Qualitative and quantitative study of flavonoids in Notoginseng Radix et Rhizoma based on UPLC-Q-TOF-MS and HPLC-DAD / 中国中药杂志

The flavonoids in Panax notoginseng were qualitatively analyzed by ultra-high performance liquid chromatography-quadrupole-time of flight mass spectrometry(UPLC-Q-TOF-MS), and the content of three main flavonoids in P. notoginseng of different specifications and grades collected from different habitats was determined by HPLC-DAD. Flavonoids and anthocyanins were analyzed by UPLC-Q-TOF-MS/MS in the positive and negative ion modes, respectively. Twelve flavonoid glycosides and one anthocyanin glycoside in P. notoginseng were identified, but no flavonoid aglycones were detected. Among them, 12 compounds were identified in the underground part of P. notoginseng for the first time and eight compounds were first reported in this plant. Moreover, six and four compounds were identified in the Panax genus and the Araliaceae family for the first time, respectively. A method for simultaneous determination of three flavonoids in P. notoginseng was established by HPLC-DAD. The content of flavonoids in 721 P. notoginseng samples of 124 specifications and grades collected from 20 different habitats was simultaneously determined. Among three flavonoids determined, the content of quercetin-3-O-(2″-β-D-xylosyl)-β-D-galactoside was the highest with the average content in the tested samples of 161.0 μg·g~(-1). The content of compounds quercetin-3-O-hexosyl-hexoside and kaempferol-3-O-pentosyl-hexoside was relatively low, with the average content of 18.5 μg·g~(-1)(calculated as quercetin-3-O-sophoroside) and 49.4 μg·g~(-1)(calculated as kaempferol-3-O-sangbu diglycoside). There were significant differences in flavonoids content of samples from different production area. The content of flavonoids in spring P. notoginseng was significantly lower than that in winter P. notoginseng when the other influencing factors such as production areas, germplasm resources, and cultivation conditions were fixed. As for P. notoginseng of different specifications, the flavonoid content in the part connecting the taproot and the aboveground stem was significantly higher than that in other parts. The results of large-scale data showed that the flavonoid content gradually increased with the increase in the number of heads. There were significant differences between the flavonoid content in most specifications and grades, especially the 20-head P. notoginseng and countless head P. notoginseng, whose content was significantly lower and significantly higher than that of other specifications and grades, respectively. This study provides a scientific basis for the study of the effective components and quality control of P. notoginseng from the perspective of flavonoids.

Correlation between active component content and color of Atractylodes Lancea and A. chinensis based on color difference principle / 中国中药杂志

We explored the correlations between the color difference values [ΔL~*(lightness), Δa~*(red-green), Δb~*(yellow-blue)] and the content of four active components(including sesquiterpenoids and polyacetylenes) in the powder of Atractylodes lancea and A. chinensis, aiming to provide reference for the quality evaluation of Atractylodis Rhizoma and establish a qualitative model that can distinguish between A. lancea and A. chinensis based on the chromatic values. The tristimulus values(L~*, a~*, and b~*) of 23 batches of A. lancea and A. chinensis were measured by a color difference meter. The content of atractylenolide Ⅱ, β-eudesmol, atractylodin, and atractylone in the 23 batches of samples were measured by high performance liquid chromatography(HPLC). Principal component analysis(PCA) and partial least squares-discriminant analysis(PLS-DA) were performed to establish the qualitative models for distinguishing between A. lancea and A. chinensis. SPSS was employed to analyze the correlations between the tristimulus values and the content of the four index components. The results showed that the established PCA and PLS-DA models can divide the A. lancea and A. chinensis samples into two regions, and the tristimulus values of A. lancea and A. chinensis were positively correlated with the content of β-eudesmol and atractylodin. Therefore, the PCA and PLS-DA models can successfully identify A. lancea and A. chinensis, and the appearance color can be used to quickly predict the internal quality of Atractylodis Rhizoma. This study provides a reference for the quality evaluation of Atractylodis Rhizoma and the modern research on the color of Chinese medicinal materials.

Role of pyroptosis in bilirubin-induced microglial injury / 中国当代儿科杂志

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.

Evaluation of the effect of using ultrasonic instruments to improve the shoulder of the preparations / 北京大学学报(医学版)

OBJECTIVE@#To provide the basis for the clinical development of ultrasonic shoulder preparation by comparing the roughness and three-dimensional topography of shoulder surface between ultrasonic instruments and conventional rotary instruments, to make preliminary suggestions for clinical use of ultrasonic instruments.@*METHODS@#(1) Four areas of buccal and palatal surfaces of six extracted human premolars were prepared with different grit size of rotary instruments. Polyether was used to take impression of the shoulder area, 3-D topography measurement laser microscope (3-D TMLM) was used to scan the impressions and compare the shoulder surface roughness of the four areas. (2) Six extracted human premolars were prepared, mesial half of the shoulder was finished with traditional rotary instruments and distal half with ultrasonic instruments. Polyether was used to take impression of the shoulder area, 3-D TMLM was used to scan the impressions and compare the shoulder surface roughness and 3-D topography, and the shoulder surface morphology was observed by surgical microscope (×25 magnification). (3) Twenty extracted human maxillary symmetrical homonymous anterior teeth were poured into die stone using artificial gingiva, ultrasonic instruments group and rotary instruments group were divided randomly. After preparing the teeth and taking the shoulder impression with polyether in dental simulate on the training system, the surface roughness of the shoulder impression in mesial, middle and distal areas was scanned and compared. The data were analyzed using SPSS 25.0 software package.@*RESULTS@#(1) There was no significant difference in Ra and Rz values between the abutment shoulder and impression shoulder in different areas. (2) The surface roughness of the shoulder impression prepared by ultrasonic instruments [Ra:(6.59±2.33) μm, Rz:(34.69±7.29) μm] was significantly smaller than that of the rotary instruments [Ra:(21.79±4.89) μm, Rz:(91.69±14.82) μm] (P < 0.05). The morphology of the shoulder prepared by ultrasonic instruments was clear and continuous under microscope observation. (3) The surface roughness of each area of the shoulder prepared by ultrasonic instruments was significantly lower than that of the rotary instruments (P < 0.001); there was no significant difference of the surface roughness (Ra) in each area of the shoulder impression after ultrasonic instrument preparation, while the shoulder impression roughness in the mesial and distal areas was significantly higher than that in the middle area (P < 0.001) after rotary instrument preparation.@*CONCLUSION@#Compared with the rotary instruments, the ultrasonic instruments can obtain a smoother shoulder surface, especially can significantly improve the shoulder preparation effect near the proximal surface.

Quality control of Shuanghuanglian preparations using an effect-constituent index / 药学学报

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.

Progress on HIV-1 RT inhibitors with novel mechanism of action / 药学学报

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.

Study of macrophage polarization on pulmonary fibrosis and signaling pathway / 中国中药杂志

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.

Construction of high quality Chrysanthemi Flos pieces standard system based on comprehensive analysis of ancient and modern Chinese and foreign pharmacopoeia / 中国中药杂志

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.

Evaluation of mesial displacement of mandibular complete dentures with long-centric occlusal pattern / 中华口腔医学杂志

<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>