Can the aggregation be a new approach for understanding the mechanism of Traditional Chinese Medicine?
"Frequent hitter" phenomenon emerged in the high-throughput screening; one of the most common mechanisms behind artifactual inhibition is that some organic molecules formed large colloid-like aggregates which are able to sequester and thereby inhibit enzymes. To investigate the situation in Traditional Chinese Medicine (TCM), 60 medicinal herbs and 24 Chinese herbal formulae were detected by dynamic light scattering (DLS), and aggregates were observed in all the 84 solution mixtures. The aggregates of two Chinese herbal formulae, 'Xue-Fu-Zhu-Yu Tang' (XF) and 'Jing-Guan Tang' (JG), were not only able to survive in the gastro-intestinal environment, but also had the ability to pass through the monolayer of the Caco-2 cell. The activities of XF and JG against three cardiovascular targets were also aggregates-related. Based on these findings, a new possible mechanism of the action of Chinese medicine was proposed.
Zhuang
Yan
Y
College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Yan
Jingjing
J
Zhu
Wei
W
Chen
Lirong
L
Liang
Dehai
D
Xu
Xiaojie
X
D000806:Angiotensin-Converting Enzyme Inhibitors / Q000494:pharmacology; D018938:Caco-2 Cells; D002317:Cardiovascular Agents / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D004357:Drug Synergism; D004365:Drugs, Chinese Herbal / Q000737:chemistry; D006801:Humans; D007408:Intestinal Absorption / Q000502:physiology; D008027:Light; D008516:Medicine, Chinese Traditional / Q000639:trends*; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors; D010316:Particle Size; D007703:Peptidyl-Dipeptidase A / Q000378:metabolism; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D017395:Plasminogen Activator Inhibitor 1 / Q000032:analysis / Q000378:metabolism; D012542:Scattering, Radiation
D000806:Angiotensin-Converting Enzyme Inhibitors; D002317:Cardiovascular Agents; D004365:Drugs, Chinese Herbal; D010936:Plant Extracts; D017395:Plasminogen Activator Inhibitor 1; D052247:Nitric Oxide Synthase Type II; D007703:Peptidyl-Dipeptidase A