In recent years, transdermal delivery has proven to be one of the most favorable methods among novel drug delivery systems due to avoiding the gastrointestinal tract and reducing systemic side effects. Skin is one of the most immunologically active organs due to the presence of immune cells, such as Langerhans cells(LCs), dermal dendritic cells(dDCs), and T cells. Unique immune properties of the skin offer excellent opportunities for transdermal treatment of autoimmune diseases(ADs). This review highlights the pathogenic mechanism of ADs caused by various reasons such as loss of immune self-tolerance and abnormal autoreactive T cells, and the advantages of transdermal drug delivery for the treatment of ADs, as well as expounds on the application of transdermal drug delivery systems(TDDS) in the treatment of several typical ADs. TDDS will provide new ideas and methods for the treatment and research of autoimmune diseases.

Rheumatoid arthritis(RA) is a chronic, systemic, and abnormal inflammatory immune response. It is characterized by the involvement of synovium and multiple organs and the destruction of joints and articular cartilage. In the past 30 years, some promising new compounds and antibodies have been developed to treat RA. The introduction of RA therapeutic drugs and the development of precision medicine have also given rise to several problems related to patients' access to new treatments, choice of the best regimen, cost-effectiveness, prognosis monitoring and efficacy monitoring, especially in terms of low drug response rate, drug resistance and adverse side effects. People attach great importance to the best combination of drugs for the treatment of RA, especially in patients with severe symptoms or early progression. New treatments and mechanisms are needed to solve these problems, and accurate guidelines for drug selection and drug recombination are established. According to the clinical trial database of the National Library of Medicine, this study summarizes the exciting new drugs, and discusses the trends and challenges in the development of RA drugs, which provides a meaningful reference for the accurate treatment and future research direction of RA.

Cell membrane chromatography is a bioaffinity chromatography method which has been developing rapidly in recent years, where the carriers coated with receptor-containing biomembrane are packed to stationary phase and the bioaffinity between compound and membrane receptor presents in chromatography process. This method has the advantages of biomimetic, high efficiency and low cost, and has been widely used in drug screening and identifying the affinity between membrane receptor and candidate ligand. Mitochondria, a crucial functional intracellular membrane system, with various drug targets residing in membrane. Recently, significant research advancements have been made in mitochondrial membrane chromatography technology. In this paper, the recent progresses and applications of cell membrane chromatography and mitochondria membrane chromatography are reviewed.

OBJECTIVE To screen one Monascus purpureus stain that has high yield of lovastatin and provide potential strains for the development of red yeast rice(RYR) industry. OBJECTIVE Twelve RYR samples were collected, and Monascus sp. was isolated from these samples using traditional isolation technology and identified by morphology and ITS sequencing. All M. purpureus strains were screened and their total lovastatin contents [including lactone lovastatin(C₂₄H₃₆O₅) and acid lovastatin(C₂₄H₃₈O₆)] were determined by high performance liquid chromatography(HPLC). Soft SPSS 25.0 was used for variance analysis. RESULTS A total of 35 Monascus sp. strains were isolated and 23 of them were identified at specie level, including 11 M. purpureus strains, 10 M. ruber strains and 2 M. aurantiacus strains. There was significant difference(P<0.05) in lovastatin production among 11 M. purpureus strains. Among them, SM-1 isolate produced the highest amount of total lovastatin, with the value reaching (4.652±0.001) mg·g^-1, followed by M4-1, F1-3, and F5-3 strains with the value reaching (2.903±0.033) and (3.108±0.009) mg·g^-1, respectively. M4-5 isolate produced the lowest amount of lovastatin with the value of (2.712±0.014) mg·g^-1. CONCLUSION Fungal strain is chaotic in the fermentation of RYR on the market. A high-yielding lovastatin strain SM-1 is screened and can be used a potential strain for RYR production.

OBJECTIVE To design and synthesize N-substituted methylene-3-(4-(pyridin-3-yl)pyrimidin-2-yl)amino)benzohydrazide derivatives, and evaluate their anticancer activities. OBJECTIVE Using 3-aminobenzoic acid ethyl ester as the starting reagent, a series of target compounds 4a-4p were synthesized in a 4-step reaction, and all of the target compounds were structurally characterized by ¹H-NMR, ¹³C-NMR and HRMS. MTT assay was used to detect the inhibitory effect of synthetic compounds on breast cancer cells. RESULTS It's showed that the target compounds had certain inhibitory activity on the growth of breast cancer cells, among which compound 4e was the best one, showing obvious inhibitory effect on breast cancer cells. The IC₅₀ value of breast cancer cell line MCF-7 was (2.30±0.34)μmol·L^-1, and the toxicity of 4e to normal mammary epithelial cells was low(IC₅₀>100 μmol·L^-1). Thus, 4e is better than the positive drug cisplatin. In addition, 4e could significantly up-regulate the protein expression level of Nur77 and induce the S-phase arrest of MCF-7. CONCLUSION This series of compounds have good anti-cancer activity and are of interest for further study.

OBJECTIVE To study the chemical constituents of Pinellia ternata(Thunb).Breit.. OBJECTIVE The 60% ethanol extract of Pinellia ternata(Thunb). Breit. was isolated and purified by silica, MCI, ODS and preparative HPLC, and the structures of obtained compounds were identified by physico-chemical properties and MS、NMR data. RESULTS The compound are kaempferol-3-O-β-D-rutinoside(1), inosine(2), lactariolide I(3), (2E,4E,1'S,2'R,4'S,6'R)-dihydrophaseic acid(4), tryptophan(5), 1-oleoyl-3-O-β-D-galactopyranosyl-sn-glycerol(6), 6'-O-linoleylsucrose(7), 6'-O-palmitoylsucrose(8), gingerglycolipid C(9), (2S)-1-O-6'-O-(α-D-galactopyranosyl)-β-D-galactopyranosyl-3-O-palmitoyl glyceride(10), 1-O-hexadecanoyl-3-O-β-D-galatopyranosylglycerol(11), tianshic acid(12), 4-(2-hydroxyethyl)phenol(13), phenylpropionic acid(14), 3-phenyllactic acid(15), trans-cinnamic acid(16). CONCLUSION Compound 1, 2, 3, 4, 6-13, 15-16 are firstly isolated from the genus Pinellia.

OBJECTIVE To study the protective effect of petroleum ether fraction(AERP) and water soluble fraction(AERW) of Arnebia euchroma(Royle) Johnst. on acute liver injury in mice, and to isolate the effective components of petroleum ether fraction with better effect, and to study the antihepatitis B virus effect of its effective components. OBJECTIVE Forty eight C57 mice were randomly divided into 6 groups. After 14 days of administration, lipopolysaccharide/D-galactosamine(LPS/D-Galn) was used to induce acute liver injury with inflammatory infiltration at the last 2 hours. The liver and spleen index, the content of AST and ALT in mouse serum and the content of NO in liver homogenate were measured, and the pathological section of liver tissue was investigated. The petroleum ether extract was separated by normal silica gel, reverse silica gel and thin layer preparation plate, and four active naphthoquinones were obtained. The antihepatitis B virus activity of the four active naphthoquinones on HepG2.2.15 cells was detected by MTT method. RESULTS Both AERW high-dose group and AERP low-dose group can reduce the activity of AST and ALT in serum and the content of NO in liver tissue of mice to varying degrees, and improve the pathological changes of liver tissue to varying degrees. After comparative analysis, AERP has better liver protective and anti-inflammatory effects. The extraction method of AERP was optimized to obtain AERP with more effective components, and four active naphthoquinones were isolated: isovalerylshikonin, acetylshikonin, 2,3-dimethylpentenylshikonin and shikonin. Four active naphthoquinones have good inhibitory effects on HepG2.2.15 cells. CONCLUSION The results show that AERW and AERP have a good protective effect on acute liver injury. The liver protective effect of AERP is better than that of AERW. The four active components of AERP have a good inhibitory effect on HBV. AER extract has a significant liver protective effect, and the active components of AER have a significant inhibitory effect on hepatitis B virus.

OBJECTIVE To build a text-convolutional neural network(Text-CNN)-based prediction model for anti-Staphylococcus aureus(S.aureus) activity and identify anti-S.aureus hits by virtual screening. OBJECTIVE A dataset containing 26327 compounds annotated with S.aureus activity data was collected and curated from the ChEMBL database. Ten pairs of training and test sets were generated by random partition for 10 times and then 10 models were built using the Text-CNN algorithm. The best-performing model was determined by model evaluation and further studied by Y-randomization test and applicability domain analysis. Following that, the best-performing model was used to virtually screen the in-house chemical library, by which the potential antibacterial agents were determined. The micro-broth dilution method was used to test anti-S.aureus activity of the potential hits. RESULTS The machine-learning model(named Text-CNN3) performed well in classification. Evaluated on the test set, its Mathews correlation coefficient was 0.573 and the area under the ROC curve was 0.881. With this model for virtual screening as well as antibacterial screening, compounds Y5 and Y7 were identified as antibacterial compounds, with minimum inhibitory concentrations(MIC) of 8 and 4 μg·mL^-1, respectively. CONCLUSION The Text-CNN3 model in this study is effective to identify anti-S.aureus compounds, while the antibacterial hits Y5 and Y7 are worthy of further study.

OBJECTIVE To verify the accuracy of the “water content-conductivity fitting curve” model for determining the critical point of microemulsion O/W phase, and to further use this model to optimize the microemulsion of tanshinone extract. OBJECTIVE The “water content-conductivity fitting curve” model was used to determine the phase critical point of microemulsion into O/W type. According to the proportion of microemulsion oil phase, total surfactant and water phase, the pseudo ternary was drawn using Origin 2021 software. The phase diagram was used to screen out the proportions of the larger milk-forming areas; the average particle size and PDI of the microemulsion were used as the inspection indicators, and the star point design-response surface method was used to optimize the microemulsion; high-speed centrifugation and standing at 4 ℃ and 25 ℃ for 60 days, to examine the stability of the microemulsion. RESULTS The optimized microemulsion formulation was(18.11% medicated oil phase, 61.21% Tween 80, 20.68% 1,2-propanediol, the water critical point is 64.29%), K_m was 2.96, preparation temperature was 27.4 ℃, under different experimental conditions, the stability of the microemulsion was good. CONCLUSION The O/W phase critical point determined by the “water content-conductivity fitting curve” model has high accuracy, and the optimized microemulsion has good stability, which achieves the expected research goals.

OBJECTIVE To synthesize p-toluenesulfonic acid(PTS) and famotidine(FMT) cocrystal in order to improve thesolubility of famotidine in water and the permeability. OBJECTIVE The cocrystal was prepared by solvent evaporation method combined with ultrasound. The cocrystal was characterized by scanning electron microscopy, differential scanning calorimetry, thermogravimetric analysis, infrared spectroscopy and powder X-ray diffraction. The single crystal structure of FMT-PTS-H₂O(1∶1∶1) was successfully obtained, and the solubility and permeability of the newly synthesized cocrystal were studied. RESULTS After the formation of cocrystal, the water solubility and permeability of FMT increased by 1.54 and 2.29 times, respectively. CONCLUSION Compared with FMT, the solubility and permeability of FMT after the formation of cocrystal were improved. This study provides a method for improving the permeability of biopharmaceutics classification system(BCS)Ⅲ drugs, which will contribute to the development of low permeability drugs.

OBJECTIVE To establish a method for the determination of 32 elements in COVID-19 vaccine. OBJECTIVE The 32 elements were determined by inductively coupled plasma optical emission spectrometer(ICP-OES) through semi-quantitative screening and quantitative detection, and the specificity, linearity, limit of quantification, detection limit and recovery rate of the ICP-OES method were investigated to evaluate the feasibility of the method for the detection of trace elements in vaccines. RESULTS The linear relationship of each element was good within the detection mass concentration range, and the recoveries of element added were 94.06%-115.50%. When applied to the detection of the samples at each accelerated placement point, except for the trace contents of B and Si elements, which did not increase significantly after long-term placement, the contents of other elements were far less than the prescribed limits. CONCLUSION The ICP-OES method is established. And the method has good specificity, reliable results, simple and rapid, and is suitable for the determination of 32 elements in COVID-19 vaccine.

OBJECTIVE To analyze the quality differences of Cyathulae Radix from different manufacturers on the market based on national drug sampling and testing in 2022, then analyze the problems and put forward suggestions to provide basis for the quality supervision and standard improvement of Cyathulae Radix. OBJECTIVE Inspection was conducted according to corresponding standards, inspection reports were issued, and then quality evaluation and analysis were conducted. At the same time, problems were found and suggestions were made based on targeted exploratory research on quality problems, standard problems and other related problems found in the inspection. RESULTS A total of 334 batches of Cyathulae Radix samples were taken. According to the standard inspection, two batches of samples were found to be substandard in character, and Cyathulae capitatae Radix was used as Cyathulae Radix. At the same time, it was found that the content determination methods in the standard were too complex, and the specified limit for content determination was too low. In the exploratory study, the unique component achybidensaponin I was detected in 27 batches of Cyathulae Radix and 7 batches exceeded the specified limit, which was mixed with Achyranthes bidentata. Plant growth regulator (paclobutrazol) was detected in 270 batches of Cyathulae capitatae Radix. The detection of heavy metals and harmful elements cadmium(Cd) in 114 batches exceeded the limit. Finally, the quality standard of Cyathulae Radix was improved, the supplementary test method was established, and the risk warning was put forward. CONCLUSION Through the national sampling inspection, the relevant problems in the prepared slices and quality standards of Cyathulae Radix are found, suggesting that the quality standards should be improved and the quality supervision of Cyathulae Radix should be strengthened.

OBJECTIVE To explore an evaluation method of sterile operation in pharmacy intravenous admixture services(PIVAS). OBJECTIVE The US intravenous quality assurance(IVQA) media fill test kit was used to verify the aseptic operation of the mixed dispensing personnel in our hospital, and the feasibility of applying the media fill test in the PIVAS was preliminarily explored. RESULTS The media fill test was easy to operate without harsh culture conditions and testing equipment. The test results were different under two different mixing conditions, which can verify the operation of personnel. CONCLUSION The media fill test is applicable to the quality control of personnel in sterile dispensing operations.