[MCE] High-throughput Screening and Traditional Chinese Medicine

30 May [MCE] High-throughput Screening and Traditional Chinese Medicine

Traditional Chinese Medicine – An Important Resource for Drug Discovery

Traditional Chinese medicine (TCM) is a holistic natural medicine system with thousands of years’ history [1]. According to the third national resource survey of traditional Chinese medicine materials (TCMMs), there are 12,807 kinds of materials used as TCMM, including 11,116 plant derived materials, 1,571 animal derived materials, and 80 kinds of minerals [2]. Most of these TCMMs have been used for hundreds or even thousands of years, and their efficacies and toxicities are well documented. Although the principal bioactive ingredients in many TCMMs and their underlying therapeutic mechanisms remain largely unknown, this unique national heritage has become a rich resource for drug discovery in modern times.

Active substances can be extracted from Traditional Chinese Medicine

Isolated from medicinal plants or traditional Chinese medicine formulas, active ingredients are defined as a set of compounds or fractions with known chemical composition, reproducible pharmaceutical properties and clinical efficacy. At Shanghai Institute of Materia Medica, more than 6,000 single chemical entities with novel structures have been identified from TCM since the 1950s, and several of them have been developed into clinical candidates or approved medicines, such as artemether, salvicine, huperzine A, and depside salts from Saliva Miltiorrhiza [3]. The 2015 Nobel Prize in Physiology or Medicine was awarded to Youyou Tu in recognition of her contribution in the discovery of artemisinin as an effective antimalarial medicine.

Figure 1. Youyou Tu, the 2015 Nobel Laureate in Physiology or Medicine [4]

High-throughput Screening using Traditional Chinese Medicine
Active Compound Library
Traditional Chinese Medicine Active Compound Library can be a useful tool for discovering new drugs. Recent progress made in separation and preparation of traditional Chinese medicine constituents not only added more potential lead compounds to the TCM active compound collection, it also significantly increased the chemical diversity of the available TCM active compounds. In a recent study, researchers rationally selected 30 TCM formulas from 200 anti-viral formulas collected in the ancient Chinese medicine book “Treatise on Febrile and Miscellaneous Diseases”, and prepared a 1306-fraction herbal formulae extract library by standardized chromatographic fractionation. The antiviral activity of this library was screened using HEK293T cells carrying a luciferase-driven interferon stimulated response element (ISRE). Hit compounds were identified by liquid chromatography mass spectrometry analysis, their mechanisms of action were also explored. A total of 18 ISRE-activating fractions were found, and three compounds, ononin, sec-O-β-D-glucosylhamaudol and astragaloside I, were shown to activate ISRE through their impacts on p65 phosphorylation and nuclear translocation [5].

Figure 2. Preparation and statistics of traditional Chinese medicine sublibrary [5]

MedChemExpress
provides a series of TCM/natural product derived compound libraries:

More compound libraries are available:
https://www.medchemexpress.com/screening-libraries.html

References:
[1] Front. Pharmacol, 8 (2017), pp. 1-5.
[2] Zhongguo Zhong Yao Za Zhi. 2014 Dec;39(24):4728-31.
[3] Comb Chem High Throughput Screen. 2010 Dec;13(10):837-48.
[4] Nobel Prize in Physiology or Medicine in 2015.
[5] Pharmacol Res. 2019 Jul;145:104248.