山梨提取物的优化、制备及对皮肤癌细胞系的细胞毒性研究。

IF 2.9 4区 医学 Q3 CHEMISTRY, MEDICINAL
Kiran Kangra, Vandana Garg, Anju Dhiman, Rohit Dutt
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引用次数: 0

摘要

背景:皮肤癌是全球最常见的癌症之一,被认为是与高死亡率相关的严重公共卫生问题。目前皮肤癌的治疗方案受到生物利用度低、产生耐药性或不良副作用的限制。许多以水果提取物为基础的营养保健品具有作为局部治疗方法的潜力。梨(梨)果实提取物是胆碱能酸的丰富来源,目前用于治疗各种皮肤疾病。因此,它有资格作为一个有前途的候选皮肤癌治疗。目的:研究山梨提取物包埋在酶体中的细胞毒性。方法:采用热法制备梨果提取物,并采用中心设计优化。对优化后的酶质体进行了粒径分布、zeta电位、包封效率、形态和颗粒稳定性的体外表征。结果:初步的植物化学筛选结果表明,与其他提取物(PCEA和PCAE)相比,PCHE含有大量的酚类化合物。这些酚类化合物的存在有助于PCHE的强抗氧化和细胞毒性作用,这是以剂量依赖的方式观察到的。GC-MS分析鉴定出PCHE中含有绿原酸、熊果苷、熊果酸、槲皮素和表儿茶素。通过对提取物的初步测试,选择PCHE作为制备溶酶体的原料。优化后的酶质体粒径为699 nm, zeta电位为-16.07。透射电子显微镜显示了一个封闭的球形对称结构。此外,弗朗茨扩散池分析经皮吸收使用卵膜表明稳态通量的药物从质体。通过MTT法对表皮样癌细胞系(A431)进行细胞毒性评估。结果表明,乙醇体制剂的细胞毒活性优于PCHE提取物。1结论:综上所述,本研究结果清楚地指出,热法制备的山梨提取物包埋在脂质体中,对皮肤癌细胞系具有细胞毒性。通过进一步的机制分析和动物研究,这种溶酶体制剂可用于皮肤癌治疗。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Optimization, Preparation, and Cytotoxic Potential of Pyrus communis Extract Loaded Ethosomes on Skin Cancer Cell Lines.

Background: Skin cancer is one of the most prevalent cancers globally and is considered a serious public health problem associated with high death rates. The current therapeutic regimes for skin cancer are limited by their low bioavailability, generation of resistance, or adverse side effects. Many fruit extract-based nutraceuticals hold potential as topical treatment methods. Pyrus communis (Pear) fruit extract is a rich source of cholinergic acid, presently used as therapy for various skin diseases. Thus, it qualifies as a promising candidate for skin cancer treatment.

Objective: The objective of the study is to evaluate the cytotoxicity of Pyrus communis extract entrapped in ethosomes.

Methods: In this study, Pyrus communis fruit extract was formulated in ethosomes using the hot method and optimized using central composite design. The optimized ethosomes were characterized in vitro for particle size distribution, zeta potential, entrapment efficiency, morphology, and particle stability.

Results: Preliminary phytochemical screening results suggest that PCHE contains a significant amount of phenolic compounds compared to other extracts (PCEA and PCAE). The presence of these phenolic compounds contributes to the strong antioxidant and cytotoxic effects of PCHE, which are observed in a dose-dependent manner. Analysis through GC-MS has identified chlorogenic acid, arbutin, ursolic acid, quercetin, and epicatechin are present in PCHE. Based on the initial testing of the extracts, PCHE was chosen for the preparation of ethosomes. The optimized ethosomes were found to have a particle size of 699 nm and a zeta potential of -16.07. Transmission Electron Microscopy illustrated a closed, spherically symmetrical structure of the ethosomes. Additionally, the Franz diffusion cell analysis for percutaneous absorption using egg membrane indicated a steady-state flux of the drug from the ethosomes. The formulation's cytotoxicity potential was assessed using the epidermoid carcinoma cell line (A431) through the MTT assay. The results show that the ethosome formulations exhibit cytotoxic activity better than PCHE extract. 1 Conclusion: In sum, the result of this study clearly points out that Pyrus communis extract entrapped in ethosomes, prepared by hot method, displayed a cytotoxic potential against skin cancer cell lines. This ethosomal formulation can be harnessed for skin cancer therapy through further mechanistic analysis and animal 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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