Li Yang’s research while affiliated with Jiangxi University of Traditional Chinese Medicine and other places

Cyclooxygenase‐2 (COX‐2) plays a critical role in the pathogenesis of rheumatoid arthritis (RA), while Dendropanax dentiger root (DDR) is a traditional Chinese medicine (TCM) used to treat RA. However, the specific bioactive ingredients responsible for its therapeutic effect remain unidentified. In this study, 10 phenylpropanoids, including neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, liriodendrin, isochlorogenic acid B, isochlorogenic acid A, eleutheroside E1, isochlorogenic acid C, 3,5‐di‐O‐caffeoylquinic acid methyl ester, and 4,5‐di‐O‐caffeoylquinic acid methyl ester, were identified as potential COX‐2 inhibitors in DDR using affinity ultrafiltration coupled with ultra‐high‐performance liquid chromatography and mass spectrometry (AUF‐LC‐MS). Mass spectrometric fragmentation patterns of these compounds were analyzed, revealing consistent and logical fragmentation profiles. Molecular docking results revealed that all ten compounds exhibited strong binding affinities with COX‐2, with binding energies ranging from ‐8.0 to ‐9.8 kcal/mol. Further experimental validation confirmed that these compounds exhibited potent COX‐2 inhibitory activity, with IC50 values ranging from 5.2 to 10.3 µM. These compounds are likely to represent the primary anti‐inflammatory components of DDR. Additionally, this study provides a systematic identification of chlorogenic acids within the Dendropanax genus and investigates their mass spectrometric fragmentation patterns. The findings contribute to the scientific basis for the clinical application of DDR.

Lagopsis supina (Steph. ex. Willd.) Ikonn.-Gal., an ancient Chinese herbal medicine, is traditionally used to treat blood stasis diseases such as myocardial ischemia (MI). However, its pharmacodynamics substances of the anti-MI effect and their potential mechanisms remain unclear. This study aims to elucidate the pharmacodynamics effects of L. supina against MI and reveal their underlying mechanisms in zebrafish. LSD fraction was screened out for anti-MI active fraction from L. supina by isoprenaline hydrochloride (ISO)-induced zebrafish. It could increase the stroke volume, ejection fraction, and ventricular short-axis systolic rate in the zebrafish model. A total of 30 compounds (Nos. 1–30) were isolated and identified from LSD by various chromatographic techniques and nuclear magnetic resonance spectroscopy. Among them, six compounds, including three lignin compounds (Nos. 15, 16, and 18) and three flavonoid glycosides (Nos. 14, 25, and 26), showed noticeable anti-MI activities, and tiliroside (No. 25) was more active. Molecular docking indicated that tiliroside has a strong binding ability with the proteins KDR, PI3K, Akt, Erk, p38, Bcl-2, Bax, and Caspase3. In the end, the results of RT-qPCR manifested that tiliroside markedly upregulated expression levels of genes kdr, pik3cb, akt2, mapk1, mapk11, mapk14, and bcl-2b and prominently downregulated expression levels of genes bax and caspase3. According to the above results, tiliroside activated the kdr-mediated PI3K-Akt and MAPK signaling pathways to exert the anti-MI activity. These discoveries give a scientific basis for applying L. supina in MI treatment and suggest new avenues for developing tiliroside as a candidate for MI therapy.

Hosta plantaginea flower is an important Chinese herb in treating chronic pharyngitis (CP); however, its pharmacodynamics against CP and the underlying mechanisms remain unclear. This study demonstrated that the ethyl acetate (HPB) and n‐butanol (HPC) fractions of the H. plantaginea flower were identified as the active fractions against CP, significantly increasing the body weight, improving damaged pharyngeal tissues, and reducing TNF‐α, PGE2, IL‐1β, and IL‐6 levels in rats induced by 5% ammonia solution. Metabolomics studies identified 55 differential metabolites, with 26 being reversely regulated by HPB and HPC. These 26 metabolites are closely associated with phosphoinositide 3‐kinase‐protein kinase B (PI3K‐Akt), just another kinase‐signal transducers and activators of transcription (JAK‐STAT), mitogen‐activated protein kinases (MAPKs), and nuclear factor kappa‐B (NF‐κB) pathways. Mechanically, HPB and HPC prominently suppressed the expression of phosphorylated PI3K, Akt1, JAK1, STAT3, JNK, p38, Erk, p65, and inhibitor of NF‐κB (IκBα) proteins. Finally, HPLC analysis identified flavonoids as the primary phytochemicals of HPB and HPC. In conclusion, HPB and HPC are the main active fractions of H. plantaginea flower against CP, acting through regulating energy metabolism and inhibiting PI3K‐Akt, JAK‐STAT, MAPKs, and NF‐κB signaling pathways, and the flavonoids are the primary constituents.

In the original publication [...]

Purpose: To conduct a real-world evaluation of the efficacy and safety of combined Chinese and Western medicine in treating knee osteoarthritis (KOA). Methods: A multicenter, prospective cohort study design was employed, enrolling 450 KOA patients (Kellgren-Lawrence score of 3 or less). The patients were divided into a Western medicine treatment group (WM group) and a combined Western and traditional Chinese medicine treatment group (WM-CM group). A 6-week treatment plan was administered, and follow-up visits occurred at 2 weeks, 4 weeks, and 6 weeks after initiating treatment. The primary outcome indicator was the total Western Ontario and McMaster Universities Arthritis Index (WOMAC) score after 6 weeks of treatment. Secondary outcome indicators included WOMAC subscales for pain, stiffness, and joint function, visual analogue scale (VAS) score, physical component summary (PCS), mental component summary (MCS), and clinical effectiveness. The incidence of drug-related adverse events was used as a safety evaluation indicator. Results: A total of 419 patients were included in the final analysis: 98 in the WM group and 321 in the WM-CM group. The baseline characteristics of the two groups were comparable, except for the incidence of stiffness symptoms and stiffness scores. After 6 weeks of treatment, the WM-CM group exhibited superior results to the WM group in improving the total WOMAC score (24.71 ± 1.38 vs. 16.36 ± 0.62, p < 0.001). The WM-CM group also outperformed the WM group in WOMAC pain and joint function scores, VAS score, PCS score, MCS score, and clinical effectiveness (p < 0.05), which was consistent with the findings of the main evaluation index. Subgroup analysis indicated that the combined Chinese and Western medicine treatment showed more pronounced benefits in patients under 65 years of age and in those with a Kellgren-Lawrence (K-L) classification of 0-I. Throughout the study, no adverse effects were observed in either group. Conclusion: The combination of Chinese and Western medicine demonstrated superiority over Western medicine alone in relieving knee pain symptoms, improving knee function, and enhancing the quality of life for KOA patients with a K-L score of 3 or less. Moreover, the treatment exhibited a good safety profile. Clinical Trial Registration: (https://www.chictr.org.cn/), identifier (ChiCTR1900027175).