Prenylated Phenolic Compounds from the Leaves of Sabia limoniacea and Their Antiviral Activities against Porcine Epidemic Diarrhea Virus.

Porcine epidemic diarrhea virus (PEDV), a serious swine epidemic, has been rampant in Asia since the 1990s. Despite the widespread use of PEDV vaccines, the occurrence of PEDV variants requires the discovery of new substances that inhibit these viruses. During a search for PEDV inhibitory materials from natural sources, seven new sabphenosides (1-7) and a new flavonoid (8), as well as eight known phenolic compounds (9-16), were obtained from the leaves of Sabia limoniacea. The structural determination of the new phenolic derivatives (1-8) was accomplished using comprehensive spectroscopic methods. Their absolute configurations were assigned by a combination of the ECD exciton chirality method following selective reduction and calculation of their ECD spectra. The bioactivities of the isolated compounds were measured based on their abilities to inhibit viral replication of PEDV. Among the test compounds, 15 and 16 exhibited the most promising antiviral activities, with IC50 values of 7.5 ± 0.7 µM and 8.0 ± 2.5 µM against PEDV replication. This study suggests that compounds 15 and 16 could serve as new scaffolds for the treatment of PEDV infection through the inhibition of PEDV replication.

Flavone glycosides from Sicyos angulatus and their inhibitory effects on hepatic lipid accumulation.

A library of extracted natural materials (Korea Bioactive Natural Material Bank) have been screened to discover candidates for the treatment of non-alcoholic liver disease (NAFLD), and the 70% ethanol extract of Sicyos angulatus was found to inhibit hepatic lipid accumulation. Bioassay-guided fractionation of this bioactive extract yielded five previously undescribed flavonoid glycosides and one previously undescribed flavonolignan glycoside along with seven known flavonoid glycosides. The chemical structures of these compounds were elucidated by a combination of extensive spectroscopic analysis, including MS, NMR and UV techniques. Eight compounds of all isolated compounds showed inhibitory effects on the lipid accumulation induced by high concentrations of palmitic acid and glucose in HepG2 cells. Four selected compounds were tested for lipid content in a dose-dependent manner (10, 20 and 40 µM), and among those compounds, kaempferol 3-O-ß-d-glucopyranosyl-7-O-α-l-rhamnopyranoside showed the strongest inhibition of hepatic lipid production in HepG2 cells. In an oil-red O staining assay, five compounds were shown to reduce hepatic lipid accumulation better than what was observed in the vehicle control group. The present study suggests a new class of chemical entities for developing bioactive agents for the treatment of diseases caused by fat accumulation in the liver.

Discrimination of different geographic varieties of Gymnema sylvestre, an anti-sweet plant used for the treatment of type 2 diabetes.

Gymnema sylvestre (Retz.) R.Br. ex Sm. (Asclepiadaceae) is a well-known Ayurvedic anti-sweet plant for the treatment of type 2 diabetes mellitus. Although it was previously proposed that G. sylvestre exhibits chemical variation based on geography, most research on G. sylvestre has used material originating from India. Morphological and anatomical descriptions, ITS1-5.8S-ITS2 DNA sequencing, and acid hydrolysis analyses showed that G. sylvestre samples from Vietnam are distinguishable from those of Indian origin and thus suggest a dissimilarity among G. sylvestre samples with different geographic distributions. An LC-MS-guided strategy targeting 3ß-glucuronide oleane-triterpenes in the Vietnamese G. sylvestre variety led to the isolation of four known compounds and nine previously undescribed compounds, named gymnemosides ND1-ND9. None of the isolated compounds were reported in the Indian sample, further supporting the geo-diversity of G. sylvestre. Three compounds, gymnemosides ND7-9, exerted significant stimulatory effects on the uptake of 2-NBDG in 3T3-L1 adipocyte cells and thus have potential as lead molecules for anti-diabetes agents.