Chemical profiling and antidiabetic potency of Paeonia delavayi: Comparison between different parts and constituents
Chemical profiling and antidiabetic potency of Paeonia delavayi: Comparison between different parts and constituents
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芍药的化学分析和抗糖尿病功效：不同部位和成分之间的比较
DOI：
10.1016/j.jpba.2021.113998
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发表时间：
2021-03-04
影响因子：
3.4
通讯作者：
Geng, Chang-An
中科院分区：
文献类型：
--
作者：
Huang, Qian;Chen, Ji-Jun;Geng, Chang-An
滇紫草（学名：Delavayi）是我国西南地区特有的一种植物，由于其形态和药理作用与牡丹相似，常被用作牡丹的替代品。在以往的研究中，木菠萝具有抗糖尿病的作用，但尚未研究木菠萝不同部位之间的化学差异和抗糖尿病的作用。本文通过LCMS分析和对α-葡萄糖苷酶、PTP 1B、TCPTP和DPP 4的抑制作用，研究了马缨丹的化学成分和抗糖尿病作用。通过紫外光谱和质谱分析，以及与对照品的比较，共鉴定出57种化合物，其中黄酮类化合物15种，单萜苷类化合物10种，三萜类化合物8种，没食子酰葡萄糖7种，含氮化合物6种，没食子酸5种，苯乙酮2种，其它4种。根据MS/MS裂解规律推测了两个新的单萜苷元（42和47）和一个新的降齐墩果烷型三萜（51）。主成分分析（PCA）表明，根芯和根皮的化学成分相似，根皮和叶、茎的特征成分（单萜苷类、黄酮类和苯乙酮类）可以很好地区分。4个部位（200 μ g/mL）对α-葡萄糖苷酶和PTP 1B均有明显抑制作用（81.2%~ 98.5%），对TCPTP和DPP 4有中至弱的抑制作用（19.5%~ 34.9%）。测定了九种化合物代表五种主要类型的化合物的抗糖尿病作用，表明黄酮类化合物和三萜类化合物是四种酶的主要活性物质。木犀草素对α-葡萄糖苷酶、PTP 1B和TCPTP有明显的抑制作用，IC 50值分别为94.6、136.3和157.3 μ M;木通酸对α-葡萄糖苷酶和PTP 1B有明显的抑制作用，IC 50值分别为73.5和57.8 μ M。木犀草素和Ake-bonic acid被认为是α-葡萄糖苷酶的竞争性抑制剂，但对PTP 1B分别是反竞争性和混合型抑制剂。对接研究表明，Akebonic酸通过与PTP 1 B的催化位点（B/C）键合而成为PTP 1 B的选择性抑制剂（优于TCPTP）。该LCMS结合酶比较为识别P. delavayi的化学特征和抗糖尿病效力开辟了新的视野。(C)2021爱思唯尔有限公司版权所有。
Paeonia delavayi (Paeoniaceae), an endemic plant mainly distributed in southwest China, is always used as the substitute of P. suffruticosa due to their morphological and pharmacological similarity. In the previous study, P. suffruticosa was revealed with antidiabetic potency, whereas the chemical difference and antidiabetic property between different parts of P. delavayi has not yet been studied. This paper was designed to clarify the chemical constituents and antidiabetic potency of P. delavayi by LCMS analysis and enzyme inhibition on alpha-glucosidase, PTP1B, TCPTP, and DPP4. By interpretation of their UV absorptions and MS fragmentations, and/or comparison with reference samples, 57 constituents comprising 15 flavonoids, 10 monoterpene glycosides, eight triterpenoids, seven galloyl glucose s, six N-containing compounds, five gallic acids, two acetophenones, and four other types of compounds were identified from the different parts of P. delavayi. Moreover, two new monoterpene aglycones (42 and 47) and one new noroleanane triterpenoid (51) were speculated by their MS/MS fragmentation rules. Principal component analysis (PCA) suggested the chemical resemblance between root core and root bark which could be well differentiated with the leaves and stems by their characteristic constituents (monoterpene glycosides, flavonoids, and acetophenones). All the four parts (200 mu g/mL) showed obvious inhibition on alpha-glucosidase and PTP1B (81.2%-98.5%), but moderate to weak inhibition on TCPTP and DPP4 (19.5%-34.9%). Nine compounds representing five main types of constituents in Paeonia plants were assayed for their antidiabetic effects, indicating flavonoids and triterpenoids were the main active substances regarding to the four enzymes. Luteolin displayed obvious activity on alpha-glucosidase, PTP1B, and TCPTP with IC50 values of 94.6, 136.3, and 157.3 mu M, and akebonic acid could inhibit alpha-glucosidase and PTP1B with IC50 values of 73.5 and 57.8 mu M. Luteolin and ake-bonic acid were recognized as competitive inhibitors of alpha-glucosidase, but anticompetitive and mix-type inhibitors of PTP1B, respectively. Docking study demonstrated akebonic acid as PTP1B (over TCPTP) selective inhibitor by bonding to the catalytic sites (B/C) of PTP1B. This LCMS combined with enzymatic comparison opens new sights for recognizing the chemical profiles and antidiabetic potency of P. delavayi. (C) 2021 Elsevier B.V. All rights reserved.