Antiplasmodial Isoflavanes and Pterocarpans from Apoplanesia paniculata

Abstract

Bioassay-guided fractionation of an EtOH extract of the roots of the plant Apoplanesia paniculata (Fabaceae) led to the isolation of the three known compounds amorphaquinone (1), pendulone (2) and melilotocarpan C (3) and the two new pterocarpans 4 and 5. Compounds 1 and 2 exhibited good antiplasmodial activity with IC50 values of 5.7 ± 1.5 and 7.0 ± 0.8 µM, respectively. Compound 3 exhibited weak antiplasmodial activity (41.8 ± 5.2 µM), while compounds 4 and 5 were inactive. Compound 6 was synthesized to confirm the structure of 5, and it showed enhanced antiplasmodial activity (15.8 ± 1.4 µM) compared to its analogues 3 – 5.

In vitro Assessment of Antiplasmodial Activity and Acute Oral Toxicity of Dissotis rotundifolia Extracts and Fractions on Plasmodium falciparum Strains

“…Furthermore, recent reports on phytochemical studies of D. rotundifolia mainly showed the presence of phenols, flavonoids, tannins, saponins, alkaloids and coumarins [21,22]. Many compounds belonging to these classes of phytochemicals have been found to be highly potent against several sensitive and resistant strains of P. falciparum [23][24][25][26]. The presence of phytochemical and bioactive compounds in plants is responsible for the medicinal values and is indicative of their many possible therapeutic uses [27].…”

Discovery of 3-Amino-2-Hydroxypropoxyisoflavone Derivatives as Potential Anti-HCV Agents

“…A number of natural isoflavonoids along with their synthetic analogues have been found to possess extensive biological activities including antiparasitic, anti-cancer, antiviral, anti-inflammatory, antioxidant, and anti-osteoporosis effects [ 15 , 16 , 17 , 18 , 19 ]. In order to further explore antiviral effects of isoflavonoids, we describe herein the synthesis of 3-amino-2-hydroxy-propoxyisoflavone derivatives (target compounds, Figure 1 ) and their evaluations related to the inhibition of HCV replication by inducing HO-1 expression.…”