使用回收制备型 HPLC 从玉米丝中分离天然类固醇：化学本科生的天然产物发现作业,Journal of Chemical Education

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使用回收制备型 HPLC 从玉米丝中分离天然类固醇：化学本科生的天然产物发现作业
Journal of Chemical Education ( IF 2.5 ) Pub Date : 2023-09-15 , DOI: 10.1021/acs.jchemed.2c01187
Siow-Ping Tan ₁ , Xin-Yi Keng ₁ , Bryan Chi-Wah Lim ₁ , Sook Yee Liew _{2,

3} , Mohd Azlan Nafiah ₄

Affiliation

植物源性天然产物是潜在药物的重要来源，并继续对药物发现过程产生重大影响。天然产物发现作业提供了向本科生介绍药物化学入门的各种实验技术的机会。这项作业的目的是作为一项有意义的实践练习，向本科化学学生介绍使用廉价玉米丝进行药物发现的早期阶段的常见程序，其中最后一年的本科生使用回收制备型高效液相色谱法从玉米须中分离和纯化类固醇。该学生使用先进的光谱方法，如紫外、红外、一维和二维核磁共振来阐明这些类固醇的结构。还评估了这些类固醇的细胞毒性活性，通过 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四唑溴化物测定发现，60 μg/mL 对正常人 MRC-5 细胞无细胞毒性。通过这项作业，学生可以通过药物发现早期阶段的常见程序进行有意义的多学科实践练习，并了解分离可能导致新药开发的天然化合物的过程。

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Isolation of Natural Steroids from Corn Silk Using Recycling Preparative HPLC: A Natural Products Discovery Assignment for the Undergraduate Chemistry Student

Plant-derived natural products are an important source of potential medicines and continue to have a major impact on the drug discovery process. Natural product discovery assignments provide an opportunity to present various experimental techniques to undergraduate students in introductory medicinal chemistry. This assignment was developed to serve as a meaningful hands-on exercise to introduce undergraduate Chemistry students to the common procedure in the early phase of drug discovery using inexpensive corn silk, in which the final year undergraduate student used Recycling Preparative High-Performance Liquid Chromatography to separate and purify steroids from corn silk. The student used advanced spectroscopic methods such as UV, IR, and one- and two-dimensional NMR to elucidate the structures of these steroids. The cytotoxic activity of these steroids was also evaluated and found to be non-cytotoxic to normal human MRC-5 cells at 60 μg/mL via 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. With this assignment, students gain meaningful multidisciplinary hands-on exercises with the common procedure in the early stages of drug discovery and understand the process of isolating natural compounds that may lead to the development of new drugs.

更新日期：2023-09-15

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