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已发表论文
评估氯化血根碱作为治疗多重耐药淋病的潜在药物
Authors Zhang R, Qi Y, Peng H, Tao C, Lu S, Ke Q, Shen S, Wang Z, Lin X
Received 7 May 2025
Accepted for publication 15 September 2025
Published 24 September 2025 Volume 2025:18 Pages 5109—5114
DOI https://doi.org/10.2147/IDR.S538954
Checked for plagiarism Yes
Review by Single anonymous peer review
Peer reviewer comments 2
Editor who approved publication: Dr Hazrat Bilal
Ran Zhang,1,2,* Yuqiu Qi,2,* Hui Peng,2,* Chenlong Tao,2,3 Songwei Lu,2 Qiankun Ke,2 Shangzhu Shen,2 Zhuo Wang,1,2 Xiaomian Lin1,2,4
1Department of Pharmacy, Anhui University of Chinese Medicine, Hefei, 230012, People’s Republic of China; 2Department of Pharmacy, Shanghai Changhai Hospital, The First Affiliated Hospital of Naval Medical University, Shanghai, People’s Republic of China; 3College of Life Sciences and Biopharmaceuticals, Shenyang Pharmaceutical University, Shenyang, People’s Republic of China; 4Dermatology Hospital, Southern Medical University, Guangzhou, Guangdong, People’s Republic of China
*These authors contributed equally to this work
Correspondence: Xiaomian Lin, Department of Pharmacy, Shanghai Changhai Hospital, The First Affiliated Hospital of Naval Medical University, Shanghai, 510000, People’s Republic of China, Email linxm@smmu.edu.cn Zhuo Wang, Department of Pharmacy, Shanghai Changhai Hospital, The First Affiliated Hospital of Naval Medical University, Shanghai, 510000, People’s Republic of China, Email wangzhuo088@163.com
Objective: Neisseria gonorrhoeae (N. gonorrhoeae) is responsible for the sexually transmitted infection (STI) gonorrhea, which has an estimated global annual incidence of 82.4 million cases among adults. The recommended first-line treatment typically involves a single-dose systemic therapy, comprising injectable ceftriaxone and oral azithromycin. Nonetheless, the first-line treatment failures caused by antimicrobial resistance represent a major global public health concern, threatening the efficacy of current gonorrhea treatments and highlighting the urgent need for the development of alternative therapeutic approaches.
Methods: A total of 54 clinical strains of N. gonorrhoeae were collected in Nanchang City, 2021. To assess the efficacy of antibiotics and chelerythrine chloride, we determined the minimum inhibitory concentrations (MICs) using agar dilution and broth microdilution methods, respectively. To explicitly evaluate the potential for resistance induction, the ATCC49226 strain was subjected to continuous passaging for 30 days in sub-MIC concentrations of chelerythrine chloride, with MIC assessments every 5 days.
Results: In clinical samples, antimicrobial resistance was observed for penicillin (67.27%), tetracycline (81.82%), ciprofloxacin (98.18%), azithromycin (5.45%), and spectinomycin (0%), with decreased susceptibility for ceftriaxone (16.36%) and cefixime (20.00%). High-throughput screening of a natural product library identified chelerythrine chloride as exhibiting significant inhibitory activity against N. gonorrhoeae, including strains with decreased susceptibility to cephalosporins. The MIC range was 0.002– 8 mg/L, with both the MIC50 and MIC90 values at 8 mg/L. Furthermore, N. gonorrhoeae did not develop resistance, maintaining a stable MIC of 4 mg/L over a 30-day treatment period.
Conclusion: In this study, we have established a novel association between chelerythrine chloride and N. gonorrhoeae, demonstrating for the first time its preliminary efficacy in eradicating multidrug-resistant strains of N. gonorrhoeae. Considering the significant resistance challenges posed by N. gonorrhoeae. chelerythrine chloride emerges as a promising antibacterial agent with substantial potential for clinical development.
Keywords: N. gonorrhoeae, antimicrobial resistance, chelerythrine chloride, antimicrobial agent
1Department of Pharmacy, Anhui University of Chinese Medicine, Hefei, 230012, People’s Republic of China; 2Department of Pharmacy, Shanghai Changhai Hospital, The First Affiliated Hospital of Naval Medical University, Shanghai, People’s Republic of China; 3College of Life Sciences and Biopharmaceuticals, Shenyang Pharmaceutical University, Shenyang, People’s Republic of China; 4Dermatology Hospital, Southern Medical University, Guangzhou, Guangdong, People’s Republic of China
*These authors contributed equally to this work
Correspondence: Xiaomian Lin, Department of Pharmacy, Shanghai Changhai Hospital, The First Affiliated Hospital of Naval Medical University, Shanghai, 510000, People’s Republic of China, Email linxm@smmu.edu.cn Zhuo Wang, Department of Pharmacy, Shanghai Changhai Hospital, The First Affiliated Hospital of Naval Medical University, Shanghai, 510000, People’s Republic of China, Email wangzhuo088@163.com
Objective: Neisseria gonorrhoeae (N. gonorrhoeae) is responsible for the sexually transmitted infection (STI) gonorrhea, which has an estimated global annual incidence of 82.4 million cases among adults. The recommended first-line treatment typically involves a single-dose systemic therapy, comprising injectable ceftriaxone and oral azithromycin. Nonetheless, the first-line treatment failures caused by antimicrobial resistance represent a major global public health concern, threatening the efficacy of current gonorrhea treatments and highlighting the urgent need for the development of alternative therapeutic approaches.
Methods: A total of 54 clinical strains of N. gonorrhoeae were collected in Nanchang City, 2021. To assess the efficacy of antibiotics and chelerythrine chloride, we determined the minimum inhibitory concentrations (MICs) using agar dilution and broth microdilution methods, respectively. To explicitly evaluate the potential for resistance induction, the ATCC49226 strain was subjected to continuous passaging for 30 days in sub-MIC concentrations of chelerythrine chloride, with MIC assessments every 5 days.
Results: In clinical samples, antimicrobial resistance was observed for penicillin (67.27%), tetracycline (81.82%), ciprofloxacin (98.18%), azithromycin (5.45%), and spectinomycin (0%), with decreased susceptibility for ceftriaxone (16.36%) and cefixime (20.00%). High-throughput screening of a natural product library identified chelerythrine chloride as exhibiting significant inhibitory activity against N. gonorrhoeae, including strains with decreased susceptibility to cephalosporins. The MIC range was 0.002– 8 mg/L, with both the MIC50 and MIC90 values at 8 mg/L. Furthermore, N. gonorrhoeae did not develop resistance, maintaining a stable MIC of 4 mg/L over a 30-day treatment period.
Conclusion: In this study, we have established a novel association between chelerythrine chloride and N. gonorrhoeae, demonstrating for the first time its preliminary efficacy in eradicating multidrug-resistant strains of N. gonorrhoeae. Considering the significant resistance challenges posed by N. gonorrhoeae. chelerythrine chloride emerges as a promising antibacterial agent with substantial potential for clinical development.
Keywords: N. gonorrhoeae, antimicrobial resistance, chelerythrine chloride, antimicrobial agent