ABSTRACT
Wulfenioidones A - K (1-11) were abietane diterpenoids with highly oxidized 6/6/6 aromatic tricyclic skeleton isolated from the whole plant of Orthosiphon wulfenioides, and their planar structures and absolute configurations were elucidated by spectroscopic data interpretation, electronic circular dichroism calculation as well as X-ray crystallography analysis. Bioactivity screening indicated that compounds 1-4, 6 and 8 exhibited lactate dehydrogenase (LDH) inhibition effect with IC50 values ranging from 0.23 to 3.43 µM by preventing the mononuclear macrophage cell pyroptosis induced by double signal stimulation of LPS and nigericin. Western Blot analyses of Caspase-1 and IL-1ß down-regulation exhibited that compound 1 could selectively inhibit NLRP3 inflammasome, and the cell morphological observation further supported that compound 1 prevented macrophage cell pyroptosis.
Subject(s)
Inflammasomes , Orthosiphon , NLR Family, Pyrin Domain-Containing 3 Protein , Abietanes/pharmacology , Abietanes/chemistry , MacrophagesABSTRACT
Four new norceanothane-type triterpenes, cyclopalin A-D (1-4), and sixteen known compounds (5-20) were obtained from the fruits of Cyclocarya paliurus. Their structures were determined by spectroscopic data, experimental electronic circular dichroism (ECD) and X-ray single crystal analyses. All isolated compounds were assayed for their anti-HIV-1IIIB activity. Compound 18 exhibited potent anti-HIV-1IIIB activity with an EC50 value of 1.32 µM (SI = 151.52).
Subject(s)
Juglandaceae , Triterpenes , Triterpenes/chemistry , Fruit , Spectrum Analysis , Juglandaceae/chemistry , Plant Leaves/chemistryABSTRACT
Our study on the roots and leaves of the never-hitherto-chemically studied S. glandulosa led to the isolation of five new diterpenes, referred to as stroglandulons A-E (1-5), alongside 18 known constituents (6-23). The structures of the new compounds were elucidated on the basis of their spectroscopic data, while the known ones were determined based on the comparison of their data with the literature values. Compounds 1-5 were evaluated for their inhibitory effects against NLRP3 inflammasome activation; compound 5 showed inhibition by an IC50 value of 6.12±0.03â µM.
Subject(s)
Diterpenes , Euphorbiaceae , Inflammasomes , NLR Family, Pyrin Domain-Containing 3 Protein , Molecular Structure , Diterpenes/pharmacology , Diterpenes/chemistry , Euphorbiaceae/chemistryABSTRACT
Three new compounds, citrusauranosides A (1), B (2), and C (3), along with 22 known compounds (4-25) were obtained from the 70% ethanol-water extract of the fruits of Citrus aurantium L.. Their structures were identified by spectroscopic methods. Among the known compounds, 14, 15, 17 and 23 were firstly obtained from Citrus genus, and the NMR data of 17 is reported here for the first time. Moreover, inhibitory effects of all compounds on motility of mouse isolated intestine tissue were determined. As a result, 1, 4-8, and 11 displayed significant inhibitory effects on contraction tension.
Subject(s)
Citrus/chemistry , Fruit/chemistry , Plant Extracts/chemistry , Animals , Humans , Male , MiceABSTRACT
Seven new protopanaxatriol type saponins, 20S-sanchirhinosides A1 (1), A2 (2), A3 (3), A4 (4), A5 (5), and A6 (6), and sanchirhinoside B (7) were obtained as minor constituents from the root extract of Panax notoginseng (Burkill, F. H. Chen), which showed protection effects against antimycin A induced mitochondrial oxidative stress. Their structures were elucidated by chemical and spectroscopic methods (IR, HRESI-TOF-MS, 1D and 2D NMR). Among them, compounds 4, 6 and 7 showed significant protective effects against antimycin A-induced L6 cell injury.
