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The bromodomain and extraterminal (BET) family member BRD4 is pivotal in the pathogenesis of cardiac hypertrophy. BRD4 induces hypertrophic gene expression by binding to the acetylated chromatin, facilitating the phosphorylation of RNA polymerases II (Pol II) and leading to transcription elongation. The present study identified a novel post-translational modification of BRD4: poly(ADP-ribosyl)ation (PARylation), that was mediated by poly(ADP-ribose)polymerase-1 (PARP1) in cardiac hypertrophy. BRD4 silencing or BET inhibitors JQ1 and MS417 prevented cardiac hypertrophic responses induced by isoproterenol (ISO), whereas overexpression of BRD4 promoted cardiac hypertrophy, confirming the critical role of BRD4 in pathological cardiac hypertrophy. PARP1 was activated in ISO-induced cardiac hypertrophy and facilitated the development of cardiac hypertrophy. BRD4 was involved in the prohypertrophic effect of PARP1, as implied by the observations that BRD4 inhibition or silencing reversed PARP1-induced hypertrophic responses, and that BRD4 overexpression suppressed the anti-hypertrophic effect of PARP1 inhibitors. Interactions of BRD4 and PARP1 were observed by co-immunoprecipitation and immunofluorescence. PARylation of BRD4 induced by PARP1 was investigated by PARylation assays. In response to hypertrophic stimuli like ISO, PARylation level of BRD4 was elevated, along with enhanced interactions between BRD4 and PARP1. By investigating the PARylation of truncation mutants of BRD4, the C-terminal domain (CTD) was identified as the PARylation modification sites of BRD4. PARylation of BRD4 facilitated its binding to the transcription start sites (TSS) of hypertrophic genes, resulting in enhanced phosphorylation of RNA Pol II and transcription activation of hypertrophic genes. The present findings suggest that strategies targeting inhibition of PARP1-BRD4 might have therapeutic potential for pathological cardiac hypertrophy.
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0.05).Conclusion:Treatment of angina pectoris with syndrome of accumulation phlegm-heat in the interior with cariac blood stasis by Xihuang Pills was safe and effective.
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[Objective] To establish the quality standard for Guanxin Qiwei Tablet. [Methods] Radix Salviae Miltiorrhizae, Lignum Dalbergiae Odoriferae, Rhizoma Kaempferiae and Fructus Choerospondiatis in Guanxin Qiwei Tablet were identified by TLC. TanshinoneⅡA content was determined by HPLC.[Results] Radix Salviae Miltiorrhizae, Lignum Dalbergiae Odoriferae, Rhizoma Kaempferiae and Fructus Choerospondiatis can be identified by TLC, the spot being clear without the interference of negative control. A good linearity was in the range of 0.022-0.154 ?g, the average recovery of tanshinone ⅡA was 97.9%, and RSD was 1.22%. [Conclusion] This method is simple and can be used to evaluate the quality of Guanxin Qiwei Tablet.
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Objective To establish the quality standard for Tiaojing Pills. Methods Radix Angelicae Sinensis and Rhizoma Chuanxiong in Tiaojing Pills were identified by TLC and the content of paeoniflorin was determined by HPLC. Results Radix Angelicae Sinensis and Rhizoma Chuanxiong could be identified by TLC. Paeoniflorin showed a good linearity in the range of 0.086 88～0.868 8 ?g,r=0.999 6.The average recovery was 101.28 %,and RSD was 1.31 %. Conclusion The established methods are simple,convenient and reproducible,and can be used for the quality control of Tiaojing Pills.
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Objective To establish a method of determining effective components in Tangzhiqing Capsule.Methods Gin- seng saponin Rg_1,Rb_1,Re and notoginseng saponin R_1 in the capsule were separated and purified by D_(101)macroporous absorption resin,and then determined by HPLC.Results The linearity arrange of ginseng saponin Rg_1,Re,Rb_1 and no- toginseng saponin R_1 were 1.88～11.28?g,1.76～10.56?g,0.294～1.764?g,0.752～2.256?g and the recov- eries were 101.51%(RSD=0.75%),100.58%(RSD=0.46%),100.29%(RSD=1.01%),98.64% (RSD = 0.73%)respectively.Conclusion The method is simple,feasible and reproducible,and can be used for the determination of effective components in Tangzhiqing Capsule.
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Objective To compare the influence of different extraction technology on the pharmacodynamic actions of drug pair of Rhizoma Atractylodis Macrocephalae and Radix Paeoniae Alba.Methods The influences of water extraction,alcohol extraction,and SFE-CO2 extraction on pharmacodynamic actions of drug pair of Rhizoma Atractylodis Macrocephalae and Radix Paeoniae Alba were evaluated by mice intestine propulsive motility test,rats repelling acute gastric mucosa damage test,mice twisting test and hot-plate test.Results The paired drugs extracted by SFE-CO2 combining with water extraction or alcohol extraction had better pharmacological actions.Conclusion This study provides a scientific basis for optimizing the extraction technology of drug pair of Rhizoma Atractylodis Macrocephalae and Radix Paeoniae Alba.
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AIM: To establish a method of determining the content of volatility contents in Baicao Oil. METHODS: The content of menthol, cinnamaldehyde, and eugenol were determined by gas chromatography. RESULTS: Menthol, cinnamaldehyde, and eugenol were well separated and the linearity was fine with the recovery in the range of 98%-102%. CONCLUSION: The method is rapid, stable and accurate. It can be used to control the quality of this preparation.
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AIM: To establish the quality standard for Compound Lonicera Granules. METHODS: Fructus Forsythiae was identified by TLC.Chlorogenic acid and Baicalin were determined by HPLC. RESULTS: Fructus Forsythiae could be detected by TLC. Chlorogenic acid showed a good linear relationship at a range of 0.108～0.649?g,r=0.9999. The average recovery was 100.87%,and RSD was 1.28%.The linearity of baicalin was found in the range of 0.156～1.400?g.The average recovery was 101.31%, and RSD was 0.32%. CONCLUSION: The established methods are simple,quick and good reproductive. This study provids a method for the quality control of Compound Lonicera Granules.