Abstract |
Seven undescribed withanolides (1-7) and six artificial withanolides (8-13), along with 20 known compounds (14-33) were isolated from the aerial parts of Tubocapsicum anomalum. Their structures were confirmed by comprehensive spectroscopic analyses. The absolute configuration of compound 1 was defined by single-crystal X-ray crystallography. All isolates were evaluated for their antiproliferative effects against five human tumor cell lines (Hep3B, MDA-MB-231, SW480, HCT116 and A549), among which compound 24 ( tubocapsanolide A) exhibited the highest activities against the MDA-MB-231 cells with an IC50 value of 1.89 ± 1.03 μM. Further studies showed that 24 exhibited significant damage to mitochondria in MDA-MB-231 cells, including excess reactive oxygen species, decreased mitochondrial membrane potential, and apoptosis initiation. In addition, compound 24 also inhibited cell migration. These findings show that tubocapsanolide A may be a promising molecule for triple-negative breast cancer treatment and merit further evaluation.
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Authors | Ke Xiang, Chen Li, Ming-Xue Li, Zhuo-Rui Song, Xiao-Xin Ma, De-Juan Sun, Hua Li, Li-Xia Chen |
Journal | Bioorganic chemistry
(Bioorg Chem)
Vol. 110
Pg. 104809
(05 2021)
ISSN: 1090-2120 [Electronic] United States |
PMID | 33752145
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 2021 Elsevier Inc. All rights reserved. |
Chemical References |
- Antineoplastic Agents, Phytogenic
- Plant Extracts
- Withanolides
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Topics |
- Antineoplastic Agents, Phytogenic
(chemistry, isolation & purification, pharmacology)
- Cell Proliferation
(drug effects)
- Cell Survival
(drug effects)
- Dose-Response Relationship, Drug
- Drug Screening Assays, Antitumor
- Humans
- Molecular Conformation
- Plant Extracts
(chemistry, isolation & purification, pharmacology)
- Solanaceae
(chemistry)
- Structure-Activity Relationship
- Tumor Cells, Cultured
- Withanolides
(chemistry, isolation & purification, pharmacology)
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