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弥合提取物的化学成分与生物效应之间的差距:从天然宝藏到药店货架的新贡献。

Bridging the Chemical Profiles and Biological Effects of Extracts: A New Contribution on the Road from Natural Treasure to Pharmacy Shelves.

机构信息

Department of Virology with SARS Laboratory, Medical University of Lublin, Chodzki 1, 20-093 Lublin, Poland.

Department of Natural Products Chemistry, Medical University of Lublin, 20-093 Lublin, Poland.

出版信息

Molecules. 2022 Jul 22;27(15):4694. doi: 10.3390/molecules27154694.

Abstract

is an important medicinal plant with traditional uses in the tropical zone. In the current work, we aimed to determine the chemical profiles and biological effects of extracts (methanolic and infusion (water)) from the leaves and stem bark of . The chemical components of the tested extracts were identified using LC-ESI-QTOF-MS. Biological effects were tested in terms of antioxidant (radical scavenging, reducing power, and metal chelating), enzyme inhibitory (cholinesterase, amylase, glucosidase, and tyrosinase), antineoplastic, and antiviral activities. Fifty-seven components were identified in the tested extracts, including iridoids, flavonoids, and phenolic acids as the main constituents. In general, the leaves-MeOH extract was the most active in the antioxidant assays (DPPH, ABTS, CUPRAC, FRAP, metal chelating, and phosphomolybdenum). Antineoplastic effects were tested in normal (VERO cell line) and cancer cell lines (FaDu, HeLa, and RKO). The leaf infusion, as well as the extracts obtained from stem bark, showed antineoplastic activity (CC 119.03-222.07 µg/mL). Antiviral effects were tested against HHV-1 and CVB3, and the leaf methanolic extract (500 µg/mL) exerted antiviral activity towards HHV-1, inhibiting the viral-induced cytopathic effect and reducing the viral infectious titre by 5.11 log and viral load by 1.45 log. In addition, molecular docking was performed to understand the interactions between selected chemical components and viral targets (HSV-1 DNA polymerase, HSV-1 protease, and HSV-1 thymidine kinase). The results presented suggest that may be a bright spot in moving from natural sources to industrial applications, including novel drugs, cosmeceuticals, and nutraceuticals.

摘要

是一种具有传统热带药用价值的重要药用植物。在目前的工作中,我们旨在确定叶和茎皮的提取物(甲醇和浸液(水))的化学特征和生物效应。使用 LC-ESI-QTOF-MS 鉴定了测试提取物的化学成分。从抗氧化(自由基清除、还原力和金属螯合)、酶抑制(胆碱酯酶、淀粉酶、葡萄糖苷酶和酪氨酸酶)、抗肿瘤和抗病毒活性方面测试了生物效应。在测试的提取物中鉴定了 57 种成分,包括作为主要成分的裂环烯醚萜、黄酮类和酚酸。一般来说,叶甲醇提取物在抗氧化测定(DPPH、ABTS、CUPRAC、FRAP、金属螯合和磷钼酸盐)中最活跃。在正常(VERO 细胞系)和癌细胞系(FaDu、HeLa 和 RKO)中测试了抗肿瘤作用。叶浸液以及茎皮提取物均显示出抗肿瘤活性(CC 119.03-222.07 µg/mL)。针对 HHV-1 和 CVB3 测试了抗病毒作用,叶甲醇提取物(500 µg/mL)对 HHV-1 表现出抗病毒活性,抑制病毒诱导的细胞病变效应,并使病毒感染滴度降低 5.11 log,病毒载量降低 1.45 log。此外,还进行了分子对接,以了解选定化学组分与病毒靶标的相互作用(HSV-1 DNA 聚合酶、HSV-1 蛋白酶和 HSV-1 胸苷激酶)。结果表明,可能是从天然来源向工业应用(包括新型药物、化妆品和营养保健品)发展的一个亮点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3cdc/9330408/131cbf75d48c/molecules-27-04694-g001.jpg

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