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Simultaneous Determination of Baicalin, Berberine and Rhein by HPLC in Traditional Chinese Patent Medicine Sanhuang Tablets 被引量:5
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作者 李奕 高建平 许旭 《Journal of Chinese Pharmaceutical Sciences》 CAS 2005年第2期110-114,共5页
Aim To establish a reversed phase liquid chromatographic method forsimultaneous determination of three main medicinal constituents, baicalin, berberine and rhein, inSanhuang tablets. Methods The separation was perform... Aim To establish a reversed phase liquid chromatographic method forsimultaneous determination of three main medicinal constituents, baicalin, berberine and rhein, inSanhuang tablets. Methods The separation was performed on a Kromasil C_(18) column with TEA-adjusted0.02 mol·L^(-1) H_3PO_4 (pH 6.78)-acetonitrile-methanol (40 : 9 : 7) as mobile phase at aflow-rate of 1.0 mL·min^(-1), with detection at 254 ran. Considering interaction between acidic andalkaline compounds, three standard markers were added respectively and the volume of samplesolution was doubled in recovery experiments. Results Three regression equations revealed excellentlinear relationship between the peak areas and concentrations and the correlation coefficients allsurpassed 0.999 8. The average recovery was 96.1% (RSD = 2.1%) baicalin, 98.5% (RSD = 2.4%) forberberine, and 101.5% (RSD =1.3%) for rhein. Conclusion The method developed can be used to controlthe quality of Sanhuang tablets comprehensively. 展开更多
关键词 sanhuang tablets BAICALIN rhein BERBERINE HPLC
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坏死亲和性MRI对比剂Gd-DO3A-rhein的合成及其靶向性 被引量:1
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作者 卞丽 高萌 +3 位作者 黄德健 彭飞 张健 殷志琦 《中国药科大学学报》 CAS CSCD 北大核心 2017年第3期282-288,共7页
以大黄酸为底物合成磁共振成像(MRI)对比剂并评价其坏死靶向性。经两步酰化和两步脱保护方法得到新的配体10-{[6-(1,8-二羟基蒽醌-3-甲酰氨基)己基]氨基}乙酰基-1,4,7,10-四氮杂环十二烷-1,4,7-三乙酸(DO3A-rhein),再与Gd3+配位得到顺... 以大黄酸为底物合成磁共振成像(MRI)对比剂并评价其坏死靶向性。经两步酰化和两步脱保护方法得到新的配体10-{[6-(1,8-二羟基蒽醌-3-甲酰氨基)己基]氨基}乙酰基-1,4,7,10-四氮杂环十二烷-1,4,7-三乙酸(DO3A-rhein),再与Gd3+配位得到顺磁性对比剂10-{[6-(1,8-二羟基蒽醌-3-甲酰氨基)己基]氨基}乙酰基-1,4,7,10-四氮杂环十二烷-1,4,7-三乙酸钆(Gd-DO3A-rhein)。采用大鼠再灌注肝坏死和肌肉坏死模型评价Gd-DO3A-rhein的坏死靶向性,分别在给予GdDO3A-rhein(0.1 mmol/kg)前和给药后0~12 h进行MRI成像,Gd-DOTA作为对照,成像结束后处死大鼠,对坏死组织进行HE和TTC染色验证坏死模型。MRI成像结果表明,在注射Gd-DO3A-rhein(0.1 mmol/kg)后3、12 h,坏死肝信号呈显著增强,坏死肝与正常肝对比度分别为1.61±0.14、2.36±0.20与给药前(1.16±0.10)呈显著性差异(P<0.05),坏死肌肉呈现同样的结果。以上结果说明,该对比剂具有良好的坏死靶向性,具有成像坏死组织的潜力。 展开更多
关键词 大黄酸 Gd-DO3A-rhein 坏死靶向性 肝坏死 磁共振成像
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Effects of rhein on intestinal epithelial tight junction in IgA nephropathy 被引量:13
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作者 Sheng-Nan Peng Hui-Hong Zeng +2 位作者 Ai-Xiang Fu Xiao-Wen Chen Qing-Xian Zhu 《World Journal of Gastroenterology》 SCIE CAS 2013年第26期4137-4145,共9页
AIM: To investigate the effects of rhein on intestinal epithelial tight junction proteins in rats with IgA nephropathy (IgAN). METHODS: Twenty-eight female Sprague-Dawley rats were randomly divided into four groups (7... AIM: To investigate the effects of rhein on intestinal epithelial tight junction proteins in rats with IgA nephropathy (IgAN). METHODS: Twenty-eight female Sprague-Dawley rats were randomly divided into four groups (7 per group): Control, IgAN, Rhein-treated, and Rheinprevented. Bovine serum albumin, lipopolysaccharide and CCl4 were used to establish the rat model of IgA nephropathy. The Rhein-treated group was given rhein from week 7 until the rats were sacrificed. The Rheinprevented group was given rhein from week 1. Animals were sacrificed at the end of week 10. We observed the changes in the intestinal epithelial tight junctions using transmission electron microscopy, and expression of intestinal epithelial tight junction proteins zona occludens protein (ZO)-1 and occludin by immunofluorescence using laser confocal microscopy. Changes in mRNA and protein expression of ZO-1 and occludin were measured by reverse transcriptase polymerase chain reaction and Western blotting. The ratio of urinary lactulose/mannitol was measured by high performance liquid chromatography (HPLC) for assessing the intestinal permeability. RESULTS: In the control group, the tight junctions lied between epithelial cells on the top of the outer side of the cell membrane, and appeared in dense dotted crystal structures, the neighboring cells were binded tightly with no significant gap, and the tight junction protein ZO-1 and occludin were evenly distributed in the intestinal epithelial cells at the top of the junction. Compared with the control group, in the IgAN group, the structure of the tight junction became obscured and the dotted crystal structures had disappeared; the fluorescence of ZO-1 and occludin was uneven and weaker (5.37 ± 1.27 vs 10.03 ± 1.96, P < 0.01; 4.23 ± 0.85 vs 12.35 ± 4.17, P < 0.01); the mRNA expression of ZO-1 and occludin decreased (0.42 ± 0.19 vs 0.92 ± 0.24, P < 0.01; 0.40 ± 0.15 vs 0.97 ± 0.25, P < 0.01); protein expression of ZO-1 and occludin was decreased (0.85 ± 0.12 vs 1.98 ± 0.43, P < 0.01; 0.72 ± 0.15 vs 1.38 ± 0.31, P < 0.01); and the ratio of urinary lactulose/mannitol increased (3.55 ± 0.68 vs 2.72 ± 0.21, P < 0.01). In the Rheinprevented and Rhein-treated groups, compared with the IgAN group, the intestinal epithelial tight junctions were repaired; fluorescence of ZO-1 and occludin was stronger (11.16 ± 3.52 and 8.81 ± 2.30 vs 5.37 ± 1.27, P < 0.01; 10.97 ± 3.40 and 9.46 ± 2.40 vs 4.23 ± 0.85, P < 0.01); mRNA of ZO-1 and occludin increased (0.81 ± 0.17 and 0.64 ± 0.16 vs 0.42 ± 0.19, P < 0.01; 0.82± 0.22 and 0.76 ± 0.31 vs 0.40 ± 0.15, P < 0.01); protein expression of ZO-1 and occludin was increased (2.07 ± 0.41 and 1.57 ± 0.23 vs 0.85 ± 0.12, P < 0.01; 1.34 ± 0.21 and 1.15 ± 0.17 vs 0.72 ± 0.15, P < 0.01); and the ratio of urinary lactulose/mannitol decreased (2.83 ± 0.43 and 2.87 ± 0.18 vs 3.55 ± 0.68, P < 0.01). CONCLUSION: Rhein can enhance the expression of ZO-1 and occludin, repair damaged tight junctions, and protect the intestinal barrier. 展开更多
关键词 INTESTINE TIGHT JUNCTION rhein IGA NEPHROPATHY Rat
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MRI对比剂Gd-DO3A-Ether-Rhein的合成及其坏死亲和性研究
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作者 张立邦 张东建 +5 位作者 高萌 金乔梅 吴天泽 杨阳 张健 殷志琦 《中国药科大学学报》 CAS CSCD 北大核心 2019年第4期444-451,共8页
以大黄酸为底物、醚链为连接臂合成磁共振成像(MRI)对比剂并评价其坏死亲和性。合成新的配体10-{[6-(1,8-二羟基蒽醌-3-甲酰氨基)乙氧基乙基]氨基}羰酰甲基-1,4,7,10-四氮杂环十二烷-1,4,7-三乙酸(DO3A-Ether-Rhein,即E1),再与Gd 3+配... 以大黄酸为底物、醚链为连接臂合成磁共振成像(MRI)对比剂并评价其坏死亲和性。合成新的配体10-{[6-(1,8-二羟基蒽醌-3-甲酰氨基)乙氧基乙基]氨基}羰酰甲基-1,4,7,10-四氮杂环十二烷-1,4,7-三乙酸(DO3A-Ether-Rhein,即E1),再与Gd 3+配位得到顺磁性对比剂10-{[6-(1,8-二羟基蒽醌-3-甲酰氨基)乙氧基乙基]氨基}羰酰甲基-1,4,7,10-四氮杂环十二烷-1,4,7-三乙酸合钆(Gd-DO3A-Ether-Rhein,即GdE1)。分别在高热诱导的人肝癌HepG2细胞坏死模型和微波消融诱导的大鼠肌肉坏死模型上评价探针的坏死亲和性。动物试验中,分别在给予GdE1(0.1 mmol/kg)前和给药后0~9 h进行MRI成像,Gd-DOTA(1,4,7,10-四乙酸-1,4,7,10-四氮杂环十二烷合钆)作为对照。MRI成像结果表明,坏死细胞的信号强度(4 369±70)显著高于正常细胞(2 555±84)(P<0.05);在GdE1给药后3 h,坏死肌肉与正常肌肉的对比度为2.00±0.12,显著高于给药后0 h(1.27±0.03)(P<0.05)。上述结果表明,GdE1具有良好的坏死亲和性,在坏死相关疾病的诊断上显示出良好的应用潜力。 展开更多
关键词 大黄酸 Gd-DO3A-Ether-rhein 坏死亲和性 对比剂 磁共振成像
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Anti-inflammatory Effects and Mechanisms of Rhein, an Anthraquinone Compound, and Its Applications in Treating Arthritis: A Review 被引量:4
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作者 Hongjuan Wang Dezhi Yang +3 位作者 Li Li Shiying Yang Guanhua Du Yang Lu 《Natural Products and Bioprospecting》 CAS 2020年第6期445-452,共8页
Inflammation is a defensive response of living tissues to damaging agents,which exists in two forms,acute inflammation and chronic inflammation,and chronic inflammation is closely related to arthritis.Currently,the co... Inflammation is a defensive response of living tissues to damaging agents,which exists in two forms,acute inflammation and chronic inflammation,and chronic inflammation is closely related to arthritis.Currently,the commonly prescribed anti-inflammatory medications are greatly limited by high incidence of gastrointestinal erosions in the clinical applications.Rhein,a bioactive constituent of anthraquinone,exhibits excellent anti-inflammatory activities and therapeutic effects on arthritis with less gastrointestinal damages.Although there are numbers of studies on anti-inflammatory effects and mechanisms of rhein in the last few decades,to the best of our knowledge,only a few review articles pay attention to the interactive relationships of rhein on multiple inflammatory signaling pathways and cellular processes from a comprehensive perspective.Herein,we summarized anti-inflammatory effects and mechanisms of rhein and its practical applications in the treatment of arthritis,thereby providing a reference for its basic researches and clinical applications. 展开更多
关键词 rhein ANTHRAQUINONE ANTI-INFLAMMATORY ARTHRITIS
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Rhein OT Strategy附着体义齿修复双侧游离缺失的临床观察
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作者 陈健钊 邓雪莲 劳均平 《河北医学》 CAS 2008年第8期949-951,共3页
目的:观察Rhein OT Strategy冠外附着体义齿修复双侧游离缺失(肯氏Ⅰ类牙列缺损)的临床效果。方法:对1 8例肯氏Ⅰ类牙列缺损,应用Rhein OTStrategy附着体固位的义齿进行修复。结果:经6个月~3年的临床随访,Rhein OTStrategy附着体... 目的:观察Rhein OT Strategy冠外附着体义齿修复双侧游离缺失(肯氏Ⅰ类牙列缺损)的临床效果。方法:对1 8例肯氏Ⅰ类牙列缺损,应用Rhein OTStrategy附着体固位的义齿进行修复。结果:经6个月~3年的临床随访,Rhein OTStrategy附着体固位的义齿稳定性好,90%(16/18)以上患者认为附着体美观,舒适,稳固,易适应,咀嚼有力。对4 1个基牙复查结果显示,基牙没有叩痛,松动,根尖周病变及牙槽骨吸收等反应。结论:Rhein OTStrategy冠外附着体义齿是修复肯氏Ⅰ类牙列缺损的较好方法,有利于基牙组织健康。 展开更多
关键词 rhein OT STRATEGY 冠外附着体 义齿修复 牙列缺损
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德国Rhein纸厂的创新实践
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作者 林一亭 《中华纸业》 CAS 北大核心 2003年第8期26-27,共2页
过去十年,西欧在工业上的投资很活跃,大大改善了它在国际市场上的竞争力,某些纸种,包括新闻纸,价格降低了,这又促进了消费,导致可持续发展。本文叙述德国Rhein纸厂年产28万吨新闻纸的创新实践。
关键词 德国 rhein纸厂 新闻纸项目 创新 投资建设 外协
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The protective effect and mechanism of rhein on diabetic cardiomyopathy by regulating Sirt1/PGC-1α pathway
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作者 WANG Tian-tian WANG Wei +1 位作者 YANG Cui-hua LU Bin 《Journal of Hainan Medical University》 CAS 2023年第19期8-8,共1页
Objective:To explore the protective effects of rhein on cardiomyocyte injury in DCM and its possible mecha-nism.Methods:The diabetic model was induced by intraperitoneal injection with streptozotocin and high-fat diet... Objective:To explore the protective effects of rhein on cardiomyocyte injury in DCM and its possible mecha-nism.Methods:The diabetic model was induced by intraperitoneal injection with streptozotocin and high-fat diet.The mice were randomly divided into control group,DM group,and DM+RH group.After 12 weeks treatment with rhein,the change of fast blood glucose,body weight,and heart weight/body weigh(t HW/BW)were observed.HE and Masson staining were used to evalu-ate myocardial structural damage.Transmission electron microscope was used to observe the myocardial mitochondrial structure.The mRNA levels of Sirt1,PGC-1α,TFAM,ANP,BNP andβ-MHC were quantified by RT-PCR.Sirt1,PGC-1α and TFAM protein levels were estimated by Western blot and IHC.Results:Compared with control group,the blood glucose,HW/BW,ANP,BNP andβ-MHC mRNA of DM group were significantly increased(P<0.05).The structures of myocardium and mitochondria were obviously destroyed in DM group.Sirt1,PGC-1α and TFAM expression were significantly decreased(P<0.05).Compared with DM group,the blood glucose,HW/BW,ANP,BNP and β-MHC mRNA of DM+RH group were decreased(P<0.05).The myocardial and mitochondrial injury were improved.Sirt1,PGC-1α and TFAM expression were significantly increased(P<0.05).Conclusion:Rhein exhibits protective effects on diabetic cardiomyopathy which may be achieved by activating Sirt1/PGC-1α pathway. 展开更多
关键词 rhein Diabetic cardiomyopathy SIRT1 PGC‐1α
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Embryotoxicity and Teratogenicity of Rhein
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作者 Yanchun Hu Chaorong Zeng +7 位作者 Fei Liao Hui Tan Lei Wu Xi Liu Zhicai Zuo Junliang Deng Anchun Cheng Yahui Wei 《Journal of Health Science》 2014年第4期180-184,共5页
To study the effect ofrhein on embryo development of rats and fetuscs, the SD rats were divided into rhein (87.5, 175 and 350 mg/kg) group and negative control group treated with 0.5% CMC (carboxyl methyl cellulose... To study the effect ofrhein on embryo development of rats and fetuscs, the SD rats were divided into rhein (87.5, 175 and 350 mg/kg) group and negative control group treated with 0.5% CMC (carboxyl methyl cellulose). The rats were administrated with rhein daily for 10 days from 6th to 15th day after pregnancy. The pregnancy rats were dissected at 20th day after pregnancy. The total weight of the fetuses, the number of corpus luteum, plant gland, absorbed fetus, live fetus, dead futus, monsters, body weight, body height and tail length were recorded. Compared with the control group, rhein group occurred with the administration of toxicity-related clinical symptoms. The changes in weight increase related with the amount ofrhein (P 〈 0.05) and the increased number of absorbed fetuses in each rhein group (P 〈 0.05) were presented. Obvious differences occurred in the rhein groups in terms of the incidence of visceral abnormalities, each organ abnormalities and fossa malformations, etc. (P 〈 0.05). Compared with the control group, there was no significant difference in the low-dose group by fetal rat bone examination (P 〉 0.05), while the remaining dose groups manifested various bone deformities such as sternum sections missing, incomplete ossification of the skull and thoracic vertebrae separation or deformation, which was obviously different from the control group (P 〈 0.01). Rhein had a significant effect on the reproductive function of pregnant rats. It can even result in the bones' and internal organs' dysplasia of fetal rats. Rhein has a significant teratogenic effect in rats. 展开更多
关键词 rhein EMBRYOTOXICITY teratogenicity.
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Rhein Chemie回归朗盛总公司
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《环球聚氨酯》 2015年第8期87-87,共1页
朗盛(LANXESS)旗下的子公司(Rhein Chemie)已回归到朗盛总公司,不再是独立的法定单位实体,并将改名为Rhein Chemie Additives。合并是朗盛集团先前宣布重组计划的一部分,该计划与2014年启动,目前已有几个业务部门完成了合并。Rhein Chem... 朗盛(LANXESS)旗下的子公司(Rhein Chemie)已回归到朗盛总公司,不再是独立的法定单位实体,并将改名为Rhein Chemie Additives。合并是朗盛集团先前宣布重组计划的一部分,该计划与2014年启动,目前已有几个业务部门完成了合并。Rhein Chemie additives由之前的朗盛功能化学业务部门和Rhein Chemie部门及朗盛橡胶化学业务部门的特种化学生产线联合组成。 展开更多
关键词 橡胶化学 法定单位 rhein CHEMIE ADDITIVES
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Potential Medicinal Value of Rhein for Diabetic Kidney Disease 被引量:3
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作者 MAO Xi XU Ding-qiao +3 位作者 YUE Shi-jun FU Rui-jia ZHANG Sai TANG Yu-ping 《Chinese Journal of Integrative Medicine》 SCIE CAS CSCD 2023年第10期951-960,共10页
Diabetic kidney disease(DKD)is the primary cause of mortality among diabetic patients.With the increasing prevalence of diabetes,it has become a major concern around the world.The therapeutic effect of clinical use of... Diabetic kidney disease(DKD)is the primary cause of mortality among diabetic patients.With the increasing prevalence of diabetes,it has become a major concern around the world.The therapeutic effect of clinical use of drugs is far from expected,and therapy choices to slow the progression of DKD remain restricted.Therefore,research on new drugs and treatments for DKD has been a hot topic in the medical field.It has been found that rhein has the potential to target the pathogenesis of DKD and has a wide range of pharmacological effects on DKD,such as anti-nephritis,decreasing blood glucose,controlling blood lipids and renal protection.In recent years,the medical value of rhein in the treatment of diabetes,DKD and renal disease has gradually attracted worldwide attention,especially its potential in the treatment of DKD.Currently,DKD can only be treated with medications from a single symptom and are accompanied by adverse effects,while rhein improves DKD with a multi-pathway and multi-target approach.Therefore,this paper reviews the therapeutic effects of rhein on DKD,and proposes solutions to the limitations of rhein itself,in order to provide valuable references for the clinical application of rhein in DKD and the development of new drugs. 展开更多
关键词 rhein diabetic kidney disease rhein derivatives TOXICITY BIOAVAILABILITY
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Rhein: a novel potential antitumor drug 被引量:4
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作者 俞璐 姚国栋 马卫成 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2016年第5期321-328,共8页
Rhein (4,5-dihydroxyanthraquinone-2-carboxylic acid) is an anthraquinone compound enriched in the rhizome of rhubarb (Rheum palmatum or Rheum tanguticum Maxim), a traditional Chinese medicine herb. Natural product... Rhein (4,5-dihydroxyanthraquinone-2-carboxylic acid) is an anthraquinone compound enriched in the rhizome of rhubarb (Rheum palmatum or Rheum tanguticum Maxim), a traditional Chinese medicine herb. Natural product compounds are a source of novel therapeutic agents. Rhein has been initially identified as an anti-inflammatory and anti-oxidant agent. Recent studies indicate that rhein may also have an antitumor effect. However, the molecular mechanisms are still unclear. This review aims to summarize the research of rhein to better understand the anti-tumor activities by targeting cell cycle arrest, apoptosis, invasion, and metastasis of cancer cells. Meanwhile, we also intend to give an overview of the mechanisms identified so far. The breakthrough findings may shed light on using rhein as a targeted-cancer therapy. 展开更多
关键词 rhein Cancer cells APOPTOSIS Cell cycle arrest
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Protective effects of catalpol and rhein in murine experimental autoimmune encephalomyelitis via regulation of T helper (Th)1, Th2,Th17, and regulatory T cell responses 被引量:3
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作者 Wei Mingyan Yang Tao +3 位作者 Li Qian Zhou Dongdong Du Zongpan Fan Yongping 《Journal of Traditional Chinese Medicine》 SCIE CAS CSCD 2019年第6期809-817,共9页
OBJECTIVE:To examine the effects of catalpol and rhein on pro-and anti-inflammatory responses in C57 BL/6 mice with experimental autoimmune encephalomyelitis(EAE),a model of multiple sclerosis.METHODS:Female C57 BL/6 ... OBJECTIVE:To examine the effects of catalpol and rhein on pro-and anti-inflammatory responses in C57 BL/6 mice with experimental autoimmune encephalomyelitis(EAE),a model of multiple sclerosis.METHODS:Female C57 BL/6 mice were randomly divided into four groups(n=30):(a)normal salinecontrol,(b)EAE control,(c)EAE+prednisone acetate(PA,6 mg/kg),and(d)EAE+catalpol(40 mg/kg)and rhein(5 mg/kg).EAE was induced by injection of myelin oligodendrocyte glycoprotein 35-55 plus pertussis toxin.Treatments were orally administered daily for 40 d.Disease progression and neurological function were assessed using a semi-quantitative scale of tail and limb paralysis.Brains and spinal cords were collected on Days 6,20,and 40 and assessed for histopathological changes by hematoxylin and eosin staining.Production of interleukin(IL)-2,IL-4,IL-10,and IL-17 A protein was measured by enzyme-linked immunosorbent assay.Expression of the T helper(Th)1-,Th2-,Th17-,and regulatory T cell(Treg)-specific transcription factors T-bet,GATA3,ROR-γt,and Foxp3,respectively,were analyzed by quantitative reverse-transcription polymerase chain reaction and western blot analysis.RESULTS:Combination treatment with catalpol and rhein significantly alleviated the clinical disability and neurological dysfunction of mice with EAE.Catalpol and rhein treatment also reduced the infiltration of pro-inflammatory T cells into pathological lesions;significantly increased the expression of the anti-inflammatory factors GATA3,Foxp3,IL-4,and IL-10;and significantly decreased the expression of the pro-inflammatory factors T-bet,ROR-γt,IL-2,and IL-17 A.CONCLUSION:Catalpol and rhein reduced the neurological disabilities of mice with EAE,at least in part by rebalancing the pro-and anti-inflammatory environment in the brains and spinal cords. 展开更多
关键词 Multiple sclerosis ENCEPHALOMYELITIS AUTOIMMUNITY CATALPOL rhein Th1-Th2 balance Th17 cells
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Rhein inhibits transforming growth factor β1 induced plasminogen activator inhibitor-1 in endothelial cells 被引量:3
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作者 朱加明 刘志红 +2 位作者 黄海东 陈朝红 黎磊石 《Chinese Medical Journal》 SCIE CAS CSCD 2003年第3期35-40,共6页
Objectives To investigate the effect of rhein on endothelial plasminogen activator inhibitor-1 (PAI-1) mRNA expression and protein production induced by transforming growth factor β1 (TGFβ1), and to explore the mech... Objectives To investigate the effect of rhein on endothelial plasminogen activator inhibitor-1 (PAI-1) mRNA expression and protein production induced by transforming growth factor β1 (TGFβ1), and to explore the mechanism of the protective action of rhein on endothelial cells. Methods A human umbilical endothelium derived cell line (ECV-304) from ATCC was used in this study. The PAI-1 mRNA expression and protein synthesis in the endothelial cells were detected by Northern blot and flow cytometry analysis, respectively. The activity of phospho-p44/p42 MAP kinase induced by TGFβ1 was determined by immunoprecipitation analysis and western blot. Results TGFβ1 rapidly increased PAI-1 mRNA expression in the endothelial cells, and this effect lasted at least 24 hours. The upregulation of PAI-1 mRNA expression induced by TGFβ1 in endothelial cells was inhibited by rhein in a dose-dependent manner. In addition, rhein inhibited endothelial PAI-1 protein production. Further study revealed that rhein had a significant inhibitory effect on the activity of phospho-p44/p42 MAP kinase induced by TGFβ1 in human endothelial cells. Conclusions Our results showed that rhein may have a protective effect on the endothelial dysfunction by inhibiting overexpression of PAI-1, indicating a way for the treatment of vascular diseases. 展开更多
关键词 rhein endothelial cells plasminogen activator inhibitor-1
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Effects and wavelet spectral entropy analysis of rhubarb extracts rhein on synaptic transmission in rat hippocampal ca1 area in vitro 被引量:12
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作者 GUJian-wen ZHENGChong-xun +6 位作者 ZHANGAi-hua HiroshiHasuo TakashiAkasu YANGWen-tao YANGli-bin XIAXun MAYuan 《Chinese Medical Journal》 SCIE CAS CSCD 2005年第10期817-823,共7页
Background 5-dihydroxyanthraquinone-2-carboxylic acid (rhein) inhibits oxidoreduction induced by reducing nicotingamide adenine dinucleotide in the mitochondria and reducing reactive oxygen species, it also suppresses... Background 5-dihydroxyanthraquinone-2-carboxylic acid (rhein) inhibits oxidoreduction induced by reducing nicotingamide adenine dinucleotide in the mitochondria and reducing reactive oxygen species, it also suppresses lipid peroxidation in rat brain homogenates. This study was to assess the effects of anthraquinone derivatives, rhein on synaptic transmission in the rat hippocampal CA_1 pyramidal cell layer by intracellular recording.Methods The excitatory postsynaptic potential (EPSP) evoked by stimulation of the Schaffer collaterals in the presence of bicuculline (15 μmol/L) was depressed by application of rhein (0.3-30 μmol/L). The amplitude of the EPSP was restored within 20 minutes after removal of rhein from the supernatant. At a concentration of 30 μmol/L, rhein reduced the amplitude of the EPSP to 42%±3.7% (n=24) of the control. Subsequently, wavelet spectral entropy was used to analyze the EPSP. Results A strong positive correlation was observed between the wavelet spectral entropy and other parameters such as amplitude, slope of rising phase and slope of descending phase of the EPSP. The paired-pulse facilitation (PPF) of the EPSP was significantly increased by rhein (30 μmol/L). The inhibitory postsynaptic potential (IPSP) recorded in the presence of CNQX (20 μmol/L) and APV (40 μmol/L) is not altered by rhein (30 μmol/L). Conclusions Rhein (30 μmol/L) can decrease the frequency but not the amplitude of the miniature EPSP (mEPSP). It is suggested that rhein inhibits excitatory synaptic transmission by decreasing the release of glutamate in rat hippocampal CA_1 pyramidal neurons. 展开更多
关键词 rhein · hippocampus CA_1 · excitatory postsynaptic potential · presynaptic inhibition
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Effect of rhein on glucose transporter-1 expression and its function in glomerular mesangial cells 被引量:1
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作者 章精 刘志红 +2 位作者 陈朝红 李颖健 黎磊石 《Chinese Medical Journal》 SCIE CAS CSCD 1999年第12期21-23,共3页
Objective To explore the effect of rhein on the regulation of glucose transporter 1 (GLUT1) overexpression and the possible molecular mechanism that rhein antagonize the effect of transforming growth factor β1 (TGF ... Objective To explore the effect of rhein on the regulation of glucose transporter 1 (GLUT1) overexpression and the possible molecular mechanism that rhein antagonize the effect of transforming growth factor β1 (TGF β1) in glomerular mesangial cells Methods Cultured mouse mesangial cells were used The expression of GLUT1 mRNA was detected by Northern blotting; the ability of glucose uptake was determined by 2 deoxy [ 3H] D glucose uptake assay Results Rhein had no effect on glucose uptake in mesangial cells cultured in normal glucose concentration TGF β1 could upregulate the expression of GLUT1 mRNA and glucose uptake in mesangial cells This effect was markedly attenuated by the addition of rhein in a dose dependent manner Conclusions TGF β1 could upregulate the expression of GLUT1 mRNA and glucose uptake in mesangial cells, resulting in excessive glucose consumption and extracellular matrix production in diabetic nephropathy Rhein antagonized the effect of TGF β1 in mesangial cells, so it might be a hopeful remedy for the treatment of patients with diabetic 展开更多
关键词 GLUCOSE TRANSPORTER 1 · TRANSFORMING growth FACTOR β1 · rhein · MESANGIAL cells
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Nano Calcium-Deficient Hydroxyapatite/O-carboxymethyl Chitosan-CaCl_(2) Microspheres Loadedwith RheinforBone Defect Repair 被引量:1
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作者 Zhenzhen Tian Yuanyuan Guo +3 位作者 Xiuying Yang Kebing Guo Jingou Ji Shilei Hao 《Journal of Bionic Engineering》 SCIE EI CSCD 2022年第4期1087-1099,共13页
Glutaraldehyde(GA),the most widely used crosslinking agent for biomaterials,is cytotoxic.CaCl_(2) is of particular interest due to its non-toxic nature.Rhein can chelate Ca^(2+)and promote bone growth.Here we reported... Glutaraldehyde(GA),the most widely used crosslinking agent for biomaterials,is cytotoxic.CaCl_(2) is of particular interest due to its non-toxic nature.Rhein can chelate Ca^(2+)and promote bone growth.Here we reported a novel nano calcium-deficient hydroxyapatite/O-carboxymethyl chitosan-CaCl_(2) microspheres loaded with rhein(RH-nCDHA/OCMC-CaCl_(2) microspheres)using CaCl_(2) as crosslinking agent for bone defect repair.The obtained microspheres were characterized by X-ray diffraction(XRD),scanning electron microscopy(SEM),thermogravimetric analysis(TG)and Fourier transform infrared spectroscopy(FT-IR).The surface of the obtained microspheres is rough with quite a few voids.The nano calcium-deficient hydroxyapatite(nCDHA)accounts for about 70% of the total weight of the microspheres,which is equivalent to the proportion of inorganic substances in human bones.A high encapsulation efficiency(EE)and loading capacity(LC)of the microspheres loaded with rhein was 90.20±0.60% and 11.03±0.30%,respectively.For microspheres using CaCl_(2) in simulated body fluid(SBF)after 14 days,the drug released continuously and bone-like apatite formed like layer.The cells on the surface of the RH-nCDHA/OCMC-CaCl_(2) microspheres grew better comparing with nCDHA/OCMC-GA microspheres and the skull defects of rats after landfill can be almost repaired after 8 weeks,which revealed the potential of the microspheres for bone repair. 展开更多
关键词 Nano calcium-deficient hydroxyapatite O-carboxymethyl chitosan rhein MICROSPHERES Bone repair
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Anti-inflammatory mechanism of rhein in treating asthma based on network pharmacology 被引量:1
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作者 FENG Junfang CHEN Ou WANG Yibiao 《Journal of Traditional Chinese Medicine》 SCIE CSCD 2022年第2期296-303,共8页
OBJECTIVE:To predict the anti-inflammatory targets and related pathways of rhein in the treatment of asthma by using network pharmacology,and to further explore its potential mechanism in asthma.METHODS:The correspond... OBJECTIVE:To predict the anti-inflammatory targets and related pathways of rhein in the treatment of asthma by using network pharmacology,and to further explore its potential mechanism in asthma.METHODS:The corresponding targets of rhein were obtained from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP),and the rhein-target network was constructed with Cytoscape 3.7.1 software.The Genbank and Drugbank databases were used to collect and screen asthma targets,and the rhein-target-disease interaction network was constructed.A target protein-protein interaction(PPI)network was constructed using the STRING database to screen key targets.Finally,Kyoto Encyclopedia of Genes and Genomes(KEGG)enrichment analysis was used to identify biological processes and signaling pathways.The anti-asthmatic effects of rhein were tested in vitro,and the expression levels of proteins in the mitogen-activated protein kinase/nuclear factor kappa-B(MAPK/NF-κB)signaling pathway were assessed by western blot analysis.RESULTS:Altogether,83 targets of rhein were screened in the relevant databases,989 targets of asthma were obtained in the National Center for Biotechnology Information(NCBI)GENE Database.PPI network analysis and KEGG pathway enrichment analysis predicted that rhein could regulate the epidermal active growth factor receptor(EGFR),mitogen-activated protein kinase 14(MAPK14),tumour necrosis factor receptor superfamily member 1A(TNFRSF1A),receptor tyrosineprotein kinase erb B-2(ERBB2),and other signaling pathways.Furthermore,we selected the MAPK signaling pathway to determine the anti-inflammatory effects of rhein.Consistently,further in vitro experiments demonstrated that rhein was shown to inhibit HBE cells inflammation.CONCLUSION:The anti-inflammatory mechanism of rhein in the treatment of asthma may be related to EGFR,MAPK14,TNFRSF1A and ERBB2 as well as their signaling pathways.To prevent the exacerbation of asthma,instead of targeting a single pathway or a single target,all these targets and their signaling pathways should be controlled holistically.Rhein may alleviate the inflammation of asthma by inhibiting the MAPK/NF-κB pathway. 展开更多
关键词 ASTHMA rhein anti-inflammatory agents PHARMACOLOGY drug development
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An innovative rhein-matrine cocrystal: Synthesis, characterization,formation mechanism and pharmacokinetic study 被引量:1
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作者 Hongjuan Wang Dezhi Yang +8 位作者 Wen Zhang Junke Song Ningbo Gong Mingchao Yu Shiying Yang Baoxi Zhang Qiwen Liu Guanhua Du Yang Lu 《Chinese Chemical Letters》 SCIE CAS CSCD 2023年第2期546-549,共4页
Rhein(Rhe), an anthraquinone derivative, exhibits excellent anti-inflammatory effects and other pharmacological activities, but its clinical application remains limited due to poor solubility. The present work aims at... Rhein(Rhe), an anthraquinone derivative, exhibits excellent anti-inflammatory effects and other pharmacological activities, but its clinical application remains limited due to poor solubility. The present work aims at the improvement of solubility and oral bioavailability of Rhe through cocrystal formation. For this purpose, Rhe and matrine(Mat) were selected as pharmaceutical ingredient(API) and cocrystal former(CCF), respectively, and the Rhe-Mat cocrystal was synthesized and characterized by single crystal X-ray diffraction(SXRD), powder X-ray diffraction(PXRD), thermogravimetric analysis(TGA), differential scanning calorimetry(DSC). The formation mechanism of Rhe-Mat cocrystal was elucidated by molecular surface electrostatic potential(MSEP). It is worth mentioning that the 50-fold increment of dissolution in vitro was observed in pure water in the form of Rhe-Mat cocrystal. Furthermore, the in vivo studies revealed that Rhe-Mat cocrystal indicated the faster absorption rate and the higher peak blood concentration than the pure Rhe. Hence, it can be concluded that current study successfully improved the solubility and oral bioavailability of Rhe. 展开更多
关键词 rhein MATRINE COCRYSTAL Poor solubility Molecular surface electrostatic potential
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Structural landscape on a series of rhein:Berberine cocrystal salt solvates:The formation,dissolution elucidation from experimental and theoretical investigations
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作者 Dezhi Yang Hongjuan Wang +7 位作者 Qiwen Liu Penghui Yuan Ting Chen Li Zhang Shiying Yang Zhengzheng Zhou Yang Lu Guanhua Du 《Chinese Chemical Letters》 SCIE CAS CSCD 2022年第6期3207-3211,共5页
The specific crystalline form of a compound remarkably affects its physicochemical properties.Therefore,a detailed analysis of the structural features and intermolecular interactions of a multi-component crystal is fe... The specific crystalline form of a compound remarkably affects its physicochemical properties.Therefore,a detailed analysis of the structural features and intermolecular interactions of a multi-component crystal is feasible to understand the relationships among the structure,physicochemical properties and the formation mechanism.In the present study,three novel cocrystal salt solvates of rhein and berberine were reported for the first time.Various solid characterizations and theoretical computations based on density functional theory(DFT)were carried out to demonstrate the intermolecular interactions.The theoretical computation shows that the strongest interaction existed between berberine cation and rhein anion,and the electrostatic interaction play a dominant role.However,no salt bond was observed between them.Further intrinsic dissolution rate analysis in water shows that the monohydrate exhibits 17 times enhancement in comparison with rhein.The rhein and berberine combined in ionic state in cocrystal salt is the main reason for the solubility improvement.This paper suggests that the interactions between the different components can be visualized and qualitatively and quantitatively analyzed by theoretical computation,which is helpful to understand the relationship between stereochemical structure and physicochemical properties of multi-component complex. 展开更多
关键词 COCRYSTAL rhein BERBERINE Theoretical computation Energy decomposition analysis SOLUBILITY
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