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OBJECTIVE@#To investigate the spectrum-effect relationship between the total anthraquinone extract of Cassia seeds and fluorouracil (5-Fu)-induced liver injury in mice and identify the effective components in the extract.@*METHODS@#A mouse model of liver injury was established by intraperitoneal injection of 5-Fu, with bifendate as the positive control. The serum levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) and myeloperoxidase (MPO), superoxide dismutase (SOD) and total antioxidant capacity (T-AOC) in the liver tissue were detected to investigate the effect of the total anthraquinone extract of Cassia seeds (0.4, 0.8 and 1.6 g/kg) on liver injury induced by 5-Fu. HPLC fingerprints of 10 batches of the total anthraquinone extracts were established to analyze the spectrum- effectiveness of the extract against 5- Fu- induced liver injury in mice and screen the effective components using the grey correlation method.@*RESULTS@#The 5- Fu- treated mice showed significant differences in liver function parameters from the normal control mice (P < 0.05), suggesting successful modelling. Compared with those in the model group, serum ALT and AST activities were decreased, SOD and T- AOC activities significantly increased, and MPO level was significantly lowered in the mice treated with the total anthraquinone extract (all P < 0.05). HPLC fingerprints of the 31 components in the total anthraquinone extract of Cassia seeds showed good correlations with the potency index of 5-Fu-induced liver injury but with varying correlation strengths. The top 15 components with known correlations included aurantio-obtusina (peak 6), rhein (peak 11), emodin (peak 22), chrysophanol (peak 29) and physcion (peak 30).@*CONCLUSION@#The effective components in the total anthraquinone extract of Cassia seeds, including aurantio-obtusina, rhein, emodin, chrysophanol, and physcion, are coordinated to produce protective effects against 5-Fu-induced liver injury in mice.
Subject(s)
Animals , Mice , Emodin , Cassia , Chemical and Drug Induced Liver Injury, Chronic , Anthraquinones , Antioxidants , Fluorouracil/adverse effects , Plant Extracts/pharmacologyABSTRACT
OBJECTIVE@#To study the plasma concentration and pharmacokinetics of 3, 29-Dibenzoyl Karounitriol (3, 29-DK) from sustained- release pellets and extracts of Trichosanthes at different time points in rats using high-performance liquid chromatography- tandem mass spectrometry (LC-MS/MS).@*METHODS@#Healthy male SD rats were given a single gavage of Trichosanthes sustained-release pellets or Trichosanthes extract, and orbital blood samples were taken at different time points within 48 h after drug administration in the pellet group and within 5 h in Trichosanthes extract group for determination of the plasma concentrations of 3, 29-DK using LC-MS/MS. The standard curve of 3, 29-DK content was established, and the specificity, minimum detection limit, precision and accuracy, extraction recovery, stability and matrix effect of LC-MS/MS analysis were assessed. The mean plasms levels of 3, 29-DK at different time points after the drug administration were determined and its pharmacokinetic parameters were calculated using Das 2.0 software.@*RESULTS@#LC-MS/MS analysis showed a good linearity of 3, 29-DK concentration within the range of 0.5-32 ng/mL, and the results of methodological validation confirmed the validity of this method for biological sample determination. Trichosanthes sustained-release pellets and Trichosanthes extract showed significant differences in their AUC, AUC, MRT, MRT, t and T of 3, 29-DK after administration in rats ( < 0.05).@*CONCLUSIONS@#Trichosanthes sustained-release pellets are capable of sustained-release of 3, 29-DK in rats, and thus provides a basis for the study of new dosage forms of Trichosanthes.
Subject(s)
Animals , Male , Rats , Chromatography, High Pressure Liquid , Delayed-Action Preparations , Rats, Sprague-Dawley , Reproducibility of Results , Tandem Mass Spectrometry , TrichosanthesABSTRACT
OBJECTIVE@#To explore the target, signaling pathways and their biological functions of Decoction in the treatment of COVID-19 based on network pharmacology and molecular docking technology.@*METHODS@#The active components and target proteins in 21 drugs such as and in decoction were analyzed, and the signaling pathways and biological functions of the target proteins common with COVID-19 were screened by using TCMSP, Swiss Target Prediction, CooLGeN, GeneCards, DAVID and other databases. The network diagram of decoction was constructed using Gephi software.@*RESULTS@#We identified 163 active ingredients, including MOL004798, MOL000519, MOL004824, MOL000554, MOL010428, and MOL013443, from 18 drugs in decoction (such as , , , , and ). These ingredients activate renin-angiotensin system signaling pathway and apoptosis signaling pathway by regulating 10 protein targets (ACE, ACE2, AGTR1, FURIN, TNF, CASP3, CASP6, DPP4, MCL1 and POLD1) to execute 42 biological functions such as renin-angiotensin regulation of blood volume and systemic arterial blood pressure to treat COVID-19. The results of preliminary molecular docking showed that MOL000519 (from ), MOL000554 (from ), MOL004798 (from ), MOL004824 (from ), MOL010428 (from ), and MOL013443 (from ) had good affinity with SARS-CoV-2 3CL hydrolase to form complexes with stable conformations and high binding activity (binding energy ≤- 5 kJ/mol).@*CONCLUSIONS@# decoction can treat COVID-19 through its multiple medicinal ingredients that have multiple targets and involve multiple signaling pathways for different biological functions. Our finding provides reference for further investigation into the pharmacological mechanism of decoction in treating COVID-19.
Subject(s)
Humans , Betacoronavirus , Coronavirus Infections , Drug Therapy , Drugs, Chinese Herbal , Molecular Docking Simulation , Pandemics , Pneumonia, Viral , Drug TherapyABSTRACT
OBJECTIVE@#To study the plasma concentration and pharmacokinetics of 3, 29-Dibenzoyl Karounitriol (3, 29-DK) from sustained- release pellets and extracts of Trichosanthes at different time points in rats using high-performance liquid chromatography- tandem mass spectrometry (LC-MS/MS).@*METHODS@#Healthy male SD rats were given a single gavage of Trichosanthes sustained-release pellets or Trichosanthes extract, and orbital blood samples were taken at different time points within 48 h after drug administration in the pellet group and within 5 h in Trichosanthes extract group for determination of the plasma concentrations of 3, 29-DK using LC-MS/MS. The standard curve of 3, 29-DK content was established, and the specificity, minimum detection limit, precision and accuracy, extraction recovery, stability and matrix effect of LC-MS/MS analysis were assessed. The mean plasms levels of 3, 29-DK at different time points after the drug administration were determined and its pharmacokinetic parameters were calculated using Das 2.0 software.@*RESULTS@#LC-MS/MS analysis showed a good linearity of 3, 29-DK concentration within the range of 0.5-32 ng/mL, and the results of methodological validation confirmed the validity of this method for biological sample determination. Trichosanthes sustained-release pellets and Trichosanthes extract showed significant differences in their AUC, AUC, MRT, MRT, t and T of 3, 29-DK after administration in rats ( < 0.05).@*CONCLUSIONS@#Trichosanthes sustained-release pellets are capable of sustained-release of 3, 29-DK in rats, and thus provides a basis for the study of new dosage forms of Trichosanthes.
Subject(s)
Animals , Male , Rats , Area Under Curve , Benzoates , Pharmacokinetics , Chromatography, Liquid , Delayed-Action Preparations , Rats, Sprague-Dawley , Reproducibility of Results , Tandem Mass Spectrometry , Trichosanthes , ChemistryABSTRACT
Objective To optimize the color conditions of spectrophotometric determination of total saponins in Fructus Trichosanthis. Methods Several factors affecting the content determination of total saponins in Fructus Trichosanthis were studied , including the color temperature,color time,5%vanillin-acetic acid dosage,as well as the amount of perchloric acid. The analysis con-ditions were optimized by Box-Behnken response surface method. Results The optimized conditions were:temperature 60℃,the col-or time 25 min,5%vanillin-acetic acid 0.1 ml and perchloric 0.6 ml. The color was stable and the determination results were accurate. Conclusion The color conditions determined by Box-Behnken response surface method can be used for content determination of total saponins in Fructus Trichosanthis.
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Objective To study the similarity of chemical fingerprints of different proportion of Gualoupi-Gualouzi and Fruc?tus Trichosanthis,so as to provide the theoretical basis for the reasonable proportion of Gualoupi-Gualouzi. Methods The HPLC fin?gerprints and the common patterns of 6 the proportion of the 6 kinds of compatibility(30:70,35:65,40:60,45:55,50:50 and 55:45)of Gualoupi-Gualouzi and Fructus Trichosanthis were established,and the similarity of chemical fingerprints of different compati?bility proportion of Gualoupi-Gualouzi and Fructus Trichosanthis between their common patterns were compared. Results Compared with the common pattern of Fructus Trichosanthis,the similarities of the common patterns of chemical fingerprints of the above 6 kinds of compatibility proportion of Gualoupi-Gualouzi were 0.8808 ± 0.0407,0.8930 ± 0.0236,0.8995 ± 0.0195,0.9033 ± 0.0190,0.9363 ± 0.0082 and 0.8904 ± 0.0144,respectively. Among them,Gualoupi-Gualouzi ratio of 50:50 had the highest similarity,and compared with other groups,the differences were statistically significant(P<0.05 or 0.01). Conclusion The optimum proportion of Gualoupi-Gualouzi can be determined by the fingerprint technology,which provides the theoretical basis for the reasonable proportion of Gualou?pi-Gualouzi.
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Objective To explore whether the basic principle of Fisher component analysis(FCA)can be used in the catego?ry analysis of Fructus Trichosanthis fruit and its processed products. Methods Their fingerprints were established by using HPLC-PDAD,and the standard fingerprints of them were obtained by digitizing with quercetin as the internal reference peak. Then,their chemical fingerprint information was extracted by FCA and classified by quality model,and the classification results were compared with those classified by principal component analysis and standard atlas analysis. Results Fructus Trichosanthis and its processed products can be accurately divided into two categories by FCA. Conclusion FCA can extract the implied chemical information in fin?gerprints,and analyze them accurately.
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Objective To verify the protective effects of Gualou Xiebai dropping pills(GX)on myocardial ischemia-reperfu?sion injury(MIRI)in rats. Methods After screening the qualified SPF rats were randomly divided into four groups,with 12 in each group. Sham-operated group and model group rats were respectively treated with normal saline,and rats in GX group and compound Danshen dropping pills group were given the corresponding dropping pills equivalent to 22.5 g/kg and 85.05 mg/kg of the crude herb,re?spectively. All groups were administered once a day for 7 successive days. One hour after the last administration,the MIRI models were produced by occluding the left coronary artery for 30 min and releasing the occlusion for 120 min. The changes in ST segment were observed,and the contents of creatine kinase-MB(CK-MB),cardiac troponin-T(CTNT)and myoglobin(MYO)in blood plas?ma were measured. The pathological changes in myocardial tissues were observed by optics and electric-microscope and the percentage of myocardial infarction was measured by detecting the content of Evan blue in myocardium. Results Compared to normal saline in the model group,GX had antagonism to ECG S-T segments elevation in rats with myocardial ischemia,while the contents of CK-MB, MYO,and CTNT in blood plasma declined significantly(P<0.05 or P<0.01);the disorder condition of myocardial cell fiber arrange?ment was improved,and edema between myocardial tissue and cells was relieved;the inflammatory cell infiltration and myocardial ne?crosis in cardiac allograft were significantly alleviated,and the percentage of myocardial infarction was decreased significantly(P<0.01). Conclusion GX may play an important protective role against the MIRI in rats.
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Objective To study the in situ intestinal absorption behaviors of 3,29-dibenzoyl-karounitriol(DK)in Gualou-Xiebai(GX)extract in rats. Methods A rat in situ single-pass perfusion model was used and the concentrations of the perfusate were determined by HPLC-PDAD to investigate the intestinal absorption site and mechanism. Results The main absorption site of DK in GX extract was jejunum,ileum and colon,and the absorption had no significant difference in the three different segments of rat intes?tine(P>0.05),but was significantly higher than that in duodenum(P0.05). Conclusion DK in GX extract could be absorbed in whole intestinal segment,with the best intestinal absorption site of jejunum,ileum and colon. Its absorbing mechanism may be related to passive diffusion.
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<p><b>OBJECTIVE</b>To investigate the principle and basis about the chromatographic fingerprint peak matching of Semen Cassiae by the asymptotic window orthogonal projection analytical method.</p><p><b>METHOD</b>The samples of Semen Cassiae were hydrolyzed in the 1.5 mol x L(-1) hydrochloride acid and then reflux extracted with chloroform. The chromatographic condition was that the HPLC was run on Agilent 1100 column, Zorbax Eclipse XDB-C18 (4.6 mm x 250 mm, 5 microm). The protected column was Scienhome C18 column (3.0 mm x 20 mm, 5 microm) with acetonitrile-water (0.1% phosphoric acid) as mobile phase in gradient elution at a flow rate of 1.0 mL x min(-1). The detection wavelength and reference wavelength were 278 nm and 550 nm, respectively.</p><p><b>RESULT</b>The characteristic fingerprint collection of illustrative plates of Semen Cassiae were obtained with different HPLC instruments and chromatographic columns. And the asymptotic window orthogonal projection analytical method was used to decide the chromatographic fingerprint peak matching of Semen Cassiae, promptly and prapidly.</p><p><b>CONCLUSION</b>The asymptotic window orthogonal projection analytical method can progress the matching of different fingerprint collection of illustrative plates peak matching well and truly.</p>
Subject(s)
Chromatography , Methods , Cinnamomum aromaticum , Chemistry , Drugs, Chinese Herbal , ChemistryABSTRACT
OBJECTIVE:To study the HPLC fingerprint profiles of crude and processed Semen Cassiae so as to provide basis for the establishment of chromatographic fingerprint of Semen Cassiae.METHODS: The samples of Semen Cassiae were hydrolyzed in the 1.5 mol?L-1 hydrochloride acid and then reflux extracted with chloroform.The HPLC analysis was run in gradient elution.The whole information of single-wavelength chromatographic fingerprint,two-dimension information data at full wavelength 220 nm～550 nm and the data of 18 fingerprint peaks compared with chrysophanol were treated by cluster analysis.RESULTS:It was observed that the contents of several chemical components were higher in the crude or processed Semen Cassiae than in chrysophanol.There were differences between the crude and the processed Semen Cassiae in HPLC fingerprint profiles though they were of good similarity.CONCLUSION: The HPLC fingerprints of liposoluble constituents were obtained with good resolution under the experimental chromatographic system.Three pure chromatographic peaks of chrysophanol,emodin and physcion have been identified.More reliable cluster result can be obtained from two-dimension information data at full wavelength 220 nm～550 nm than from the whole information of single-wavelength chromatographic fingerprint or from the information of chromatographic fingerprint of characteristic peaks.