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Withanolides derived from Physalis peruviana (Poha) with potential anti-inflammatory activity.从灯笼果(酸浆)中提取的具潜在抗炎活性的睡茄内酯。
Bioorg Med Chem Lett. 2016 Jun 15;26(12):2755-2759. doi: 10.1016/j.bmcl.2016.04.077. Epub 2016 Apr 26.
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17β-Hydroxy-18-acetoxywithanolides from Aeroponically Grown Physalis crassifolia and Their Potent and Selective Cytotoxicity for Prostate Cancer Cells.气培酸浆中 17β-羟基-18-乙酰氧基甾烷类化合物及其对前列腺癌细胞的强选择性细胞毒性
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Induction of cell cycle arrest and apoptosis with downregulation of Hsp90 client proteins and histone modification by 4β-hydroxywithanolide E isolated from Physalis peruviana.秘鲁酸浆中分离出的4β-羟基睡茄内酯E通过下调热休克蛋白90(Hsp90)客户蛋白和组蛋白修饰诱导细胞周期停滞和凋亡。
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Discovery of Potent 17β-Hydroxywithanolides for Castration-Resistant Prostate Cancer by High-Throughput Screening of a Natural Products Library for Androgen-Induced Gene Expression Inhibitors.通过对天然产物文库进行高通量筛选以寻找雄激素诱导基因表达抑制剂,发现用于去势抵抗性前列腺癌的强效17β-羟基睡茄内酯类化合物
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Withanolide E sensitizes renal carcinoma cells to TRAIL-induced apoptosis by increasing cFLIP degradation.睡茄内酯E通过增加cFLIP降解使肾癌细胞对TRAIL诱导的凋亡敏感。
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气培灯笼果中的醉茄内酯及其对前列腺癌细胞和肾癌细胞的选择性细胞毒性

Withanolides from Aeroponically Grown Physalis peruviana and Their Selective Cytotoxicity to Prostate Cancer and Renal Carcinoma Cells.

作者信息

Xu Ya-Ming, Wijeratne E M Kithsiri, Babyak Ashley L, Marks Hanna R, Brooks Alan D, Tewary Poonam, Xuan Li-Jiang, Wang Wen-Qiong, Sayers Thomas J, Gunatilaka A A Leslie

机构信息

Natural Products Center, School of Natural Resources and the Environment, College of Agriculture and Life Sciences, University of Arizona , 250 E. Valencia Road, Tucson, Arizona 85706, United States.

Basic Research Program, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research, and Cancer and Inflammation Program, National Cancer Institute , Frederick, Maryland 21702, United States.

出版信息

J Nat Prod. 2017 Jul 28;80(7):1981-1991. doi: 10.1021/acs.jnatprod.6b01129. Epub 2017 Jun 15.

DOI:10.1021/acs.jnatprod.6b01129
PMID:28617598
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6993142/
Abstract

Investigation of aeroponically grown Physalis peruviana resulted in the isolation of 11 new withanolides, including perulactones I-L (1-4), 17-deoxy-23β-hydroxywithanolide E (5), 23β-hydroxywithanolide E (6), 4-deoxyphyperunolide A (7), 7β-hydroxywithanolide F (8), 7β-hydroxy-17-epi-withanolide K (9), 24,25-dihydro-23β,28-dihydroxywithanolide G (10), and 24,25-dihydrowithanolide E (11), together with 14 known withanolides (12-25). The structures of 1-11 were elucidated by the analysis of their spectroscopic data, and 12-25 were identified by comparison of their spectroscopic data with those reported. All withanolides were evaluated for their cytotoxic activity against a panel of tumor cell lines including LNCaP (androgen-sensitive human prostate adenocarcinoma), 22Rv1 (androgen-resistant human prostate adenocarcinoma), ACHN (human renal adenocarcinoma), M14 (human melanoma), SK-MEL-28 (human melanoma), and normal human foreskin fibroblast cells. Of these, the 17β-hydroxywithanolides (17-BHWs) 6, 8, 9, 11-13, 15, and 19-22 showed selective cytotoxic activity against the two prostate cancer cell lines LNCaP and 22Rv1, whereas 13 and 20 exhibited selective toxicity for the ACHN renal carcinoma cell line. These cytotoxicity data provide additional structure-activity relationship information for the 17-BHWs.

摘要

对气培灯笼果的研究导致分离出11种新的睡茄内酯,包括秘鲁内酯I-L(1-4)、17-脱氧-23β-羟基睡茄内酯E(5)、23β-羟基睡茄内酯E(6)、4-脱氧酸浆醇A(7)、7β-羟基睡茄内酯F(8)、7β-羟基-17-表睡茄内酯K(9)、24,25-二氢-23β,28-二羟基睡茄内酯G(10)和24,25-二氢睡茄内酯E(11),以及14种已知的睡茄内酯(12-25)。通过对其光谱数据的分析阐明了1-11的结构,并通过将其光谱数据与报道的数据进行比较鉴定了12-25。对所有睡茄内酯针对一组肿瘤细胞系进行了细胞毒性活性评估,这些细胞系包括LNCaP(雄激素敏感的人前列腺腺癌)、22Rv1(雄激素抵抗的人前列腺腺癌)、ACHN(人肾腺癌)、M14(人黑色素瘤)、SK-MEL-28(人黑色素瘤)和正常人包皮成纤维细胞。其中,17β-羟基睡茄内酯(17-BHWs)6、8、9、11-13、15和19-22对两种前列腺癌细胞系LNCaP和22Rv1表现出选择性细胞毒性活性,而13和20对ACHN肾癌细胞系表现出选择性毒性。这些细胞毒性数据为17-BHWs提供了额外的构效关系信息。