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从叶片中分离出的新型鞘脂类化合物及其他成分的抗菌和细胞毒性活性

Antibacterial and cytotoxic activities of new sphingolipids and other constituents isolated from leaves.

作者信息

Nocedo-Mena Deyani, Rivas-Galindo Verónica M, Navarro Patricia, Garza-González Elvira, González-Maya Leticia, Ríos María Yolanda, García Abraham, Ávalos-Alanís Francisco G, Rodríguez-Rodríguez José, Camacho-Corona María Del Rayo

机构信息

Universidad Autónoma de Nuevo León, Facultad de Ciencias Químicas. Av. Universidad S/N, Ciudad Universitaria, 66451, San Nicolás de los Garza, Nuevo León, Mexico.

Department of Organic Chemistry II, University of the Basque Country UPV/EHU, 48940, Leioa, Spain.

出版信息

Heliyon. 2020 Aug 29;6(8):e04671. doi: 10.1016/j.heliyon.2020.e04671. eCollection 2020 Aug.

Abstract

is used in traditional Mexican medicine to treat certain ailments, infectious or cancerous diseases. Excepting for our previous research, this species had no scientific reports validating its traditional use. In this study, we evaluated the antibacterial and cytotoxic properties of the phingolipids and others phytocompounds isolated from leaves to increase the scientific knowledge of the Mexican flora. The antibacterial activity was evaluated against Gram-positive and Gram-negative bacteria by the Microdilution method. Meanwhile, the cytotoxic potential was determined on six human cancer cells: PC3, Hep3B, HepG2, MCF7, A549, and HeLa; using an aqueous solution cell proliferation assay kit. A cell line of immortalized human hepatocytes (IHH) was included as a control of non-cancerous cells. Selectivity index (SI) was determined only against the hepatocellular carcinoma cell lines. The phytochemical investigation of leaves resulted in the isolation and characterization of five compounds: 2-(2'-hydroxydecanoyl amino)-1,3,4-hexadecanotriol-8-ene , 2,3-dihydroxypropyl tetracosanoate , -sitosterol-D-glucopyranoside , -amyrin-3---D-glucopyranoside , and a mixture of cerebrosides . Until now, this is the first report of the sphingolipids , and . Only the compound and cerebrosides exhibited antibacterial activity reaching a MIC value of 100 μg/mL against resistant to carbapenems. While, the acetylated derivate of , compound showed the best cytotoxic result against PC3 (IC = 43 ± 4 μg/mL) and Hep3B (IC = 49.0 ± 4 μg/mL) cancer cell lines. Likewise, achieved better SI values on HepG2 and Hep3B cell lines. This research reveals the importance of study medicinal plants, to identify bioactive molecules as sources of potential drugs. The presence of these compounds allows us to justify the use of this plant in traditional Mexican medicine.

摘要

在墨西哥传统医学中用于治疗某些疾病,包括传染性疾病或癌症。除了我们之前的研究外,该物种没有科学报告证实其传统用途。在本研究中,我们评估了从叶片中分离出的鞘脂和其他植物化合物的抗菌和细胞毒性特性,以增加对墨西哥植物群的科学认识。通过微量稀释法评估对革兰氏阳性和革兰氏阴性细菌的抗菌活性。同时,使用水溶液细胞增殖测定试剂盒,在六种人类癌细胞上测定细胞毒性潜力:PC3、Hep3B、HepG2、MCF7、A549和HeLa;将永生化人类肝细胞(IHH)细胞系作为非癌细胞的对照。仅针对肝癌细胞系确定选择性指数(SI)。对叶片的植物化学研究导致分离和鉴定了五种化合物:2-(2'-羟基癸酰氨基)-1,3,4-十六碳三烯-8-醇、2,3-二羟基丙基二十四烷酸酯、β-谷甾醇-D-葡萄糖苷、α-香树脂醇-3-O-β-D-葡萄糖苷和脑苷脂混合物。到目前为止,这是鞘脂、[具体名称1]和[具体名称2]的首次报告。只有化合物[具体名称3]和脑苷脂混合物表现出抗菌活性,对碳青霉烯耐药的[细菌名称]的最低抑菌浓度值达到100μg/mL。而化合物[具体名称4],即[具体名称3]的乙酰化衍生物,对PC3(IC50 = 43 ± 4μg/mL)和Hep3B(IC50 = 49.0 ± 4μg/mL)癌细胞系显示出最佳的细胞毒性结果。同样,[具体名称5]在HepG2和Hep3B细胞系上获得了更好的SI值。这项研究揭示了研究药用植物以鉴定作为潜在药物来源的生物活性分子的重要性。这些化合物的存在使我们能够证明这种植物在墨西哥传统医学中的用途是合理的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e131/7475184/1fd97ff41550/gr1.jpg

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