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澳洲朱蕉中牡荆素2″-O-α-L-鼠李糖苷抗肿瘤特性的分子机制:分离与成分分析

The Molecular Mechanisms Underlying the Antineoplastic Profile of Vitexin 2″-O-α-L-Rhamnopyranoside From Cordyline australis (G.Frost.): Isolation and Constituent Profiling.

作者信息

Raslan Mona A, Mounier Marwa M, Taher Rehab F

机构信息

Pharmacognosy Department, Pharmaceutical and Drug Industries Research Institute, National Research Centre, Dokki, Giza, Egypt.

Natural Compounds Chemistry Department, Pharmaceutical and Drug Industries Research Institute, National Research Centre, Dokki, Giza, Egypt.

出版信息

Arch Pharm (Weinheim). 2025 Jul;358(7):e70054. doi: 10.1002/ardp.70054.

DOI:10.1002/ardp.70054
PMID:40685791
Abstract

Cordyline australis (G.Forst.) Endl. Red Star leaves have been used in traditional medicine for several disorders. This study investigated the anticancer potential of C. australis leaves extract and characterized its bioactive constituents. Three compounds, a steroidal saponin, fruticoside K 23, and two flavonoids, vitexin 2″-O-α-l-rhamnopyranoside 35 and helichrysoside 68, were isolated and identified from its aqueous methanolic extract (CAME) using column chromatography. Seventy-nine additional compounds were tentatively identified using high-performance liquid chromatography coupled with electrospray ionization mass spectrometry (HPLC-ESI-MS/MS) analysis and The Global Natural Product Social Molecular Networking (GNPS-MN), with 57 compounds reported for the first time in the Cordyline genus. CAME and its isolated compounds were evaluated for cytotoxicity by MTT assay against seven different cancer cell lines. Vitexin 2″-O-α-l-rhamnopyranoside 35 exhibited significant cytotoxicity against HCT-116 colon cancer cells. Additionally, CAME, fruticoside K 23, and vitexin 2″-O-α-l-rhamnopyranoside 35 demonstrated significant cytotoxicity against osteosarcoma (HOS) cells. Afterwards, the safety profile of CAME and all the isolated compounds were examined upon human normal cells BJ-1. At 100 μg/mL, CAME and all isolated compounds showed a safe response on human normal BJ-1 cells (0.6%-8.5% cytotoxicity). Vitexin 2″-O-α-l-rhamnopyranoside 35 possessed the most significant selective anticancer response on osteosarcoma cells (HOS), with the least IC value of 43.7 μg/mL. It induced apoptosis in HOS cells by modulating Bax, Bcl-2, and caspase-3 expression and caused G1 phase cell-cycle arrest. These results highlight C. australis as a source of potential anticancer agents, particularly vitexin 2″-O-α-l-rhamnopyranoside 35, which warrants further investigation for its therapeutic potential.

摘要

澳洲朱蕉(Cordyline australis (G.Forst.) Endl.)的红星叶在传统医学中被用于治疗多种疾病。本研究调查了澳洲朱蕉叶提取物的抗癌潜力,并对其生物活性成分进行了表征。使用柱色谱法从其甲醇水提取物(CAME)中分离并鉴定出三种化合物,一种甾体皂苷、弗鲁蒂可苷K 23,以及两种黄酮类化合物,牡荆素2″-O-α-L-鼠李吡喃糖苷35和蜡菊苷68。使用高效液相色谱-电喷雾电离质谱联用(HPLC-ESI-MS/MS)分析和全球天然产物社会分子网络(GNPS-MN)初步鉴定出另外79种化合物,其中57种化合物在朱蕉属中首次报道。通过MTT法评估CAME及其分离出的化合物对七种不同癌细胞系的细胞毒性。牡荆素2″-O-α-L-鼠李吡喃糖苷35对HCT-116结肠癌细胞表现出显著的细胞毒性。此外,CAME、弗鲁蒂可苷K 23和牡荆素2″-O-α-L-鼠李吡喃糖苷35对骨肉瘤(HOS)细胞表现出显著的细胞毒性。之后,在人正常细胞BJ-1上检测CAME和所有分离出的化合物的安全性。在100μg/mL时,CAME和所有分离出的化合物对人正常BJ-1细胞表现出安全反应(细胞毒性为0.6%-8.5%)。牡荆素2″-O-α-L-鼠李吡喃糖苷35对骨肉瘤细胞(HOS)具有最显著的选择性抗癌反应,最低IC值为43.7μg/mL。它通过调节Bax、Bcl-2和caspase-3的表达诱导HOS细胞凋亡,并导致G1期细胞周期停滞。这些结果突出了澳洲朱蕉作为潜在抗癌剂来源的地位,特别是牡荆素2″-O-α-L-鼠李吡喃糖苷35,其治疗潜力值得进一步研究。

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