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JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH · 2022 · IF 1.61

Synthesis and antitumor activity of benzophenone compound

Bei-Dou Zhou,Rong-Rong Wei,Jia-Li Li,Zi-Han Yu,Zhi-Min Weng,Zhi-Peng Ruan,Jian Lin,Yuan-Yuan Fang,Gui-Fen Xu,Dong-Bao Hu

Seven benzophenone compounds were synthesized in one or two steps, then their antitumor activity was evaluated. The total yields ranged from 9% to 44%. Compounds 3c–5c exhibited obvious antitumor activity. Among them, compounds 3c and 4c exhibited excellent and broad-spectrum antitumor activity. Compound 3c exhibited much stronger inhibitory activities against fourteen cancer cells than cisplatin. In particular, compound 3c exhibited stronger cytotoxicity against hepatocarcinoma SMMC-7721 cells than Taxol, with a half maximal inhibitory concentration (IC50) of approximately 0.111 μM. These results demonstrated that compounds 3c, 4c and 5c were very promising antitumor leads for further structural modification.

研究领域: 药理学 · 肿瘤学

✓ 已验证 DOI PubMed 高影响因子

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Frontiers in Pharmacology · 2025 · IF 4.8

In vitro and in vivo characterization of oridonin analogs as anti-inflammatory agents that regulate the NF-κB and NLRP3 inflammasome axis

Huiping Ou,Zhanpan Wu,Jinhua Ning,Qiufeng Huang,Wancun Wang,Guochun Yang,Yingxun Zhou,Anguo Hou,Peng Li,Lingyun Chen,Wen Bin Jin

Introduction: A series of oridonin hybrids were synthesized and evaluated for anti-inflammatory potential, focusing on their ability to inhibit NO production in RAW264.7 cells and their therapeutic prospects for NLRP3-driven disorders.Methods: Anti-inflammatory activity was assessed by measuring NO inhibition in LPS-stimulated RAW264.7 cells. The most active compound, 4c, was further analyzed using ELISA and WB to evaluate its effects on inflammatory proteins (p-NF-κB, p-IκB, NLRP3, IL-6, IL-1β, COX-2, iNOS). In vivo efficacy was tested in a murine acute lung injury model, with RT‒qPCR and WB used to assess inflammatory markers in lung tissues. Molecular docking predicted 4c’s binding mode with NLRP3, while RNA-seq and RT‒qPCR identified differentially expressed genes.Results: Compound 4c significantly inhibited NO production and suppressed key inflammatory proteins in vitro. In vivo, it alleviated acute lung injury, reduced IL-6 and TNF-α mRNA levels, and inhibited NLRP3, p-NF-κB, and IL-6 protein expression. Docking suggested covalent binding to NLRP3. RNA-seq revealed 4c upregulated Trdc, Stfa2, and Gsta2 while downregulating Spib, Csf2, and Nr4a1.Discussion: Compound 4c demonstrates potent anti-inflammatory effects via NLRP3 pathway inhibition and modulation of inflammatory genes. These findings highlight oridonin hybrids, particularly 4c, as promising candidates for NLRP3-driven inflammatory disorders, warranting further investigation.

研究领域: 药理学 · 免疫学 · 分子生物学 · 炎症研究

✓ 已验证 DOI PubMed 高影响因子

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Synthesis and antitumor activity of benzophenone compound

In vitro and in vivo characterization of oridonin analogs as anti-inflammatory agents that regulate the NF-κB and NLRP3 inflammasome axis