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| 1 | Microcalorimetric investigation of the effect of berberine alkaloids from Coptis chinensis Franch on Staphylococcus aureus growth显示文摘The inhibitory effects of three berberine alkaloids (BAs) from rhizome of Coptis chinensis Franch, a traditional Chinese medicinal (TCM) herb, on Staphylococcus aureus growth were investigated by mi- crocalorimetry. The power–time curves of S. aureus with and without BAs were acquired; meanwhile the extent and duration of inhibitory effects on the metabolism were evaluated by studying the growth rate constant (k), half inhibitory ratio (IC50), maximum heat-output power (Pmax), peak time of maximum heat-output power (tp) and total heat production (Qt). The value of k of S. aureus in the presence of the three BAs decreased with the increasing concentrations of BAs. Moreover, Pmax was reduced and the value of tp increased with increasing concentrations of the three drugs. The inhibitory activity varied with different drugs. The values of IC50 of the three BAs are respectively, 101.4 μg/mL for berberine, 241.0 μg/mL for palmatine and 792.3 μg/mL for jateorrhizine. The sequence of antimicrobial activity of the three BAs is: berberine > palmatine > jateorrhizine. It is suggested that the functional group me- thylenedioxy or methoxyl at C2 on the phenyl ring could possibly improve antimicrobial activity more strongly than hydroxyl at C2 on the phenyl ring. | YAN Dan XIAO XiaoHe JIN Cheng DONG XiaoPing | 2008 | Science China Chemistry2008,51,7: | 27 |
| 2 | Hepatoprotective and antioxidant activity of a mangrove plant Lumnitzera racemosa显示文摘Objective:To identify the hepatoprotective and in vitro antioxidant activity of Lumnitzera racemosa(L.racemosa)leaf extract.Methods:Animals in Group 1 served as vehicle control,Group 2 served as liepatoloxin(CCL_4 treated)group,Group 3 served as positive control(Silyinarin)group,and Group 4,5 and 6 served as(75,150 and 300 mg/kg bw p.o.)L.raremosa leaf extract treated groups.Moreover,in vitro antioxidant DPPH,hydroxyl radical scavenging activity(HRSA),NO,ferric reducing antioxidant power(FRAP),lipid hydroperoxide(LPO)and super oxide dismutase(SOD)were also analyzed for the leaf extract.Results:The levels of the serum parameters such as serum glutamic oxaloacetic transaminase(SCOT),serum glutamic pyruvic transaminase(SGPT),alkaline phosphatase(ALP),bilirubin,cholesterol(CHL),sugar and lactate dehydrogenase(LDU)were significantly increased in CCL_4 treated rats when compared with the control group(P<0.05).But the L.racemosa leaf extract treated rats showed maximum reduction of SGOT[(210.36±19.63)IU/L],SGPT[(82.37±13.87)IU/L],ALP[(197.63±23.43)IU/L],bilurubin[(2.15±0.84)mg/dL],cholesterol[(163.83±15.63)mg/dL],sugar[(93.00±7.65)mg/dL]and LDH[(1134.00±285.00)IU/L]were observed with the high dose(300 mg/kg bw)of leaf extract treated rats.Histopathological scores showed that,no visible changes were observed with high dose(300 mg/kg bw)of leaf extract treated rats except few mild necrosis.The IC_(50)values were observed as(56.37±4.87)μg/mL,(57.68±1.98)μg/mL,(64.I5±2.90)μg/mL,(61.94±3.98)μg/mL,(94.53±1.68)μg/mL and(69.7±2.65)μg/mL for DPPH,HRSA,NO,FRAP,LPO and SOD radical scavenging activities,respectively.Conclusions:In conclusion,the hepatoprotective effect of the L.racemosa leaf extract might be due to the presence of phenolic groups,terpenoids and alkaloids and in vitro antioxidant properties. | Sundaram Ravikumar Murugesan Gnanadesigan | 2011 | Asian Pacific Journal of Tropical Biomedicine2011,1,5: | 21 |
| 3 | A review on medicinal importance,pharmacological activity and bioanalytical aspects of beta-carboline alkaloid 'Harmine'显示文摘Harmine,a beta-carboline alkaloid,is widely distributed in the plants,marine creatures,insects, mammalians as well as in human tissues and body fluids.Harmine was originally isolated from seeds of Peganum harmal in 1847 having a core indole structure and a pyridine ring.Harmine has various types of pharmacological activities such as antimicrobial,antifungal,antitumor,cytotoxic, antiplasmodial,antioxidaant,antimutagenic,antigenotoxic and hallucinogenic properties.It acts on gamma-aminobutyric acid type A and monoamine oxidase A or B receptor,enhances insulin sensitivity and also produces vasorelaxant effect.Harmine prevents bone loss by suppressing osteoclastogenesis.The current review gives an overview on pharmacological activity and analytical techniques of harmine,which may be useful for researcheres to explore the hidden potential of harmine and and will also help in developing new drugs for the treatment of various diseases. | K Patel M Gadewar R Tripathi SK Prasad Dinesh Kumar Patel | 2012 | Asian Pacific Journal of Tropical Biomedicine2012,2,8: | 17 |
| 4 | Alkaloid profiling of the traditional Chinese medicine Rhizoma corydalis using high performance liquid chromatography-tandem quadrupole time-of-flight mass spectrometry显示文摘Since alkaloids are the major active constituents of Rhizoma corydalis(RC),a convenient and accurate analytical method is needed for their identification and characterization.Here we report a method to profile the alkaloids in RC based on liquid chromatography-tandem quadrupole time-of-flight mass spectrometry(LC–Q-TOF-MS/MS).A total of 16 alkaloids belonging to four different classes were identified by comparison with authentic standards.The fragmentation pathway of each class of alkaloid was clarified and their differences were elucidated.Furthermore,based on an analysis of fragmentation pathways and alkaloid profiling,a rapid and accurate method for the identification of unknown alkaloids in RC is proposed.The method could also be useful for the quality control of RC. | Mingqian Sun Jianxun Liu Chengren Lin Lan Miao Li Lin | 2014 | Acta Pharmaceutica Sinica B2014,4,3: | 14 |
| 5 | Three pairs of alkaloid enantiomers from the root of Isatis indigotica显示文摘Three pairs of enantiomerically pure alkaloids with diverse structure features, named isatindigoticoic acid A and epiisatindigoticoic acid A [(—)-1 and(+)-1], phaitanthrin A and epiphaitanthrin A [(—)-2 and(+)-2], and isatindopyrromizol A and epiisatindopyrromizol A [(—)-3and(+)-3], respectively, were isolated from an aqueous extract of the roots of Isatis indigotica. Racemic and scalemic mixtures of these enantiomers were separated by HPLC on a chiral semi-preparative column.Their structures including absolute configurations were determined by extensive spectroscopic analysis in conjunction with the calculation of electronic circular dichroism(ECD) spectra. The enantiomer pairs possess parent structures of 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid, indolo[2,1-b]quinazolinone, and 3-thioxohexahydro-1H-pyrrolo[1,2-c]imidazol-1-one, respectively. Except for phaitanthrin A[(—)-2] which the configuration was previously undetermined, these compounds are new enantiomeric natural products. | Yufeng Liu Xiaoliang Wang Minghua Chen Sheng Lin Li Li Jiangong Shi | 2016 | Acta Pharmaceutica Sinica B2016,6,2: | 12 |
| 6 | Gynura Rhizoma containing pyrrolizidine alkaloids induces the hepatic sinusoidal obstruction syndrome in mice via upregulating fibrosis-related factors显示文摘Recently, hepatic sinusoidal obstruction syndrome (HSOS) caused by herbal preparations containing pyrrolizidine alkaloids (PAs), such as Gynura Rhizoma (Tusanqi), has gained global attention. However, the lack of a reliable and reproducible animal model has greatly hampered mechanistic studies. Therefore, we aimed to establish a reproducible HSOS mouse model and investigate the hepatotoxic mechanism. The model was established by intragastrical administration of Gynura Rhizoma extract, i.e., 1.0 g extract/kg per day (equal to 16.7 g crude drug/kg per day based on extraction rate and 49.1 mg PA/kg per day based on the total PA content in the extract determined) for 40 successive days. Then, the mice were sacrificed, and their blood samples and livers were collected for analyses. Using hematoxylin-eosin (HE) and Masson staining, scanning electron microscopy imaging, clinical biomarkers, and other assays, we showed that the HSOS was successfully induced in our mouse model. Furthermore, we detected the key factors involved in liver fibrosis in the mice, revealing significantly increased hydroxyproline concentration;elevated expression of a-smooth muscle actin (a-SMA) and fibrosis-related genes such as Collagen-1, Collagen-3, Mmp2, M m pl3, Timph Timp3, and Activin, upregulated Smad3 phosphorylation, and increased serum TGF-β levels. Moreover, pro-inflammatory cytokines, including Tnf-a, ll-ip , and 11-6, were also increased in the model. All these results demonstrate the key roles of the TGF-p-Smad3 and inflammatory signaling pathways in this Gynura Rhizoma-induced HSOS mouse model, suggesting that blockade of fibrosis and/or inflammation should be an effective treatment for HSOS. | Fang Zhang Yue Zhou Xiao Yang Ai-zhen Xiong Zheng-tao Wang Li Yang | 2019 | Acta Pharmacologica Sinica2019,40,6: | 11 |
| 7 | A novel alkaloid from the fruiting bodies of Ganoderma sinense Zhao,Xu et Zhang显示文摘A new alkaloid,sinensine(1),had been isolated from the fruiting bodies of Ganoderma sinense Zhao,Xu et Zhang.Its structure was elucidated on the basis of 1D and 2D spectral analysis.This alkaloid exhibited activity in protecting the injury induced by hydrogen peroxide oxidation on HUVEC,with EC_(50) value 6.2μmol/L. | Liu, Chao Zhao, Fen Chen, RuoYun | 2010 | Chinese Chemical Letters2010,21,2: | 11 |
| 8 | Analysis of the bioactive components from different growth stages of Fritillaria taipaiensis P. Y. Li显示文摘High-performance liquid chromatography(HPLC)coupled with an evaporative light scattering detector(ELSD)or a diode array detector(DAD)were utilized for the quantitative analysis of 4 alkaloids(peimisine,sipeimine,peimine and peiminine)and 9 nucleosides and nucleobases(uracil,uridine,adenosine,adenine,inosine,thymine,cytidine,guanosine and thymidine)from Fritillaria taipaiensis P.Y.Li that had been cultivated in the same field for 2–6 years.The content of peimisine,sipeimine,peimine,peiminine,uracil,thymine,adenine and inosine in plants cultivated for 2–4 years was significantly higher than that of plants cultivated for 5–6 years,while the content of cytidine,uridine,guanosine,thymidine and adenosine did not change over this period.This is the first evaluation of variation in the bioactive compounds in F.taipaiensis over its life cycle. | Rui Peng Peng Ma Rangyu Mo Nianxi Sun | 2013 | Acta Pharmaceutica Sinica B2013,3,3: | 11 |
| 9 | New steroidal alkaloid and furostanol glycosides isolated from Solanum lyratum with cytotoxicity显示文摘Two previously undescribed steroidal compounds, 16, 23-epoxy-22, 26-epimino-cholest-22(N), 23, 25(26)-trien-3β-ol-3-O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranosyl-(1→4)-β-D-galactopyranoside(1) and 26-O-β-D-glucopyranosyl-(25 R)-5α-furost-20(22)-en-3β, 26-diol(2), together with 7 known ones including 26-O-β-D-glucopyranosyl-(25 R)-5, 20(22)-dien-furost-3β, 26-diol(3),(25 R)-5-en-spirost-3β-ol-O-β-D-glucopyranosyl-(1→4)-[α-L-rhmanopyranosyl-(1→2)]-β-D-galactopyranoside(4), funkioside D(5), aspidistrin(6), tigogenin-3-O-β-D-lucotrioside(7), desglucolanatigonin II(8), and degalactotigonin(9), were isolated from Solanum lyratum Thunb. Their cytotoxic activities were tested in two cancer cell lines by MTT method. One of the steroidal glycosides(6) showed significant cytotoxic activity against gastric cancer SGC7901 and liver cancer BEL-7402 cells. | XU Yun-Ling LV Jia WANG Wei-Fang LIU Yue XU Ya-Juan XU Tun-Hai | 2018 | Chinese Journal of Natural Medicines2018,16,7: | 8 |
| 10 | Investigation of benzylisoquinoline alkaloid biosynthetic pathway and its transcriptional regulation in lotus显示文摘Lotus predominantly accumulates benzylisoquinoline alkaloids(BIAs),but their biosynthesis and regulation remain unclear.Here,we investigated structural and regulatory genes involved in BIA accumulation in lotus.Two clustered CYP80 genes were identified to be responsible for the biosynthesis of bis-BIAs and aporphine-type BIAs,respectively,and their tissue-specific expression causes divergence in alkaloid component between leaf and embryo.In contrast with the common(S)-reticuline precursor for most BIAs,aporphine alkaloids in lotus leaf may result from the(S)-N-methylcoclaurine precursor.Structural diversity of BIA alkaloids in the leaf is attributed to enzymatic modifications,including intramolecular C–C phenol coupling on ring A and methylation and demethylation at certain positions.Additionally,most BIA biosynthetic pathway genes show higher levels of expression in the leaf of high-BIA cultivar compared with low-BIA cultivar,suggesting transcriptional regulation of BIA accumulation in lotus.Five transcription factors,including three MYBs,one ethylene-responsive factor,and one basic helix–loop–helix(bHLH),were identified to be candidate regulators of BIA biosynthesis in lotus.Our study reveals a BIA biosynthetic pathway and its transcriptional regulation in lotus,which will enable a deeper understanding of BIA biosynthesis in plants. | Xianbao Deng Li Zhao Ting Fang Yaqian Xiong Collins Ogutu Dong Yang Sornkanok Vimolmangkang Yanling Liu Yuepeng Han | 2018 | Horticulture Research2018,5,1: | 8 |
| 11 | The transcription factor OpWRKY2 positively regulates the biosynthesis of the anticancer drug camptothecin in Ophiorrhiza pumila显示文摘The limited bioavailability of plant-derived natural products with anticancer activity poses major challenges to the pharmaceutical industry.An example of this is camptothecin,a monoterpene indole alkaloid with potent anticancer activity that is extracted at very low concentrations from woody plants.Recently,camptothecin biosynthesis has been shown to become biotechnologically amenable in hairy-root systems of the natural producer Ophiorrhiza pumila.Here,time-course expression and metabolite analyses were performed to identify novel transcriptional regulators of camptothecin biosynthesis in O.pumila.It is shown here that camptothecin production increased over cultivation time and that the expression pattern of the WRKY transcription factor encoding gene OpWRKY2 is closely correlated with camptothecin accumulation.Overexpression of OpWRKY2 led to a more than three-fold increase in camptothecin levels.Accordingly,silencing of OpWRKY2 correlated with decreased camptothecin levels in the plant.Further detailed molecular characterization by electrophoretic mobility shift,yeast one-hybrid and dual-luciferase assays showed that OpWRKY2 directly binds and activates the central camptothecin pathway gene OpTDC.Taken together,the results of this study demonstrate that OpWRKY2 acts as a direct positive regulator of camptothecin biosynthesis.As such,a feasible strategy for the over-accumulation of camptothecin in a biotechnologically amenable system is presented. | Xiaolong Hao Chenhong Xie Qingyan Ruan Xichen Zhang Chao Wu Bing Han Jun Qian Wei Zhou Hans-Wilhelm Nutzmann Guoyin Kai | 2021 | Horticulture Research2021,8,1: | 7 |
| 12 | 土三七致肝窦阻塞综合征显示文摘土三七作为民间常用的促进微循环、缓解疼痛、治疗外伤的中药材,在我国应用较多。目前研究发现,土三七中含有的吡咯生物碱(pyrrolizidine alkaloid,PA)成分会导致肝窦阻塞综合征(hepatic sinusoidal obstruction syndrome,HSOS),严重时可导致肝衰竭。这一点长期以来被人们忽视,因而常出现误食、服食过量导致肝中毒的情况。目前为止,国内外对HSOS的治疗方法仍然有限,病情严重的患者预后较差。本文就土三七致HSOS的临床诊断、病理特征、影像学表现和治疗做一总结和分析。 | 叶天和 梁惠民 叶进 郑传胜 熊斌 潘峰 夏向文 袁锋 陶然 | 2014 | 中华介入放射学电子杂志2014,2,4: | 6 |
| 13 | The chromosome-level Hemerocallis citrina Borani genome provides new insights into the rutin biosynthesis and the lack of colchicine显示文摘Hemerocallis citrina Borani(huang hua cai in Chinese)is an important horticultural crop whose flower buds are widely consumed as a delicious vegetable in Asia.Here we assembled a high-quality reference genome of H.citrina using single-molecule sequencing and Hi-C technologies.The genome assembly was 3.77 Gb and consisted of 3183 contigs with a contig N50 of 2.09 Mb,which were further clustered into 11 pseudochromosomes.A larger portion(3.25 Gb or 86.20%)was annotated as a repetitive content and 54,295 protein-coding genes were annotated in the genome.Genome evolution analysis showed that H.citrina experienced a recent whole-genome duplication(WGD)event at~15.73 million years ago(Mya),which was the main factor leading to many multiple copies of orthologous genes.We used this reference genome to predict 20 genes involved in the rutin biosynthesis pathway.Moreover,our metabolomics data revealed neither colchicine nor its precursors in H.citrina,challenging the long-standing belief that this alkaloid causes poisoning by the plant.The results of our disruptive research are further substantiated by our genomic finding that H.citrina does not contain any genes involved in colchicine biosynthesis.The high-quality genome lays a solid foundation for genetic research and molecular breeding of H.citrina. | Zhixing Qing Jinghong Liu Xinxin Yi Xiubin Liu Guoan Hu Jia Lao Wei He Zihui Yang Xiaoyan Zou Mengshan Sun Peng Huang Jianguo Zeng | 2021 | Horticulture Research2021,8,1: | 6 |
| 14 | Enhancing terpenoid indole alkaloid production by inducible expression of mammalian Bax in Catharanthus roseus cells显示文摘Bax,a mammalian pro-apoptotic member of the Bcl-2 family,triggers hypersensitive reactions when expressed in plants.To investigate the effects of Bax on the biosynthesis of clinically important natural products in plant cells,we generate transgenic Catharanthus roseus cells overexpressing a mouse Bax protein under the β-estradiol-inducible promoter.The expression of Bax in transgenic Catharanthus roseus cells is highly dependent on β-estradiol concentrations applied.Contents of catharanthine and total terpenoid indole alkaloid of the transgenic cells treated with 30 μmol/L β-estradiol are 5.0-and 5.5-fold of the control cells.Northern and Western blotting results show that expression of mammalian Bax induces transcriptional activation of Tdc and Str,two key genes in terpenoid indole alkaloid bio-synthetic pathway of Catharanthus roseus cells,and stimulates the accumulation of defense-related protein PR1 in the cells,showing that the mouse Bax triggers the defense responses of Catharanthus roseus cells and activates the terpenoid indole alkaloid biosynthetic pathway.Thus,our data suggest that the mammalian Bax might be a potential regulatory factor for secondary metabolite biosynthesis in plant cells and imply a new secondary metabolic engineering strategy for enhancing the metabolic flux to natural products by activating the whole biosynthetic pathway rather than by engineering the single structural genes within the pathways. | XU MaoJun & DONG JuFang Department of Biotechnology,Zhejiang Gongshang University,Hangzhou 310035,China | 2007 | Science China(Life Sciences)2007,50,2: | 5 |
| 15 | Two new C_(19)-diterpenoid alkaloids from roots Aconitum hemsleyanium var. atropurpureum显示文摘A new franchetine-type C19-diterpenoid alkaloid 3-hydroxyfranchetine 1 and a new aconitine-type C19-diterpenoid alkaloid atropurpursine 2 have been isolated from the roots of Aconitum hemsleyanium var. atropurpureum. The structures of these new alkaloids were established on the basis of spectral data. | Pei Tang, Dong Lin Chen, Xi Xian Jian, Feng Peng Wang Department of Chemistry of Medicinal Natural Products, West China College of Pharmacy, Sichuan University, Chengdu 610041, China | 2007 | Chinese Chemical Letters2007,18,6: | 4 |
| 16 | ISORHYNCHOPHYLLIC ACID,A NEW AIKALOID FROM UNCARIA SINENSIS显示文摘From the hook of Uncaria sinensis, a new alkaloid, isorhynchophyllicacid was isolated and its structure was elucidated by spectral data and chemicalreaction. | Hong Mei LIU Xiao Zhang FENG Yang LU Qi Tai ZHENG Institetu of Materia Medica, Chinese Academy of Medical Sciences, 1 Xian Nong Tan Street, Beijing 100050 | 1992 | Chinese Chemical Letters1992,3,6: | 4 |
| 17 | Genome and transcriptome of Papaver somniferum Chinese landrace CHM indicates that massive genome expansion contributes to high benzylisoquinoline alkaloid biosynthesis显示文摘Opium poppy(Papaver somniferum)is a source of morphine,codeine,and semisynthetic derivatives,including oxycodone and naltrexone.Here,we report the de novo assembly and genomic analysis of P.somniferum traditional landrace‘Chinese Herbal Medicine’.Variations between the 2.62 Gb CHM genome and that of the previously sequenced high noscapine 1(HN1)variety were also explored.Among 79,668 protein-coding genes,we functionally annotated 88.9%,compared to 68.8%reported in the HN1 genome.Gene family and 4DTv comparative analyses with three other Papaveraceae species revealed that opium poppy underwent two whole-genome duplication(WGD)events.The first of these,in ancestral Ranunculales,expanded gene families related to characteristic secondary metabolite production and disease resistance.The more recent species-specific WGD mediated by transposable elements resulted in massive genome expansion.Genes carrying structural variations and large-effect variants associated with agronomically different phenotypes between CHM and HN1 that were identified through our transcriptomic comparison of multiple organs and developmental stages can enable the development of new varieties.These genomic and transcriptomic analyses will provide a valuable resource that informs future basic and agricultural studies of the opium poppy. | Li Pei Baishi Wang Jian Ye Xiaodi Hu Lihong Fu Kui Li Zhiyu Ni Zhenlong Wang Yujie Wei Luye Shi Ying Zhang Xue Bai Mengwan Jiang Shuhui Wang Chunling Ma Shujin Li Kaihui Liu Wanshui Li Bin Cong | 2021 | Horticulture Research2021,8,1: | 4 |
| 18 | Liensinine attenuates inflammation and oxidative stress in spleen tissue in an LPS-induced mouse sepsis model显示文摘Sepsis is a complex syndrome caused by multiple pathogens and involves multiple organ failure,particularly spleen dysfunction.In 2017,the worldwide incidence was 48.9 million sepsis cases and 1l million sepsis-related deaths were reported(Rudd et al.,2020).Inflammation,oxidative stress,and apoptosis are the most common pathologies seen in sepsis.Liensinine(LIE)is a bisbenzylisoquinoline-type alkaloid extracted from the seed embryo of Nelumbo nucifera.Lotus seed hearts have high content of LIE which mainly has antihypertensive and antiarrhythmic pharmacological effects.It can exert anti-carcinogenicactivityby regulating cell. | HANYU WANG YUANHAO YANG XIAO ZHANG YAN WANG HUI FAN JINFENG SHI XUELIAN TAN BAOSHI XU JINGCHAO QIANG ENZHUANG PAN MINGYI CHU ZIBO DONG JINGQUAN DONG | 2023 | Journal of Zhejiang University-Science B(Biomedicine & Biotechnology)2023,24,2: | 4 |
| 19 | Different structures of berberine and five other protoberberine alkaloids that affect P-glycoprotein-mediated efflux capacity显示文摘Berberine,berberrubine,thalifendine,demethyleneberberine,jatrorrhizine,and columbamine are six natural protoberberine alkaloid (PA)compounds that display extensive pharmacological'properties and share the same protoberberine molecular skeleton with only slight substitution differences.The oral delivery of most PAs is hindered by their poor bioavailability,which is largely caused by P-glycoprotein (P-gp)-mediated drug efflux.Meanwhile,P-gp undergoes large-scale conformational changes (from an inward-facing to an outward-facing state)when transporting substrates,and these changes might strongly affect the P-gp-binding specificity.To confirm whether these six compounds are substrates of P-gp,to investigate the differences in efflux capacity caused by their trivial structural differences arid to reveal the key to increasing their binding affinity to P-gp,we conducted a series of in vivo,in vitro,and in silico assays.Here,we first confirmed that all six compounds were substrates of P-gp by comparing the drug concentrations in wild-type and P-gp-knockout mice in vivo.The efflux capacity (net efflux)ranked as berberrubine >berberine > columbamine ~jatrorrhizine >thalifendine >demethyleneberberine based on in vitro transport studies in Caco-2 monolayers. Using molecular dynamics simulation and molecular docking techniques,we determined the transport pathways of the six compounds and their binding affinities to P-gp.The results suggested that at the early binding stage,different hydrophobic and electrostatic interactions collectively differentiate the binding affinities of the compounds to P-gp,whereas electrostatic interactions are the main determinant at the late release stage.In addition to hydrophobic interactions,hydrogen bonds play an important role in discriminating the binding affinities. | Yi-ting Zhang Yu-qi Yu Xiao-xia Yan Wen-jie Wang Xiao-ting Tian Le Wang Wei-liang Zhu Li-kun Gong Guo-yu Pan | 2019 | Acta Pharmacologica Sinica2019,40,1: | 3 |
| 20 | Dynamic observation of bone marrow suppression and chromosomal aberrations in patients with acute colchicine poisoning显示文摘Colchicine is a neutral lipophilic tricyclic alkaloid toxic to human cells containing tubulin,[1-2]and primarily stops the proliferation of active cells in the mitotic metaphase,such as intestinal mucosal cells and hematopoietic cells.It is widely used in treating gout and familial Mediterranean fever,while it is also used in establishing animal and plant experimental model.[3]In the recent study,treatment of patients affected by coronavirus disease 2019(COVID-19)with colchicine may prove a viable path.[4]The course of colchicine poisoning can be divided into three stages,[5]and most of the patients died in the second stage(2-7 d,the multiple organ injury stage).The cause of death was heart failure[6]and bone marrow hematopoietic failure in the terminal phase.[7]Hematopoiesis is a classic sign of colchicine poisoning.Many cases of colchicine poisoning have been comprehensively reported,and the target organs included heart,digestive tract,muscle,lung,kidney,hematopoietic system,etc.[8-11]This study aimed to investigate the injury of bone marrow hematopoietic system after colchicine poisoning and evaluate the therapeutic effect of bone marrow hematopoietic stimulation drugs. | Yan-qing Liu Xiao-xia Lu Kai-xun Hu Xiao-bo Peng Yun Jiang Li-mei Han Zhi-qiang Ma Ming-fei Peng Kun Wan Xi-gang Zhang Ze-wu Qiu | 2022 | World Journal of Emergency Medicine2022,13,2: | 3 |