• Title/Summary/Keyword: therapeutic agents

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Metabolism-based Anticancer Drug Design

  • Kwon, Chul-Hoon
    • Archives of Pharmacal Research
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    • v.22 no.6
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    • pp.533-541
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    • 1999
  • Many conventional anticancer drugs display relatively poor selectivity for neoplastic cells, in particular for solid tumors. Furthermore, expression or development of drug resistance, increased glutathione transferases as well as enhanced DNA repair decrease the efficacy of these drugs. Research efforts continue to overcome these problems by understanding these mechanisms and by developing more effective anticancer drugs. Cyclophosphamide is one of the most widely used alkylating anticancer agents. Because of its unique activation mechanism, numerous bioreversible prodrugs of phosphramide mustard, the active species of cyclophosphamide, have been investigated in an attempt to improve the therapeutic index. Solid tumors are particularly resistant to radiation and chemotherapy. There has been considerable interest in designing drugs selective for hypoxic environments prevalent in solid tumors. Much of the work had been centered on nitroheterocyclics that utilize nitroreductase enzyme systems for their activation. In this article, recent developments of anticancer prodrug design are described with a particular emphasis on exploitation of selective metabolic processes for their activation.

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Effects of Sojihwangamibang on Hyperlipidemia in Rats Induced by High Cholesterol Diet (소지환가미방이 고지혈 병리인자 및 동물 병태 모델에 미치는 영향)

  • Yu, Mao-Lun;Kim, Dong-Hee
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.23 no.6
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    • pp.1358-1367
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    • 2009
  • This experimental study was designed to investigate the inhibitory effects of Sojihwangamibang on hyperlipidemia in rats induced by high cholesterol diet diet. Sprague- Dawley rats were divided into normal group, control group, SJB treated group. Obese rats were induced by high cholesterol diet treatment for 6 weeks including a oral administration of SJB for 4 weeks. In SJB group, serum total cholesterol, LDL cholesterol, triglyceride and glucose were significantly decreased, and HDL cholesterol was significantly increased compared with untreated control group. In SJB group, HMG-CoA and ACAT concentration of hepatic homogenate were significantly decreased compared with untreated control group. These results provide experimental evidence that SJB, applied currently in the clinical practice, appears to be effective for down-regulating risk factors of hyperlipidemia, and thus may be used as an objective information for the development of therapeutic agents.

Mitochondrial DNA Somatic Mutation in Cancer

  • Kim, Aekyong
    • Toxicological Research
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    • v.30 no.4
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    • pp.235-242
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    • 2014
  • Cancer cells are known to drastically alter cellular energy metabolism. The Warburg effect has been known for over 80 years as pertaining cancer-specific aerobic glycolysis. As underlying molecular mechanisms are elucidated so that cancer cells alter the cellular energy metabolism for their advantage, the significance of the modulation of metabolic profiles is gaining attention. Now, metabolic reprogramming is becoming an emerging hallmark of cancer. Therapeutic agents that target cancer energy metabolism are under intensive investigation, but these investigations are mostly focused on the cytosolic glycolytic processes. Although mitochondrial oxidative phosphorylation is an integral part of cellular energy metabolism, until recently, it has been regarded as an auxiliary to cytosolic glycolytic processes in cancer energy metabolism. In this review, we will discuss the importance of mitochondrial respiration in the metabolic reprogramming of cancer, in addition to discussing the justification for using mitochondrial DNA somatic mutation as metabolic determinants for cancer sensitivity in glucose limitation.

Therapeutic Potential of Membrane Fatty Acid Modifiaction in Tumor Cells

  • Shon, Yun-Hee;Park, Kun-Young;Kim, Kwang-Soo
    • Preventive Nutrition and Food Science
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    • v.1 no.1
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    • pp.143-150
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    • 1996
  • The membrane fatty acid composition of tumor cell can be modified either in cell by altering the lipid composition of the medium of during growth in animals by changing the dietaty fat composition. These modifications are associated with changes in membrane physical properties and certain cellular functions, including carrier-mediated transport and enzyme contained within the membrane. Such effects influence the transport of nutrients and chemotherapeutic agents in cancer cells .Fatty acid modification also can enhance the sensitivity of the neoplastic cell to chemotherapy. The alteration in plasma membrane composition will be affected through dietary supplementations and the potential value to cancer patients could be a better understanding of the effects of diet on responsiveness of neoplasms to chemotherapy, i.e. cancer patients' chances for a "cure" can be improved by diet changes prior to treatment.

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Toxicity of disulfiram, a therapeutic agent for chronic alcoholism, to mouse spleen cells

  • Han, Yong;Joo, Hong-Gu
    • Journal of Preventive Veterinary Medicine
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    • v.42 no.4
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    • pp.177-181
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    • 2018
  • Disulfiram is a drug used to treat alcohol dependence. Recent studies have shown that disulfiram also has anti-cancer effects. Considering that many anti-cancer agents have side effects, including immunosuppression, it is important to check if disulfiram has some cytotoxicity to immune cells. In this study, mouse spleen cells were treated with disulfiram and the metabolic activity was measured. Disulfiram increased the cell death of spleen cells according to annexin V-FITC/PI staining analysis. In addition, disulfiram decreased the mitochondrial membrane potential of spleen cells. The toxicity of disulfiram was concentration dependent. Interestingly, disulfiram affected the population of lymphocytes and the subset of spleen cells was altered. This study provides clinicians and researchers with valuable information regarding the toxicity of disulfiram to mouse spleen cells, particularly lymphocytes.

Design and Synthesis of Chromenone derivatives as Potential Antioxidants

  • Kang, Hae-Eun;Lee, Kum-Ho;Lee, Dae-Hee;Cho , Jung-Sook;Lee, Hee-Soon
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.351.3-353
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    • 2002
  • Oxygen radicals are produced in many pathophysiologic states whether the event is a causal factor of illness or is a result of their progression. Oxygen radicals including superoxide anions. hydrogen peroxide are thought to be involved in a number of type of acute. and chronic pathologic condition in the brain and neural tissue. So the antioxidants have recently received much attention as therapeutic agent for the treatment of neurodegenerative disease. In this study. we describe synthesis of a series of chromenone derivatives as antioxidant agents. The target compounds are designed to include the structural frature of caffeic acid. flavoniod. and focopherol known as antioxidants.

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Effect of Puffing in the Extraction of Active Ingredients from the Roots of Paeonia lactiflora and Astragalus membranaceus

  • Lee, Hyojin;Jang, Kyoung Won
    • Natural Product Sciences
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    • v.28 no.2
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    • pp.89-92
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    • 2022
  • In Asia, the roots of Paeonia lactiflora and Astragalus membranaceus have been used as therapeutic agents for thousands of years. Once the medicinal plants are harvested, they are dried and their ingredients are extracted by heat-mediated reflux extraction. However, the condensed structure of organic products (especially roots) limits the extraction of bioactive components. In this study, we assessed the effect of the puffing method (using high temperature and pressure) before the extraction process in relation to the profile and antioxidant capacity of active ingredients. We demonstrated that the additional puffing process before extraction methods improves the yield of polyphenol concentrations and antioxidant activities from the roots of P. lactiflora and A. membranaceus.

Flavonoids as Novel Therapeutic Agents Against Chikungunya Virus Capsid Protein: A Molecular Docking Approach

  • E. Vadivel;Gundeep Ekka;J. Fermin Angelo Selvin
    • Journal of the Korean Chemical Society
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    • v.67 no.4
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    • pp.226-235
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    • 2023
  • Chikungunya fever has a high morbidity rate in humans and is caused by chikungunya virus. There are no treatments available until now for this particular viral disease. The present study was carried out by selecting 19 flavonoids, which are available naturally in fruits, vegetables, tea, red wine and medicinal plants. The molecular docking of selected 19 flavonoids was carried out against the Chikungunya virus capsid protein using the Autodock4.2 software. Binding affinity analysis based on the Intermolecular interactions such as Hydrogen bonding and hydrophobic interactions and drug-likeness properties for all the 19 flavonoids have been carried out and it is found that the top four molecules are Chrysin, Fisetin, Naringenin and Biochanin A as they fit to the chikungunya protein and have binding energy of -8.09, -8.01, -7.6, and 7.3 kcal/mol respectively. This result opens up the possibility of applying these compounds in the inhibition of chikungunya viral protein.

Current scenario and future applicability of antivirals against herpes zoster

  • Sang Hun Kim
    • The Korean Journal of Pain
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    • v.36 no.1
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    • pp.4-10
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    • 2023
  • Herpes zoster (HZ) is a common disease in the aging population and immunocompromised individuals, with a lifetime risk of 20%-30% that increases with age. HZ is caused by reactivation of the varicella-zoster virus (VZV), which remains latent in the spinal dorsal root ganglia and cranial sensory ganglia after resolution of the primary VZV infection. The main focus of HZ management is rapid recovery from VZV infection as well as the reduction and prevention of zoster-associated pain (ZAP) and postherpetic neuralgia (PHN). The use of antivirals against VZV is essential in the treatment of HZ. However, limited antivirals are only licensed clinically for the treatment of HZ, including acyclovir, valacyclovir, famciclovir, brivudine, and amenamevir. Fortunately, some new antivirals against different types of Herpesviridae have been investigated and suggested as novel drugs against VZV. Therefore, this review focuses on discussing the difference in efficacy and safety in the currently licensed antivirals for the treatment of HZ, the applicability of future novel antivirals against VZV, and the preventive or therapeutic effects of these antivirals on ZAP or PHN.