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New Metabolite With Inhibitory Activity Against α-Glucosidase and α-Amylase From Endophytic Chaetomium globosum
Natural Product Communications ( IF 1.5 ) Pub Date : 2020-07-31 , DOI: 10.1177/1934578x20941338
Jianzhao Qi 1 , Dacheng Wang 1 , Xia Yin 1 , Qiang Zhang 1 , Jin-Ming Gao 1
Affiliation  

An efficient bioactive tracking separation strategy based on liquid-liquid extraction and high-speed counter-current chromatography (HSCCC) was developed and used to isolate bioactive natural products from the endophytic fungus Chaetomium globosum residing in Ginkgo biloba. Using HSCCC, the novel metabolite chaetoglobol acid (1) as well as 11 known compounds (2-12), including 6 chlorinated azaphilones and 3 cytochalasans, were successfully isolated. The structure of compound 1 was elucidated through spectroscopic analyses and HRESIMS data. Compound 1 possesses a rare C11-polyketide skeleton. All isolates were evaluated for their α-glucosidase and α-amylase inhibitory activities in vitro. Compound 1 showed high inhibition against α-glucosidase (IC50 = 3.04 μM), 18-fold higher than that of acarbose (IC50 = 54.74 μM), and also displayed moderate inhibitory activity against α-amylase (IC50 = 22.18 μM). As the results indicated that 1 has inhibitory effects against both α-glucosidase and α-amylase, 1 may be a promising candidate for mediating type 2 diabetes.



中文翻译:

具有内生球壳球菌α-葡萄糖苷酶和α-淀粉酶抑制活性的新代谢产物

根据液-液萃取和高速逆流色谱(HSCCC)一种有效的生物活性跟踪分离的策略的开发,并从内生真菌用于分离生物活性天然产物球毛壳霉驻留在银杏。使用HSCCC,成功地分离了新型代谢物Chaetoglobol酸(1)以及11种已知化合物(2-12),其中包括6种氯化氮杂苯酮和3种细胞松弛素。通过光谱分析和HRESIMS数据阐明了化合物1的结构。化合物1具有稀有的C 11-聚酮骨架。评价所有分离株的体外α-葡萄糖苷酶和α-淀粉酶抑制活性。化合物1表现出对α葡糖苷酶高的抑制(IC 50 = 3.04μM),18倍的比阿卡波糖的较高(IC 50 = 54.74μM),并且还针对α淀粉酶显示中等抑制活性(IC 50 = 22.18μM) 。结果表明1具有对α-葡萄糖苷酶和α-淀粉酶的抑制作用,1可能是介导2型糖尿病的有希望的候选者。

更新日期:2020-07-31
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