Tong xie yao fang relieves irritable bowel syndrome in rats via mechanisms involving regulation of 5-hydroxytryptamine and substance P

AIM: To investigate whether the Chinese medicine Tong Xie Yao Fang(TXYF) improves dysfunction in an irritable bowel syndrome(IBS) rat model. METHODS: Thirty baby rats for IBS modeling were separated from mother rats(1 h per day) from days 8 to 21, and the rectum was expanded by angioplasty from days 8 to 12. Ten normal rats were used as normal controls. We examined the effects of TXYF on defection frequency, colonic transit function and smooth muscle contraction, and the expression of 5-hydroxytryptamine(5-HT) and substance P(SP) in colonic and hypothalamus tissues by Western blot and RT-PCT techniques in both normal rats and IBS model rats with characterized visceral hypersensitivity.in normal rats and 4.5 ± 1.58 in IBS model rats(P < 0.001). However, the defecation frequency was significantly decreased(3.0 ± 1.25 vs 4.5 ± 1.58, P < 0.05), while the time(in seconds) of colon transit function was significantly increased(256.88 ± 20.32 vs 93.36 ± 17.28, P < 0.001) in IBS + TXYF group rats than in IBS group rats. Increased colonic smooth muscle tension and contract frequency in IBS model rats were significantly decreased by administration of TXYF. Exogenous agonist stimulants increased spontaneous activity and elicited contractions of colon smooth muscle in IBS model rats, and all of these actions were significantly reduced by TXYF involving 5-HT and SP down-regulation. CONCLUSION: TXYF can modulate the activity of the enteric nervous system and alter 5-HT and SP activities, which may contribute to the symptoms of IBS.

Clinical application and mechanism of traditional Chinese medicine in treatment of lung cancer

Lung cancer is a malignant tumor characterized by a rapid proliferation rate,less survivability,high mortality,and metastatic potential.This review focuses on updated research about the clinical application of traditional Chinese medicine(TCM)as an adjuvant therapy to lung cancer treatment and the mechanisms of TCM effect on lung cancer in vitro and in vivo.We summarized the recent 5 years of different research progress on clinical applications and antitumor mechanisms of TCM in the treatment of lung cancer.As a potent adjuvant therapy,TCM could enhance conventional treatments(chemotherapy,radiation therapy,and epidermal growth factor receptors[EGFRs]tyrosine kinase inhibitors[TKIs])effects as well as provide synergistic effects,enhance chemotherapy drugs chemosensitivity,reverse drug resistance,reduce adverse reactions and toxicity,relieve patients’pain and improve quality of life(QOL).After treating with TCM,lung cancer cells will induce apoptosis and/or autophagy,suppress metastasis,impact immune reaction,and therapeutic effect of EGFR-TKIs.Therefore,TCM is a promisingly potent adjuvant therapy in the treatment of lung cancer and its multiple mechanisms are worthy of an in-depth study.

Investigation of Radix Achyranthis Bidentatae Phytochemistry and Pharmacology

Radix achyranthis bidentatae(RAB), a member of the Amaranthaceae family, has been widely used in Traditional Chinese Medicine for1000 s of years. Increasing interest in RAB-derived medicinal has led to the discovery of additional triterpenoid saponins, phytoecdysones,polysaccharides, and many other compounds, as well as investigations into their pharmacology. A large number of pharmacological studies have shown RAB and its active components possess a range of pharmacological activities, including anti-tumor, anti-fertility, anti-senile, and anti?inflammatory effects. This review is an up?to?date summary and synthesis of the uses of RAB from phytochemical and pharmacological perspectives.

Probiotics with anti-type 2 diabetes mellitus properties:targets of polysaccharides from traditional Chinese medicine

Traditional Chinese medicine polysaccharides is a biologically active ingredient that is not easy to be digested.It is fermented by intestinal microflora to promote qualitative and selective changes in the composition of the intestinal microbiome,which often result in beneficial effects on the health of the host.People call it“prebiotics”.In this review,we systematically summarized the anti-diabetic effect of traditional Chinese medicine polysaccharides.These polysaccharides regulate the metabolism of sugar and lipids by inter-influence with the intestinal microflora,and maintain human health,while improving type 2 diabetes-like symptoms such as high blood glucose,and abnormal glucose and lipid metabolism.

Anti-proliferative Properties of Schinensilactone A,A Schinortriterpenoid with 7,8-Seco-1,8-cyclo Scaffold against Caco-2 by Inducing Cell Apoptosis from the Leaves of Schisandra chinensis

A novel schinortriterpenoid(SNT),schinensilactone A(1),characterized by a unique 7,8-seco-1,8-cyclo-schisanartane scaffold,was isolated from the leaves of Schisandra chinensis(Turcz.)Baill,together with a new SNT(schinensilactone B,2)and two known(3,4).Their structures were elucidated using spectroscopy and X-ray diffraction.Furthermore,a hypothetical biosynthetic pathway for 1 was postulated due to its novel carbon skeleton.In addition,1 exhibited significant anti-proliferative activity against Caco-2 cells originat-ing from five different tumor cell lines,and its preliminary mechanism of action was investigated with respect to the expression of apoptosis-related proteins,including P53,Caspase 3,Bax,PUMA,and Bcl2.These biological activities would further our understanding of the food function of Schisandra chinensis leaves.

Pharmacokinetic and Relative Bioavailability of Three Secoiridoid Glycosides in Beagle Dog Plasma After Oral Administration of Conventional and Enteric-Coated Capsules of Gentianella acuta Extract

Objective:To simultaneously investigate the pharmacokinetics of gentiopicroside,sweroside,and swertiamarin,which are constituents of Gentianella acuta,by developing and validating a simple,sensitive,and fast ultra-high-performance liquid chromatography–tandem mass spectrometry method.Materials and Methods:Blood samples were collected from the forward limb veins of six beagle dogs following oral gavage with G.acuta,the whole plant extract(39.90 mg/kg).Plasma samples were processed using liquid–liquid extraction.The analytes and paeoniflorin(internal standard[IS])were separated using an Acquity?UPLC ethylene bridged hybrid amide column(2.1 mm×100 mm,1.7μm)with isocratic elution using a mobile phase consisting of acetonitrile and 0.1%formic acid in water(80:20,v/v)at a flow rate of 0.4 mL/min.Quantification was performed using multiple reaction monitoring of the fragmentation transitions at m/z 401.1→179.0,403.1→195.0,419.1→179.0,and 525.2→449.1 for gentiopicroside,sweroside,swertiamarin,and the IS,respectively.Results:The linearity of the analytical response was good and the calibration curves were linear over concentration ranges of 1.20–192.0,0.40–159.0,and 0.20–209.3 ng/mL for gentiopicroside,sweroside,and swertiamarin,respectively.The extraction recovery was in the range of 84.72%–91.34%,84.58%–93.43%,and 82.75%–91.37%for gentiopicroside,sweroside,and swertiamarin,respectively.Conclusions:The method was successfully used to evaluate the pharmacokinetic parameters of gentiopicroside,sweroside,and swertiamarin in beagle dogs.

Simultaneous Determination and Pharmacokinetics of Tetrandrine,Fangchinoline,and Cyclanoline in Rat Plasma by Ultra-High Performance Liquid Chromatography-Mass Spectrometry after Oral Administration of Stephaniae Tetrandrae Radix Extract

Objective:The objective of the study was to develop a rapid and sensitive ultra-performance liquid chromatography-tandem mass spectrometric method for the determination of tetrandrine,fangchinoline,and cyclanoline in rat plasma and to investigate their pharmacokinetics after oral administration of Stephaniae Tetrandrae Radix extracts.Methods:Sample pretreatment involved methanol pretreatment and liquid–liquid extraction of ethyl acetate from plasma with methanol.Tramadol was used as the internal standard.The analysis was performed using an high strength silica T3 column(100 mm×2.1 mm,1.8μm)and a gradient elution method consisting of mobile phase solution A(0.1%formic acid in water)and B(acetonitrile)at a flow rate of 0.4 mL/min.The detection was performed using a triple quadrupole tandem mass spectrometer in the multiple reaction monitoring mode and using an electrospray ionization source in the positive ionization mode.Results:High efficiency was achieved with an analysis time of 4 min/sample.The calibration curve linear in the concentration range of 1250 ng/ml(R^(2)≥0.9900)and the lower limit of quantification is 1 ng/ml.The intraday and interday precision(relative standard deviation)values were lower than 9.4.Accuracy(relative error)was within 10.3%at all three quality control levels.Conclusions:This method was successfully applied in pharmacokinetics of tetrandrine,fangchinoline,and cyclanoline in rats after oral administration of Stephaniae Tetrandrae Radix extracts.The maximum plasma concentration(C_(max))of tetrandrine,fangchinoline,and cyclanoline was 124.71±16.08,84.56±3.28,and 57.61±6.26 ng/mL,respectively.The time to reach C_(max)was 10.39±3.04 for tetrandrine,10.17±3.04 for fangchinoline,and 6.40±3.16 for cyclanoline.The pharmacokinetic results might help further guide the clinical application of Stephaniae Tetrandrae Radix.

The Fruits of Xanthium sibiricum Patr: A Review on Phytochemistry, Pharmacological Activities, and Toxicity

In recent years,drug development and research have gradually shifted from chemical synthesis to biopharmaceutical and natural drugs.Natural medicines,such as traditional Chinese medicine,have been among the first studied because of their long medicinal history,simplicity,and the relatively low cost of research.Among them,Xanthii Fructus(XF)is famous for the treatment of sinusitis.In this article,the achievements of research on XF from 1953 to 2020 are systematically reviewed,focusing on the aspects of chemical constituents,pharmacological effects,clinical applications,toxicity and side effects,and processing methods.To date,there have been significant advances in both the phytochemistry and pharmacology of XF.Some traditional uses have been validated and clarified in modern pharmacological studies.However,its mechanism of action in the treatment of allergic diseases has not been satisfactorily explained.Further in vitro and in vivo studies are required to rationally develop new drugs and to elucidate the therapeutic potential of XF.A comprehensive evaluation of XF and an understanding of network pharmacology are also needed.

Simultaneous Determination of Six Compounds in Rat Plasma by Ultra-Performance Liquid Chromatography with Tandem Mass Spectrometry: Application in the Pharmacokinetic Study of Qing Gan-Shu Yu-Fang

A rapid and high selective ultra-performance liquid chromatography(UPLC)with tandem mass spectrometry method for simultaneous determination of six compounds including albiflorin,paeoniflorin,picroside I,picroside II,saikosaponin A,and saikosaponin D in rat plasma was developed and validated using butyl p-hydroxybenzoate as an internal standard.One-step direct protein precipitation with acetonitrile was used to extract the compounds from the rat plasma samples.Chromatographic separation was achieved using an ACQUITY UPLC BEH C18 column(100 mm×2.1 mm,1.7μm)at a flow rate of 0.4 m L/min,using gradient mode containing 0.1%formic acid in water and acetonitrile were used as the Mobile phase A and B.Electrospray ionization in negative ion mode and multiple reaction monitoring were used to identify and quantify active components.Calibration curves showed good linearity(R^2>0.9908)over a wide concentration range for all compounds.The intra-and interday precision(relative standard deviation)ranged 2.4%–7.0%and 2.6%–8.0%,respectively.The accuracy(relative error)was from-13.0%to 13.2%at all quality control levels.The recovery ranged from 81.1%to 92.5%.The validated method was successfully applied to pharmacokinetic study in rats after oral administration of Qing Gan-Shu Yu-Fang.The results show that one can draw a conclusion that these six active ingredients can be quickly absorbed and play a pharmacodynamic role rapidly in vivo.

Exploring the Molecular Mechanism of Radix Astragali on Colon Cancer Based on Integrated Pharmacology and Molecular Docking Technique

Objective:The objective of this study was to study the mechanism of Radix Astragali on colon cancer by integrated pharmacology and molecular docking technique.Methods:Integrative pharmacology-based research platform of traditional Chinese medicine(TCMIP)V2.0 was used to obtain the chemical components and corresponding targets of Radix Astragali and the target information of colon cancer to create the main target network of drugs and diseases.Gene Ontology(GO),Kyoto Encyclopedia of Genes and Genomes(KEGG)enrichment analysis was carried out using Hiplot website,and the interaction network of“Traditional Chinese Medicine-component-target-pathway”was established,and molecular docking with main targets was carried out for the key components.Results:Twenty-seven chemical constituents of Radix Astragali,their 254 corresponding targets,and 44 colon cancer-related targets were obtained.Through proteins interacting,70 nodes were obtained as core targets.GO analysis showed that it mainly acts on lipid metabolism,nuclear receptor activity,phagocytic cup,etc.KEGG pathway analysis showed that it was mainly enriched in the estrogen signaling pathway,C-type lectin receptor signaling pathway,PI3K-Akt signaling pathway,etc.The multidimensional network,quantitative estimate of the drug,and molecular docking showed that the main targets are AKT1,BCL2,and CDK6,and the key components involved are kumatakenin,astragaloside VIII,and choline.Conclusion:Kumatakenin,AstragalosideⅧ,Choline and other compounds of Radix Astragali may affect colon cancer by acting on AKT1,BCL2 and other targets,thereby regulating estrogen signaling pathway,C-type lectin receptor signaling pathway,PI3K-Akt signaling pathway and so on.Those will provide theoretical reference for future research on the material basis and mechanism of its pharmacodynamics.

CHEMISTRY AND BIOACTIVITY OF POLYSACCHARIDES FROM TRADITIONAL CHINESE MEDICINE MAHUANG

The long-term clinical practice of traditional Chinese medicine(TCM)confirms its importance and essential role in the health care system in China,especially in the prevention and treatment of chronic diseases.TCM is the holistic medicine under the guidance of system theory,emphasizing harmony between human and nature,focusing on equilibrium and balance,and focusing on

MONOSACCHARIDE COMPOSITION OF POLYSACCHARIDES THROUGH HILIC-UPLC-TQ-MS/MS

A simple,sensitive and direct method was developed for compositional analysis of plant polysaccharides using hydrophilic interaction ultra-performance liquid chromatography coupled with triple-quadrupole tandem mass spectrometry(HILIC-UPLC-TQ-MS/MS)in multiple-reaction monitoring(MRM).The effects of chromatographic columns,scan time,additive types,

NEW ANTIPROLIFERATIVE WITHANOLIDES FROM THE SEEDS OF DATURA METEL

Three new with anolides,daturaselines A-C(1-3),and three new with anolides glycosides,daturasesides A-C(4-6),were isolated and identified from ethyl acetate-soluble fraction of ethanol extract of Datura metel seeds.The structures of new compounds were established according to the 1D and 2D NMR spectra,combined with high resolution