Objective To review the research progress in new formulations of norcantharidin. Methods The foreign and domestic literature search in the new formulations of norcantharidin was conducted. The research and development of norcantharidin formulations were summarized and commented. Results The drug delivery systems, such as microspheres, nanoparticles, liposomes, and microemulsions, have great development potential as the new formulations for norcantharidin. Conclusion Norcantharidin is an excellent anti-tumor drug. The traditional injections and tablets have serious side effects in clinical application. The new formulations reduced the renal and urinary toxicity and side effects. Those formulations provided better therapeutic effects as target medication. Therefore, the new norcantharidin formulations have great development prospects.

Signal transducer and activator of transcription 3 (STAT3) is a signal transcription protein that exists in the cytoplasm. The abnormal activation of STAT3 is closely related to cell proliferation, differentiation, and canceration. It has abnormal expression in cancer stem cells such as breast cancer, pancreatic cancer, lymphoma, and lung cancer. Therefore, inhibiting the abnormal expression of STAT3 has become a new approach for antitumor therapy.

Baicalein (BE) is an active ingredient derived from the root of Scutellaria baicalensis Georgi. It is a polyhydroxyflavonoid in structure and has many biological activities. Among them, the antitumor effects of baicalein have received widespread attention. It exerts anti-tumor effects by inducing tumor cell apoptosis and invasion, inhibiting tumor angiogenesis, and eliminating free radicals. This article reviews the most recent research works of baicalein in its anti-tumor effects and mechanisms. It is aimed to provide a theoretical basis for the search and development of potential new anti-tumor drugs.

Objective To investigate the effects of Nicotinamide mononucleotide (NMN) on ulcerative colitis induced by dextran sulfate sodium (DSS) in mice. Methods DSS-induced ulcerative colitis mice were used to evaluate the effects of NMN. After NMN administration, the survival time, weight, disease activity index (DAI), colon tissue length and pathological changes of colon tissue slices were observed. Results NMN did not cause significant changes in the survival time, weight, DAI, and intestinal morphology of ulcerative colitis mice. Conclusion NMN has no significant effect on DSS-induced ulcerative colitis mice.

Objective To explore the molecular targets and associated potential pathways of Sinomenii caulis in the treatment of rheumatoid arthritis (RA) based on network pharmacology. Methods The constituents of Sinomenii caulis were searched by Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP). The potential active ingredients were screened based on oral bioavailability (OB) and drug like index (DL) in TCMSP database. The potential targets of active ingrediens were explored based on DRAR-CPI docking server. RA related gene targets were retrieved through GeneCards and OMIM database. Venn online software was used to obtain the common target of drugs and diseases. The "herbs-compound-target-disease" network diagram was constructed by using Cytoscape software. String database was used to draw the protein interaction (PPI) network. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis of the intersection network were conducted by Bioconductor Database. Results 6 active ingredients and 176 targets were identified. 305 target genes directly related to RA were obtained from the GeneCards and OMIM databases. 15 genes were obtained from the intersection of component-target and disease-target. The GO function analysis found 500 items on biological process (BP), 18 items on cellular component (CC), and 28 items on molecular function (MF). KEGG pathway enrichment analysis revealed 77 pathways. Conclusion This study identified six active ingredients from Sinomenii caulis and revealed the key targets of the anti-RA treatment with Sinomenii caulis being IL10、IL4、INS、MAPK8、ELANE、MAPK1 and MAPK14. The important biological processes and signaling pathways including infection, inflammation and immunity were explored. It has laid the foundation for further molecular biology experiments.

Objective To establish an online quantitative analysis model for moisture content assay of hydroxychloroquine sulfate particles by near infrared (NIR) spectroscopy. Methods The NIR spectra were collected in real time when the material particles were dried in the fluidized bed. Meanwhile the water content of the particles was measured with the standard moisture tester. The multiplicative signal correction (MSC) and first derivative followed by Karl Norris smoothing were used for spectra pretreatment. Two spectral range (4 935−5 336 cm⁻¹ and 6 911−7 297 cm⁻¹) were selected for the quantitative model with the partial least squares (PLS) regression. Results The quantitative calibration model had good correlation coefficients with Rc value=0.952 9 and Rp value=0.936 6. The root mean square error of calibration (RMSEC) was 0.408 and the root mean square error of prediction error (RMSEP) was 0.435. The ratio of standard deviation of validation set to prediction standard deviation (RPD) was 5.18. There was no significant difference between the predicted value and the reference value by t test when the established model was applied in large-scale production. Conclusion The online model established for monitoring water content has high accuracy and stability, which can be applied in industrial scale process to monitor the particle moisture in real time.

Objective Colon-targeting capsules based on gastric pellets and enteric pellets were prepared from Baizhu Huanglian prescription. The formulation composition and preparation process were optimized and the in-vitro release characteristics were investigated. Methods Optimum formulation composition and process parameters of Baizhu Huanglian pellets were screened out by single factor experiment and orthogonal design. The pellets core were prepared by extrusion-spheronization technique and coated in the fluid bed using bottom spray coating technique. To investigate the effect of coating level of the isolation layer, the proportion of polymer, the amount of plasticizer and weight gain of enteric coating on the release behavior of the enteric pellets. The pellets release behavior was fitted by model as well. Results The prescription of gastric pellets was drug loading 50%, PVPP 5%, MCC to lactose 1∶2 and wetting agent 40%. The process parameters were extrusion frequency 20 Hz, rounding speed 500 r/min and rounding time 5 min. The prescription of enteric pellets was drug loading 27%, PVPP 5%, MCC to lactose 5∶2, wetting agent 30% and adhesive 20%. The process parameters were extrusion frequency 20 Hz, rounding speed 700 r/min and rounding time 7 min. For enteric coating layer, the coating mixture of EUDRAGIT®L30D-55 to EUDRAGIT® FS30D was 1∶2. The amount of plasticizer was 10%. The increased weight of coating layer was 15%. The release time of enteric pellets in-vitro was up to 24 hours. The release behavior of the pellets conforms to the Higuchi model. Conclusion The colon targeting capsule of Baizhu Huanglian pellets were successfully prepared and showed the characteristics of sustained release and colon targeting.

Objective To search for novel potent 3-ester derivatives of arenobufagin and test their antitumor activities in vitro. Methods Target compounds were synthesized by esterification of arenobufagin with acids. CellTiter method was used to assay the in vitro antitumor activities. Results 3-Ester derivatives exhibited excellent antitumor activities against all the cancer cells. Conclusion Among the 3-ester derivatives, compound 2a had the best activities with the IC₅₀ of 4.0−91.7 nmol/L and appeared to be a valuable candidate for further study.

Objective To study the synergistic effects of aspirin and atorvastatin on cell proliferation of non-small cell lung cancer cell A549 and NCI-H460 and the mechanism of these actions. Methods The proliferation of A549 and NCI-H460 cells treated by aspirin or/and atorvastatin were determined by MTS assay. The migration of A549 and NCI-H460 cells were conducted by wound-healing assay. The expression of relevant protein in mTOR and NFκB signaling pathway were detected by western blotting. The mRNA expression of TNF-α and IL-1β were detected by quantitative real-time PCR. Results Aspirin or/and atorvastatin inhibited the proliferation and migration of A549 and NCI-H460 at concentration of 100 and 5 μmol/L or greater. The effect was enhanced by the combination of aspirin and atorvastatin. Aspirin or/and atorvastatin inhibited the protein expression of the phosphorylation of mTOR and NFκB, and down-regulated anti-apoptotic regulators Bcl-2 and Mcl-1 in NCI-H460 cells. The combination treatment of aspirin and atorvastatin was more efficacious than the single treatment. Atorvastatin decreased the mRNA expression of TNF-α. The combination of atorvastatin with aspirin decreased the mRNA expression of IL-1β by nearly 50 percent compared to the control (P<0.05). Conclusion Aspirin and atorvastatin have synergistic inhibitory effects on cell growth of non-small cell lung cancer cell A549 and NCI-H460 by suppressing mTOR and NFκB signaling pathway.

Objective To prepare an ultra-porous hydrogel capable of controlled release and investigate the drug loading, releasing, administration route and efficacy with insulin as a model drug. Methods The polymer interpenetrating network method was used to prepare ultra-porous hydrogels (SPH-IPN). Insulin was selected as a model drug to study the drug loading and efficacy. Fourier transform infrared spectroscopy and nuclear magnetic resonance carbon spectroscopy were used to investigate the structure of the gel. The swelling ratio and porosity were measured to evaluate the gel performance. Results The drug loading capacity of insulin ultra-porous hydrogel was 3.19%. The insulin-loaded freeze-dried gel exhibited good hypoglycemic effect on diabetic rats in 1−24 hours from the experimental results on rats with subcutaneous implantation. Conclusion The subcutaneously embedded lyophilized insulin ultra-porous hydrogel provided good controlled release efficacy. It maintained stable blood glucose levels within 24 hours.