Background: TLC bioautography is a hyphenated technique combining planar chromatographic separation and in situ biological activity detection. This coupled method has been receiving much attention in screening bio-active natural products because of its properties of being simple, rapid, inexpensive, and effective.

Methods: The recent progress in the development of method of TLC bioautography for detecting antimicrobial and enzyme inhibitory activities dating between 2012 and early 2018 has been reviewed. The applications of this method in biological screening of natural products were also presented.

Results: Some anaerobic and microaerophilic bacteria and a causative bacterium of tuberculosis have been adopted to TLC direct bioautography. Seven types of enzymes including acetylcholinesterase, glucosidase, lipase, xanthine oxidase, tyrosinase, monoamine oxidase, and dipeptidyl peptidase IV have so far been adopted on TLC bioautography. Its new application in screening antiurolithiatic agents was included.

Conclusion: The standard experimental procedures are required for TLC antioxidant and antimicrobial assays. Some new enzymes should be attempted and adopted on TLC bioautography. The existing TLC methods for enzyme inhibition need more application studies to assess their screening capacity in the discovery of active compounds. The GC-MS or LC-MS approaches have gradually been coupled to TLC bioautography for fast structural characterization of active compounds.

背景：TLC生物自显影技术是一种结合了平面色谱分离和原位生物活性检测的联用技术。这种偶联方法由于其简单，快速，廉价和有效的性质而在筛选生物活性天然产物中受到了广泛的关注。

方法：回顾了2012年至2018年初之间薄层色谱生物自显影技术用于检测抗菌和酶抑制活性的方法的最新进展。还介绍了该方法在天然产物生物筛选中的应用。

结果：TLC直接生物自显影术已采用了一些厌氧和微需氧菌以及结核病的致病菌。迄今为止，在薄层色谱生物自显影术中已采用了七种类型的酶，包括乙酰胆碱酯酶，葡糖苷酶，脂肪酶，黄嘌呤氧化酶，酪氨酸酶，单胺氧化酶和二肽基肽酶IV。它在筛选抗尿石症药物中的新应用也包括在内。

结论：TLC抗氧化剂和抗菌测定需要标准的实验程序。一些新的酶应尝试并在TLC生物自显影中采用。现有的酶抑制TLC方法需要更多的应用研究，以评估其在发现活性化合物中的筛选能力。GC-MS或LC-MS方法已逐渐与TLC生物自显影相结合，以快速表征活性化合物。