Lignan glucosides from Gentiana macrophylla with potential anti-arthritis and hepatoprotective activities.

Ten lignans, including six previously undescribed phenolic ester glycosyl lignans (1-6), were isolated from a well-known traditional Chinese medicine, Qin-Jiao, which is the dry root of Gentiana macrophylla Pall. (Gentianaceae). Their structures were determined by spectroscopic and chemical methods, especially 2D NMR techniques. Quantum chemical calculations of theoretical ECD spectra allowed the determination of their absolute configurations. Refer to its traditional applications for the treatment of rheumatic arthralgia and hepatopathy, these compounds were evaluated on a TNF-α induced MH7A human synoviocyte inflammation model and a D-GalN induced AML12 hepatocyte injury model. Compounds 1, 2, 5, and 6 significantly reduced the release of proinflammatory cytokine IL-1ß in MH7A cells at 15 µM and they also could strongly protect AML12 cells against D-GalN injury at 30 µM. Flow cytometry and Western blot analysis showed that compound 5 ameliorated D-GalN induced AML12 cell apoptosis by upregulating the expression of anti-apoptotic Bcl-2 protein and down-regulating the expression of pro-apoptotic Bax protein.

The regulatory effects of the apelin/APJ system on depression: A prospective therapeutic target.

Depression is a debilitating neuropsychological disorder characterized by high incidence, high recurrence, high suicide, and high disability rates, which poses serious threats to human health and imposes heavy psychological and economic burdens on family and society. The pathogenesis of depression is extremely complex, and its etiology is multifactorial. Mounting evidence suggests that apelin and apelin receptor APJ, which compose the apelin/APJ system, are related to the development of depression. However, the specific mechanism is still unclear, and research in this area in human is still insufficient. Acceleration of research into the regulatory effects and underlying mechanisms of the apelin/APJ system in depression may identify attractive therapeutic targets and contribute to the development of novel intervention strategies against this devastating psychological disorder. In this review, we mainly discuss the regulatory effects of apelin/APJ system on depression and its potential therapeutic applications.

Study on the mechanism of stir-fried Fructus Tribuli in enhancing the essential hypertension treatment by an integrated "spectrum-effect relationship-network pharmacology-metabolomics" strategy.

Essential hypertension (EH) is a leading cause of cardiovascular morbidity and mortality. Fructus Tribuli (FT), as a traditional medicine, has been frequently used for thousands of years. The crude Fructus Tribuli (CFT), decoction pieces being processed to remove impurities, have been listed as an important medicine for the treatment of hypertension in the elderly. According to the theory of traditional Chinese medicine, the CFT can enhance the EH treatment after being stir-fried into stir-fried Fructus Tribuli (SFT). At present, whether the SFT can enhance the EH treatment and its potential pharmacodynamic substances and mechanism are unknown. In this study, an integrated "spectrum-effect relationship-network pharmacology-metabolomics" strategy was used. Using male spontaneously hypertensive rats as an experimental model, we compared the therapeutic effects of CFT and SFT on EH. Subsequently, to define the pharmacodynamic material basis of SFT in enhancing the EH treatment, the steroidal saponins (main active components of FT) were selected for spectrum-effect relationship analysis. Furthermore, we applied the joint pathway analysis of network pharmacology and metabolomics to explore the underlying mechanism of SFT in enhancing the EH treatment. Results showed that SFT was better than CFT in the EH treatment. The steroidal saponins transformed by stir-frying were the potential pharmacodynamic substances that SFT could enhance the EH treatment. And the mechanism of action might be associated with regulating glycerophospholipid metabolism and arachidonic acid metabolism, especially arachidonic acid metabolism. This study provided a scientific basis for the clinical use of SFT as an important medicine for the EH treatment.

The moisturizing effect of Capparis spinosa fruit extract targeting filaggrin synthesis and degradation.

BACKGROUND: Small molecular natural products, such as betaine, have unique moisturizing advantages. Capparis spinosa L. fruit is rich in quaternary ammonium alkaloids such as betaine and stachydrine. However, few studies investigated its efficacy and mechanism on human skin. OBJECTIVE: Polysaccharides-free C. spinosa fruit extract (CS) was obtained to study its moisturizing effect and mechanisms focusing on filaggrin (FLG) synthesis and degradation. METHODS: The clinical moisturizing test was carried out on human arms, calves, and faces after CS treatment for 0.5-6 h. The change in the level of FLG, caspase 14, loricrin, and transglutaminase 5 (TGM 5) was measured by immunofluorescence after CS treatment for 4 and 24 h in a reconstructed epidermis model. Also, the content of pyrrolidone carboxylic acid (PCA) in the stratum corneum was tested by high-performance liquid chromatography (HPLC) both in the epidermis model and human calves. RESULTS: Compared with glycerin (positive control), 5% CS showed a strong skin hydration effect on arms and calves when applied for 0.5-6 h. Also, the face hydration increased at 0.5 and 4 h. In addition, 3% CS applied to the recombinant epidermis model under low humidity promoted the immunodetected levels of caspase 14 and PCA content but reduced the levels of FLG at 4 h, however, the levels of FLG, loricrin, and TGM 5 were promoted at 24 h. Meanwhile, CS treatment for 4 h in human calves increased the PCA content in the stratum corneum by 29.9%. CONCLUSIONS: Topical application of CS on human skin showed an instant and long-lasting increase in skin hydration by regulating the FLG network. It promoted FLG degradation to form PCA at 4 h both in vivo and in vitro, increasing FLG synthesis after 24 h, potentially reforming the FLG monomer reservoir to alleviate the skin's dry condition.

Chemical composition of Blumea balsamifera and Magnolia sieboldii essential oils and prevention of UV-B radiation-induced skin photoaging.

Blumea balsamifera essential oils (BBEOs) and Magnolia sieboldii essential oils (MSEOs) have exhibited outstanding antioxidant, anti-bacterial and anti-inflammatory activities. However, their anti-photoaging ability is still unclear. In this study, the chemical compositions of BBEOs and MSEOs are firstly determined by GC-MS analysis, and then their anti-photoaging is evaluated via an ultraviolet radiation (UV-B) induced mice skin-injury model. A total of 35 and 33 components are identified from BBEOs and MSEOs, and their dominant compositions are caryophyllene (18.54%) and borneol (18.33%) in BBEOs, and ß-elemene (29.10%), γ-terpinene (17.01%) and (E)-ß-ocymene (11.69%) in MSEOs. According to the skin injury model, the application of BBEOs and MSEOs to mice skin can effectively inhibit skin photoaging by down-regulating the expression of inflammatory factors including TNF-α, IL-6 and IL-10. Clearly, both essential oils reveal the potential as additives in cosmetics for anti-photoaging.

Profiling of organosulfur compounds and amino acids in garlic from different regions of China.

The quality of garlic is mainly attributed to organosulfur compounds that are the secondary metabolites of certain amino acids. Herein, a sensitive and rapid method for the simultaneous determination of 7 organosulfur compounds and 21 amino acids using ultra-high-performance liquid chromatography coupled with tandem mass spectrometry (UHPLC-MS/MS) was developed. Then the levels of these 28 compounds and allicin in garlic among 242 samples from 6 provinces in China were profiled with multivariate data analysis. The results showed that garlic was rich in organosulfur compounds and could be a good supplement for amino acids. Contents of 29 compounds varied greatly among the provinces. The multivariate data analysis demonstrated two major groups for all samples, indicating that the location has a significant influence on the metabolism of garlic. Besides, the compositional differences of garlic from 6 provinces and correlations for growing conditions and contents of components were also analyzed.

[Rapid simultaneous determination of 10 nutrients in ginger by ultra-high performance liquid chromatography-tandem mass spectrometry].

An analytical method by ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) was developed for the simultaneous determination of the two types of nutrients, viz. gingerol-related compounds and curcuminoids in ginger, including 6-gingerol, 8-gingerol, 10-gingerol, 6-shogaol, 8-shogaol, 10-shogaol, tetrahydrocurcumin, curcumin, demethoxycurcumin and bisdemethoxycurcumin. The 10 target compounds were separated on a ZORBAX RRHD Eclipse Plus C18 column (100 mm×2.1 mm, 1.8 µm) using gradient elution with 0.1% (v/v) formic acid aqueous solution and methanol containing 0.1% (v/v) formic acid as the mobile phases. Qualitative confirmation and quantitative analysis of the target compounds were performed using an electrospray ionization (ESI) source in the positive ion and multiple reaction monitoring (MRM) modes. The linear correlation coefficients (r) of the 10 nutrients were ≥ 0.9995. The limits of quantification were 0.10-7.71 µg/L. The average spiked recoveries of the samples at the three levels were 82.8%-115.3%, the relative standard deviations (RSDs) were 0.58%-11.49%. The results showed that all the 10 nutrients in ginger were detected, and the content of 6-gingerol was the highest at 373.35-702.48 mg/kg. This method is convenient, rapid, accurate and reliable, and is suitable for the analysis of gingerol-related and curcuminoids in ginger. It provides a technical means for the quality identification and control of ginger.

Deanxit relieves symptoms in a patient with jackhammer esophagus: A case report.

Jackhammer (hypercontractile) esophagus presents with dysphagia and chest pain. Current treatments are limited. We describe a 60-year-old man who presented with dysphagia, chest pain and heartburn for a period of 1 year. His workup showed Barrett's esophagus on endoscopy and high-resolution manometry demonstrated jackhammer esophagus with esophagogastric junction outflow obstruction. The patient was treated with proton pump inhibitor and nifedipine but without resolution of his symptoms. He was followed up to assess the efficacy of treatment with deanxit (flupentixol + melitracen). Dysphagia and chest pain resolved during the therapeutic trial and efficacy was maintained on maintenance treatment without troublesome side effects.

Analysis of six organophosphorus pesticide residues in apples and pears using cloud-point extraction coupled with HPLC-UV.

A cloud-point extraction (CPE) method with Triton X-114 has been developed for analysis of six organophosphorus pesticides (OPPs) in apples and pears. In this CPE procedure, the effects of the surfactant volume, mass of sodium chloride, equilibrium temperature, equilibrium time, and pH on the extraction procedure were investigated. Under the optimal CPE conditions, the analytes were enriched 20-fold and the LODs dropped to 0.44-5.20 microg/kg. Furthermore, the proposed extraction method was validated by the correlation coefficient (R2) of the calibration curve, repeatability (RSD, n = 6), and fortified recoveries, which were 0.9967-0.9993, 2.7-6.5, and 74.7-104.5%, respectively. Based on these results, it could be concluded that the proposed CPE method with Triton X-114 was suitable for the effective extraction and enrichment of OPP residues in the apple and pear samples.

Mechanism of the Synergistic Toxicity of Malononitrile and p -Nitrobenzaldehyde with Photobacterium phosphoreum.

In this study the mechanism of synergistic toxicity between malononitrile and p -nitrobenzaldehyde was revealed by examining their toxicodynamic and toxicokinetic interactions. The investigation of the toxicodynamic interactions focused on the interactions among malononitrile, p -nitrobenzaldehyde, and luciferase, and found that malononitrile does not induce luciferase to bind p -nitrobenzaldehyde. This result suggested that the synergistic toxicity does not arise from toxicodynamic interactions. Further research on toxicokinetic interactions compared the amounts of p -nitrobenzaldehyde being transported from the water phase to the biotic phase in two circumstances--in the presence of malononitrile and in its absence. The results of this research indicated that in the presence of malononitrile, more p -nitrobenzaldehyde is transported, and it is the increased amount of p -nitrobenzaldehyde that leads to the synergistic toxicity of malononitrile and p -nitrobenzaldehyde.