Allotetraploidization event of Coptis chinensis shared by all Ranunculales

Coptis chinensis Franch.,also named Chinese goldthread is a member of Ranunculaceae in the order Ranunculales and represents an important lineage of early eudicots with traditional medicinal value.In our study,by using syntenic analysis combined with phylogenomic analysis of C.chinensis and four other representative genomes from basal and core eudicots,we confirmed that the WGD event in C.chinensis was shared by Aquilegia coerulea and Papaver somniferum L.and quickly occurred after Ranunculales diverged from other eudicots,likely a Ranunculales common tetraploidization(RCT).The synonymous nucleotide substitutions at synonymous sites distribution of syntenic blocks across these genomes showed that the evolutionary rate of the P.somniferum genome is faster than that of the C.chinensis genome by approximately 13.7%,possibly due to Papaveraceaes having an additional special tetraploidization event(PST).After Ks correction,the RCT dated to 115—130 million years ago(MYA),which was close to the divergence of Ranunculaceaes and Papaveraceaes approximately115.45—130.51 MYA.Moreover,we identified homologous genes related to polyploidization and speciation and constructed multiple sequence alignments with different reference genomes.Notably,the event-related subgenomes in the basal genomes all showed genomic fractionation bias,suggesting a likely allopolyploid nature of the RCT,PST and T-Alpha and T-Beta events in Tetracentron sinense.In addition,we detected that the sixteen P450 subfamilies were markedly expanded in the genomes of Ranunculales,and most of them were related to the RCT and PST events.We constructed a new platform for Early Eudicot Comparative Genomic Research(http://www.cgrpoee.top/index.html)to store more information.In summary,our findings support the WGD of C.chinensis shared by Ranunculales,which is likely an allotetraploidization event.This present effort offered new insights into the evolution of key polyploidization events and the genes related to secondary metabolites during the diversification of early eudicots.

Effects of Different Alkaloids in Coptis chinensis on Inhibiting TGEV Proliferation

[Objectives]To study the effects of different alkaloids in Coptis chinensis on inhibiting the proliferation of Transmissible gastroenteritis virus(TGEV).[Methods]The components and content of the main alkaloids in the extract of C.chinensis were analyzed.The main alkaloids were selected as drugs to inhibit the proliferation of TGEV.The maximum non-toxic concentration of Columbamine,Jatrorrhizine,Epiberberine,Coptisine,Palmatine,and Berberine was screened.The protective rate of each drug on TGEV-infected ST cells was determined,and the transcriptional inhibitory effect of the drug on TGEV N gene was detected by fluorescent quantitative PCR.[Results]The extract of C.chinensis mainly contains 6 alkaloids:Columbamine,Jatrorrhizine,Epiberberine,Coptisine,Palmatine,and Berberine,accounting for 2.03%,8.88%,9.21%,15.07%,14.63%,and 50.18%,respectively.In the range of the safe concentration,Jatrorrhizine,Palmatine,and Coptisine had better protective effects on ST cells infected with TGEV;compared with the Columbamine group,the cell protection rate was significantly different(P<0.05);compared with the Berberine group,the difference was extremely significant(P<0.01).The Coptisine and Palmatine groups had significant inhibitory effects on the transcription of TGEV N gene,and the difference was extremely significant compared with the virus group(P<0.05).[Conclusions]Jatrorrhizine and Palmatine in C.chinensis are the main components to inhibit the proliferation of TGEV.

Correlation between Yield of Coptis chinensis Franch. and Soil Nutrients under Different Forests

[Objective] This study was conducted to investigate the correlation be- tween yield of Coptis chinensis Franch. and soil nutrients under different forests. [Method] The soil nutrients and yields of C. chinensis in fallow field, Cryptomeria japonica forest, Magnolia officinalis forest and Phellodendron chinense forest planted with C. chinensis were investigated. [Result] The contents of soil nitrogen （total ni- trogen, alkali-hydrolyzale nitrogen）, organic matter, potassium and phosphorous under the planting mode of C. chinensis under C. japonica forest were the highest; and the contents of organic matter and total nitrogen in the soils of M. officinalis and P. chinense forests were close to each other at the medium abundant level, and the phosphorous contents were more abundant than those in fallow field. [Conclusion] This study could provide a theoretical basis for scientific fertilization.

Study of Total Alkaloids from Rhizoma Coptis Chinensis on Experimental Gastric Ulcers

Objective： To study the effects of total alkaloids （TA） extracted from Rhizoma Coptis Chinensis on experimental gastric ulcer models. Methods： Four kinds of experimental ulcer models were established respectively by water-immersion stress, intragastric ethanol, acetic acid erosion, and pylorus ligation. The anti-ulcer effects of TA were evaluated, and compared with that of berberine （Bet） and cimetidine （Oim）. Results： TA showed significant inhibitory effects on ulcerative formation induced by water-immersion stress, intragastric ethanol, and pylorus l igation in dose-dependent manner, and showed therapeutic effect on acetic acid erosion-inducing ulcer, in comparison with the control group. The anti-ulcer activity of Bet was less than TA containing equal content of Bet. TA significantly reduced the free acidity, total acidity and total acid output, but didn＇t affect the gastric juice volume, gastric pepsin activity, adherent mucus quantity of stomach wall and free mucus dissolving in gastric juice. The suppressive activities of TA on gastric acid secretion didn＇t occur when it was administered into dodecadactylon at a dose of 360 mg/kg wt. Moreover, when compared with Oim, the inhibitory effect of TA on gastric acid secretion isn＇t proportional to the inhibitory effects on the formation of the 4 kinds of experimental ulcers. Conclusion： TA is a potent candidate in therapeutic drugs for treating gastric ulcer. Its anti-ulcer effective components and mechanism is not only related to Bet and inhibition of gastric acid, but also to other ingredients of TA and mechanism so far unknown.

Structural and Histochemical Features of the Slow-Growing Perennial Coptis chinensis Franch.(Ranunculaceae)

Huanglian(Coptis chinensis Franch.)is a slow-growing perennial medicinal herb with considerable economic value.This study aimed to determine the structural characteristics and the levels of berberine deposits in the organs and tissues of Huanglian using light and epifluorescence microscopy.The adventitious roots are composed of primary and secondary structures with endodermis,exodermis,and phellem.The rhizome structures are composed of primary and secondary structures with cuticle and phellem.The leaves are composed of sclerenchymatous rings,isolateral mesophyll,and thin cuticles.We detected berberine in the xylem walls of the roots and rhizomes as well as in the sclerenchymatous rings of the petioles.We postulate that as the exodermis is developed,the deposition of berberine in the xylem closest to the root tips may affect water and nutrient absorption and transfer.Leaf blades had a thin cuticle and isolateral mesophyll,suggesting shade tolerance.These structural and histochemical features suggest that Huanglian is adapted to the slow growing nature of a shady environment.

Study of dual-directional regulatory effect of Banxia （Pinellia ternata） and Huanglian （Coptis chinensis） drug pair on gastrointestinal movement of mice

Objective： To evaluate the regulatory effects of Banxia （Pinellia ternata, P） and Huanglian （Coptis chinensis, C） drugpair, derived from Banxiaxiexin soup, on the gastrointestinal movement of mice with functional dyspepsia. Methods：Mice were treated with different proportions of the P and C drug pair （1：1, 3：1, and 4：1） for 10 days, and subsequentlyinjected with atropine （ATR） or neostigmine （NEO）. The effects of the different proportions of P and C were evaluatedbased on the alvine advance rate. In addition, we used the same modeling method used in the first experiment andadministered P： C at ratio of 3：1 and at different doses respectively （4.68 g/L, 2.34 g/L, and 1.17 g/L）, and tested levelsof the gastrointestinal hormones, gastrin （GAS）, vasoactive intestinal polypeptide （VIP）, and somatostatin （SS） in thesmall intestinal tissue using an enzyme-linked immunosorbent assay. Results： In the groups of NEO-induced mice, P：Cat ratios of 1：1, 3：1, and 4：1 significantly reduced the alvine advance rate compared with the NEO model group （P =0.003, P = 0.012 and P = 0.021, respectively）. In the groups of ATR-induced mice, only P：1 at ratio of 3：1 significantlyincreased the alvine advance rate compared with the ATR model group （P = 0.007）. After exposure to P： C at ratio of 3：1and at different dose, the GAS level was lower in the low-, medium-, and high-dose NEO groups than that in the NEOmodel group （P = 0.001, P = 0.004, and P = 0.003, respectively）. The VIP levels were higher in the medium-andhigh-dose NEO groups than that in the NEO model group （P = 0.004 and P = 0.002, respectively）. In addition, the SSlevel increased in the NEO medium-dose group compared with that in the NEO model group （P = 0.002）. The GAS levelwas higher in the ATR medium- and high-dose groups than in the ATR model group （P = 0.007 and P = 0.021,respectively）. The VIP level was lower in the ATR low-, medium-, and high-dose than that in the ATR model group （P =0.001, P = 0.001, and P = 0.001, respectively）. Furthermore, the SS level was lower in the ATR medium- and high-dosegroups than that in the ATR model group （P = 0.001 and P = 0.006）. Conclusion： The PC drug pair bidirectionallyadjusted the NEO- and ATR-induced functional dyspepsia in mice by modulating GAS, VIP, and SS levels in theintestine.

Optimization ratio between Coptis chinensis and cinnamo of Jiaotai pill plus benzodiazepines for insomnia in China:a network meta-analysis

OBJECTIVE To explore the efficacy of Jiaotai pill(JTW)and JTW modified prescriptions(JTW^(+))plus benzodiazepines(BDZ)for insomnia in China by systematic review and network meta-analysis,especially optimization ratio(_(m:n))between Coptis chinensis and Cinnamo.METHODS Randomized controlled trials(RCTs)regarding JTW and JTW^(+)+BDZ for insomina were comprehensively searched in CNKI,VIP,Wanfang,and PubMed,Cochrane Library,OVID,Embase databases from their inception to December 2017.The risk of bias was assessed by the Cochrane collaboration′s tool and Jadad scale.Systematic review and network meta-analysis were performed to evaluate the relative risk(RR)plus 95%confidence interval(95%CI)or prediction interval(95%PrI),and draw surface under the cumulative ranking curves(SUCRA)by Stata 14.0 and RevMan 5.0 software.RESULTS A total of 13 RCTs(1 RCT was omitted by sensitivity analysis)with 1040 patients were included.Overall heterogeneity was acceptable,except publication bias.Based on classical meta-analysis,JTW and JTW_(m:n)^(+)+BDZ,such as JTW_(2:1)^(+)+BDZ,JTW_(5:1)^(+)+BDZ,JTW_(6:1)^(+)+BDZ,JTW_(10:1)^(+)+BDZ,had more efficacy than BDZ.Based on network meta-analysis,JTW and JTW_(m:n)^(+)+BDZ,such as JTW_(2:1)^(+)+BDZ,JTW_(6:1)^(+)+BDZ,JTW_(10:1)^(+)+BDZ,had more efficacy than BDZ;meanwhile,SUCRA showed the best rank of JTW/JTW+(BDZ<JTW_(m:n)^(+)+BDZ<JTW)for insomina,as same as that of JTW_(m:n)+(BDZ<JTW_(5:1)^(+)+BDZ<JTW_(10:1)^(+)+BDZ<JTW_(2:1)^(+)+BDZ<JTW_(6:1)^(+)+BDZ).CONCLUSION Based on the existing clinical evidence,JTW has efficacy for insomnia,but the optimization ratio between Coptis chinensis and cinnamo of JTW_(m:n)^(+)+BDZ for insomnia needs more supports.

Analysis on Quality of Coptis chinensis Grown under Different Woods

[Objectives] To analyze the quality of Coptis chinensis grown under woods of Magnolia officinalis Rehd. et Wils.,Platycladus orientalis( Linn.) Franco.,and Cunninghamia lanceolata( Lamb.). [Methods] The content of five kinds of alkaloids in C. chinensis grown under three different woods was determined by high-performance liquid chromatography( HPLC). Detection conditions: 0. 03 mol/L methanol and potassium dihydrogen phosphate solution( volume ratio of 65∶ 35) as the mobile phase,flow rate of 1. 0 mL/min,detection wavelength of 350 nm,and column temperature of 35℃. [Results] In these three woods,the quality of C. chinensis grown under P. orientalis woods was the highest. [Conclusions] This study is expected to provide certain references for cultivation and planting of C. chinensis under woods.

Network pharmacology and molecular dynamics study of the effect of the Astragalus-Coptis drug pair on diabetic kidney disease

BACKGROUND Diabetic kidney disease(DKD)is the primary cause of end-stage renal disease.The Astragalus-Coptis drug pair is frequently employed in the management of DKD.However,the precise molecular mechanism underlying its therapeutic effect remains elusive.AIM To investigate the synergistic effects of multiple active ingredients in the Astragalus-Coptis drug pair on DKD through multiple targets and pathways.METHODS The ingredients of the Astragalus-Coptis drug pair were collected and screened using the TCMSP database and the SwissADME platform.The targets were predicted using the SwissTargetPrediction database,while the DKD differential gene expression analysis was obtained from the Gene Expression Omnibus database.DKD targets were acquired from the GeneCards,Online Mendelian Inheritance in Man database,and DisGeNET databases,with common targets identified through the Venny platform.The protein-protein interaction network and the“disease-active ingredient-target”network of the common targets were constructed utilizing the STRING database and Cytoscape software,followed by the analysis of the interaction relationships and further screening of key targets and core active ingredients.Gene Ontology(GO)function and Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway enrichments were performed using the DAVID database.The tissue and organ distributions of key targets were evaluated.PyMOL and AutoDock software validate the molecular docking between the core ingredients and key targets.Finally,molecular dynamics(MD)simulations were conducted to simulate the optimal complex formed by interactions between core ingredients and key target proteins.RESULTS A total of 27 active ingredients and 512 potential targets of the Astragalus-Coptis drug pair were identified.There were 273 common targets between DKD and the Astragalus-Coptis drug pair.Through protein-protein interaction network topology analysis,we identified 9 core active ingredients and 10 key targets.GO and KEGG pathway enrichment analyses revealed that Astragalus-Coptis drug pair treatment for DKD involves various biological processes,including protein phosphorylation,negative regulation of apoptosis,inflammatory response,and endoplasmic reticulum unfolded protein response.These pathways are mainly associated with the advanced glycation end products(AGE)-receptor for AGE products signaling pathway in diabetic complications,as well as the Lipid and atherosclerosis.Molecular docking and MD simulations demonstrated high affinity and stability between the core active ingredients and key targets.Notably,the quercetin-AKT serine/threonine kinase 1(AKT1)and quercetin-tumor necrosis factor(TNF)protein complexes exhibited exceptional stability.CONCLUSION This study demonstrated that DKD treatment with the Astragalus-Coptis drug pair involves multiple ingredients,targets,and signaling pathways.We propose a novel approach for investigating the molecular mechanism underlying the therapeutic effects of the Astragalus-Coptis drug pair on DKD.Furthermore,we suggest that quercetin is the most potent active ingredient and specifically targets AKT1 and TNF,providing a theoretical foundation for further exploration of pharmacologically active ingredients and elucidating their molecular mechanisms in DKD treatment.

Establishment and reliability evaluation of the design space for HPLC analysis of six alkaloids in Coptis chinensis(Huanglian) using Bayesian approach

Coptis chinensis(Huanglian) is a commonly used traditional Chinese medicine(TCM) herb and alkaloids are the most important chemical constituents in it. In the present study, an isocratic reverse phase high performance liquid chromatography(RP-HPLC) method allowing the separation of six alkaloids in Huanglian was for the first time developed under the quality by design(Qb D) principles. First, five chromatographic parameters were identified to construct a Plackett-Burman experimental design. The critical resolution, analysis time, and peak width were responses modeled by multivariate linear regression. The results showed that the percentage of acetonitrile, concentration of sodium dodecyl sulfate, and concentration of potassium phosphate monobasic were statistically significant parameters(P < 0.05). Then, the Box-Behnken experimental design was applied to further evaluate the interactions between the three parameters on selected responses. Full quadratic models were built and used to establish the analytical design space. Moreover, the reliability of design space was estimated by the Bayesian posterior predictive distribution. The optimal separation was predicted at 40% acetonitrile, 1.7 g·m L-1of sodium dodecyl sulfate and 0.03 mol·m L-1 of potassium phosphate monobasic. Finally, the accuracy profile methodology was used to validate the established HPLC method. The results demonstrated that the Qb D concept could be efficiently used to develop a robust RP-HPLC analytical method for Huanglian.

Homology Modeling and Molecular Docking Studies of （S）-Scoulerine 9-O-Methyltransferase from Coptis chinensis

（S）-Scoulerine 9-O-methyltransferase （SMT）, belonging to the S-adenosyl-L-methionine （SAM）-dependent O-methyltransferase family, is an essential enzyme in the berberine biosynthetic pathways. In order to study the in- teractions of SMT with its substrate and further to understand the catalytic mechanism and substrate specificity, a three dimensional model of SMT from Coptis chinensis was constructed by homology modeling using the crystal structure of caffeic acid/5-hydroxyferulic acid 3/5-O-methyltransferase （COMT） as a template. The three dimen- sional structure of SMT, which was mainly composed of a-helices and some fl-sheets, was similar to that of COMT. In contrast with COMT, the non-conserved residues in the substrate binding pocket of SMT might be responsible for their differences in the substrate specificity. Val119 and Asp254 in SMT were the key residues for orienting substrate for methylation as both residues had H-bonds with （S）-scoulerine. The methylation of （S）-scoulerine in- volved deprotonation of the 9-hydroxyl group by His253 and Asp254 in SMT followed by a nucleophilic attack on the SAM-methyl resulting in the product, （S）-tetrahydrocolumbamine.

Effects of Coptis chinensis on Lipid Peroxidation and Antioxidases Activity of Rats

Coptis chinensis and the brain homogenate of rat were mixed and incubated to investi-gate the effects of Coptis on lipid peroxidation. The results showed that the malondialdehyde product ofrat brain homogenate inhibited by 5% Coptis was significantly different from that of the control group (P<0. 001). On the basis of the above-mentioned results, the effect of Coptis on lipid peroxidation and dia-betes in rats induced by alloxan was investigated. The results showed : (1) The malondialdehyde productof both the pancreas and liver homogenate in the Coptis (test) group was significantly less than that inblank control and the alloxan (control) group (P<0. 01 , P<0. 05). (2) Superoxide dismutases in erythro-cytes activity was the same for all groups (P>0. 50). (3) The blood catalase activity in the control groupmarkedly decreased compared with the blank control group (P<0. 05) , but no significant change betweenthe test and control group (P>0. 05) occurred. (4)The value of serum glucose in the control group wassignificantly increased compared with the blank control group (P<0. 05). A decrease in the value ofserum glucose in the test group compared with the control group occurred, but with no significant differ-ence between the two groups (P<O. 05).

湖北省黄连炭疽病的病原鉴定及其生物学特性

为了鉴定湖北省黄连(Coptis chinensis Franch.)炭疽病致病菌,了解其生物学特性,研制有效的防治药剂,于湖北省恩施市板桥镇采集病斑叶片,利用组织分离法得到真菌12株。其中EsH2和EsH6接种离体叶片能够产生典型病斑。经形态学和ITS序列系统发育分析鉴定,明确致病菌株均属博宁炭疽菌Colletotrichum boninense复合群。对菌株EsH2和EsH6的生物学特性分析,统计不同培养基或光照条件下生长速率,并且测定了常用的5种杀菌剂对菌丝生长的抑制率。结果表明,EsH2、EsH6分别在绿豆培养基和PDA培养基上生长较快,供试菌株缺乏光照情况下生长显著减慢,5种供试药剂中苯醚甲环唑、甲基硫菌灵和吡唑醚菌酯的抑制中浓度较小,抑菌相关性较好。

Antioxidant activity and hepatoprotective effect of 10 medicinal herbs on CCl4-induced liver injury in mice

BACKGROUND Many natural products confer health benefits against diverse diseases through their antioxidant activities.Carbon tetrachloride(CCl4)is often used in animal experiments to study the effects of substances on liver injury and the related mechanisms of action,among which oxidative stress is a major pathogenic factor.AIM To compare antioxidant and hepatoprotective activities of ten herbs and identify and quantify phytochemicals for the one with strongest hepatoprotection.METHODS The antioxidant activity of ten medicinal herbs was determined by both ferricreducing antioxidant power and Trolox equivalent antioxidant capacity assays.The total phenolic and flavonoid contents were determined by Folin–Ciocalteu method and aluminum chloride colorimetry,respectively.Their effects on CCl4-induced oxidative liver injury were evaluated and compared in a mouse model by administrating each water extract(0.15 g/mL,10 mL/kg)once per day for seven consecutive days and a dose of CCl4 solution in olive oil(8%,v/v,10 mL/kg).The herb with the strongest hepatoprotective performance was analyzed for the detailed bioactive components by using high-performance liquid chromatography-electrospray ionization source-ion trap tandem mass spectrometry.RESULTS The results revealed that all tested herbs attenuated CCl4-induced oxidative liver injury;each resulted in significant decreases in levels of serum alanine transaminase,aspartate transaminase,alkaline phosphatase,and triacylglycerols.In addition,most herbs restored hepatic superoxide dismutase and catalase activities,glutathione levels,and reduced malondialdehyde levels.Sanguisorba officinalis(S.officinalis)L.,Coptis chinensis Franch.,and Pueraria lobata(Willd.)Ohwi root were the three most effective herbs,and S.officinalis L.exhibited the strongest hepatoprotective effect.Nine active components were identified in S.officinalis L.Gallic acid and(+)-catechin were quantified(7.86±0.45 mg/g and 8.19±0.57 mg/g dried weight,respectively).Furthermore,the tested herbs displayed a range of in vitro antioxidant activities proportional to their phenolic content;the strongest activities were also found for S.officinalis L.CONCLUSION This study is of value to assist the selection of more effective natural products for direct consumption and the development of nutraceuticals or therapeutics to manage oxidative stress-related diseases.

Three new pyrrole alkaloids from the endophytic fungus Albifimbria viridis

Three new pyrrole alkaloids albifipyrrols A-C(1-3),were isolated from the endophytic fungus Albifimbria viridis col-lected from the Chinese medicinal plant.Their structures were elucidated by extensive NMR and HRESIMS spectro-metric analyses.All compounds were evaluated for immunosuppressive activity.Fortunately,compound 2 exhibits certain inhibition specifically against the LPS-induced proliferation of B lymphocyte cells with IC50 value 16.16μM.

恩施州建南镇黄连病害情况调查及成因分析

针对恩施州利川市建南镇黄连(Coptis chinensis Franch.)病害发生情况进行调查,详细介绍了建南镇黄连病害的发生情况,分析了可能造成黄连病害严重的原因。同时对黄连病害防治的有效措施进行了总结,旨在为黄连产品质量提供保障,为黄连产业的可持续发展保驾护航。

Effect of Hoechunyangkyeok-San Extract on Melanogenesis

Forsythia fructus has been shown to have antioxidative, anti-inflammatory, antibacterial, anti-aging and whitening effects. Hoechunyangkyeok-san (Forsythia viridissima-prescription) is a traditional herbal medicine, which has been clinically used for treating febrile and inflammatory disorders. This work was carried out to investigate the skin whitening effects of Forsythia viridissima-prescription extract (a hydrolyzed extract of Hoechunyangkyeok-san: SID White HYC) on skin. The effects of SID White HYC were assessed the melanin contents in B161 melanoma cells and the pigmented equivalent with HMB45 and Fontana Masson staining in 3D skin model. Then, we examined the expression of major pigment enzymes regulating melanin synthesis and melanosome transport related proteins in B16F1 cells. SID White HYC significantly inhibited the melanin synthesis (56.7% and 30.6% inhibition at 100 μg/mL, intracellular and secreted, respectively) in B16F1 cells and 3D skin model. In addition, western blotting analysis showed that SID White HYC reduced the expression of melanin synthesis and melanosome transport related proteins in B16F1 cells. In clinical trials, the cream containing 0.05% SID White HYC showed skin depigmentation effect without any irritation. These results suggest that SID White HYC may be useful inhibition of melanogenesis and melanosome transport. Therefore, SID White HYC may have potential as a skin-whitening ingredient in cosmetics.

Citrinsorbicillin A,a novel homotrimeric sorbicillinoid isolated by LC-MS-guided with cytotoxic activity from the fungus Trichoderma citrinoviride HT-9

Citrinsorbicillin A(1),a novel homotrimeric sorbicillinoid,along with two new monomers citrinsor-bicillins B(2)and C(3),were isolated from the Coptis chinensis endophyte Trichoderma citrinoviride HT-9 by liquid chromatograph mass spectrometer(LC-MS)-guided strategy.1 was the first trimeric-example from terrestrial fungi,which possessed a unique carbon skeleton with two bicyclo[2.2.2]octanedione ring connected through an enolated carbon forming by[4+2]cycloaddition.Their structures were elucidated by spectroscopic analysis and X-ray diffraction.1 exhibited moderate cytotoxicity against human colon cancer HT29 cells,and it induced significant cell cycle arrest by reducing the protein expression of cyclin D1.

Biological properties and clinical applications of berberine

Berberine,an isoquinoline alkaloid isolated from the Chinese herb Coptis chinens is and other Berber is plants,has a wide range of pharmacological properties.Berberine can be used to treat many diseases,such as cancer and digestive,metabolic,cardiovascular,and neurological diseases.Berberine has protective capacities in digestive diseases.It can inhibit toxins and bacteria,including Helicobac terpylo riprotect the intestinal epithelial barrier from injury,and ameliorate liver injury.Berberine also inhibits the proliferation of various types of cancer cells and impedes invasion and metastasis.Recent evidence has confirmed that berberine improves the efficacy and safety of chemoradiotherapies.In addition,berberine regulates glycometabolism and lipid metabolism,improves energy expenditure,reduces body weight,and alleviates nonalcoholic fatty liver disease.Berberine also improves cardiovascular hemodynamics,suppresses ischemic arrhythmias,attenuates the development of atherosclerosis,and reduces hypertension.Berberine shows potent neuroprotective effects,including antioxidative,antiapoptotic,and anti-ischemic.Furthermore,berberine exerts protective effects against other diseases.The mechanisms of its functions have been extensively explored,but much remains to be clarified.This article summarizes the main pharmacological actions of berberine and its mechanisms in cancer and digestive,metabolic,cardiovascular,and neurological diseases.

Advance of Studies on Anti-atherosclerosis Mechanism of Berberine

Coptis Chinensis is a traditional Chinese medicine herb that has the effect of clearing heat and drying dampness,purging fire to eliminate toxin.Berberine is the main alkaloid of Coptis Chinensis,and recent researches showed that berberine had the effect of anti-atherosclerosis.This paper reviewed the anti-atherosclerosis mechanism of berberine,which may be related to regulating lipids,anti-inflammation, decompression,reducing blood sugar,and inhibiting vascular smooth muscle cell proliferation.