Wirasathien L, Pengsuparp T, Suttisri R, Ueda H, Moriyasu M, Kawanishi K
Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand.
Phytomedicine. 2007 Aug;14(7-8):546-50. doi: 10.1016/j.phymed.2006.09.001. Epub 2006 Nov 3.
Two dihydroflavonol glycosides, engeletin and astilbin, were isolated from an EtOAc extract of the leaves of Stelechocarpus cauliflorus R.E. Fr. (Annonaceae). The inhibitory activity of engeletin against a recombinant human aldose reductase (IC50 value=1.16 microM) was twice that of quercetin as a positive control (2.48 microM), and 23 times greater than that of astilbin (26.7 microM). Engeletin inhibited the enzyme uncompetitively. Astilbin was about as potent as the positive control, quercetin, in its inhibition of advanced glycation end-products formation. These flavonoids displayed therapeutic potential in the prevention and treatment of diabetic complications.
从番荔枝科植物多蕊含笑（Stelechocarpus cauliflorus R.E. Fr.）叶的乙酸乙酯提取物中分离得到了两种二氢黄酮醇苷，即恩格勒亭和落新妇苷。作为阳性对照的槲皮素对重组人醛糖还原酶的抑制活性（IC50值 = 2.48 μM），而恩格勒亭的抑制活性（IC50值 = 1.16 μM）是其两倍，且比落新妇苷（26.7 μM）高23倍。恩格勒亭对该酶的抑制作用为非竞争性抑制。落新妇苷在抑制晚期糖基化终产物形成方面的效力与阳性对照槲皮素相当。这些黄酮类化合物在预防和治疗糖尿病并发症方面显示出治疗潜力。
