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1.
Entropy (Basel) ; 25(3)2023 Mar 16.
Article in English | MEDLINE | ID: mdl-36981401

ABSTRACT

Text-to-SQL is a task that converts natural language questions into SQL queries. Recent text-to-SQL models employ two decoding methods: sketch-based and generation-based, but each has its own shortcomings. The sketch-based method has limitations in performance as it does not reflect the relevance between SQL elements, while the generation-based method may increase inference time and cause syntactic errors. Therefore, we propose a novel decoding method, Hybrid decoder, which combines both methods. This reflects inter-SQL element information and defines elements that can be generated, enabling the generation of syntactically accurate SQL queries. Additionally, we introduce a Value prediction module for predicting values in the WHERE clause. It simplifies the decoding process and reduces the size of vocabulary by predicting values at once, regardless of the number of conditions. The results of evaluating the significance of Hybrid decoder indicate that it improves performance by effectively incorporating mutual information among SQL elements, compared to the sketch-based method. It also efficiently generates SQL queries by simplifying the decoding process in the generation-based method. In addition, we design a new evaluation measure to evaluate if it generates syntactically correct SQL queries. The result demonstrates that the proposed model generates syntactically accurate SQL queries.

2.
Mitochondrial DNA B Resour ; 7(4): 580-582, 2022.
Article in English | MEDLINE | ID: mdl-35386626

ABSTRACT

Citrus erythrosa (Dongjeongkyool in Korean) is a medicinal citrus landrace that grows in Korea. In this study, we characterized the complete chloroplast (Cp) genome (160,120 bp) of C. erythrosa. The Cp genome was consisted of 4 distinct regions: a large single copy (87,731 bp), a small single copy (18,393 bp), and a pair of inverted repeat regions (26,998 bp). The Cp genome encodes a total of 133 genes including 88 protein-coding genes, 37 tRNA genes and 8 rRNA genes. The phylogenetic analysis reveals that C. erythrosa is a sister group to the clade of species including C. reticulata within the genus Citrus.

3.
Nutrients ; 12(3)2020 Mar 01.
Article in English | MEDLINE | ID: mdl-32121602

ABSTRACT

Non-alcoholic fatty liver disease (NAFLD) is prevalent in the elderly population, and has symptoms ranging from liver steatosis to advanced fibrosis. Citrus peel extracts (CPEs) contain compounds that potentially improve dyslipidemia; however, the mechanism of action and effects on hepatic steatosis regulation remains unclear. Current study was aimed to investigate the protective effect of CPEs extracted through hot-air drying (CPEW) and freeze-drying (CPEF) and the underlying mechanism in a rat model of high-fat diet-induced NAFLD. The high-fat diet (HFD)-fed rats showed significant increase in total cholesterol, alanine aminotransferase (ALT), triglycerides, aspartate aminotransferase (AST), and lipid peroxidation compared to the normal chow-diet (NCD) group rats; but CPEW and CPEF limited this effect. CPEW and CPEF supplementation reduced both hepatocyte steatosis and fat accumulation involving the regulatory effect of mTORC1. Collectively, CPEW and CPEF protected deterioration of liver steatosis with AMPK activation and regulating ROS accumulation associated with interstitial disorders, which are also associated with endoplasmic reticulum (ER) redox. Thus, the application of CPEW and CPEF may lead to the development of novel therapeutic or preventive agents against NAFLD.


Subject(s)
AMP-Activated Protein Kinases/metabolism , Citrus/chemistry , Liver/drug effects , Non-alcoholic Fatty Liver Disease/prevention & control , Plant Extracts/administration & dosage , Animals , Diet, High-Fat/adverse effects , Disease Models, Animal , Endoplasmic Reticulum/drug effects , Endoplasmic Reticulum/metabolism , Freeze Drying , Humans , Lipid Metabolism/drug effects , Liver/metabolism , Liver/pathology , Male , Non-alcoholic Fatty Liver Disease/etiology , Non-alcoholic Fatty Liver Disease/metabolism , Non-alcoholic Fatty Liver Disease/pathology , Oxidation-Reduction/drug effects , Plant Extracts/isolation & purification , Rats , Reactive Oxygen Species/metabolism , Signal Transduction/drug effects
4.
Article in English | MEDLINE | ID: mdl-30327679

ABSTRACT

OBJECTIVES: Several experimental studies have reported antiobesity and lipid-improving effects of Citrus unshiu. However, clinical studies on its effects are lacking. This study was designed to evaluate the impact of Citrus unshiu peel pellet (CUPP) on obesity and lipid profile. METHODS: For 118 patients with body mass index (BMI) > 23 who took Citrus unshiu peel pellet (CUPP) for 4 weeks in a Public Health Center, laboratory and biometric readings before and after CUPP administration were analyzed. RESULTS: Mean age of these subjects was 53.8±10.6 years (range: 18-75 years). There were 88 (74.6%) females in the study sample (n = 118). A significant (p < 0.01) decrease in BMI from 27.47±2.24 to 27.27±2.22 was observed in all subjects after CUPP treatment and 65.3% (N = 77) of them lost 1.03±0.83 kg of weight after 4 weeks of treatment. Total cholesterol level was significantly (p < 0.01) decreased from 204.0±37.4 mg/dL to 193.5±36.5 mg/dL. Significant (p < 0.05) decreases in levels of low-density lipoprotein, cholesterol, and triglyceride were also observed. CONCLUSIONS: These results suggest that CUPP in practice could help weight control and improve total cholesterol level. Findings of this study provide clinical foundation for future large-scale trials to establish clinical benefits of CUPP.

5.
Nat Prod Commun ; 11(6): 729-32, 2016 Jun.
Article in English | MEDLINE | ID: mdl-27534103

ABSTRACT

A new homomonoterpene, 1,3,3-trimethyl-7-oxabicyclo[3.1.1]hexa-9-en-10-oic acid, named madhusic acid A (1), together with ten known compounds (2-11) were isolated from the methanolic extract of the dried leaves of Madhuca pasquieri (Dubard) H. J. Lam. The structure of the new compound was elucidated on the basis of 1D, 2D NMR (COSY, HMQC, and HMBC) and mass spectral analyses. We examined the effects of the isolated compounds against LPS-induced NO production in macrophage RAW264.7 cells and compound 2 showed effective activity with an IC50 value of 14.5 µM.


Subject(s)
Macrophages/drug effects , Madhuca/chemistry , Monoterpenes/pharmacology , Nitric Oxide/metabolism , Plant Extracts/pharmacology , Animals , Cell Line , Macrophages/metabolism , Magnetic Resonance Spectroscopy , Mice , Molecular Structure , Monoterpenes/chemistry , Plant Extracts/chemistry , Plant Leaves/chemistry , RAW 264.7 Cells
6.
Chem Pharm Bull (Tokyo) ; 64(5): 507-11, 2016.
Article in English | MEDLINE | ID: mdl-27150484

ABSTRACT

Three new sesquiterpenoids, 13-hydroxyl-atractylenolide II (1), 4-ketone-atractylenolide III (2), and eudesm-4(15)-ene-7ß,11-diol (3), along with eleven known compounds (4-14), were isolated from the rhizomes of Atractylodes macrocephala. The structures and relative configurations of 1-3 were determined by analysis of the spectroscopic data, and the absolute configurations of 1 and 2 were assigned by circular dichroism technique. The anti-inflammatory activities of these isolates were evaluated against lipopolysaccharide-induced nitric oxide production in macrophage RAW264.7 cells; compounds 4, 7, and 8 exhibited moderate efficacy with IC50 values of 48.6±0.5, 46.4±3.2, and 32.3±2.9 µM, respectively.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Inflammation/metabolism , Sesquiterpenes/pharmacology , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/isolation & purification , Cells, Cultured , Dose-Response Relationship, Drug , Inflammation/prevention & control , Inhibitory Concentration 50 , Lipopolysaccharides/antagonists & inhibitors , Lipopolysaccharides/pharmacology , Macrophages/drug effects , Macrophages/metabolism , Mice , Molecular Structure , Nitric Oxide/antagonists & inhibitors , Nitric Oxide/biosynthesis , Sesquiterpenes/chemistry , Sesquiterpenes/isolation & purification , Structure-Activity Relationship
7.
Clin Cancer Res ; 21(5): 1139-50, 2015 Mar 01.
Article in English | MEDLINE | ID: mdl-25733708

ABSTRACT

PURPOSE: To determine the pharmacokinetics and the antitumor activity in pediatric cancer models of MM-398, a nanoliposomal irinotecan (nal-IRI). EXPERIMENTAL DESIGN: Mouse plasma and tissue pharmacokinetics of nal-IRI and the current clinical formulation of irinotecan were characterized. In vivo activity of irinotecan and nal-IRI was compared in xenograft models (3 each in nu/nu mice) of Ewing's sarcoma family of tumors (EFT), neuroblastoma (NB), and rhabdomyosarcoma (RMS). SLFN11 expression was assessed by Affymetrix HuEx arrays, Taqman RT-PCR, and immunoblotting. RESULTS: Plasma and tumor concentrations of irinotecan and SN-38 (active metabolite) were approximately 10-fold higher for nal-IRI than for irinotecan. Two doses of NAL-IRI (10 mg/kg/dose) achieved complete responses maintained for >100 days in 24 of 27 EFT-xenografted mice. Event-free survival for mice with RMS and NB was significantly shorter than for EFT. High SLFN11 expression has been reported to correlate with sensitivity to DNA damaging agents; median SLFN11 mRNA expression was >100-fold greater in both EFT cell lines and primary tumors compared with NB or RMS cell lines or primary tumors. Cytotoxicity of SN-38 inversely correlated with SLFN11 mRNA expression in 20 EFT cell lines. CONCLUSIONS: In pediatric solid tumor xenografts, nal-IRI demonstrated higher systemic and tumor exposures to SN-38 and improved antitumor activity compared with the current clinical formulation of irinotecan. Clinical studies of nal-IRI in pediatric solid tumors (especially EFT) and correlative studies to determine if SLFN11 expression can serve as a biomarker to predict nal-IRI clinical activity are warranted.


Subject(s)
Antineoplastic Agents/administration & dosage , Camptothecin/analogs & derivatives , Gene Expression , Liposomes , Nuclear Proteins/genetics , Sarcoma, Ewing/genetics , Sarcoma, Ewing/pathology , Sucrose/analogs & derivatives , Animals , Antineoplastic Agents/pharmacokinetics , Camptothecin/administration & dosage , Camptothecin/pharmacokinetics , Cell Line, Tumor , Disease Models, Animal , Drug Combinations , Female , Humans , Irinotecan , Macrophages/immunology , Macrophages/pathology , Mice , Sarcoma, Ewing/drug therapy , Sarcoma, Ewing/mortality , Sucrose/administration & dosage , Sucrose/pharmacokinetics , Tissue Distribution , Tumor Burden/drug effects , Xenograft Model Antitumor Assays
8.
Bioorg Med Chem Lett ; 25(5): 1129-34, 2015 Mar 01.
Article in English | MEDLINE | ID: mdl-25637363

ABSTRACT

Six new phenolics, scutellariosides A-F (1-3, 5-6, and 8), together with six known compounds (4, 7, 9-12) were isolated from the whole plant of Scutellaria indica (Labiatae). The chemical structures of these compounds were determined by spectroscopic analyses including 2D NMR. Their anti-inflammatory activities were evaluated against LPS-induced NO production in macrophage RAW 264.7 cells. Among them, compounds 10-12 had inhibitory effects with IC50 values ranging from 7.2 to 27.8µM. Compound 12 reduced LPS-induced iNOS expression in a dose-dependent manner.


Subject(s)
Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacology , Macrophages/drug effects , Phenols/chemistry , Phenols/pharmacology , Scutellaria/chemistry , Animals , Anti-Inflammatory Agents/isolation & purification , Cell Line , Flavonoids/chemistry , Flavonoids/isolation & purification , Flavonoids/pharmacology , Lipopolysaccharides/immunology , Macrophages/immunology , Mice , Nitric Oxide/antagonists & inhibitors , Nitric Oxide/immunology , Nitric Oxide Synthase Type II/antagonists & inhibitors , Nitric Oxide Synthase Type II/immunology , Phenols/isolation & purification , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Extracts/pharmacology
9.
Appl Radiat Isot ; 73: 74-8, 2013 Mar.
Article in English | MEDLINE | ID: mdl-23291562

ABSTRACT

The present investigation was carried out with the objective of studying in vivo imaging of 3-iodothyronamine (T(1)AM) compound in mice. A simple and efficient synthesis of [(125)I]-T(1)AM was established, and a molecular imaging study was performed using micro-SPECT/CT at 1h post-injection of [(125)I]-T(1)AM. Imaging studies revealed the activity in the gastrointestinal tract and liver, indicating that [(125)I]-T(1)AM was distributed primarily in the liver, and excreted into the gastrointestinal tract through a bile duct.


Subject(s)
Iodine Radioisotopes , Radiopharmaceuticals/analysis , Thyronines/analysis , Animals , Female , Gastrointestinal Tract/diagnostic imaging , Gastrointestinal Tract/metabolism , Iodine Radioisotopes/chemistry , Liver/diagnostic imaging , Liver/metabolism , Magnetic Resonance Spectroscopy , Mice , Mice, Inbred ICR , Radiopharmaceuticals/chemistry , Specific Pathogen-Free Organisms , Thyronines/chemistry , Tomography, Emission-Computed, Single-Photon/methods
10.
Toxicol Res ; 28(4): 235-40, 2012 Dec.
Article in English | MEDLINE | ID: mdl-24278615

ABSTRACT

(99m)Tc tricarbonyl glycine monomers, trimers, and pentamers were synthesized and evaluated for their radiolabeling and in vivo distribution characteristics. We synthesized a (99m)Tc-tricarbonyl precursor with a low oxidation state (I). (99m)Tc(CO)3(H2O)3 (+) was then made to react with monomeric and oligomeric glycine for the development of bifunctional chelating sequences for biomolecules. Labeling yields of (99m)Tc-tricarbonyl glycine monomers and oligomers were checked by high-performance liquid chromatography. The labeling yields of (99m)Tc-tricarbonyl glycine and glycine oligomers were more than 95%. We evaluated the characteristics of (99m)Tc-tricarbonyl glycine oligomers by carrying out a lipophilicity test and an imaging study. The octanol-water partition coefficient of (99m)Tc tricarbonyl glycine oligomers indicated hydrophilic properties. Single-photon emission computed tomography imaging of (99m)Tc-tricarbonyl glycine oligomers showed rapid renal excretion through the kidneys with a low uptake in the liver, especially of (99m)Tc tricarbonyl triglycine. Furthermore, we verified that the addition of triglycine to prototype biomolecules (AGRGDS and RRPYIL) results in the improvement of radiolabeling yield. From these results, we conclude that triglycine has good characteristics for use as a bifunctional chelating sequence for a (99m)Tc-tricarbonyl- based biomolecular imaging probe.

11.
Arch Pharm Res ; 33(10): 1665-70, 2010 Oct.
Article in English | MEDLINE | ID: mdl-21052942

ABSTRACT

Five flavonoids, myricetin-3'-methylether 3-O-ß-D: -galactopyranoside (1), myricetin-3',5'-dimethylether 3-O-ß-D: -galactopyranoside (2), quercetin (3), kaempferol (4), and tamarixetin (5) were isolated from the buds of Cleistocalyx operculatus (Myrtaceae). The chemical structures of these compounds were determined on the basis of spectroscopic analyses, including 2D NMR. Their anti-Alzheimer effects were evaluated via acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity assays. All five compounds 1-5 showed potential inhibitory activities against AChE with IC(50) values of 19.9, 37.8, 25.9, 30.4 and 22.3 µM, respectively, while compounds 1, 3, 4 and 5 also possessed BChE inhibitory activity with IC(50) values of 152.5, 177.8, 62.5, and 160.6 µM, respectively.


Subject(s)
Cholinesterase Inhibitors/isolation & purification , Cholinesterase Inhibitors/pharmacology , Drug Discovery , Flavonoids/isolation & purification , Flavonoids/pharmacology , Flowers/chemistry , Syzygium/chemistry , Alzheimer Disease/drug therapy , Butyrylcholinesterase , Cholinesterase Inhibitors/chemistry , Flavonoids/chemistry , Galactose/analysis , Galactose/chemistry , Glycosides/chemistry , Glycosides/isolation & purification , Glycosides/pharmacology , Magnetic Resonance Spectroscopy , Molecular Structure , Optical Rotation , Osmolar Concentration , Spectrometry, Mass, Electrospray Ionization , Spectrophotometry, Ultraviolet , Spectroscopy, Fourier Transform Infrared
12.
Biol Pharm Bull ; 31(5): 949-54, 2008 May.
Article in English | MEDLINE | ID: mdl-18451525

ABSTRACT

Ergosterol peroxide (EPO, 1) is a major antitumor sterol produced by edible or medicinal mushrooms. Following oral administration of 1 to rats or anaerobic in vitro incubation of 1 with rat fecal bacteria, three metabolites were detected and their structures were identified to be 5alpha,6alpha-epoxyergosta-8(14),22-diene-3beta,7alpha-diol (M1, 2), 5alpha,6alpha-epoxyergosta-8,22-diene-3beta,7alpha-diol (M2, 3), and 5alpha,6alpha-epoxy-3beta-hydroxyergosta-22-ene-7-one (M3, 4) by spectroscopic analysis. Of these, M2 and M3 showed more potent inhibitory activity than the original compound 1 against proliferation of CACO-2, WiDr, DLD-1 and Colo320 human colorectal adenocarcinoma cells. These findings suggest that bacterial metabolites of EPO play a significant role in its cytotoxic activity against human colorectal cancer cells.


Subject(s)
Bacteria/metabolism , Cytotoxins/metabolism , Ergosterol/analogs & derivatives , Intestines/microbiology , Animals , Caco-2 Cells , Cell Line, Tumor , Chromatography, High Pressure Liquid , Ergosterol/metabolism , Feces/chemistry , Feces/microbiology , Humans , Magnetic Resonance Spectroscopy , Male , Mass Spectrometry , Rats
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