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通过生物活性导向分级分离和液相色谱-串联质谱法从松茎和(布兰科)梅里尔与罗尔夫树皮中筛选出的抗糖尿病和抗炎生物活性成分。

Anti-diabetic and anti-inflammatory bioactive hits from Matsum. stem and (Blanco) Merr. & Rolfe bark through bioassay-guided fractionation and liquid chromatography-tandem mass spectrometry.

作者信息

Fabian Mavis Colleen Porciuncula, Astorga Rezzaira Marie Neduelan, Atis Arnelson Arwin Gray, Pilapil Luis Agustin Elido, Hernandez Christine Chichioco

机构信息

Bioorganic and Natural Products Laboratory, Institute of Chemistry, University of the Philippines Diliman, Quezon City, Philippines.

出版信息

Front Pharmacol. 2024 Mar 8;15:1349725. doi: 10.3389/fphar.2024.1349725. eCollection 2024.

Abstract

Women have been found to be at a higher risk of morbidity and mortality from type 2 diabetes mellitus (T2DM) and asthma. α-Glucosidase inhibitors have been used to treat T2DM, and arachidonic acid 15-lipoxygenase (ALOX15) inhibitors have been suggested to be used as treatments for asthma and T2DM. Compounds that inhibit both enzymes may be studied as potential treatments for people with both T2DM and asthma. This study aimed to determine potential anti-diabetic and anti-inflammatory bioactive hits from Matsum. stem and (Blanco) Merr. & Rolfe bark. A bioassay-guided fractionation framework was used to generate bioactive fractions from stem and bark. Subsequently, dereplication through ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) and database searching was performed to putatively identify the components of one bioactive fraction from each plant. Seven compounds were putatively identified from the stem active fraction, and six of these compounds were putatively identified from this plant for the first time. Nine compounds were putatively identified from the bark active fraction, and seven of these compounds were putatively identified from this plant for the first time. One putative compound from the stem active fraction (corilagin) has been previously reported to have inhibitory activity against both α-glucosidase and 15-lipoxygenase-1. It is suggested that further studies on the potential of corilagin as an anti-diabetic and anti-inflammatory treatment should be pursued based on its several beneficial pharmacological activities and its low reported toxicity.

摘要

研究发现,女性患2型糖尿病(T2DM)和哮喘的发病及死亡风险更高。α-葡萄糖苷酶抑制剂已用于治疗T2DM,花生四烯酸15-脂氧合酶(ALOX15)抑制剂也被建议用于治疗哮喘和T2DM。抑制这两种酶的化合物可作为同时患有T2DM和哮喘的患者的潜在治疗药物进行研究。本研究旨在从水团花茎和九节树皮中确定潜在的抗糖尿病和抗炎生物活性成分。采用生物测定指导的分级分离框架从水团花茎和九节树皮中生成生物活性级分。随后,通过超高效液相色谱-串联质谱(UHPLC-MS/MS)和数据库搜索进行去重复,以推定鉴定每种植物中一个生物活性级分的成分。从水团花茎活性级分中推定鉴定出7种化合物,其中6种化合物首次从该植物中推定鉴定出来。从九节树皮活性级分中推定鉴定出9种化合物,其中7种化合物首次从该植物中推定鉴定出来。水团花茎活性级分中的一种推定化合物(柯里拉京)此前已报道具有对α-葡萄糖苷酶和15-脂氧合酶-1的抑制活性。鉴于柯里拉京具有多种有益的药理活性且报道的毒性较低,建议对其作为抗糖尿病和抗炎治疗的潜力进行进一步研究。

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