Latest ArticlesOBJECTIVE To construct a multi-dimensional network system of “component-target-disease”, find the quality markers related to the efficacy of Shensong Yangxin capsules, and establish an efficient and rapid determination method. METHODS The pharmacodynamic substances selected by network pharmacology were used as quality markers and a novel HPLC-ESI-MS/MS method was developed. During the development of the method, multiple-reaction monitoring scanning and a multi-periods program were applied for quantification by switching electrospray ion source polarity between positive and negative modes at appropriate time points in a single run. Chromatographic separation was performed on a Waters C18 column with linear gradient elution of 0.1% formic acid aqueous solution and acetonitrile at a flow rate of 0.8 mL·min-1. RESULTS According to the results of network pharmacology, twenty compounds with high contribution were selected as quality markers for content determination. The results of methodological verification showed that all calibration curves had good linearity (r2>0.991 1) within the test ranges. The precision, accuracy and stability of the method were all satisfying. CONCLUSION The analytical method is simple, rapid, specific and reliable, which is useful for pharmacodynamic substance screening and comprehensive quality evaluation of Shensong Yangxin capsules.
OBJECTIVE To explore the occurrence and characteristics of interstitial lung disease (ILD) induced by novel oral anticoagulants (NOACs) and provide references for clinical safe drug use. METHODS The case reports of ILD induced by NOACs published in PubMed, Embase, CNKI, Wanfang and VIP were searched from the establishment of each database to March 2023, and statistical analysis was conducted on relevant information and data. RESULTS A total of 11 male patients from 8 articles were identified and included in the analysis, including 5 cases of apixaban, 5 cases of dabigatran etexilate and 1 case of edoxaban. The age of the patients was 65-91 (79.6±7.1) years old. All patients suffered from dyspnea and were diagnosed with ILD after imaging examination, in which diffuse alveolar hemorrhage was relatively common. ILD was found from 3 days to 4 years after medication. After treatment including drug withdrawal, mechanical ventilation and methylprednisolone pluse therapy, 9 cases had good prognosis and 2 cases died of respiratory failure. CONCLUSIONS ILD could be induced by different NOACs. Attention should be paid to dyspnea and other symptoms at the early stage of treatment, and imaging examination should be performed when necessary. Once ILD was suspected to be caused by NOACs, withdraw in time and appropriate measures such as glucocorticoid should be taken.
OBJECTIVE To establish a method for the determination of 37 kinds of inorganic elements by microwave digestion and inductively coupled plasma mass spectrometer (ICP-MS), and to detect and analyze 37 kinds of inorganic elements in cistanches herba from different habitats, and to preliminatively explore the pollution distribution of various inorganic elements in cistanches herba from different habitats. METHODS Using nitric acid and hydrogen peroxide as digestion reagent, microwave digestion was used to pretreat the samples. The contents of 37 inorganic elements in cistanches herba were determined simultaneously by internal standard correction and external standard quantitative ICP-MS method. RESULTS In the curve range of 0.50-100 μg·L-1(Hg: 0.20-20 μg·L-1) showed a good linear relationship with the peak area (r≥0.997 4). The detection limits were 0.000 27-0.045 μg·L-1. The average recoveries were 76.5% to 110.0% at high, medium and low levels. RSD of precision and repeatability were lower than 4.8%. The detection rates of 5 harmful heavy metal elements (copper, lead, arsenic, mercury, cadmium) that need to be controlled by Chinese Pharmacopoeia (2015 edition) in 40 batches of cistanches herba were 27.5%, 7.5%, 82.5%, 0 and 100%, respectively. The detection rate of barium, manganese, rubidium and strontium in 40 batches of samples is 100%, and the content is much higher than other elements,there are obvious regional differences. CONCLUSION This method has high sensitivity, good reproducibility, reduced the inspection time and cost, and can simultaneously detect various inorganic elements in cistanches herba, providing data support for optimal cultivation, quality assurance and drug safety of cistanches herba.
Euphorbia pekinensis is a traditional medicine of draining water, dispersing swelling and dissipating binds, first recorded in Shennong's Herbal Classic of Materia Medica. E. pekinensis is used to treat edama, phlegm-fluid retention, carbuncle swollen and toxic and other disease. The major components of E. pekinensis include diterpenoids, triterpenoids, flavonoids, coumarins, organic acids and tannins. E. pekinensis has always emphasized the use of processed products as medicine due to strong toxicity. After processing, its drug properties and chemical components are changed, under heating and acidic conditions, diterpenoids undergo oxidation, hydrolysis and rearrangement, which lead to structural transformation and decrease in content, while glycoside-containing compounds undergo hydrolysis, resulting in an increase in the content of aglycones. This paper summarizes the processing history, composition changes, pharmacological effects and toxicity comparison of E. pekinensis by consulting literature over the years, which provides reference for the rational development and utilization of medicinal material resources of E. pekinensis.
Rectal in situ gel combines the double characteristics of gel and rectal administration, and has become the focus of pharmaceutics research. Rectal in situ gel is a kind of non-chemical crosslinked semi-solid gel which can be transformed from liquid to gel immediately after administration in solution. It has unique reverse hot gel properties, good sustained release effect and high bioavailability. Referring to the relevant literature at domestic and abroad in the past 10 years, the characteristics, preparation technology, quality evaluation methods and application of rectal in situ gel were summarized.By analyzing the research progress of rectal in situ gel new ideas for the research and development of efficient rectal administration preparations are provided.
OBJECTIVE To study the chemical constituents of ethyl acetate extract from Moringa oleifera leaves. METHODS The chemical constituents of ethyl acetate extract from Moringa oleifera leaves were isolated and purified by chromatographic methods. The structures of isolated compounds were identified by MS and NMR data. DPPH and ABTS were used to test the antioxidant activities of the compounds in vitro. RESULTS Fourteen compounds were isolated from ethyl acetate extract of Moringa oleifera leaves and identified as icariside B1 (1), (3S)-O-β-D-glucopyranosyl-6-[3-oxo-(2S)-butenylideny]-1, 1, 5-trimethylcyclohexan-(5R)-ol (2), icariside B2 (3), 9-hydroxy-megastigma-4, 7-dien-3-one-9-O-β-D-glucopyranoside (4), tectorigenin (5), tectoridin (6), iristectorin A (7), iristectorin B (8), 5-hydroxy-2-hydroxymethylpyridine (9), androsin (10), 3, 4, 5-trimethoxyphenyl-1-O-β-D-glucopyranoside (11), 1-O-(4-hydroxymethylphenyl)-α-L-rhamnopyranoside (12), benzyl-O-β-D-glucopyranoside (13) and methyl 2-[4-(α-L-rhamnopyranosyl) phenyl] acetate (14), respectively. Among them, compounds 6, 7 and 8 had certain antioxidant activities, but the activities were weaker than that of vitamin C as positive control. CONCLUSION Compounds 2-11 are isolated from Moringa genus for the first time.
OBJECTIVE To compare the anti-alcohol and liver-protecting effects of four ancient prescriptions, Baibei powder, Shigao decoction, Jupi decoction and Gegen powder, and explore the potential mechanisms of the four ancient prescriptions in the treatment of alcoholic liver disease (ALD). METHODS Rats were randomly divided into normal group, model group and drug administration groups, and the rat drunken model was prepared with 56° liquor. The rats in each administration group were given Chinese medicine decoction by gavage, and the normal group and the model group were given pure water by gavage. The drunken sleep time of rats was recorded, and the blood ethanol concentration and the activities of alcohol dehydrogenase (ADH) and aldehyde dehydrogenase (ALDH) in serum and liver were measured. Network pharmacology method was used to analyze the effective components, key targets and signaling pathways of the four ancipent prescriptions in the treatment of ALD. RESULTS The four ancient prescriptions could significantly prolong the drunkenness time and shorten the sobering time of drunken model rats. Among them, Baibei powder could significantly increase the serum activities of ADH, ALDH and super-oxide dismutase (SOD) and improve triglyceride (TG) and glutathione (GSH) contents (P<0.05). Shigao decoction could significantly reduce the content of serum TG. Jupi decoction could significantly improve the serum GSH and malondialdehyde (MDA) content. Gegen powder could significantly reduce the concentration of blood ethanol, improve the activities of ADH, ALDH and SOD and the contents of TG, total cholesterol (TC), glutathione S-transferase (GST), GSH and MDA in the serum or liver (P<0.05 or P<0.01). The four prescriptions could reduce the degree of liver pathological damage and reduce the area of lipid droplets to varying degrees. Through the network pharmacology analysis, a total of 78 targets were screened out for the treatment of ALD by the four prescriptions. Among them, tumor necrosis factor (TNF), protein kinase B1(AKT1), estrogen receptor 1 (ESR1), epidermal growth factor receptor (EGFR), cytochrome P450 2C19(CYP2C19) and peroxisome proliferator activated receptorα (PPARα) could be used as important targets for the treatment of ALD. Kyoto encyclopedia of genes and gnomes pathway enrichment analysis showed that the ancient prescriptions may play a pharmacodynamic role through PPAR, AMP-activated protein kinase(AMPK), TNF/PPARα-CYP2E1-ALDH signaling pathway. CONCLUSION The four prescriptions all have certain anti-alcohol and liver protection effects, and the effect of Gegen powder is more significant. The four prescriptions may regulate key targets such as TNF, AKT1, cytochrome P450 2E1(CYP2E1), PPARα and ALDH by acting on the TNF/PPARα-CYP2E1-ALDH pathway, thereby accelerating alcohol metabolism, improving lipid metabolism, and reducing oxidative stress.
Anti-tumor drugs have high toxicity and adverse reactions. Liposome formulation can reduce drug toxicity and degradation of drug activity, which is a promising target vector. At present, the pharmacokinetic study of most anti-tumor drug liposomes mainly takes the total concentration as the index, but the free drugs are the part that really plays the pharmacological effect in vivo. So the separation and determination of the free drugs are very important. Sample pretreatment is a key step in the separation and extraction of free drugs after liposome administration. This article focuses on common detection methods, pretreatment methods and analysis examples, to provide reference for the establishment of analysis methods in vivo for anti-tumor drug liposomes.
OBJECTIVE To investigate the effect of total saponin of Aralia taibaiensis (SAT) on cognitive dysfunction of mice with traumatic brain injury (TBI) by mediating silent information regulator 1 (SIRT1)/ forkhead transcription factor 1 (FoxO1)/peroxisome proliferator-activated receptor γ coactivator-1α (PGC-1α) pathway. METHODS C57BL/6 mice were divided into Con group, model group, SAT group (135 mg·kg-1), EX-527 group (10 mg·kg-1 SIRT1 inhibitor EX-527), and SAT+EX-527 group, 12 per group. Mice in the Con group received all surgical operations except cortical shock, and the controllable cortical shock method was used to construct the TBI model for the other groups. After the modeling was successful, the corresponding administration was performed, once a day for 7 d. Morris water maze test was performed to measure the learning and spatial memory abilities of mice; HE staining was performed to measure the pathological changes of damaged cortex; ELISA method was performed to measure the contents of interleukin 6 (IL-6) and tumor necrosis factor-α (TNF-α) in damaged cortex; TUNEL staining was performed to measure neuronal apoptosis; and Western blot was performed to measure the expressions of Caspase-3, Bcl-2 related X protein (Bax), SIRT1, Ace-FoxO1, and Ace-PGC-1α proteins in damaged cortex. RESULTS Compared with the Con group, the mice in the model group had severe pathological damage to the cerebral cortex, the escape latency was extended and the number of crossing platforms was reduced, the levels of IL-6 and TNF-α, neuronal apoptosis rate, and the expressions of Caspase-3, Bax, Ace-FoxO1, and Ace-PGC-1α proteins in damaged cortex were increased, the expression of SIRT1 proteins was decreased (P<0.05). Compared with the model group, the pathological damage of the cerebral cortex of the mice in the SAT group was reduced, the escape latency was shortened and the number of crossing platforms was increased, the levels of IL-6 and TNF-α, neuronal apoptosis rate, and the expressions of Caspase-3, Bax, Ace-FoxO1, and Ace-PGC-1α proteins in damaged cortex were decreased, the expression of SIRT1 proteins was increased (P<0.05), the changes in the corresponding indicators of the EX-527 group showed an opposite trend. EX-527 reversed the improvement effect of SAT on cognitive dysfunction in TBI mice. CONCLUSION SAT may improve the cognitive dysfunction of TBI mice by activating the SIRT1/FoxO1/PGC-1α pathway.
OBJECTIVE To investigate the effect of pharmacokinetic-related gene polymorphisms of rosuvastatin on plasma concentrations of rosuvastatin(RST)and its metabolites: rosuvastatin lactone(RSTL). METHODS The plasma concentrations of RST and its metabolites were determined through an established performance liquid chromatography mass spectrometry method. And the plasma concentrations were determined and DNA was extracted in the Chinese group of 520 people who were stably taking RST for more than one week. Nine SNPs in RST pharmacokinetics-related organic anion transporter, breast cancer resistance protein, cytochrome P450 enzyme genes were genotyped by using the Sequenom MassArray iPlex platform. Univariate and multiple linear regression were used to analyze the effects of baseline characteristics and gene polymorphisms on RST and RSTL respectively. RESULTS The reserch results revealed that ABCG2 rs2231142 variations were highly associated with the plasma concentrations of RST, RSTL (P<0.05; RST: r2=9.7%; RSTL: r2=3.3%). SLCO1B1 rs4149056 significantly affected the concentrations of RST (P<0.05, r2=1%). But, SLCO1B1 rs4149056 had no significant effect on the concentration of RSTL. After inclusion in the multiple regression model, ABCG2 rs2231142, age, and creatinine were retained in the regression model(P<0.05). CONCLUSION The effect of ABCG2 rs2231142 gene polymorphisms on the plasma concentration of RST in the Chinese is greater than that of SLCO1B1 rs4149056. ABCG2 rs2231142 variations are the independent factor affecting the plasma concentrations of RST and RSTL.