Abstract

Antibacterial activity of berberine (Ber) and 8-acetonyl-dihydroberberine (A-Ber) alone and combined uses with antibacterial agents ampicillin (AMP), azithromycin (AZM), cefazolin (CFZ) and levofloxacin (LEV) was studied on 10 clinical isolates of SCCmec III type methicillin-resistant Staphylococcus aureus (MRSA). Susceptibility to each agent alone was tested using a broth microdilution method and the chequerboard and time-kill tests for the combined evaluations, respectively. The alone MICs/MBCs (μg/mL) ranges were 32–128/64–256 (Ber) and 32-128/128-512 (A-Ber). Significant synergies were observed for the Ber (A-Ber)/AZM and Ber (A-Ber)/LEV combinations against 90% of the tested MRSA strains, with fractional inhibitory concentration indices (FICIs) values ranged from 0.188 to 0.500. An additivity result was also observed for the Ber/AZM combination by time-kill curves. These results demonstrated for the first time that Ber and A-Ber enhanced the in vitro inhibitory efficacy of AZM and LEV to a same extent, which had potential for further investigation in combinatory therapeutic applications of patients infected with MRSA.

Highlights

  • The first clinical isolate of methicillin-resistant Staphylococcus aureus (MRSA) was reported in when only a year after methicillin was introduced for clinical use [1]

  • We have been working on searching for anti-MRSA compounds from the Chinese herbal medicines [6,7,8] and the interactions of the compounds with conventional antibacterial agents [9,10]

  • The present report deals with the comparison of anti-MRSA activity between berberine (Ber) and its synthetic derivative 8-acetonyl-dihydroberberine (A-Ber) (Figure 1)

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Summary

Introduction

The first clinical isolate of methicillin-resistant Staphylococcus aureus (MRSA) was reported in when only a year after methicillin was introduced for clinical use [1]. (Berberidaceae) and other spp. in several different families, such as Coptis chinensis Franch (Ranunculaceae) and Phellodendron amurense Ruprecht (Rutaceae). It is a classic plant antimicrobial which has been used in the treatment of gastroenteritis, diarrhea, and cholera diseases [11]. The present report deals with the comparison of anti-MRSA activity between berberine (Ber) and its synthetic derivative 8-acetonyl-dihydroberberine (A-Ber) (Figure 1). Their synergistic effects on four conventional antibacterial agents ampicillin (AMP), azithromycin (AZM), cefazolin (CFZ) and levofloxacin (LEV) are involved

Results and Discussion
Antibacterial Agents
Bacterial Strains
Susceptibility Testing
Synergy Testing
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