Porcine epidemic diarrhea virus (PEDV) infections have resulted in a severe economic loss in the swine industry in many countries due to no effective treatment approach. Fifteen oleanane triterpenes (1-15), including nine new ones (1-4 and 10-14), were isolated from the flowers of Camellia japonica, and their molecular structures were determined by extensive spectroscopic methods. These compounds were evaluated for their antiviral activity against PEDV replication, and the structure-activity relationships (SARs) were discussed. Compounds 6, 9, 11, and 13 showed most potent inhibitory effects on PEDV replication. They were found to inhibit PEDV genes encoding GP6 nucleocapsid, GP2 spike, and GP5 membrane protein synthesis based on RT-PCR data. Western blot analysis also demonstrated their inhibitory effects on PEDV GP6 nucleocapsid and GP2 spike protein synthesis during viral replication. The present study suggested the potential of compounds 6, 9, 11, and 13 as promising scaffolds for treating PEDV infection via inhibiting viral replication.
Five Ib-type cyclopeptide alkaloids, jubanines F-J (1-5), and three known compounds, nummularine B (6), daechuine-S3 (7), and mucronine K (8) were isolated from the roots of Ziziphus jujuba. Their structures were fully characterized by spectroscopic analyses in combination with chemical derivatization. Compounds 1-3, and 6 were evaluated for their antiviral activity against the porcine epidemic diarrhea virus (PEDV). Compounds 2, 3, and 6 showed potent inhibitory effects on PEDV replication.
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 IC 50 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.
Alzheimer’s disease (AD),
a neurocognitive impairment affecting
human mental capacity, is related to the accumulation of amyloid-β
peptide (Aβ) and the hyperphosphorylation of tau protein. In
addition to modern therapies approved for AD treatment, natural products
with antioxidant and anti-inflammatory properties have been studied
for their potential to prevent AD pathogenesis. Six new noroleanane
triterpenoids from the fruit peels of Camellia japonica were isolated, and their structures were determined by diverse spectroscopic
methods. The neuroprotective effects of the six new compounds were
tested against Aβ-induced neurotoxicity and neuroinflammation
in mouse hippocampal and microglial cells. In the model of HT22-transfected
cells, compounds 1–4 showed strongly
neuroprotective effects via antioxidant response element gene activation
and decreased the level of glutamate uptake. Compounds 1–4 also appeared to have strong inhibitory effects
on NO production in Aβ1–42-transfected BV2
microglial cells. A docking simulation study was used to explain the
inhibitory effects of compounds 1–4 on β-secretase 1 (BACE1). Noroleanane triterpenoids 1–4 had potential neuroprotective and
anti-inflammatory effects against Aβ-induced neuronal damage.
The structure–activity relationships of the 30 oleanane triterpenoids
from C. japonica were assessed in a model of Aβ1–42-transfected HT22 cells.
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