• 제목/요약/키워드: Anticancer therapy

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Development of Radiopharmaceutical DW-166HC for Anticancer drug

  • Man, Ryu-Jei
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1999년도 춘계학술대회
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    • pp.53-61
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    • 1999
  • Radiation therapy has been used for the cancer treatment and radiation synovectomy$\^$1-3)/. There are two kinds of radiation therapy; the external radiation therapy and the internal radiation therapy. Hitherto, the external radiation therapy has been widely used, but for the lack of its selectivity it requires strong radiation dose and causes the irritation and damage of the normal tissue or organ. Therefore many researchers give their interests to the internal radiation therapy in which the radioactive materials are injected directly into the target organ or tissue. Many ${\beta}$-emitting radionuclides have been studied for the application of the internal radiation theraily. Among them, Holmium-166 has the many beneficial physical characteristics for the internal radiation therapy such as appropriate half life (26.8hr), high ${\beta}$ energy (max. 1.85 MeV(51%), 1.77 MeV (48%), mean 0.67MeV), and low ${\gamma}$ energy (0.081MeV) easily detected by ${\gamma}$-camera. In the internal radiation therapy, the administered radioactive materials should be retained in the target long enough to increase the therapeutic effects and avoid the damage in the normal tissue or organ. For this purpose, radionuclides are used as complex form with carriers. Carriers should have a high affinity with radionuclides in vivo and in vitro, so the complex can be evenly distributed in the lesion but can not be leaked out from the lesion.

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Ethanol but not Aqueous Extracts of Tubers of Sauromatum Giganteum(Engl.) Cusimano and Hett Inhibit Cancer Cell Proliferation

  • Gao, Shi-Yong;Li, Jun;Wang, Long;Sun, Qiu-Jia;Gong, Yun-Fei;Gang, Jian;Su, Yi-Jun;Ji, Yu-Bin
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권24호
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    • pp.10613-10619
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    • 2015
  • Background: Both alcohol and aqueous extracts of Sauromatum giganteum(Engl.) Cusimano and Hett, the dried root tuber of which is named Baifuzi in Chinese, have been used for folklore treatment of cancer in Northeast of China. However, little is known about which is most suitable to the cancer therapy. Materials and Methods: Serum pharmacology and MTT assays were adopted to detect the effects of ethanol and aqueous extracts of Sauromatum giganteum(Engl.) Cusimano and Hett, prepared by heat reflux methods, on proliferation of different cancer cells. Results: Cancer cells treated with medium supplemented with 10%, 20%, 40% serum(v/v) containing ethanol extract had a decline in viability, with inhibition rates of 7.69%, 21.8%, 41.9% in MCF-7 cells, 42.8%, 48.1%, 51.8% in SGC-7901 cells, 44.1%, 49.2%, 53.7% in SMMC-7721 cells, 6.8%, 15.2%, 39.8% in HepG2 cells, 7.57%, 16.3%, 36.2% in HeLa cells, 6.24%, 12.5%, 27.4% in A549 cells, and 7.20%, 17.5%, 31.3% in MDA-MB-231 cells, respectively. Viability in the aqueous extract groups was no different with that of controls. Conclusions: An ethanol extract of Sauromatum giganteum(Engl.) Cusimano and Hett inhibited the proliferation of SMMC-7721, SGC-7901 and MCF-7 cells, which supports the use of alcoholic but not aqueous extracts for control of sensive cancers, which might include hepatocarcinoma, gastric cancer and breast cancer.

Differential Behaviour of Selenium Analogs against Anticancer Drug Induced Apoptosis of Lymphocytes in Human Peripheral Blood

  • Elango, Sonaa;Subbiah, Usha;Jain, Jeong
    • Asian Pacific Journal of Cancer Prevention
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    • 제17권5호
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    • pp.2527-2533
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    • 2016
  • Sensitising cancer cells and at the same time desensitizing normal cells is a double task in cancer management. Agents which can combat the debilitating side effects of cancer therapeutics and simultaneously synergize with anticancer agents in specifically targeting cancer cells are needed. Selenium, a proven anticarcinogen, gains due importance in terms of its efficacy to combat the side effects of cancer therapy. This study is a comparative analysis of the chemoprotective effects of selenium compounds, methyl selenol (generated from organic selenomethionine (5mmol/L ; METase 40U/L)) and sodium selenite (inorganic form)($30{\mu}M$) in peripheral blood human lymphocytes exposed to cisplatin and mitomycin. Biochemical alterations occurring in many cells during apoptosis include loss of plasma membrane phospholipid asymmetry, DNA fragmentation, and activation of caspase-3. The present study demonstrated that the selenium metabolite and selenite are efficient in protecting lymphocytes undergoing DNA damage and exerted their activity by reducing caspase 3 expression. Interestingly organic methylselenol (MeSe) was found to offer more protective effects compared to inorganic selenite (SeL), by reducing the induction of apoptosis by the cytotoxic agents. This suggests that MeSe and to a lesser extent selenite might have potential for assessment in clinical trials and could be considered as strong candidates in pharmacogenomics or in the nutriprotective arena.

Anticancer effect of mountain ginseng Pharmacopuncture to the nude mouse of lung carcinoma induced by NCI-H460 human non-small cell lung cancer cells

  • Kwon, Ki-Rok
    • 대한약침학회지
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    • 제13권1호
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    • pp.5-14
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    • 2010
  • Objectives : This study was performed to examine the anticancer effect of mountain ginseng Pharmacopuncture(MGP) to the nude mouse of lung carcinoma induced by NCI-H460 human nonsmall lung cancer cells. Methods : Human lung cancer (NCI-H460) cells were cultured and applied to evaluate anti-tumor activity in nude mice. After confirmed tumor growth in mice, MGP was treated per 0.1ml/kg dose to intraperitoneal and intravenous injection everyday for four weeks. And checked the changes in body weights, tumor volume, mean survival time and percent, increase in life span, histo-pathological findings, organ weights, and blood chemistry levels. Results : The results of in vivo study showed that MGP may have potential as growth inhibitor of solid tumor induced NCI-H460 without marked side effects. MGP inhibited dosage-dependently the growth of NCI-H460 cell-transplanted solid tumor compared with the control group. And mean survival time of MGP treated group was prolonged comparing with control group. Generally the group of intravenous injection is more effective than intraperitoneal injection. Conclusion : These results were suggested that MGP may be a useful anticancer agent for therapy of human lung cancer. And follow study need for the certain evidence.

패독산류의 구강편평세포암종 및 악성중피종에 대한 항암 활성 (Anticancer Effect of Paedoksans for Oral Squamous Cell Carcinoma and Malignant Pleural Mesothelioma)

  • 오하나;김현정;채정일;심정현;윤구
    • 생약학회지
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    • 제48권3호
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    • pp.213-218
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    • 2017
  • In order to search for anticancer agent as therapy of oral squamous cell carcinoma (OSCC) and malignant pleural mesothelioma (MPM) from Korean traditional prescriptions, we selected 58 traditional prescriptions based on a review of the Korean traditional medicine books. Among the selected traditional prescriptions, only water extracts of paedoksan (敗毒散) showed relatively good cytotoxicity at the concentration of $50{\mu}g/ml$. Additionally, we evaluated cytotoxicity for various paedoksans and each herbal ingredient in paedoksans. The root of Anthriscus sylvestris exhibited more cytotoxic effect than any other ingredients in paedoksans. Bioactivity-guided fractionation of the MC layer of Anthriscus sylvestris led to the isolation of deoxypodophyllotoxin (DPT). DPT exhibited dose-dependently significant cytotoxicity against OSCC and MPM cell with nM range. Therefore, DPT from A. sylvestris might be a potential candidate as an effective anticancer therapeutic agent for OSCC and MPM.

Antiproliferative effect of gold(I) compound auranofin through inhibition of STAT3 and telomerase activity in MDA-MB 231 human breast cancer cells

  • Kim, Nam-Hoon;Park, Hyo Jung;Oh, Mi-Kyung;Kim, In-Sook
    • BMB Reports
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    • 제46권1호
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    • pp.59-64
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    • 2013
  • Signal transducer and activator of transcription 3 (STAT3) and telomerase are considered attractive targets for anticancer therapy. The in vitro anticancer activity of the gold(I) compound auranofin was investigated using MDA-MB 231 human breast cancer cells, in which STAT3 is constitutively active. In cell culture, auranofin inhibited growth in a dose-dependent manner, and N-acetyl-L-cysteine (NAC), a scavenger of reactive oxygen species (ROS), markedly blocked the effect of auranofin. Incorporation of 5-bromo-2'-deoxyuridine into DNA and anchorage-independent cell growth on soft agar were decreased by auranofin treatment. STAT3 phosphorylation and telomerase activity were also attenuated in cells exposed to auranofin, but NAC pretreatment restored STAT3 phosphorylation and telomerase activity in these cells. These findings indicate that auranofin exerts in vitro antitumor effects in MDA-MB 231 cells and its activity involves inhibition of STAT3 and telomerase. Thus, auranofin shows potential as a novel anticancer drug that targets STAT3 and telomerase.

miR-181b as a Potential Molecular Target for Anticancer Therapy of Gastric Neoplasms

  • Guo, Jian-Xin;Tao, Qing-Song;Lou, Peng-Rong;Chen, Xiao-Chun;Chen, Jun;Yuan, Guang-Bo
    • Asian Pacific Journal of Cancer Prevention
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    • 제13권5호
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    • pp.2263-2267
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    • 2012
  • Objective: MicroRNAs (miRNAs) play important roles in carcinogenesis. The aim of the present study was to explore the effects of miR-181b on gastric cancer. Methods: The expression level of miR-181b was quantified by qRT-PCR. MTT, flow cytometry and matrigel invasion assays were used to test proliferation, apoptosis and invasion of miR-181b stable transfected gastric cancer cells. Results: miR-181b was aberrantly overexpressed in gastric cancer cells and primary gastric cancer tissues. Further experiments demonstrated inducible expression of miR-181b by Helicobacter pylori treatment. Cell proliferation, migration and invasion in the gastric cancer cells were significantly increased after miR-181b transfection and apoptotic cells were also increased. Furthermore, overexpression of miR-181b downregulated the protein level of tissue inhibitor of metalloproteinase 3 (TIMP3). Conclusion: The upregulation of miR-181b may play an important role in the progress of gastric cancer and miR-181b maybe a potential molecular target for anticancer therapeutics of gastric cancer.

Naltriben Analogues as Peptide Anticancer Drugs

  • Kim, Min-Woo;Shin, Choon-Shik;Yang, Hee-Jung;Kim, Seung-Hyun;Lim, Hae-Young;Lee, Chul-Hoon;Kim, Min-Kyun;Lim, Yoong-Ho
    • Journal of Microbiology and Biotechnology
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    • 제14권4호
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    • pp.881-884
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    • 2004
  • Apoptosis inducers for cancer therapy have been studied. Among hundreds of inducers, peptide anticancer drugs have many advantages such as being not harmful to humans, high selectivity, and dependence on their structures. Naltriben (NTB) is an octapeptide consisting of DPhe-Cys-Tyr-DTrp-Orn-Thr-Pen-Thr-$NH_2$. Several NTB analogues are known. In this experiment, apoptotic activities of NTB analogues with 8 amino acids were tested using flow cytometry. The conformational study of NTB was carried out using NMR spectroscopy and molecular modeling. Here, the relationships between conformations of NTB analogues and their apoptotic effects are reported.

한약치료와 표적항암요법(아피니토)을 병행하여 부분 관해 된 신세포암 간전이 환자 1례 (A Case Report of Partial Remission of Renal Cell Carcinoma with Multiple Liver Metastases Treated with Korean Herbal Medicine in Conjunction with Targeted Anticancer Therapy Afinitor)

  • 장성환;박지혜;유화승
    • 대한암한의학회지
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    • 제22권2호
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    • pp.13-24
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    • 2017
  • Objectives: The purpose of this study is to report the effect of Korean Herbal Medicine (KHM) on a Renal Cell Carcinoma with multiple liver metastases patient. Methods: One renal cell carcinoma with multiple liver metastases patient was treated by KHM in conjunction with targeted anticancer agent (Afinitor). The effect of KHM was measured by scanning with Computed Tomography (CT), Blood Test, Visual Analogue Scale (VAS) and Eastern Cooperative Oncology Group scale. Results: Multiple hepatic tumors were reduced after the treatment during 5 months (Partial Remission, PR). As treatment was performed, complications induced by targeted anticancer agent (Afinitor) were alleviated. Conclusions: This case provides us a possibility that Korean Herbal Medicine offers potential benefits for renal cell carcinoma with multiple liver metastases patient.

Discovery of Novel and Potent Cdc25 Phosphatase Inhibitors Based on the Structure-Based De Novo Design

  • Park, Hwang-Seo;Jung, Suk-Kyeong;Bahn, Young-Jae;Jeong, Dae-Gwin;Ryu, Seong-Eon;Kim, Seung-Jun
    • Bulletin of the Korean Chemical Society
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    • 제30권6호
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    • pp.1313-1316
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    • 2009
  • Cdc25 phosphatases have been considered as attractive drug targets for anticancer therapy due to the correlation of their overexpression with a wide variety of cancers. We have been able to identify five novel Cdc25 phosphatase inhibitors with micromolar activity by means of a structure-based de novo design method with a known inhibitor scaffold. Because the newly discovered inhibitors are structurally diverse and have desirable physicochemical properties as a drug candidate, they deserve further investigation as anticancer drugs. The differences in binding modes of the identified inhibitors in the active sites of Cdc25A and B are addressed in detail.