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New pregnane glycosides from Caralluma hexagona Lavranos and their in vitro α-glucosidase and pancreatic lipase inhibitory effects
Phytochemistry Letters ( IF 1.3 ) Pub Date : 2020-01-23 , DOI: 10.1016/j.phytol.2020.01.015
Akram A. Shalabi , Ali M. El Halawany , Mouchira A. Choucry , Fatma S. El-Sakhawy , Hiroyuki Morita , Dae-Won Ki , Essam Abdel-Sattar

Three new pregnane glycosides in addition to four known compounds were isolated from the methylene chloride fraction of Caralluma hexagona Lavranos using bioassay-guided fractionation. The new compounds were identified as 12,20-di-O-benzoyl-3β,8β,12β,14β,20-pentahydroxy-(20R)-pregn-5-ene-3-O-β-d-glucopyranosyl-(1→4)-β-d-digitaloside (1), 3β,8β,14β,20-tetrahydroxy (20R)-pregn-5-ene-3-O-β-d-glucopyranosyl-(1→4)-O-β-d-digitaloside-20-O-βd-glucopyranoside (2), 3β,8β,14β,20-tetrahydroxy-(20R)-pregn-5-ene-3-O-β-d-glucopyranosyl-(1→6)-O-β-d-glucopyranosyl-(1→4)-O-β-d-digitaloside-20-O-βd-glucopyranoside (3), along with the known compounds luteolin 4`-O-neohesperidoside (4), apigenin-8-C-neohesperoside (5), β-sitosterol (6) and β-sitosterol glucoside (7). Preliminary studies of the crude methanolic extract and methylene chloride fraction showed inhibitory effects against α-glucosidase and pancreatic lipase. Among the isolated compounds, compound 5 showed the most potent α-glucosidase inhibition with IC50 value of 0.82 ± 2.50 μM compared to acarbose (0.81 ± 0.86 μM). Whereas compound 1 showed the highest inhibitory activity on pancreatic lipase with an IC50 value of 23.59 ± 2.49 μM compared to orlistat (7.41 ± 2.26 μM).



中文翻译:

六倍体香葱新孕烷糖苷及其体外α-葡萄糖苷酶和胰脂肪酶的抑制作用

使用生物测定指导的分馏方法,从六倍体Carallumahexaa Lavranos的二氯甲烷馏分中分离出三种新的孕烷糖苷。新的化合物,分别为12,20二ø -苯甲酰基-3 β,8 β,12 β,14 β,20-pentahydroxy-(20 - [R )-孕-5-烯-3- ø - β - d -glucopyranosyl-(1→4) - β - d -digitaloside (1), 3 β,8 β,14 β,20四羟基(20 - [R )-孕-5-烯-3- ö- β - d -glucopyranosyl-(1→4) - ø - β - d -digitaloside -20- ø - β - d吡喃葡萄糖苷(2),3 β,8个β,14 β,20-四羟基(20 - [R) -孕-5-烯-3- ø - β - d -glucopyranosyl-(1→6) - ø - β - d -glucopyranosyl-(1→4) - ø - β - d -digitaloside -20- ø - β - d-葡吡喃糖苷(3)以及已知化合物木犀草素4`- O-新芥子苷(4),芹菜素-8- C-新芥子苷(5)β-谷甾醇(6)β-谷甾醇糖苷(7)。对粗甲醇提取物和二氯甲烷馏分的初步研究表明,其对α-葡萄糖苷酶和胰腺脂肪酶具有抑制作用。在分离的化合物中,与阿卡波糖(0.81±0.86μM)相比,化合物5表现出最有效的α-葡萄糖苷酶抑制作用,IC 50值为0.82±2.50μM。而复合与奥利司他(7.41±2.26μM)相比,图1显示了对胰腺脂肪酶的最高抑制活性,IC 50值为23.59±2.49μM。

更新日期:2020-01-23
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