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通过体外和计算机模拟研究探讨积雪草提取物对肝细胞癌的治疗潜力。

Therapeutic potential of Bacopa monnieri extracts against hepatocellular carcinoma through in-vitro and computational studies.

作者信息

Altaf Awais, Kiran Asia, Sarwar Muhammad, Maqbool Tahir, Sharif Sumaira, Iqbal Hana'a, Farooq Saba, Ali Qurban, Han Shiming, Ahmad Ajaz

机构信息

Institute of Molecular Biology and Biotechnology, The University of Lahore, Lahore, Pakistan.

Faculty of Health Sciences, Equator University of Science and Technology, Masaka, Uganda.

出版信息

PLoS One. 2025 Apr 28;20(4):e0321445. doi: 10.1371/journal.pone.0321445. eCollection 2025.

Abstract

BACKGROUND

Among various cancers, primary liver cancer is the seventh most diagnosed malignancy and is the second most prevalent contributor to cancer-causing deaths. During conventional treatment, the recurrence of disease, low drug inefficacy, and severe side effects are the main limitations. Recently, natural anticancer medicines from the Middle East, Korea, China, Europe, North America, and India have attracted a lot of interest due to their low side effects and better remedial properties. The current study investigated the antioxidative and anticancer effects of ethanolic (BME) and n-hexane (BMH) extracts of B. monnieri (L.) Wettst.

METHODS

In the current study, phytochemical profiling was done using gas chromatography-mass spectrometry (GC-MS) analysis. The antioxidant potential was measured using DPPH, nitric oxide, superoxide anion, and hydrogen peroxide assays, while the cell viability and apoptotic effect were measured by MTT, crystal violet, and annexin V/PI protocols, respectively.

RESULTS

Higher concentrations of total phenolic contents (274.92±3.52 mgGAE/g), total flavonoid contents (141.99±4.14 mgQE/g) and tannins (55.49±4.63 mgTAE/g) were observed in BME extract with strong antioxidant potential than BMH extract. Also, BME extract showed higher cytotoxicity with less IC50 value (24.70 μg/mL) and a lower percentage of cell viability, while the same extract exhibited 58.65% apoptosis against HepG2 cells in comparison to cisplatin and BMH extract. Furthermore, Spiro[(tricyclo[6.2.2.0(2,7)]dodeca-5,9-diene)-4,1'-cyclobutane]-11,2'-dione from BME extract showed the lead docking score of -8.8, -8.1 and -7.8 kcal/mol against TGF-βR1, TNF-α, and iNOS, respectively.

CONCLUSION

In conclusion, the ethanolic extract of B. monnieri has a significant potential for becoming a potent anticancer drug that effectively treats liver damage, including HCC.

摘要

背景

在各种癌症中,原发性肝癌是第七大最常被诊断出的恶性肿瘤,也是导致癌症死亡的第二大常见原因。在传统治疗过程中,疾病复发、药物低效以及严重的副作用是主要限制因素。最近,来自中东、韩国、中国、欧洲、北美和印度的天然抗癌药物因其低副作用和更好的治疗特性而备受关注。本研究调查了莫尼氏婆罗门参(Bacopa monnieri (L.) Wettst.)乙醇提取物(BME)和正己烷提取物(BMH)的抗氧化和抗癌作用。

方法

在本研究中,使用气相色谱 - 质谱(GC - MS)分析进行植物化学谱分析。通过DPPH、一氧化氮、超氧阴离子和过氧化氢测定法测量抗氧化潜力,而分别通过MTT、结晶紫和膜联蛋白V/PI方案测量细胞活力和凋亡效应。

结果

与BMH提取物相比,BME提取物中观察到更高浓度的总酚含量(274.92±3.52 mgGAE/g)、总黄酮含量(141.99±4.14 mgQE/g)和单宁(55.49±4.63 mgTAE/g),且具有较强的抗氧化潜力。此外,BME提取物显示出更高的细胞毒性,IC50值更低(24.70 μg/mL),细胞活力百分比更低,而与顺铂和BMH提取物相比,该提取物对HepG2细胞表现出58.65%的凋亡率。此外,BME提取物中的螺[(三环[6.2.2.0(2,7)]十二碳 - 5,9 - 二烯)-4,1'-环丁烷]-11,2'-二酮对转化生长因子 - βR1、肿瘤坏死因子 - α和诱导型一氧化氮合酶的对接得分分别为 - 8.8、 - 8.1和 - 7.8 kcal/mol。

结论

总之,莫尼氏婆罗门参乙醇提取物具有成为有效治疗包括肝癌在内的肝损伤的强效抗癌药物的巨大潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0899/12036942/a6395369a319/pone.0321445.g001.jpg

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