γ环糊精辅助的肉桂水提取物用于癌症和压力管理。

IF 2.9 4区 医学 Q3 CHEMISTRY, MEDICINAL Current topics in medicinal chemistry Pub Date : 2024-08-20 DOI:10.2174/0115680266309291240808114508
Yang Shi, Huifu He, Huayue Zhang, Tian Yuan, Zhenya Zhang, Ranil DeSilva, Yoshiyuki Ishida, Keiji Terao, Sunil C Kaul, Renu Wadhwa
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引用次数: 0

摘要

目的:我们的目标是研究如何使用环糊精提取出具有高生物活性成分的肉桂水提取物,并通过基于细胞的检测进行验证:背景:天然化合物因其安全性和成本效益,在癌症治疗中备受关注。肉桂(Cinnamomum verum,又称锡兰肉桂)是一种常用香料,在民间医学中具有治疗各种疾病的历史。然而,其活性成分的溶解性、稳定性和生物利用度较差,限制了其使用和功效:我们制备了γ-环糊精(γCD)辅助的肉桂水提取物(CD-CIN),并将其活性与 DMSO 提取物(DM-CIN)进行了比较:在正常和应激(氧化、金属和缺氧)条件下,将细胞暴露于 CD-CIN 和 DM-CIN 提取物,然后使用各种分子检测方法分析应激和癌症表型:结果:我们发现 CD-CIN 具有相当强的抗癌活性,其中包括激活肿瘤抑制蛋白和 DNA 损伤反应。分子标记分析证实,低无毒浓度的 DM-CIN 和 CD-CIN 对细胞迁移和侵袭能力的抑制作用相当。此外,与对照组相比,DM-CIN 和 CD-CIN 处理过的细胞对氧化、金属和缺氧应激以及诱导分化都有保护作用:我们报告的 CD-CIN 是一种新的经济、简便的肉桂衍生资源,具有相当强的抗癌和抗应激活性,因此值得进行进一步的化学、体外和体内研究。
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γCyclodextrin-assisted Aqueous Extract of Cinnamon for Cancer and Stress Management.

Aim: Our goal was to investigate the use of Cyclodextrin in creating an aqueous extract of Cinnamon with a high content of its bioactive ingredients, validated by cell-based assays.

Background: Due to their safety and cost-effectiveness, natural compounds have garnered attention for cancer therapy, which often faces challenges related to drug toxicity and resistance. Cinnamon (Cinnamomum verum; also known as Ceylon Cinnamon) is a commonly used spice with a history in folk medicine for treating various ailments. However, its active ingredients suffer from poor solubility, stability, and bioavailability, which limits its use and benefits.

Objective: We prepared γCyclodextrin (γCD)-assisted aqueous extract of Cinnamon (CD-CIN) and compared its activity with the DMSO extract (DM-CIN).

Methods: The cells were exposed to CD-CIN and DM-CIN extracts under normal and stressed (oxidative, metal, and hypoxic) conditions and then analyzed for stress and cancerous phenotypes using various molecular assays.

Results: We found that CD-CIN possesses considerable anticancer activity that involves the activation of tumor suppressor proteins and DNA damage response. Low, non-toxic concentrations of DM-CIN and CD-CIN caused comparable inhibition of migration and invasion capability of cells, supported by molecular marker analyses. Furthermore, protection against oxidative, metal, and hypoxia stress, as well as induction of differentiation, was recorded in both DM-CIN and CD-CIN treated cells, as compared to the control.

Conclusion: We report CD-CIN as a new economic and easy Cinnamon-derived resource that possesses considerable anticancer and antistress activities and hence warrants further chemical, in vitro, and in vivo studies.

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来源期刊
CiteScore
6.40
自引率
2.90%
发文量
186
审稿时长
3-8 weeks
期刊介绍: Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.
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