三种喹诺酮类药物的体外抗菌活性和防突变能力评价

doi:10.12092/j.issn.1009-2501.2026.08.006

中国临床药理学与治疗学 ›› 2026, Vol. 31 ›› Issue (8): 1064-1069.doi: 10.12092/j.issn.1009-2501.2026.08.006

• 基础研究 • 上一篇

三种喹诺酮类药物的体外抗菌活性和防突变能力评价

罗开萍¹^,²(), 徐杰³, 张险峰³, 石新¹^,*(), 杭永付¹^,²^,*()

1. 苏州大学附属第一医院药学部，苏州 215006，江苏
2. 苏州大学药学院，苏州 215006，江苏
3. 苏州大学附属第一医院临床检测中心，苏州 215006，江苏

收稿日期:2025-12-30 修回日期:2026-02-24 出版日期:2026-08-26 发布日期:2026-09-09
通讯作者: 石新,杭永付 E-mail:20245226037@stu.suda.edu.cn;306828072@qq.com;hangyongfu1986@163.com
作者简介:罗开萍，女，硕士研究生在读，研究方向：临床药学。E-mail：20245226037@stu.suda.edu.cn
基金资助:
江苏省医学重点学科（ZDXK202247）；白求恩公益基金会－社区感染性疾病科研能力建设项目（BCF-XC-SQ-20221206-10）

Evaluation of the in vitro antibacterial activity and mutant prevention potential of three quinolone antibiotics

Kaiping LUO¹^,²(), Jie XU³, Xianfeng ZHANG³, Xin SHI¹^,*(), Yongfu HANG¹^,²^,*()

1. Department of Pharmacy, The First Affiliated Hospital of Soochow University, Suzhou 215006, Jiangsu, China
2. School of Pharmacy, Soochow University, Suzhou 215006, Jiangsu, China
3. Center of Clinical Laboratory, the First Affiliated Hospital of Soochow University, Suzhou 215006, Jiangsu, China

Received:2025-12-30 Revised:2026-02-24 Online:2026-08-26 Published:2026-09-09
Contact: Xin SHI,Yongfu HANG E-mail:20245226037@stu.suda.edu.cn;306828072@qq.com;hangyongfu1986@163.com

摘要/Abstract

摘要：

目的: 探讨奈诺沙星、左氧氟沙星及莫西沙星三种喹诺酮类抗菌药物对革兰氏阳性菌（G⁺）和革兰氏阴性菌（G^?）的体外抑菌效果，为临床合理使用提供依据。方法: 采用微量肉汤稀释法（broth microdilution method）对292株临床分离菌株[包括甲氧西林敏感金黄色葡萄球菌（methicillin-susceptible Staphylococcus aureus，MSSA）、表皮葡萄球菌、屎肠球菌、纹带棒状杆菌、大肠埃希菌、肺炎克雷伯菌、铜绿假单胞菌和鲍曼不动杆菌]进行药物敏感性试验，比较三种药物的最低抑菌浓度（MIC）分布、药效学特征。用琼脂稀释法进一步测定部分菌株的防突变浓度（MPC），评估防突变能力。结果: 在G⁺菌中，奈诺沙星对金黄色葡萄球菌（MIC₉₀=16 μg/mL）、表皮葡萄球菌（MIC₉₀=2 μg/mL）及纹带棒状杆菌（MIC₉₀=4 μg/mL）的活性均优于左氧氟沙星和莫西沙星。在耐甲氧西林金黄色葡萄球菌（methicillin-resistant Staphylococcus aureus，MRSA）菌株中，奈诺沙星的敏感率达66.96%。在G^?菌中，铜绿假单胞菌对左氧氟沙星的 MIC₉₀为2 μg/mL，低于奈诺沙星和莫西沙星（均为4 μg/mL）；肺炎克雷伯菌、大肠埃希菌及鲍曼不动杆菌对三药的MIC₉₀多为64 μg/mL，整体敏感性较低。在防突变能力方面，MSSA中奈诺沙星的MPC₉₀为2 μg/mL，低于莫西沙星（4 μg/mL）和左氧氟沙星（16 μg/mL），其选择指数（selection index，SI）的范围最小；在耐药G^?菌中三药MPC₉₀普遍较高，SI也明显增大。但左氧氟沙星对耐药铜绿假单胞菌的MPC₉₀（16 μg/mL）低于莫西沙星（32 μg/mL）和奈诺沙星（64 μg/mL）。结论: 奈诺沙星在金黄色葡萄球菌（含MRSA）等G⁺菌中显示出更强的抗菌活性，且在MSSA中表现出最强的防突变能力。左氧氟沙星在铜绿假单胞菌中维持了较好的抗菌活性，且其防突变浓度在受试药中相对较低。临床应用中应结合病原体类型和耐药风险进行选择。

关键词: 奈诺沙星, 左氧氟沙星, 莫西沙星, 最低抑菌浓度, 防突变浓度

Abstract:

AIM: To evaluate the in vitro antibacterial efficacy of three quinolones—nemonoxacin, levofloxacin, and moxifloxacin—against Gram-positive (G⁺) and Gram-negative (G^?) bacteria, providing a scientific basis for rational clinical use. METHODS: Drug susceptibility tests were conducted on 292 clinical isolates (including Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecium, Corynebacterium striatum, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Acinetobacter baumannii) using the broth microdilution method to compare the distribution of minimum inhibitory concentrations (MICs) and pharmacodynamic characteristics. The mutant prevention concentration (MPC) of selected strains was further determined by the agar dilution method to evaluate their mutant prevention capabilities. RESULTS: For G⁺ bacteria, nemonoxacin exhibited superior activity against Staphylococcus aureus (MIC₉₀=16 μg/mL), Staphylococcus epidermidis (MIC₉₀=2 μg/mL), and Corynebacterium striatum (MIC₉₀=4 μg/mL) compared to levofloxacin and moxifloxacin. In MRSA strains, the susceptibility rate of nemonoxacin reached 66.96%. For G^? bacteria, the MIC₉₀ of levofloxacin against P. aeruginosa was 2 μg/mL, which was lower than that of nemonoxacin and moxifloxacin (both 4 μg/mL). For K. pneumoniae, E. coli, and A. baumannii, the MIC₉₀ values for all three drugs were mostly 64 μg/mL, indicating overall low susceptibility. In terms of mutant prevention, nemonoxacin showed an MPC₉₀ of 2 μg/mL in MSSA, which was lower than that of moxifloxacin (4 μg/mL) and levofloxacin (16 μg/mL), with the narrowest range of selection index (SI). In resistant G^— bacteria, the MPC₉₀ and SI values for all three drugs were generally higher. However, the MPC₉₀ of levofloxacin against resistant P. aeruginosa (16 μg/mL) was lower than that of moxifloxacin (32 μg/mL) and nemonoxacin (64 μg/mL). CONCLUSION: Nemonoxacin demonstrates stronger antibacterial activity against G⁺ bacteria such as S. aureus (including MRSA) and possesses the most potent mutant prevention capability in MSSA. Levofloxacin maintains favorable antibacterial activity against P. aeruginosa, and its MPC is relatively lower among the tested drugs. Clinical selection should be based on the specific pathogen type and the risk of resistance.

Key words: nemonoxacin, levofloxacin, moxifloxacin, minimum inhibitory concentration, mutant prevention concentration

中图分类号:

R965.2

罗开萍, 徐杰, 张险峰, 石新, 杭永付. 三种喹诺酮类药物的体外抗菌活性和防突变能力评价[J]. 中国临床药理学与治疗学, 2026, 31(8): 1064-1069.

Kaiping LUO, Jie XU, Xianfeng ZHANG, Xin SHI, Yongfu HANG. Evaluation of the in vitro antibacterial activity and mutant prevention potential of three quinolone antibiotics[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2026, 31(8): 1064-1069.

图/表 3

参考文献 18

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Strain types	Antibacterials	MIC₅₀	MIC??	Range	Sensitivity rate
Staphylococcus aureus (n=148)	Levofloxacin	0.5	≥64	0.125 - >64	56.08%
	Moxifloxacin	0.125	64	0.03 - >64	60.81%
	Nemonoxacin	0.125	16	0.03 - 16	70.95%
MRSA (n=112)	Levofloxacin	1	≥64	0.25->64	51.79%
	Moxifloxacin	0.125	64	0.03- >64	56.25%
	Nemonoxacin	0.125	16	0.03 - 16	66.96%
MSSA (n=36)	Levofloxacin	0.25	32	0.125- >64	69.44%
	Moxifloxacin	0.06	8	0.03 - 64	75%
	Nemonoxacin	0.06	2	0.03 - 16	83.33%
Staphylococcus epidermidis (n=14)	Levofloxacin	4	≥64	0.125 - >64	21.43%
	Moxifloxacin	1	8	0.06 - 32	35.71%
	Nemonoxacin	0.25	2	0.03 - 4	85.71%
Enterococcus faecium (n=17)	Levofloxacin	32	64	0.25 - >64	-
	Moxifloxacin	8	32	0.06- 64	-
	Nemonoxacin	2	16	0.06- 32	-
Corynebacterium striatum (n=17)	Levofloxacin	32	32	16- >64	0%
	Moxifloxacin	8	16	4 - 64	0%
	Nemonoxacin	2	4	1-8	-

Strain types	Antibacterials	MIC₅₀	MIC??	Range	Sensitivity rate
Staphylococcus aureus (n=148)	Levofloxacin	0.5	≥64	0.125 - >64	56.08%
	Moxifloxacin	0.125	64	0.03 - >64	60.81%
	Nemonoxacin	0.125	16	0.03 - 16	70.95%
MRSA (n=112)	Levofloxacin	1	≥64	0.25->64	51.79%
	Moxifloxacin	0.125	64	0.03- >64	56.25%
	Nemonoxacin	0.125	16	0.03 - 16	66.96%
MSSA (n=36)	Levofloxacin	0.25	32	0.125- >64	69.44%
	Moxifloxacin	0.06	8	0.03 - 64	75%
	Nemonoxacin	0.06	2	0.03 - 16	83.33%
Staphylococcus epidermidis (n=14)	Levofloxacin	4	≥64	0.125 - >64	21.43%
	Moxifloxacin	1	8	0.06 - 32	35.71%
	Nemonoxacin	0.25	2	0.03 - 4	85.71%
Enterococcus faecium (n=17)	Levofloxacin	32	64	0.25 - >64	-
	Moxifloxacin	8	32	0.06- 64	-
	Nemonoxacin	2	16	0.06- 32	-
Corynebacterium striatum (n=17)	Levofloxacin	32	32	16- >64	0%
	Moxifloxacin	8	16	4 - 64	0%
	Nemonoxacin	2	4	1-8	-

Strain types	Antibacterials	MIC₅₀	MIC??	Range	Sensitivity rate
Pseudomonas aeruginosa (n=10)	Levofloxacin	0.5	2	0.25 - 4	72.73%
	Moxifloxacin	1	4	1 - 16	54.55%
	Nemonoxacin	2	4	1 -8	-
Klebsiella pneumoniae (n=42)	Levofloxacin	2	64	0.015 - >64	40.48%
	Moxifloxacin	2	64	0.03 - >64	42.86%
	Nemonoxacin	8	64	0.008 - >64	-
Escherichia coli (n=21)	Levofloxacin	8	16	0.25 - 32	14.29%
	Moxifloxacin	16	64	0.125- 64	9.52%
	Nemonoxacin	16	64	1 -64	-
Acinetobacter baumannii (n=23)	Levofloxacin	8	64	0.06 - >64	26.09%
	Moxifloxacin	16	64	0.015 - >64	26.09%
	Nemonoxacin	16	64	0.06- >64	-

Strain types	Antibacterials	MIC₅₀	MIC??	Range	Sensitivity rate
Pseudomonas aeruginosa (n=10)	Levofloxacin	0.5	2	0.25 - 4	72.73%
	Moxifloxacin	1	4	1 - 16	54.55%
	Nemonoxacin	2	4	1 -8	-
Klebsiella pneumoniae (n=42)	Levofloxacin	2	64	0.015 - >64	40.48%
	Moxifloxacin	2	64	0.03 - >64	42.86%
	Nemonoxacin	8	64	0.008 - >64	-
Escherichia coli (n=21)	Levofloxacin	8	16	0.25 - 32	14.29%
	Moxifloxacin	16	64	0.125- 64	9.52%
	Nemonoxacin	16	64	1 -64	-
Acinetobacter baumannii (n=23)	Levofloxacin	8	64	0.06 - >64	26.09%
	Moxifloxacin	16	64	0.015 - >64	26.09%
	Nemonoxacin	16	64	0.06- >64	-

Strain types	Antibacterials	MPC_range	MPC₅₀	MPC₉₀	SI
MSSA (n=20)	Levofloxacin	0.5-32	2	16	2 - 32
	Moxifloxacin	0.25 -8	0.5	4	2 - 33.33
	Nemonoxacin	0.125- 4	0.5	2	2 - 16.67
Resistant Klebsiella pneumoniae (n=8)	Levofloxacin	2 - 32	8	32	4 - 64
	Moxifloxacin	2- 32	16	32	4 - 64
	Nemonoxacin	4- 64	16	32	4- 32
Resistant Pseudomonas aeruginosa (n=6)	Levofloxacin	8-64	16	16	8 - 32
	Moxifloxacin	16-64	32	32	2 - 32
	Nemonoxacin	16-64	32	64	8 -32
Resistant Escherichia coli (n=6)	Levofloxacin	2- 64	4	16	4 - 16
	Moxifloxacin	2-128	4	32	2 - 16
	Nemonoxacin	8 -128	16	32	4- 32

三种喹诺酮类药物的体外抗菌活性和防突变能力评价

Evaluation of the in vitro antibacterial activity and mutant prevention potential of three quinolone antibiotics

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