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烹饪香草中的生物活性化合物可抑制2型糖尿病治疗的分子靶点——二肽基肽酶IV。

Bioactive compounds from culinary herbs inhibit a molecular target for type 2 diabetes management, dipeptidyl peptidase IV.

作者信息

Bower Allyson M, Real Hernandez Luis M, Berhow Mark A, de Mejia Elvira Gonzalez

机构信息

Division of Nutritional Sciences and ‡Department of Food Science and Human Nutrition, University of Illinois at Urbana-Champaign , 228 ERML, 1201 West Gregory Avenue, Urbana, Illinois 61801, United States.

出版信息

J Agric Food Chem. 2014 Jul 2;62(26):6147-58. doi: 10.1021/jf500639f. Epub 2014 Jun 13.

Abstract

Greek oregano (Origanum vulgare), marjoram (Origanum majorana), rosemary (Rosmarinus officinalis), and Mexican oregano (Lippia graveolens) are concentrated sources of bioactive compounds. The aims were to characterize and examine extracts from greenhouse-grown or commercially purchased herbs for their ability to inhibit dipeptidyl peptidase IV (DPP-IV) and protein tyrosine phosphatase 1B (PTP1B), enzymes that play a role in insulin secretion and insulin signaling, respectively. Greenhouse herbs contained more polyphenols (302.7-430.1 μg of gallic acid equivalents/mg of dry weight of extract (DWE)) and flavonoids (370.1-661.4 μg of rutin equivalents/mg of DWE) compared to the equivalent commercial herbs. Greenhouse rosemary, Mexican oregano, and marjoram extracts were the best inhibitors of DPP-IV (IC₅₀=16, 29, and 59 μM, respectively). Commercial rosemary, Mexican oregano, and marjoram were the best inhibitors of PTP1B (32.4-40.9% at 500 μM). The phytochemicals eriodictyol, naringenin, hispidulin, cirsimaritin, and carnosol were identified by LC-ESI-MS as being present in greenhouse-grown Mexican oregano and rosemary. Computational modeling indicated that hispidulin, carnosol, and eriodictyol would have the best binding affinities for DPP-IV. Biochemically, the best inhibitors of DPP-IV were cirsimaritin (IC₅₀=0.43±0.07 μM), hispidulin (IC₅₀=0.49±0.06 μM), and naringenin (IC₅₀=2.5±0.29 μM). Overall, herbs contain several flavonoids that inhibit DPP-IV and should be investigated further regarding their potential in diabetes management.

摘要

希腊牛至(牛至)、马郁兰(甜牛至)、迷迭香(迷迭香)和墨西哥牛至(灰莉)是生物活性化合物的浓缩来源。目的是对温室种植或商业购买的草药提取物进行表征和检测,以评估它们抑制二肽基肽酶IV(DPP-IV)和蛋白酪氨酸磷酸酶1B(PTP1B)的能力,这两种酶分别在胰岛素分泌和胰岛素信号传导中起作用。与同等的商业草药相比,温室草药含有更多的多酚(302.7 - 430.1微克没食子酸当量/毫克提取物干重(DWE))和黄酮类化合物(370.1 - 661.4微克芦丁当量/毫克DWE)。温室迷迭香、墨西哥牛至和马郁兰提取物是DPP-IV的最佳抑制剂(IC₅₀分别为16、29和59微摩尔)。商业迷迭香、墨西哥牛至和马郁兰是PTP1B的最佳抑制剂(在500微摩尔时为32.4 - 40.9%)。通过LC-ESI-MS鉴定出植物化学物质圣草酚、柚皮素、异鼠李素、橙皮素和鼠尾草酸存在于温室种植的墨西哥牛至和迷迭香中。计算模型表明,异鼠李素、鼠尾草酸和圣草酚对DPP-IV具有最佳的结合亲和力。从生化角度来看,DPP-IV的最佳抑制剂是橙皮素(IC₅₀ = 0.43±0.07微摩尔)、异鼠李素(IC₅₀ = 0.49±0.06微摩尔)和柚皮素(IC₅₀ = 2.5±0.29微摩尔)。总体而言,草药含有几种抑制DPP-IV的黄酮类化合物,应进一步研究它们在糖尿病管理中的潜力。

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