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| WoS | SCOPUS | Document Type | Document Title | Abstract | Authors | Affiliation | ResearcherID (WoS) | AuthorsID (SCOPUS) | Author Email(s) | Journal Name | JCR Abbreviation | ISSN | eISSN | Volume | Issue | WoS Edition | WoS Category | JCR Year | IF | JCR (%) | FWCI | FWCI Update Date | WoS Citation | SCOPUS Citation | Keywords (WoS) | KeywordsPlus (WoS) | Keywords (SCOPUS) | KeywordsPlus (SCOPUS) | Language | Publication Stage | Publication Year | Publication Date | DOI | JCR Link | DOI Link | WOS Link | SCOPUS Link |
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| ○ | ○ | Article | Developing pH-Modulated Spray Dried Amorphous Solid Dispersion of Candesartan Cilexetil with Enhanced In Vitro and In Vivo Performance | Candesartan cilexetil (CC), a prodrug and highly effective antihypertensive agent, is a poorly soluble (BCS Class II) drug with limited bioavailability. Here, we attempted to improve CC's bioavailability by formulating several CC-loaded amorphous solid dispersions with a hydrophilic carrier (PVPK30) and pH modifier (sodium carbonate) using the spray drying technique. Solubility, in vitro dissolution, and moisture content tests were used for screening the optimized formulation. We identified an optimized formulation of CC/PVPK30/SC, which at the ratio of 1:0.5:1 (w/w/w) exhibited a 30,000-fold increase in solubility and a more than 9-fold enhancement in dissolution compared to pure CC. Solid-state characterization revealed that in pH-modulated CC amorphous solid dispersion (CCSDpM), CC's crystallinity was altered to an amorphous state with the absence of undesirable interactions. Stability studies also showed that the optimized formulation was stable with good drug content and drug release under accelerated conditions of up to 4 weeks and real-time stability conditions of up to 12 weeks. Furthermore, pharmacokinetic parameters, such as AUC and C-max of candesartan, had a 4.45-fold and 7.42-fold improvement, respectively, in CCSDpM-treated rats compared to those in the CC-treated rats. Thus, these results suggest that CCSDpM is highly effective for increasing oral absorption. The application of these techniques can be a viable strategy to improve a drug's bioavailability. | Poudel, Surendra; Kim, Dong Wuk | Kyungpook Natl Univ, Res Inst Pharmaceut Sci, BK21 FOUR Community Based Intelligent Novel Drug, Coll Pharm,MRC,Vessel Organ Interact Res Ctr VOIC, Daegu 41566, South Korea | 57218799520; 57193445049 | surendrapoudel1016@gmail.com;dkim17@knu.ac.kr; | PHARMACEUTICS | PHARMACEUTICS | 1999-4923 | 13 | 4 | SCIE | PHARMACOLOGY & PHARMACY | 2021 | 6.525 | 13.8 | 1.1 | 2025-07-30 | 15 | 13 | amorphous solid dispersion; candesartan Cilexetil; PVPK30; pH-modulation; spray drying; bioavailability | Amorphous solid dispersion; Bioavailability; Candesartan Cilexetil; PH-modulation; PVPK30; Spray drying | candesartan hexetil; drug carrier; irbesartan; povidone; sodium carbonate; amorphous solid dispersion; animal experiment; area under the curve; Article; chemical structure; controlled study; differential scanning calorimetry; drug absorption; drug bioavailability; drug blood level; drug delivery system; drug design; drug formulation; drug half life; drug release; drug screening; drug solubility; drug stability; drug structure; elimination rate constant; evaporation; Fourier transform infrared spectroscopy; hydrophilicity; in vitro study; in vivo study; maximum concentration; moisture; nonhuman; pH; plasma concentration-time curve; rat; scanning electron microscopy; single drug dose; spray drying; time to maximum plasma concentration; X ray diffraction | English | 2021 | 2021-04 | 10.3390/pharmaceutics13040497 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | ||||
| ○ | ○ | Article | Dissolution of franchise relationships: Intention, behavior, and the role of uncertainty | Academic research has paid more attention to formation and management of business relationships than to their dissolution. For example, not much is known about the extent to which dissolution intentions are predictive of actual dissolution, and whether certainty with which these intentions are held influences the likelihood of relationship dissolution. To address these questions, authors collect data in two stages from a franchise system in Korea. They specify the judgment uncertainty and magnitude parameters (JUMP) model to tease apart the magnitude and uncertainty of intention from a single measure, and a duration analysis model to study translation of intentions into behavior. Results show that not only strong intentions to dissolve a relationship are more likely to result in actual dissolution but weak intentions also are more likely to lead to dissolution if the holder is doubtful and uncertain about the relationship. Ignoring uncertainty of dissolution intentions thus can seriously downplay their risk of translating into actual dissolution. | Jindal, Rupinder P.; Sivadas, Eugene; Kang, Bohyeon | Univ Washington Tacoma, Milgard Sch Business, 1900 Commerce St, Tacoma, WA 98402 USA; San Francisco State Univ, Lam Family Coll Business, San Francisco, CA 94132 USA; Kyungpook Natl Univ, Sch Business, Daegu 41566, South Korea | Sivadas, Eugene/AAN-6619-2021 | 15848122500; 6505903135; 55221742900 | jindalrp@uw.edu;sivadas@sfsu.edu;bohyeonkang@knu.ac.kr; | INDUSTRIAL MARKETING MANAGEMENT | IND MARKET MANAG | 0019-8501 | 1873-2062 | 92 | SSCI | BUSINESS;MANAGEMENT | 2021 | 8.89 | 13.8 | 0.15 | 2025-07-30 | 7 | 7 | Relationship marketing; Relationship lifecycle; Dissolution; Intention; Behavior; Uncertainty | BUYER-SUPPLIER RELATIONSHIPS; SWITCHING BEHAVIOR; PERCEIVED UNFAIRNESS; DEPENDENCE; TRUST; DETERMINANTS; ANTECEDENTS; POWER; SATISFACTION; OPPORTUNISM | Behavior; Dissolution; Intention; Relationship lifecycle; Relationship marketing; Uncertainty | English | 2021 | 2021-01 | 10.1016/j.indmarman.2020.11.012 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | |||
| ○ | ○ | Article | Effect of Lactic Acid Bacteria on the Pharmacokinetics and Metabolism of Ginsenosides in Mice | This study aims to investigate the effect of lactic acid bacteria (LAB) on in vitro and in vivo metabolism and the pharmacokinetics of ginsenosides in mice. When the in vitro fermentation test of RGE with LAB was carried out, protopanaxadiol (PPD) and protopanaxadiol (PPD), which are final metabolites of ginsenosides but not contained in RGE, were greatly increased. Compound K (CK), ginsenoside Rh1 (GRh1), and GRg3 also increased by about 30%. Other ginsenosides with a sugar number of more than 2 showed a gradual decrease by fermentation with LAB for 7 days, suggesting the involvement of LAB in the deglycosylation of ginsenosides. Incubation of single ginsenoside with LAB produced GRg3, CK, and PPD with the highest formation rate and GRd, GRh2, and GF with the lower rate among PPD-type ginsenosides. Among PPT-type ginsenosides, GRh1 and PPT had the highest formation rate. The amoxicillin pretreatment (20 mg/kg/day, twice a day for 3 days) resulted in a significant decrease in the fecal recovery of CK, PPD, and PPT through the blockade of deglycosylation of ginsenosides after single oral administrations of RGE (2 g/kg) in mice. The plasma concentrations of CK, PPD, and PPT were not detectable without change in GRb1, GRb2, and GRc in this group. LAB supplementation (1 billion CFU/2 g/kg/day for 1 week) after the amoxicillin treatment in mice restored the ginsenoside metabolism and the plasma concentrations of ginsenosides to the control level. In conclusion, the alterations in the gut microbiota environment could change the ginsenoside metabolism and plasma concentrations of ginsenosides. Therefore, the supplementation of LAB with oral administrations of RGE would help increase plasma concentrations of deglycosylated ginsenosides such as CK, PPD, and PPT. | Jeon, Ji-Hyeon; Lee, Jaehyeok; Park, Jin-Hyang; Lee, Chul-Haeng; Choi, Min-Koo; Song, Im-Sook | Kyungpook Natl Univ, Vessel Organ Interact Res Ctr VOICE, BK21 FOUR Community Based Intelligent Novel Drug, Res Inst Pharmaceut Sci,Coll Pharm, Daegu 41566, South Korea; Dankook Univ, Coll Pharm, Cheonan 31116, South Korea | 57204685946; 57219980183; 57267338300; 57219051827; 8695781400; 7201564500 | kei7016@naver.com;here0723@gmail.com;wlsgid1957@naver.com;hang1130@naver.com;minkoochoi@dankook.ac.kr;isssong@knu.ac.kr; | PHARMACEUTICS | PHARMACEUTICS | 1999-4923 | 13 | 9 | SCIE | PHARMACOLOGY & PHARMACY | 2021 | 6.525 | 13.8 | 1.65 | 2025-07-30 | 21 | 24 | red ginseng extract (RGE); lactic acid bacteria (LAB); ginsenoside metabolism; pharmacokinetics | HUMAN INTESTINAL BACTERIA; PANAX-GINSENG; IN-VITRO; RED GINSENG; COMPOUND K; ANTIBIOTIC SUSCEPTIBILITY; PROTEIN-BINDING; DOUBLE-BLIND; BIOTRANSFORMATION; IDENTIFICATION | Ginsenoside metabolism; Lactic acid bacteria (LAB); Pharmacokinetics; Red ginseng extract (RGE) | amoxicillin; compound K; ginseng extract; ginsenoside; ginsenoside Rb 1; ginsenoside Rb 2; ginsenoside Rc; ginsenoside Rd; ginsenoside Rf; ginsenoside Rg 3; ginsenoside Rh 2; ginsenoside Rh1; protopanaxadiol; unclassified drug; animal cell; animal experiment; animal tissue; Article; controlled study; deglycosylation; drug blood level; drug decomposition; drug effect; drug metabolism; ginseng; in vitro study; in vivo study; incubation time; Institute for Cancer Research mouse; intestine flora; lactic acid bacterium; male; mouse; nonhuman | English | 2021 | 2021-09 | 10.3390/pharmaceutics13091496 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | |||
| ○ | ○ | Article | Enhanced Bioavailability and Efficacy of Silymarin Solid Dispersion in Rats with Acetaminophen-Induced Hepatotoxicity | We evaluated the bioavailability, liver distribution, and efficacy of silymarin-D-alpha-tocopherol polyethylene glycol 1000 succinate (TPGS) solid dispersion (silymarin-SD) in rats with acetaminophen-induced hepatotoxicity (APAP) compared with silymarin alone. The solubility of silybin, the major and active component of silymarin, in the silymarin-SD group increased 23-fold compared with the silymarin group. The absorptive permeability of silybin increased by 4.6-fold and its efflux ratio decreased from 5.5 to 0.6 in the presence of TPGS. The results suggested that TPGS functioned as a solubilizing agent and permeation enhancer by inhibiting efflux pump. Thus, silybin concentrations in plasma and liver were increased in the silymarin-SD group and liver distribution increased 3.4-fold after repeated oral administration of silymarin-SD (20 mg/kg as silybin) for five consecutive days compared with that of silymarin alone (20 mg/kg as silybin). Based on higher liver silybin concentrations in the silymarin-SD group, the therapeutic effects of silymarin-SD in hepatotoxic rats were evaluated and compared with silymarin administration only. Elevated alanine aminotransferase, aspartate aminotransferase, and alkaline phosphatase levels were significantly decreased by silymarin-SD, silymarin, and TPGS treatments, but these decreases were much higher in silymarin-SD animals than in those treated with silymarin or TPGS. In conclusion, silymarin-SD (20 mg/kg as silybin, three times per day for 5 days) exhibited hepatoprotective properties toward hepatotoxic rats and these properties were superior to silymarin alone, which may be attributed to increased solubility, enhanced intestinal permeability, and increased liver distribution of the silymarin-SD formulation. | Song, Im-Sook; Nam, So-Jeong; Jeon, Ji-Hyeon; Park, Soo-Jin; Choi, Min-Koo | Kyungpook Natl Univ, Coll Pharm, Vessel Organ Interact Res Ctr VOICE, Res Inst Pharmaceut Sci,BK21 Four Community Based, Daegu 41566, South Korea; Daegu Haany Univ, Coll Korean Med, Daegu 38610, South Korea; Dankook Univ, Coll Pharm, Cheonan 31116, South Korea | 7201564500; 57195054110; 57204685946; 56563264400; 8695781400 | isssong@knu.ac.kr;goddns159@nate.com;kei7016@naver.com;sjp124@dhu.ac.kr;minkoochoi@dankook.ac.kr; | PHARMACEUTICS | PHARMACEUTICS | 1999-4923 | 13 | 5 | SCIE | PHARMACOLOGY & PHARMACY | 2021 | 6.525 | 13.8 | 2.2 | 2025-07-30 | 21 | 28 | silymarin; D-alpha-Tocopherol polyethylene glycol 1000 succinate (TPGS); liver distribution; acetaminophen-induced hepatotoxicity | VITAMIN-E-TPGS; IN-VITRO EVALUATION; GLYCOL 1000 SUCCINATE; ORAL BIOAVAILABILITY; DELIVERY-SYSTEMS; PHARMACOKINETICS; NANOPARTICLES; FORMULATION; INHIBITION; SOLUBILITY | Acetaminophen-induced hepatotoxicity; D-α-tocopherol polyethylene glycol 1000 succinate (TPGS); Liver distribution; Silymarin | alanine aminotransferase; alkaline phosphatase; aspartate aminotransferase; paracetamol; silymarin; alanine aminotransferase blood level; alkaline phosphatase blood level; animal tissue; Article; aspartate aminotransferase blood level; controlled study; drug bioavailability; drug distribution; drug efficacy; drug formulation; drug penetration; drug solubility; drug synthesis; intestine mucosa permeability; liver protection; liver toxicity; male; nonhuman; rat; repeated drug dose; single drug dose | English | 2021 | 2021-05 | 10.3390/pharmaceutics13050628 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | |||
| ○ | ○ | Article | Extracellular Vesicles Act as Nano-Transporters of Tyrosine Kinase Inhibitors to Revert Iodine Avidity in Thyroid Cancer | A new approach for using extracellular vesicles (EVs) to deliver tyrosine kinase inhibitors (TKIs) to enhance iodine avidity in radioactive iodine-refractory thyroid cancer is needed. We isolated and characterized primary human adipose-derived stem cells (ADSCs) and isolated their EVs. The EVs were characterized by transmission electron microscopy, nanoparticle tracking analysis, and western blotting. A new TKI was loaded into the EVs by incubation (37 degrees C; 10 min) or sonication (18 cycles; 4 s per cycle) with 2 s intervals and a 2 min ice bath every six cycles. TKI loading was confirmed and measured by mass spectrometry. EV uptake into radioactive iodine-refractory thyroid cancer cells (SW1736 cells) was confirmed by microscopy. We treated the SW1736 cells with vehicle, TKI, or TKI-loaded EVs (sonication TKI-loaded EVs [EVs(TKI(S))]) and examined the expression of iodide-metabolizing proteins and radioiodine uptake in the SW1736 cells. ADSCs cells showed >99% of typical stem cell markers, such as CD90 and CD105. The EVs displayed a round morphology, had an average size of 211.4 +/- 3.83 nm, and were positive for CD81 and Alix and negative for cytochrome c. The mass spectrometry results indicate that the sonication method loaded similar to 4 times more of the TKI than did the incubation method. The EVs(TKI(S)) were used for further experiments. Higher expression levels of iodide-metabolizing mRNA and proteins in the EVs(TKI(S))-treated SW1736 cells than in TKI-treated SW1736 cells were confirmed. EVs(TKI(S)) treatment enhanced I-125 uptake in the recipient SW1736 cells compared with free-TKI treatment. This is the first study that demonstrated successful delivery of a TKI to radioactive iodine-refractory thyroid cancer cells using EVs as the delivery vehicle. This approach can revert radioiodine-resistant thyroid cancer cells back to radioiodine-sensitive thyroid cancer cells. | Rajendran, Ramya Lakshmi; Paudel, Sanjita; Gangadaran, Prakash; Oh, Ji Min; Oh, Eun Jung; Hong, Chae Moon; Lee, Sangkyu; Chung, Ho Yun; Lee, Jaetae; Ahn, Byeong-Cheol | Kyungpook Natl Univ, Sch Med, Dept Nucl Med, Daegu 41944, South Korea; Kyungpook Natl Univ, Coll Pharm, BK21 FOUR Community Based Intelligent Novel Drug, Daegu 41566, South Korea; Kyungpook Natl Univ, Res Inst Pharmaceut Sci, Daegu 41566, South Korea; Kyungpook Natl Univ, Sch Med, BK21 FOUR KNU Convergence Educ Program Biomed Sci, Daegu 41944, South Korea; Kyungpook Natl Univ, Kyungpook Natl Univ Hosp, Sch Med, Dept Plast & Reconstruct Surg,CMRI, Daegu 41944, South Korea; Kyungpook Natl Univ Hosp, Dept Nucl Med, Daegu 41404, South Korea | ; Rajendran, Ramya/AAV-6338-2021; Lee, Jaetae/AAR-3317-2021; Gangadaran, Prakash/AAV-3102-2021 | 57195318729; 57203320448; 54393130400; 57190370462; 35746789300; 37050876700; 57209046767; 7404007181; 7601451907; 7202791511 | ramyag@knu.ac.kr;sanjitapd199@gmail.com;prakashg@knu.ac.kr;ojm0366@naver.com;fullrest74@hanmail.net;shahking@hanmail.net;pharm239@gmail.com;hy-chung@knu.ac.kr;jaetae@knu.ac.kr;abc2000@knu.ac.kr; | PHARMACEUTICS | PHARMACEUTICS | 1999-4923 | 13 | 2 | SCIE | PHARMACOLOGY & PHARMACY | 2021 | 6.525 | 13.8 | 1.74 | 2025-07-30 | 19 | 21 | extracellular vesicles; tyrosine kinase inhibitor; drug delivery; radioactive iodine; thyroid cancer | Drug delivery; Extracellular vesicles; Radioactive iodine; Thyroid cancer; Tyrosine kinase inhibitor | CD81 antigen; cytochrome c; endoglin; messenger RNA; protein tyrosine kinase inhibitor; radioactive iodine; Thy 1 membrane glycoprotein; adipose derived stem cell; Article; binding affinity; cell isolation; cell tracking; controlled study; drug binding; drug transport; exosome; human; human cell; human tissue; mass spectrometry; microscopy; protein expression; SW1736 cell line; thyroid cancer; transmission electron microscopy; ultrasound; Western blotting | English | 2021 | 2021-02 | 10.3390/pharmaceutics13020248 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | |||
| ○ | ○ | Review | Functionalized Lanthanide Oxide Nanoparticles for Tumor Targeting, Medical Imaging, and Therapy | Recent progress in functionalized lanthanide oxide (Ln(2)O(3)) nanoparticles for tumor targeting, medical imaging, and therapy is reviewed. Among the medical imaging techniques, magnetic resonance imaging (MRI) is an important noninvasive imaging tool for tumor diagnosis due to its high spatial resolution and excellent imaging contrast, especially when contrast agents are used. However, commercially available low-molecular-weight MRI contrast agents exhibit several shortcomings, such as nonspecificity for the tissue of interest and rapid excretion in vivo. Recently, nanoparticle-based MRI contrast agents have become a hot research topic in biomedical imaging due to their high performance, easy surface functionalization, and low toxicity. Among them, functionalized Ln(2)O(3) nanoparticles are applicable as MRI contrast agents for tumor-targeting and nontumor-targeting imaging and image-guided tumor therapy. Primarily, Gd2O3 nanoparticles have been intensively investigated as tumor-targeting T-1 MRI contrast agents. T-2 MRI is also possible due to the appreciable paramagnetic moments of Ln(2)O(3) nanoparticles (Ln = Dy, Ho, and Tb) at room temperature arising from the nonzero orbital motion of 4f electrons. In addition, Ln(2)O(3) nanoparticles are eligible as X-ray computed tomography contrast agents because of their high X-ray attenuation power. Since nanoparticle toxicity is of great concern, recent toxicity studies on Ln(2)O(3) nanoparticles are also discussed. | Ahmad, Mohammad Yaseen; Yue, Huan; Tegafaw, Tirusew; Liu, Shuwen; Ho, Son Long; Lee, Gang Ho; Nam, Sung-Wook; Chang, Yongmin | Kyungpook Natl Univ, Coll Nat Sci, Dept Chem, Taegu 41566, South Korea; Kyungpook Natl Univ, Sch Med, Dept Mol Med, Taegu 41405, South Korea | ; Liu, Shuwen/ABD-5719-2021; Ahmad, Mohammad/AAH-2164-2020; Nam, Sung-Wook/V-5519-2019; Ho, Son Long/P-3183-2015 | 57203054570; 57200329016; 55983618600; 57208926248; 55659242700; 7404851841; 16167127700; 7501840633 | yaseen.knu@gmail.com;yuehuan888@gmail.com;tirukorea@gmail.com;liushuwen0701@gmail.com;sonlongh@gmail.com;ghlee@mail.knu.ac.kr;nams@knu.ac.kr;ychang@knu.ac.kr; | PHARMACEUTICS | PHARMACEUTICS | 1999-4923 | 13 | 11 | SCIE | PHARMACOLOGY & PHARMACY | 2021 | 6.525 | 13.8 | 0.51 | 2025-07-30 | 21 | 22 | imaging agent; lanthanide oxide nanoparticle; tumor targeting; toxicity | NEUTRON-CAPTURE THERAPY; IN-VIVO BIODISTRIBUTION; MRI CONTRAST AGENTS; POLYACRYLIC-ACID; GADOLINIUM(III) COMPLEXES; GD2O3 NANOPARTICLES; SOFT ACIDS; TOXICITY; STRATEGIES; DESIGN | Imaging agent; Lanthanide oxide nanoparticle; Toxicity; Tumor targeting | contrast medium; lanthanide oxide nanoparticle; nanoparticle; unclassified drug; coating (procedure); diagnostic imaging; drug targeting; human; in vivo study; magnetism; molecularly targeted therapy; nonhuman; nuclear magnetic resonance imaging; particle size; physical chemistry; Review; x-ray computed tomography | English | 2021 | 2021-11 | 10.3390/pharmaceutics13111890 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | ||
| ○ | ○ | Article | Identification of Angiogenic Cargo in Extracellular Vesicles Secreted from Human Adipose Tissue-Derived Stem Cells and Induction of Angiogenesis In Vitro and In Vivo | Angiogenesis is defined as the generation of new blood vessels or the sprouting of endothelial cells from a pre-existing vascular network. Angiogenesis occurs during the growth and development of an organism, the response of organs or tissues to injury, and during cancer development and progression. The majority of studies on stem-cell-derived extracellular vesicles (EVs) have used cell lines, and have primarily focused on well-known solitary proteins. Here, we isolated stem cells from human adipose tissue (ADSCs), and we isolated EVs from them (ADSC-EVs). The ADSC-EVs were characterised and 20 angiogenic proteins were analysed using an angiogenic antibody array. Furthermore, we analysed the ability of ADSC-EVs to induce angiogenesis in vitro and in vivo. ADSC-EVs were positive for CD81 and negative for GM130, calnexin, and cytochrome-C. ADSC-EVs showed typical EV spherical morphology and were similar to 200 nm in size. ADSC-EVs were found to contain angiogenic proteins as cargo, among which interleukin 8 (IL-8) was the most abundant, followed by chemokine (C-C motif) ligand 2 (CCL2), a tissue inhibitor of metalloproteinases 1 (TIMP-1), TIMP-2, and vascular endothelial growth factor-D (VEGF-D). ADSC-EVs treatment increased the proliferation, migration, total vessel length, total number of junctions, and junction density of endothelial cells in vitro. The results of an in vivo Matrigel plug assay revealed that ADSC-EVs induced more blood vessels in the Matrigel compared with the control. These results demonstrate that ADSC-EVs contain angiogenic proteins as cargo and promote angiogenesis in vitro and in vivo. Therefore, ADSC-EVs have potential for therapeutic use in ischaemia. | Gangadaran, Prakash; Rajendran, Ramya Lakshmi; Oh, Ji Min; Oh, Eun Jung; Hong, Chae Moon; Chung, Ho Yun; Lee, Jaetae; Ahn, Byeong-Cheol | Kyungpook Natl Univ, BK21 FOUR KNU Convergence Educ Program Biomed Sci, Dept Biomed Sci, Sch Med, Daegu 41944, South Korea; Kyungpook Natl Univ, Sch Med, Dept Nucl Med, Daegu 41944, South Korea; Kyungpook Natl Univ, Kyungpook Natl Univ Hosp, Sch Med, Dept Plast & Reconstruct Surg,CMRI, Daegu 41944, South Korea; Kyungpook Natl Univ, Kyungpook Natl Univ Hosp, Sch Med, Dept Nucl Med, 680 Gukchaebosangro, Daegu 41944, South Korea | Rajendran, Ramya/AAV-6338-2021; Gangadaran, Prakash/AAV-3102-2021; Lee, Jaetae/AAR-3317-2021 | 54393130400; 57195318729; 57190370462; 35746789300; 37050876700; 7404007181; 7601451907; 7202791511 | prakashg@knu.ac.kr;ramyag@knu.ac.kr;ojm0366@knu.ac.kr;fullrest74@knu.ac.kr;cmhong@knu.ac.kr;hy-chung@knu.ac.kr;jaetae@knu.ac.kr;abc2000@knu.ac.kr; | PHARMACEUTICS | PHARMACEUTICS | 1999-4923 | 13 | 4 | SCIE | PHARMACOLOGY & PHARMACY | 2021 | 6.525 | 13.8 | 2.39 | 2025-07-30 | 28 | 27 | adipose tissue; stem cell; extracellular vesicle; angiogenesis | LIMB ISCHEMIA; EXOSOMES; METALLOPROTEINASES; PROLIFERATION; CHALLENGES; MIGRATION; THERAPY; PROMOTE; BIOLOGY | Adipose tissue; Angiogenesis; Extracellular vesicle; Stem cell | angiogenic protein; calnexin; CD81 antigen; cytochrome c; Golgi matrix; interleukin 8; monocyte chemotactic protein 1; protein GM130; tissue inhibitor of metalloproteinase 1; tissue inhibitor of metalloproteinase 2; unclassified drug; vasculotropin D; adipose derived stem cell; adipose tissue; angiogenesis; angiogenesis assay; animal experiment; animal tissue; antibody microarray; antigen expression; Article; cell isolation; cell junction; cell migration; cell proliferation; cell stimulation; controlled study; endothelium cell; exosome; human; human cell; human tissue; in vitro study; in vivo study; internalization (cell); ischemia; Matrigel plug assay; mouse; nonhuman; organelle shape; organelle size; protein analysis; protein expression | English | 2021 | 2021-04 | 10.3390/pharmaceutics13040495 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | ||
| ○ | ○ | Article | Improved Bioavailability and High Photostability of Methotrexate by Spray-Dried Surface-Attached Solid Dispersion with an Aqueous Medium | Low aqueous solubility and poor bioavailability are major concerns in the development of oral solid-dosage drug forms. In this study, we fabricated surface-attached solid dispersion (SASD) to enhance the solubility, bioavailability, and photostability of methotrexate (MTX), a highly lipophilic and photo-unstable drug. Several MTX-loaded SASD formulations were developed for spray-drying using water as the solvent, and were investigated for their aqueous solubility and dissolution kinetics. An optimized ternary SASD formulation composed of MTX/ sodium carboxymethyl cellulose (Na-CMC)/sodium lauryl sulfate (SLS) at 3/0.5/0.5 (w/w) had 31.78-fold and 1.88-fold higher solubility and dissolution, respectively, than MTX powder. For SASD, the in vivo pharmacokinetic parameters AUC and C-max were 2.90- and 3.41-fold higher, respectively, than for the MTX powder. Solid-state characterizations by differential scanning calorimetry and X-ray diffraction revealed that MTX exists in its crystalline state within the spray-dried SASD. The MTX-loaded SASD formulation showed few physical changes with photostability testing. Overall, the results indicate that the spray-dried MTX-loaded SASD formulation without organic solvents enhances the solubility and oral bioavailability of MTX without a significant deterioration of its photochemical stability. | Giri, Bhupendra Raj; Kim, Jung Suk; Park, Jong Hyuck; Jin, Sung Giu; Kim, Kyeong Soo; Din, Fakhar ud; Choi, Han Gon; Kim, Dong Wuk | Kyungpook Natl Univ, FOUR Community Based Intelligent Novel Drug Disco, Vessel Organ Interact Res Ctr VOICE, Coll Pharm,Res Inst Pharmaceut Sci,MRC, Daegu 41566, South Korea; Hanyang Univ, Coll Pharm, Ansan 15588, South Korea; Dankook Univ, Dept Pharmaceut Engn, Cheonan 31116, South Korea; Gyeongnam Natl Univ Sci & Technol, Dept Pharmaceut Engn, Jinju 52725, South Korea; Quaid I Azam Univ, Dept Pharm, Islamabad 45320, Pakistan | ; Choi, HanGon/E-5252-2017; Giri, Bhupendra/GRR-3256-2022; Din, Fakhar-Ud-/AAR-1034-2020; KIM, JUNG SUK/IAL-8910-2023; Kim, Kyeong Soo/AAJ-6800-2021; Din, Fakhar Ud/AAR-1034-2020 | 57210211620; 58290556000; 56352674100; 22979508200; 51763618300; 55905043600; 7404339910; 57193445049 | giribhupen77@gmail.com;jay910612@daum.net;parkingjong@naver.com;sklover777@dankook.ac.kr;soyoyu79@gntech.ac.kr;fudin@qau.edu.pk;hangon@hanyang.ac.kr;dkim17@knu.ac.kr; | PHARMACEUTICS | PHARMACEUTICS | 1999-4923 | 13 | 1 | SCIE | PHARMACOLOGY & PHARMACY | 2021 | 6.525 | 13.8 | 4.13 | 2025-07-30 | 45 | 49 | methotrexate; solid dispersion; solubility; bioavailability; photostability | Bioavailability; Methotrexate; Photostability; Solid dispersion; Solubility | carboxymethylcellulose; dodecyl sulfate sodium; methotrexate; organic solvent; water; animal experiment; aqueous solution; area under the curve; Article; controlled study; crystal structure; differential scanning calorimetry; dissolution kinetics; drug bioavailability; drug dosage form; drug dosage form comparison; drug formulation; drug half life; drug solubility; drug stability; elimination rate constant; Fourier transform infrared spectroscopy; in vitro study; in vivo study; kinetics; lipophilicity; male; maximum concentration; microtechnology; nonhuman; particle size; photochemistry; photostability; physical phenomena; powder; rat; scanning electron microscopy; solid state; surface attached solid dispersion; time to maximum plasma concentration; X ray powder diffraction | English | 2021 | 2021-01 | 10.3390/pharmaceutics13010111 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | |||
| ○ | ○ | Article | Improved Hygroscopicity and Bioavailability of Solid Dispersion of Red Ginseng Extract with Silicon Dioxide | This study aims to develop a powder formulation for the Korean red ginseng extract (RGE) and to evaluate its in vitro and in vivo formulation characteristics. The solid dispersion of RGE was prepared with hydrophilic carriers using a freeze-drying method. After conducting the water sorption-desorption isothermogram (relative humidity between 30 and 70% RH), differential scanning calorimetry thermal behavior, dissolution test, and intestinal permeation study, a solid dispersion formulation of RGE and silicon dioxide (RGE-SiO2) was selected. RGE-SiO2 formulation increased intestinal permeability of ginsenoside Rb1 (GRb1), GRb2, GRc, and GRd by 1.6-fold in rat jejunal segments as measured by the Ussing chamber system. A 1.6- to 1.8-fold increase in plasma exposure of GRb1, GRb2, GRc, and GRd in rats was observed following oral administration of RGE-SiO2 (375 mg/kg as RGE). No significant difference was observed in the time to reach maximum concentration (T-max) and half-life in comparison to those in RGE administered rats (375 mg/kg). In conclusion, formulating solid dispersion of RGE with amorphous SiO2, the powder formulation of RGE was successfully formulated with improved hygroscopicity, increased intestinal permeability, and enhanced oral bioavailability and is therefore suitable for processing solid formulations of RGE product. | Jin, Sojeong; Lee, Chul Haeng; Lim, Dong Yu; Lee, Jaehyeok; Park, Soo-Jin; Song, Im-Sook; Choi, Min-Koo | Dankook Univ, Coll Pharm, Cheonan 31116, South Korea; Kyungpook Natl Univ, Coll Pharm, Res Inst Pharmaceut Sci,Vessel Organ Interact Res, BK21 FOUR Community Based Intelligent Novel Drug, Daegu 41566, South Korea; Daegu Haany Univ, Coll Korean Med, Daegu 38610, South Korea | 57204690167; 57219051827; 57219057824; 57219980183; 56563264400; 7201564500; 8695781400 | astraea327@naver.com;hang1130@naver.com;twins3639@naver.com;here0723@gmail.com;sjp124@dhu.ac.kr;isssong@knu.ac.kr;minkoochoi@dankook.ac.kr; | PHARMACEUTICS | PHARMACEUTICS | 1999-4923 | 13 | 7 | SCIE | PHARMACOLOGY & PHARMACY | 2021 | 6.525 | 13.8 | 1.38 | 2025-07-30 | 17 | 16 | Korean red ginseng extract; solid dispersion formulation; hygroscopicity; intestinal permeability; oral bioavailability | ENHANCED ORAL BIOAVAILABILITY; PANAX-GINSENG; IN-VITRO; GINSENOSIDES; BIOTRANSFORMATION; CLASSIFICATION; EXCIPIENTS; ABSORPTION; SUBSTRATE; DELIVERY | Hygroscopicity; Intestinal permeability; Korean red ginseng extract; Oral bioavailability; Solid dispersion formulation | berberine; caffeine; carbon 13; ginseng extract; ginsenoside; ginsenoside Rb 1; growth factor receptor bound protein 1; growth factor receptor bound protein 2; growth hormone releasing factor C; growth hormone releasing factor D; growth hormone releasing factor E; growth hormone releasing factor F; growth hormone releasing factor G1; hydroxypropylcellulose; isoflurane; lactose; macrogol 6000; mannitol; polyethyleneglycol 1500; povidone; protopanaxadiol; protopanaxatriol; silicon dioxide; trehalose; unclassified drug; adult; alpha radiation; animal experiment; animal model; Article; biopharmaceutical classification system; centrifugation; controlled study; differential scanning calorimetry; dissolution; dissolution test; dissolution value; drug bioavailability; drug formulation; drug stability; equilibrium; femoral artery cannulation; freeze drying; humidity; in vitro study; in vivo study; intestinal permeability; jejunal segment; liquid chromatography; male; maximum plasma concentration; molecular mobility; nonhuman; oxygen flow; similarity factor; solid dispersion; tandem mass spectrometry; temperature; thermal behavior; water content change; water sorption desorption isothermogram; water sorption rate; wettability; X ray diffraction | English | 2021 | 2021-07 | 10.3390/pharmaceutics13071022 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | |||
| ○ | ○ | Article | In Vitro Metabolism of Donepezil in Liver Microsomes Using Non-Targeted Metabolomics | Donepezil is a reversible acetylcholinesterase inhibitor that is currently the most commonly prescribed drug for the treatment of Alzheimer's disease. In general, donepezil is known as a safe and well-tolerated drug, and it was not associated with liver abnormalities in several clinical trials. However, rare cases of drug-related liver toxicity have been reported since it has become commercially available. Few studies have investigated the metabolic profile of donepezil, and the mechanism of liver damage caused by donepezil has not been elucidated. In this study, the in vitro metabolism of donepezil was investigated using liquid chromatography-tandem mass spectrometry based on a non-targeted metabolomics approach. To identify metabolites, the data were subjected to multivariate data analysis and molecular networking. A total of 21 donepezil metabolites (17 in human liver microsomes, 21 in mice liver microsomes, and 17 in rat liver microsomes) were detected including 14 newly identified metabolites. One potential reactive metabolite was identified in rat liver microsomal incubation samples. Metabolites were formed through four major metabolic pathways: (1) O-demethylation, (2) hydroxylation, (3) N-oxidation, and (4) N-debenzylation. This study indicates that a non-targeted metabolomics approach combined with molecular networking is a reliable tool to identify and detect unknown drug metabolites. | Kim, Sin-Eun; Seo, Hyung-Ju; Jeong, Yeojin; Lee, Gyung-Min; Ji, Seung-Bae; Park, So-Young; Wu, Zhexue; Lee, Sangkyu; Kim, Sunghwan; Liu, Kwang-Hyeon | Kyungpook Natl Univ, BK21 Four KNU Community Based Intelligent Novel D, Coll Pharm, Daegu 41566, South Korea; Kyungpook Natl Univ, Res Inst Pharmaceut Sci, Daegu 41566, South Korea; Kyungpook Natl Univ, Mass Spectrometry Based Convergence Res Inst, Daegu 41566, South Korea; Kyungpook Natl Univ, Dept Chem, Daegu 41566, South Korea | ; Kim, Sunghwan/HKN-9812-2023 | 57217828200; 57204496397; 57224538974; 57217829865; 57217827900; 57211630074; 55523767300; 57209046767; 57203772967; 55768214700 | hjkopsty@gmail.com;hlhl103@naver.com;duwls9902@gmail.com;lgm00179@naver.com;wltmdqo2377@naver.com;soyoung561@hanmail.net;wuzhexue@knu.ac.kr;sangkyu@knu.ac.kr;sunghwank@knu.ac.kr;dstlkh@knu.ac.kr; | PHARMACEUTICS | PHARMACEUTICS | 1999-4923 | 13 | 7 | SCIE | PHARMACOLOGY & PHARMACY | 2021 | 6.525 | 13.8 | 0.73 | 2025-07-30 | 9 | 9 | donepezil; metabolism; metabolomics; molecular networking; multivariate analysis | DRUG-METABOLISM; ALICYCLIC AMINES; IDENTIFICATION; BIOACTIVATION; ION; BIOTRANSFORMATION; DISCOVERY | Donepezil; Metabolism; Metabolomics; Molecular networking; Multivariate analysis | donepezil; animal experiment; animal model; Article; controlled study; data analysis; debenzylation; demethylation; drug metabolism; electrospray; flow rate; high performance liquid chromatography; human; hydroxylation; in vitro study; liquid chromatography-mass spectrometry; liver microsome; liver toxicity; major clinical study; metabolomics; mouse; nonhuman; oxidation; quadrupole mass spectrometry; rat; retention time (chromatography) | English | 2021 | 2021-07 | 10.3390/pharmaceutics13070936 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | ||
| ○ | ○ | Article | In Vitro Metabolism Study of Seongsanamide A in Human Liver Microsomes Using Non-Targeted Metabolomics and Feature-Based Molecular Networking | Seongsanamide A is a bicyclic peptide with an isodityrosine residue discovered in Bacillus safensis KCTC 12796BP which exhibits anti-allergic activity in vitro and in vivo without significant cytotoxicity. The purpose of this study was to elucidate the in vitro metabolic pathway and potential for drug interactions of seongsanamide A in human liver microsomes using non-targeted metabolomics and feature-based molecular networking (FBMN) techniques. We identified four metabolites, and their structures were elucidated by interpretation of high-resolution tandem mass spectra. The primary metabolic pathway associated with seongsanamide A metabolism was hydroxylation and oxidative hydrolysis. A reaction phenotyping study was also performed using recombinant cytochrome P450 isoforms. CYP3A4 and CYP3A5 were identified as the major metabolic enzymes responsible for metabolite formation. Seongsanamide A did not inhibit the cytochrome P450 isoforms commonly involved in drug metabolism (IC50 > 10 mu M). These results will contribute to further understanding the metabolism and drug interaction potential of various bicyclic peptides. | Wu, Zhexue; Kim, Geum Jin; Park, So-Young; Shon, Jong Cheol; Liu, Kwang-Hyeon; Choi, Hyukjae | Kyungpook Natl Univ, Mass Spectrometry Based Convergence Res Inst, Daegu 41566, South Korea; Yeungnam Univ, Coll Pharm, Gyongsan 38541, South Korea; Yeungnam Univ, Res Inst Cell Culture, Gyongsan 38541, South Korea; Kyungpook Natl Univ, Coll Pharm, BK21 FOUR Community Based Intelligent Novel Drug, Daegu 41566, South Korea; Kyungpook Natl Univ, Res Inst Pharmaceut Sci, Daegu 41566, South Korea | 55523767300; 54585532800; 57211630074; 56010668800; 55768214700; 7404339587 | wuzhexue@knu.ac.kr;canta87@ynu.ac.kr;soyoung561@hanmail.net;sleier7640@naver.com;dstlkh@knu.ac.kr;h5choi@yu.ac.kr; | PHARMACEUTICS | PHARMACEUTICS | 1999-4923 | 13 | 7 | SCIE | PHARMACOLOGY & PHARMACY | 2021 | 6.525 | 13.8 | 0.09 | 2025-07-30 | 4 | 4 | Bacillus sp; KCTC 12796BP; metabolism; drug interaction; high-resolution mass spectrometry; seongsanamide A | ELECTROSPRAY-IONIZATION; MASS-SPECTROMETRY; INHIBITION; SAQUINAVIR; PEPTIDES; REVEALS | Bacillus sp. KCTC 12796BP; Drug interaction; High-resolution mass spec-trometry; Metabolism; Seongsanamide A | cytochrome P450; cytochrome P450 3A4; cytochrome P450 3A5; drug metabolite; isoenzyme; recombinant cytochrome P450; recombinant enzyme; seongsanamide A; unclassified drug; Article; Bacillus safensis; chemical structure; controlled study; drug interaction; drug metabolism; drug potency; drug structure; enzyme inhibition; human; hydrolysis; hydroxylation; IC50; in vitro study; liver metabolism; liver microsome; metabolism; metabolomics; molecular networking; network analysis; oxidative hydrolysis; phenotype; tandem mass spectrometry | English | 2021 | 2021-07 | 10.3390/pharmaceutics13071031 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | |||
| ○ | ○ | Article | Inhibitory Effects of Schisandra Lignans on Cytochrome P450s and Uridine 5′-Diphospho-Glucuronosyl Transferases in Human Liver Microsomes | Schisandra chinensis has been widely used as a traditional herbal medicine to treat chronic coughs, fatigue, night sweats, and insomnia. Numerous bioactive components including lignans have been identified in this plant. Lignans with a dibenzocyclooctadiene moiety have been known to possess anti-cancer, anti-inflammatory, and hepatoprotective activity. Fragmentary studies have reported the ability of some lignans to modulate some cytochrome P450 (P450) enzymes. Herein, we investigated the drug interaction potential of six dibenzocyclooctadiene lignans (schisandrin, gomisin A, B, C, and N, and wuweizisu C) on nine P450 enzymes (CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A) and six uridine 5 '-diphosphoglucuronosyl transferase (UGT) enzymes (UGT1A1, 1A3, 1A4, 1A6, 1A9, and 2B7) using human liver microsomes. We found that lignans with one or two methylenedioxyphenyl groups inhibited CYP2B6, CYP2C8, CYP2C9, CYP2C19, and CYP2E1 activities in a time- and concentration-dependent like their CYP3A inhibition. In comparison, these lignans do not induce time-dependent inhibition of CYP1A2, CYP2A6, and CYP2D6. The time-dependent inhibition of gomisin A against CYP2C8, CYP2C19, and CYP3A4 was also elucidated using glutathione as a trapping reagent of reactive carbene metabolites given that gomisin A strongly inhibits these P450 enzymes in a time-dependent manner. A glutathione conjugate of gomisin A was generated in reactions with human recombinant CYP2C8, CYP2C19, and CYP3A4. This suggests that the time-dependent inhibition of gomisin A against CYP2C8, CYP2C9, and CYP3A4 is due to the production of carbene reactive metabolite. Six of the lignans we tested inhibited the activities of six UGT to a limited extent (IC50 > 15 mu M). This information may aid the prediction of possible drug interactions between Schisandra lignans and any co-administered drugs which are mainly metabolized by P450s. | Seo, Hyung-Ju; Ji, Seung-Bae; Kim, Sin-Eun; Lee, Gyung-Min; Park, So-Young; Wu, Zhexue; Jang, Dae Sik; Liu, Kwang-Hyeon | Kyungpook Natl Univ, Coll Pharm, BK21 FOUR Community Based Intelligent Novel Drug, Daegu 41566, South Korea; Kyungpook Natl Univ, Res Inst Pharmaceut Sci, Daegu 41566, South Korea; Kyungpook Natl Univ, Mass Spectrometry Based Convergence Res Inst, Daegu 41566, South Korea; Kyungpook Natl Univ, Dept Chem, Daegu 41566, South Korea; Kyung Hee Univ, Dept Life & Nanopharmaceut Sci, Seoul 02447, South Korea | ; Jang, Dae/AAI-4526-2020 | 57204496397; 57217827900; 57217828200; 57217829865; 57211630074; 55523767300; 7102794507; 55768214700 | seohj1992@naver.com;wltmdqo2377@naver.com;hjkopsty@gmail.com;lgm00179@naver.com;soyoung561021@gmail.com;wuzhexue527@gmail.com;dsjang@khu.ac.kr;dstlkh@knu.ac.kr; | PHARMACEUTICS | PHARMACEUTICS | 1999-4923 | 13 | 3 | SCIE | PHARMACOLOGY & PHARMACY | 2021 | 6.525 | 13.8 | 1.38 | 2025-07-30 | 17 | 18 | Schisandra chinensis; lignans; cytochrome P450; uridine 5′ -diphosphoglucuronosyl transferase; drug interaction | Cytochrome P450; Drug interaction; Lignans; Schisandra chinensis; Uridine 5'-diphosphoglucuronosyl transferase | amfebutamone; amodiaquine; carbene; chlorzoxazone; coumarin; cytochrome P450; cytochrome P450 1A2; cytochrome P450 2A6; cytochrome P450 2B6; cytochrome P450 2C19; cytochrome P450 2C8; cytochrome P450 2C9; cytochrome P450 2D6; cytochrome P450 2E1; cytochrome P450 3A; dextromethorphan; diclofenac; glucuronosyltransferase; glucuronosyltransferase 1A1; glucuronosyltransferase 1A3; glucuronosyltransferase 1A4; glucuronosyltransferase 1A6; glucuronosyltransferase 1A9; glucuronosyltransferase 2B7; glutathione; gomisin; gomisin A; lignan; mephenytoin; midazolam; nifedipine; phenacetin; Schisandra chinensis extract; schisandrin; testosterone; unclassified drug; uridine 5' diphospho glucuronosyl transferase; wuweizisu C; Article; comparative study; controlled study; drug effect; drug isolation; drug mechanism; drug structure; electrospray; enzyme activity; enzyme inhibition; human; human cell; IC50; incubation temperature; incubation time; liquid chromatography-mass spectrometry; liver microsome; metabolite; process optimization; protein function; Schisandra chinensis | English | 2021 | 2021-03 | 10.3390/pharmaceutics13030371 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | |||
| ○ | ○ | Article | Involvement of Organic Anion Transporters in the Pharmacokinetics and Drug Interaction of Rosmarinic Acid | We investigated the involvement of drug transporters in the pharmacokinetics of rosmarinic acid in rats as well as the transporter-mediated drug interaction potential of rosmarinic acid in HEK293 cells overexpressing clinically important solute carrier transporters and also in rats. Intravenously injected rosmarinic acid showed bi-exponential decay and unchanged rosmarinic acid was mainly eliminated by urinary excretion, suggesting the involvement of transporters in its renal excretion. Rosmarinic acid showed organic anion transporter (OAT)1-mediated active transport with a K-m of 26.5 mu M and a V-max of 69.0 pmol/min in HEK293 cells overexpressing OAT1, and the plasma concentrations of rosmarinic acid were increased by the co-injection of probenecid because of decreased renal excretion due to OAT1 inhibition. Rosmarinic acid inhibited the transport activities of OAT1, OAT3, organic anion transporting polypeptide (OATP)1B1, and OATP1B3 with IC50 values of 60.6 mu M, 1.52 mu M, 74.8 mu M, and 91.3 mu M, respectively, and the inhibitory effect of rosmarinic acid on OAT3 transport activity caused an in vivo pharmacokinetic interaction with furosemide by inhibiting its renal excretion and by increasing its plasma concentration. In conclusion, OAT1 and OAT3 are the major transporters that may regulate the pharmacokinetic properties of rosmarinic acid and may cause herb-drug interactions with rosmarinic acid, although their clinical relevance awaits further evaluation. | Kang, Yun Ju; Lee, Chul Haeng; Park, Soo-Jin; Lee, Hye Suk; Choi, Min-Koo; Song, Im-Sook | Kyungpook Natl Univ, Coll Pharm, Daegu 41566, South Korea; Kyungpook Natl Univ, Pharmaceut Sci Res Inst, Daegu 41566, South Korea; Dankook Univ, Coll Pharm, Cheonan 31116, South Korea; Daegu Haany Univ, Coll Korean Med, Daegu 38610, South Korea; Catholic Univ Korea, Coll Pharm, Bucheon 14662, South Korea; Kyungpook Natl Univ, BK21 FOUR Community Based Intelligent Novel Drug, Daegu 41566, South Korea | 57195055693; 57219051827; 56563264400; 35316111800; 8695781400; 7201564500 | yun-ju6895@nate.com;hang1130@naver.com;sjp124@dhu.ac.kr;sianalee@catholic.ac.kr;minkoochoi@dankook.ac.kr;isssong@knu.ac.kr; | PHARMACEUTICS | PHARMACEUTICS | 1999-4923 | 13 | 1 | SCIE | PHARMACOLOGY & PHARMACY | 2021 | 6.525 | 13.8 | 1.29 | 2025-07-30 | 16 | 17 | rosmarinic acid; organic anion transporter (OAT); pharmacokinetics; herb-drug interaction | GLUCOSE INJECTION; EXCRETION; BIOAVAILABILITY; FORMULATION; METABOLISM; EXTRACT; CELLS; RATS; OAT1 | Herb-drug interaction; Organic anion transporter (OAT); Pharmacokinetics; Rosmarinic acid | furosemide; organic anion transporter; organic anion transporter 1; organic anion transporter 3; organic cation transporter 1; organic cation transporter 2; probenecid; rosmarinic acid; sodium bile acid cotransporter; solute carrier organic anion transporter 1B1; solute carrier organic anion transporter 1B3; valsartan; animal experiment; area under the curve; Article; controlled study; drug blood level; drug clearance; drug distribution; drug elimination; drug half life; drug inhibition; drug metabolism; drug protein binding; drug structure; elimination half-life; HEK293 cell line; herb drug interaction; IC50; in vivo study; male; nonhuman; pharmacokinetic parameters; plasma concentration-time curve; rat; renal clearance; urinary excretion | English | 2021 | 2021-01 | 10.3390/pharmaceutics13010083 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | |||
| ○ | ○ | Article | Measurement of the cosmic muon annual and diurnal flux variation with the COSINE-100 detector | We report measurements of annual and diurnal modulations of the cosmic-ray muon rate in the Yangyang underground laboratory (Y2L) using 952 days of COSINE-100 data acquired between September 2016 and July 2019. A correlation of the muon rate with the atmospheric temperature is observed and its amplitude on the muon rate is determined. The effective atmospheric temperature and muon rate variations are positively correlated with a measured effective temperature coefficient of alpha(T) = 0.82 +/- 0.10. This result is consistent with a model of meson production in the atmosphere. We also searched for a diurnal modulation in the underground muon rate by comparing one-hour intervals. No significant diurnal modulation of the muon rate was observed. | Prihtiadi, H.; Adhikari, G.; Barbosa de Souza, E.; Carlin, N.; Choi, J. J.; Choi, S.; Djamal, M.; Ezeribe, A. C.; Franca, L. E.; Ha, C.; Hahn, I. S.; Jeon, E. J.; Jo, J. H.; Kang, W. G.; Kauer, M.; Kim, H.; Kim, H. J.; Kim, K. W.; Kim, S. K.; Kim, Y. D.; Kim, Y. H.; Ko, Y. J.; Lee, E. K.; Lee, H. S.; Lee, J.; Lee, J. Y.; Lee, M. H.; Lee, S. H.; Leonard, D. S.; Manzato, B. B.; Maruyama, R. H.; Neal, R. J.; Olsen, S. L.; Park, B. J.; Park, H. K.; Park, H. S.; Park, K. S.; Pitta, R. L. C.; Ra, S. J.; Rott, C.; Shin, K. A.; Scraff, A.; Spooner, N. J. C.; Thompson, W. G.; Yang, L.; Yu, G. H. | Bandung Inst Technol, Dept Phys, Bandung 40132, Indonesia; Inst Basic Sci IBS, Ctr Underground Phys, Daejeon 34126, South Korea; Sejong Univ, Dept Phys, Seoul 05006, South Korea; Yale Univ, Dept Phys, New Haven, CT 06520 USA; Yale Univ, Wright Lab, New Haven, CT 06520 USA; Univ Sao Paulo, Phys Inst, BR-05508090 Sao Paulo, Brazil; Seoul Natl Univ, Dept Phys & Astron, Seoul 08826, South Korea; Univ Sheffield, Dept Phys & Astron, Sheffield S3 7RH, S Yorkshire, England; Chung Ang Univ, Dept Phys, Seoul 06973, South Korea; Ewha Womans Univ, Dept Sci Educ, Seoul 03760, South Korea; Univ Wisconsin, Dept Phys, Madison, WI 53706 USA; Univ Wisconsin, Wisconsin IceCube Particle Astrophys Ctr, Madison, WI 53706 USA; Kyungpook Natl Univ, Dept Phys, Daegu 41556, South Korea; Univ Sci & Technol UST, IBS Sch, Daejeon 34113, South Korea; Korea Res Inst Stand & Sci, Daejeon 34113, South Korea; Korea Univ, Dept Accelerator Sci, Sejong 30019, South Korea; Sungkyunkwan Univ, Dept Phys, Suwon 16419, South Korea; Univ Calif San Diego, Dept Phys, La Jolla, CA 92093 USA | Kauer, Matt/AAY-7581-2020; Thompson, William/H-2407-2011; KIM, Sun Kee/IQT-8178-2023; Kim, Seongjun/HMV-6287-2023; DJAMAL, MITRA/JFJ-1152-2023; Maruyama, Reina/A-1064-2013; Lee, Moo/AAK-4266-2020; Lee, Jong/A-3198-2011; Schneider Hahn, Ivanete/H-9015-2016; Ko, Young/AEI-0838-2022; Funo de Moura Franca, Luis Eduardo/AET-2735-2022; Kim, Hong Joo/AAE-1178-2022; Ha, Chang Hyon/AAR-8120-2021; Rott, Carsten/ABB-1304-2021; Laranjeira Couto Pitta, Ricardo/K-4152-2018; Lee, Seunghyun/AAS-8066-2021; França, Luis Eduardo/AET-2735-2022; Lee, Jooyoung/HTN-0335-2023 | 57188983477; 56811058500; 57200584326; 7006320391; 58263015500; 57199723894; 6506355194; 56300952200; 57219686017; 17342119700; 7201832280; 57204519171; 55575536700; 24401181300; 55196156000; 37090888000; 59051568100; 57209988432; 59102407800; 7410207253; 57196171764; 56030036300; 57226673940; 56113238600; 57226402706; 57204797944; 57198252980; 57257129200; 7201953933; 57211139944; 9334469000; 57211139925; 35227722100; 57204904910; 8455192000; 57216599536; 35225979300; 57208178150; 16480794500; 35227850400; 57203522213; 57219742173; 7005922145; 57200581630; 57192656960; 57208174900 | hafizh@ibs.re.kr; | JOURNAL OF COSMOLOGY AND ASTROPARTICLE PHYSICS | J COSMOL ASTROPART P | 1475-7516 | 2 | SCIE | ASTRONOMY & ASTROPHYSICS;PHYSICS, PARTICLES & FIELDS | 2021 | 7.28 | 13.8 | 0.94 | 2025-07-30 | 15 | 16 | cosmic ray experiments; dark matter detectors; dark matter experiments | VETO | cosmic ray experiments; dark matter detectors; dark matter experiments | English | 2021 | 2021-02 | 10.1088/1475-7516/2021/02/013 | 바로가기 | 바로가기 | 바로가기 | 바로가기 | ||||
| ○ | ○ | Article | Metabolism of Diterpenoids Derived from the Bark of Cinnamomum cassia in Human Liver Microsomes | Cinnamomum cassia L. is used as a spice and flavoring agent as well as a traditional medicine worldwide. Diterpenoids, a class of compounds present in C. cassia, have various pharmacological effects, such as anti-inflammatory, antitumor, and antibacterial activities; however, there are insufficient studies on the metabolism of diterpenoids. In this study, the metabolism of seven diterpenoids, namely, anhydrocinnzeylanol, anhydrocinnzeylanine (AHC), cinncassiol A, cinncassiol B, cinnzeylanol, cinnzeylanone, and cinnzeylanine, obtained from the bark of C. cassia was studied in human liver microsomes (HLMs). All studied diterpenoids, except for AHC, exhibited strong metabolic stability; however, AHC was rapidly metabolized to 3% in HLMs in the presence of beta-NADPH. Using a high-resolution quadrupole-orbitrap mass spectrometer, 20 metabolites were identified as dehydrogenated metabolites (M1-M3), dehydrogenated and oxidated metabolites (M4-M10), mono-oxidated metabolites (M11-M13), or dioxidated metabolites (M14-M20). In addition, CYP isoforms involved in AHC metabolism were determined by profiling metabolites produced after incubation in 11 recombinant cDNA-expressed CYP isoforms. Thus, the diterpenoid compound AHC was identified in a metabolic pathway involving CYP3A4 in HLMs. | Choi, Su Min; Pham, Van Cong; Lee, Sangkyu; Kim, Jeong Ah | Kyungpook Natl Univ, Coll Pharm, BK21 FOUR Community Based Intelligent Novel Drug, Daegu 41566, South Korea; Kyungpook Natl Univ, Coll Pharm, Daegu 41566, South Korea; Kyungpook Natl Univ, Res Inst Pharmaceut Sci, Daegu 41566, South Korea; Kyungpook Natl Univ, Coll Pharm, Vessel Organ Interact Res Ctr, VOICE MRC, Daegu 41566, South Korea | 57212768203; 57194459888; 57209046767; 24722570900 | ys01216@naver.com;phamcong1990@gmail.com;sangkyu@knu.ac.kr;jkim6923@knu.ac.kr; | PHARMACEUTICS | PHARMACEUTICS | 1999-4923 | 13 | 8 | SCIE | PHARMACOLOGY & PHARMACY | 2021 | 6.525 | 13.8 | 0.46 | 2025-07-30 | 6 | 5 | diterpenoids; anhydrocinnzeylanine; CYPs; human liver microsomes; metabolism | CONSTITUENTS; CORTEX; DEHYDROGENATION; IDENTIFICATION; CHEMISTRY; EXTRACT | Anhydrocinnzeylanine; CYPs; Diterpenoids; Human liver microsomes; Metabolism | anhydrocinnzeylanine; anhydrocinnzeylanol; cinncassiol A; cinncassiol B; cinnzeylanine; cinnzeylanol; cinnzeylanone; cytochrome P450 3A4; diterpenoid; reduced nicotinamide adenine dinucleotide phosphate; unclassified drug; Article; bark; chemical structure; Cinnamomum cassia; controlled study; dehydrogenation; dioxidation; human; human cell; liver microsome; metabolic stability; metabolism; metabolite; mono oxidation; oxidation; reaction time | English | 2021 | 2021-08 | 10.3390/pharmaceutics13081316 | 바로가기 | 바로가기 | 바로가기 | 바로가기 |
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