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Article in Chinese | WPRIM | ID: wpr-906159


Objective:To study the material basis and potential molecular mechanism of Epimedii Folium against osteoporosis. Method:The chemical components in 14 batches of Epimedii Folium were analyzed by ultra-performance liquid chromatography-quadrupole-time of flight-tandem mass spectrometry (UPLC-Q-TOF-MS/MS). With the activity of alkaline phosphatase (ALP) as the pharmacodynamic index,the partial least squares regression analysis (PLSR) was conducted to establish a model uncovering the spectrum-effect relationship between UPLC-Q-TOF-MS/MS spectral peak and ALP activity and screen the active components against osteoporosis. Online databases such as the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP),Comparative Toxicogenomics Database (CTD),Database for Annotation,Visualization,and Integrated Discovery (DAVID) and Cytoscape 3.6.1 were employed to predict the possible mechanism of action of Epimedii Folium against osteoporosis. Result:A total of 61 peaks and 56 compounds were identified by UPLC-Q-TOF-MS/MS. PLSR showed that icariin,baohuoside Ⅰ,epimedin A,sagittatoside A,and baohuoside Ⅱ might be the active components for Epimedii Folium to inhibit osteoporosis considering their strong correlation with ALP activity. As revealed by the network pharmacological analysis of the five components mentioned above,Epimedii Folium<italic> </italic>mainly regulated seven targets such as tumor necrosis factor (TNF),androgen receptor (AR),and estrogen receptor 1 (ESR1) and eight key pathways like endocrine and other factor-regulated calcium reabsorption,vascular endothelial growth factor (VEGF) signaling pathway,and transient receptor potential (TRP) channels to exert its anti-osteoporosis effect. Conclusion:The exploration of material basis and potential molecular mechanism of Epimedii Folium against osteoporosis based on UPLC-Q-TOF-MS/MS,spectrum-effect relationship,and network pharmacology has provided an experimental basis for the scientific explanation and clinical application of Epimedii Folium in treating osteoporosis.

Article in Chinese | WPRIM | ID: wpr-846595


Objective: To compare the effects of different drying methods on the quality of Trichosanthis Pericarpium, and screen the suitable drying methods for its modern drying processing. Methods: The fresh Trichosanthis Pericarpium collected from Anhui were processed by traditional and modern drying processing methods [hot air drying (40, 50, 60, 70 ℃), microwave vacuum drying (40, 50, 60, 70 ℃; vacuum -0.08 MPa), short-wave infrared drying (50, 60, 70 ℃), vacuum -80 ℃ lyophilization, traditional solar drying, shadow drying]. Combined with the appearance of the samples after drying, the composition and content of the 40 resource chemical compositions [five kinds of flavonoids (rutin, luteoloside, apigenin-7-O-glucuronide, apigenin, tangeretin), three kinds of triterpenoids (cucurbitacin D, cucurbitacin B, cucurbitacin E)] and nutritional nourishing ingredients [two kinds of saccharides (glucose, fructose), eighteen kinds of amino acids (phenylalanine, L-leucine, iso-leucine, L-tryptophan, γ-aminobutyric acid, L-methionine, L-valine, L-proline, L-tyrosine, trans-4-hydroxy-L-proline, L-threonine, L-glutamic acid, L-glutamine, L-serine, L-asparagine, L-citrulline, L-arginine, L-lysine), and twelve kinds of nucleosides (thymidine, 2’-deoxyuridine, adenine, uridine, adenosine, 2’-deoxyinosine, inosine, cytosine, guanine, 2’-deoxyguanosine, cytidine, guanosine)] were evaluated for comprehensively evaluating the quality of the different samples. The best modern drying method for Trichosanthis Pericarpium was preferred by principal component analysis. Results: Among different dry samples, the content of medicinal ingredients and nutrient nourishing ingredients varied greatly, among which fructose and glucose content ranged from 9.78% to 21.32% and 4.46% to 15.63%, respectively. Samples of 70 ℃ microwave vacuum drying had the highest total amount of flavonoids and tetracyclic triterpenoids, while those of 40 ℃ hot air drying treatment were the lowest. Through comprehensive evaluation of 14 kinds of Trichosanthis Pericarpium samples obtained by different drying methods, it was found that samples of 70 ℃ hot air drying, 70 ℃ short-wave infrared drying, vacuum -80 ℃ lyophilization, 50 ℃ microwave vacuum drying and 60 ℃ hot air drying were better than the traditional solar drying. Conclusion: Combined with the appearance of the medicinal properties, color, texture, drying time and functional ingredients, it was recommended that 70 ℃ hot air drying method was the preferred conditions for production based on the current state of the equipment of company. Based on the development of new equipment in the future, short-wave infrared 70 ℃ drying can be used as the development direction of Trichosanthis Pericarpium. The study provided reference for the standardization and quality characteristics of production of Trichosanthis Pericarpium.

Article in Chinese | WPRIM | ID: wpr-774604


To investigate the effects of essential oil from three kinds of pungent herbs,namely Menthae Haplocalycis Herba,Atractylodis Rhizoma and Cnidii Fructus,on the transdermal absorption in vitro of alkaloids from Sophorae Flavescentis Radix. The modified vertical Franz diffusion cell was used to conduct a transdermal experiment in vitro with the isolated abdominal skin of the SD rats as the transdermal absorption barrier. The effects of such three kinds of pungent essential oil on percutaneous absorption of alkaloids from Sophorae Flavescentis Radix were investigated by determining the content of 6 alkaloids( oxymatrine,oxysophocarpine,N-methylcytisine,sophoridine,matrine,and sophocarpidine) in the transdermal acceptor with ultra-performance liquid chromatography-triple quadruple mass spectrometry( UPLC-TQ-MS) technique simultaneously. With enhancement ratio( ER) as the index,their effects on promoting penetration was as follows: 1% Atractylodis Rhizoma oil > 1% Cnidii Fructus oil > 3% Azone ≈ 3% Atractylodis Rhizoma oil > 5%Atractylodis Rhizoma oil > 3% Cnidii Fructus oil ≈ 5% Cnidii Fructus oil > 3% Menthae Haplocalycis Herba oil > 5% Menthae Haplocalycis Herba oil > 1% Menthae Haplocalycis Herba oil > Blank. The results showed that these three kinds of pungent essential oil could be used as enhancers for alkaloids of Sophorae Flavescentis Radix,providing scientific guidance for improving percutaneous absorption of alkaloids from Sophorae Flavescentis Radix.

Alkaloids , Metabolism , Animals , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Metabolism , Oils, Volatile , Pharmacology , Plant Roots , Chemistry , Rats , Rats, Sprague-Dawley , Skin Absorption , Sophora , Chemistry
Acta Pharmaceutica Sinica ; (12): 1148-1155, 2018.
Article in Chinese | WPRIM | ID: wpr-779983


This study was designed to determine the metabolites of Renduining injection in rats. The ultra-high performance liquid chromatography-LTQ Orbitrap mass spectrometric (UHPLC-LTQ-Orbitrap-MS) and mass defect filter techniques were applied to analyze the metabolites of Reduning injection in rat plasma, bile, urine and feces. As a result, we determined 14 metabolites of geniposide, including oxidation, dehydration, hydroxymethylene loss, hydrolysis, ring-opened, cysteine conjugation and glucuronidation conjugation of aglycone; 9 metabolites of geniposidic acid, consisting of dehydration, ring-opened, double-bond reduction and cysteine conjugation; 6 metabolites of secoxylogain including hydrolysis, hydroxymethylene loss, hydroxylation and ethylation; 12 metabolites of chlorogenic acid, containing decarboxylation, hydrolysis, methylation, acetylation, cysteinylglycine conjugation and glutathione conjugation. It provided information for the therapeutic effect of Reduning in vivo.

Article in Chinese | WPRIM | ID: wpr-230953


This study established a rapid UPLC-TQ-MS/MS method for determination of eight active ingredients in Lilium lancifolium. The contents range of regaloside E, F, C and B are as follows: 0.604 0×10⁻¹-18.62×10⁻¹, 0.680 0×10⁻²-44.75×10⁻², 0.700 0×10⁻³-29.65×10⁻¹, 0.170 0×10⁻¹-4.724 mg•g⁻¹; the contents of chlorogenic acid, caffeic acid, protocatechualdehyde and ferulic acid, within the range of 6.827×10⁻³-16.07×10⁻³, 0.011 1×10⁻³-79.71×10⁻³, 0.593 7×10⁻³-2.962×10⁻³, 2.606×10⁻²-45.89×10⁻² mg•g⁻¹, respectively. According to PCA (principal components analysis) plotting, 35 batches can be divided into two categories, namely Anhui Huoshan and Hunan Longshan. The main different elements between these two categories are caffeic acid and ferulic acid according to the VIP (variable importance in the projection) points figure. Based on comprehensive principal component values, there are eight batches of L. lancifolium from Huoshan among the comprehensive ranking of ten. The UPLC-TQ-MS method for simultaneous analysis of eight active ingredients is accurate, efficient and convenient. This result can provide scientific basis for quality control of L. lancifolium.

Article in Chinese | WPRIM | ID: wpr-231011


This study intends to explore the potential resource-orientedutilization value of the flower of Sophora flavescents by analyzing alkaloids and flavonoids in the flower of S. flavescens from Shanxi province. This study established a rapid UPLC-TQ-MS/MS method that is used for determination of seven alkaloids and seven flavonoids in the flower of S.flavescens. The different florescences all have the seven detected alkaloids such as cytisine, oxy-matrine, oxy-sophocarpine, sophoridine, N-methylcytisine, matrine, sophocarpine.The total contents of detected alkaloids are as follows: flower buds 1.47%, primal flowers 1.34%, full bloomed flowers 1.17%, faded flowers 1.01%. The top three contents of alkaloids are N-methylcytisine , oxy-sophocarpine and oxymatrine, accounting for about 83% of the total amount of detected alkaloids. All the samples in different florescences have the seven detected flavonoids such as rutin, luteolin, quercetin, isoquercitrin, trifolirhizin, kurarinone, and kushenol I. The total contents of detected alkaloids are as follows: flower buds 495.2 μg•g⁻¹, primal flowers 313.7 μg•g⁻¹, faded flowers 224.2 μg•g⁻¹, full bloomed flowers 193.0 μg•g⁻¹. The content of luteolinis relatively higher than other detected flavonoids, accounting for about 89%-94% of the total amount of detected flavonoids. The results indicated that the flower of S.flavescens could be an important material resource to obtain the resourceful alkaloids. This result can provide scientific basis for resource-oriented utilization and industrial development of the flower of S. flavescens.