ABSTRACT
The serotonin (5-hydroxytryptamine) type 3 receptor is an important target in the control of digestive dysfunction such as anorexia and bulimia, and 5-HT3 receptor antagonists are effective against eating disorder and the early-phase chemotherapy and radiotherapy evoked vomiting. Our previous research of Valeriana jatamansi revealed the presence of iridoids, which showed potent antitumor activities. Here, we explored the effects of 10π aromatic iridoid desacylbaldrinal isolated from V. jatamansi on the 5-HT3 receptor current. We performed whole cell recordings of 5-HT3A receptor currents in the presence of the compound. The result indicated that desacylbaldrinal inhibited the 5-HT-mediated 5-HT3A receptor current.
Subject(s)
Iridoids/pharmacology , Receptors, Serotonin, 5-HT3 , Serotonin 5-HT3 Receptor Antagonists/pharmacology , Serotonin , Valerian/chemistry , Humans , Iridoids/isolation & purification , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Serotonin 5-HT3 Receptor Antagonists/isolation & purificationABSTRACT
A new abietane diterpenoid glycoside, ajugaside B (1), along with three known compounds (2-4), were isolated from the whole plants of Ajuga ovalifolia var. calantha. The structure of the new compound (1) was elucidated by means of spectroscopic analyses (HRESIMS, IR, NMR and ECD). All of the isolated compounds were evaluated for their antitumor activities against MGC803, MCF-7, A549, HT29 and HepG2 cell lines. Compounds 3-4 showed moderate cytotoxicity against all tested cell lines with IC50 values of 1.8-7.3 µM.