原牛角霉和赤霉的药理学分析:揭示化学活性代谢物的抗菌和抗癌潜力。

IF 3.3 3区 医学 Q2 ONCOLOGY
Sahar S Alghamdi, Allulu Y Alturki, Rizwan Ali, Rasha S Suliman, Afrah E Mohammed, Atheer Al Dairem, Zeyad I Alehaideb, Raghad A Alshafi, Sara A Alghashem, Ishrat Rahman
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引用次数: 0

摘要

背景:随着癌症患病率和细菌耐药性的增加,需要更有效的抗癌和抗菌治疗。本研究探讨了药用植物,特别是Calotropis procera (C. procera)和Rhazya stricta (R. stricta)在解决这一需求方面的潜力,旨在发现新的治疗干预措施。方法:采用不同的提取方法,对黄芪、黄芪叶进行抑菌、抑癌活性研究。采用水、氯仿和乙酸乙酯制备提取物,测定其对耐甲氧西林金黄色葡萄球菌(MRSA)和大肠杆菌(E. coli)的抑菌活性。通过对各种癌细胞进行MTT细胞毒性试验,并进一步使用高含量成像(HCI)-凋亡试验和apox - glotm三重试验来评估其抗癌潜力。采用液相色谱-质谱联用(LC-MS)技术鉴定了procera的次级代谢物,并对这些代谢物的活性进行了计算预测。结果:赤霉叶提取物对金黄色葡萄球菌和大肠杆菌均有抑菌活性。果仁乙酸乙酯提取物对多种癌细胞具有明显的抗癌作用。该研究还揭示了剂量依赖性诱导细胞凋亡和细胞活力下降。计算预测表明,鉴定的代谢物作为核受体配体和酶抑制剂具有活性,具有良好的口服生物利用度。大多数代谢物被发现是免疫和细胞毒性的,除了proceragenin和calotropone,它们被确定为无心脏毒性。结论:醋酸乙酯制备的原果仁提取物具有明显的细胞毒和抑菌作用。这些结果为进一步的体外研究铺平了道路,以探索这些提取物的全部潜力,并强调了C. procera中化学活性代谢物的存在,这些代谢物有望作为开发针对细菌感染和癌症的新疗法的先导分子,同时最大限度地减少潜在的副作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Pharmacological Profiling of Calotropis Procera and Rhazya Stricta: Unraveling the Antibacterial and Anti-Cancer Potential of Chemically Active Metabolites.

Background: The increasing prevalence of cancer and bacterial resistance necessitates more effective anti-cancer and anti-bacterial treatments. This study explores the potential of medicinal plants, specifically Calotropis procera (C. procera) and Rhazya stricta (R. stricta), in addressing this need, aiming to uncover new therapeutic interventions. Methods: Various extraction methods for the leaves of C. procera and R. stricta were employed to investigate the anti-bacterial and anti-cancer properties of these herbs. For anti-bacterial testing, extracts were prepared using water, chloroform, and ethyl acetate, and their activity against methicillin-resistant Staphylococcus aureus (S. aureus) (MRSA) and Escherichia coli (E. coli) was assessed. The anti-cancer potential was evaluated through MTT cytotoxicity assays on various cancer cell lines and further testing using high-content imaging (HCI)-Apoptosis Assay and the ApoTox-GloTM Triplex Assay. Liquid chromatography-mass spectrometry (LC-MS) was used to identify the secondary metabolites of C. procera, and computational predictions were performed to assess the activity of these metabolites. Results: The leaf extracts of both C. procera and R. stricta demonstrated antibacterial activity against S. aureus and E. coli. The C. procera ethyl acetate extract exhibited potent anti-cancer effects on several cancer cell lines. The research also revealed a dose-dependent induction of apoptosis and a decline in cell viability. Computational predictions suggested the identified metabolites were active as nuclear receptor ligands and enzyme inhibitors, with good oral bioavailability. Most metabolites were found to be immunologic and cytotoxic, except for proceragenin and calotropone, which were determined to be non-cardiotoxic. Conclusion: The study's findings demonstrate the remarkable cytotoxic and antibacterial effects of C. procera extracts prepared using ethyl acetate. These results pave the way for further in vitro studies to explore the full potential of these extracts and highlight the presence of chemically active metabolites in C. procera, which hold promise as lead molecules for the development of novel therapies targeting bacterial infections and cancer while minimizing potential side effects.

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来源期刊
Journal of Cancer
Journal of Cancer ONCOLOGY-
CiteScore
8.10
自引率
2.60%
发文量
333
审稿时长
12 weeks
期刊介绍: Journal of Cancer is an open access, peer-reviewed journal with broad scope covering all areas of cancer research, especially novel concepts, new methods, new regimens, new therapeutic agents, and alternative approaches for early detection and intervention of cancer. The Journal is supported by an international editorial board consisting of a distinguished team of cancer researchers. Journal of Cancer aims at rapid publication of high quality results in cancer research while maintaining rigorous peer-review process.
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