• Title/Summary/Keyword: New drugs

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Synthesis, Physico-Chemical and Biological Properties of Complexes of Cobalt(II) Derived from Hydrazones of Isonicotinic Acid Hydrazide (Isonicotinic Acid Hydrazide의 Hydrazone으로부터 유도된 코발트(II) 착물의 합성, 물리-화학 및 생물학적 성질)

  • Prasad, Surendra;Agarwal, Ram K.
    • Journal of the Korean Chemical Society
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    • v.53 no.1
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    • pp.17-26
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    • 2009
  • Hydrazones of isonicotinic acid hydrazide, viz., N-isonicotinamido-furfuralaldimine (INH-FFL), N-isonicotnamido-cinnamalidine (INH-CIN) and N-isonicotnamido-3',4',5'-trimethoxybenzaldimine (INH-TMB) were prepared by reacting isonicotinic acid hydrazide with respective aromatic aldehydes, i.e., furfural, cinnamaldehyde or 3,4,5-trimethoxy-benzaldehyde. A new series of fifteen complexes of cobalt(II) with these new hydrazones, INH-FFL, INH-CIN and INH-TMB, were synthesized by their reaction with cobalt(II) salts. The infrared spectral data reveal that hydrazone ligands behave as a bidentate ligand with N, O donor sequence towards the $Co^{2+}$ ion. The complexes were characterized on the basis of elemental analysis, magnetic susceptibility, conductivity, infrared and electronic spectral measurements. Analytical data reveal that the complexes have general composition [Co($L)_2X_2]\;and\;[Co(L)_3](ClO_4)_2$ where L= INH-FFL, INH-CIN or INH-TMB and X = $Cl^-,{NO_3}-,\;NCS^-\;or\;CH_3COO^-.$ The thermal behaviour of the complexes were studied using thermogravimetrictechnique. Electronic spectral results and magnetic susceptibility measurements are consistent with the adoption of a six-coordinate geometry for the cobalt(II) chelates. The antimicrobial properties of cobalt(II) complexes and few standard drugs have revealed that the complexes have very moderate antibacterial activities.

Screening and isolation of antibacterial proteinaceous compounds from flower tissues: Alternatives for treatment of healthcare-associated infections

  • de Almeida, Renato Goulart;Silva, Osmar Nascimento;de Souza Candido, Elizabete;Moreira, Joao Suender;Jojoa, Dianny Elizabeth Jimenez;Gomes, Diego Garces;de Souza Freire, Mirna;de Miranda Burgel, Pedro Henrique;de Oliveira, Nelson Gomes Junior;Valencia, Jorge William Arboleda;Franco, Octavio Luiz;Dias, Simoni Campos
    • CELLMED
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    • v.4 no.1
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    • pp.5.1-5.8
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    • 2014
  • Healthcare-associated infection represents a frequent cause of mortality that increases hospital costs. Due to increasing microbial resistance to antibiotics, it is necessary to search for alternative therapies. Consequently, novel alternatives for the control of resistant microorganisms have been studied. Among them, plant antimicrobial protein presents enormous potential, with flowers being a new source of antimicrobial molecules. In this work, the antimicrobial activity of protein-rich fractions from flower tissues from 18 different species was evaluated against several human pathogenic bacteria. The results showed that protein-rich fractions of 12 species were able to control bacterial development. Due its broad inhibition spectrum and high antibacterial activity, the protein-rich fraction of Hibiscus rosa-sinensis was subjected to DEAE-Sepharose chromatography, yielding a retained fraction and a non-retained fraction. The retained fraction inhibits 29.5% of Klebsiella pneumoniae growth, and the non-retained fraction showed 31.5% of growth inhibition against the same bacteria. The protein profile of the chromatography fractions was analyzed by using SDS-PAGE, revealing the presence of two major protein bands in the retained fraction, of 20 and 15 kDa. The results indicate that medicinal plants have the biotechnological potential to increase knowledge about antimicrobial protein structure and action mechanisms, assisting in the rational design of antimicrobial compounds for the development of new antibiotic drugs.

A Trend of Artificial Intelligence in the Healthcare (헬스케어산업에서의 인공지능 활용 동향)

  • Lee, Sae Bom;Song, Jaemin;Park, Arum
    • The Journal of the Korea Contents Association
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    • v.20 no.5
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    • pp.448-456
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    • 2020
  • In the era of the Fourth Industrial Revolution, how well the explosive information and data are handled and used is recognized as a problem directly related to the competitiveness of the industry. In particular, the introduction of artificial intelligence technology in the medical field can be said to have a great social impact on its use, and this research was conducted to understand the trends of artificial intelligence according to the range of use case. In this study, the application of artificial intelligence in the healthcare field is divided into four scopes, (1) hospital solutions, (2) personal health care, (3) insurance, and (4) new drug development. Based on various cases and trends in artificial intelligence technology, this study tried to give directions on how to develop artificial intelligence in Korea. In this study, we wanted to find out the use cases of artificial intelligence in various areas of healthcare industry and describe the latest issues in healthcare to help the overall medical industry. The development of artificial intelligence-based medical systems has made it easier to manage the chronic patients, increased the accuracy of cancer or disease diagnosis, and helped developing new drugs faster and more efficiently. Through this study, the medical industry we wanted to give a direction to the future development of artificial intelligence in Korea.

Lack of Prognostic Value of Mean Corpuscular Volume with Capecitabine Therapy in Metastatic Breast Cancer

  • Bozkurt, Oktay;Berk, Veli;Kaplan, Muhammed Ali;Cetin, Bulent;Ozaslan, Ersin;Karaca, Halit;Inanc, Mevlude;Duran, Ayse Ocak;Ozkan, Metin
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.6
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    • pp.2501-2504
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    • 2014
  • Background: Capecitabine is an oral fluoropyrimidine derivative which is frequently used alone or in combination regimens for the treatment of metastatic breast cancer. Although overall and progression free survivals have increased in recent years with the use of new generation drugs, predictive factors that would further improve the outcomes are needed. Previous studies have demonstrated the relation between post-treatment increase in mean corpuscular volume (MCV) and predicting therapy response as well as survival. The present study investigated the clinical impact of MCV elevation in metastatic breast cancer patients treated with capecitabine. Materials and Methods: The data of a total of 82 patients from three centers followed between June 2005 and June 2013 were retrospectively analyzed. The demographic data and hormone receptor status of the patients, as well as initial examination before and after treatment and data concerning progression were recorded. MCV ${\geq}100$ fl was considered as macrocytosis. Capecitabine was given at a dose of $2500mg/m^2$ daily for 14 days every three weeks. Pre-treatment and post-treatment MCV and other parameters of complete blood count were recorded. Post-treatment initial evaluation was performed after 2 cycles of therapy. Results: The median age of the patients was 46.5 years (range 26-72 years) and 54% were premenopausal. Performance status was ECOG 0 and 1 in 81 (99%) patients. The median number of cycles for capecitabine therapy was 5 (min-max: 2-18). The median ${\Delta}MCV$ level (post-treatment values at sixth week - baseline) was 6.4. Whilst ${\Delta}MCV$ was ${\geq}6.4$ in 42 patients, it was <6.4 in 40 patients. Clinical benefit (complete response+partial response+stable disease) was observed in 37 (88%) of 42 patients with a median ${\Delta}MCV$ ${\geq}6.4$ and in 30 (75%) of 40 patients with ${\Delta}MCV$ <6.4 with no statistically significant difference (p=0.158). No significant difference was determined between the group with ${\Delta}MCV$ ${\geq}6.4$ and the group with ${\Delta}MCV$ <6.4 in terms of progression-free survival (11 vs 12 months) (p=0.55) and overall survival (20 months vs. 24 months) (p=0.11). Conclusions: The identification of new predictive markers in metastatic breast cancer is very important. In some recent studies, increase in MCV has been suggested as a marker in tumor response. In the present study, however, no significant difference was determined between tumor response and increase in MCV. Further studies including higher numbers of patients are needed to determine whether increase in MCV is a predictive marker or not.

Hepatitis C Virus - Proteins, Diagnosis, Treatment and New Approaches for Vaccine Development

  • Keyvani, Hossein;Fazlalipour, Mehdi;Monavari, Seyed Hamid Reza;Mollaie, Hamid Reza
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.12
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    • pp.5917-5935
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    • 2012
  • Background: Hepatitis C virus (HCV) causes acute and chronic human hepatitis infection and as such is an important global health problem. The virus was discovered in the USA in 1989 and it is now known that three to four million people are infected every year, WHO estimating that 3 percent of the 7 billion people worldwide being chronically infected. Humans are the natural hosts of HCV and this virus can eventually lead to permanent liver damage and carcinoma. HCV is a member of the Flaviviridae family and Hepacivirus genus. The diameter of the virus is about 50-60 nm and the virion contains a single-stranded positive RNA approximately 10,000 nucleotides in length and consisting of one ORF which is encapsulated by an external lipid envelope and icosahedral capsid. HCV is a heterogeneous virus, classified into 6 genotypes and more than 50 subtypes. Because of the genome variability, nucleotide sequences of genotypes differ by approximately 31-34%, and by 20-23% among subtypes. Quasi-species of mixed virus populations provide a survival advantage for the virus to create multiple variant genomes and a high rate of generation of variants to allow rapid selection of mutants for new environmental conditions. Direct contact with infected blood and blood products, sexual relationships and availability of injectable drugs have had remarkable effects on HCV epidemiology. Hundreds of thousands of people die each year from hepatitis and liver cancer caused by HCV virus infection. Approximately 80% of patients with acute hepatitis C progress into a chronic disease state leading to serious hepatic disorders, 10-20% of which develop chronic liver cirrhosis and hepatocellular carcinoma. The incubation period of HCV is 6-8 weeks and the infection is often asymptomatic so it is very hard to detect at early stages, making early treatment very difficult. Therefore, hepatitis C is called a "silent disease". Neutralizing antibodies are produced against several HCV proteins during infection but the virus mutates to escape from antibodies. Some patients with chronic hepatitis C may have some symptoms such as fatigue, muscle aches, nausea and pain. Autoimmune and immunecomplex-mediated diseases have also been reported with chronic HCV infection.

Pepper Blight Disease Inhibition Metagenome Clone Screening Using Soil Metagenome Library (토양 Metagenome Library로부터 고추역병 저해 클론 탐색)

  • Park, Hae-Chul;Sung, So-Ra;Kim, Dong-Gwan;Koo, Bon-Sung;Jeong, Byeong-Moon;Kim, Jin-Heung;Yoon, Moon-Young
    • Korean Journal of Microbiology
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    • v.45 no.2
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    • pp.228-231
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    • 2009
  • We have purified Phytophthora capsici alpha and beta tubulin from Escherchia coli BL21(DE3). The recombinant alpha and beta tubulins were assembled into microtubule in vitro with specific conditions. The metagenome library was isolated from soil in the Mt. Yeo-Ki, Suwon, Korea and manufactured with the method mentioned in experiment contents for in vitro screening of microtubule assembly screening. FRET effect was used for microtubule assembly inhibitor screening with metagenome library. We got 2 metagenome clones from in vitro screening, and these 2 hit clones showed P. capsici growth inhibition activity on the growing pepper plants. These results suggest that new development of potent inhibitor for pepper blight disease and new approach to prevention of pepper blight disease.

A New Bioluminescent Rat Prostate Cancer Cell Line: Rapid and Accurate Monitoring of Tumor Growth (효과적인 항암효능측정을 위한 발광 전립선 세포의 개발 및 평가)

  • Lee, Mi-Sook;Jung, Jae-In;Kwon, Seung-Hae;Shim, In-Sop;Hahm, Dae-Hyun;Han, Jeong-Jun;Han, Dae-Seok;Yoonpark, Jung-Han;Her, Song
    • Journal of Life Science
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    • v.20 no.11
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    • pp.1738-1741
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    • 2010
  • Caliper measurements of tumor volume have been widely used in the assessment of tumors in animal models. However, experiments based on caliper data have resulted in unreliable estimates of tumor growth, due to necrotic areas of tumor mass. To overcome this systematic bias, we engineered a new luciferase-expressing rat prostate cancer cell line (MLL-Luc) that produces bioluminescence from viable cancer cells. MLL-Luc cells showed a strong correlation between bioluminescence intensity and cell number ($R^2$=0.99) and also accurately quantified tumor growth, with reduced bioluminescence signals caused by necrotic cells in a subcutaneous MLL-Luc xenograft model. The accurate quantification of tumor growth with bioluminescence imaging (BLI) was confirmed by a better antitumor effect of combination chemotherapy, compared to that based on caliper measurements with a correlation between the bioluminescence signal and tumor volume ($R^2$=0.84). These data suggest that bioluminescent MLL xenografts are a powerful and quantitative tool for monitoring tumor growth and are useful in evaluating the efficacy of anticancer drugs, with less systematic bias.

The Clinical Characteristics and Outcomes of Short-term Treatment in Patients with Recurrent Pulmonary Tuberculosis (한 대학병원에서 반복성 폐결핵 환자의 임상적 특성과 6개월 단기요법의 치료 성적)

  • Yoo, Seung Soo;Kwon, Jee Suk;Kang, Yeh Rim;Lee, Jeong Woo;Cha, Seung Ick;Park, Jae Yong;Jung, Tae Hoon;Kim, Chang Ho
    • Tuberculosis and Respiratory Diseases
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    • v.64 no.5
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    • pp.341-346
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    • 2008
  • Background: Recurrent pulmonary tuberculosis (TB) can be due to relapse of the original infecting strain or due to reinfection with a new strain of Mycobacterium tuberculosis. We investigated the clinical characteristics and efficacy of short-term treatment (6 months) in patients with recurrent pulmonary TB. Methods: Twenty-nine patients with recurrent pulmonary TB were compared with control patients who received primary treatment for pulmonary TB with respect to drug sensitivity and outcomes of treatment. Results: Most patients with recurrent pulmonary TB (25 cases, 86.2%) recurred more than 2 years after the completion of previous treatment. Twenty-three patients (82.1%) with recurrent pulmonary TB were sensitive to all anti-tuberculous drugs and a ratio was similar to the drug sensitivities observed in control patients. The outcomes of short-term treatment in patients with drug-sensitive TB were not significantly different between the two groups. Conclusion: Recurrent pulmonary TB in the study area was likely due to reinfection with new strains. Thus the short-term treatment of patients with drug-sensitive recurrent pulmonary TB may be successful.

Synthesis, Magneto-Spectral, Electrochemical, Thermal Characterization and Antimicrobial Investigations of Some Nickel(II) Complexes of Hydrazones of Isoniazid (Isoniazid의 hydrazone을 갖는 몇 가지 니켈(II) 착물들의 합성, 자기적 및 전기적 성질, 열적 특성과 항균성에 대한 연구)

  • Prasad, Surendra;Agarwal, Ram K.
    • Journal of the Korean Chemical Society
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    • v.53 no.6
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    • pp.683-692
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    • 2009
  • The synthesis of a novel series of nickel(II) complexes with new ligands derived from hydrazones of isoniazid have been reported in present work. The complexes have general compositions [$Ni(L)_2X_2$] or $[Ni(L)_3](ClO_4)_2$ {L = N-isonicotinamido-furfuraldimine (INH-FFL), N-isonicotinamido-3',4',5'-trimethoxybenzaldimine (INH-TMB) or N-isonicotinamido-cinnamalidene (INH-CIN) and X = $Cl^-$, ${NO_3}^-$, $ NCS^-$ or $CH_3COO^-$}. The ligands hydrazones behave as neutral bidentates (N and O donor) through the carbonyl oxygen and azomethine nitrogen. The new complexes with octahedral geometry have been characterized by elemental analysis, molecular weight determinations, magnetic susceptibility/moment, thermogravimetric, electrochemical and spectroscopic studies viz. infrared and electronic spectra. On the basis of conductivity measurements in nitrobenzene ($PhNO_2$) solution the [$Ni(L)_2X_2$] and $[Ni(L)_3](ClO_4)_2$ complexes have been found to be non-electrolytes and 1:2 electrolytes, respectively. Thermal properties have also been investigated, which support the geometry of the complexes. Antibacterial and antifungal properties of nickel(II) complexes and few standard drugs have also been examined and it has been observed that the complexes have moderate antibacterial activities.

In vitro Anti-Cancer Effect of Wellness-Compound (Ochnaflavone) (In vitro 웰니스 화합물 (Ochnaflavone)에 의한 암세포 성장 저해)

  • Lee, Jae-Sook;Choi, Hwa-Jung;Kim, Myung-Ju;Park, Jang-Soon
    • Journal of Digital Convergence
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    • v.13 no.5
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    • pp.337-344
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    • 2015
  • Medicinal plants containing wellness-fusion-complex compound are increasingly being pursued as suitable alternative sources of various biological properties. In this study, inhibitory effect of Quintinia acutifolia, which is a New Zealand plant, on P388 murine lymphocytic leukemia cells using MTT [3-(4,5-dimethylthiazol-2-yl)- 2,5-diphenyl-tetrazolium bromide] assay. Based on $^1H-NMR$, $^{13}C-NMR$ spectral data and other spectral analysis, 2,3,2'',3''-tetrahydroochanaflavone (1) and 2'',3''-dihydroochana-flavone (3) inhibited the leukemia cells were purified from the plants. 2,3,2'',3''-tetrahydroochanaflavone (1) and 2'',3''-dihydroochana-flavone (3) are biflavonoids possessing two basic flavonoids and actively inhibited growth of P388 murine lymphocytic leukemia cells with a 50% inhibitory concentration ($IC_{50}$) of $8.2{\mu}g/mL$ and $3.1{\mu}g/mL$, respectively. Specially, 2'',3''-dihydroochana-flavone (3) possessed unconjugated flavonone system, which isn't consist of a pair with B ring of 2,3,2'',3''-tetrahydroochanaflavone (1). Therefore, the two compounds could be considered as a candidate for development of anticancer drugs and need to much studies in the future.