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  • SAGE Publications  (6)
  • Pharmacy  (6)
  • 1
    Online Resource
    Online Resource
    A 96-Week Randomized Trial of Switching to Entecavir in Chronic Hepatitis B Patients with a Partial Virological Response to Lamivudine
    SAGE Publications ; 2012
    In:  Antiviral Therapy Vol. 17, No. 8 ( 2012-11), p. 1563-1570
    Details
    In: Antiviral Therapy, SAGE Publications, Vol. 17, No. 8 ( 2012-11), p. 1563-1570
    Abstract: Growing numbers of chronic hepatitis B (CHB) patients in the Asia-Pacific region have failed first-line therapy with low genetic barrier drugs. This prospective, 96-week study investigated the antiviral efficacy, safety and tolerability of switching to entecavir versus maintaining lamivudine in CHB patients with a partial virological response to lamivudine. Methods A total of 72 hepatitis B e antigen (HBeAg)-positive patients, with serum HBV DNA≥60 IU/ml after ≥6 months lamivudine monotherapy were randomized 1:1 to receive either entecavir 1.0 mg/day, or continued lamivudine 100 mg/day. Results Mean duration of prior lamivudine treatment was 15.1 months in the lamivudine-maintained patients and 16.1 months in the entecavir-switch patients, with mean baseline HBV DNA levels of 4.66 and 4.55 log 10 IU/ml, respectively. A greater proportion of entecavir-switch than lamivudine-maintained patients achieved undetectable HBV DNA at all time points (67.6% versus 11.4% at week 96; P 〈 0.001). Entecavir-switch patients achieved a greater mean decrease in HBV DNA level by week 4, maintained through week 96. Entecavir-switch patients with baseline HBV DNA 〈 5 log 10 IU/ml were more likely to achieve a virological response at week 96. A total of 6 (17.6%) entecavir-switch and 2 (5.7%) lamivudine- maintained patients achieved HBeAg loss, and 3 (8.8%) entecavir and 1 (2.9%) lamivudine patients achieved HBeAg seroconversion. Genotypic resistance to the assigned intervention emerged in 82.9% (29/35) of lamivudine-maintained patients, and in 3% (1/34) of entecavir-switch patients after 96 weeks. Conclusions Switching to entecavir in patients with a partial virological response to lamivudine resulted in increased virological efficacy and lower rates of antiviral resistance than maintaining lamivudine.
    Type of Medium: Online Resource
    ISSN: 1359-6535 , 2040-2058
    URL: Article
    DOI: 10.3851/IMP2277
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2012
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  • 2
    Online Resource
    Online Resource
    Anti-inflammatory Activities of 7,8-Dihydroxy-4-Methylcoumarin Acetylation Products via NF-κB and MAPK Pathways in LPS-Stimulated RAW 264.7 Cells
    SAGE Publications ; 2022
    In:  Natural Product Communications Vol. 17, No. 5 ( 2022-05), p. 1934578X2210868-
    Details
    In: Natural Product Communications, SAGE Publications, Vol. 17, No. 5 ( 2022-05), p. 1934578X2210868-
    Abstract: Coumarins are phenolic compounds that are characterized by fused benzene and α-pyrone rings. Among coumarin-based compounds, 7,8-dihydroxy-4-methylcoumarin (DHMC) has anti-inflammatory activities, but whether the level of this activity varies according to the degree of acetylation remains unknown. Therefore, we acetylated DHMC to yield monoacetylated 8-acetoxy-4-methylcoumarin (8AMC) and 7,8-diacetoxy-4-methylcoumarin (DAMC). We then compared the anti-inflammatory activities of DHMC with its acetylated derivatives and discovered a novel anti-inflammatory agent. We evaluated whether DHMC, 8AMC, and DAMC could inhibit lipopolysaccharide (LPS)-induced stimulation in RAW 264.7 cells. We found that DHMC, 8AMC, and DAMC induced a dose-dependent downregulation of nitric oxide (NO), prostaglandin E2 (PGE 2 ), pro-inflammatory cytokine, inducible NO synthase (iNOS), and cyclooxygenase-2 (COX-2) expression at the mRNA and protein levels. Western blotting showed that DHMC, 8AMC, and DAMC inhibited phosphorylated mitogen-activated protein kinase (MAK), extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK), p38, and nuclear factor-kappa B (NF-κB) expression in a concentration-dependent manner. Furthermore, 8AMC was the most effective inhibitor with powerful anti-inflammatory activity. These results indicate that acetylation can improve the anti-inflammatory activity of natural precursors. We also discovered the new anti-inflammatory compounds 8AMC and DAMC.
    Type of Medium: Online Resource
    ISSN: 1934-578X , 1555-9475
    URL: Article
    DOI: 10.1177/1934578X221086893
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2022
    detail.hit.zdb_id: 2430442-6
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  • 3
    Online Resource
    Online Resource
    Biotransformation of Naringenin by Bacillus amyloliquefaciens Into Three Naringenin Derivatives
    SAGE Publications ; 2019
    In:  Natural Product Communications Vol. 14, No. 5 ( 2019-05), p. 1934578X1985197-
    Details
    In: Natural Product Communications, SAGE Publications, Vol. 14, No. 5 ( 2019-05), p. 1934578X1985197-
    Abstract: In this study, a whole-cell biotransformation by Bacillus amyloliquefaciens Korean Collection for Type Culture 13588 was carried out to acquire naringenin derivatives. High-performance liquid chromatography analysis of the reaction metabolites showed the presence of 3 different products. The structure of the metabolites was confirmed through high-resolution quadrupole-time-of-flight electrospray-ionization mass spectrometry and nuclear magnetic resonance analysis. The result revealed that B. amyloliquefaciens catalyzes naringenin into 3 derivatives, naringenin 7- O-phosphate, naringenin 7- O-glucoside (prunin), and 6''- O-succinylprunin. To our knowledge, this is the first report of the production of 3 different derivatives when naringenin was used as a substrate. Furthermore, our study also revealed that the product naringenin 7- O-phosphate has approximately 45-fold higher water solubility than that of naringenin. Our finding suggests that biotransformation might solve the low bioavailability of flavonoids.
    Type of Medium: Online Resource
    ISSN: 1934-578X , 1555-9475
    URL: Article
    DOI: 10.1177/1934578X19851971
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2019
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  • 4
    Online Resource
    Online Resource
    Synthesis and Melanogenesis Effect of 7,8-Dimethoxy-4-Methylcoumarin via MAPK Signaling-Mediated Microphthalmia-Associated Transcription Factor Upregulation
    SAGE Publications ; 2022
    In:  Natural Product Communications Vol. 17, No. 2 ( 2022-02), p. 1934578X2210766-
    Details
    In: Natural Product Communications, SAGE Publications, Vol. 17, No. 2 ( 2022-02), p. 1934578X2210766-
    Abstract: Tyrosinase ultimately controls the melanogenesis rate of the skin, and tanning and haircare products generally induce the activation of tyrosinase. Moreover, various enzymes, including tyrosinase, tyrosinase-related protein 1 (TRP1), and tyrosinase-related protein 2 (TRP2), mediate melanogenesis in which microphthalmia-associated transcription factor (MITF) is a master regulator. One coumarin family member 7,8-dihydroxy-4-methylcoumarin (DHMC) shows extensive biological activities with beneficial health effects; however, it also induces cytotoxicity and its melanogenic effect has not been reported yet. Therefore, we first synthesized DHMC derivatives via methylation to obtain 7,8-dimethoxy-4-methylcoumairn (DMMC), and investigated the pro- or anti-melanogenic effects of DHMC and DMMC in B16-F10 melanoma cells as well as the underlying mechanism. DHMC showed cytotoxicity at all tested concentrations, whereas DMMC did not reduce cell viability, even at the high concentration. DMMC also drives the significant increase in intracellular melanin and tyrosinase activity. Moreover, DMMC induced MITF expression by significantly increasing tyrosinase activity, which activates the gene expression of TRP1 and TRP2. Western blotting confirmed that DMMC induced the activation of mitogen-activated protein kinase (MAPK) signaling by the phosphorylation of C-Jun N-terminal kinase (JNK), resulting in the increased melanin production and the decreased phosphorylation of protein kinase B. Collectively, this study showed the pro-melanogenic effect of DMMC and its potential as a safe tanning and dyeing agent.
    Type of Medium: Online Resource
    ISSN: 1934-578X , 1555-9475
    URL: Article
    DOI: 10.1177/1934578X221076647
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2022
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  • 5
    Online Resource
    Online Resource
    In Vitro Anti-Inflammatory and Skin Moisturizing Properties of Pilea martini (Levl.) Hand.-Mazz. Extracts
    SAGE Publications ; 2020
    In:  Natural Product Communications Vol. 15, No. 11 ( 2020-11), p. 1934578X2096786-
    Details
    In: Natural Product Communications, SAGE Publications, Vol. 15, No. 11 ( 2020-11), p. 1934578X2096786-
    Abstract: The in vitro anti-inflammatory and skin moisturizing activities of Pilea martini (Levl.) Hand.-Mazz. were investigated on lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages and human immortalized keratinocytes. Chromatographic analysis was performed to identify the chemical composition of the extracts. Pilea martini extracts significantly suppressed LPS-induced nitric oxide, prostaglandin E 2 , interleukin 6, and tumor necrosis factor α production in dose-dependent manners. In addition, the extracts inhibited LPS-induced inducible nitric oxide synthase and cyclooxygenase-2 proteins and their mRNA expression through causing a downregulation of nuclear factor-κB, activator protein 1, and mitogen-activated protein kinase signaling cascades. The extracts increased the production of hyaluronic acid levels and enhanced the expression levels of both filaggrin and serine palmitoyltransferase regulation. Liquid chromatography-mass spectroscopy analysis showed that the extracts contained 6 different compounds (malic acid, tryptophan, chlorogenic acid, caffeic acid, p-coumaric acid, and isoquercetin) that may contribute to their bioactivities. Taken together, Pilea martini extract showed remarkable promise as an anti-inflammatory and moisturizing agent.
    Type of Medium: Online Resource
    ISSN: 1934-578X , 1555-9475
    URL: Article
    DOI: 10.1177/1934578X20967866
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2020
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  • 6
    Online Resource
    Online Resource
    Long-term adefovir dipivoxil monotherapy for up to 5 years in lamivudine-resistant chronic hepatitis B
    SAGE Publications ; 2010
    In:  Antiviral Therapy Vol. 15, No. 2 ( 2010-02), p. 235-241
    Details
    In: Antiviral Therapy, SAGE Publications, Vol. 15, No. 2 ( 2010-02), p. 235-241
    Abstract: Large clinical studies assessing long-term adefovir dipivoxil salvage monotherapy in patients with lamivudine-resistant chronic hepatitis B (CHB) are lacking, particularly in patients positive for hepatitis B e antigen (HBeAg). We assessed the efficacy and resistance profile of adefovir dipivoxil monotherapy for up to 5 years in a large cohort of Korean patients with lamivudine-resistant CHB. Methods A total of 320 patients (81.3% HBeAg-positive; 100% genotype C) with confirmed genotypic lamivudine-resistant CHB were switched to adefovir dipivoxil 10 mg once daily. Liver function tests and HBV DNA were monitored every 3 months. Genotypic resistance to adefovir dipivoxil was performed in patients with detectable HBV DNA. Results The overall cumulative virological response rate at 5 years of adefovir dipivoxil therapy was 48.8%. The virological response rate was significantly higher in HBeAg-negative patients (62.0% versus 45.9%; P=0.010). Most cases of virological response (131/134, 97.8%) occurred within the first 36 months of therapy. The 5-year cumulative probability of genotypic resistance and virological breakthrough was 65.6% and 61.8%, respectively. Predictive factors for a virological response included baseline HBeAg seronegativity, HBV DNA≤8 log 10 copies/ml and achievement of an on-treatment initial virological response. Conclusions Adefovir dipivoxil salvage monotherapy for lamivudine-resistant CHB resulted in a modest cumulative virological response rate at 5 years, which was associated with progressive antiviral resistance. Consequently, adefovir monotherapy is not preferable as a first-line strategy for lamivudine resistance where combination lamivudine plus adefovir dipivoxil therapy is available.
    Type of Medium: Online Resource
    ISSN: 1359-6535 , 2040-2058
    URL: Article
    DOI: 10.3851/IMP1510
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2010
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