CAJ | 학술논문

齐墩果酸属于五环三萜类化合物，在自然界广泛分布，并且显示出多种生物活性，如：抗菌、抗炎、抗病毒及抗肿瘤等。但对其衍生物抑菌活性研究方面的报道较少。为了更为深入地研究齐墩果酸及其衍生物的构效关系，我们以具有较好生物活性的齐墩果酸为先导化合物，通过对其C-28位进行结构修饰，设计合成了6种未见报道的齐墩果酸衍生物。目标化合物的结构经IR和1HNMR表征确证，并对金黄色葡萄球菌、抗甲氧西林金黄色葡萄球菌、抗喹诺酮金黄色葡萄球菌、变形链球菌和大肠杆菌进行抑菌活性测试。结果表明，经修饰后的齐墩果酸衍生物对变形链球菌的抗菌活性较母体化合物有不同程度的提升。
제돈과산속우오배삼첩류화합물，재자연계엄범분포，병차현시출다충생물활성，여：항균、항염、항병독급항종류등。단대기연생물억균활성연구방면적보도교소。위료경위심입지연구제돈과산급기연생물적구효관계，아문이구유교호생물활성적제돈과산위선도화합물，통과대기C-28위진행결구수식，설계합성료6충미견보도적제돈과산연생물。목표화합물적결구경IR화1HNMR표정학증，병대금황색포도구균、항갑양서림금황색포도구균、항규낙동금황색포도구균、변형련구균화대장간균진행억균활성측시。결과표명，경수식후적제돈과산연생물대변형련구균적항균활성교모체화합물유불동정도적제승。
Oleanolic acid belongs to pentacyclic triterpenoid compounds .It widely distributes in nature and show s many bioactivities such as anti-bacterial ,anti-inflammatory ,antiviral ,anti-tumor ,et al . However ,the research about their anti-bacterial activity are rare .In order to study the structure ac-tivity relationship of oleanolic acid and its derivatives in depth ,we take the natural product oleanolic acid with biological activity as the lead compound for modifying their structures in this paper .Six de-rivatives of oleanolic acid were designed and synthesized through modification at C-28 position of oleanolic acid .Structures of all target compounds were confirmed by IR and 1 H NMR .These com-pounds were tested antibacterial activity ,which were Staphylococcus aureus ,Methicillin-resistent staphylococcus aureus ,Quinolone-resistant ,Staphylococcus aureus ,Streptococcus mutans and Esche-richia coli .The results showed that their anti-bacterial activities for Streptococcus mutans were im-proved compared to oleanolic acid .