deoxygoniopypyrone acetate 9, along with six known styryl lactones (1, 10-15) were also isolated and characterized. 6S-goniothalamin 1 is reported for the first time from a Goniothalamus species. 1, 11 and 12 showed cytotoxic activity against human colon and lung cancer cell lines with IC 50 values ranging from 2.38-7.59 µM.
Eight new bis-styryllactones, goniolanceolatins A−H (1−8), possessing a rare α,β-unsaturated δ-lactone moiety with a (6S)-configuration, were isolated from the CH 2 Cl 2 extract of the stembark and roots of Goniothalamus lanceolatus Miq., a plant endemic to Malaysia. Absolute structures were established through extensive 1D-and 2D-NMR data analysis, in combination with electronic dichroism (ECD) data. All of the isolates were evaluated for their cytotoxicity against human lung and colorectal cancer cell lines. Compounds 2 and 4 showed cytotoxicity, with IC 50 values ranging from 2.3 to 4.2 μM, and were inactive toward human noncancerous lung and colorectal cells. Compounds 1, 3, 6, 7, and 8 showed moderate to weak cytotoxicity. Docking studies of compounds 2 and 4 showed that they bind with EGFR tyrosine kinase and cyclin-dependent kinase 2 through hydrogen bonding interactions with the important amino acids, including Lys721,
This study is aimed at investigating the antiplasmodial activity and acute toxicity of the methanol (MeOH) extracts of the leaves and roots, and the dichloromethane (DCM) extracts of the stem bark, leaves, and roots of Goniothalamus lanceolatus. Phytochemical analysis was then carried out on the most active extract. In vivo antiplasmodial activity was assessed using the 4-day suppressive test against Plasmodium berghei ANKA (PbANKA) in mice. The plant extracts were administered intraperitoneally (i.p.) as a single dose (30 mg/kg) starting 4 h after infection. At a dose level of 30 mg/kg (i.p.), the DCM extracts of the stem bark and leaves, and the MeOH root extracts, prolonged the survival period of infected mice compared to that of the negative control. In addition, all crude extracts, except for the DCM root extract, exhibited parasitemia suppressive activity. The highest level of parasitemia suppression was recorded in mice treated with the DCM stem bark extract at 66.3%. No mortality was observed in mice treated with the DCM extracts of the stem bark and leaves, and the MeOH extract of the leaves, indicating that the LD 50 is greater than 300 mg/kg. On the other hand, both the MeOH and DCM extracts of the roots showed toxic effects at a dose of 300 mg/kg (i.p) with an 83.3% mortality rate. The results obtained indicate that the stem bark of G. lanceolatus (DCM crude extract) possesses good antiplasmodial activity against PbANKA infected mice without causing acute toxicity. Five known styrylpyrone derivatives namely goniodiol 1, 8-epi-9-deoxygoniopypyrone 2, 9-deoxygoniopypyrone 3, digoniodiol 4 and goniothalamin 5 have been isolated from the bark of Goniothalamus lanceolatus (DCM crude extract). The structures and stereochemistry of all compounds were elucidated by interpretation of spectroscopic data. This study provides a scientific basis to support the traditional use of the plant as a remedy for malaria.
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