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A fast and efficient method for synthesising ipomone (4), a bicyclo[3.2.1]octanone containing aromatised derivative, from gibberellic acid (1) has been developed using molecular iodine as a mild and effective mediator under heating conditions in a single step. Evidence was obtained that the reaction simultaneously proceeds through aromatisation and pinacol-pinacolone type 1,2-alkyl shift. Use of excess iodine afforded iodomethyl derivative (5) that could serve as starting material for the synthesis of additional analogs. [ABSTRACT FROM AUTHOR]

Chemical composition of the essential oil (EO) of Eucalyptus tereticornis leaves was studied by gas chromatography–mass spectrometry. Forty-five constituents were identified in the oil hydrodistilled from the sample collected from Ghudda Village, Bathinda (Pb), India of which eucalyptol (34.39%) and ledol (9.92%) were the major constituents. In vitro antioxidant and anticancer potential of EO was analysed by DPPH 2,2-diphenylpicrylhydrazyl (DPPH) and MTT assay. The percentage free radical scavenging activity was found to be 63.77%. The antiproliferative activity was analysed using MTT assay in adenocarcinomic human alveolar basal epithelial A549 cancer cell line and showed IC50 value of 47.14 µg/ml. In silico study of EO, constituents were performed using Maestro 12.9 against EGFR (PDB ID-2RGP). Five constituents from EO showed high dockscore as compared to standard Mobicertinib which indicated the effectiveness of oil constituents against lung cancer. [ABSTRACT FROM AUTHOR]

One new (compound 3) along with two previously known ursane type triterpenoids (compounds 1 and 2) were purified by chromatographic techniques from ethyl acetate extract of aerial parts of Potentilla atrosanguniea and characterized by HRMS, 1 D and 2 D-NMR. Compounds 1 (ursolic acid), 2 (euscaphic acid) and 3 (3α,20α-dihydroxy 2-oxo-urs-12-en-28-oic acid) were tested for their antiproliferative activity along with standard bazedoxifene. Compounds 1 and 3 were found to be of higher activity (3.71 and 6.05 μg/mL) as compared to compound 2 and bazedoxifene (IC50: 24.53 and 17.87 μg/mL). Anti-estrogenic activity of three compounds on breast cancer (BC) were studied in vitro by accessing their antiproliferative activity and binding with estrogen receptor alpha (ER-α). All three compounds have effective binding affinity towards ER-α and decreased cell growth by downregulating the expression of mRNA and its translational protein as tested by semi-qRT-PCR and western blotting. In terms of effectiveness compounds 1 and 3 were found more active due to their antiproliferative, and antiestrogenic activity as compared to standard bazedoxifene. [ABSTRACT FROM AUTHOR]

Decalepisarayalpathra (J. Joseph and V. Chandras.) Venter, which belongs to the family Apocynaceae, is a perennial under shrub, endemic to southern Western Ghats, India. The highly aromatic tuberous roots of the D. arayalpathra are used as an effective remedy for peptic ulcer, cancer-like afflictions and as rejuvenating tonic by native tribes. The objective of this study was to characterise the root aroma of D. arayalpathra for possible industrial applications. Hydrodistilled volatile oil of the roots was analysed by gas chromatography-flame ionisation detector and gas chromatography–mass spectrometry. The volatile oil was characterised by the presence of higher amount of an industrially important flavour molecule, 2-hydroxy-4-methoxybenzaldehyde (96.8%) along with some other minor or trace constituents. Owing to characteristic vanillin-like flavour, the root oil of the D. arayalpathra can be explored as a potential substitute of vanillin-aroma in the flavour industry. [ABSTRACT FROM AUTHOR]