Excochinlignan: A new coumarino lignan from Excoecaria cochinchinensis Lour

IF 3.1 4区 医学 Q3 CHEMISTRY, MEDICINAL
Huong Thi Thu Le, Phan-Si-Nguyen Dong, Le-Thuy-Thuy-Trang Hoang, Hoai-Vu Nguyen-Si, Hoang-Vinh-Truong Phan, Thi-Minh-Thao Vo, Thi-Tu-Linh Tran, Tin-Thanh Le, Van-Kieu Nguyen
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Abstract

Excoecaria cochinchinensis Lour. is a well-known medicinal plant in Vietnam, whose parts, particularly leaves, are applied as essential medicine in folk remedies. In this study, the chemical constituents of the plant’s aerial parts, together with their feasibility in enzyme inhibition and antioxidants, were investigated. Seven compounds, including a new coumarino lignan – excochinlignan (1), five known flavonol derivatives (2-6) and one monophenolic (7), were isolated and identified via chromatographic and spectroscopic approaches. In vitro biological evaluation of these compounds revealed the potential of kaempferol (2) and its glycosides (3-6) in all assays. Among them, kaempferol (2) was determined as the most active antioxidant (IC50 2.86 μM) while its 3-O-xylose derivatives (3) displayed the most significant α-glucosidase (IC50 65.88 μM) and tyrosinase (IC50 58.97 μM) inhibition. In silico evaluation via molecular docking simulation suggested the supportive effect of 3-O-xylose, C-4′ hydroxyl and C-4 ketone moieties in the structure of the isolated flavanols (2-6) on their enzyme inhibition and antioxidant properties.

香豆素:一种新的香豆素
胭脂虫(Excoecaria cochinchinensis)在越南是一种著名的药用植物,其部分,特别是叶子,被用作民间偏方的基本药物。在本研究中,研究了植物地上部分的化学成分,以及它们在酶抑制和抗氧化剂方面的可行性。通过色谱和光谱方法分离鉴定了7个化合物,其中包括一种新的香豆素木脂素-外cochin木脂素(1)、5种已知的黄酮醇衍生物(2-6)和1种单酚类化合物(7)。这些化合物的体外生物学评价显示山奈酚(2)及其糖苷(3-6)在所有检测中的潜力。其中山奈酚(2)对α-葡萄糖苷酶(IC50为2.86 μM)和酪氨酸酶(IC50为58.97 μM)的抑制作用最强,其3- o -木糖衍生物(3)对α-葡萄糖苷酶(IC50为65.88 μM)和酪氨酸酶(IC50为58.97 μM)的抑制作用最强。通过分子对接模拟的硅评价表明,分离的黄烷醇(2-6)结构中的3- o -木糖、C-4 '羟基和C-4酮部分对其酶抑制和抗氧化性能有支持作用。
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来源期刊
Medicinal Chemistry Research
Medicinal Chemistry Research 医学-医药化学
CiteScore
4.70
自引率
3.80%
发文量
162
审稿时长
5.0 months
期刊介绍: Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.
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