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  • Author: Nikolas Fokialakis x
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The chemical composition of the essential oils obtained by hydrodistillation of roots, stems with leaves and inflorescences of Valeriana italica Lam. and Valeriana tuberosa L. were studied by GC/MS. Seventy-three and fourty-one constituents were identified from each plant, respectively. The major constituent of the oil obtained from the roots of V. italica was isolated and identified as 15-acetoxyvaleranone. Its stereochemistry and conformation has been studied using NMR spectroscopy and molecular modelling. The oils obtained from V. tuberosa completely lacked the characteristic valerane or kessane sesquiterpenes.

Running title: Essential oils of Valeriana italica and V. tuberosa

A new quinolone alkaloid, megistolactone (1) was isolated from the bark of Sarcomelicope megistophylla. Its structure has been elucidated on the basis of MS and NMR data. From a biogenetic point of view, this compound should be considered as an oxidation product of 1,2,3,4-tetra-O-subsituted acridone alkaloids, which are also present in the bark.

Abstract

The synthesis of 17 novel conformationally constrained pyrazole derivatives is reported herein, along with the assessment of their anti-proliferative and anti-angiogenic activities. The evaluation of their inhibitory effect on cell proliferation against HepG2, HeLa, and MCF-7 cells revealed the pyrrolo[2,3-g]indazole 23 as a potent inhibitor of cell growth with IC50 values of 5 μm. Additionally, the inhibition of vascular endothelial growth factor by pyrazoles 20 and 23 (30 % and 35 %, respectively) in HeLa supernatant cells was evidenced. These findings highlight the usefulness of these compounds as potential scaffolds for the design and development of novel anti-cancer agents with pronounced anti-angiogenic activity.