El-Feky Amal M, El-Rashedy Ahmed A
Pharmacognosy Department, National Research Centre, 33 El Bohouth St. (Former El Tahrir St.), Dokki, P.O. 12622, Giza, Egypt.
Chemistry of Natural and Microbial Products Department, National Research Center (NRC), Giza, Egypt.
Sci Rep. 2025 Sep 18;15(1):32602. doi: 10.1038/s41598-025-19442-4.
The therapeutic potential of plant-derived polyphenols has garnered significant attention due to their roles in modulating inflammation and cancer progression. Viola odorata (V. odorata), traditionally used in herbal medicine, is known for its bioactive constituents, yet comprehensive profiling of its floral phytochemicals-particularly phenolic acids, flavonoids, and anthocyanins-remains limited. This study was pharmacologically designed to investigate the detailed phytochemical composition of V. odorata flowers and evaluate their anti-inflammatory and anticancer activities, aiming to identify novel natural agents for therapeutic development. Methanolic extracts of V. odorata flowers were analyzed for total phenolics, flavonoids, and anthocyanins using spectrophotometric methods. HPLC and UPLC/ESI-MS techniques were employed to identify and quantify individual compounds. Structural elucidation of isolated flavonoids was performed using advanced spectroscopic techniques. The anti-inflammatory and cytotoxic effects of the extract and isolated flavonoids were assessed in vitro using hepatocellular carcinoma (HepG2), human colonic epithelial (Caco-2), and colorectal carcinoma (HTC-116) cell lines. Molecular dynamics simulations were conducted to explore the interactions underlying the observed bioactivities. The methanolic extract contained 81.34 ± 0.17 mg GAE/g of total phenolics, 69.45 ± 0.24 mg CE/g of flavonoids, and 92.43 mg cyanidin-3-glucoside/100 g of anthocyanins. HPLC analysis revealed twelve phenolic acids and ten flavonoids, with gentisic acid (391.37 μg/g), apigenin-7-glucoside (417.22 μg/g), catechin (372.56 μg/g), and rutin (262.73 μg/g) being predominant. UPLC/ESI-MS identified 8 phenolic acids and derivatives, 3 flavonols, 4 flavones, 14 flavonoid glycosides, and 5 anthocyanins derived from cyanidin, delphinidin, and petunidin. Three flavonoids-5,7-dihydroxy-3,6-dimethoxyflavone, luteolin 7-O-glucoside, and kaempferol 3-O-rutinoside-were isolated and structurally characterized. The extract and isolated compounds exhibited dose-dependent cytotoxicity and anti-inflammatory effects across all tested cell lines. Molecular dynamics studies supported the observed inhibitory mechanisms. This study highlights the rich polyphenolic profile of V. odorata flowers and their promising anti-inflammatory and anticancer properties. The correlation between phytochemical composition and pharmacological activity underscores the therapeutic potential of V. odorata as a source of bioactive compounds for drug development.
植物来源的多酚类物质因其在调节炎症和癌症进展中的作用而备受关注。传统上用于草药的香堇菜，以其生物活性成分而闻名，但其花部植物化学成分（特别是酚酸、黄酮类化合物和花青素）的全面分析仍然有限。本研究从药理学角度设计，旨在研究香堇菜花的详细植物化学成分，并评估其抗炎和抗癌活性，以确定用于治疗开发的新型天然药物。采用分光光度法分析香堇菜花的甲醇提取物中的总酚、黄酮类化合物和花青素。采用HPLC和UPLC/ESI-MS技术鉴定和定量单个化合物。使用先进的光谱技术对分离出的黄酮类化合物进行结构解析。在体外使用肝癌（HepG2）、人结肠上皮（Caco-2）和结肠直肠癌（HTC-116）细胞系评估提取物和分离出的黄酮类化合物的抗炎和细胞毒性作用。进行分子动力学模拟以探索观察到的生物活性背后的相互作用。甲醇提取物含有81.34±0.17mg GAE/g总酚、69.45±0.24mg CE/g黄酮类化合物和92.43mg矢车菊素-3-葡萄糖苷/100g花青素。HPLC分析显示有十二种酚酸和十种黄酮类化合物，其中龙胆酸（391.37μg/g）、芹菜素-7-葡萄糖苷（417.22μg/g）、儿茶素（372.56μg/g）和芦丁（262.73μg/g）占主导。UPLC/ESI-MS鉴定出8种酚酸及其衍生物、3种黄酮醇、4种黄酮、14种黄酮苷和5种源自矢车菊素、飞燕草素和矮牵牛素的花青素。分离并鉴定了三种黄酮类化合物——5,7-二羟基-3,6-二甲氧基黄酮、木犀草素7-O-葡萄糖苷和山奈酚3-O-芸香糖苷的结构。提取物和分离出的化合物在所有测试细胞系中均表现出剂量依赖性的细胞毒性和抗炎作用。分子动力学研究支持了观察到的抑制机制。本研究突出了香堇菜花丰富的多酚谱及其有前景的抗炎和抗癌特性。植物化学成分与药理活性之间的相关性强调了香堇菜作为药物开发生物活性化合物来源的治疗潜力。
