Effect of hepatocyte damage in hepatic fibrogenesis of patients infected with Schistosoma japonicum.

Schistosomiasis is a serious public health problem, and previous studies found that liver function and hepatic cells are damaged. To evaluate the serum parameters of liver function and fibrosis in schistosomiasis patients infected with Schistosoma japonicum (Schistosoma J.) and analyze the correlations between liver function and serum fibrosis markers in patients infected with Schistosoma J., this retrospective study enrolled 133 patients. The study population was divided into four groups: healthy people control group (n = 20), chronic schistosomiasis without liver cirrhosis (CS) group (n = 21), schistosomiasis cirrhosis without hypoalbuminemia (SC-HA) group (n = 68), and schistosomiasis cirrhosis with hypoalbuminemia (SC +HA) group (n = 24). Clinical and laboratory data were collected for analysis. In the multiple comparison of abnormal rates of aspartate aminotransferase (AST) and total bilirubin (TBIL), the abnormal rate of the SC +HA group was significantly higher than that of the other three groups (P < 0.05), and the abnormal rate of γ-GT in the SC +HA group was significantly higher than that in the control group (P < 0.05). Multiple comparison results of serum levels of fibrosis markers showed that the SC group had a significantly higher level of indexes than other groups (P < 0.05). The levels of TGF-ß1 in the CS group, SC-HA group and SC +HA group were significantly higher than those in the control group (P < 0.001). Our study demonstrated that the liver function and hepatic cells were damaged with the progression of liver disease in patients infected with Schistosoma J., and they played an important role in the occurrence and development of liver fibrosis.

Design, synthesis, and evaluation of a carboxylesterase detection probe with therapeutic effects.

In this study, a lysosomal targeting fluorescent probe recognition on CEs was designed and synthesized. The obtained probe BF2-cur-Mor demonstrated excellent selectivity, sensitivity, pH-independence, and enzyme affinity towards CEs within 5 min. BF2-cur-Mor could enable recognition of intracellular CEs and elucidate that the CEs content of different cancer cells follows the rule of HepG2 > HCT-116 > A549 > HeLa, and the CEs expression level of hepatoma cancer cells far exceeds that of normal hepatic cells, being in good agreement with the previous reports. The ability of BF2-cur-Mor to monitor CEs in vivo was confirmed by zebrafish experiment. BF2-cur-Mor exhibits some pharmacological activity in that it can induce apoptosis in hepatocellular carcinoma cells but is weaker in normal hepatocyte cells, being expected to be a potential "diagnostic and therapeutic integration" tool for the clinical diagnosis of CEs-related diseases.

Development and Validation of a Nomogram to Predict Overall Survival in Stage I-III Colorectal Cancer Patients after Radical Resection with Normal Preoperative Serum Carcinoembryonic Antigen.

We aimed to develop a clinical predictive model for predicting the overall survival (OS) in stage I-III CRC patients after radical resection with normal preoperative CEA. This study included 1082 consecutive patients. They were further divided into a training set (70%) and a validation set (30%). The selection of variables for the model was informed by the Akaike information criterion. After that, the clinical predictive model was constructed, evaluated, and validated. The net reclassification index (NRI) and integrated discrimination improvement (IDI) were employed to compare the models. Age, histologic type, pT stage, pN stage, carbohydrate antigen 242 (CA242), and carbohydrate antigen 125 (CA125) were selected to establish a clinical prediction model for OS. The concordance index (C-index) (0.748 for the training set and 0.702 for the validation set) indicated that the nomogram had good discrimination ability. The decision curve analysis highlighted that the model has superior efficiency in clinical decision-making. NRI and IDI showed that the established nomogram markedly outperformed the TNM stage. The new clinical prediction model was notably superior to the AJCC 8th TNM stage, and it can be used to accurately assess the OS of stage I-III CRC patients undergoing radical resection with normal preoperative CEA.

Glucoraphanin and sulforaphane biosynthesis by melatonin mediating nitric oxide in hairy roots of broccoli (Brassica oleracea L. var. italica Planch): insights from transcriptome data.

Glucoraphanin (GRA) is present in the seeds and nutrient organs of broccoli and is the precursor of the anti-cancer compound sulforaphane (SF). The hairy roots obtained by infecting broccoli (Brassica oleracea L. var. Italic Planch) leaves with Agrobacterium rhizogenes (ATCC15834) are phytohormonally autonomous, genetically stable, and can produce large amounts of the anti-cancer substance SF. Melatonin (MT) is a natural hormone widely found in plants. Studies have shown that melatonin can regulate the synthesis of secondary metabolites of downstream targets by mediating the synthesis of signal molecules. However, whether MT regulates the synthesis of NO and H2O2 and mediates the synthesis mechanism of secondary metabolites, GRA and SF, is not yet clear. In this study, the hairy roots of broccoli were treated with 500 µmol/L MT, and the genome of broccoli (Brassica oleracea L. var. botrytis L) was used as the reference genome for transcriptome analysis. By this approach, we found that MT regulates the synthesis of NO and H2O2 and mediates the synthesis of secondary metabolites GRA and SF. GO annotations indicated that DEGs involved in the MT treatment of broccoli hairy roots were mainly related to catalytic activity, cells, and metabolic processes; the KEGG pathway analysis indicated that MT treatment likely affects the hormone signal transduction process in broccoli hairy roots; broccoli hairy roots were treated with 500 µmol/L MT for 0, 6, 12, 20, and 32 h, respectively; compared with 0 h, the yield of GRA and SF increased under the other treatments. The highest yields of GRA and SF occurred at 12 h. The NO content was the highest at 12 h, and the H2O2 content was positively correlated with MT concentration. The content of NO and H2O2 were regulated, and the content of GRA and SF was increased under MT treatment. NO synthase inhibitor (L-NAME and TUN) could effectively inhibit the content of NO in broccoli hairy roots and reduce GRA and SF yield; MT could regulate NO levels by regulating NO synthesis-related enzymes and could alleviate the reduction of NO content in tissue cells caused by NO synthase inhibitor and promote NO synthesis. These results have important theoretical implications for understanding the regulation of GRA and SF synthesis events by NO and H2O2.

Transcriptome analysis of genes related to glucoraphanin and sulforaphane synthesis in methyl jasmonate treated broccoli (Brassica oleracea var. italica) hairy roots.

Hairy roots obtained by infecting broccoli (Brassica oleracea var. italica) leaves with Agrobacterium rhizogenes (ATCC15834) have the characteristics of phytohormone autonomy, genetic stability and can produce a large amount of the anti-cancer substance Sulforaphane (SF) and the biosynthetic precursor Glucoraphanin (GRA). Under the induction of the exogenous signaling molecule methyl jasmonate (MeJA), the production of SF in broccoli hairy roots was significantly increased. However, the molecular mechanism of GRA and SF synthesis in hairy roots of broccoli treated with MeJA has not been reported. In this study, according to the yield of GRA and SF, the best concentration of MeJA treatment for hairy roots of broccoli was selected. After 18 days of growth, broccoli hairy roots were treated with 10 mmol L-1 MeJA for 0, 3, 6, 9 and 12 h. Compared with 0 h, the yield of GRA and SF increased under other treatments. The highest yield of GRA and SF occurred at 9 h, which were 2.22-fold and 1.74-fold higher than those at 0 h. Brassica oleracea var. botrytis was used as reference genome, and 5,757 differentially expressed genes (DEG) were observed at 0, 3, 6, 9 and 12 h under 10 mmol L-1 MeJA treatment, of which 4,673 were down-regulated and 1084 were up-regulated. The key genes regulating GRA synthesis, CYP79F1, CYP83A1, UGT74B1, FMOGS-OX5 and GSL-OH, were up-regulated at 0 and 3 h, and down-regulated the rest of the time; BCAT2 was up-regulated at 6, 9, 12 h, and at 0, 3 h expression was down-regulated, transcription factors MYB28 and MYB29 were down-regulated by exogenous MeJA treatment. A pathway of GRA biosynthesis and transformation pathways in MeJA-treated broccoli hairy roots was simulated and the molecular mechanism of GRA biosynthesis and SF accumulation in broccoli hairy roots under MeJA treatment was revealed.

An Injectable Peptide Hydrogel Constructed of Natural Antimicrobial Peptide J-1 and ADP Shows Anti-Infection, Hemostasis, and Antiadhesion Efficacy.

Postoperative adhesion is a common complication of abdominal surgery, which always has many adverse effects in patients. At present, there is still a lack of effective treatment measures and materials to prevent adhesion in the clinics. Herein, we report the potential use of J-1-ADP hydrogel formed by natural antimicrobial peptide jelleine-1 (J-1) self-assembling in adenosine diphosphate (ADP) sodium solution to prevent postsurgery adhesion formation. J-1-ADP hydrogel was found to have good antimicrobial activity against the bacteria and fungi tested and can be used to prevent tissue infection, which was thought to be one of the incitements of adhesion. Due to ADP being a platelet-activating factor, J-1-ADP hydrogel showed significant hemostatic activity in vitro verified by whole blood coagulation, plasma coagulation, platelet activation, and platelet adhesion assays. Further, it showed potent hemostatic activity in a mouse liver hemorrhage model. Bleeding was believed to be a cause of the formation of postsurgery adhesion. J-1-ADP hydrogel had a significant antiadhesion effect in a rat side wall defect-cecum abrasion model. In addition, it had good biocompatibility and degradation properties. So the present study may provide an alternative strategy for designing antimicrobial peptide hydrogel material to prevent postoperative adhesion formation in the clinic.

The effects of incorporation of the counterparts and mimics of L-lysine on the antimicrobial activity, hemolytic activity, cytotoxicity and tryptic stability of antimicrobial peptide polybia-MPII.

Due to the limited effects of conventional antibiotics on the increasing emergence of drug-resistant bacteria and fungi, novel antimicrobial agents were urgently needed to alleviate this phenomenon. Nowadays, antimicrobial peptides are believed to be a promising candidate for a new generation of antimicrobial drugs. Antimicrobial peptide polybia-MPII (MPII) was first isolated from the venom of the social wasp Polybia paulista with a broad spectrum of antimicrobial activity. In the present study, the counterparts and mimics of cationic amino acids of Lys, such as Arg, His, Orn, Dab and Dap were employed to substitute Lys in the sequence of MPII. The effects of the incorporation of these amino acids on its antimicrobial activity, hemolytic activity, cytotoxicity, enzyme stability and therapeutic potential were explored. Our results showed that although the incorporation of Arg could improve its antimicrobial activity, there is no improvement in enzyme stability. The incorporation of His makes MPII exert its antimicrobial activity in a pH-dependent manner. Notably, incorporating Dap could effectively decrease its hemolytic activity and cytotoxicity and enhance its enzyme stability against trypsin. In conclusion, this study would provide an effective strategy to improve the bioavailability and metabolic stability of AMPs while decrease their hemolytic activity and cytotoxicity.

Hepatoprotective effects of Cassiae Semen on mice with non-alcoholic fatty liver disease based on gut microbiota.

Cassiae Semen (CS), the seeds of Cassia obtusifolia L. and C. tora L, have a long medicinal history in China, with suggestions for it to relieve constipation and exert hepatoprotective effects. However, the underlying mechanisms are still unclear. In this study, mice with high-fat diet (HFD)-induced non-alcoholic fatty liver disease (NAFLD) were used to study the hepatoprotective effects of CS. The relationship between gut microbiota and hepatoprotective effect mechanisms mediated by CS extracts, the total aglycone extracts of CS, rubrofusarin-6-ß-gentiobioside, and aurantio-obtusin were examined. Our data indicate that CS extracts and components confer a protective effect by ameliorating lipid accumulation, intestinal barrier damage, liver damage, and inflammation on HFD-induced liver injury. Meanwhile, fecal microbe transplantation exerted the pharmacological effect of CS on HFD-fed mice; however, the efficacy of CS was inhibited or eliminated by antibiotic-induced dysbiosis. In conclusion, the therapeutic effects of CS on NAFLD were closely related to the gut microbiota, suggesting a role for TCM in treating disease.

[Complanatoside A and complanatoside B in rats administered with raw and salt-processed Astragali Complanati Semen: a pharmacokinetics study].

An UPLC-MS/MS method was developed to simultaneously determine complanatoside A and complanatoside B in rat plasma with rutin as the internal standard and applied to examine the effect of salt-processing on pharmacokinetics of these two flavonoid glycosides. The pharmacokinetic parameters were estimated using DAS 3.2.6 and subjected to independent sample t-test with SPSS 23.0. No significant difference in T_(max) of complanatoside B was observed between the raw and processed groups; however, in the processed group, C_(max) and AUC_(0-12 h) of complanatoside B increased obviously(P<0.05), while MRT_(0-12 h) decreased from(3.34±0.44) h to(1.81±0.36) h(P<0.05). C_(max) [(14.72±11.13) µg·L~(-1)] and MRT_(0-24) [(3.93±0.26) h] of complanatoside A in the raw group were statistically different from those [(35.64±21.99) µg·L~(-1),(1.43±0.24) h] in the processed group(P<0.05). As a result, salt-processing can facilitate the in vivo adsorption and accelerate the excretion of complanatoside A and complanatoside B.

Transcriptomics analysis of genes induced by melatonin related to glucosinolates synthesis in broccoli hairy roots.

Glucoraphanin (GRA) is found in the seeds and vegetative organs of broccoli (Brassica oleracea L. var. italica Planch) as the precursor of anti-carcinogen sulforaphane (SF). The yield of GRA obtained from these materials is weak and the cost is high. In recent years, the production of plant secondary metabolites by large-scale hairy roots culture in vitro has succeeded in some species. Melatonin (MT) is a natural hormone which existed in numerous organisms. Studies have demonstrated that MT can improve the synthesis of secondary metabolites in plants. At present, it has not been reported that MT regulates the biosynthesis of glucoraphanin in broccoli hairy roots. In this study, the broccoli hairy roots that grew for 20 d were respectively treated by 500 µM MT for 0, 6, 12, 20 and 32. To explore the reason of changes in secondary metabolites and reveal the biosynthetic pathway of glucoraphanin at transcriptional level. Compared with 0 h, the yield of GRA under other treatments was increased, and the overall trend was firstly increased and then decreased. The total yield of GRA reached the highest at 12 h, which was 1.22-fold of 0 h. Then, the genome of broccoli as the reference, a total of 13234 differentially expressed genes (DEGs) were identified in broccoli hairy roots under treatment with 500 µM MT for 0, 6, 12, 20 and 32 h, respectively. Among these DEGs, 6266 (47.35%) were upregulated and 6968 (52.65%) were downregulated. It was found that the pathway of 'Glucosinolates biosynthesis (ko00966)' was enriched in the 16th place by Kyoto Encyclopedia of Genes and Genomes pathway enrichment analysis of the upregulated DEGs. The expression of key genes in the GRA biosynthesis pathway was upregulated at all time points, and a deduced GRA biosynthesis pathway map was constructed for reference.

Clinical significance of blood platelets and mean platelet volume in patients with ulcerative colitis.

OBJECTIVES: This retrospective study aimed to investigate and analyze the clinical significance of blood platelets (PLTs) and mean platelet volume (MPV) in patients with ulcerative colitis (UC). METHODS: A total of 132 patients with UC and 208 healthy subjects were enrolled. PLTs, MPV, platelet-large cell rate (P-LCR), C-reactive protein (CRP), fibrinogen (FIB) and D-dimer were analyzed. Correlations were calculated between disease activity/extent of disease and MPV, PLT, and CRP levels in patients with UC. RESULTS: PLT levels were significantly higher while MPV and P-LCR were lower in patients with UC compared with controls. Disease activity was positive correlated with CRP (r = 0.564) and PLT (r = 0.307) but negatively correlated with MPV (r = -0.351). Extent of disease was positively correlated with CRP (r = 0.312) but showed no correlation with PLTs and MPV. FIB and D-dimer were higher in patients with UC, but the difference in FIB levels was not statistically significant. CONCLUSIONS: PLTs and MPV are potential biomarkers for UC disease activity. These data may help clinicians to attain a more comprehensive judgment of the general condition of patients with UC.

An optimized analog of antimicrobial peptide Jelleine-1 shows enhanced antimicrobial activity against multidrug resistant P. aeruginosa and negligible toxicity in vitro and in vivo.

Due to the threat of escalating multi-drug resistant gram-negative bacteria to human health and life, novel antimicrobial agents against gram-negative pathogens are urgently needed. As antimicrobial peptides are not prone to induce bacteria resistance, they are believed to be one kind of promising class of potential antimicrobial agent candidates to combat multi-drug resistant bacteria for long-term use. Jelleine-1, first isolated from the royal jelly of honeybees, is a typical amphiphilic antimicrobial peptide and shows broad antimicrobial spectrum and negligible toxicity. To promote its antimicrobial activity and extend its potential of clinical use against multi-drug resistant gram-negative bacteria, novel analogs of jelleine-1 were designed, synthesized and their antimicrobial functions and toxicity were examined in this study. Our results showed that fine tuning of the cationic charge, polarity, and basicity of the sequence through amino acids substitution at position 3, 5, 7 and maintaining position 1, 4, 6, 8 unchanged could improve the bioactivity of jelleine-1 significantly. Meanwhile, we also found that the substitution of phenylalanine by tryptophan also could improve the antimicrobial activity of jelleine-1. Among all the analogs, analog 15, which is enriched in arginine and leucine, showed the most potent antimicrobial activity against both gram-negative and gram-positive bacteria, especially to multi-drug resistant Pseudomonas aeruginosa in vivo and in vitro. In addition, analog 15 also showed potent inhibition of the formation of multi-drug resistant P. aeruginosa biofilm and negligible toxicity, which was certified by MTT, hemolysis, blood assay, and biochemical analysis.

Multiple action mechanism and in vivo antimicrobial efficacy of antimicrobial peptide Jelleine-I.

With the extensive use of antibiotics in medicine, agriculture and food chemistry, the emergence of multi-drug resistant bacteria become more and more frequent and posed great threats to human health and life. So novel antimicrobial agents were urgently needed to defend the resistant bacteria. Jelleine-I was a small antimicrobial peptide (AMP) with eight amino acids in its sequence. It was believed to be an ideal template for developing antimicrobial agents. In the present study, the possible action mode against both gram-negative bacteria and gram-positive bacteria and in vivo antimicrobial activity was explored. Our results showed that Jelleine-I exhibits its antimicrobial activity mainly by disrupting the integrity of the cell membrane, which would not be affected by the conventional resistant mechanism. It also aims at some intracellular targets such as genomic DNA to inhibit the growth of microbes. In addition, the result of in vivo antimicrobial activity experiment showed that Jelleine-I performed a good therapeutic effect toward the mice with Escherichia coli infected peritonitis. Notably, Jelleine-I has negligible cytotoxicity toward the tested mammalian cells, indicating excellent cell selectivity between prokaryotic cells and eurkayotic cells. In summary, our results showed that Jelleine-I would be a potential candidate to be developed as a novel antimicrobial agent.

Farfarae Flos: A review of botany, traditional uses, phytochemistry, pharmacology, and toxicology.

ETHNOPHARMACOLOGICAL RELEVANCE: Farfarae Flos (FF; dried flower buds of Tussilago farfara L.), a widely used traditional Chinese medicine (TCM), is also known as "Kuandonghua" (Chinese: ). It has a wide range of pharmacological effects and has long been used to treat various respiratory conditions including cough, asthma, and acute or chronic bronchitis. AIMS: This study reviews the current advances in the research on the botany, ethnopharmacology, phytochemistry, pharmacology, and toxicology of Farfarae Flos. Prospects for future investigation and application of this herb are also discussed. MATERIALS AND METHODS: Information on FF was collected from both published materials (such as ancient and modern books, Ph.D. and M. Sc. dissertations, monographs on medicinal plants, and pharmacopoeia) and electronic databases (such as CNKI, SciFinder, WanFang data, PubMed, ScienceDirect, Web of Science, Taylor&Francis, ACS Publications, Wiley, Springer, Europe PMC, EBSCOhost, J-STAGE, and Google Scholar). RESULTS: Approximately 175 chemical compounds, including terpenoids, organic acids, flavonoids, alkaloids, chromones, volatile oils, and other compounds, have been isolated from FF. This TCM has been reported to produce pharmacological effects on the respiratory, cardiovascular, and digestive systems, and exert antioxidant, anti-inflammatory, and neuroprotective activities. FF is safe in the traditional dose range, but the potential toxicity due to the emergence of pyrrolidine alkaloids needs to be paid more attention. CONCLUSIONS: FF is a commonly used TCM with pharmacological activities mainly on the respiratory system. This study suggests that the further expansion of the pharmacological effect of FF and in-depth study of its prescription need to be concerned about. The investigations of the role of more active substances and the pharmacokinetics of the hepatotoxic components of FF will help to maximize the therapeutic potential and promote its popularization and application. Meanwhile, it is important to pay attention to pursue research on the similarities and differences between the leaves and the flower buds to find their respective advantages and make rational use of T. farfara L.

Traditional Chinese Medicine of Angelicae Pubescentis Radix: A Review of Phytochemistry, Pharmacology and Pharmacokinetics.

Angelicae Pubescentis Radix (APR) is a widely used antirheumatic Chinese medicinal herb known as "Duhuo" in China. It has the effects of dispelling wind and removing dampness, diffusing impediment, and relieving pain, and is mainly indicated for rheumatic arthritis with pain in the lower back and knees, and headache. To the best of our knowledge, an attempt is made to provide an up-to-date review on these aspects based on published materials, including ancient and modern books; Master's and doctoral theses; monographs on medicinal plants; the pharmacopoeia of different countries, websites for publication of patent and electronic databases, such as SCI finder, PubMed, Web of Science, ACS, Science Direct, Wiley, Springer, Taylor, CNKI, and Google Scholar. APR, which has a good clinical effect, has been used for traditional Chinese medicine more than 2000 years. Since 1957, a variety of chemical constituents have been reported from the medicinal plants of this herb, mostly coumarins and volatile oil. In the past 30 years, numerous studies have shown that the extracts and compounds isolated from APR showed effective analgesic and anti-inflammatory actions, also showing well effects on central nervous system, effects on cardiovascular system and deworming activity. In addition, we also present and discuss the botany, traditional medicinal use, pharmacokinetics, toxicity, quality control, future trends and prospects of APR. All this information suggest that future research of APR should be supplemented in the area of pharmacology and toxicology to provide further insight on the clinical use and quality control.

A model beyond protein corona: thermodynamics and binding stoichiometries of the interactions between ultrasmall gold nanoclusters and proteins.

Nanoparticles (NPs) will inevitably interact with proteins and form protein coronas once they are exposed to biological fluids. This conventional model for nano-bio interactions has been used for over twenty years. Growing numbers of new nanomaterials are emerging every year. Among them, noble metal nanoclusters (NMNCs) are new types of fluorescent nanomaterials with considerable advantages in biomedical applications. Compared with NPs (typically >10 nm) like Au NPs, carbon nanotubes, etc., NMNCs have ultrasmall sizes (∼2 nm), so when NMNCs are exposed to biological milieu, will they form protein coronas like NPs? Due to a lack of characterization techniques for ultrasmall nanoparticles (USNPs), to date, studies on the binding stoichiometries of USNPs to proteins have been heavily hampered. To address this challenge, we combined the characteristics of various methods and selected human serum albumin (HSA) and transferrin (Trf) as model proteins to study their interactions with dihydrolipoic acid (DHLA) protected gold nanoclusters (DHLA-AuNCs). Steady-state fluorescence, transient fluorescence spectroscopy and isothermal titration calorimetry (ITC) were used to study the thermodynamic parameters (K, ΔH, ΔS, ΔG) and interaction mechanisms. The results showed that the intrinsic fluorescence of both proteins was quenched by DHLA-AuNCs, and the quenching process of HSA was an endothermic dynamic process. In contrast, the quenching process of Trf was an exothermic static process. The combination of ITC, agarose gel electrophoresis (AGE) and zeta potential showed that one HSA could bind 8 ± 1 DHLA-AuNCs and one Trf could bind 7 ± 2 DHLA-AuNCs, which was quite different from the conventional model of protein coronas. Based on these findings, the "protein complex" was termed for proteins upon binding with USNPs. Dynamic light scattering (DLS), transmission electron microscopy (TEM), and atomic force microscopy (AFM) showed that DHLA-AuNCs could induce the agglomeration of proteins. Circular dichroism (CD) and synchronous fluorescence spectroscopy showed that DHLA-AuNCs had a very minor effect on the secondary structures of HSA and Trf, which demonstrated the good biocompatibility of DHLA-AuNCs at the molecular scale. This work has shed light on a new interaction model beyond the protein corona, indicating a possible biological identity of USNPs.

[Effects of processing on pharmacokinetics of Descurainiae Semen's constituents in rats].

An UPLC-MS/MS method simultaneously determining contents of quercetin-3-O-ß-D-glucose-7-O-ß-D-gentiobioside and sinapic acid in rats' plasma was firstly established and applied to study the effects of processing on pharmacokinetics of Descurainiae Semen's active constituents. Complantatoside A as internal standard,methanol used for protein precipitation,the method was validated according to the instructions of CFDA. Rats' plasma was collected after being oral administrated equal dosage of 60% ethanal extract of raw or processed Descurainiae Semen at different point of time,then the concentrations were determined to calculate pharmacokinetic parameters using DAS 3. 2. 6. And the parameters were analyzed using SPSS 23. 0,meantime the concentration-time curve was drawn.The results showed that processing had no effects on the pharmacokinetics of QGG,but could improve the absorption of sinapic acid and slow down the excretion.

MOFs-Derived Nano-CuO Modified Electrode as a Sensor for Determination of Hydrazine Hydrate in Aqueous Medium.

It very important to be able to efficiently detect hydrazine hydrate in an aqueous medium due to its high toxicity. Here, we have proposed a new idea: to construct a sensor for the rapid determination of hydrazine hydrate based on the nano-CuO derived by controlled pyrolysis of HKUST-1 [Cu3(BTC)2(H2O)3]. The as-prepared CuO at 400 °C possesses a uniform appearance with nano-structure via SEM images, and the nano-CuO-400 has exhibited excellent electrocatalytic activity towards hydrazine oxidation. Amperometric i-t curves shows the peak current as linearly proportional to the hydrazine concentration within 1.98-169.3 µmol L-1 and 232-2096 µmol L-1 with the detection limit of 2.55 × 10-8 mol L-1 and 7.01 × 10-8 mol L-1, respectively. Moreover, the sensor constructed in the experiment shows good selectivities, and it is feasible to determining actual water samples.

Chemical constituents from the seeds of Cassia obtusefolia and their in vitro α-glucosidase inhibitory and antioxidant activities.

Basing on chromatographic separation techniques, fifteen aglycones (1-15), including two new anthraquinone aglycones (1, 2) and thirteen known compounds (3-15), were isolated from the small polar fraction of Cassia obtusefolia (petroleum ether extract). Structural elucidations were performed by 1D/2D NMR spectroscopy and mass spectrometry. The in vitro antioxidant and α-glucosidase inhibitory activities of these fifteen compounds were determined. Except compounds 12 (IC50 3.03 ±â€¯0.31 µg/mL, stronger than ascorbic acid, which IC50 was 6.48 ±â€¯2.30 µg/mL) and 13 (IC50 78.40 ±â€¯2.39 µg/mL), the free radical scavenging capacities of other compounds were weak. Compounds 4, 5, 6 and 13 exhibited inhibitory activities on α-glucosidase with IC50 values of 50.60 ±â€¯1.10, 22.57 ±â€¯0.07, 60.09 ±â€¯1.40, and 80.01 ±â€¯2.66 µg/mL separately, however, all the α-glucosidase inhibitory activities were weaker than positive control (acarbose).

A review of the phytochemistry and pharmacological activities of Magnoliae officinalis cortex.

ETHNOPHARMACOLOGICAL RELEVANCE: Magnoliae Officinalis Cortex (the dried bark of Magnolia officinalis), a widely used traditional Chinese medicine, is also known as 'Houpo' (Chinese: ). Magnoliae Officinalis Cortex has a wide range of pharmacological effects and has been used to treat conditions such as abdominal distention, vomiting, diarrhea, food accumulation, Qi stagnation, constipation, phlegm and fluid retention and cough resulting from asthma. AIMS OF THE REVIEW: The present paper reviews advances in research relating to the botany, ethnopharmacology, phytochemistry, pharmacology and toxicology of Magnoliae Officinalis Cortex. Prospects for future investigation and application of this herb are also discussed. MATERIALS AND METHODS: Information on Magnoliae Officinalis Cortex was obtained from published materials, including ancient and modern books; PhD and MSc dissertations; monographs on medicinal plants; the pharmacopoeia of different countries and electronic databases, such as SCI finder, PubMed, Web of Science, ACS, Science Direct, Wiley, Springer, Taylor, AGRIS, Europe PMC, EBSCO host, CNKI, WanFang DATA, J-STAGE and Google Scholar. RESULTS: More than 200 chemical compounds have been isolated from Magnoliae Officinalis Cortex, including lignans, phenylethanoid glycosides, phenolic glycosides, alkaloids, steroids and essential oils. The plant has been reported to have pharmacological effects on the digestive system, nervous system and cardiovascular and cerebrovascular systems, as well as antibacterial, anti-tumour, analgesic, anti-inflammatory and anti-oxidative effects. CONCLUSIONS: Magnoliae Officinalis Cortex is an essential traditional Chinese medicine with pharmacological activities that mainly affect the digestive system, nervous system and cardiovascular and cerebrovascular systems. This review summarises its botany, ethnopharmacology, phytochemistry, pharmacology and toxicology. These information suggest that we should focus on the development of new drugs related to Magnoliae Officinalis Cortex, including specific constituents, so that Magnoliae Officinalis Cortex can exert greater therapeutic potential. Meanwhile, it is important to pay attention to the rational use of Magnolia resources, avoiding over-harvesting which could lead to lack of resources. We should also pursue research on Magnolia substitutes and develop resources such as Magnoliae Officinalis Flos and Magnolia Leaf.