Morales-Montesinos Itzel B, Rios Maria Yolanda, Ocampo-Acuña Yordin D, Esquivel-Rodríguez Baldomero, Bustos-Brito Celia, Osorio-Ramírez María Del Carmen, Durán-Riveroll Lorena M, González-Maya Leticia
Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Av. Universidad 1001, Col. Chamilpa, Cuernavaca 62209, Mexico.
Centro de Investigaciones Químicas, IICBA, Universidad Autónoma del Estado de Morelos, Av. Universidad 1001, Col. Chamilpa, Cuernavaca 62209, Mexico.
Mar Drugs. 2025 Mar 14;23(3):127. doi: 10.3390/md23030127.
Among aquatic organisms, marine dinoflagellates are essential sources of bioactive metabolites. The benthic dinoflagellate produces metabolites that have exhibited substantial and specific cytotoxicity on cancer cells; however, isolation and identification of the purified compounds remain a challenge. This study reports biomass multi-step extraction plus chemical analyses for identifying compounds with antineoplastic activity. Through bio-directed fractionation, the cytotoxicity of extracts and fractions was tested on H1299 (lung), PC-3 (prostate), HeLa (cervical), and MCF-7 (breast) cancer cell lines. Dichloromethane (DCM) phase, hydroalcoholic (HYD) secondary extract, and methanolic (MET) extract showed cytotoxic effects on all cell lines. Active extracts and fractions were analyzed by HPLC-QTOF-MS, H, and C NMR. Cell lines H1299 and PC-3 treated with fractions F4, F7, and DCM2-AQ-Ch sub-extract showed morphological changes resembling those observed in the apoptosis control, and no signs of necrosis were observed. The selectivity of fraction F7 was above 100 μg mL for healthy cells, while cytotoxic activity was observed in cancer cells. This fraction was identified as mostly fatty acids (FA) by NMR. Seventeen compounds with reported biological activities, such as antioxidant, analgesic, antiviral, and anticancer, were identified from extracts and fractions. Among them, the phycotoxins gambieric acid A and B, okadaic acid, and dinophysistoxin-1 were detected. Further studies are needed to reveal more significant anti-cancer potential from .
在水生生物中,海洋甲藻是生物活性代谢物的重要来源。底栖甲藻产生的代谢物对癌细胞表现出显著且特异的细胞毒性;然而,纯化化合物的分离与鉴定仍然是一项挑战。本研究报告了用于鉴定具有抗肿瘤活性化合物的生物量多步提取及化学分析方法。通过生物导向分级分离,在H1299(肺癌)、PC-3(前列腺癌)、HeLa(宫颈癌)和MCF-7(乳腺癌)癌细胞系上测试了提取物和馏分的细胞毒性。二氯甲烷(DCM)相、水醇(HYD)二级提取物和甲醇(MET)提取物对所有细胞系均显示出细胞毒性作用。通过HPLC-QTOF-MS、1H和13C NMR对活性提取物和馏分进行了分析。用馏分F4、F7和DCM2-AQ-Ch亚提取物处理的H1299和PC-3细胞系显示出与凋亡对照中观察到的相似的形态变化,未观察到坏死迹象。馏分F7对健康细胞的选择性高于100μg/mL,而在癌细胞中观察到细胞毒性活性。通过NMR鉴定该馏分主要为脂肪酸(FA)。从提取物和馏分中鉴定出17种具有抗氧化、镇痛、抗病毒和抗癌等报道生物活性的化合物。其中,检测到了冈比亚酸A和B、大田软海绵酸和鳍藻毒素-1等藻毒素。需要进一步研究以揭示[原文此处不完整,未明确具体指代内容]更显著的抗癌潜力。