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Article in Chinese | WPRIM | ID: wpr-828626


OBJECTIVE@#To study whether pyroptosis is involved in the bilirubin-induced injury of primary cultured rat cortical microglial cells.@*METHODS@#Primary cultured rat cortical microglial cells were randomly administered with 30 μmol/L bilirubin (bilirubin group), 30 μmol/L bilirubin following 30 μmol/L VX-765 pretreatment (VX-765+bilirubin group), or an equal volume of dimethyl sulfoxide (control group). Modified MTT assay was used to measure the viability of microglial cells. Western blot was used to measure the expression of the pyroptosis-related proteins Caspase-1 and gasdermin D (GSDMD). Lactate dehydrogenase (LDH)-release assay was used to evaluate the cytotoxicity of microglial cells. EtBr/EthD2 with different molecular weights (394 Da/1 293 Da) was used to measure the size of plasma membrane pores. ELISA was used to measure the level of the inflammatory factor interleukin-1β (IL-1β) in culture supernatant.@*RESULTS@#After bilirubin stimulation, the viability of microglial cells decreased and LDH release increased, both in a time-dependent manner. Compared with the control group, the bilirubin group had a significantly higher positive rate of small-molecule EtBr passing through the cell membrane (P0.05). The expression of activated Caspase-1 significantly increased at 0.5 hour after bilirubin stimulation (P<0.05), and that of activated GSDMD significantly increased at 6 hours after bilirubin stimulation (P<0.05). The release of IL-1β significantly increased at 6 hours after bilirubin stimulation and reached the peak at 24 hours (P<0.001). Compared with the bilirubin group, the VX-765+bilirubin group had a significant increase in cell viability (P<0.05) and significant reductions in the expression of activated GSDMD, the pass rate of EtBr, and the release of LDH and IL-1β (P<0.05).@*CONCLUSIONS@#Pyroptosis is involved in bilirubin-induced injury of primary cultured microglial cells.

Animals , Bilirubin , Caspase 1 , Cell Survival , Interleukin-1beta , Pyroptosis , Rats
Acta Pharmaceutica Sinica ; (12): 2149-2154, 2019.
Article in Chinese | WPRIM | ID: wpr-780333


We established a quality evaluation method for Shuanghuanglian preparations based on an effect-constituent index (ECI), which is guided by the clinical efficacy of Shuanghuanglian and a dose-efficacy correlation. An HPLC method was used to establish the quantitative fingerprint of Shuanghuanglian from different manufacturers and to determine the content of 10 fingerprint components, including baicalin, chlorogenic acid, forsythin, galuteolin, wogonin, forsythoside A, luteolin, caffeic acid, baicalein, and scutellarin. Using Staphylococcus aureus as biological model, the potency of Shuanghuanglian preparations was determined by antibiotic microbial assay. Using the method of PLC-DA, the efficacious antibacterial components were screened by "dose-efficacy" correlation analysis. According to the antibacterial potency and content of the antibacterial ingredients, combined with the method of the custom weight coefficient, ECI was calculated and verified. The results show that the antibacterial ECI can facilitate evaluation of the efficacy of Shuanghuanglian based on the composition of its contents, providing a new method for the quality control of traditional Chinese medicine.

Article in Chinese | WPRIM | ID: wpr-775332


Macrophages are a group of immune cells with pluripotency and plasticity that can differentiate into different phenotypes under different microenvironments in vitro and in vivo. In the development of pulmonary fibrosis, there are alveolar macrophages and interstitial macrophages, which are polarized to different cell phenotypes at different stages of development. And their polarized phenotypes include M1 macrophages and M2 macrophages. In the inflammation early stages of pulmonary fibrosis, the increase of classical activated macrophages are helpful to clear pathogenic microorganisms and promote the progress of inflammation. In the fibrosis stage, the alternatively activated macrophages increased, which inhibiting the inflammatory reaction or directly promoting tissue fibrosis, on the other hand, it also promoting the fibrosis degradation. To clarify the polarization and polarization mechanisms of macrophages in pulmonary fibrosis will be conducive to the treatment of pulmonary fibrosis. In IPF, the polarization mechanism of M1 and M2 is closely related to TGF-β1/Smad. TGF-β1/Smad pathway plays an important regulatory role in liver fibrosis, renal fibrosis, myocardial fibrosis, scars, tumors and other diseases. Blocking the signaling of TGF-β1 by Smad3 and Smad4 is beneficial to inhibit the polarization of AM, which in turn helps to inhibit the progression of IPF.

Fibrosis , Humans , Inflammation , Macrophages , Pulmonary Fibrosis , Signal Transduction
Article in Chinese | WPRIM | ID: wpr-690689


To study the evolution of Chinese ancient and modern pharmacopoeia standards and compare the domestic and foreign pharmacopoeias, further understand the international requirements on chrysanthemum quality, and establish a more suitable and modern standard system for high quality Chrysanthemi Flos pieces. Newly Revised Materia Medica, Welfare Pharmacy, Collected Essentials of Species of Materia Medica (Bencao Pinhui Jingyao), Chinese Pharmacopoeia and other herbal remedies in various generations were reviewed to summarize the evolution of domestic standards on Chrysanthemi Flos pieces. Then they were compared with those in European Pharmacopoeia, United States Pharmacopoeia, Japanese Pharmacopoeia and other foreign Pharmacopoeias to establish a modern and international high-quality Chrysanthemi Flos pieces standard system with Chinese medicine characteristics and produce more internationally recognized high-quality Chinese medicine pieces.

Acta Pharmaceutica Sinica ; (12): 691-700, 2018.
Article in Chinese | WPRIM | ID: wpr-779924


HIV-1 reverse transcriptase (RT) plays an important role in HIV-1 life cycle. At present, the listed NRTIs and NNRTIs targeting the RT showed high efficiency as clinical first-line drugs. However, the rapid emergence of multidrug-resistant viruses and significant cumulative drug toxicities compromises antiretroviral therapy efficacy and limits therapeutic options. Therefore, there is an urgent demand for new types of RT inhibitors with novel mechanism of action to address this challenge. In recent years, additional inhibitors with novel mechanism of action have been reported, including nucleic acid competitive inhibitors, reverse transcriptase-directed mutagenesis inhibitors, primers/templates-competitive reverse transcriptase inhibitors, polymerase-RNase H inhibitors, reverse transcription initiation process inhibitors, peptide inhibitors etc., which have brought new hope to the development of novel anti-HIV drugs. This article focuses on the development of these inhibitors.

Chinese Journal of Stomatology ; (12): 418-421, 2008.
Article in Chinese | WPRIM | ID: wpr-251041


<p><b>OBJECTIVE</b>To evaluate whether the mesial displacement of the mandibular complete dentures with long-centric occlusal pattern could meet the long centric of edentulous patients and to verify the design theory of the long-centric occlusal pattern of complete dentures.</p><p><b>METHODS</b>Complete dentures with three different occlusal patterns were made for each of 10 edentulous patients. Gothic arch tracing apparatus was used to record the long centric of edentulous patients. Three-dimensional measuring apparatus was used to measure the mesial displacement of mandibular dentures with three occlusal patterns. Comparison of the mesial displacement of three occlusal pattern dentures was made each other and with the long centric of the patients respectively.</p><p><b>RESULTS</b>The mean of long centric was (1.02 +/- 0.36) mm. The means of mesial displacement of mandibular complete dentures were as follows: the long-centric occlusal pattern dentures (1.016 +/- 0.348) mm, the linear occlusal dentures (1.092 +/- 0.448) mm, the anatomic occlusal dentures (0.409 +/- 0.253) mm.</p><p><b>CONCLUSIONS</b>The mandibular complete dentures with long-centric occlusal pattern can meet the physiological requirement for the long centric of edentulous patients and achieve a free slide from the centric relation position to the muscular contact position of the mandible.</p>

Aged , Centric Relation , Dental Occlusion , Denture Design , Denture, Complete , Female , Humans , Male , Middle Aged