Jingyong Sun

Carabrol, isolated from Carpesium macrocephalum Franch. & Sav., showed anti-inflammatory potential in LPS-induced RAW264.7 murine macrophages. We transformed the structure of carabrol and modified the carbon atoms at positions 11 and 13 to obtain a series of carabrol derivatives. The anti-inflammatory activity of 26 carabrol derivatives was synthesized and screened. Their structures were established using ¹H NMR, ¹³C NMR, and HRMS spectroscopic data. All compounds were tested against RAW264.7 cells using the Griess assay; the bioassay test suggested that most of the compounds were found to have in vitro anti-inflammatory activities with low cytotoxicity. We identified several novel carabrol derivatives, which have potent anti-inflammatory activities for tested RAW264.7 cells with IC₅₀ values that ranged from 0.82 to 1.31 μM. Among these, compound a9 was identified as the most potent anti-inflammatory agent, effectively suppressing key pro-inflammatory mediators such as nitric oxide (NO), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α). In a xylene-induced ear swelling model in mice, compound a9 demonstrated a significant inhibitory effect on ear swelling, highlighting its potent in vivo anti-inflammatory activity.

Dencichine, a precious medicinal material, also known as Tianqi acid, is a non-protein amino acid contained in Leguminous and Araliaceae plants. For years, the raw form of dencichine has been widely used in Chinese medicine for its hemostatic and cardiovascular properties to arrest various internal or external hemorrhage, eliminate blood stasis, improve blood circulation, disperse bruises, and reduce swelling and pain. The research on the separation and determination, pharmacological efficacy, and toxicology of dencichine in recent years is systematically reviewed to provide reference for further research, development, and utilization.

As lung cancer remains the leading cause of cancer‐related deaths worldwide, the development of novel therapeutic drugs is essential. 20‐Acetylsinularolide B (ASB) is a diterpene isolated from marine soft coral Lobophytum crassum . Our previous studies demonstrated that ASB exhibits growth‐inhibitory effects on non–small cell lung cancer (NSCLC) cells. This study employed network pharmacology to predict ASB's potential targets in NSCLC treatment. The predicted target was validated using the cellular thermal shift assay (CETSA). In vitro anticancer activity was assessed through MTT and crystal violet assays for proliferation, along with Western blotting, cell cycle and apoptosis analysis, mitochondrial membrane potential, reactive oxygen species (ROS) levels, and nuclear morphology evaluation. Migration and invasion were evaluated using wound healing and Transwell assays. The results showed that ASB significantly arrests the cell cycle of H1299 cells at the G ₂ /M phase by modulating the IGF1R/PI3K/AKT/mTOR signaling pathway, thereby inhibiting cell mitosis. Simultaneously, ASB promoted intracellular ROS production, reduced mitochondrial membrane potential, and ultimately induced cell apoptosis. In addition, ASB significantly inhibited the colony formation, migration, and invasion abilities of H1299 cells, which are closely associated with the function of the IGF1R target. These findings highlight the significant potential of ASB as a lead anticancer compound for NSCLC therapy.

There has been limited research on the preparation of analogues of cycloartane‐type sapogenols (9,19‐cyclolanostanes). Therefore, we decided to use cycloastragenol as a lead compound for structural modification. The semi‐synthetic derivatives were mainly obtained by reactions such as oxidation, alkylation, acylation, and aldol reactions. In this study, we synthesized 27 cycloastragenol derivatives, 20 of which were novel compounds, and evaluated their protective activity on t‐BHP‐induced C2C12 cell growth inhibition and anti‐aging activities. We found that most derivatives inhibited t‐BHP‐induced cell damage. And certain derivatives reduced the formation of ROS and decreased the production of MDA induced by t‐BHP. The findings indicate that these cycloastragenol derivatives might be useful in the treatment of age‐related diseases.

Cycloartane triterpenoids are widely distributed in the plant kingdom, and there have been reports of hundreds of families containing cycloartane triterpenoids. But the types and content of cycloartane are different among various plants. In recent years, a large amount of cycloartane triterpenoids have been extracted and studied from different plants, and some types of cycloartane triterpenoids exhibit great pharmacological activities in terms of antiaging, antioxidant, anti‐inflammatory, anticancer, antiarrhythmic effects, and so on. Herein, we have systematically reviewed these research on the structure of naturally occurring, synthetic, and semisynthetic cycloartane triterpenoids, with particular emphasis on their pharmacological activities.

The ocean has always been one of the important sources of natural products. In recent years, many natural products with different structures and biological activities have been obtained, and their value has been clearly recognized. Researchers have been deeply engaged in the field of separation and extraction, derivative synthesis, structural studies, biological evaluation, and other fields of research for marine natural products. Thus, a series of marine indole natural products which have structural and biological prospect have caught our eyes. In this review, we summarize some of these marine indole natural products with relatively good pharmacological activity and research value, and discuss issues concerning chemistry, pharmacological activity, biological evaluation, and synthesis, including monomeric indoles, indole peptides, bis-indoles, and annelated indoles. Most of the compounds have cytotoxic, antiviral, antifungal, or anti-inflammatory activities.

The roots of Gypsophila oldhamiana Miq. (Caryophyllaceae) have been used as a traditional Chinese medicine to treat fever, consumptive disease, infantile malnutrition and so on.

KRAS is a member of the RAS gene family, which is involved in the regulation of human life activities. KRAS^G12C mutation is distributed in many tumors and has been the focus of attention. In our study, we analyzed the binding of BAY-293 to KRAS protein using molecular docking technology. We designed and synthesized 20 compounds and tested their bioactivity. At the same time, we found that compound 8P (IC₅₀ = 2.6 ± 1.2 μM) had good inhibitory activity against the A549 cell line and compound 8e had a good inhibitory effect on the McF-7 cell line with IC₅₀ = 5.5 ± 0.3 μM.

It has been shown in many studies that kirenol is a diterpene with significant biological activity. In this study, thirty-one kirenol derivatives were synthesized. The structures of thirty-one kirenol derivatives were established using IR, ¹H NMR, ¹³C NMR, and LC-MS spectroscopic data. Among them, twenty-nine kirenol derivatives were evaluated for their cytotoxic activities and anti-inflammatory activities. In MTT analysis, all tested compounds showed weak cytotoxicity. Cultured macrophage RAW 264.7 cells were used for the anti-inflammatory experiments. Griess assay was used to evaluate the inhibitory effect of all tested compounds on the overproduction of nitric oxide (NO). The preliminary bioassay test suggested that all of the kirenol derivatives showed strong anti-inflammatory activity. In particular, seven compounds showed better activities than the positive control. We believe that these compounds have greater potential for future druggability and improvement of human health.

Forty-five gypsogenin and gypsogenic acid derivatives were synthesized and screened for their cytotoxic activities. Their structures were established using IR, ¹H NMR, ¹³C NMR, and LC-MS spectroscopic data, and they were subjected to extensive biological testing. In the MTT assays, nearly all the compounds displayed good cytotoxicity in the low μM range for several human tumor cell lines (A549, MC3-8, TE-1, HepG-2 and MCF-7). The preliminary bioassay test suggested that most of these gypsogenin and gypsogenic acid derivatives showed different degrees of antitumor activities. In particular, some compounds displayed moderate antitumor activity. They were shown to destroy cell membranes and increase their permeability, which led to the outflow of intracellular nucleic acid.