Xuebijing injection, a Chinese patent medicine, against severe pneumonia: Current research progress and future perspectives.

Severe pneumonia is one of the most common infectious diseases and the leading cause of sepsis and septic shock. Preventing infection, balancing the patient's immune status, and anti-coagulation therapy are all important elements in the treatment of severe pneumonia. As multi-target agents, Xuebijing injection (XBJ) has shown unique advantages in targeting complex conditions and saving the lives of patients with severe pneumonia. This review outlines progress in the understanding of XBJ's anti-inflammatory, endotoxin antagonism, and anticoagulation effects. From the hundreds of publications released over the past few years, the key results from representative clinical studies of XBJ in the treatment of severe pneumonia were selected and summarized. XBJ was observed to effectively suppress the release of pro-inflammatory cytokines, counter the effects of endotoxin, and assert an anticoagulation effect in most clinical trials, which are consistent with experimental studies. Collectively, this evidence suggests that XBJ could play an important and expanding role in clinical medicine, especially for sepsis, septic shock and severe pneumonia. Please cite this article as: Zhang M, Zheng R, Liu WJ, Hou JL, Yang YL, Shang HC. Xuebijing injection, a Chinese patent medicine, against severe pneumonia: Current research progress and future perspectives. J Integr Med. 2023; 21(5): 413-422.

Online pharmaceutical process analysis of Chinese medicine using a miniature mass spectrometer: Extraction of active ingredients as an example.

The automation of traditional Chinese medicine (TCM) pharmaceuticals has driven the development of process analysis from offline to online. Most of common online process analytical technologies are based on spectroscopy, making the identification and quantification of specific ingredients still a challenge. Herein, we developed a quality control (QC) system for monitoring TCM pharmaceuticals based on paper spray ionization miniature mass spectrometry (mini-MS). It enabled real-time online qualitative and quantitative detection of target ingredients in herbal extracts using mini-MS without chromatographic separation for the first time. Dynamic changes of alkaloids in Aconiti Lateralis Radix Praeparata (Fuzi) during decoction were used as examples, and the scientific principle of Fuzi compatibility was also investigated. Finally, the system was verified to work stably at the hourly level for pilot-scale extraction. This mini-MS based online analytical system is expected to be further developed for QC applications in a wider range of pharmaceutical processes.

Discovery of imidazo[1,2-b]pyridazine macrocyclic derivatives as novel ALK inhibitors capable of combating multiple resistant mutants.

Anaplastic lymphoma kinase (ALK)-tyrosine kinase inhibitor (TKI) often loses effectiveness against non-small cell lung malignancies (NSCLCs) with ALK gene rearrangements (ALK+). 19 novel imidazo[1,2-b]pyridazine macrocyclic derivatives were designed, synthesized, and tested for their biological activities in an effort to develop ALK inhibitors that would overcome second-generation ALK-TKIs, particularly the G1202R mutation and the lorlatinib-resistant L1196M/G1202R double mutations. Of all the target substances, O-10 had the most effective enzymatic inhibitory activity, with IC50 values for ALKWT, ALKG1202R, and ALKL1196M/G1202R of 2.6, 6.4, and 23 nM, respectively. O-10, on the other hand, reduced the growth of ALK-positive Karpas299, BaF3-EML4-ALKG1202R, and BaF3-EML4-ALKL1196M/G1202R cells with IC50 values of 38, 52, and 64 nM, respectively. This was equally effective to the reference drug Repotrectinib (IC50 = 40, 164, and 208 nM). The kinase selectivity profile, liver microsome stability test and in vivo pharmacokinetic properties in SD rats of compound O-10 were further evaluated. O-10 was regarded as an effective ALK inhibitor for the treatment of mutations overall.

Forensic Examination of Six Homicide Injection Cases.

OBJECTIVES: To retrospectively analyze homicide cases of death after injection and provide reference for forensic identification. METHODS: Six homicide cases of death after injection which were investigated by the Criminal Investigation Team of Shanghai Public Security Bureau were collected and analyzed, including case situation, scene investigation, autopsy and other materials. RESULTS: The 6 cases were premeditated crimes, 5 cases took place in private spaces, and 5 cases involved the victims approached by suspects' decoy. There were no obvious abnormalities at the scene of the 6 cases. In 6 cases, the victim's body surface injury was mild or no, lividity color was abnormal, and the needlestick injury showed different manifestations from conventional medical measures. CONCLUSIONS: Death after injection is a highly concealed crime and easy to be ignored. For the suspected injection injury found in autopsy, it is necessary to carefully examine, identify and analyze, be alert to the situation of injecting poison (drug) and do a good job in evidence fixation and material extraction.

Design, synthesis and biological evaluation of novel macrocyclic derivatives bearing aniline pyrimidine scaffolds as EGFR-TKIs.

Based on EGFR-TKI Osimertinib as lead compound, a series of novel macrocyclic derivatives bearing aniline pyrimidine scaffolds were designed and synthesized by macrocyclization. Their structures were identified by 1H NMR, 13C NMR, 19F NMR and HRMS. The pharmacological activities of the target compounds were tested and the preliminary structure-activity relationship was discussed. Among them, 17-membered ring compound H1 displayed the best inhibitory activities against EGFRL858R/T790M and EGFRd746-750/T790M with IC50 value of 2.92 nM and 0.34 nM, respectively. Exhilaratingly, 17-membered ring compound H7 possessed the most potent antiproliferative activity against BaF3-EGFRdel19/T790M cell lines (IC50 = 0.035 µm), which rivaled that of Osimertinib (IC50 = 0.033 µm).

[Pollution Characteristics and Source Analysis of Aromatic Compounds in Shijiazhuang].

To understand the pollution characteristics of aromatic compounds in Shijiazhuang, PM2.5 samples were collected day and night for 30 days from September 18 to October 17, 2016. Qualitative and quantitative analyses were conducted using gas chromatography-mass spectrometry (GC-MS). The results showed that total average concentration of aromatic compounds was 33.5 ng·m-3, lower than that of levoglucosan (487 ng·m-3). Concentration of nitro-aromatic compounds was the highest (20.4 ng·m-3), followed by aromatic acids (9.94 ng·m-3) and aromatic aldehydes (3.14 ng·m-3). Influenced by the decrease in the boundary layer and temperature, concentration of 8 substances during night was higher than during the day. There was a significant positive correlation between levoglucosan and nitro-aromatic, aromatic aldehyde, and aromatic acid compounds, with correlation coefficients (r) of 0.6829, 0.6443, and 0.6782, respectively, indicating that biomass burning is an important primary source of aromatic compounds that directly affects their concentrations in the atmosphere. Based on the analysis of daily variation trends in total concentration of aromatic compounds and the backward trajectory model, it was found that the pollution of aromatic compounds in Shijiazhuang in autumn was affected by regional transportation and local emissions.

Enantiomeric separation of vilanterol trifenatate by chiral liquid chromatography.

Vilanterol trifenatate is a novel chiral long-acting ß2-agonist developed. Vilanterol combined with inhaled corticosteroids can treat COPD and asthma. A simple liquid chromatographic method is developed for the quantitative determination of R-vilanterol and S-vilanterol (impurity S). HPLC separation was achieved on Chiralpak ID (250 × 4.6 mm; particle size 5 µm) column using hexane-ethanol-ethanolamine (75:25:0.1, v/v/v) as mobile phase at a flow rate of 1.0 mL/min. The resolution is greater than 3.3. Ethanolamine in the mobile phase is vital to enhance chromatographic efficiency and resolution between the isomers. The method was validated with respect to accuracy, specificity, precision, LOD, LOQ, linearity, and robustness as ICH guidelines.

Chemical Synthesis of the ODM-201's Diastereomers through an Efficient Intramolecular 1,3-Dipolar Cycloaddition.

An efficient synthesis of ODM-201's diastereomers has been developed from (R)-methyl 3-hydroxybutanoate or (S)-methyl 3-hydroxybutanoate, respectively, with high overall yield and excellent diastereomeric purity. The key step in this synthesis is the preparation of the key intermediate (R)-5-(1-((tert-butyldimethylsilyl)oxy)ethyl)-1H-pyrazole-3-carboxylic acid or (S)-5-(1-((tert-butyldimethylsilyl)oxy)ethyl)-1H-pyrazole-3-carboxylic acid through intramolecular 1,3-dipolar cycloaddition of the vinyl diazo carbonyl compounds.

Retrospective analysis of 319 hanging and strangulation cases between 2001 and 2014 in Shanghai.

In this study, we retrospectively analyzed 141 cases of hanging and 178 cases of ligature strangulation recorded in the Shanghai Municipal Public Security Bureau between January 2001 and December 2014 to explore the characteristics of hanging and ligature strangulation and to supply a scientific reference for forensic pathology. Several significant differences between hanging and ligature strangulation were found. Hanging cases were mostly suicide, with some accidental cases. Strangulation cases were mostly homicide, with a few cases of suicide or sexual asphyxia. Male hanging was more common than female hanging, with a ratio of 5:2. However, there were more female than male strangulation cases, with a ratio of 13:5. The ligature marks in hanging cases were almost all of a "U" type and above the hyoid bone. The ligature marks in strangulation cases were almost always a closed circle, but the position varied. The most common vital reactions were subcutaneous hemorrhage, exfoliation and blister, which are strong evidence of antemortem injury. Hemorrhagic spots were found on the temporalis, scalp, chest and back in strangulation cases, but were rare in hanging cases. Hemorrhagic manifestations were most common in the sternocleidomastoid muscle in hanging cases, and in the sternohyoid and sternothyroid muscles in strangulation cases. Fractures occurred in only ∼17% of victims. There are notable differences between hanging and ligature strangulation, which can help distinguish between these causes of death. These characteristics should be considered in forensic practice.

[Analysis of false-positive hyoid fractures: 12 forensic identification cases].

OBJECTIVE: To study the causes of false-positive hyoid fractures and forensic identification. METHODS: Twelve cases of false-positive hyoid fractures were collected and analyzed. RESULTS: Improper dissection technique (4 cases) and congenital separation (8 cases) were the main reasons for false-positive hyoid fractures. CONCLUSION: True fractures can be differentiated from false-positive hyoid fractures. False-positive hyoid fracture caused by improper dissection technique can be identified through examination of peripheral muscle, soft tissue hemorrhage, and the characteristics of fracture end.