다. 2. 5-fluorouracil은 설유두중 nallate papillae 성장에 가장 억제적 현상을 보였고, 그 다음이 fungiform papillae, filiform papillae의 순위였다. 3. 5-fluorouracil 이 백서설의 기저세포층의 핵산합성을 억제함을 알 수 있고, 아울러 백서설의 조기정상 발육에 영향을 줌울 알 수 있다.

• The Journal of the Korean dental association
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• v.14 no.3
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• pp.285-295
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• 1976

항암 화학요법제의 하나인 5-Fluorouracil 이 과상돌기의 성장에 미치는 영향을 연구하기 위하여 20두의 백서를 반씩 나누어 실험군에는 동약물을 체중 kg당 25mg씩 2일간 복강내주사하고 대조군에는 생리식 염수를 주사한 후 각각 제1,3,7,14 및 21일에 두 마리씩 도살하여 과상골디연골부의 조직학적 변화를 관찰하였다. 또한 도살 2시간 전에 5μCi/kg mM 의 ³H-thymidine을 주사하여 표본의 일부는 자기방사법적으로 처리 관찰 하였다. 관찰 결과는 다음과 같다. 1. 과상돌기 연골부의 후경에 상당한 감소가 일어났으며 제7일에서 가장 현저하였다. 2. 이러한 영향은 연골제거대와 세포증식대에서 가장크고 그 다음이 비대층이었다. 3. 제 7일의 변화 증식대엣는 기질 호 염색성의 증가, 핵 형태의 난원형화가 오고 소와내의 세포수는 1~2개였다. 비태층의 소와는 현저하게 작아지고 기질의 호염기성이 뚜렷하며 세포의 배열은 츹어지고 약간의 핵은 그 배 열이 불규칙하며 숫자고 대조군보다 적었다. 4. 위와같은 변화는 제 14일에서 감소하고 점차 회복적인 조직소견을 보여 제21일에는 성장이 거의 대조군에 근접한 조직상을 보였다. 5. 자기방사법적으로 세포증식대 및 연골제거대에서 세포분열에 대한 억제효과를 관찰한 바 제 7일 에서 가장 시하였고 특히 연골제거대에서 심하였다. 대체적으로 자기방사법적 관찰소견은 조직학적 소견과 일치하였다. 결론적으로 하악골 과상돌기의 성장은 5-Fluorouracil의 영향하에서 세포의 증식 및 분화상태로 보아 일정기간동안 저해되며 제 7일의 극기를 지나 점차 회복되어감을 나타내었다.

• Journal of Microbiology and Biotechnology
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• v.11 no.5
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• pp.876-879
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• 2001

${\gamma}$ -Tubulin is an essential component involved in microtubule nucleation. The present work examined whether the fast proliferation of cancer cells can be retarded by the depletion of ${\gamma}$ -tubulin expression. Two different gastric cancer cell lines and one control cell line were treated with antisence oligonucleotides complementary to the messenger RNA of ${\gamma}$ -tubulin. The$[^3H]$ -thymidine incorporation in the two gastric cancer cell lines, SNU-1 and SNU-216, was dramatically reducd by treatment with the ${\gamma}$ -tubulin antisense oligonucleotides in a dosage-dependent manner. In contrast, the control cell line, NIH/3T3, showed no significant effect from the antisense oligonucleotides even at a high concentration. The ablation of ${\gamma}$ -tubulin expression in the tumor cells resulted in an altered DNA synthesis during mitosis and it decreased the cell progression. Accordingly, the use of antisense oligonucleotides may be an effective way of inhibiting the proliferation of human gastric cancers.

• Natural Product Sciences
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• v.16 no.1
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• pp.20-25
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• 2010

Fourteen compounds were isolated from the n-BuOH fraction of the roots of Aralia cordata (syn. = A. continentalis). Through spectroscopic method, the chemical structures were elucidated as: caffeic acid (1), protocatechuic acid (2), thymidine (3), uridine (4), methyl-$\alpha$-D-fructofuranoside (5), a mixture (3 : 1) of $\beta$-D-fructopyranoside and $\beta$-D-fructofuranoside (6), 1-methyl 1,2,3,4-tetrahydro-$\beta$-carboline-3-carboxylic acid (7), methyl-$\beta$-D-fructofuranoside (8), sucrose (9), 5-caffeoylquinic acid (chlorogenic acid) (10), 3-caffeoylquinic acid (neochlorogenic acid) (11), 4-caffeoylquinic acid (cryptochlorogenic acid) (12), 3,5-di-O-caffeoylquinic acid (13), and 1-kestose [$\beta$-D-fructofuranosyl-($2{\rightarrow}1$)-$\beta$-D-fructofuranosyl-($2{\rightarrow}1$)-$\alpha$-D-glucopyranoside] (14). Among them, compounds 5, 7, 8, and 10 - 14 were isolated from this plant for the first time.

• Biomolecules & Therapeutics
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• v.8 no.3
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• pp.228-234
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• 2000

We have synthesized a novel platinum(II) coordination complex containing trans-ι-1,2-diaminocy-clohexane (DACH) as a carrier ligand and 1,2-dichloroethane (DCE) as a leaving group. A new series of [Pt(trans-ι-DACH)(DCE)](PC) was evaluated for its cytotoxic activity on MKN-45 human gastric adenocar-cinoma cells and normal primary cultured kidney cells. The new platinum complex has demonstrated high efficacy in the cytotoxicity against MKN-45/P, MKN-45/ADM and MKN-45/CDDP cell-lines. The cytotoxicity of PC against rabbit proximal renal tubular cells, human renal cortical cells and human renal cortical tissues, determined by MTT assay, the [$^3H$]-thymidine uptake arid glucose consumption tests, was found to be quite less than those of cisplatin. Based on these results, this novel platinum(II) coordination complex appears to be better for improving antitumor activities with low nephrotoxicity and is a valuable lead in the development of new, clinically available anticancer chemotherapeutic agents.

• Preventive Nutrition and Food Science
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• v.2 no.2
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• pp.167-173
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• 1997

The inhibitory effects of kale juice on the growh and DNA incorporation of human cancer cells, using HT-29 colon cancer cells, MG-63 osteosarcoma cells, AGS gastric adenocarcinoma cells and K-562 leukemia cells, were studied. The growth of human cancer cells were inhibited in the presence of kale juice (10, 20 nd 40$\mu$l/ml) and the effects were the juice concentration- and incubation time-dependent up to 6 days. When 20$\mu$l/ml of kale juice was added to the media of HT-29, MG-63, AGS and K-562 cancer cells, the cell growth after 6 or 4 days of incubation was retarded by 83~95% of control group. Morphological changes of HT-29 colon cancer cells wre studied under inverted microscope. As the concentration of kale juice increased up to 20$\mu$l/ml, degree of cell aggregation was decreased. Moreover, the DNA incorporation o AGS gastric adenocarcinoma cells and MG-63 osteosarcoma cells which were labeled with [$^3$H] thymidine was significantly reduced after 2 days of incubation at 37$^{\circ}C$ with kale juice. Therefore, we concluded that kale juice strongly decreased the growth of various human cancer cells.

• Journal of the Korean Society of Food Science and Nutrition
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• v.26 no.6
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• pp.1194-1199
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• 1997

The effect of hot taste preference on selected immune responses was investigated in human peripheral immunocompetent cells. Human lymphocytes and natural killer(NK) cells were prepared at a concentration of 2$\times$$10^{6}$ cells/ml in RPMI-1640 containing 10% fetal bovine serum. Lymphocytes proliferation was determined with the [$^{3}H$]-thymidine pulse for 18hrs after concanavalin A, phytohemagglutinin, Salmonella typhimurium mitogen, or media alone. NK cell activity was measured by cytolysis of $^51Cr$-labeled target cells K562. Serum antibodies levels such as IgM, IgG, IgA were also measured by ELISA method. There was no difference of serum IgM level among the groups, but IgG and IgA levels were greater in the group with hot taste preference than those of the group without hot taste preference. In lymphocytes of the group with hot taste preference there was a greater mitogen-induced lymphocyte proliferative responses compared to the group without hot taste preference. In addition, NK cell activity in group with hot taste preference was lower than that of the group without hot taste preference. These results suggest that the eating habit of spicy food containing hot components may affect immune status by modulating selective immunocompetent cells function.

• YAKHAK HOEJI
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• v.44 no.5
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• pp.399-405
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• 2000

We have synthesized a novel platinum (II) coordination complex containing trans-ι-1,2-diaminocyclohexane (DACH) as a carrier ligand and 1,2-bis (diphenylphosphino)ethane (DPPE) as a leaving group. In addition, nitrate was added to improve the water-solubility. A new series of [Pt (trans-ι-DACH) (DPPE)].2NO$_3$(PC) was evaluated for its cytotoxic activity on MKN-45 human gastric adenocarcinoma cells and normal primary cultured kidney cells. PC has demonstrated high levels of cytotoxicity against MKN-45/S, MKN-45/ADR and MKN-45/CDDP cells. The cytotoxicity of PC against rabbit proximal renal tubular cells, human renal cortical cells, and human renal cortical tissues, determined using the MTT assaying technique, the ($^3$H)-thymidine uptake and the glucose consumption tests, was found to be quite less than those of cisplatin. Based on these results, this novel platinum (II) coordination complex appears to be better for improving antitumor activities with low nephrotoxicity and is a valuable lead in the development of new clinically available anticancer chemotherapeutic agents.

• Journal of Microbiology and Biotechnology
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• v.29 no.2
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• pp.268-273
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• 2019

The specificity of a Bacillus licheniformis uridine diphosphate (UDP) glycosyltransferase, YjiC, was increased towards thymidine diphosphate (TDP)-sugar by site-directed mutagenesis. The Arg-282 of YjiC was identified and investigated by substituting with Trp. Conversion rate and kinetic parameters were compared between YjiC and its variants with several acceptor substrates such as 7-hydroxyflavone (7-HF), 4',7-dihydroxyisoflavone, 7,8-dihydroxyflavone and curcumin. Molecular docking of TDP-glucose and 7-HF with YjiC model showed pi-alkyl interaction with Arg-282 and His-14, and pi-pi interaction with $His^{14}$ and thymine ring. YjiC (H14A) variant lost its glucosylation activity with TDP-glucose validating significance of His-14 in binding of TDP-sugars.