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目的:针对潜在肿瘤治疗靶点sirtuin5(SIRT5),从天然产物中筛选出SIRT5抑制剂。方法:利用SIRT5的去琥珀酰化酶反应活性,建立HPLC活性检测方法,并对已有天然产物库进行SIRT5抑制剂的筛选以及IC50的测定。结果:发现含羧基的刺囊酸、齐墩果酸的IC50值分别为40和70μmol·L-1。结论:齐墩果酸、刺囊酸等天然产物对SIRT5具有较显著的抑制活性,为进一步的SIRT5靶向药物化学研究奠定了基础。
OBJECTIVE: To screen for sirtuin5 (SIRT5), a potential tumor therapeutic target, and to screen for SIRT5 inhibitors from natural products. Methods: The activity of desmokyase of SIRT5 was used to establish the HPLC method for the determination of the activity of SIRT5. The screening of SIRT5 inhibitors and the determination of IC50 were carried out on the existing natural product pools. Results: The IC50 values of carboxyl group-containing echinocystic acid and oleanolic acid were found to be 40 and 70 μmol·L-1, respectively. CONCLUSION: Oleanolic acid, echinocystic acid and other natural products have significant inhibitory activity on SIRT5, which lays the foundation for further SIRT5 targeted drug chemistry research.