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从 和 的地上部分中分离得到的白细胞介素-6 抑制化合物及其对卵巢癌细胞系的抗癌活性。

IL-6 Inhibitory Compounds from the Aerial Parts of and Their Anticancer Activities on Ovarian Cancer Cell Lines.

机构信息

College of Pharmacy, Integrated Research Institute of Pharmaceutical Sciences, The Catholic University of Korea, Bucheon 14662, Republic of Korea.

College of Pharmacy, Integrated Research Institute of Pharmaceutical Sciences, BK21FOUR Team for Advanced Program for Smart Pharma Leaders, The Catholic University of Korea, Bucheon 14662, Republic of Korea.

出版信息

Molecules. 2024 Jun 23;29(13):2981. doi: 10.3390/molecules29132981.

Abstract

Buch-Ham, a perennial woody vine belonging to the Piperaceae family, is traditionally used in Southeast Asia for treating various ailments such as malaria, headache, and hepatitis. This study described the isolation and identification of three new compounds, piperamides I-III (-), which belong to the maleimide-type alkaloid skeletons, along with fifteen known compounds (-) from the methanol extract of the aerial parts of . Their chemical structures were elucidated using spectroscopic methods (UV, IR, ESI-Q-TOF-MS, and 1D/2D NMR). All the isolates were evaluated for their ability to inhibit IL-6 activity in the human embryonic kidney-Blue™ IL-6 cell line and their cytotoxic activity against ovarian cancer cell lines (SKOV3/SKOV3-TR) and chemotherapy-resistant variants (cisplatin-resistant A2780/paclitaxel-resistant SKOV3). The compounds , , , , , and exhibited IL-6 inhibition comparable to that of the positive control bazedoxifene. Notably, compound displayed the most potent anticancer effect against all the tested cancer cell lines. These findings highlight the importance of researching the diverse activities of both known and newly discovered natural products to fully unlock their potential therapeutic benefits.

摘要

Buch-Ham 是胡椒科的一种多年生木本藤本植物,传统上用于治疗疟疾、头痛和肝炎等各种疾病。本研究描述了从 Buch-Ham 的地上部分甲醇提取物中分离和鉴定的三种新化合物 piperamides I-III (-),它们属于马来酰亚胺型生物碱骨架,以及十五种已知化合物 (-)。它们的化学结构通过光谱方法 (UV、IR、ESI-Q-TOF-MS 和 1D/2D NMR) 阐明。所有分离物均评估了它们抑制人胚肾-Blue™ IL-6 细胞系中 IL-6 活性的能力及其对卵巢癌细胞系 (SKOV3/SKOV3-TR) 和化疗耐药变体 (顺铂耐药 A2780/紫杉醇耐药 SKOV3) 的细胞毒性。化合物 、 、 、 、 和 显示出与阳性对照 bazedoxifene 相当的 IL-6 抑制作用。值得注意的是,化合物 对所有测试的癌细胞系表现出最强的抗癌作用。这些发现强调了研究已知和新发现的天然产物的多种活性的重要性,以充分挖掘它们的潜在治疗益处。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/394e/11242996/7c1c447a7a9f/molecules-29-02981-g001.jpg

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