• Tuberculosis and Respiratory Diseases
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• v.74 no.3
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• pp.129-133
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• 2013

The presence of epidermal growth factor receptor (EGFR ) mutation is a prognostic and predictive marker for EGFR-tyrosine kinase inhibitor (TKI) therapy. However, inevitably, relapse occurs due to the development of acquired resistance, such as T790M mutation. We report a case of repeated responses to EGFR-TKIs in a never-smoked woman with adenocarcinoma. After six cycles of gemcitabine and cisplatin, the patient was treated by gefitinib for 4 months until progression. Following the six cycles of third-line pemetrexed, gefitinib retreatment was initiated and continued with a partial response for 6 months. After progression, she was recruited for an irreversible EGFR inhibitor trial, and the time to progression was 11 months. Although EGFR direct sequencing on the initial diagnostic specimen revealed a wild-type, we performed a rebiopsy from the progressed subcarinal node at the end of the trial. The result of peptide nucleic acid clamping showed L858R/L861Q.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.42 no.3
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• pp.285-295
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• 2016

To investigate the effect of dietary fiber from mozuku, Cladosiphon novae-caledoniae kylin (C. novae-caledoniae kylin) on the skin care, we measured anti-oxidant activity, anti-microbial activities, tyrosinase activity inhibition and elastic activity. B16F10 melanoma cell (MTT assay) were used to measure cell viability. MC and MI exhibited in vitro antibacterial activity against Staphyloccus aureus (S. aureus) and MRSA without antifungal activity. Mozuku extract (MS) showed excellent tyrosinase inhibition effect compared to arbutin as a positive control (to 49% for tyrosine). The wrinkle-improving effect was relatively low. However, wrinkle-improving effect was relatively low. DPPH free radical scavenging activity was 89% in a concentrations at $500{\mu}g/mL$. These results indicate that the mozuku extracts may be an effective cosmetic ingredient for skin whitening.

• Clinical and Experimental Reproductive Medicine
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• v.49 no.2
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• pp.93-100
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• 2022

Objective: The impact of imatinib, a tyrosine kinase inhibitor, on ovarian follicles and several proteins related to follicular function and apoptosis was investigated in mice. Methods: Saline, cyclophosphamide (Cp; 50 or 75 mg/kg), or imatinib (7.5 or 15 mg/kg) was injected once intraperitoneally into female B6D2F1 mice (18 mice in each group). In multiple ovarian sections, the number of various types of follicles and the proportion of good-quality (G1) follicles were counted. The levels of six proteins (anti-Müllerian hormone [AMH], BCL-xL, BAX, acid sphingomyelinase [A-SMase], caspase-3, and α-smooth muscle actin [α-SMA]) within the whole ovaries were quantified using Western blots. Results: Compared to the saline group, a significant reduction of the primordial follicle count was observed in the group treated with imatinib 7.5 and 15 mg/kg, as well as in the group treated with Cp 75 mg/kg. Administration of Cp significantly decreased the proportion of G1 primordial follicles, but administration of imatinib did not. No differences in the AMH, anti-apoptotic BCLX-L, pro-apoptotic BAX, and A-SMase levels in the ovarian tissues were observed among the five groups. However, caspase-3 and α-SMA levels were significantly higher in the imatinib and Cp groups than in the saline group. Conclusion: The administration of imatinib to mice significantly reduced the primordial follicle count and increased the protein levels of caspase-3 and α-SMA. Our findings suggest that imatinib potentially exerts ovarian toxicity via apoptotic processes, similarly to Cp.

• Proceedings of the Korean Society of Applied Pharmacology
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• 2003.11a
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• pp.70-70
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• 2003

Estrogen receptor is a ligand-activated transcription factor. Its action depends on the receptor, its ligand, and its coactivator proteins. As a consequence, the concentration of the receptor is a major component that governs the magnitude of the estrogen response. Despite the extensive knowledge on mechanism of estrogen receptor action, regulation of estrogen receptor itself is not very well understood. Estrogen receptor is known to be downregulated under hypoxia leading to inhibition of estrogen receptor mediated transcription activation. We have studied mechanism of loss of estrogen responsiveness under hypoxia. We found that Hif-l${\alpha}$, a major transcription factor regulating hypoxic response, inhibited transcription of estrogen response element driven luciferase gene by expression of HIF-l${\alpha}$/vp16 construct designed to contain transcription activity under normoxia. This loss of estrogen responsiveness appears to be the result of ER${\alpha}$ downregulation. ER${\alpha}$was downregulated at the levels of ligand-biding and protein within l2-24h, and the response was blocked by the proteasome inhibitor MG132, protein synthesis inhibitor cyclohexamide, and tyrosine kinase inhibitor Genistein. These results demonstrate that Hif-l${\alpha}$ downregulates ER${\alpha}$ by proteasome dependent pathway.

• Korean Journal of Pharmacognosy
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• v.52 no.2
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• pp.77-83
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• 2021

The number of people suffering from diabetes have been increased around the world. In this study, we investigated the antidiabetic and antioxidant effects of Anthriscus sylvestris(L.) Hoffm and its main compounds. It was divided into root(R) and aerial part(AP) for comparative analysis. Total polyphenol, total flavonoid content was higher in AP extract, but nodakenin content was higher in R(1169.13 ± 6.00 mg/g) extract. Antioxidant activity was also higher in AP extract. To compare antidiabetic efficacy, we analyzed the effects of R and AP extracts on ɑ-glucosidase inhibition(AGI), dipeptidyl peptidase-4(DPP-4) and protein tyrosine phosphatase(PTP)1B activity. R and AP extracts showed similar effects on AGI and DPP-4 activity in a concentration dependent manner, and there was no effect on PTP1B activation. Glucose uptake(139.51 ± 3.19%) in 3T3-L1 cells was more effective in the AP extract-treated group than the positive control, rosiglitazone, group. Both R and AP extracts were effective in protecting against pancreatic beta cell damage caused by hyperglycemia. These results suggest that Anthriscus sylvestris(L.) Hoffm. could be used as a candidate for diabetes treatment.

• The Korean Journal of Malacology
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• v.19 no.2
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• pp.95-106
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• 2003

The compositions of amino acid in 6 monocultured benthic diatoms used in aquaculture of Haliotis discus hannai were analyzed, and effects of 15 artificial synthetic amino acids on the settlement and metamorphosis of H. discus hannai larvae. Results showed that the content of L-aspartic acid was highest in all diatoms, and that of L-glutamic acid was second high. In experiment using settlement slat without benthic diatom attached, the highest settlement rate (33.3 ${\pm}$ 8.8%) was obtained with L-glutamic acid, and a higher value (16.7 ${\pm}$ 3.3%) was found with L-aspartic acid at 24 h after experimental commencement, compared to that of control (8.6 ${\pm}$ 5.1%). 80 h later the metamorphosis rates of L-glutamic acid (86.7 ${\pm}$ 10.7%) and L-aspartic acid (80.0 ${\pm}$ 3.3%) groups were higher than control group(0) and other amino acids significantly. The response rate of L-glutamic acid was the highest (62.0%), and those of L-aspartic acid (30.0%) and L-threonine (25.3%) groups were also significantly higher than control group. In the experiment using settlement slat with benthic diatom attached, the best effect of various amino acids on induction of larval settlement was obtained with L-glutamic (82.0 ${\pm}$ 6.9%) and L-aspartic acid (78.7 ${\pm}$ 5.1%) at 24 h after experimental commencement. The settlement rates of L-histidine, L-leucine, L-lysine, L-methionine, L-phenylalanine, and L-tyrosine groups were significantly lower than control group. The same differences in the metamorphosis rate at 56 h after experimental commencement and in the response rate were found. It should be noted that after 80 h the metamorphosis rates of L-histidine (74.0 ${\pm}$ 12.0%) and L-lysine (87.0 ${\pm}$ 8.8%) declined rapidly compared to those of 56 h (8.0 ${\pm}$ 12.0%; 7.7 ${\pm}$ 12.0%).

• Asian-Australasian Journal of Animal Sciences
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• v.32 no.5
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• pp.614-628
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• 2019

Objective: The inhibitory leukocyte immunoglobulin-like receptors (LILRBs) play an important role in innate immunity. The present study represents the first description of the cloning and structural and functional analysis of LILRB1 and LILRB3 isolated from two genetically disparate chicken lines. Methods: Chicken LILRB1-3 genes were identified by bioinformatics approach. Expression studies were performed by transfection, quantitative polymerase chain reaction. Signal transduction was analyzed by western blots, immunoprecipitation and flow cytometric. Cytokine levels were determined by enzyme-linked immunosorbent assay. Results: Amino acid homology and phylogenetic analyses showed that the homologies of LILRB1 and LILRB3 in the chicken line 6.3 to those proteins in the chicken line 7.2 ranged between 97%-99%, while homologies between chicken and mammal proteins ranged between 13%-19%, and 13%-69%, respectively. Our findings indicate that LILRB1 and LILRB3 subdivided into two groups based on the immunoreceptor tyrosine-based inhibitory motifs (ITIM) present in the transmembrane domain. Chicken line 6.3 has two ITIM motifs of the sequence LxYxxL and SxYxxV while line 7.2 has two ITIM motifs of the sequences LxYxxL and LxYxxV. These motifs bind to SHP-2 (protein tyrosine phosphatase, non-receptor type 11) that plays a regulatory role in immune functions. Moreover, our data indicate that LILRB1 and LILRB3 associated with and activated major histocompatibility complex (MHC) class I and ${\beta}2-microglobulin$ and induced the expression of transporters associated with antigen processing, which are essential for MHC class I antigen presentation. This suggests that LILRB1 and LILRB3 are transcriptional regulators, modulating the expression of components in the MHC class I pathway and thereby regulating immune responses. Furthermore, LILRB1 and LILRB3 activated Janus kinase2/tyrosine kinase 2 (JAK2/TYK2); signal transducer and activator of transcription1/3 (STAT1/3), and suppressor of cytokine signaling 1 genes expressed in Macrophage (HD11) cells, which induced Th1, Th2, and Th17 cytokines. Conclusion: These data indicate that LILRB1 and LILRB3 are innate immune receptors associated with SHP-2, MHC class I, ${\beta}2-microglobulin$, and they activate the Janus kinase/signal transducer and activator of transcription signaling pathway. Thus, our study provides novel insights into the regulation of immunity and immunopathology.

• Journal of Microbiology and Biotechnology
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• v.27 no.5
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• pp.975-982
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• 2017

Curcumin, a hydrophobic polyphenol derived from the rhizome of the herb Curcuma longa, possesses diverse pharmacological properties, including anti-inflammatory, antioxidant, antiproliferative, and antiangiogenic activities. Two curcuminoids (dicinnamoylmethane and bisdemethoxycurcumin) were synthesized from glucose in Escherichia coli. PAL (phenylalanine ammonia lyase) or TAL (tyrosine ammonia lyase), along with Os4CL (p-coumaroyl-CoA ligase) and CUS (curcumin synthase) genes, were introduced into E. coli, and each strain produced dicinnamoylmethane or bisdemethoxycurcumin, respectively. In order to increase the production of curcuminoids in E. coli, the shikimic acid biosynthesis pathway, which increases the substrates for curcuminoid biosynthesis, was engineered. Using the engineered strains, the production of bisdemethoxycurcumin increased from 0.32 to 4.63 mg/l, and that of dicinnamoylmethane from 1.24 to 6.95 mg/l.

• Journal of the Korean Chemical Society
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• v.14 no.2
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• pp.161-168
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• 1970

In order to obtain the more effective evidence, supporting the hypothesis which have been previously described by former report that pepsin (EC 3.4. 4.1) forms a hydrophobic bond with the nonpolar side chain of its substrate, the inhibitory effect of carboxylic acids(from formic acid to iso-butyric acid) on the activity of pepsin to the synthetic dipeptide, N-Carbobenzoxy-L-glutamyl-L-tyrosine, was discussed. The kinetic study showed that the inhibition by carboxylic acids was competitive. The Kidecreased with increasing size of the inhibitor molecule. The $-{\Delta}F^{\circ}$increased linearly with increasing number of carbon atoms in the hydrocarbon chain of the inhibitor. It was confirmed that the hydrophobic bond between more than one side chain of amino acid residues(phenylalanine) in the binding region of the active center of pepsin and the side chain of amino acid residues in the substrate was formed as the first step of its enzymic mechanism. The inhibitory effect of carboxylic acids was due to the competition of the hydrocarbon group of the carboxylic acids with the side chain of the substrate for the hydrophobic binding site(the side chain of phenylalanine) of the pepsin.

• Korean Journal Plant Pathology
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• v.14 no.6
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• pp.689-692
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• 1998

Bacterial species isolated from common scab lesion on potato (Solanum tuberosum L. cv. Dejima) was identified as Streptomyces acidiscabies. This organism had flexuous spore chains and white spore mass color, produced melanin pigment on tyrosine agar medium but did not produce on peptone agar medium. S. acidiscabies grew on agar medium at pH 4.0, used L-arabinose, D-fructose, D-glucose, D-mannitol, rhamnose, sucrose, D-xylose and meso-inositol except reffinose as carbon sources. It was also susceptible to thallium acetate (10 $\mu\textrm{g}$/ml, 100$\mu\textrm{g}$/ml), phenol (0.1%, wt/vol), streptomycin (20 $\mu\textrm{g}$/ml), and was resistant to 7% NaCl, crystal violet (0.5 $\mu\textrm{g}$/ml), penicillin (10 IU/ml) and oleandomycin (25 $\mu\textrm{g}$/ml, 100 $\mu\textrm{g}$/ml).