![]() ![]() Two major compounds (myricetin-3- O-rhamnoside and quercetin-3- O-rhamnoside) showed additive or synergistic effects on α-glucosidase inhibition, while displayed antagonistic effect on DPP-IV inhibition. TI exhibited the strongest inhibitory effect on the formation of AGEs with IC 50 of 0.43 ± 0.03 mg/mL ( p < 0.05). Results showed that the TF had the strongest inhibition against α-glucosidase and DPP-IV with IC 50 of 0.56 ± 0.04 and 66.08 ± 1.36 μg/mL, respectively ( p < 0.05). fruits on α-glucosidase, Dipeptidyl Peptidase-4 (DPP-IV), and the formation of Advanced Glycation End (AGE) products. SYBR green flow cytometry antimalarial drug interactions dehydroemetine drug discovery emetine malaria repositioning.This study investigated the inhibitory effects of the Ethanol Extract (EE), Free Phenolic (TF), Esterified Phenolic (TE) and Insoluble-bound Phenolic (TI) from Rhus chinensis Mill. Emetine dihydrochloride and (-)- R, S-dehydroemetine failed to show any inhibition of the hERG potassium channel and displayed activity affecting the mitochondrial membrane potential, indicating a possible multimodal mechanism of action. Drug interaction studies showed (-)- R, S-dehydroemetine to have synergistic antimalarial activity with atovaquone and proguanil. falciparum, the compound exhibited gametocidal properties with no cross-resistance against any of the multidrug-resistant strains tested. In addition to its effect on the asexual erythrocytic stages of P. falciparum compared with (-)- S, S-dehydroisoemetine (IC 50, 2.07 ± 0.26 μM), which loses its potency due to the change of configuration at C-1'. (-)- R, S-dehydroemetine (IC 50 71.03 ± 6.1 nM) was also found to be highly potent against the multidrug-resistant K1 strain of P. falciparum 80S ribosome in complex with emetine), and it was found that (-)- R, S-dehydroemetine mimicked the bound pose of emetine more closely than did (-)- S, S-dehydroisoemetine. The structures of two diastereomers of dehydroemetine were modeled on the published emetine binding site on the cryo-electron microscopy (cryo-EM) structure with PDB code 3J7A ( P. Dehydroemetine, a synthetic analogue of emetine dihydrochloride, has been reported to have less-cardiotoxic effects than emetine. The antiamoebic compound emetine dihydrochloride has been identified as a potent in vitro inhibitor of the multidrug-resistant strain K1 of Plasmodium falciparum (50% inhibitory concentration, 47 nM ± 2.1 nM ). Drug repositioning offers an effective alternative to de novo drug design to tackle the urgent need for novel antimalarial treatments. ![]()
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