Murrieta-Dionicio Ulises, Calzada Fernando, Barbosa Elizabeth, Valdés Miguel, Reyes-Trejo Benito, Zuleta-Prada Holber, Guerra-Ramírez Diana, Del Río-Portilla Federico
Laboratorio de Productos Naturales, Área de Química, Departamento de Preparatoria Agrícola, Universidad Autónoma Chapingo, km 38.5 Carretera México-Texcoco, Chapingo 56230, Mexico.
Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades, 2° Piso CORSE Centro Médico Nacional Siglo XXI, IMSS, Av. Cuauhtémoc 330, Col. Doctores, Ciudad de México 06725, Mexico.
Molecules. 2024 Nov 28;29(23):5636. doi: 10.3390/molecules29235636.
Diseases caused by intestinal parasites such as protozoa represent a worldwide problem mainly for developing countries. From morbidity in different groups of people to cases of mortality in children and/or immunocompromised patients. In addition to the above, there is growing resistance to the drugs used in the treatment of these diseases, as well as undesirable side effects in patients. Therefore, there is an interest in the search for new alternatives for the base and/or development of new drugs with antiparasitic activities without harmful effects. In this sense, natural products offer to be a diverse source of compounds with biological activities. In this work, we describe the isolation and elucidation by 1D and 2D NMR spectroscopy of three cyclopeptides obtained from seeds of Saff.: cherimolacyclopeptide D (), squamin D (), and squamin C (). The fractions enriched in cyclopeptides, as well as a pure compound (), showed antiprotozoal activity against Schaudinn and Kunstler in vitro assays, with values of IC = 3.49 and 5.39 μg mL, respectively. The molecular docking study revealed that has a strong interaction with targets used, including aldose reductase and PFOR enzymes. The antiprotozoal activity of cherimolacyclopeptide D is reported for the first time in this study.
由原生动物等肠道寄生虫引起的疾病是一个全球性问题，主要影响发展中国家。从不同人群的发病率到儿童和/或免疫功能低下患者的死亡率。除此之外，用于治疗这些疾病的药物耐药性不断增加，患者还会出现不良副作用。因此，人们有兴趣寻找新的药物研发基础和/或开发具有抗寄生虫活性且无有害影响的新药。从这个意义上说，天然产物是具有生物活性化合物的多样来源。在这项工作中，我们描述了通过一维和二维核磁共振光谱从番荔枝种子中分离和鉴定出的三种环肽：番荔枝环肽D（）、鳞甲素D（）和鳞甲素C（）。富含环肽的馏分以及一种纯化合物（）在体外试验中对肖丁氏菌和昆氏菌显示出抗原虫活性，IC值分别为3.49和5.39 μg/mL。分子对接研究表明，与所使用的靶点包括醛糖还原酶和磷酸转乙酰酶有强烈相互作用。本研究首次报道了番荔枝环肽D的抗原虫活性。
