毛蕊花的生物活性成分及其α-葡萄糖苷酶抑制剂和 PPAR-γ 激动剂活性。

IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Fitoterapia Pub Date : 2024-10-20 DOI:10.1016/j.fitote.2024.106266
Yingbo Yang , Qian Zhang , Jia Wang , Haijun Hu , Meng Wang , Zhengtao Wang , Zhuzhen Han , Ying Xiao , Li Yang
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引用次数: 0

摘要

从三疣小檗中分离出了三种新的新蛇床子二萜(1-3)、两种新的甾体(4-5)、一种新的单萜(6)、一种新的苯甲醛衍生物(7)和一种新的鸢尾甙(8),以及 19 种已知的酚类化合物。通过详细的光谱分析(一维和二维核磁共振)和高分辨率电喷雾离子化质谱(HRESIMS),确定了这些化合物的结构。对分离出的化合物进行了α-葡萄糖苷酶抑制活性和过氧化物酶体增殖激活受体γ(PPAR-γ)激动活性的筛选,结果表明三种苯乙醇苷类化合物具有抑制α-葡萄糖苷酶和过氧化物酶体增殖激活受体γ(PPAR-γ)激动活性、马鞭草苷(9)、白果苷 a(10)和异内酯苷(13)以及芹菜素(22)和木犀草素(26)这两种黄酮类化合物对α-葡萄糖苷酶具有强效抑制作用,IC50 值在 15 到 700 μM 之间。此外,四种黄酮类化合物芹菜素 7-O-β-D-葡萄糖醛酸(19)、芹菜素(22)、木犀草素(26)和槲皮素(27)显示出显著的 PPAR-γ 激动活性,其 EC50 值在 2.3-24.9 μM 之间。
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Bioactive constituents from Clerodendrum trichotomum and their α-glucosidase inhibitory and PPAR-γ agonist activities
Three new neoclerodane diterpenoids (1–3), two new steroids (4–5), one new monoterpene (6), one new derivative of benzaldehyde (7) and one new iridoid glycoside (8), along with 19 known phenolic compounds, were isolated from Clerodendrum trichotomum. Their structures were established by a combination of detailed spectroscopic analyses (1D and 2D NMR) and high resolution electrospray ionization mass spectroscopy (HRESIMS). The isolated compounds were screened on α-glucosidase inhibitory and the peroxisome proliferator-activated receptor gamma (PPAR-γ) agonist activities, and the results showed that three phenylethanoid glycosides, verbascoside (9), leucosceptoside a (10), and isoacteoside (13), and two flavonoids, apigenin (22) and luteolin (26) showed potent inhibitory effects against α-glucosidase, with IC50 values in the range from 15 to 700 μM. In addition, four flavonoids apigenin 7-O-β-D-glucuronide (19), apigenin (22), luteolin (26), and quercetin (27) exhibited significant PPAR-γ agonistic activities with EC50 values in the range 2.3–24.9 μM.
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来源期刊
Fitoterapia
Fitoterapia 医学-药学
CiteScore
5.80
自引率
2.90%
发文量
198
审稿时长
1.5 months
期刊介绍: Fitoterapia is a Journal dedicated to medicinal plants and to bioactive natural products of plant origin. It publishes original contributions in seven major areas: 1. Characterization of active ingredients of medicinal plants 2. Development of standardization method for bioactive plant extracts and natural products 3. Identification of bioactivity in plant extracts 4. Identification of targets and mechanism of activity of plant extracts 5. Production and genomic characterization of medicinal plants biomass 6. Chemistry and biochemistry of bioactive natural products of plant origin 7. Critical reviews of the historical, clinical and legal status of medicinal plants, and accounts on topical issues.
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