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1.
Acta Pharmaceutica Sinica ; (12): 1128-1137, 2023.
Article in Chinese | WPRIM | ID: wpr-978692

ABSTRACT

As a treasure resource of novel drug lead compounds, how to rapidly and high-efficiently screen and isolate active components from natural products is critical. Thanks to its high resolution, high automation and flexible integration, online two-dimensional liquid chromatography has great potential for screening active ingredients from complex matrices by integrating a highly specific bio-recognition process into a two-dimensional liquid chromatography system before, on or after the column separation. This review comprehensively summarized recent developments, applications and shortcomings of online two-dimensional liquid chromatography for natural product screening from different integration modes, including pre-column, on-column and post-column screening methods.

2.
China Journal of Chinese Materia Medica ; (24): 1249-1263, 2023.
Article in Chinese | WPRIM | ID: wpr-970596

ABSTRACT

The chemical components of Huanglian Decoction were identified by ultra-performance liquid chromatography-quadrupole-time-of-flight-tandem mass spectrometry(UPLC-Q-TOF-MS/MS) technology. The gradient elution was conducted in Agilent ZORBAX Extend-C_(18) column(2.1 mm×100 mm, 1.8 μm) with the mobile phase of 0.1% formic acid aqueous solution(A)-acetonitrile(B) at a flow rate of 0.3 mL·min~(-1) and the column temperature of 35 ℃. The MS adopted the positive and negative ion mode of electrospray ionization(ESI), and the MS data were collected under the scanning range of m/z 100-1 500. Through high-resolution MS data analysis, combined with literature comparison and confirmation of reference substances, this paper identified 134 chemical components in Huanglian Decoction, including 12 alkaloids, 23 flavonoids, 22 terpenes and saponins, 12 phenols, 7 coumarins, 12 amino acids, 23 organic acids, and 23 other compounds, and the medicinal sources of the compounds were ascribed. Based on the previous studies, 7 components were selected as the index components. Combined with the network pharmacology research and analysis me-thods, the protein and protein interaction(PPI) network information of the intersection targets was obtained through the STRING 11.0 database, and 20 core targets of efficacy were screened out. In this study, UPLC-Q-TOF-MS/MS technology was successfully used to comprehensively analyze and identify the chemical components of Huanglian Decoction, and the core targets of its efficacy were discussed in combination with network pharmacology, which laid the foundation for clarifying the material basis and quality control of Huanglian Decoction.


Subject(s)
Tandem Mass Spectrometry , Network Pharmacology , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal/chemistry , Technology
3.
Journal of Central South University(Medical Sciences) ; (12): 846-851, 2023.
Article in English | WPRIM | ID: wpr-982355

ABSTRACT

OBJECTIVES@#Early detection of asymptomatic diastolic dysfunction is essential to prevent the development of heart failure in hypertensive patients. Current studies suggest that left atrial strain contributes to the evaluation of left ventricular diastolic function, but there are fewer studies on the correlation between left atrial strain and diastolic function in hypertensive patients. In this study, we applied a two-dimensional speckle tracking technique to evaluate the changes in left atrial strain in hypertensive patients, and to investigate the relationship between left atrial strain and left ventricular diastolic function.@*METHODS@#A total of 82 hypertensive patients who were visited the Department of Cardiology at the Third Xiangya Hospital of Central South University from July 2021 to January 2022, were enrolled for this study, and 59 healthy subjects served as a control group. According to the number of left ventricular diastolic function indexes recommended by the 2016 American Society of Echocardiography Diastolic Function Guidelines (mitral annular e´ velocity: Septal e´<7 cm/s, lateral e´<10 cm/s, E/e´ ratio>14, left atrial volume index>34 mL/m2, peak tricuspid regurgitation velocity>2.8 m/s), the hypertensive patients were divided into 3 groups: Group Ⅰ (0 index, n=36 ), Group Ⅱ (1 index, n=39), and Group Ⅲ (2 indexes, n=7). Two-dimensional speckle tracking technique was used to measure left atrial reservoir strain (LASr), conduit strain, and contraction strain, and to analyze the correlation between left atrial strain and left ventricular diastolic function in hypertensive patients.@*RESULTS@#The LASr, left atrial conduit strain (LAScd), and LASr/(E/septal e´) of the hypertension group were lower than those of the control group, and E/LASr was higher than that of the control group. There was no significant difference in left atrium volume index between the 2 groups (P>0.05). Compared with Group Ⅰ, LASr, LAScd, and LASr/(E/septal e´) were decreased in Group Ⅱ and Group Ⅲ, LASr/(E/septal e´) was also decreased in Group Ⅲ compared with Group Ⅱ (all P<0.05). Compared with Group Ⅰ, E/LASr was increased in Group Ⅲ. LASr was positively correlated with septal e´, lateral e´, E, and E/A, and negatively correlated with E/septal e´.@*CONCLUSIONS@#The changes of left atrial function in patients with early hypertension are earlier than those of left atrial structure. Left atrial strain and its combination with conventional ultrasonographic indices [LASr/(E/septal e´)] of diastolic function are potentially useful in assessing left ventricular diastolic function in hypertensive patients.


Subject(s)
Humans , Atrial Fibrillation , Atrial Appendage , Heart Atria/diagnostic imaging , Hypertension/complications , Diastole
4.
China Journal of Chinese Materia Medica ; (24): 313-323, 2022.
Article in Chinese | WPRIM | ID: wpr-927973

ABSTRACT

Following the preparation of substance benchmarks in Huanglian Decoction from 18 batches, the method for detecting their characteristic spectra was established to identify the similarity range and peak attribution. The content and transfer rate ranges of the index components coptisine, palmatine, berberine, liquiritin, glycyrrhizic acid, 6-gingerol, and cinnamaldehyde and the extraction amount were combined for analyzing the quality value transfer from the Chinese medicinal pieces to substance benchmarks and clarifying the key quality attributes of substance benchmarks in Huanglian Decoction. The results showed that the substance benchmarks in Huang-lian Decoction of 18 batches exhibited good similarity in characteristic spectra(all greater than 0.98). There were 17 characteristic peaks identified in the substance benchmarks of Huanglian Decoction, including 10 from Coptidis Rhizoma, 3 from Glycyrrhizae Radix Et Rhizoma Praeparata Cum Melle(processed with water), 1 from Zingiberis Rhizoma, and 3 from Cinnamomi Ramulus. The contents and average transfer rates of the index components were listed as follows: coptisine 2.20-6.46 mg·g~(-1) and 18.50%±2.93%; palmatine 3.03-8.13 mg·g~(-1) and 26.56%±4.69%; berberine 7.71-22.29 mg·g~(-1) and 17.34%±3.00%; liquiritin 0.88-2.18 mg·g~(-1) and 9.88%±4.88%; glycyrrhizic acid 1.83-4.44 mg·g~(-1) and 8.50%±3.72%; 6-gingerol 0.56-1.43 mg·g~(-1) and 11.36%±2.37%; cinnamaldehyde 1.55-3.48 mg·g~(-1) and 19.02%±4.36%. The extraction amount of the substance benchmarks from the 18 batches was controlled at 10.65%-13.88%. In this paper, the quality value transfer of substance benchmarks in Huanglian Decoction was analyzed based on the characteristic spectra, the index component contents and the extraction amount, which has provided a basis for the subsequent development of Huanglian Decoction and the quality control of its related preparations.


Subject(s)
Chromatography, High Pressure Liquid , Drugs, Chinese Herbal/standards , Quality Control
5.
China Journal of Chinese Materia Medica ; (24): 306-312, 2022.
Article in Chinese | WPRIM | ID: wpr-927972

ABSTRACT

A total of 18 batches of Zhuru Decoction samples were prepared. Chromatographic fingerprints were established for Zhuru Decoction and single decoction pieces, the content of which was then determined. The extraction rate ranges, content, and transfer rate ranges of puerarin, liquiritin, and glycyrrhizic acid, together with the common peaks and the similarity range of the fingerprints, were determined to clarify key quality attributes of Zhuru Decoction. The 18 batches of Zhuru Decoction samples had 25 common peaks and the fingerprint similarity higher than 0.95. Puerariae Lobatae Radix, Glycyrrhizae Radix et Rhizoma, and Zingiberis Rhizoma Recens had 21, 3, and 1 characteristic peaks, respectively. The 18 batches of samples showed the extraction rates within the range of 18.45%-25.29%. Puerarin had the content of 2.20%-3.07% and the transfer rate of 38.5%-45.9%; liquiritin had the content of 0.24%-0.85% and the transfer rate of 15.9%-37.5%; glycyrrhizic acid had the content of 0.39%-1.87% and the transfer rate of 16.2%-32.8%. In this paper, the quality value transmitting of substance benchmarks of Zhuru Decoction was analyzed based on chromatographic fingerprints, extraction rate, and the content of index components. A scientific and stable method was preliminarily established, which provided a scientific basis for the quality control and formulation development of Zhuru Decoction.


Subject(s)
Chromatography, High Pressure Liquid , Drugs, Chinese Herbal/standards , Glycyrrhizic Acid/analysis , Quality Control , Rhizome/chemistry
6.
China Tropical Medicine ; (12): 1061-2022.
Article in Chinese | WPRIM | ID: wpr-974021

ABSTRACT

@#Abstract: Objective To understand the general situation of death causes of permanent residents in Hainan Province from 2014 to 2020, analyze the causes of death, and provide scientific basis for the formulation of policies related to healthy Hainan. Methods The Hainan Provincial Population Death Information Registration and Management System was used to report data, and the death information of permanent residents in Hainan Province from 2014 to 2020 was obtained. Excel 2010 and SPSS 26.0 software were applied to perform statistical analysis related to the indicators including crude mortality rate, standardized mortality rate, ranking of causes of death, and composition ratio; the standardized mortality rate was calculated based on the data of the 2010 National Census Data. Results From 2014 to 2020, the average annual resident population of Hainan Province was 9 175 300, and average annual resident population at each of the eight monitoringp oints is 297 100, anaverage of 83 878 cumulative deaths were reported, the annual total mortality rate was 504.09/100 000, the standard mortality rate was 618.69/100 000. The standardized mortality rates of male and female were 806.18/100 000 and 444.36/100 000 respectively (P<0.01). The mortality rate of all age groups showed that the crude mortality rate of 0~<1 years old group showed a decreasing trend with the passage of time, and the crude mortality rate was significantly higher than that of other age groups. From the age of 20, with the increase of age, the overall crude mortality rate of residents keeps increasing. The crude death rate increases rapidly after the age of 65, and peaks especially after the age of 85. The leading causes of death were circulatory diseases, tumors and respiratory diseases. From 2014 to 2020, the mortality rate of circulatory diseases and tumors, the two main causes of death, was more than 100/100 000. Conclusion Chronic non-communicable diseases are still the first cause of death among permanent residents in Hainan Province. Targeted intervention and treatment of chronic non-communicable diseases is beneficial to reduce their mortality.

7.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 221-228, 2022.
Article in English | WPRIM | ID: wpr-929255

ABSTRACT

Four new prenylflavonoid glycosides, namely koreanoside H-K (1-4), together with eleven known ones (5-15) were isolated from the leaves of Epimedium koreanum Nakai. Their structures were elucidated by 1D NMR, 2D NMR, HR-ESI-MS, IR and UV. The identification of the sugar moieties was carried out by means of acid hydrolysis and HPLC analysis of their derivatives. It is worth noting that compound 3 and compound 4 were elucidated to contain fucose and quinovose moieties, which were two extremely rare sugar units from the genus Epimedium. The anti-pulmonary fibrosis activity of the new compounds was evaluated using A549 cell line. Compounds 1, 2 and 4 showed significant anti-pulmonary fibrosis activities.


Subject(s)
Chromatography, High Pressure Liquid , Epimedium/chemistry , Glycosides/pharmacology , Plant Extracts/pharmacology , Plant Leaves/chemistry
8.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 648-655, 2021.
Article in English | WPRIM | ID: wpr-888794

ABSTRACT

Ocotillol (OT)-type ginsenosides, one subtype of ginsenosides, consist of a dammarane skeleton and a tetrahydrofuran ring. Most naturally-occurring OT-type ginsenosides exist in Panax species, particularly in Panax quinquefolius, which may be attributed to the warm and humid climate of its native areas. Till now, merely 28 types of naturally-occurring OT-type ginsenosides have been isolated. In contrast, semi-synthesized OT-type ginsenosides are attracted considerable attentions. These ginsenosides can be obtained through oxidation and cyclization of side chains of dammarane-type ginsenosides, and other methods, which may change their physical and chemical properties and further improve their bioavailabilities. It is also notable that the pharmacological activities of ginsenosides are closely related to the stereoisomers caused by the configuration at C-20. Semi-synthesis of OT-type ginsenosides can facilitate our understanding of the biosynthesis, transformation and metabolism of OT-type ginsenosides in the body. This review will systematically summarize the research progress on naturally-occurring and semi-synthetic OT-type ginsenosides, which provides a theoretical basis for their bioactivity-guided research.

9.
Acta Pharmaceutica Sinica ; (12): 2419-2425, 2021.
Article in Chinese | WPRIM | ID: wpr-886966

ABSTRACT

italic>α-Glucosidase inhibitors play an important role in the treatment of diabetes. This study established a high-resolution bioassay profiling platform for rapidly screening α-glucosidase inhibitors in natural product extracts. Five α-glucosidase inhibitors were identified from Malus hupehensis, namely, 3-hydroxyphloridzin, quercetin-3-O-β-D-glucopyranoside, phloridzin, avicularin and quercitrin. The establishment and successful application of this platform provides a powerful tool for the efficient discovery of anti-diabetic active ingredients in complex systems.

10.
China Journal of Chinese Materia Medica ; (24): 2079-2083, 2021.
Article in Chinese | WPRIM | ID: wpr-879133

ABSTRACT

Nine secondary metabolites(S)-5-hydroxy-4-methylchroman-2-one(1), 4-methoxynaphthalene-1,5-diol(2), 8-methoxynaphthalene-1,7-diol(3), 1,8-dimethoxynaphthalene(4),(2R,4S)-2,3-dihydro-2-methyl-benzopyran-4,5-diol(5),(2R,4R)-3,4-dihydro-4-methoxy-2-methyl-2H-1-benzopyran-5-ol(6), 7-O-α-D-ribosyl-2,3-dihydro-5-hydroxy-2-methyl-chromen-4-one(7),(R)-3-methoxyl-1-(2,6-dihydroxyphenyl)-butan-1-one(8) and helicascolide A(9) were isolated from endophytic fungus Cladosporium sp. JJM22 by using column chromatographies of silica gel and ODS, and semi-preparative HPLC. Their structures were analyzed on the basis of spectroscopic and chemical data, especially NMR and MS. All isolated compounds were evaluated for their anti-inflammatory activities by examining the inhibitory activities on nitric oxide(NO) production induced by lipopolysaccharide in mouse macrophage RAW264.7 cells in vitro. Compounds 2-4 showed inhibitory activities.


Subject(s)
Animals , Mice , Benzopyrans , Cladosporium , Fungi , Molecular Structure , Rhizophoraceae
11.
West China Journal of Stomatology ; (6): 195-202, 2021.
Article in Chinese | WPRIM | ID: wpr-878430

ABSTRACT

OBJECTIVES@#This study was performed to review the efficacy of curcumin in the treatment of oral submucous fibrosis systematically.@*METHODS@#We searched seven databases, including Web of Science, PubMed, EBSCO, The Cochrane Library, CNKI, WanFang Data, and VIP, to obtain randomized controlled trials related to the treatment of oral submucous fibrosis by curcumin. Each database was searched from inception to 30 June 2019. RevMan 5.3 software was used for the meta-analysis.@*RESULTS@#Six randomized controlled trials involving 350 patients were included in this study. Meta-analysis showed that curcumin can increase the maximal mouth opening and improve burning sensation compared with placebo treatment. Curcumin was not as effective as the controls in achieving maximal mouth opening after 1 month of treatment. However, no statistically significant difference was observed between the treatments from 2 months to 6 months. Curcumin significantly improved burning sensation compared with the controls after 3 months of treatment. No statistically significant diffe-rence in burning sensation was observed between the curcumin and control groups after 1, 2, and 6 months of treatment.@*CONCLUSIONS@#The current evidence shows that curcumin is an effective treatment for improving maximal mouth opening and burning sensation in patients with oral submucous fibrosis. Given the limited number and low quality of the included studies, however, more high-quality studies are needed to verify these findings.


Subject(s)
Humans , Curcumin , Databases, Factual , Oral Submucous Fibrosis/drug therapy , Randomized Controlled Trials as Topic , Treatment Outcome
12.
Chinese Journal of Experimental Traditional Medical Formulae ; (24): 13-23, 2021.
Article in Chinese | WPRIM | ID: wpr-906388

ABSTRACT

Huaihuasan, first recorded in Puji Benshifang by XU Shu-wei from the Southern Song dynasty, consists of four herbs, namely Sophorae Flos (fried), Platycladi Cacumen (smashed with pestle and baked), Schizonepetae Spica, and Aurantii Fructus (cut into pieces after the removal of pulp and then fried yellow with wheat bran). At present, Huaihuasan and its modified formulas vary in clinical usages and dosages, and the resulting outcomes have been investigated. However, there are few reviews uncovering its historical evolution. On this basis, this review systematically combed and verified the historical evolution, dose conversion between ancient and modern times, efficacy, and indications of Huaihuasan, as well as the origin and processing of the contained herbs. The findings have demonstrated that Huaihuasan is composed of four herbs, with the original plants and medicinal parts basically the same as those recorded in the 2020 edition of Chinese Pharmacopoeia. Sophorae Flos refers to the dried flower and bud of Sophora japonica in family Leguminosae, Platycladi Cacumen the dried branch and leaf of Platycladus orientalis in family Cupressaceae, Schizonepetae Spica the dried flower spike of Schizonepeta tenuifolia in family Labiatae, and Aurantii Fructus the dried immature fruit of Citrus aurantium in family Rutaceae or its cultivated varieties. On account of the efficacy in clearing intestine, stopping bleeding, dispersing wind, and moving Qi, Huaihuasan has been mainly used to treat intestinal diseases such as bloody defecation and perianal abscess. In modern clinical practice, it is mainly applicable to patients with hematochezia and bleeding due to internal hemorrhoid, ulcerative colitis, or anal fissure. It was suggested that the raw medicinal materials should be decocted and processed according to the methods described in the 2020 edition of Chinese Pharmacopoeia. Following the conversion formula of one Qian=4 g, this paper determined the dosages of Sophorae Flos (fried), Platycladi Cacumen (smashed with pestle and baked), Schizonepetae Spica, and Aurantii Fructus (cut into pieces after the removal of pulp and then fried yellow with wheat bran) all to be 2 g, with the total dosage being 8 g. Such comprehensive analysis based on ancient books and modern literature has provided a more scientific reference for the clinical application, research, and development of this classical formula.

13.
Chinese Journal of Nephrology ; (12): 359-365, 2020.
Article in Chinese | WPRIM | ID: wpr-870974

ABSTRACT

Objective:To investigate the incidence of acute kidney injury (AKI) following cardiac surgery and related risk factors in 4 878 patients.Methods:The information from patients who underwent cardiac surgery through March 2015 to October 2015 was collected retrospectively from the electronic database of Beijing Anzhen Hospital. A total of 4 878 patients were divided into AKI group and non-AKI group according to whether AKI occurred within 7 days after cardiac surgery. The incidence of AKI was calculated, and the AKI incidence in different types of cardiac surgeries were compared. Clinical data such as baseline clinical information, operation information, comorbidity, hospital stay time, life ability score in discharge from the hospital, and so on, were compared between AKI group and the non-AKI group using univariate analysis. Risk factors for AKI following cardiac surgery were analyzed using the binary multivariate logistic regression.Results:A total of 933 patients suffered from AKI (19.1%) following cardiac surgery. The time of stay in the hospital was longer in AKI group than that in the non-AKI group [(14.4±8.9) vs (13.7±7.7) d, P<0.05)]. The incidence of AKI in different types of cardiac surgeries varied significantly ( P<0.001). The logistic regression analysis showed that male, diabetes, hypertension, the elevated basic serum creatinine, cardiac dysfunction (NYHA grade≥Ⅲ), cardiopulmonary bypass, a combination of operations≥3, the rethoracotomy exploration and hemostasia, and using an invasive ventilator for over 96 hours were the independent risk factors for the AKI following cardiac surgery (all P<0.05), and the odds ratio (95% confidence interval) were 1.81(1.46-2.24), 1.29(1.03-1.62), 5.85(4.73-7.22), 1.81(1.36-2.40), 4.49(3.60-5.60), 1.84(1.49-2.27), 23.24(18.25-29.59), 2.34(1.45-3.77) and 1.94(1.09-3.43) respectively. Conclusions:The incidence of AKI after cardiac surgery in Beijing Anzhen Hospital is 19.1%. AKI following cardiac surgery prolongs the time of stay in the hospital. Independent risk factors for AKI following cardiac surgery are multiple, and one of the most critical factors is a combination of operations≥3.

14.
Chinese Journal of Practical Nursing ; (36): 1426-1429, 2019.
Article in Chinese | WPRIM | ID: wpr-752659

ABSTRACT

Objective To investigate and analyze the humane care quality and behavior of clinical nurses in informed consent, and provide theoretical basis about how to implement humane care in clinical nursing practice. Methods Using Nurse Humanities Care Quality Table which developed by Liu Yuxi , and Nurse Informed Consent Humanistic Behavior Self-rating Scale witch designed by self, To investigate 110 clinical nurses who picked out by hierarchical random sampling. Results In the humanistic care quality assessment, the score of the ability was the lowest in nurses′humanistic care quality, the average score (23.06 ± 1.72) accounted for 65.88% of the total score (35). the score of knowledge dimension was positively correlated with age and working years (r=0.339, 0.294, both P<0.01). the score of perceived dimension was positively correlated with age (r=0.250, P<0.01). In the humanistic care behavior assessment of informed consent, the score of the communication and emergency ability dimension were the lowest. The average score (21.65±1.93) accounted for 86.60% of the total score (25). The marital status of the clinic nurses was negatively correlated with respect and care (r=-0.305, P<0.01). The humanistic knowledge was positively correlated with support and communication and emergency response (r=0.422, 0.371, both P<0.01), the concept was positively correlated with respect and care, support and security (r=0.640, 0.587, both P<0.01). Conclusions The quality of nurses′humanistic care is significantly related to the humanistic care behavior in informed consent. It should improve the quality of nurses′humanistic care for cultivating humanistic care behavior in nursing practice.

15.
Chinese Acupuncture & Moxibustion ; (12): 637-642, 2019.
Article in Chinese | WPRIM | ID: wpr-775853

ABSTRACT

OBJECTIVE@#To explore the effect of electrical stimulation at auricular points (EAS) combined with sound masking on the expression of cAMP-response element binding protein (CREB), brain-derived neurotrophic factor (BDNF) and tyrosine receptor kinase B (TrkB) in the auditory cortex of tinnitus rats.@*METHODS@#A total of 27 adult male SD rats were randomly divided into a control group, a model group and an EAS group. The rats in the model group and the EAS group were intervened with intraperitoneal injection of sodium salicylate to induce tinnitus model, while the rats in the control group were intervened with injection of 0.9% NaCl solution. After the model was successfully established, the rats in the EAS group were treated with electrical stimulation at "Shenmen" (TF) and "Yidan" (CO), combined with sound masking; the treatment was given once a day for 15 days. The gap prepulse inhibition of acoustic startle (GPIAS) and prepulse inhibition (PPI) testing were performed using the acoustic startle reflex starter package for rats. The expression of BDNF, TrkB, CREB and p-CREB in the auditory cortex of each group were measured with Western Blot analysis.@*RESULTS@#① Compared with the control group, the GPIAS values in 12 kHz, 16 kHz, 20 kHz and 28 kHz were significantly decreased in the model group (all 0.05).@*CONCLUSION@#EAS could improve the GPIAS values of high-frequency background sound in tinnitus rats, which may be related with the upregulation of the BDNF/TrkB/CREB signaling pathway in the auditory cortex, leading to the reversion of the maladaptive plasticity.


Subject(s)
Animals , Male , Rats , Acupuncture Points , Auditory Cortex , Brain-Derived Neurotrophic Factor , Metabolism , Cyclic AMP Response Element-Binding Protein , Metabolism , Electric Stimulation , Rats, Sprague-Dawley , Receptor, trkB , Metabolism , Tinnitus , Metabolism , Therapeutics
16.
China Pharmacy ; (12): 2497-2502, 2019.
Article in Chinese | WPRIM | ID: wpr-817266

ABSTRACT

OBJECTIVE: To establish a determination method for the concentration of cajanonic acid A (CAA) in liver microsome incubation system, and to compare the metabolism characteristics of it in different species of liver microsomes. METHODS: CAA was dissolved in liver microsome incubation system of rat, Beagle dog and human initiated by reduced nicotinamide adenine dinucleotide phosphate (NADPH), and was incubated in water at 37 ℃. The reaction was terminated with acetonitrile at 0, 5, 10, 15, 30, 45 and 60 min, respectively. Using genistein as internal standard, the concentration of CAA in  different incubation systems was determined by UPLC-MS/MS. The determination was performed on Waters BEH C18 column with mobile phase consisted of water (containing 0.1% formic acid)-acetonitrile (containing 0.1% formic acid) (45 ∶ 55, V/V) at the flow rate of 0.25 mL/min. The column temperature was 30 ℃, and the sample size was 2 μL. The electrospray ionization source was used to the select reaction monitoring mode for negative ion scanning. The ion pairs for quantitative analysis were m/z 353.14→309.11 (CAA), m/z 269.86→224.11 (internal standard) respectively. The residual percentage and enzymatic kinetic parameters of CAA in different incubation systems were calculated according to the mass concentration of CAA at 0 min. RESULTS: The linear range of CAA was 0.05-20 μg/mL; the limit of quanti- tation was 0.05 μg/mL, and the lowest detection limit was 0.01 μg/mL. RSDs of intra-day and inter-day were lower than 10%; relative errors ranged -4.83%-8.94%; extraction method and matrix effect did not affect the determination of the substance to be measured. At 60 min of incubation, residual percentages of CAA in rat, Beagle dog and human liver microsomes were(62.79±9.99)%,(64.07±11.59)%,(96.66±5.71)%, respectively. The half-life period (72.19, 68.61 min) of CAA in rat and Beagle dog liver microsomes were significantly shorter than human liver microsome (364.74 min). The clearance rates [0.019 2, 0.020 2 mL/(min·mg)] were significantly higher than human liver microsome [0.003 8 mL/(min·mg)] (P<0.05). CONCLUSIONS: Established UPLC-MS/MS method is simple, rapid, specific and sensitive, and can be used for the determination of CAA concentration in liver microsome incubation system and the study of metabolism stability in vitro. The stability of CAA metabolism in rat and Beagle dog liver microsomes are poorer than human liver microsome.

17.
China Journal of Chinese Materia Medica ; (24): 249-260, 2019.
Article in Chinese | WPRIM | ID: wpr-777446

ABSTRACT

Panax japonicus( PJ) is a valuable medicinal plant belonging to the genus Panax of Araliaceae,the recumbent rhizome of which is widely used in clinic therapy,healthcare products and as cosmetic additives with functions of dissipating stasis,reducing swelling,stanching bleeding,and reinforcing deficiency,etc. PJ contains abundant levels of oleanane-and dammarane-type triterpene saponins,which are considered as the material basis for exerting pharmacodynamic action. Based on the previous researches,more than110 triterpene saponins have been reported from PJ. These triterpene saponins were summarized in this review,and could be classified into dammarenediol Ⅱ,protopanaxadiol,protopanaxatiol,ocotillol,oleanolic acid,ursolic acid and miscellaneous subtypes,according to their molecular skeletons in biosynthesis processes. Further more,the structural features of these triterpene saponins in the seven different subtypes,together with their~(13)C-NMR spectroscopic characteristics were described,hoping to provide available information for chemical diversity research of PJ.


Subject(s)
Magnetic Resonance Spectroscopy , Panax , Chemistry , Plants, Medicinal , Chemistry , Saponins , Chemistry , Triterpenes , Chemistry
18.
Acta Pharmaceutica Sinica ; (12): 761-767, 2019.
Article in Chinese | WPRIM | ID: wpr-780209

ABSTRACT

Among various technologies used in drug design and discovery, deep learning is still in its infancy. Recently, deep learning approaches have been rapidly developed and applied to address various problems in drug discovery, including generation of virtual compound library, prediction of compound activity, metabolism and toxicity, and prediction of organic synthesis routes. Compared with the traditional machine learning methods, the prediction power of deep learning did not show significant improvement. However, proactively learning and automatically feature extraction bring advantages for deep learning approaches. Compared to first principle-based computational chemistry methods, deep learning can not be generalized because it depends on large-scale and high-quality annotated data sets. But its molecular representation with single-atom atomic environment vectors could be useful for computational chemists. As an emerging technology, deep learning, especially the unsupervised learning method that does not rely on large datasets with labels, is gradually improving. It is expected that someday deep learning method will become practical for drug discovery.

19.
Chinese Journal of Practical Nursing ; (36): 1425-1428, 2019.
Article in Chinese | WPRIM | ID: wpr-802993

ABSTRACT

Objective@#To investigate and analyze the humane care quality and behavior of clinical nurses in informed consent, and provide theoretical basis about how to implement humane care in clinical nursing practice.@*Methods@#Using Nurse Humanities Care Quality Table which developed by Liu Yuxi, and Nurse Informed Consent Humanistic Behavior Self-rating Scale witch designed by self, To investigate 110 clinical nurses who picked out by hierarchical random sampling.@*Results@#In the humanistic care quality assessment, the score of the ability was the lowest in nurses′ humanistic care quality, the average score (23.06±1.72) accounted for 65.88% of the total score (35). the score of knowledge dimension was positively correlated with age and working years (r=0.339, 0.294, both P<0.01). the score of perceived dimension was positively correlated with age (r=0.250, P<0.01). In the humanistic care behavior assessment of informed consent, the score of the communication and emergency ability dimension were the lowest. The average score (21.65±1.93) accounted for 86.60% of the total score (25). The marital status of the clinic nurses was negatively correlated with respect and care (r=-0.305, P<0.01). The humanistic knowledge was positively correlated with support and communication and emergency response (r=0.422, 0.371, both P <0.01), the concept was positively correlated with respect and care, support and security (r=0.640, 0.587, both P<0.01).@*Conclusions@#The quality of nurses′ humanistic care is significantly related to the humanistic care behavior in informed consent. It should improve the quality of nurses′ humanistic care for cultivating humanistic care behavior in nursing practice.

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Chinese Journal of Experimental Traditional Medical Formulae ; (24): 112-117, 2019.
Article in Chinese | WPRIM | ID: wpr-801840

ABSTRACT

Objective: Cimicifuga dahurica (Ranunculaceae) has many bioactivities. Although there have been intensive studies for saponin constituents at present, only a few studies have focused on for chemical constituents of phenolic acid. To define the phenolic acid constituents,C. dahurica was separated, and the structures of the compounds were identified,in the expectation of providing a basis for its further development,utilization and quality control. Method: A total of 16 kg rhizome of C. dahurica was extracted with 70%ethanol for three times by heating reflux. These 3 extracts were decompressed and concentrated,and then dissolved in water. Then the solvent was successively extracted with petroleum ether,ethyl acetate(EtOAc) and n-butanol(BuOH). The components of EtOAc and water extract were isolated and purified by macroporous,silica gel,ODS,Sephadex LH-20 column chromatography,preparative HPLC and recrystallization,and the structures were identified by nuclear magnetic resonance(NMR) and physicochemical analysis etc. Result: Fifteen compounds were isolated from the ethyl acetate and water fractions,and identified as cimicifugic G (1),2-caffeoyl piscidic acid (2),cimicifugic A (3),cimicifugic B (4),caffeic acid 3-O-β-D-glucopyranoside (5),cimicifugic E (6),cimicifugic F (7),trans-ferulic acid 4-O-β-D-glucopyranoside (8),carboxymethyl isoferulate (9),3,4-dimethoxycinnamic acid (10),ethyl ferulate (11),caffeic ester glucoside (12),shomaside A (13),isoferulic acid (14),caffeic acid (15). Conclusion: Compounds 1-7,9-10,13 were isolated from the plant for the first time.

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