• Title/Summary/Keyword: Metabolic stability

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Evaluation of Metabolic Stability of Kinsenoside, an Antidiabetic Candidate, in Rat and Human Liver Microsomes

  • Rehman, Shaheed Ur;Kim, n Sook;Choi, Min Sun;Luo, Zengwei;Yao, Guangming;Xue, Yongbo;Zhang, Yonghui;Yoo, Hye Hyun
    • Mass Spectrometry Letters
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    • v.6 no.2
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    • pp.48-51
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    • 2015
  • Kinsenoside is a principle bioactive compound of Anoectochilus formosanus. It exhibits various pharmacological effects such as antihyperglycemic, antioxidant, anti-inflammatory, immunostimulating, and hepatoprotective activities and has recently been developed as an antidiabetic drug candidate. In this study, as part of an in vitro pharmacokinetic study, the stability of kinsenoside in rat and human liver microsomes was evaluated. Kinsenoside was found to have good metabolic stability in both rat and human liver microsomes. These results will provide useful information for further in vivo pharmacokinetic and metabolism studies.

Secretory Expression, Functional Characterization, and Molecular Genetic Analysis of Novel Halo-Solvent-Tolerant Protease from Bacillus gibsonii

  • Deng, Aihua;Zhang, Guoqiang;Shi, Nana;Wu, Jie;Lu, Fuping;Wen, Tingyi
    • Journal of Microbiology and Biotechnology
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    • v.24 no.2
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    • pp.197-208
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    • 2014
  • A novel protease gene from Bacillus gibsonii, aprBG, was cloned, expressed in B. subtilis, and characterized. High-level expression of aprBG was achieved in the recombinant strain when a junction was present between the promoter and the target gene. The purified recombinant enzyme exhibited similar N-terminal sequences and catalytic properties to the native enzyme, including high affinity and hydrolytic efficiency toward various substrates and a superior performance when exposed to various metal ions, surfactants, oxidants, and commercial detergents. AprBG was remarkably stable in 50% organic solvents and retained 100% activity and stability in 0-4 M NaCl, which is better than the characteristics of previously reported proteases. AprBG was most closely related to the high-alkaline proteases of the subtilisin family with a 57-68% identity. The secretion and maturation mechanism of AprBG was dependent on the enzyme activity, as analyzed by site-directed mutagenesis. Thus, when taken together, the results revealed that the halo-solvent-tolerant protease AprBG displays significant activity and stability under various extreme conditions, indicating its potential for use in many biotechnology applications.

Enzymatic Synthesis of Ascorbic Acid Fructoside by Transfructosylation Using Levan Fructotransferase

  • LEE CHOONG YEUL;KIM KI HO;HUR SUN YEON;HEO JOO-HYUNG;CHOI MIN HO;RHEE SANG KI;KIM CHUL HO
    • Journal of Microbiology and Biotechnology
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    • v.16 no.1
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    • pp.64-67
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    • 2006
  • To enhance the stability of ascorbic acid, the glycosylation of ascorbic acid was studied using the transfructosylation activity of levan fructotransferase. When levan was used as glycosyl donor, a novel fructoside (ascorbic acid 2-ffuctoside) was formed by the transfructosylation activity of the levan fructotransferase. The production of ascorbic acid 2-fructoside was highly affected by the concentration of the fructosyl acceptor (ascorbic acid). When $35\%$ of ascorbic acid and $2\%$ of levan were incubated with LFTase of 0.5 unit/glevan at $37^{\circ}C$ for 85 h, a maximum 52 g/l of AA-2F was produced.

Rapid Analysis of Metabolic Stability and Structure of Metabolites in New Drug Development

  • Kim, Dong-Hyun
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.86-87
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    • 2002
  • Recent technological innovations in the drug discovery process such as combinatorial synthesis and high throughput screening have led to the identification of an increasingly large number of compounds at the hits-to-leads stage. Therefore, rapid and precise pharmacokinetic/metabolic screening is essential to enhance the tractability of selected leads and to minimize the risk of failure in the later stages of drug development. (omitted)

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Screening and Characterization of a Novel Cellulase Gene from the Gut Microflora of Hermetia illucens Using Metagenomic Library

  • Lee, Chang-Muk;Lee, Young-Seok;Seo, So-Hyeon;Yoon, Sang-Hong;Kim, Soo-Jin;Hahn, Bum-Soo;Sim, Joon-Soo;Koo, Bon-Sung
    • Journal of Microbiology and Biotechnology
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    • v.24 no.9
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    • pp.1196-1206
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    • 2014
  • A metagenomic fosmid library was constructed using genomic DNA isolated from the gut microflora of Hermetia illucens, a black soldier fly. A cellulase-positive clone, with the CS10 gene, was identified by extensive Congo-red overlay screenings for cellulase activity from the fosmid library of 92,000 clones. The CS10 gene was composed of a 996 bp DNA sequence encoding the mature protein of 331 amino acids. The deduced amino acids of CS10 showed 72% sequence identity with the glycosyl hydrolase family 5 gene of Dysgonomonas mossii, displaying no significant sequence homology to already known cellulases. The purified CS10 protein presented a single band of cellulase activity with a molecular mass of approximately 40 kDa on the SDS-PAGE gel and zymogram. The purified CS10 protein exhibited optimal activity at $50^{\circ}C$ and pH 7.0, and the thermostability and pH stability of CS10 were preserved at the ranges of $20{\sim}50^{\circ}C$ and pH 4.0~10.0. CS10 exhibited little loss of cellulase activity against various chemical reagents such as 10% polar organic solvents, 1% non-ionic detergents, and 0.5 M denaturing agents. Moreover, the substrate specificity and the product patterns by thin-layer chromatography suggested that CS10 is an endo-${\beta}$-1,4-glucanase. From these biochemical properties of CS10, it is expected that the enzyme has the potential for application in industrial processes.

Effects of an Agro-Healing Activity Program on the Physiological Condition of Adults with Chronic Metabolic Diseases

  • Jang, Hye Sook;Yoo, Eunha;Jeong, Sun-Jin;Kim, Jae Soon;Ryu, Doo Young
    • Journal of People, Plants, and Environment
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    • v.22 no.4
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    • pp.355-364
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    • 2019
  • This study was conducted to find out the effects of agro-healing activities and strolling on the physiological conditions of patients with chronic metabolic diseases. A total of 11 subjects participated in agro-healing activities, and their average age was 49.6±11.3. Changes in their salivary cortisol were compared and analyzed before and after participating in the agro-healing activity program, and it was found that the stress hormone decreased after participating in the program. Differences in brain wave between before and after participating in agro-healing activities and strolling were measured, and the ratio of alpha to high beta (RAHB) of subjects increased in most of the measured points after participating in agro-healing activities. In addition, the increase in the value in the temporal lobe (T3) that controls mortor skills and occipital lobe (O2) that controls visual functions indicates that the activities were effective in improving relaxation and stability. The relative low beta (RLB) power spectrum of subjects also statistically significantly decreased in the right occipital lobe (O2) that controls visual functions, the relative mid beta (RMB) and relative high beta (RHB) power spectrum decreased in the left temporal lobe (T3) and the right occipital lobe (O2). These results indicate that the activities were effective in improving relaxation under no stress and tension. The systolic and diastolic blood pressure of subjects after participating in agro-healing activities decreased from the prehypertension level to the normal level. These results indicate that horticultural activities and visual elements in healing farms, such as agro-healing activities and strolling, have positive impacts on patients with chronic metabolic diseases accompanied with diabetes or high blood pressure by increasing the brain activity and psycho-physiological conditions of participants.

Modulation of the Somatotropic Axis in Periparturient Dairy Cows

  • Kim, Jin Wook
    • Asian-Australasian Journal of Animal Sciences
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    • v.27 no.1
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    • pp.147-154
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    • 2014
  • This review focuses on modulation of growth hormone (GH) and its downstream actions on periparturient dairy cows undergoing physiological and metabolic adaptations. During the periparturient period, cows experience a negative energy balance implicating that the feed intake does not meet the total energy demand for the onset of lactation. To regulate this metabolic condition, key hormones of somatotropic axis such as GH, IGF-I and insulin must coordinate adaptations required for the preservation of metabolic homeostasis. The hepatic GHR1A transcript and GHR protein are reduced at parturition, but recovers on postpartum. However, plasma IGF-I concentration remains low even though hepatic abundance of the GHR and IGF-I mRNA return to pre-calving value. This might be caused by alternation in IGFBPs and ALS genes, which consequently affect the plasma IGF-I stability. Plasma insulin level declines in a parallel manner with the decrease in plasma IGF-I after parturition. Increased GH stimulates the lipolytic effects and hepatic glucose synthesis to meet the energy requirement for mammary lactose synthesis, suggesting that GH antagonizes insulin-dependent glucose uptake and attenuates insulin action to decrease gluconeogenesis.