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ObjectiveTo examine the inhibitory effects of berberine compounds, including columbamine, on acetylcholinesterase from the perspectives of drug-target binding affinity and kinetics and explore the blood-brain barrier (BBB) permeability of these compounds in different multi-component backgrounds. MethodThe median inhibitory concentration (IC50) of acetylcholinesterase by berberine compounds including columbamine was measured using the Ellman-modified spectrophotometric method. The binding kinetic parameters (Koff) of these compounds with acetylcholinesterase were determined using the enzyme activity recovery method. A qualitative analysis of the ability of these components to penetrate the BBB and arrive at the brain tissue in diverse multi-component backgrounds (including medicinal herbs and compound formulas) was conducted using ultra performance liquid chromatography-high resolution mass spectrometry (UPLC-HRMS). ResultBerberine compounds, including columbamine, exhibited strong inhibition of acetylcholinesterase, with IC50 values in the nanomolar range. Moreover, they displayed better drug-target binding kinetics characteristics (with smaller Koff values) than the positive control of donepezil hydrochloride (P<0.01), indicating a longer inhibition duration of acetylcholinesterase. Berberine components such as columbamine could penetrate the BBB to arrive at brain tissue in the form of a monomer, as well as in the multi-component backgrounds of Coptis and Phellodendri Chinensis Cortex medicinal extracts and the compound formula Huanglian Jiedutang. ConclusionThese berberine compounds such as columbamine exhibit a strong inhibitory effect on acetylcholinesterase and can arrive at brain tissue in multi-component backgrounds. In the level of pharmacological substance, this supports the clinical efficacy of compound Huanglian Jiedutang in improving Alzheimer's disease, providing data support for elucidating the pharmacological basis of compound Huanglian Jiedutang.
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ObjectiveTo identify the prototypical components and metabolites absorbed into blood and cerebrospinal fluid of Schisandrae Chinensis Fructus(SCF) based on sequential metabolism combined with liquid chromatography-mass spectrometry. MethodBlood and cerebrospinal fluid samples of integrated metabolism, intestinal metabolism and hepatic metabolism were collected from male SD rats after gavage and in situ intestinal perfusion administration, and ultra-performance liquid chromatography-quadrupole/electrostatic field orbitrap high-resolution mass spectrometry(UPLC Q-Exactive Orbitrap MS) was used to analyze and compare the differences in the spectra of SCF extract, blank plasma, administered plasma, blank cerebrospinal fluid and administered cerebrospinal fluid with ACQUITY UPLC BEH Shield RP18 column(2.1 mm×100 mm, 1.7 µm), the mobile phase was acetonitrile(A)-0.1% formic acid aqueous solution(B) for gradient elution(0-7 min, 95%B; 7-12 min, 95%-35%B; 12-17 min, 35%-15%B; 17-20 min, 15%-12%B; 20-22 min, 12%-5%B; 22-23 min, 5%B; 23-25 min, 5%-95%B; 25-28 min, 95%B). And heated electrospray ionization(HESI) was used with positive and negative ion modes, the scanning range was m/z 100-1 500. The prototypical constituents and their metabolites absorbed into blood and cerebrospinal fluid of SCF were identified according to the retention time, characteristic fragments, molecular formulae and the information of reference substances. ResultA total of 42 chemical components were identified in the extract of SCF, including lignans, flavonoids, amino acids, tannins, and others, of which lignans were the main ones. A total of 27 prototypical components and 14 metabolites were identified in plasma samples from different sites. A total of 15 prototypical components and 9 metabolites were identified in cerebrospinal fluid. The main metabolic reactions involved in the formation of metabolites were mainly demethylation, methylation, demethoxylation and hydroxylation. ConclusionThrough the systematic identification of the prototypical components and metabolites of SCF in rats, it provides data support for further better exploring the material basis of SCF in the treatment of central nervous system diseases.
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Objective:To evaluate the efficacy and safety of corneal bandage lens in the treatment of dry eye after cataract surgery in patients with mild meibomian gland dysfunction (MGD).Methods:A non-randomized controlled clinical study was conducted.Sixty eyes of 60 patients with mild MGD after cataract surgery were enrolled in Yantai Yuhuangding Hospital from June 2020 to February 2021.The patients were divided into bandage lens group and control group according their willingness, with 30 eyes in each group.All the patients received phacoemulsification and intraocular lens implantation and were administered with the same postoperative medication.Patients in bandage lens group wore lenses for 14 days continuously after the operation.Patients in control group did not wear the corneal bandage lens after the operation.The structure and inflammation of the anterior segment were observed with a slit-lamp microscope before operation and on days 1, 7, and 14 after the operation.Best corrected visual acuity (BCVA) was obtained using a standard logarithmic visual acuity chart.Ocular surface symptoms were evaluated via an ocular surface disease index (OSDI) questionnaire.The intraoperative changes of meibomian glands were assessed with an ocular surface analyzer and the non-invasive first tear film break-up time (NIFBUT) was recorded.Corneal epithelium defects were observed by corneal fluorescein sodium staining (CFS). This study adhered to the Declaration of Helsinki and was approved by an Ethics Committee of Yantai Yuhuangding Hospital (No.2021-363). Written informed consent was obtained from each patient before any medical examination.Results:On the 1st, 7th, and 14th day after surgery, no inflammatory reaction or complication was observed in both groups.Statistically significant differences in BCVA among different postoperative time points were found ( Ftime=3.610, P=0.016). BCVA on the 7th day after surgery were higher than that on the 1st day after surgery, and the BCVA on the 14th day after surgery were significantly higher than those on the 1st and 7th day after surgery in both groups, with statistically significant differences (all at P<0.05). There were statistically significant differences in OSDI scores between the two groups at different postoperative time points ( Fgroup=31.219, P<0.001; Ftime=15.672, P<0.001). The OSDI scores of bandage lens group were significantly lower than those of control group on the 7th and 14th day after surgery, OSDI scores in both groups on the 14th day after surgery were significantly lower than those on the 1st and 7th day after surgery, with statistical significance (all at P<0.05). The NIFBUT values on the 7th and 14th day after surgery were (6.62±0.93)s and (8.02±1.13)s, in control group, bandage lens group and (9.81±0.91)s and (10.03±0.49)s in bandage lens group, with a statistically significant difference between them ( Fgroup=2.351, P=0.037), and the NIFBUT values of bandage lens group on the 7th and 14th day after surgery were higher than those of control group, with statistically significant differences (both at P<0.05). The number of high CFS score eyes of bandage lens group were lower than those of control group on the 7th and 14th day after surgery, and the differences were statistically significant ( χ 2=7.391, P=0.025; χ 2=9.317, P=0.002). Conclusions:For patients with mild MGD after cataract surgery, wearing bandage contact lens has no obvious ocular adverse reaction and can promote the growth of corneal epithelium, enhance the stability of tear film, improve dry eye symptoms, and relieve dry eye manifestations after surgery.
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Objective:To analyze the metabolites of isoacteoside in rat's urine after oral administration by UHPLC-LTQ-Orbitrap and then summarize its metabolic pathways.Methods:The rats were randomly divided into treatment and control groups. Isoacteoside dissolved in saline was orally administered to the rats in the treatment group witht a single dose of 100 mg/kg. At the same time, saline was orally administered to the control group with the same volume. The urine samples were collected for 12 h and then purified. Sample analyses were performed on a Thermo Scientific BOS Hypersil C18 column (2.1 mm × 150 mm, 2.4 μm), the mobile phase consisted of water containing 0.1% formic acid-acetonitrile in a gradient program, the flow rate was set at 0.3 ml/min and the column was maintained at 30 ℃. The urine samples of the treatment group and control groups were detected with negative ion mode.Results:The metabolites were identified according to their protonated molecular ions and fragment ions and by comparing the mass data with that of reference standards and the published data. In total, 8 metabolites of isoacteoside were detected and identified in the urine samples of treatment group and the major metabolic pathway of isoacteoside included glucuronide conjugation, dehydroxylation, hydrolyzation, methyl conjugation and sulphate conjugation.Conclusions:UHPLC-LTQ-Orbitrap could be used to analyze the main metabolites and metabolic pathways of isophylloside in rats, which can provide references for further studies on pharmacodynamics and pharmacological mechanisms.
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Objective The aims of this study were to develop an ultraviolet-visible spectrophotometry (UV-Vis) for the determination of quaternary ammonium alkaloid content in Lycium ruthenicumMurr., and to analysis the constitution of its nitrogenous compounds by liquid chromatograph - mass spectrometry(LC-MS). Methods The quaternary ammonium alkaloid content was determined by a UV-Vis spectrophotometer at 524 nm. The ultra performance liquid chromatography(UPLC) analysis was performed on BOS Hypersil C18 column(2.1 mm × 150 mm, 2.4μm), with 0.1% formic acid solution(A)–acetonitrile(B) as the mobile phase for gradient elution. The flow rate was 0.3 ml/min, and the column temperature was 35℃, Multiple reaction monitoring (MRM) equipped with electrospray ion source was performed in positive ion mode for structure analysis.Results As a standard, the betaine was linear in the range of 981μg-4906μg,Y=0.0001X-0.0055, r=0.9993, and the average recovery rate was 98.53%,RSD=1.19%(n=6). There were 12 nitrogenous compounds analyzed by LC-MS, with N(1)-dihydrocaffeoyl-N(12)-caffeoyl spermine and p-Hydroxyl-cinnamyl-dihydrocaffeoyl spermidine were first reported.Conclusions The method developed in this subject is simple, accurate with good repeatability, which can be applied for determination of quaternary ammonium alkaloid content in Lycium ruthenicumMurr. And the structure analysis of its nitrogenous compounds will deepen the understanding of the compounds inLycium ruthenicumMurr.
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Objective DryLab software was used to assist high performance liquid chromatography (HPLC) method to test and isolate six Cytochrome P450 (CYP450) probe substrates.Methods Six CYP450 probe substrates were selected and the right HPLC method was developed and validated with the assistance of DryLab software.Results The new HPLC method with the assistance of DryLab software could test and isolate six probe substrates with degrees of isolation more than 2.00. The correlation coefficients (R> 0.999 8) indicated high linear correlation between the concentrations and the peak areas among six probe substrates. Recovery studies showed good results for all the probe substrat from 86.38% to 110.29%. And therelative standard deviation (RSD) ranged from 1.69% to 3.80% with its intra-day and inter-day precision ranging from 0.42% to 2.01%, and 1.36% to 2.29%, respectively.Conclusions The developed HPLC method with the assistance of DryLab could test and isolate six probe substrates with shortertime than the HPLC method alone.
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With the deepening of the study on traditional Chinese medicinal quality and the rising requirements of TCM quality control, the demand of setting TCM quality were emphasized,as well as higher education course. Surrounding the purpose of exploring the related issues of the traditional Chinesemedicinal courses setting and promoting the college curriculum innovation capability,the paper mainly discussed the course open orientation, the teaching characteristics, objectives, idea, the core content and the training scheme, as well as the plan of course and teaching material construction depended on these contents.
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Objective The alm of this study was to determine the solubility and permeability of daldzin and daldzein and the interaction of these two components.Methods With the method inChinese Pharmacopoeia and in situ single-pass intestinal perfusion model we tested the solubility and permeability of daldzin, daldzein and their interaction.Results In pH 7.4 K-R buffer the solubility of daldzin was 6 times than daldzein and both the solubility of these two components were enhanced when they were determined together. In small intestine of rat, the permeability of daldzein was 3 times than daldzin. Daldzin could enhance the permeability of daldzein but the daldzein manifested an opposite trend.Conclusion When compared to daldzin, daldzein owned a lower solubility but a better permeability. When used together, both the solubility and permeability of daldzein would be enhanced. The solubility of daldzin could be enhanced slightly but its permeability would be reduced.
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Objective This paper was to study the absorption and metabolism differences of intestine and liver for multicomponent licorice.Methods The components were identified with the UPLC-MS/MS. In situ closed-loop method was used to carry out the comparative experiments of absorption and metabolism differences between intestine and liver.Results 13 components were identified by UPLC-MS/MS. The absorption and metabolism results indicated some components in licorice water extract could be absorbed into blood and metabolism happened during this process. 14 metabolites were detected in the plasma sample. The hepatic metabolism results indicated many components could experience complex metabolism and more metabolites could be generated.Conclusions Liver was the major metabolism organ for licorice water extract and some components could be metabolized along with the absorption process in intestine. The absorption and metabolism differences between intestine and liver were significant.
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To study the initiatives and progress of African nations in promoting the development of traditional medicine to determine if these measures can be applied to the protection of traditional Chinese medicine knowledge. Information research methods were used to collect and analyze relevant literature. The development of African traditional medicine has been effectively promoted through various measures taken by African organizations and governments. In recent years, Africa has achieved remarkable results in promoting the development of traditional medicine. Many other countries will benefit from studying their examples and adopting similar measures.
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Objective To select the components for quality control of Fructus Lycii based on the absorption of its extract. Methods To investigate metabolism of components of Fructus Lycii, everted rat gut sacs was carried out as well as the blood was taken from abdominal aorta,.and all samples were analysised by HPLC. Results There are twelve constituents absorbed between ileum and jejunum of rat , and four constituents were detected in the blood. Compound 2, 3, 4, 5, 6, 9, 10, 11 were absorbed in prototype forms in the intestine directly,and compound 1, 7, 8, 12 were new ones. On the other hand, four compositions(3, 7, 10, 13)could be absorbed into blood through analysis serum samples obtaining from aorta abdominalis of rats. Two of them (3, 10)could be absorbed directly by intestine, while(7)was absorbed into blood in new form . Conclusion Based on the intestinal absorption experiment and analysion of compsition in blood, components (3, 10, 13) can be the quality control ingredients of Fructus Lycii.
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With the daily increase of living and working pressure in people,sub-health problem has been more and more predominant.How to guide people to throw of the attack of sub-health has been our major task.Through analyzing the distribution,type and attention degree of sub-health population,this article investigates points of science popularization for providing target-orientation science popularization knowledge.
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Good Agricultural Practice for Chinese Crude Drugs is one of the effective measures for protecting and developing resource of Chinese crude drugs..We analyzed the current situation of GAP,discussed its questions and development.
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Objective To Analyze the proprietary usage of Chinese medicine prescriptions in our hospital and to improve the level of rational drug use.Methods 1780 prescriptions were randomly collected from our hospital during January to June,2011 and analyzed.Results The rational prescriptions had a 83.01% share in the whole.while the irrational prescriptions had a 21.2% share in the whole,among which 13.37% were unqualified writing,3.45% were irrational drug use.The irrationality mainly manifested as missing items in the prescription,and improper usage and dosage.Conclusion It is suggested to strengthen the awareness of physicians on standard prescription writing,strict pharmacist review,and establish prescription quality management system to improve the quality of prescription.
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The preventative treatment theory is a very important part of traditional Chinese medicine. When this theory is used in the treatment of common cold disease, it focuses on the prevention of common cold disease. The preventative treatment theory is very important and can be applied in the whole process of the treatment common cold disease.
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ObjectiveTo research the metabolism of components in the Radix of Paeonia lactiflora Pall. Methods(①) we established the HPLC fingerprint of water extract of Paeonia lactiflora Pall. and real-time monitored the chemical composition. (②) We established the HPLC fingerprint of rats' serum samples from hepatic portal vein, serum samples from aorta abdominalis and samples of intestinal absorption of Paeonia lactiflora Pall. (③) On this basis, using the established methods, I-IPLC fingerprint spectrum of serum samples,the sample of herb, the sample after intestinal metabolism, rats' serum samples from hepatic portal vein and rats'serum samples from aorta abdominalis were analyzed and compared in order to infer the metabolism of components in the Radix of Paeonia lactiflora Pall. Results24 compositions were detected, seven of which were metabolized by intestinal flora and could not be absorbed into blood; six of them could not be absorbed directedly into intestinal; eight new compounds were absorbed into blood after bowel metabolism while they were not detected in water extract in Paeonia lactiflora Pall. ConclusionWe could infer the metabolic processes of chemicals of Paeonia lactiflora Pall. in oral administration with this method.
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Based on the literatures published from January 1994 to December 2008 on chronic respiratory diseases treated by the therapy of “Dongbing-Xiazhi” (which means treating diseases occurred in winter but treated in summer),the time,region,specific therapies,herbs,and acupoints of these literature were reviewed end analyzed by bibliometric methods to explore its distribution and trends.The research showed that the therapy was effective and widely used in recurrent chronic respiratory diseases.It also demonstrated that such studies as focusing on the scientific design and the mechanism were needed.
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Objective To analyze the correlation of metabolic syndrome (MS) and its components with a future development of diabetes mellitus (DM) in elderly patients. Methods In 2007, the cohort study was carried out among the 2001 baseline population. The criteria which was proposed by international diabetes federation in 2005 was referred to diagnose MS. Results MS predicted the future development of DM (RR = 4. 70, 95% CI:3.23~6.85). Among MS components, fasting glucose exhibited the highest association with DM. The univariate analysis showed that while fasting glucose was more than 5. 6 mmol/L, the RR(95% CD was 9. 68(6. 59~ 14.23). And multiple factors analysis showed that while fasting glucose was 5.60 mmol/L~6. 09 mmol/L, the RR(95% CD was 5. 49(3. 38~8. 92). While glucose level was more than 6. 1 but less than 7.0 mmol/L, the RR(95% CI) increased to 14.44(9.29~22.44). However, along with the increasing of cluster number of MS components from 1,2,3,4 to 5, the corresponding RR increased from 2. 92, 5. 67, 12. 28, 19. 52 to 37. 83. Conclusions MS increases the risk of DM. Among MS components, fasting glucose level is the strongest risk indicator of DM.
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By reviewing the selection principle and evaluation criterion on the periodicals in the well-known evaluation and index system of China and abroad, the article provides both the related information for researchers to get a general idea of this system and the criterion for periodicals to join the system.
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AIM: To study the FT-IR fingerprinting characteristic of Huangjinju Powder Injection(HJJ)(Flos Trollii chinensis,Flos chrysanthemi indici,Flos Lonicerae Japonicae) and its effective constituents.METHODS: We adopt FT-IR and the second order derivative FT-IR,analysis by the related ratio,and then describe its mass characteristic by its crude drugs and the effective constituents. RESULTS: HJJ has fifteen peaks that are in turn,3735,2931,1664,1614,1450,1408,1360,1291,1191,1067,915,768,687,597 and 417 cm~(-1).Its special peak in the second order derivative is 1416 cm~(-1).The characteristics of the constituents of its crude drug that Flos Trollii Chinensis has 2926 and 1609 cm~(-1),Flos Chrysanthemi Indici has 1660 and 1609 cm~(-1) and Flos Lonicerae Japonicae has 767.The effective constituents that Baicalin owns 1664,1614,1450,1408,1067,915,768,687,597 and 417 cm~(-1),Orientin owns 2931,1614,1291 and 1191 cm~(-1),Vitexin owns 1614,1360,1067 and 597,Linarin owns 1450,1067 and 597 cm~(-1),Chlorogenic acid owns 1614,1291 and 1191 cm~(-1),Caffeic acid owns 1450 and 1360,and Hyperin owns 1360 and 1291. CONCLUSION: The effective constituents of FT-IR can be used in evaluating the mass of Huangjinju Powder Injection and reflect the key characteristic of its essence.It owns the obvious characteristics and specificity.