Antiviral chlorinated daphnane diterpenoid orthoesters from the bark and wood of Trigonostemon cherrieri

Potential Antivirals: Natural Products Targeting Replication Enzymes of Dengue and Chikungunya Viruses

“…This is an important approach since inhibition of these enzymes can disrupt virus life cycle. Most of the studies herein described were conducted in vitro using enzymatic assays [8,[47][48][49][50][51][52] or viral strain/replicon on cells evaluating replication, inhibition and/or protein expression [49, 51-54, 56, 68-71. Three studies were conducted utilizing in silico docking approach [57,58,72].…”

“…Compounds 18-20 were capable of inhibiting the DENV NS5 RdRp. Compound 19 was the most potent (IC50 = 3.1 µM), with an inhibitory activity more than 150 times lower than 3-deoxy-GTP (0.02 µM), which was used as the reference compound, 3´-deoxy GTP [49].…”

“…From the data presented in Table 1, the selective indices for compounds 18, 19, and 20 correspond to 23, 2.4, and 2.7, respectively. Compounds 18-20 were found to be more potent than chloroquine, which was used as a positive control [49]. Using a cell-based bioassay, the natural products shown in Figure 5 were also evaluated for inhibitory activities against CHIKV.…”

LC-MS2-Based dereplication of Euphorbia extracts with anti-Chikungunya virus activity

“…In an effort to identify novel inhibitors of CHIKV replication, Euphorbiaceae species have been selected and investigated by means of bioassay-guided purification, which resulted in the isolation of daphnane-and tigliane-type esters with anti-CHIKV activities [7][8][9]. In particular tigliane-type esters, such as 12-O-tetradecanoylphorbol-13-acetate (TPA) (13), phorbol-12,13-didecanoate (11) and prostratin (21), were found to be potent and selective inhibitors of CHIKV (and HIV) replication in vitro [10,11].…”

Evaluation of subchronic (13week) toxicity and genotoxicity potential of vinegar-processed Genkwa Flos

“…The flavonoids isolated from GF are known to have remarkable biological activities, such as anti-inflammatory (Lee et al, 2009), analgesic (Wang et al, 2005) and immunoregulatory action . In addition, daphnane diterpenoids isolated from GF possess antitumor (Badawi et al, 1983;Jo et al, 2012), antifertility (Hu et al, 1985), antihyperglycemic (Carney et al, 1999), and antiviral (Allard et al, 2012) properties. In particular, daphnane diterpenoids exhibit potent anti-proliferative effects against A549 human lung cancer cells in contrast to normal lung epithelial cells (Hong et al, 2010), indicating the antitumor properties of GF.…”