Mechanism of Marsdenia tenacissima against ovarian cancer based on network pharmacology and experimental verification / 中国中药杂志

The present study aimed to explore the main active components and underlying mechanisms of Marsdenia tenacissima in the treatment of ovarian cancer(OC) through network pharmacology, molecular docking, and in vitro cell experiments. The active components of M. tenacissima were obtained from the literature search, and their potential targets were obtained from SwissTargetPrediction. The OC-related targets were retrieved from Therapeutic Target Database(TTD), Online Mendelian Inheritance in Man(OMIM), GeneCards, and PharmGKB. The common targets of the drug and the disease were screened out by Venn diagram. Cytoscape was used to construct an "active component-target-disease" network, and the core components were screened out according to the node degree. The protein-protein interaction(PPI) network of the common targets was constructed by STRING and Cytoscape, and the core targets were screened out according to the node degree. GO and KEGG enrichment analyses of potential therapeutic targets were carried out with DAVID database. Molecular docking was used to determine the binding activity of some active components to key targets by AutoDock. Finally, the anti-OC activity of M. tenacissima extract was verified based on SKOV3 cells in vitro. The PI3K/AKT signaling pathway was selected for in vitro experimental verification according to the results of GO function and KEGG pathway analyses. Network pharmacology results showed that 39 active components, such as kaempferol, 11α-O-benzoyl-12β-O-acetyltenacigenin B, and drevogenin Q, were screened out, involving 25 core targets such as AKT1, VEGFA, and EGFR, and the PI3K-AKT signaling pathway was the main pathway of target protein enrichment. The results of molecular docking also showed that the top ten core components showed good binding affinity to the top ten core targets. The results of in vitro experiments showed that M. tenacissima extract could significantly inhibit the proliferation of OC cells, induce apoptosis of OC cells through the mitochondrial pathway, and down-regulate the expression of proteins related to the PI3K/AKT signaling pathway. This study shows that M. tenacissima has the characteristics of multi-component, multi-target, and multi-pathway synergistic effect in the treatment of OC, which provides a theoretical basis for in-depth research on the material basis, mechanism, and clinical application.

Effect and mechanism of essential oil from Zanthoxylum bungeanum in microemulsion gel preparation on percutaneous delivery of complex components / 中国中药杂志

This study aimed to investigate the transdermal enhancing effect of essential oil from Zanthoxylum bungeanum(Z. bungeanum oil) in microemulsion gel(ZO-ME-gel) on permeation of different components,and reveal the transdermal enhancing mechanism of ZO-ME-gel. A series of components with different log P values were selected as model drugs and encapsulated in ZO-ME-gel to simplify and characterize the complex components of traditional Chinese medicine. The transdermal behavior of the model drugs was further examined using the improved Franz diffusion cell method. Then attenuated total reflection Fourier transform infrared spectroscopy(ATR-FTIR),differential scanning calorimetry(DSC) studies and hematoxylin-eosin(HE) staining were used to investigate the effects of Z. bungeanum oil and ZO-ME-gel on keratin,intercellular lipids and microstructure of the stratum corneum(SC). The results showed that Z. bungeanum oil and ZO-ME-gel had a good transdermal enhancing effect on both hydrophilic and lipophilic drugs,and the best effect was achieved when log P value was-0. 5. The transdermal enhancing mechanism of Z. bungeanum oil and ZO-ME-gel was related to affecting the order of the SC lipids,changing lipid fluidity and protein conformation,and disrupting the integrity of the SC structure. 5% Z. bungeanum oil had greater transdermal enhancing effect and destruction of SC structure than ZO-ME-gel. These results suggested that Z. bungeanum oil loaded in microemulsion gel still had a good transdermal enhancing effect although the effect was not as great as Z. bungeanum oil itself,in addition,ZO-ME-gel was less irritating to the skin and safer to use,which had a guiding role in the development and clinical application of Z. bungeanum oil-containing traditional Chinese medicine topical preparations.

Optimization of multicomponent microemulsion of Chinese materia medica with different oil-water partition coefficients by simplex lattice method / 中草药

Objective To prepare multicomponent microemulsion of Chinese materia medica (CMM) with different oil-water partition coefficients (logP values) by simplex lattice method and evaluate its quality. Methods The surfactants, cosurfactants and oil phases were screened by saturated solubility method. Ochratins, ligustrazine, ferulic acid, puerarin and geniposide were model drugs to represent the complex components of CMM. Based on the pseudo-ternary diagram, simplex lattice method was adopted to optimize the multicomponent microemulsion of CMM with different logP values by appearance, particle size and polydispersity index as evaluation indexes. The experimental design and model building were constructed by Design Expert 8.06 software to optimize the response surface data analysis and validate the optimal prescription composition. The quality of microemulsion was evaluated by observing appearance and stability as well as measuring particle size and potential. Results The optimum formulation was oleic acid-Labrasol-propylene glycol-water (5.303:29.336:7.334:58.027). The prepared microemulsion was clear in appearance with good yellowish color and stable property. The average particle size was (118.77 ± 0.37) nm, PDI was 0.282 ± 0.02 and Zeta potential was (0.346 ± 0.05) mV. Conclusion The results indicated that the multicomponent microemulsion of CMM with different logP values is optimized and the drug loading was high. The multicomponents microemulsion of CMM with different logP values (-1.01-3.85) is established and optimized, providing a feasible microemulsion carrier for the multicomponent CMM to simplify its prescription screening work.

Determination of IgM-RF, IgA-RF, IgG-RF, IL-1RI, CDK2 and ROC evaluation in patients with rheumatoid arthritis / 南方医科大学学报

<p><b>OBJECTIVE</b>To assess the value of rheumatoid factors IgM-RF, IgA-RF, IgG-RF, interleukin-1 receptor type I (IL-1RI) and cyclin-dependent kinase 2 (CDK2) in the diagnosis of rheumatoid arthritis (RA).</p><p><b>METHODS</b>IgM-RF, IgA-RF, IgG-RF, IL-1RI and CDK2 were detected in 47 patients with active RA, 47 with inactive RA, 20 with active systemic lupus erythematosus (SLE), 20 with inactive SLE, 20 with acute upper respiratory tract infection (AURTI), and 20 healthy controls using enzyme-linked immunosorbent assay (IgM-RF, IgA-RF, IgG-RF, IL-1RI) and time-resolved fluoroimmunoassay (CDK2).</p><p><b>RESULTS</b>Patients with active and inactive RA showed significant differences in peripheral serum CDK2 and IgA-RF levels (P<0.05). Between active and inactive RA patients, RA patients and SLE patients, RA patients and AURTI patients, and RA patients and the control subjects, the area under curve (AUC) of the receiver operating characteristic curve (ROC) was 0.561, 0.814, 0.799, and 0.888 for IgM-RF, 0.596, 0.678, 0.729, and 0.850 for IgA-RF, 0.614, 0.718, 0.692, and 0.791 for IgG-RF, 0.646, 0.691, 0.762, and 0.835 for IL-1RI, 0.803, 0.753, 0.741, and 0.840 for CDK2, respectively.</p><p><b>CONCLUSIONS</b>IgM-RF may have high value in the diagnosis and differential diagnosis of RA, and CDK2 can be useful for differential diagnosis between active and inactive RA.</p>