Pharmacognosy Research Laboratories, Medway School of Science, University of Greenwich , Chatham-Maritime, Kent, UK.
Pharm Biol. 2012 Dec;50(12):1519-22. doi: 10.3109/13880209.2012.688838. Epub 2012 Sep 14.
During the last few decades, the prevalence of obesity in the western world has dramatically increased with epidemic proportions. Hand in hand with this statistic, the incidences of obesity-linked diseases such as diabetes are increasing with pandemic rate. The search for novel drugs and nutritional intervention approaches for obesity is now of significant importance.
The anti-obesity potential of eriodictyol (ERD) and its close structural analogue, sigmoidin A (SGN), were evaluated. SGN was isolated from Erythrina abyssinica Lam. ex DC. (Fabaceae).
Concentrations between 300 and 0.1 µM of test samples and reference drugs made in three-fold dilutions were tested for enzyme inhibitory effects. The major obesity target, pancreatic lipase, was used to test the anti-obesity potential while the selective effects of the compounds were determined through assessments of effects on α-glucosidase.
The inhibitory effect of SGN on pancreatic lipase (IC₅₀, 4.5 ± 0.87 µM) was 30-times greater than that of ERD (IC₅₀, 134 ± 19.39 µM) while their effect on α-glucosidase enzyme was comparable (IC₅₀ value of 62.5 ± 9.47 and 57.5 ± 13.15 µM). The anti-obesity drug, orlistat, inhibited pancreatic lipase with an IC₅₀ value of 0.3 ± 0.04 µM, while the anti-diabetic drug, acarbose, inhibited α-glucosidase with an IC₅₀ value of 190.6 ± 16.05 µM.
Although less active than the standard anti-obesity drug, orlistat, the observed activity indicated that prenylation of the flavonoid skeleton potently enhances anti-lipase activity.
Such groups of flavonoids need to be further investigated for their therapeutic and nutritional benefit in combating obesity problems.
在过去的几十年中，西方世界的肥胖症患病率呈爆炸性增长。与此统计数据相伴的是，肥胖相关疾病（如糖尿病）的发病率也呈流行趋势上升。因此，寻找新型药物和营养干预方法来治疗肥胖症变得至关重要。
评估橘皮苷（ERD）及其紧密结构类似物西格马因 A（SGN）的抗肥胖潜力。SGN 是从 Erythrina abyssinica Lam. ex DC.（Fabaceae）中分离出来的。
用 3 倍稀释法测试浓度在 300 到 0.1μM 之间的测试样品和参考药物的酶抑制作用。主要肥胖靶标——胰腺脂肪酶，用于测试抗肥胖潜力，同时通过评估对α-葡萄糖苷酶的影响来确定化合物的选择性作用。
SGN 对胰腺脂肪酶的抑制作用（IC₅₀，4.5 ± 0.87μM）比 ERD 强 30 倍（IC₅₀，134 ± 19.39μM），而它们对α-葡萄糖苷酶的作用相当（IC₅₀值分别为 62.5 ± 9.47 和 57.5 ± 13.15μM）。抗肥胖药物奥利司他对胰腺脂肪酶的抑制作用 IC₅₀ 值为 0.3 ± 0.04μM，而抗糖尿病药物阿卡波糖对α-葡萄糖苷酶的抑制作用 IC₅₀ 值为 190.6 ± 16.05μM。
尽管不如标准抗肥胖药物奥利司他活跃，但观察到的活性表明，黄酮骨架的 prenylation 强烈增强了抗脂肪酶活性。
需要进一步研究此类黄酮类化合物在治疗和营养方面对抗肥胖问题的益处。
