• Title/Summary/Keyword: Anticancer agents

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Recent Progress in Drug Delivery Systems for Anticancer Agents

  • Kim, Chong-Kook;Lim, Soo-Jeong
    • Archives of Pharmacal Research
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    • v.25 no.3
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    • pp.229-239
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    • 2002
  • Recent progress in understanding the molecular basis of cancer brought out new materials such as oligonucleotides, genes, peptides and proteins as a source of new anticancer agents. Due to their macromolecular properties, however, new strategies of delivery for them are required to achieve their full therapeutic efficacy in clinical setting. Development of improved dosage forms of currently marketed anticancer drugs can also enhance their therapeutic values. Currently developed delivery systems for anticancer agents include colloidal systems (liposomes, emulsions, nanoparticles and micelles), polymer implants and polymer conjugates. These delivery systems have been able to provide enhanced therapeutic activity and reduced toxicity of anticancer agents mainly by altering their pharmacokinetics and biodistribution. Furthermore, the identification of cell-specific receptor/antigens on cancer cells have brought the development of ligand- or antibody-bearing delivery systems which can be targeted to cancer cells by specific binding to receptors or antigens. They have exhibited specific and selective delivery of anticancer agents to cancer. As a consequence of extensive research, clinical development of anticancer agents utilizing various delivery systems is undergoing worldwide. New technologies and multidisciplinary expertise to develop advanced drug delivery systems, applicable to a wide range of anticancer agents, may eventually lead to an effective cancer therapy in the future.

Production of Bioactive 3'-Hydroxystilbene Compounds Using the Flavin-Dependent Monooxygenase Sam5

  • Heo, Kyung Taek;Lee, Byeongsan;Son, Sangkeun;Ahn, Jong Seog;Jang, Jae-Hyuk;Hong, Young-Soo
    • Journal of Microbiology and Biotechnology
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    • v.28 no.7
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    • pp.1105-1111
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    • 2018
  • The flavin-dependent monooxygenase Sam5 was previously reported to be a bifunctional hydroxylase with coumarate 3-hydroxylase and resveratrol 3'-hydroxylase activities. In this article, we showed the Sam5 enzyme has 3'-hydroxylation activities for methylated resveratrols (pinostilbene and pterostilbene), hydroxylated resveratrol (oxyresveratrol), and glycosylated resveratrol (piceid) as substrates. However, piceid, a glycone-type stilbene used as a substrate for bioconversion experiments with the Sam5 enzyme expressed in Escherichia coli, did not convert to the hydroxylated compound astringin, but it was converted by in vitro enzyme reactions. Finally, we report a novel catalytic activity of Sam5 monooxygenase for the synthesis of piceatannol derivatives, 3'-hydroxylated stilbene compounds. Development of this bioproduction method for the hydroxylation of stilbenes is challenging because of the difficulty in expressing P450-type hydroxylase in E. coli and regiospecific chemical synthesis.

A CoMFA Study of Quinazoline-based Anticancer Agents

  • Balupuri, Anand;Balasubramanian, Pavithra K.;Cho, Seung Joo
    • Journal of Integrative Natural Science
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    • v.8 no.3
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    • pp.214-220
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    • 2015
  • Cancer has emerged as one of the leading cause of deaths worldwide. A three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis was performed on a series of quinazoline-based anticancer agents. Purpose of the study is to understand the structural basis for their inhibitory activity. Comparative molecular field analysis (CoMFA) technique was employed to develop 3D-QSAR model. Ligand-based alignment scheme was used to generate a reliable CoMFA model. The model produced statistically significant results with a cross-validated correlation coefficient ($q^2$) of 0.589 and a non-cross-validated correlation coefficient ($r^2$) of 0.928. Model was further validated by bootstrapping and progressive scrambling analysis. This study could assist in the design of novel and more potent anticancer agents.

Therapeutic Effect of HM 10411 on Neutropenia Caused by Anticancer Agents in Mice (마우스에서 항암제 유발 호중구 감소에 대한 HM 10411의 회복촉진효과)

  • 강경선;제정환;김경배;이지해;조성대;조종호;박준석;안남식;양세란
    • Toxicological Research
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    • v.17 no.2
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    • pp.151-157
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    • 2001
  • Neutropenia is a major dose-limiting side effect of cancer chemotherapy. The therapeutic effect of HM 10411 was examined on neutropenia caused by anticancer agents. Neutropenia in normal ICR mice was induced by a single combined intraperitoneal injection of 130 mg/kg of cyclophosphamide (CPA). 4.5 mg/kg of doxorubicin (DXR). and 1 mg/kg of vincristine (VCR) on day O. Neutropenia in tumor-bearing mice was made by a single intraperitoneal injection of 200 mg/kg of cyclophosphamide (CPA) into BALB/c mice bearing Colon 26 adenocarcinoma at 7 day after tumor implantation. HM 10411 or filgrastim (100 $\mu\textrm{g}$/kg/day) was subcutaneously administered for 5 consecutive days starting 1 day after injection of anticancer agents in order to stimulate neutrophil production. Injection of HM 10411 accelerated the recovery from these anticancer drug-induced neutropenia. In normal and tumor-bearing mice. neutrophil production efficacy of HM 10411 was similar than that of filgrastim. These results suggest that HM 10411 could be useful in the clinical treatment for neutropenia induced by anticancer agents.

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General Pharmacology of the New Platinum (II) Anticancer Agents with Diaminocyclohexane as a Carrier Ligand (Diaminocyclohexane을 배위자로 한 새로운 항암성 백금(II)착체류의 일반약리작용)

  • 고석태;강선영;임동윤;신현준;최승기;노영수;정지창
    • Biomolecules & Therapeutics
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    • v.6 no.3
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    • pp.303-311
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    • 1998
  • The general pharmacological properties of new platinum (II) coordination complexes, SA : [Pt(trans-ι-DACH)(DPPE)] . 2NO$_3$, SB : [Pt(cia-DACH)(DPPP)] 2NO$_3$ and SC : [Pt(cia-DACH)(DPPE)] 2NO$_3$on central nervous, respiratory, cardiovascular and digestive systems were studied in various experimental animals. These platinum (II) anticancer agents had no effects on analgesia, thiopental-induced sleeping time, body temperature, strychnine-induced convulsion, inflammation and local anesthetic action in mice and rats. Intestinal motility, stomach-ulcer induced by serotonin and bile-secretion of rats were not influenced by the dose of 30 mg/kg. However SB and SC induced a mild decrease in heart rate in anesthetized rats. Based on these results, these new platinum (II) complexes may be regarded as a valuable lead compound in the development of new anticancer chemotherapeutic agents with marked antitumor activity and low toxicity.

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Selection of Oriental Medicinal Plants for Screening of Anticancer Agents (항암소재의 발굴을 위한 한방소재의 선별)

  • Park, Keun-Hyoung;Kim, So-Young;Chae, Hee-Jeong
    • KSBB Journal
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    • v.22 no.3
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    • pp.139-145
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    • 2007
  • An oriental medicinal database was used from medicinal plants for screening of anticancer agents. The prescription frequency and dosage of medicinal plats in 170 anticancer prescriptions were analyzed. From the total prescription score of each medical plant, it was found that high-scored medicinal plants have been widely studied in the previous research on the cancer treatment. Consequently, dangui, hwangui, banha, bachul, jinpy, insam, bacjakyak, deahwang, chungoong, jimo, chunnamsung, omija, hyunggae, huekchook, banggi, boclyung, osooyou were selected as raw materials for the screening of anticancer agents.

Isolation. structure. and NF-${\kappa}$B modulatory activity of Harzianum A and B: trichothecene from fungi(B000527)

  • Jin, Hui-Zi;Lee, Jeong-Hyung;Kim, Young-Ho;Lee, Jung-Joon
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.320.3-321
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    • 2002
  • Nuclear factor ${\kappa}$B (NF-${\kappa}$B) represents a family of eukaryotic transcription factors participating in the regulation of various cellular genes. Since aberrant regulation of NF-${\kappa}$B has been implicated in the pathogenesis of various diseases including inflammation. asthma. atherosclerosis. AIDS. septic shock. arthritis, and cancer. this transcription factor has been shown to be an interesting target of new drug discovery. (omitted)

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Therapeutic Effect of CJ-50(101 (rG-CSF) on Neutropenia Caused by Anticancer Agents in Mice (마우스에서 항암제 유발 호중구감소에 대한 CJ-50001의 회복촉진효과)

  • 백남진;강재구;최재묵;김기완;김달현;김제학;김현수
    • Biomolecules & Therapeutics
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    • v.5 no.4
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    • pp.384-389
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    • 1997
  • Neutropenia is a major dose-limiting side effect of cancer chemotherapy. The therapeutic effects of CJ-50001 were examined on neutropenia caused by anticancer agents. Neutropenia was induced by cyclophosphomide (130 mg/kg), doxorubicin (4.5 mg/kg), and vincristine (1 mg/kg) in normal ICR mice and by cyclophosphamide (200 mg/kg) in CT26 adenocarcinoma bearing BALB/C mice. After the subcutaneous injection of anticancer agents, we administered subcutaneously recombinant human granulocyte-colonystimulating factor (100$\mu$g/kg/day) to mice in order to stimulate neutrophil production. In normal and tumor-bearing mice, neutrophil production efficacy of CJ-50001 (rG-CSF) was similar to that of Grasin. These results suggest that CJ-50001 could be effective in its clinical use for neutropenia treatment.

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