Kombiyil Salini, Sivasithamparam Niranjali Devaraj
Department of Biochemistry, University of Madras, Guindy Campus, Chennai, 600025, India.
Appl Biochem Biotechnol. 2023 Apr;195(4):2687-2708. doi: 10.1007/s12010-021-03724-4. Epub 2022 Mar 9.
Breast cancer treatment strategy depends mainly on the receptor status. Our aim was to identify a herbal preparation, effective against breast cancer, irrespective of hormone sensitivity, and to understand its molecular mechanism. The rich antioxidant composition of hawthorn (Crataegus oxyacantha) makes it a promising anti-cancer drug candidate. Polyphenol-rich methanolic extract of C. oxyacantha berry (M.Co) was found to be cytotoxic on hormone receptor positive (MCF-7) and triple negative (MDA-MB-231) breast cancer cell lines, at a dose (75 μg/ml) safe on normal cells. It could effectively inhibit tumor cell proliferation and arrest cell cycle at G1/S transition in both cell lines. Molecular targets were selected from different levels of canonical Wnt signaling pathway (such as autocrine and antagonistic ligands, receptor, effector, cytoplasmic components, downstream targets, and pathway antagonist), since they are frequently found dysregulated in all breast cancers and their aberrant activation is associated with cancer stem cell expansion. M.Co could significantly downregulate the expression of Wnt pathway agonists and upregulate that of Wnt antagonists at transcriptional and translational levels, in both cell lines. To conclude, C. oxyacantha berry extract is effective against breast cancer irrespective of its hormone dependency, and cancer growth inhibition at stem cell level can be expected.
乳腺癌的治疗策略主要取决于受体状态。我们的目标是确定一种草药制剂,它对乳腺癌有效,且不考虑激素敏感性,并了解其分子机制。山楂(Crataegus oxyacantha)丰富的抗氧化成分使其成为一种有前景的抗癌药物候选物。发现富含多酚的山楂浆果甲醇提取物(M.Co)对激素受体阳性(MCF-7)和三阴性(MDA-MB-231)乳腺癌细胞系具有细胞毒性,而其剂量(75μg/ml)对正常细胞是安全的。它可以有效抑制两种细胞系中的肿瘤细胞增殖并使细胞周期停滞在G1/S期转换。分子靶点是从经典Wnt信号通路的不同水平中选择的(如自分泌和拮抗配体、受体、效应器、细胞质成分、下游靶点和通路拮抗剂),因为它们在所有乳腺癌中经常被发现失调,且其异常激活与癌症干细胞扩增有关。在两种细胞系中,M.Co在转录和翻译水平上均可显著下调Wnt通路激动剂的表达并上调Wnt拮抗剂的表达。总之,山楂浆果提取物对乳腺癌有效,无论其激素依赖性如何,并且有望在干细胞水平抑制癌症生长。