Dong Huihua, Guan Aixing, Yang Shixian, Wang Luyao, Zhao Lijuan, Chen Hao, Wei Hongyu, Luo Peipei, Huang Yanqiang
Guangxi Technology Innovation Cooperation Base of Prevention and Control Pathogenic Microbes with Drug Resistance, Youjiang Medical University for Nationalities, Baise, 533000, China.
Affiliated Hospital of Youjiang Medical University for Nationalities, Baise, 533000, China.
Mater Today Bio. 2025 Aug 13;34:102194. doi: 10.1016/j.mtbio.2025.102194. eCollection 2025 Oct.
Objectives With the increase of () drug resistance, it is increasingly difficult to cure fundamentally. Frequent and excessive use of antibiotics can lead to disturbances in the intestinal flora and even inflammatory bowel disease, so new drugs are urgently needed. Luteolin (LUT) has been found to have antimicrobial effects, but its water solubility is very low, and the antimicrobial effect is not ideal. To improve the water solubility of LUT and enhance its antibacterial activity, we encapsulated it with liposomes and coated it with chitosan quaternary ammonium salts to increase its targeting and acid responsiveness. Results Compared with LUT, H-L-NPs solubility is significantly improved, and the MIC is reduced by 1024 times, which is also effective against drug-resistant strains. The effect of treatment is significantly better than that of clinical triple therapy. In addition, H-L-NPs have the advantages of high safety and specificity, which can target the treatment of gastric and maintain the diversity of intestinal microbiota, and is not easy to develop drug resistance, making it a very promising anti- lead. In conclusion, H-L-NPs greatly improved the antimicrobial activity of LUT and , and possessed the antimicrobial advantages of high targeting, acid responsiveness, specificity, and low toxicity. It is a kind of agent with a broad application prospect.
目的 随着（）耐药性的增加，从根本上治愈越来越困难。频繁且过量使用抗生素会导致肠道菌群紊乱甚至引发炎症性肠病，因此迫切需要新药。已发现木犀草素（LUT）具有抗菌作用，但其水溶性非常低，抗菌效果不理想。为提高LUT的水溶性并增强其抗菌活性，我们用脂质体对其进行包封并用壳聚糖季铵盐进行包覆，以增加其靶向性和酸响应性。结果 与LUT相比，H-L-NPs的溶解度显著提高，最低抑菌浓度（MIC）降低了1024倍，对耐药菌株也有效。其治疗效果明显优于临床三联疗法。此外，H-L-NPs具有高安全性和特异性的优点，可靶向治疗胃溃疡并维持肠道微生物群的多样性，且不易产生耐药性，使其成为一种非常有前景的抗（）药物。总之，H-L-NPs极大地提高了LUT的抗菌活性，并且具有高靶向性、酸响应性、特异性和低毒性等抗菌优势。它是一种具有广阔应用前景的抗菌剂。
