Synthesis, and anti-inflammatory activities of gentiopicroside derivatives / 中国天然药物

A series of 26 novel derivatives have been synthesized through structural modification of gentiopicroside, a lead COX-2 inhibitor. And their in vivo and in vitro anti-inflammatory activities have been investigated. The in vitro anti-inflammatory activities were evaluated against NO, PGE2, and IL-6 production in the mouse macrophage cell line RAW264.7 stimulated by LPS. Results showed that most compounds had good inhibitory activity. The in vivo inhibitory activities were further tested against xylene-induced mouse ear swelling. Results demonstrated that several compounds were more active than the parent compound gentiopicroside. The inhibition rate of the most active compound P23 (57.26%) was higher than positive control drug celecoxib (46.05%) at dose 0.28 mmol·kg-1. Molecular docking suggested that these compounds might bind to COX-2 and iNOS. Some of them, e.g P7, P14, P16, P21, P23, and P24, had high docking scores in accordance with their potency of the anti-inflammatory activitiy, that downregulation of the inflammatory factors, NO, PGE2, and IL-6, was possibly associated with the suppression of iNOS and COX-2. Therefore, these gentiopicroside derivatives may represent a novel class of COX-2 and iNOS inhibitors.

Chinese Medicine Prevention and Treatment of Tumor Based on Ferroptosis： A Review / 中国实验方剂学杂志

Ferroptosis is a new type of cell death caused by abnormal accumulation of iron-dependent reactive oxygen species （ROS） and imbalance of redox with the participation of iron ions. In recent years， studies have found that ferroptosis is associated with various diseases and can especially regulate the development of tumors. Chinese medicine has unique advantages in tumor prevention and treatment. How to use ferroptosis theory to guide the prevention and treatment of cancer and other tumor diseases by Chinese medicine is a new research hotspot. This paper summarizes the proposal， action mechanism， and signaling pathway of ferroptosis， its application in tumor therapy， and the research on the activity of Chinese medicine based on ferroptosis. Results found that the occurrence of ferroptosis is related to iron metabolism， lipid ROS metabolism， and other signaling pathways and gene expressions. Ferroptosis can regulate tumor initiation and development， treatment， and tumor immunity， which provides strategies for tumor treatment and anti-tumor drug development. By analyzing the biological activity of Chinese medicine against ferroptosis， we found that Chinese medicines （Scutellariae Radix， Puerariae Lobatae Radix， Astragali Radix， Ginkgo， Epimedii Folium， Artemisiae Annuae Herba， and Salviae Miltiorrhizae Radix et Rhizoma）， Chinese herbal compounds （ Naotaifang， Si Junzitang， and Shenmai injection）， and Chinese medicine effective components （baicalein， dihydroartemisinin， puerarin， piperlongumine， luteolin， and quercetin） can exert antitumor and other biological activities by regulating ferroptosis. Therefore， Chinese medicine has great potential in preventing and controlling tumors and other diseases by regulating ferroptosis. This paper provides theoretical basis and research ideas for the in-depth study of ferroptosis theory and guides the prevention and treatment of tumor diseases by Chinese medicine.

Application of Cell Membrane Chromatography Coupled with Mass Spectrometry in Screening of Active Ingredients of Traditional Chinese Medicines / 中国实验方剂学杂志

The chemical components (groups) contained in traditional Chinese medicine(TCM) and its compound preparations are the material basis for its curative effect, because of the integrity of the action of TCM and the complexity of its compositions and mechanism. The separation and analysis of chemical constituents in TCM and its compound prescriptions by various methods is always a key problem to be solved in the research of disease prevention and treatment of TCM. The binding of drug molecules to receptors at the cellular level was explored to provide a new idea for the screening of active components of TCM or its compound preparations. Traditional methods have some drawbacks, such as cumbersome operation, time-consuming, waste of solvents and irreversible adsorption of samples. The basic information of pharmacological parameters cannot be given in the separation process, and the active ingredients cannot be efficiently and accurately located. At present, cell membrane chromatography (CMC), one of the methods, is used to study the interaction between drug molecules and receptors, and can combine the existing chromatography and mass spectrometry technology, cell biology and receptor pharmacology, and correctly reflect the interaction between active parts, active components and cell membrane and membrane receptors, so it has unique advantages in screening effective parts, separation of active components and high-throughput screening from complex TCM system. The principles and characteristics of CMC, the cell membrane model in the field of active ingredient selection of TCM and its research status in combination with gas chromatography-mass spectrometry (GC-MS) and liquid chromatography-mass spectrometry (LC-MS) were reviewed, and its development prospects and future research methods were discussed, which provides theoretical basis and practical guidance for the research and utilization of CMC in the field of TCM.