• Bulletin of the Korean Chemical Society
• /
• 제34권5호
• /
• pp.1349-1354
• /
• 2013

Twenty two new 5-fluorouracil (5-FU) derivatives, 2-butoxy-4-substituted 5-fluoropyrimidines, were synthesized and characterized by IR, $^1H$ NMR, MS, HRMS. All compounds were preliminarily evaluated by MTT assay on human liver BEL-7402 cancer cell line in vitro. Ten compounds were selected to test their cytotoxic activity against A549, HL-60 and MCF-7 cancer cell lines in vitro. These compounds were more sensitive to BEL-7402 than other cell lines, particularly, cytotoxic activity of compounds 6b, 6d-f, 6p, 6s-u were in sub-micromolar scale. The highest cytotoxic potency against A549, HL-60 and MCF-7 was shown by 2-butoxy-4-chloro-5-fluoropyrimidine (5) with $IC_{50}$ values of 0.10, 1.66 and $0.59{\mu}M$, respectively. Compounds 6d and 6e were effective against MCF-7 with $IC_{50}$ $9.73{\mu}M$ and HL-60 with $IC_{50}$ $8.83{\mu}M$, respectively.

• Biomolecules & Therapeutics
• /
• 제10권4호
• /
• pp.287-292
• /
• 2002

To find new inhibitory effects from oriental drugs, Albizziae root was extracted in methanol and the extracted was stepwisely fractionated by hexane, chloroform, ethylacetate, butanol and water. In cytotoxic effect of Albizziae root fractions against cancer cell lines including human hepatoma cells(HepG2) were investigated. Expecially the butanol fraction exhibited a inhibition effects on the growth of human hepatoma cells(HepG2). It inhibited of HepG2 cells with the value of IC50. The activities of qutathione after B(a)P treatment were markedly decreased than control, but those levels were increased by the treatment of Albizziae root methanol fraction. The activity of glutathione-S-transferase after B(a)P treatment were markedly decreased than control, but those levels were increased by the treatment of Albizziae root methanol traction. Induction of phase II enzymes is a major mechanism of chemoprevention. The induction levels of quinone reductase(QR) activity in cultured murine hepatoma(Hepa IcIc7)cell by methanol extract of Albizziae root were measured. Among the tested tractions, the extracts of butanol were found to induce QR activities over 2.8 fold than control. These results suggest that Albizziae root has chemopreventive Potential by inducing QR activities and GST levels and increasing GSH

• 한국콘텐츠학회논문지
• /
• 제22권3호
• /
• pp.567-575
• /
• 2022

본 연구에서는 국내산 방울토마토의 폴리페놀 및 플리보노이드 함량, 항산화 활성 및 암세포 억제 활성을 알아보았다. Summerking, Qutiquti 및 Minichal 품종의 총 폴리페놀 함량은 각각 12.56±1.88 mg/g, 12.50±1.92 mg/g 및 11.65±1.85 mg/g, 총 플라보이드 함량은 각각 4.58±1.03 mg/g, 4.19±0.40 mg/g 및 4.30±0.49 mg/g이었다. DPPH 및 ABTS radical 소거활성 측정을 통한 항산화 활성 측정 결과 모두 뚜렷한 항산화활성을 나타내었다. 암세포 억제 활성을 알아본 결과 세가지 품종 모두 정상 간세포(Chang)에 대한 세포독성은 관찰되지 않았고 자궁경부암세포(HeLa)에 대해서는 강한 억제 활성을 보였다. 간암세포(HepG2)에 대해서도 생육억제 효과가 확인되었다. 본 연구를 통해 국내산 방울토마토의 생리활성 식품소재로서의 유용성이 밝혀졌다.

• KSBB Journal
• /
• 제30권4호
• /
• pp.175-181
• /
• 2015

Cells proliferate via repeating process that growth and division. This process is G1, S, G2 and M four phases consists. Monitoring the progression of the cell cycle is a specific step that to be a continuous process is repeated to adjust the start of the next step. At this time, this process is called a Checkpoint. Currently, there are three known checkpoints that G1-S phase, G2-M phase, and the M phase. In this study, we confirmed that cell cycle arrest effects by ethanol extracts of Artemisia annua Linne (AAE) in Hep3B liver cancer cells. AAE was regulated proteins which involved in cell cycle such as pAkt, pMDM2, p53, p21, pCDK2 (T14/Y15). AAE induced cell cycle arrest in G1 checkpoint through phosphorylation of CDK2. Akt and p53 upstream is inhibited by AAE and p53 activated by non-activated pMDM2, p53 inhibitor. Thereby, activated p53 is transcript to p21 and activated p21 protein is combined with Cyclin E-pCDK2 complex. Therefore, we confirmed that AAE-induced cell cycle arrest was occurred by p21-Cyclin E-pCDK2 complex by inhibition of pAkt signal. Because of this cell cycle can't pass to S phase from G1 phase.

• Tuberculosis and Respiratory Diseases
• /
• 제43권4호
• /
• pp.527-535
• /
• 1996

연구배경 : 내피세포와 백혈구 및 상피세포에서 주로 발견되는 sICAM-1은 백혈구 표면의 배위자인 (ligand)인 LFA-1과 결합함으로서 염증성 질환 이외에 악성 종양의 전이와 진행에 중요한 역할을 하는 것으로 알려졌다. 최근에는 혈청내 sICAM-1의 농도가 악성 흑세포종의 전이와 비례하여 증가되는 것으로 보고되었으며, 또한 sICAM-1의 이형이 여러 질환에서 발견되고 이들의 혈청 농도의 증가는 위암, 대장암, 담낭암, 췌장암의 간전이와 관련되며, 악성 흑세포종 환자의 생존율의 감소와 관련되는 것으로 보고하였으나 폐암에서는 이에 대한 보고는 거의 없다. 이에 저자들은 폐암 환자의 혈청에서 sICAM-1을 측정하여 폐암의 조직학적 분류와 진행 및 전이의 정도에 따른 변화를 알아보고 폐암의 진단적 가치에 대하여 알아 보고자 하였다. 방법 : 1995년 1월부터 1996년 3월까지 전북대학교병원 내과에 입원하여 폐암을 진단 받은 환자 38명을 대상으로 하였으며, 정상 대조군은 비슷한 연령의 다른 질환을 갖고 있지 않은 8명을 대상으로 하였으며, 기관지 내시경을 통한 조직 생검이나 경피적 세침 흡입술을 이용하여 확진을 하였으며, 각 조직학적 분류에 따른 진행정도를 알기 위하여 TNM system 을 이용하여 분류하였고, 소세포 폐암은 limited stage와 extensive stage로 분류하였다. Genzyme사의 Predicts sICAM-1 ELISA kit를 이용하여 혈청 sICAM-1농도를 측정하였다. 결과 : 1. 소세포 폐암군에서 혈청 sICAM-1은 정상 대조군에 비해 유의한 증가가 없었으나, extensive stage군에서 limited stage군에 비해 유의한 증가를 보였다. 2. 편평상피암군에서 혈청 sICAM-1은 정상 대조군에 비해 유의한 증가를 보였으며, stage IIIa기 이하군에 비해 stage IIIb기 이상군에서 유의한 증가를 보였다. 3. 선폐암 환자군에서 혈청내 sICAM-1은 정상 대조군에 비해 유의한 증가를 보였다. 결론 : 혈청 sICAM-1농도의 변화는 폐암의 조직학적 분류에 따라 다르게 나타나며, 폐암의 전이 및 진행과 관련이 있을 것으로 보인다. 폐암 환자에서 혈청 sICAM-1농도의 측정은 폐암에서 진행의 정도를 평가하는 데 지표로서 이용될 수 있을 것으로 사료된다.

• Journal of Gastric Cancer
• /
• 제21권2호
• /
• pp.191-202
• /
• 2021

Purpose: A near-infrared (NIR) fluorescence imaging is a promising tool for cancer-specific image guided surgery. Human epidermal receptor 2 (HER2) is one of the candidate markers for gastric cancer. In this study, we aimed to synthesize HER2-specific NIR fluorescence probes and evaluate their applicability in cancer-specific image-guided surgeries using an animal model. Materials and Methods: An NIR dye emitting light at 800 nm (IRDye800CW; Li-COR) was conjugated to trastuzumab and an HER2-specific affibody using a click mechanism. HER2 affinity was assessed using surface plasmon resonance. Gastric cancer cell lines (NCI-N87 and SNU-601) were subcutaneously implanted into female BALB/c nu (6-8 weeks old) mice. After intravenous injection of the probes, biodistribution and fluorescence signal intensity were measured using Lumina II (Perkin Elmer) and a laparoscopic NIR camera (InTheSmart). Results: Trastuzumab-IRDye800CW exhibited high affinity for HER2 (K_D=2.093(3) pM). Fluorescence signals in the liver and spleen were the highest at 24 hours post injection, while the signal in HER2-positive tumor cells increased until 72 hours, as assessed using the Lumina II system. The signal corresponding to the tumor was visually identified and clearly differentiated from the liver after 72 hours using a laparoscopic NIR camera. Affibody-IRDye800CW also exhibited high affinity for HER2 (K_D=4.71 nM); however, the signal was not identified in the tumor, probably owing to rapid renal clearance. Conclusions: Trastuzumab-IRDye800CW may be used as a potential NIR probe that can be injected 2-3 days before surgery to obtain high HER2-specific signal and contrast. Affibody-based NIR probes may require modifications to enhance mobilization to the tumor site.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
• /
• pp.166.2-167
• /
• 2003

The important biological activities of estrogen were reproduction and physiological processes in a number of tissues, including liver, bone, brain, blood vessels, adipose tissue and so on. The regulation of estrogen level is important a prevention of estrogen-related disease. Ginkgo biloba extracts (GSE) are extracted from leaves of the Ginkgo biloba tree. GSE contains 24％ phytoestrogen, which are kaempferol, quercetin, and isorhamnetin. (omitted)

• 생약학회지
• /
• 제34권4호통권135호
• /
• pp.297-302
• /
• 2003

Cnidii Rhizoma water extract (CRW) was tested for liver cancer chemopreventive potential by measuring the inhibition of phase I enzyme and benzo[a]pyrene-DNA adduct formation and induction of phase II detoxification enzymes. There was 17.0% inhibition in the activity of cytochrome P450 1A1 enzyme with the treatment of 150 mg/ml CRW. At concentration of 30 mg/ml CRW, the binding of $[^3H]B[a]P$ metablites to DNA of NCTC-clone 1469 cell was inhibited by 33.3%. CRW was potent inducer of quinone reductase (QR) and glutathione S-transferase (GST) activities in cultured murine hepatoma Hepalc1c7 cells. However, hepatic glutathione (GSH) level was not influenced by CRW. These findings suggest that CRW has chemopreventive potential of liver cancer by inhibiting cytochrome P450 1A1 activity and benzo[a]pyrene-DNA adduct formation and inducing QR and GST activities.

• 대한본초학회지
• /
• 제38권5호
• /
• pp.49-60
• /
• 2023

Objectives : In this study, it was investigated the anti-inflammatory, anticancer, and antioxidant effects of Jayangdaebo-tang (JDT) consisting of twelve herbs before and after fermentation. Methods : JDT extract was fermented using the Lactoplantibacillus plantanum (JDT-L), Bacillus subtilis (JDT-B), and L. plantanum plus B. subtilis (JDT-L+B). The effects of each extract were measured in LPS-stimulated RAW264.7 cells, MCF-7 breast cancer and A549 lung cancer cells, and H₂O₂-stimulated HepG2 cells. Results : The extracts of JDT-L, JDT-B and JDT-L+B at 1 ㎎/㎖ decreased significantly the levels of nitric oxide (NO) in LPS-treated RAW264.7 cells and also inhibited the expression of iNOS and COX-2, and the phosphorylation of ERK and NF-κB. The JDT-L+B extract decreased significantly the expression of apoptotic proteins, Bax, cleaved caspase-3, and PARP in MCF-7 and A549 cancer cells. The JDT-L, JDT-B and JDT-L+B extracts increased significantly the cell viability in H₂O₂-stimulated HepG2 cells and the JDT-L+B extract decreased significantly the expression of SOD, catalase, HO-1, and NRF-2. Among fermented JDT extracts, JDT-L+B was the best effective on response of macrophage inflammation, cancer cell apoptosis, and liver cell damage. Conclusions : Our results were suggested that the fermentation can be used as a useful way to enhance the biological activity of JDT.

• Asian Pacific Journal of Cancer Prevention
• /
• 제16권15호
• /
• pp.6681-6684
• /
• 2015

Background: Metastatic cancer with invasion of skin, soft tissue and skeletal muscle is not common. Examples presenting as soft tissue masses could sometimes lead to misdiagnosis with delayed or inappropriate management. The purpose of current study was to investigate clinical characteristics in the involvement of metastatic cancer. Materials and Methods: A total of 1,097 patients complaining of skin or soft tissue masses and/or lesions were retrospectively reviewed from January 2012 to June 2013. Tumors involving skin, soft tissue and skeletal muscle of head and neck, chest wall, abdominal wall, pelvic region, back, upper and lower extremities were included in the study. Results: Fifty-seven (5.2%) patients were recognized as having malignancies on histopathological examination. The most common involvement of malignancy was basal cell carcinoma, followed by cutaneous squamous cell carcinoma, sarcoma and melanoma. The most common anatomical location in skin and soft tissue malignancies was head and neck (52.6% of the malignancies). Four (0.36%) of the malignant group were identified as metastatic cancer with the primary cancer source from lung, liver and tonsil and the most common site was upper extremities. One of them unexpectedly expired during the operation of metastatic tumor excision at the scalp. Conclusions: Discrimination between benign and malignant soft tissue tumors is crucial. Performance of imaging study could assist in the differential diagnosis and the pre-operative risk evaluation of metastatic tumors involving skin, soft tissue and skeletal muscle.