[Characterization and identification of chemical constituents from Schizonepetae Spica based on UHPLC-Q-TOF-MS/MS technique].

The chemical constituents of Schizonepetae Spica were qualitatively analyzed by UHPLC-Q-TOF-MS/MS. An Agilent poroshell 120 SB-C_(18) column(3.0 mm×100 mm, 2.7 µm) was used for gradient elution with 0.1% formic acid water(A)-acetonitrile(B) solution as mobile phase at the flow rate of 0.4 mL·min~(-1) and column temperature of 45 ℃. The data were collected by scanning in positive and negative ion modes, and the compounds were identified by comparison of reference materials and PeakView software. Ninety-seven compounds were identified from Schizonepetae Spica, including 28 flavonoids, 23 phenolic acids, 23 fatty acids, 15 terpenoids, and 8 other compounds. The UHPLC-Q-TOF-MS/MS method established in this study can identify the chemical components of Schizonepetae Spica rapidly, accurately, and comprehensively, and provide a basis for the basic study of pharmacodynamic substances of Schizonepetae Spica.

Xanthones with Potential Anti-Inflammatory and Anti-HIV Effects from the Stems and Leaves of Cratoxylum cochinchinense.

Four new xanthones, cratocochinones A-D (1-4), together with eight known analogues (5-12), were isolated from the stems and leaves of Cratoxylum cochinchinense. The chemical structures of cratocochinones A-D (1-4) were elucidated by comprehensive spectroscopic analyses and the known compounds were identified by comparisons with the spectral data reported in the literature. All isolated compounds 1-12 were evaluated for their anti-inflammatory activities and anti-HIV-1 activities. Compounds 1-12 showed remarkable inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide in mouse macrophage RAW 264.7 cells in vitro, with IC50 values in the range of 0.86 ± 0.05 to 18.36 ± 0.21 µM. Meanwhile, compounds 1-12 exhibited significant anti-HIV-1 activities with EC50 which ranged from 0.22 to 11.23 µM. These findings indicate that the discoveries of these xanthones, isolated from the stems and leaves of C. cochinchinense, showing significant anti-inflammatory and anti-HIV-1 effects could be of great importance to the research and development of new natural anti-inflammatory and anti-HIV agents.

[Chemical constituents from stems and leaves of Cratoxylum cochinchinense and their inhibitory effects on proliferation of synoviocytes in vitro].

The chemical constituents from the stems and leaves of Cratoxylum cochinchinense were isolated and purified using silica gel, ODS gel, and Sephadex LH-20 gel column chromatography, as well as preparative HPLC. The chemical structures of all isolated compounds were identified on the basis of their physicochemical properties, spectroscopic analyses, and the comparison of their physicochemical and spectroscopic data with the reported data in literature. As a result, 21 compounds were isolated from the 90% ethanol extract of the stems and leaves of C. cochinchinense, which were identified as cratocochine(1), 1-hydroxy-3,7-dimethoxyxanthone(2), 1-hydroxy-5,6,7-trimethoxyxanthone(3), ferrxanthone(4), 3,6-dihydroxy-1,5-dimethoxyxanthone(5), 3,6-dihydroxy-1,7-dimethoxyxanthone(6), 1,2,5-trihydroxy-6,8-dimethoxyxanthone(7), securixanthone G(8), gentisein(9), 3,7-dihydroxy-1-methoxyxanthone(10), pancixanthone B(11), garcimangosxanthone A(12), pruniflorone L(13), 9-hydroxy alabaxanthone(14), cochinchinone A(15), luteolin(16), 3,5'-dimethoxy-4',7-epoxy-8,3'-neolignane-5,9,9'-triol(17), N-benzyl-9-oxo-10E,12E-octadecadienamide(18), 15-hydroxy-7,13E-labdadiene(19), stigmasta-4,22-dien-3-one(20), and stigmast-5-en-3ß-ol(21). Among these isolates, compound 1 was a new xanthone, compounds 2-5, 7, 8, 12, and 16-21 were isolated from the Cratoxylum plant for the first time, and compounds 11 and 13 were obtained from C. cochinchinense for the first time. Furthermore, all isolated compounds 1-21 were appraised for their anti-rheumatoid arthritis activities by MTS method through measuring their anti-proliferative effect on synoviocytes in vitro. As a result, xanthones 1-15 displayed notable anti-rheumatoid arthritis activities, which showed inhibitory effects on the proliferation of MH7A synoviocytes with the IC_(50) values ranging from(8.98±0.12) to(228.68±0.32) µmol·L~(-1).

[Synchronous evaluation of continuous dynamic dissolution and absorption of Compound Danshen Dropping Pills based on cellular bioelectrical effect].

The real-time cell-based assay(RTCA) was used to establish the bioelectrical sensing model of Compound Danshen Dripping Pills with rat cardiomyocytes(H9 c2). The time/dose-dependent cell response profiles(TCRPs) of in vitro dissolution and absorption of the pills were determined to establish the continuous dynamic dissolution and absorption kinetic models. Thereby, the cell index(CI)-based dissolution and absorption kinetic curves and kinetic models of Compound Danshen Dripping Pills were obtained. The optimal dissolution kinetic model was Weibull model. The similarity factors f_2 of dissolution curves were greater than 50 and the correlation coefficients of absorption curves were larger than 0.95. With the experiment about the efficacy on mice, percentages of the bleeding time of mice administrated with Compound Danshen Dripping Pills were calculated, and there was a correlation among dissolution, absorption, and efficacy curves(r > 0.9). RTCA is applicable to the study of the dissolution and absorption kinetics of solid compound Chinese medicine preparations. Thus, it is an innovative and feasible method to evaluate the quality and batch consistency of compound Chinese medicine preparations.

[Study on literature of Echinacea purpurea and discussion on its herbalization].

By consulting the literatures of foreign plant medicine Echinacea purpurea at home and abroad, this paper discusses the property and function of E. purpurea from the point of view of traditional Chinese medicine theory, so as to realize "herbalization", provide the theoretical basis of traditional Chinese medicine for the correct clinical application and rational compatibility of E. purpurea, and broaden the scope and varieties of clinical selection of traditional Chinese medicine. Relevant literatures of E. purpurea were selected from PubMed and CNKI databases and classified based on clinical application, chemical composition, pharmacological action, toxic and side effects. Those with a high reliability were screened out, including 313 articles in English and 46 in Chinese. Finally, the basic theory of traditional Chinese medicine was analyzed. In our view, E. purpurea features pungent and bitter tastes and a cold nature, and enters lung, spleen, heart meridians, with effects in evacuating wind-heat, clearing heat and detoxifying, invigorating Qi, strengthening body resistance, and treating wind-heat cold, sore throat swelling pain, cough, heat toxin stagnation, sore carbuncle swelling toxin, red swelling heat pain, body deficiency and multiple diseases, fatigue burnout. This paper analyzes the research literatures of E. purpurea, "herbalize" it, endows it with the property and function of traditional Chinese medicine, lays the foundation for further animal experiment and clinical research, and provides scientific theoretical guidance for the better application of E. purpurea in clinic and its proper compatibility and rational application. This research model will also provide reference for further studies of "traditional Chinese medicine" of foreign plant drugs, enrich traditional Chinese medicine resources, and promote the healthy and sustainable development of traditional Chinese medicine.

[Study on literature of artichoke and properties of traditional Chinese medicine].

In this article, the foreign and domestic literature on alien plant medicine Cynara scolymus was reviewed to explore its properties and functions in traditional Chinese medicine theory, and provide theoretical basis for clinical application and reasonable compatibility. Based on the literature databases of PubMed, Web of Science, Embase, the Cochrane Library, CNKI, VIP and Sinomed, the articles with high reliability related to C. scolymus were screened out and the obtained articles were systematically classified according to clinical application, chemical compositions, pharmacological action, toxic and side effects, etc. In the analysis with traditional Chinese medicine theory, it is concluded that: C. scolymus tastes bitter and slightly cold, attributing to spleen, stomach, liver and gall meridians. It has the functions of eliminating accumulation and guiding stagnation, regulating Qi-flowing for harmonizing stomach, clearing away dampness and heat, resolving turbidity and lowering blood lipids. It can be used for the treatment of dyspepsia, diet reduction, vomiting, nausea, abdominal distention, hypochondriac pain, jaundice, hyperlipidemia, etc. Through the analysis and research of the relevant literature on C. scolymus, the properties and functions of the drug were clarified, which could provide a theoretical basis for further animal experiments and clinical research. The research model of "traditional Chinese medicine theory" for alien plant medicines can provide reference for the introduction and research of botanical drugs around the world, which can greatly enrich Chinese medicine resources and is of great significance for promoting the sustainable development of traditional Chinese medicine.

[Safety evaluation and risk control measures of Cassiae Semen].

In this study, the authors reviewed domestic and foreign literatures, conducted the textual research on origin and development of Cassia Semen, studied records in ancient books and ancient and modern literatures, clinical adverse reactions and relevant experimental studies in recent years, and summarized the clinical features and influencing factors related to the safety of Cassiae Semen. According to the findings,Cassia Semen's safety risks are mainly liver and kidney system damages, with the main clinical features of fatigue, anorexia, disgusting of oil, yellow urine and gray stool; digestive system injury, with the main clinical features of diarrhea, abdominal distension, nausea and loose stool; reproductive system damage, with the main clinical features of vaginal bleeding. Allergic reactions and clinical adverse events, with the main clinical features for numb mouth, itching skin, nausea and vomiting, diarrhea, wheezing and lip cyanosis were also reported. The toxicological studies on toxic components of Cassiae Semen obtusifolia were carried out through acute toxicity test, subacute toxicity test, subchronic toxicity test and chronic toxicity test. Risk factors might include patients, compatibility and physicians. Physicians should strictly abide by the medication requirements in the Pharmacopoeia, pay attention to rational compatibility, appropriate dosage,correct usage and appropriate processing, control the dosage below 15 g to avoid excessive intake, strictly control the course of treatment to avoid accumulated poisoning caused by long-term administration. At the same time, clinicians should pay attention to the latest research progress, update the knowledge structure, quickly find the latest and useful materials from clinical practice, scientific research and drug information and other literatures, make evaluation and judgment for the materials, establish a traditional Chinese medicine intelligence information library, and strengthen the control over adverse effects with a pre-warning consciousness. The authors suggested standardizing clinical medication of Cassiae Semen, and avoiding misuse or excessive use; clinicians should prescribe it in strict accordance with there commended usage and dosage in the Pharmacopoeia, and focus on the safety signal accumulation in clinic, while strengthening studies for toxic substance basis and toxicity mechanism, in order to give full play to Cassiae Semen's clinical efficacy and reduce its adverse reactions.

PCSK9: A emerging participant in heart failure.

Heart failure (HF) is a complex clinical syndrome caused by various cardiovascular diseases. Its main pathogenesis includes cardiomyocyte loss, myocardial energy metabolism disorder, and activation of cardiac inflammation. Due to the clinically unsatisfactory treatment of heart failure, different mechanisms need to be explored to provide new targets for the treatment of this disease. Proprotein convertase subtilisin/kexin type 9 (PCSK9), a gene mainly related to familial hypercholesterolemia, was discovered in 2003. Aside from regulating lipid metabolism, PCSK9 may be involved in other biological processes such as apoptosis, autophagy, pyroptosis, inflammation, and tumor immunity and related to diabetes and neurodegenerative diseases. Recently, clinical data have shown that the circulating PCSK9 level is significantly increased in patients with heart failure, and it is related to the prognosis for heart failure. Furthermore, in animal models and patients with myocardial infarction, PCSK9 in the infarct margin area was also found to be significantly increased, which further suggested that PCSK9 might be closely related to heart failure. However, the specific mechanism of how PCSK9 participates in heart failure remains to be further explored. The purpose of this review is to summarize the potential mechanism of PCSK9's involvement in heart failure, thereby providing a new treatment strategy for heart failure.

Antibacterial activity and main action pathway of benzyl isothiocyanate extracted from papaya seeds.

The development of natural antimicrobial agents has attracted long-term attention due to the increasing demand for food preservation. Papaya, a widely cultivated nutritious tropical fruit, has benzyl isothiocyanate (BITC) as one of the most important secondary metabolites in its seeds. And the antibacterial activity of BITC toward different strains and the main antibacterial pathway remain unclear. The current study focused on characterizing the antibacterial effect and exploring the major bacteriostatic pathway of BITC. BITC was shown to have a broad-spectrum antibacterial effect, with a minimum inhibitory concentration of 1 µL/mL for Escherichia coli, Bacillus subtilis, and Aspergillus niger, and 0.5 µL/mL for Salmonella enterica, Staphylococcus aureus, and Penicillium citrinum. Additionally, BITC was identified to affect the integrity of the biological oxidation system rather than the permeability or morphology of cell membranes. Furthermore, BITC was found not only to affect ATP production but also to hinder a series of important chemical reactions of the coenzymes involved in the transfer of hydrogen ions in the respiratory chain. The bacteriostatic pathway of BITC was shown to be implicated in an incomplete respiratory chain and the deregulation of the metabolism system. These results indicate the potential of BITC as a natural preservative in the food industry. PRACTICAL APPLICATION: BITC is present in papaya seeds and can be extracted and purified. Exploring its antibacterial activity and main action pathway may facilitate its application as a new bacteriostatic agent in food industry.