ABSTRACT
Asiatic acid (AA) is a ursane pentacyclic triterpenoids, which possesses a wide range of pharmacological activities, such as anti-tumor, hypoglycemic, anti-inflammatory, anti-bacterial. Due to poor solubility and low bioavailability, clinical application of asiatic acid is limited. To address these defects, the structural modifications of AA have been carried out, and large numbers of AA-based derivatives with novel structure and eximious biological activity have been developed. In this paper, the research progress of structural modifications, biological activity, structure-activity relationship and mechanism studies in recent twenty years are reviewed, which provides reference for development of AA-related drugs.
ABSTRACT
Objective: The classical formula of Dingxiang Shiditang can be used for hiccup and vomit which caused by many reasons,its molecular mechanism of this formula was investigated.Method: Based on the integrated pharmacology platform of traditional Chinese medicine,the potential molecular mechanism of Dingxiang Shiditang was revealed from the dimensions of multi-components and multi-targets.Result: There were 89 compounds related to hiccup and vomit of Dingxiang Shiditang,and there was 1 common target[cannabinoid receptor 1(CNR1)].On the one hand,CNR1 could inhibit the occurrence of hiccup and vomit by inhibiting the release of γ-aminobutyric acid(GABA),dopamine,5-hydroxytryptamine(5-HT);on the other hand,CNR1 could inhibit gastrointestinal motility and delay gastric emptying,and it was speculated that CNR1 may play a role in regulating gastrointestinal motility through brain-gut axis.Meanwhile,the mechanism of Dingxiang Shiditang may be related to nucleotide metabolism and nervous system.Conclusion: Dingxiang Shiditang may regulate gastrointestinal motility by affecting the release of neurotransmitters,mitochondrial energy metabolism,and achieve its effect on hiccup and vomit based on the joint intervention of multiple targets and multiple pathways.