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Hypoglycemic Activity of jatrorrhizine

Journal of Huazhong University of Science and Technology(Medical Sciences) 2005年第5期25卷 491-493页

作者：付燕胡本容汤强付琴向继洲 Department of Pharmacology School of Basic Medical Sciences Tongji Medical College Huazhong University of Science and Technology Wuhan 430022 China

Summary： The hypoglycemic activity and its mechanism of jatrorrhizine （Jat） were studied. The normal mice and alloxan-induced hyperglycemic mice were given with different doses of Jat. Blood glucose and liver glycogen levels were determined by spectrophotometry with glucose-oxidase and iodine reagents respectively. The levels of blood lactic acid （LC） and liver lactate dehydrogenase （LDH） activity were measured to explore the effect of Jat on anaerobic glycolysis. Succinate dehydrogenase （SDH） activity in liver was measured to evaluate the effect of Jat on aerobic glycolysis in liver. It was found that Jat （50 mg/kg, 100 mg/kg） could significantly decrease blood glucose level in a dose- and time-dependent manner in both normal and alloxan-diabetic mice, increase the activity of SDH, but had no significant effects on the LC level and LDH activity. Jat could significantly reduce the content of liver glycogen in normal mice. Moreover, Jat could inhibit the platelet aggregation in rabbits in vitro in a dose-effect relationship. It was concluded that Jat induced the pronounced decrease in blood glucose in normal and hyperglycemic mice. The hypoglycemic activity of Jat may be attributed to the enhancement of aerobic glycolysis.

关键词： jatrorrhizine hypoglycemia blood glucose succinate dehydrogenase liver glycogen platelet aggregation

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Synthesis and Biological Evaluation of Novel jatrorrhizine Derivatives with Amino Groups Linked at the 3-position as Inhibitors of Acetylcholinesterase

Synthesis and Biological Evaluation of Novel Jatrorrhizine D...

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中国生物工程学会第十一届学术年会暨2017年全国生物技术大会

作者： Xiaofei Jiang Nengling Zhang Nanqiang Xiong Yi Liu Jiangfeng Cao ShengX iang Qiu Key laboratoryof Plant Resources Conservation and Sustainable Utilization South China Botanical Graduate Chinese Academy of Sciences School of Chemistry and Life Sciences Guizhou University of Education School of Pharmacy Guizhou Medical University

jatrorrhizine was considered as one of the active constituents of Coptis chinensis Franch. jatrorrhizine derivatives with substituted amino groups linked at the 3-position were designed,synthesized, and biologically evaluated as inhibitors of acetylcholinesterase. jatrorrhizine derivatives inhibited acetylcholinesterase(AChE) to a greater extent than the lead compound jatrorrhizine. All these jatrorrhizine derivatives were potent inhibitors of AChE, with IC50 values at submicromolar,Compound 3 g gave the most potent inhibitor activity with an IC50 of 0.35μM for AChE. The inhibition activity of jatrorrhizine derivatives to butyrylcholinesterase(BuChE) is lower than AChE which suggest jatrorrhizine derivatives with good selectivity ratios of AChE/BuChE. Indicating the compounds are an excellent agents for Alzheimer’s disease(AD).

关键词： jatrorrhizine jatrorrhizine derivatives AChE/BuChE inhibitor Synthesis Structure-activity

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The telomerase-targeting Pt(Ⅱ) complex of jatrorrhizine derivative induce apoptosis in human bladder tumor cells

The telomerase-targeting Pt(Ⅱ) complex of jatrorrhizine der...

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第十一届全国化学生物学学术会议

作者： Qi-Pin Qin Zhen-Feng Wang Xiao-Ling Huang Ming-Xiong Tan Guangxi Key Lab of Agricultural Resources Chemistry and Biotechnology College of Chemistry and Food ScienceYulin Normal University

The jatrorrhizine was the major bioactive alkaloids isolated from Tinospora capillipes Gagnep. It was important compounds because of their wide range of pharmacological activities including antifungal,anti-tumor and antibacterial activities. However,no jatrorrhizine metal complexes have been ***,a new Pt(II) complex,[Pt(J-TFA)Cl]Cl(Pt1) with jatrorrhizine derivatives(J-TFA) was first prepared as desirable luminescent agents for cellular applications and potent telomerase inhibitors,which can induce bladder T-24 tumor cell apoptosis by targeting telomerase,together with induction of mitochondrial dysfunction,telomere DNA damage and cell-cycle ***,jatrorrhizine Pt1 complex may have the potential to be further developed into safe and effective Pt-based anticancer agents.

关键词： Platinum complex jatrorrhizine telomerase mitochondrial dysfunction

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Microcalorimetric Investigation of the Antibacterial Activity of jatrorrhizine

Microcalorimetric Investigation of the Antibacterial Activit...

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第十七届全国化学热力学和热分析学术会议

作者： R.Mi Y.J.Hu Hubei Key Laboratory of Pollutant Analysis ＆ Reuse Technology Department of Chemistry Hubei Normal University

Isoquinoline alkaloids exhibit not only significant activity against a variety of organisms including bacteria, viruses, fungi, protozoans, helminthes, and chlamydia, but also potential anticancer properties. jatrorrhizine, an isoquinoline alkaloid, is an important medicinal herbal extract possessing diverse pharmacological and biological activities. In this antibacterial agents study, microcalorimetry was used to investigate interaction between jatrorrhizine and three kinds of bacteria, Shigella dysenteriae（S. dysenteriae）, Staphylococcus aureus（S. aureus） and Escherichia coli（E. coli） to evaluate the antibacterial effect of jatrorrhizine through analyzing the power-time curves, quantitative parameters, such as the growth rate constant（k）, maximum heat output power（Pmax）, peak time of maximum heat output power（tp） which were obtained to characterize the interactions. The results showed that jatrorrhizine presented strong antibacterial effect on the three kinds of bacteria with the sequence of inhibitory effects as: S. aureus ＞ S. dysenteriae ＞ E. coli. And the results were in accordance with clinical efficacy trials references. jatrorrhizine might be used as a potential novel antibacterial agent in practice. Microcalorimetric investigation of the effect of antibacterial agent on bacterial pathogens was promising in comparison to other methods.

关键词： jatrorrhizine microcalorimetry S.aureus S.dysenteriae E.coli

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Screening the Synergistic Components of Acetylcholinesterase Inhibition from Phellodendron Bark Based on Fingerprint-Activity Relationship Modeling

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World Journal of Traditional Chinese Medicine 2023年第4期9卷 461-468页

作者： Hong-Shan Zhou Qi-Ming Luo Xiao-Bing Lin Chuan-Sheng Zhu Ping Li Wen Gao State Key Laboratory of Natural Medicines School of Traditional Chinese PharmacyChina Pharmaceutical UniversityNanjingChina

Objective:Phellodendron chinense(PC)bark and Phellodendron amurense(PA)bark are two herbal medicines recorded in the Chinese Pharmacopoeia(2020 edition)that are easily mistaken for one *** this study,the chemical constituents of PC and PA were compared using chromatographic fingerprints,and the potential synergistic acetylcholinesterase(ACh E)inhibitor components were screened based on the correlation of fingerprint *** and Methods:Chromatographic fingerprints based on high-performance liquid chromatography were developed for the analysis and comparison of chemical compounds in PC and PA *** ACh E inhibitory activity of PC and PA was determined using the Ellman ***,the contribution of the characterized alkaloids in PC and PA to the overall ACh E inhibition was modeled using partial least squares regression(PLSR).Results:The total alkaloid content in PC was higher than that in PA,which causes PC to have stronger anti-ACh E ***,13 and 20 common peaks were identified in the PC and PA samples,*** them,berberine(BER)was the dominant alkaloid in PC,which covered more than 65%of the total peak area in PC,but only approximately 25%of that in PA,indicating that the chemical composition is different between PC and *** spectrum–effect analysis based on PLSR and the correlation analysis showed that the BER-palmatine(PAL)and BER-jatrorrhizine(JAT)pairs have a synergistic inhibitory effect on ACh E ***:A high-performance chromatographic fingerprint was established to distinguish PC and *** efficacy-associated markers were screened,including the pairs of BER-PAL and BER-JAT with anti-ACh E activity,and the findings may assist with the quality control of PA and PC.

关键词： Berberine combination index high-performance chromatography fingerprint jatrorrhizine palmatine

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Simultaneous Determination of Effective Components of Gegen Qinlian Tablets by HPLC

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Medicinal Plant 2020年第1期11卷 24-28,36页

作者： Lili LI Yifeng LU Xueyan ZHU Guangxi Institute for Food and Drug Control Nanning 530021China

[Objectives]To establish a HPLC method for the simultaneous determination of 14 characteristic components in Gegen Qinlian tablets and the content of Gegen Qinlian tablets in 11 manufacturers.[Methods]A Inertsil ODS-3(250 mm×4.6 mm,5μm)reversed-phase high performance liquid chromatography column was used with acetonitrile-0.02 mol/L ammonium acetate+0.03%triethylamine solution(adjusted with glacial acetic acid to pH of 4.3)as the mobile phase for gradient elution at a flow rate of 1.0 mL/*** determination wavelength of 8 components(puerarin,daidzin,liquiritin,baicalin,wogonoside,daidzein,ammonium glycyrrhizinate,baicalein)was 250 nm;the determination wavelength of wogonoside was 280 nm;the determination wavelength of 5 components(epierberine,jatrorrhizine hydrochloride,coptisine,palmatine hydrochloride and berberine hydrochloride)was 346 nm.[Results]There was a good linear relationship between the injection volume of puerarin,daidzin,liquiritin,baicalin,wogonoside,epierberine,jatrorrhizine hydrochloride,coptisine,daidzein,palmatine hydrochloride,ammonium glycyrrhizinate,berberine hydrochloride,baicalein and wogonin and peak area(r>0.9990)in the range of 146.26-5850.24,24.13-965.04,18.45-738.00,79.18-3167.32,9.57-382.80,4.76-190.40,2.57-102.80,13.41-536.40,10.60-424.00,11.33-453.22,12.08-483.20,46.73-1869.25,20.28-811.20,12.11-484.50 ng,respectively;the average recovery rates(n=6)were 2.18%,1.79%,1.81%,1.68%,2.27%,2.13%,1.96%,1.07%,0.93%,0.61%,2.92%,0.77%,2.79%and 0.62%,respectively;the precision,repeatability and stability were good,and the RSD was less than 3%.This method was used to determine 16 batches of Gegen Qinlian tablets produced by 11 *** was not detected in a lot of samples,but 14 components were detected for other enterprises,but the content was different.[Conclusions]The method was accurate and feasible and could be used for the overall quality control of this variety.

关键词： Gegen Qinlian tablets Content determination High performance liquid chromatography Puerarin Daidzin Liquiritin Baicalin Wogonoside Epierberine jatrorrhizine hydrochloride Coptisine Daidzein Palmatine hydrochloride Ammonium glycyrrhizinate Berberine hydrochloride Baicalein Wogonin

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Simultaneous Determination of Six Components in Cortex Phellodendri by HPLC

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Agricultural Biotechnology 2023年第2期12卷 87-90页

作者： Lian LIAN Guosheng WAN Weili JIA Huiyuan GAO School of Biological and Chemical Engineering Liaoning Institute of Science and TechnologyBenxi 117004China College of Traditional Chinese Medicine Shenyang Pharmaceutical UniversityShenyang 110016China

[Objectives]This study was conducted to establish the method for simultaneous determination of six active components.[Methods]Simultaneous determination of chlorogenic acid,phellodendrine,magnoflorine,jatrorrhizine,palmatine and berberine in Cortex Phellodendri was carried out by HPLC with a Diamonsil C18(4.6 mm×250 mm,5μm)column was *** mobile phase was acetonitrile-water(1‰acetic acid,2 mmol ammonium acetate)solution in gradient *** detection wavelength was set at 280 nm,and the column temperature was kept at 25℃and the flow rate was 1 ml/min.[Results]The linear ranges of chlorogenic acid,phellodendrine,magnoflorine,jatrorrhizine,palmatine and berberine were 20.00-320.00,18.75-130.00,25.00-200.00,5.00-100.00,20.00-200.00,and 0.09-1.80 mg/L,*** average recovery was 98.1%,99.4%,97.5%,97.3%,104.0%,and 98.5%,respectively;and the RSDs were 0.5%,0.6%,0.8%,1.0%,1.4%,and 0.9%,respectively.[Conclusions]The method is convenient,stable,reliable and suitable for quality control of Cortex Phellodendri.

关键词： Cortex Phellodendri Chlorogenic acid Phellodendrine Magnoflorine jatrorrhizine Palmatine Berberine Determination

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