当前位置：
X-MOL 学术
›
J. Nat. Prod.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Target Separation and Potential Anticancer Activity of Withanolide-Based Glucose Transporter Protein 1 Inhibitors from Physalis angulata var. villosa
Journal of Natural Products ( IF 3.3 ) Pub Date : 2023-12-20 , DOI: 10.1021/acs.jnatprod.3c00613 Jinghan Zhang 1 , Xiao Xu 1 , Yu Zhao 1 , Chunling Ren 1 , Mengzhen Gu 1 , Haili Zhang 1 , Peiye Wu 1 , Yun Wang 1 , Lingyi Kong 1 , Chao Han 1
Journal of Natural Products ( IF 3.3 ) Pub Date : 2023-12-20 , DOI: 10.1021/acs.jnatprod.3c00613 Jinghan Zhang 1 , Xiao Xu 1 , Yu Zhao 1 , Chunling Ren 1 , Mengzhen Gu 1 , Haili Zhang 1 , Peiye Wu 1 , Yun Wang 1 , Lingyi Kong 1 , Chao Han 1
Affiliation
|
The glucose transporter 1 (GLUT1) protein is involved in the basal-level absorption of glucose in tumor cells. Inhibiting GLUT1 decreases tumor cell proliferation and induces tumor cell damage. Natural GLUT1 inhibitors have been studied only to a small extent, and the structures of known natural GLUT1 inhibitors are limited to a few classes of natural products. Therefore, discovering and researching other natural GLUT1 inhibitors with novel scaffolds are essential. Physalis angulata L. var. villosa is a plant known as Mao-Ku-Zhi (MKZ). Withanolides are the main phytochemical components of MKZ. MKZ extracts and the components of MKZ exhibited antitumor activity in recent pharmacological studies. However, the antitumor-active components of MKZ and their molecular mechanisms remain unknown. A cell membrane-biomimetic nanoplatform (CM@Fe3O4/MIL-101) was used for target separation of potential GLUT1 inhibitors from MKZ. A new withanolide, physagulide Y (2), together with six known withanolides (1, 3–7), was identified as a potential GLUT1 inhibitor. Physagulide Y was the most potent GLUT1 inhibitor, and its antitumor activity and possible mechanism of action were explored in MCF-7 human cancer cells. These findings advance the development of technologies for the targeted separation of natural products and identify a new molecular framework for the investigation of natural GLUT1 inhibitors.
中文翻译：
酸浆中基于茄内酯的葡萄糖转运蛋白 1 抑制剂的靶标分离和潜在抗癌活性绒毛
葡萄糖转运蛋白 1 (GLUT1) 蛋白参与肿瘤细胞中葡萄糖的基础水平吸收。抑制 GLUT1 可减少肿瘤细胞增殖并诱导肿瘤细胞损伤。天然 GLUT1 抑制剂的研究范围很小，已知的天然 GLUT1 抑制剂的结构仅限于几类天然产物。因此，发现和研究其他具有新型支架的天然GLUT1抑制剂至关重要。酸浆 (Physalis angulata L. var.)绒毛是一种被称为毛苦枝（MKZ）的植物。醉茄内酯是 MKZ 的主要植物化学成分。 MKZ 提取物和 MKZ 成分在最近的药理学研究中表现出抗肿瘤活性。然而，MKZ 的抗肿瘤活性成分及其分子机制仍不清楚。细胞膜仿生纳米平台（CM@Fe 3 O 4 /MIL-101）用于从MKZ中分离潜在的GLUT1抑制剂。一种新的睡茄内酯 physagulide Y ( 2 ) 以及六种已知的睡茄内酯 ( 1 , 3 – 7 ) 被确定为潜在的 GLUT1 抑制剂。 Physagulide Y 是最有效的 GLUT1 抑制剂，其抗肿瘤活性和可能的作用机制在 MCF-7 人类癌细胞中进行了探索。这些发现推动了天然产物靶向分离技术的发展，并确定了用于研究天然 GLUT1 抑制剂的新分子框架。
更新日期：2023-12-20
中文翻译：
酸浆中基于茄内酯的葡萄糖转运蛋白 1 抑制剂的靶标分离和潜在抗癌活性绒毛
葡萄糖转运蛋白 1 (GLUT1) 蛋白参与肿瘤细胞中葡萄糖的基础水平吸收。抑制 GLUT1 可减少肿瘤细胞增殖并诱导肿瘤细胞损伤。天然 GLUT1 抑制剂的研究范围很小，已知的天然 GLUT1 抑制剂的结构仅限于几类天然产物。因此，发现和研究其他具有新型支架的天然GLUT1抑制剂至关重要。酸浆 (Physalis angulata L. var.)绒毛是一种被称为毛苦枝（MKZ）的植物。醉茄内酯是 MKZ 的主要植物化学成分。 MKZ 提取物和 MKZ 成分在最近的药理学研究中表现出抗肿瘤活性。然而，MKZ 的抗肿瘤活性成分及其分子机制仍不清楚。细胞膜仿生纳米平台（CM@Fe 3 O 4 /MIL-101）用于从MKZ中分离潜在的GLUT1抑制剂。一种新的睡茄内酯 physagulide Y ( 2 ) 以及六种已知的睡茄内酯 ( 1 , 3 – 7 ) 被确定为潜在的 GLUT1 抑制剂。 Physagulide Y 是最有效的 GLUT1 抑制剂，其抗肿瘤活性和可能的作用机制在 MCF-7 人类癌细胞中进行了探索。这些发现推动了天然产物靶向分离技术的发展，并确定了用于研究天然 GLUT1 抑制剂的新分子框架。
京公网安备 11010802027423号