烹调用香草（迷迭香）中生物活性物质在2型糖尿病治疗中对二肽基肽酶IV等分子靶向目标的抑制作用

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Journal of Agricultural and Food Chemistry

《农业与食品化学杂志》

Bioactive Compounds from Culinary Herbs Inhibit a Molecular Target for Type 2 Diabetes Management, Dipeptidyl Peptidase IV

烹调用香草（迷迭香）中生物活性物质在2型糖尿病治疗中对二肽基肽酶IV等分子靶向目标的抑制作用 

Allyson M. Bower,^† Luis M. Real Hernandez,^‡ Mark A. Berhow,^§ and Elvira Gonzalez de Mejia*^,†,‡ 

^†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

^§United States Department of Agriculture Agricultural Research Service, 1815 North University Street, Peoria, Illinois 61604, United States

^†营养科学部和^‡食品科学与人类营养学系，伊利诺伊大学香槟分校，228 ERML，西格里高利大街1201号，乌尔班纳，61801年伊利诺斯州，美国

^§美国农业部农业研究局，1815北大学街，皮奥里亚，伊利诺斯州61604，美国

 

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、马郁兰、迷迭香和墨西哥牛至富含多种生物活性物质。本文的主要目的是对温室种植的（新鲜的）或商业用途的（干燥的）香草提取物抑制二肽基肽酶IV和蛋白酪氨酸磷酸酶1B的能力进行表征和检测。酶在胰岛素的分泌和胰岛素信号通路中均扮演了重要的角色。与商业用途的（干燥的）香草相比，温室种植的（新鲜的）香草含有更多的茶多酚(每毫克提取物干重中302.7–430.1微克没食子酸当量)和黄酮类物质(每毫克提取物干重中370.1–661.4微克芦丁当量) 。温室种植的（新鲜的）迷迭香、墨西哥牛至和马郁兰提取物(半抑制浓度分别为16、29和59) 是二肽基肽酶IV最好的抑制剂。商业用途的（干燥的）迷迭香、墨西哥牛至和马郁兰 (32.4–40.9% at 500 μM) 是蛋白酪氨酸磷酸酶1B最好的抑制剂。通过LC–ESI-MS（液质联用）可从温室种植的（新鲜的）墨西哥牛至和迷迭香中分析出圣草酚、柚皮素、黄酮、蓟黄素和鼠尾草酚成分。计算模型显示出黄酮、鼠尾草酚和圣草酚对DPP-IV具有最佳亲和性。从生物化学上来说，DPP-IV最好的抑制剂是蓟黄素(IC₅₀ = 0.43 ± 0.07 μM)、黄酮(IC₅₀ = 0.49 ± 0.06 μM)和柚皮素(IC₅₀ = 2.5 ± 0.29 μM)。总的说来，香草中含有可抑制DPP-IV的多种黄酮类物质，其在糖尿病治疗方面的潜在功效还需进行更深入的研究。

KEYWORDS: hispidulin, marjoram, oregano, rosemary, type 2 diabetes mellitus, DPP-IV, PTP1B

关键词：黄酮、马郁兰、牛至、迷迭香、2型糖尿病、二肽基肽酶IV、蛋白酪氨酸磷酸酶1B

 

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