The mechanism research of Xiaoyan Lidan formula for the intervention of chronic intrahepatic cholestasis based on metabolomics combined with molecular docking analysis / 药学学报

In this study, the mechanism of Xiaoyan Lidan formula (XYLDF) against 3,5-diethoxycarbonyl-1,4-dihydro-2,4,6-collidine (DDC)-induced chronic intrahepatic cholestasis (CIHC) in mice was investigated based on metabolomics, molecular docking and pharmacological methods. In the pharmacodynamics study, a dosage of 5 g·kg-1 (clinical equivalent) XYLDF was administered in DDC-induced mice, then the effect of XYLDF against CIHC was evaluated by measuring the levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (AKP) as well as total bilirubin (TBIL) in serum and observing liver histopathological changes. All experiments were approved by the Ethical Committee Experimental Animal Center of Guangzhou University of Chinese Medicine (ZYD-2021-001). The serum metabolites of mice in each group were detected and identified based on ultra-performance liquid chromatography quadrupole time-of-flight tandem mass spectrometry, and the relevant biological pathways and molecular key targets were further enriched. Molecular docking technology was used to further evaluate the binding activity of the main active ingredients of XYLDF with potential targets. Subsequently, the in vitro experiment was conducted for the validation of the vital target. The results showed that compared with the model group, XYLDF significantly decreased the levels of ALT, AST, AKP and TBIL in the serum of CIHC mice, as well as alleviated inflammatory infiltration and hepatocyte necrosis in liver tissue. According to the metabonomic study, a total of 35 differential metabolites was identified as biomarkers associated with cholestasis, 12 of which were significantly recovered by XYLDF treatment. These biomarkers were involved in the pathways of primary bile acid biosynthesis and linoleic metabolism, which are closely related to the mechanism of XYLDF against CIHC. Protein-protein interaction network indicated that cytochrome P450 3A4 (CYP3A4) and cytochrome P450 1A1 (CYP1A1) are significant potential targets with good binding properties with six major active ingredients of XYLDF. Furthermore, it was found that 4-methoxy-5-hydroxycanthin-6-one, dehydroandrographolide and isodocarpin, three of the main active components in XYLDF, markedly induced the expression of CYP3A4 mRNA in vitro. This study revealed that XYLDF mainly mediates the biosynthesis of bile acids in CIHC mice to improve liver tissue lesions and bile efflux disorders, among which, CYP3A4 is the key target in the protection of XYLDF against CIHC. This research provides a reference for further elucidation of the pharmacological mechanism of XYLDF.

Development of monoclonal antibody based IgG and IgM ELISA for diagnosis of severe fever with thrombocytopenia syndrome virus infection

ABSTRACT Introduction: Severe fever with thrombocytopenia syndrome virus (SFTSV) is a newly emerged virus that poses a great threat to human health because of high fatality rate. Methods: To develop sensitive and specific sero-diagnostic systems for SFTSV infections, monoclonal antibodies (MAbs) against recombinant SFTSV nucleocapsid (rSFTSV-N) protein were developed by immunizing BALB/C mice with rSFTSV-N protein and fusing the spleen cells with SP2/0 myeloma cells. Three hybridoma cell lines secreting MAbs against rSFTSV-N were obtained. MAb based IgG sandwich enzyme linked immunosorbent assay (ELISA) and IgM capture ELISA systems were established by using the newly developed MAbs. One hundred fifteen clinical suspected SFTS patients serum samples were used to evaluate the newly established systems by comparing with the total antibody detecting sandwich ELISA system and indirect ELISA systems. Results: The MAbs based sandwich IgG ELISA was perfectly matched with that of the total antibody sandwich ELISA and the indirect IgG ELISA. IgM capture ELISA results perfectly matched with that of the total antibody sandwich ELISA while detecting eight additional positive samples missed by the indirect IgM ELISA. Conclusions: The MAbs against rSFTSV-N protein offer new tools for SFTSV studies and our newly developed MAb-based IgG and IgM capture ELISA systems would offer safe and useful tools for diagnosis of SFTS virus infections and epidemiological investigations.

Analysis of projects funded by NSFC in field of Chinese medicine toxicology from 2012 to 2021 / 中国中药杂志

This study mainly introduced the research on Chinese medicine toxicology funded by the National Natural Science Foundation of China(NSFC) in 2012-2021 and analyzed the research content. Furthermore, key research topics and characteristic research projects were discussed, such as the toxicity mechanism, relationship between toxicity and efficacy, toxicity-alleviating mechanisms, and new technology and methods. The review suggested that researchers should gain an in-depth understanding of the "toxicity" of Chinese me-dicine, turned to characteristic research topics, and build a toxicological research paradigm suited to the characteristics of Chinese medicine in project application.

New tirucallane-type triterpenoids from the resin of Boswellia carteriiand their NO inhibitory activities / 中国天然药物

Six new tirucallane-type triterpenoids (1-6), along with ten known triterpenoids, were isolated from methylene chloride extract of the resin of Boswellia carterii Birdw. By the application of the comprehensive spectroscopic data, the structures of the compounds were clarified. The experimental electronic circular dichroism spectra were compared with those calculated, which allowed to assign the absolute configurations. Compounds 5 and 6 possesed a 2, 3-seco tirucallane-type triterpenoid skeleton, which were first reported. Their inhibitory activity against NO formation in LPS-activated BV-2 cells were evaluated. Compound 9 showed appreciable inhibitory effect, with an IC

Analysis of research status based on projects in pharmacokinetics of traditional Chinese medicine funded by National Natural Science Foundation of China / 中国中药杂志

The pharmacokinetics of traditional Chinese medicine is a subject that studies the dynamic changes of the absorption, distribution, metabolism and excretion of complex components of traditional Chinese medicine, which is an important method for elucidating the pharmacodynamic material basis, action characteristics, and compatibility mechanisms of traditional Chinese medicine. However, given on the fact that traditional Chinese medicine is a multi-dimensional and complex system with multiple components, multiple pathways, multiple targets, and an unclear pharmacodynamic material basis, the research on the pharmacokinetics of traditio-nal Chinese medicine has become a scientific and technological problem. Although the pharmacokinetics of traditional Chinese medicine has achieved remarkable development with the emergence of new theories, methods and technologies, there are still some problems in the application of the research direction of the pharmacokinetics of traditional Chinese medicine judging from the current application of the National Natural Science Foundation of China. Therefore, this article discussed the current research status on pharmacokinetics of traditional Chinese medicines by analyzing the projects funded by the National Natural Science Foundation of China in the past 5 years from 2016 to 2020, mainly including the application and funding analysis, main research contents of the projects in pharmacokinetics of traditional Chinese medicines. And the research hotspots, difficulties and deficiencies were focused in order to provide certain reference for researchers engaged in pharmacokinetics of traditional Chinese medicine.

Analysis of projects funded by NSFC in field of Chinese materia medica quality evaluation in recent five years / 中草药

The paper reviewed the funding situation of Chinese materia medica quality evaluation projects in Medical Science Department, National Natural Science Foundation of China in recent five years. The research progress and achievements of some funded projects were summarized from the perspectives of research approach, new technique and innovation of Chinese materia medica quality evaluation. The types of projects funded and supportive organizations were analyzed, and the problems of the applications have been also summarized so as to provide the reference for the subsequent applicants.

A new diterpenoid alkaloid isolated from Delphinium caeruleum / 中国天然药物

The present study was designed to determine the chemical constituents of Delphinium caeruleum Jacq. ex Camb.. The chemical constituents were isolated and purified by column chromatography with silica gel, ODS, and Sephadex LH-20. Their structures were elucidated by IR, MS, and NMR. Ten compounds were obtained and identified as caerudelphinine A (1), lycoctonine (2), talitine B (3), talitine A (4), talitine C (5), tatsienine-V (6), d-magnoflorine (7), 2-trimethyl-ammonio-3-(3-indolyl) propionate (8), vakhmatine (9), and delatisine (10). Compound 1 was a new lycoctonine-type C19-diterpenoid alkaloid, and compounds 4-10 were isolated from this plant for the first time.

Interaction of phenylethanoid glycosides and calf thymus DNA / 中国中药杂志

In physiological condition, the interaction of acteoside and forsythoside B with calf thymus DNA using neutral red (NR) as a fluorescence probe were investigated by fluorescence, UV-visible spectrophotometry, viscosity, DNA melting techniques, and molecular docking. It is observed that acteoside and forsythoside B can react with DNA. The major mode of recognition between drug and DNA is groove binding by hydrogen bonds, and the interaction of acteoside with DNA is stronger than that of forsythoside B.

Development of an Analgesia Therapy System for Delivery Based on Bio-feedback Transcuataneous Electrical Nerve Stimulation / 生物医学工程学杂志

Transcuataneous electrical nerve stimulation (TENS) analgesia as a non-drug method has received people's more and more attention recently. Considering problems of existing products, such as unstable performance and unsatisfied effectiveness, we developed a new analgesia therapy system for delivery based on bio-feedback TENS in our laboratory. We proposed a new idea for stimulation signal design, that is, we modulated a middle frequency signal by a traditional low frequency TENS wave in the new system. We designed different prescription waves for pain relief during a uterine contraction or massage between contractions. In the end, a bio-feedback TENS method was proposed, in which the waveforms of stimulation signals were selected and their parameters were modified automatically based on feedback from uterine pressure, etc. It was proved through quality tests and clinical trials that the system had good performance and satisfied analgesia effectiveness.

A new steroid with long cross-conjugation structure from the marine-derived fungus Aspergillus aculeatus / 药学学报

A new steroid with a long cross-conjugation structure, 15a-hydroxy-(22E, 24R)-ergosta-3, 5, 8 (14), 22-tetraen-7-one (1), was isolated from the marine-derived fungus Aspergillus aculeatus. Its structure was established by the extensive spectroscopic analyses, and its cytotoxicities against P388, HL-60, and PC-3 cell lines were measured in vitro.

Simultaneous determination of 4 alkaloids and a flavonoid in Picrasmae Ramulus et Folium by RP-HPLC / 中国中药杂志

A RP-HPLC method was developed to evaluate the quality of Picrasmae Ramulus et Folium by simultaneous determination of five constituents including 1-hydroxymethyl-beta-carboline (1), 1-methoxicabony-beta-carboline (2), 4-methoxy-5-hydroxy-canthin-6-one (3), 4, 5-dimethoxy-canthin-6-one (4) and maackiain (5) in Picrasmae Ramulus et Folium. The samples were separated on a Kromasil RP-C18 (4.6 mm x 250 mm, 5 microm) column eluted with acetonitrile and 0.1% phosphoric acid as mobile phases in gradient mode. The detection wavelength was set at 254 nm. The calibration curves and linearity of the above five standards were determined as (1) Y = 6 525.6X + 37.25 (0.009-1.780 microg, r = 0.996 8), (2) Y = 3 662.3X + 41.55 (0.005-0.920 microg, r = 0.999 5), (3) Y = 3763.1X + 146.87 (0.015-3.060 microg, r = 0.999 0), (4) Y = 2 174.1X + 21.52 (0.003-0.620 microg, r = 0.999 5), and (5) Y = 276.25X + 7.65 (0.010-1.960 microg, r = 0.998 9), respectively. The method is simple and repeatable, and can be used for the quality assessment of Picrasmae Ramulus et Folium.

Analysis of projects funded by NSFC in field of pharmacology of traditional Chinese medicine between 2010 to 2013 fiscal years / 中国中药杂志

Projects which supported by National Natural Science Foundation of China (NSFC) in discipline of pharmacology of Chinese medicine between 2010 to 2013 financial years were reviewed. Based on these research items, new features and problems were summarized in this field.

A new 3, 4-seco-lanostane triterpenoid from a marine-derived fungus Ascotricha sp. ZJ-M-5 / 药学学报

To study the secondary metabolites of a marine-derived fungus Ascotricha sp. ZJ-M-5, several chromatographic methods including macroporous resin, silica gel, ODS and Sephadex LH-20 were used to isolate the compounds, and their structures were elucidated on the basis of physicochemical properties and spectroscopic methods. Ten compounds were obtained and identified as ascotrichic acid B (1), (3R)-6-hydroxymellein (2), beta-carboline (3), (22E, 24R)-ergosta-7, 22-diene-3beta, 5alpha, 6beta-triol (4), (22E, 24R)-ergosta-7, 22-diene-3beta, 5alpha, 6beta, 9alpha-tetraol (5), cyclo (Leu-Pro) (6), cyclo (Ile-Leu) (7), cyclo (Pro-Val) (8), cyclo (Pro-Gly) (9), and cyclo (Hpro-Ala) (10). Among them, compound 1 is a new 3, 4-seco-lanostane triterpenoid which has been isolated from the filamentous fungi for the first time, and compounds 2-10 are firstly isolated from Ascotricha genus.

A new triterpenoid glycoside from the roots of Ilex asprella / 中国天然药物

AIM@#To study the chemical constituents of the roots of Ilex asprella Champ. ex Benth.@*METHODS@#Compounds were isolated by silica gel, ODS, and Sephadex LH-20 column chromatography, and their structures were elucidated on the basis of physicochemical properties and spectroscopic analysis.@*RESULTS@#Four triterpenoid glycosides were isolated and identified as (3β)-19-hydroxy-28-oxours-12-en-3-yl β-D-glucopyranosiduronic acid n-butyl ester (1), ilexasoside A (2), monepaloside F (3), and ilexoside A (4).@*CONCLUSION@#Compound 1 is a new triterpenoid glycoside, and compounds 3 and 4 were isolated from this plant for the first time.

A new perylenequinone from a halotolerant fungus, Alternaria sp. M6 / 中国天然药物

AIM@#To study the metabolites of a halotolerant fungus Alternaria sp. M6.@*METHODS@#The metabolites were isolated and purified by various chromatographic techniques. Their structures were determined on the basis of physical properties and spectroscopic data.@*RESULTS@#Nine compounds were isolated and identified as 8β-chloro-3, 6aα, 7β, 9β, 10-pentahydroxy-9, 8, 7, 6a-tetrahydroperylen-4(6aH)-one (1), alterperylenol (2), dihydroalterperylenol (3), adenine (4), adenosine (5), deoxyadenosine (6), guanosine (7), tryptophan (8), and hexadecanoic acid (9).@*CONCLUSION@#Compound 1 is a new perylenequinone.

Effects of Chinese herbal enema therapy combined basic treatment on BUN, SCr, UA, and IS in chronic renal failure patients / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To assess the clearance role and safety of Chinese herbal enema therapy (CHET) in clearing enterogenic uremic toxins in chronic renal failure (CRF) patients, thus providing evidence for further optimizing the comprehensive treatment.</p><p><b>METHODS</b>Using nonrandomized concurrent control trial, 96 CRF inpatients of Department of Nephropathy, Guangdong Provincial Hospital of Traditional Chinese Medicine, from March 2010 to December 2010 were assigned to the treatment group and the control group according to their willingness. All patients were treated with basic treatment referring to clinical plans in the non-dialysis phase, while those in the treatment group were additionally treated with CHET, once daily, 2 weeks as one therapeutic course. The symptoms, serum enterogenic uremic toxin levels [including indoxyl sulfate (IS), blood urea nitrogen (BUN), and uric acid (UA)], and serum creatinine (SCr) were observed in the two groups between and after treatment. The adverse reactions were also monitored during the treatment period. The clinical efficacy and safety were also assessed.</p><p><b>RESULTS</b>Totally 84 patients completed this clinical observation, 48 in the treatment group and 36 in the control group. The levels of SCr, BUN, and IS were obviously lower in the treatment group after treatment, showing statistical difference when compared with before treatment (P<0.01). There was no statistical difference in each index in the control group between before and after treatment (P>0.05). The post-treatment the IS level was lower in the treatment group than in the control group with statistical difference (P<0.05). Symptoms like fatigue, soreness of waist and knees, constipation and edema were partially relieved in both groups (P<0.05, P<0.01). The ratios of anorexia and nausea in patients of the treatment group was lowered after treatment (P<0.05). Besides, patients in the treatment group could defecate for more than once daily during the enema treatment period, dominated as rotten and soft feces. No severe adverse event occurred during the treatment period.</p><p><b>CONCLUSION</b>CHET combined basic treatment could lower the serum levels of enterogenic uremic toxins (IS and BUN) of CRF patients in a short period.</p>

Triterpenes from Callicarpa integerrima Champ / 药学学报

A new triterpenoid saponin and fourteen known triterpenoids were isolated from the methanol extract of the stems and leaves of Callicarpa integerrima Champ, which is used in Chinese folk medicine for stopping bleeding, expelling the wind, dissipating stagnation, and treating scrofula, by using various chromatographies, such as silica gel, Sephadex LH-20 and RP-C18 column chromatography. Their structures were identified as a new compound 2alpha, 3beta, 19alpha, 23-tetrahydroxy-olean-12-en-28-oic acid-28-O-beta-D-glucopyranosyl-(1 --> 4)-beta-D-glucopyranoside (1), together with fourteen known compounds: oleanolic acid (2), 3-acetyl oleanolic acid (3), 3beta-O-acetyl ursolic acid (4), 2alpha-hydroxy-ursolic acid (5), 2alpha, 3beta, 19alpha, 23-tetrahydroxy-urs-12-en-28-oic acid (6), alpha-amyrin-3-O-beta-D-glucopyranoside (7), pomolic acid (8), betulinic acid (9), ursolic acid (10), 2alpha, 3beta, 19alpha, 23-tetrahydroxy-olean-12-en-28-oic acid (arjungenin) (11), 2alpha-hydroxy-oleanolic acid (12), hederagenin (13), 2alpha, 19alpha-dihydroxy-ursolic acid (14) and pruvuloside A (15), by the spectroscopic techniques of NMR, HMBC, IR and MS, separately. All these compounds were obtained from this plant for the first time, and compounds 3, 4 and 15 were isolated from genus Callicarpa L. for the first time.

Analysis of distribution and antibiotic resistance of 233 positive results of blood cultures in neonatal intensive care unit / 中国小儿急救医学

Objective To investigate the pathogens distribution and their drug resistance of blood culture-positive neonates with sepsis in neonatal intensive care unit(NICU) and to provide evidence for clinically reasonable use of antibiotics.Methods One thousand four hundred and fifty neonates admitted to our NICU of Affiliated Hospital of Guangdong Medical College from Jan 2009 to Jul 2011 were enrolled.The blood samples from 1 450 neonates were cultured and isolated,and all of the isolates and their resistances were analyzed retrospectively.Results A total of 9 species and 233 pathogenic strains were isolated from 1 450 specimens,and the positive rate was 16.1％.Among the 233 strains,93 strains were gram-positive cocci,103 strains were gram-negative bacilli,and 37 strains were fungus.Among gram-positive cocci,the most dominant organism was coagulase negative staphylococcus,the next was Staphylococcus aureus;while among gram-negative bacilli,Ktebsiella pneumoniae were the most frequently isolated,the next were Escherichia coli and Acinetobacter baumannii,and among the fungus,monilia were the most isolated.The resistance rates of gram-positive cocci to vancomycin,linezolid and teicoplanin were high.Moreover,the antibiotic resistance rates to penicillin,oxazocilline and the β-lactamase were more than 95％.Gram-negative bacilli were sensitive to levofloxacin,imipenem and meropenem.A majority of fungus was Monilia,which was sensitive to antifungal.Conclusion Coagulase negative staphylococcus,Klebsiella pneumoniae and Escherichia coli are the the most common pathogens of neonatal sepsis in NICU,and have high drug resistance.Clinicians should select sensitive drug treatment according to bacterial identification and susceptibility testing.Besides,mycotic infection cannot be ignored and merit our attention.

Simultaneous determination of seven flavonoids in Nervilia fordii with HPLC / 药学学报

The study is to develop an HPLC method for simultaneous determination of rhamnazin (1), rhamnocitrin (2), rhamnetin (3), rhamnazin-3-O-beta-D-glucopyranoside (4), rhamnazin-3-O-beta-D-xylopyranosyl-(1-->4)-beta-D-glucopyranoside (5), rhamnazin-3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-glucopyranoside (6), and rhamnocitrin-3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-glucopyranoside (7) in Nervilia fordii. The separation was performed on a Kromasil C18 column (250 mm x 4.6 mm, 5 microm) with 0.4% phosphoric acid-acetonitrile as the mobile phase in a gradient elution at a flow rate of 1.0 mL x min(-1). The detect wavelength was set at 256 nm, and the column temperature was set at 40 degrees C. There were good linear relationships between the logarithm values of concentrations and those of the peak areas of seven flavonoids (1-7) in the range of 0.55-70.00 microg x mL(-1) (r = 0.9997), 0.86-110.00 microg x mL(-1) (r = 0.9997), 0.39-50.00 microg x mL(-1) (r = 0.999 7), 0.55-70.00 microg x mL(-1) (r = 0.999 5), 1.33-170.00 microg x mL(-1) (r = 0.9998), 1.33-170.00 microg x mL(-1) (r = 0.9998), 0.16-20.00 microg x mL(-1) (r = 0.9995), respectively. The recoveries of the seven flavonoids were between 97.19%-99.45%, the relative standard deviations (RSDs) were between 0.91%-2.69%. The established method is rapid, accurate with high repeatability, which could provide scientific evidence for the quality control of Nervilia fordii.

Application of nuclear magnetic resonance to the determination of the configuration of glycoside bond / 药学学报

In the structural determination of natural glycosides, nuclear magnetic resonance (NMR) is an important approach in determining the configuration of glycoside bond. The test of coupling constant of the anomeric proton and chemical shift of the anomeric carbon are two common methods, but these methods are not suitable for some sugars. For those sugars, detailed 13C NMR analysis is an alternative choice. This paper summarizes the characteristics of 1H and 13C NMR data of the common monosaccharides published in the literatures, in order to search an approach to determine the configuration of glycoside bond.