Aurones作为抗糖尿病药物及其益生元活性

Reham M. Samra, Mohamed S. Darwish, Noha A. Abou-Zeid, E. Khojah, V. Imieje, A. Zaki
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引用次数: 1

摘要

沙柏在传统医学中被用作润肤剂、利尿剂、镇痛剂、驱虫药和其他疾病。此外,一些生物活性的植物提取物和分离的代谢物已被报道。对其气相部位的乙酸乙酯提取物进行色谱分析,首次从该植物中分离到3个aurone衍生物(1-3)。它们的结构通过1D和2D NMR技术以及质谱鉴定为金黄色葡萄素(1)、金黄色葡萄素-4-甲基醚(2)和5-甲基金黄色葡萄素(3)。这些化合物对代谢性疾病,特别是糖尿病中至关重要的酶,如α-淀粉酶、α-葡萄糖苷酶和糖原磷酸化酶的抑制活性进行了测试。结果以抑制率表示。通过计算对接研究分析了aurones对所测酶的抑制活性,为观察结果提供了合理的解释。所测化合物与所测酶活性位点残基在氢键和疏水相互作用方面形成稳定的相互作用,结果与体外抗糖尿病活性一致。通过测定益生元活性评分(Pscore),以副干酪乳杆菌(Lacticaseibacillus paracasei)和鼠李糖乳杆菌(lactoaseibacillus rhamnosus)两种益生元活性来评估化合物支持有益菌生长和活力的能力。本研究结果表明,沙棘是一种潜在的天然生物活性物质来源。然而,有必要在体内测试,以评估该植物的功效,为未来开发新的药物实体。
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Aurones as Antidiabetic Agents and Their Prebiotic Activities
Cyperus conglomeratus has been utilized in traditional medicine as an emollient, diuretic, analgesic, anthelmintic, and for other diseases. Furthermore, several biological activities have been reported for the plant extract and the isolated metabolites. The chromatographic investigation of an ethyl acetate extract of the aerial parts led to the isolation of three aurone derivatives (1–3) from the plant for the first time. Their structures were identified as aureusidin (1), aureusidin-4-methyl ether (2), and 5-methyl aureusidin (3) using 1D and 2D NMR techniques, along with mass spectrometry. The compounds were tested for their inhibitory activities against enzymes vital in metabolic diseases, especially diabetes, such as α-amylase, α-glucosidase, and glycogen phosphorylase. The results were expressed as percentage inhibition. The inhibitory activity of aurones against the tested enzymes was also analyzed by computational docking studies to provide a rational explanation for the observed results. The tested compounds formed stable interactions in terms of hydrogen bonding and hydrophobic interaction with the active site residues of the tested enzymes, and the results are in agreement with those of the in vitro antidiabetic activity. The compounds were also evaluated for their ability to support the growth and viability of beneficial bacteria in terms of prebiotic activities using two species, Lacticaseibacillus paracasei and Lacticaseibacillus rhamnosus, through the determination of prebiotic activity scores (Pscore). The findings of this study showed that C. conglomeratus is a potential natural source of bioactive agents. There is, however, a need for in vivo testing to evaluate this plant’s efficacy for developing new drug entities in the future.
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