作为乳腺癌信号蛋白的潜在多靶点候选药物,Rubia cordifolia的Lucidin优于fda批准的拉帕替尼。

IF 5.7 3区 医学 Q2 CHEMISTRY, MEDICINAL Pharmaceuticals Pub Date : 2025-01-09 DOI:10.3390/ph18010068
Akram Ahmed Aloqbi, Hadil Alahdal, Amany I Alqosaibi, Mashael M Alnamshan, Ibtesam S Al-Dhuayan, Ahood A Al-Eidan, Hind A S Alzahrani, Nouf K ALaqeel, Fatmah Hazza Alsharif, Abeer Al Tuwaijri
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引用次数: 0

摘要

背景:乳腺癌仍然是一个重大的全球健康问题,每年约有230万确诊病例和67万例死亡。目前的靶向治疗面临着耐药性和不良副作用等挑战。本研究旨在探索天然化合物作为潜在的多靶点乳腺癌治疗药物,重点关注Lucidin,一种从Rubia cordifolia中提取的蒽醌,并将其与fda批准的药物拉帕替尼的疗效进行比较。方法:利用锌的天然化合物文库对乳腺癌关键蛋白进行多靶点分子对接研究。Lucidin和Lapatinib的比较分析包括分子相互作用指纹图谱、药代动力学、水图计算(5 ns)来评估水热力学和结合相互作用,以及分子动力学模拟(100 ns)来评估水中的复杂稳定性和动力学行为。结果:Lucidin与多种乳腺癌靶点表现出显著的结合亲和力和相互作用潜力,在稳定性和结合相互作用方面优于拉帕替尼。水图分析表明,Lucidin具有良好的水化位点能量,增强了其功效。Lucidin的多靶点特征提示了一种更广泛的治疗方法,具有克服拉帕替尼相关的耐药和副作用的潜力。结论:Lucidin作为一种新型的、多靶点的抗乳腺癌药物,其疗效优于拉帕替尼。这些发现为进一步在体外和体内验证开发Lucidin作为乳腺癌治疗的潜在治疗选择提供了基础。
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Lucidin from Rubia cordifolia Outperforms FDA-Approved Lapatinib as a Potential Multitargeted Candidate for Breast Cancer Signalling Proteins.

Background: Breast cancer remains a significant global health concern, with approximately 2.3 million diagnosed cases and 670,000 deaths annually. Current targeted therapies face challenges such as resistance and adverse side effects. This study aimed to explore natural compounds as potential multitargeted breast cancer therapeutics, focusing on Lucidin, an anthraquinone derived from Rubia cordifolia, and comparing its efficacy with Lapatinib, an FDA-approved drug. Methods: We performed multitargeted molecular docking studies on key breast cancer proteins using a natural compound library from ZINC. Comparative analyses of Lucidin and Lapatinib included molecular interaction fingerprints, pharmacokinetics, WaterMap computations (5 ns) to assess water thermodynamics and binding interactions, and Molecular Dynamics Simulations (100 ns) in water to evaluate complex stability and dynamic behaviour. Results: Lucidin demonstrated significant binding affinity and interaction potential with multiple breast cancer targets, outperforming Lapatinib in stability and binding interactions. WaterMap analysis revealed favourable hydration site energetics for Lucidin, enhancing its efficacy. The multitargeted profile of Lucidin suggests a broader therapeutic approach with potential to overcome resistance and side effects associated with Lapatinib. Conclusions: Lucidin shows promise as a novel, multitargeted anti-breast cancer agent with improved efficacy over Lapatinib. These findings provide a foundation for further in vitro and in vivo validation to develop Lucidin as a potential therapeutic option for breast cancer treatment.

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来源期刊
Pharmaceuticals
Pharmaceuticals Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.10
自引率
4.30%
发文量
1332
审稿时长
6 weeks
期刊介绍: Pharmaceuticals (ISSN 1424-8247) is an international scientific journal of medicinal chemistry and related drug sciences.Our aim is to publish updated reviews as well as research articles with comprehensive theoretical and experimental details. Short communications are also accepted; therefore, there is no restriction on the maximum length of the papers.
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