Ann Med Chem | Volume 1, Issue 1 | Research Article | Open Access

Design, Synthesis and Biological Evaluation of Novel Triterpenoid Derivatives based on 20(S)-Protopanaxadiol as PotentialAntibacterial Agents

Shao X^1#, Zeng X1^#, Zhou Y² , Zhang S¹ and Zhou Z^{1 *}

¹ Department of Pharmacy, China Three Gorges University, China ² Department of Quality Control, China Resources Sanjiu (Huangshi) Medical & Pharmaceutical Co., Ltd., China

^*Correspondance to: Zhou Z 

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Abstract

A new series of triterpenoid derivatives were synthesized based on 20(S)-Protopanaxadiol (PPD) and evaluated for their antibacterial activity against several representative pathogens. Among which, compounds 5, 9, 11, 13 and 14 displayed good antibacterial activity against Gram-positive bacteria with MIC values of 2 to 16 µg/mL. Furthermore, additional testing against MRSA USA300 demonstrated that compounds 11, 13 and 14 also possess good antibacterial activity with MIC values of 2 to 8 µg/mL. The bactericidal effects revealed that compounds 13 and 14 displayed directly bactericidal activity against B. subtilis and MRSA USA300 with MBC values of 4 to 16 µg/mL. The subsequent synergistic activity assay of these derivatives was also carried out with results showing that compounds 13 and 14 could enhance the susceptibility of MRSA USA300 and B. subtilis 168 to kanamycin and chloramphenicol (FICI<0.5). Compounds 13 and 14 were then evaluated for their cytotoxicity and showed low toxicity with IC50 values about 30 µg/mL against HeLa cells and about 95 µg/mL against HEK-293 cells, respectively. The plausible structure-activity relationship was also concluded

Keywords:

Protopanaxadiol; Triterpenoid; Antibacterial activity; Synergistic effect; Cytotoxicity

Citation:

Shao X, Zeng X, Zhou Y, Zhang S, Zhou Z. Design, Synthesis and Biological Evaluation of Novel Triterpenoid Derivatives based on 20(S)-Protopanaxadiol as Potential Antibacterial Agents. Ann Med Chem. 2019; 1(1): 1003.