Isolation, characterisation, antifungal activity and validated UPLC/MS/MS method for quantification of novel compound from Artemisia tournefortiana Reichb.

Investigation into the chemical diversity of Artemisia tournefortiana resulted in isolation of one novel compound named tournefortin A and two known artemetin and tournefortin B bioactive compounds. Tournefortin B is first time obtained from natural source. The structure of all the isolated compounds were elucidated by detailed 1D and 2D NMR including HSQC, HMBC, 1H-1HOSY and NOESY spectroscopic techniques. Minimum inhibitory concentration (MIC) of all the tested compounds against tested fungal strains lies between 0.4 and 6.4 µg/mL and lowest MIC of 0.4 µg/mL of compound tournefortin A was found against Alternaria alternate. All the isolated compounds were quantified through UPLC/MS/MS and the developed method will serve as a first fingerprint method for the rapid determination of these phytomolecules in various plant extracts. Tournefortin B was found to be present in higher concentration. The higher antifungal effect of the isolated compounds suggests that this plant could act as potential source of antimicrobial agents.[Formula: see text].

Chemical composition and pharmacological potential of aromatic water from Salix caprea inflorescence.

OBJECTIVE: To evaluate the chemical composition and pharmacological potential of hydro distillate from Salix caprea inflorescence. METHODS: Fresh flowers were subjected to conventional hydrodistillation. Antioxidant activity was assessed as free radical scavenging capacity (RSC) towards 2, 2-diphenyl-1-picrylhydrazil (DPPH) radicals. Anti inflammatory activity was examined by human red blood cell (HRBC) membrane stabilization method. Qualitative and Quantitative analysis of hexane extract of aromatic water was performed by gas chromatography (GC) and gas chromatography-mass spectrometric (GC-MS). RESULTS: A total of 19 constituents representing (99.2%) of the aromatic water were identified; Hexahydrofarnesylacetone (38.3%), 2-butyl-octanol (24.0%), 2.hexyl-1-octanol (8.6%) were the main components. Results suggest that the hydro distillate possess significant antioxidant and anti-inflammtory properties. CONCLUSIONS: The aromatic water's composition and its pharmacological evaluations has been reported in our results for this unique and endemic species.

Synthesis and screening of ursolic acid-benzylidine derivatives as potential anti-cancer agents.

Ursolic acid present abundantly in plant kingdom is a well-known compound with various promising biological activities including, anti-cancer, anti-inflammatory, hepatoprotective, antiallergic and anti-HIV properties. Herein, a library of ursolic acid-benzylidine derivatives have been designed and synthesized using Claisen Schmidt condensation of ursolic acid with various aromatic aldehydes in an attempt to develop potent antitumor agents. The compounds were evaluated against a panel of four human carcinoma cell lines including, A-549 (lung), MCF-7 (breast), HCT-116 (colon), THP-1 (leukemia) and a normal human epithelial cell line (FR-2). The results from MTT assay revealed that all the compounds displayed high level of antitumor activities compared with the triazole analogs (previously reported) and the parent ursolic acid. However, compound 3b, the most active derivative was subjected to mechanistic studies to understand the underlying mechanism. The results revealed that compound 3b induced apoptosis in HCT-116 cell lines, arrest cell cycle in the G1 phase, caused accumulation of cytochrome c in the cytosol and increased the expression levels of caspase-9 and caspase-3 proteins. Therefore, compound 3b induces apoptosis in HCT-116 cells through mitochondrial pathway.

Promise of Retinoic Acid-Triazolyl Derivatives in Promoting Differentiation of Neuroblastoma Cells.

Retinoic acid induces differentiation in various types of cells including skeletal myoblasts and neuroblasts and maintains differentiation of epithelial cells. The present study demonstrates synthesis and screening of a library of retinoic acid-triazolyl derivatives for their differentiation potential on neuroblastoma cells. Click chemistry approach using copper(I)-catalyzed azide-alkyne cycloaddition was adopted for the preparation of these derivatives. The neurite outgrowth promoting potential of retinoic acid-triazolyl derivatives was studied on neuroblastoma cells. Morphological examination revealed that compounds 8a, 8e, 8f, and 8k, among the various derivatives screened, exhibited promising neurite-outgrowth inducing activity at a concentration of 10 µM compared to undifferentiated and retinoic acid treated cells. Further on, to confirm this differentiation potential of these compounds, neuroblastoma cells were probed for expression of neuronal markers such as NF-H and NeuN. The results revealed a marked increase in the NF-H and NeuN protein expression when treated with 8a, 8e, 8f, and 8k compared to undifferentiated and retinoic acid treated cells. Thus, these compounds could act as potential leads in inducing neuronal differentiation for future studies.

Chemical composition, antimicrobial, cytotoxic and antioxidant activities of the essential oil of Artemisia indica Willd.

Essential oil from the aerial parts of Artemisia indica was analysed by GC-FID and GC-MS. A total of 43 compounds representing 96.8% of the oil were identified and the major components were found to be artemisia ketone (42.1%), germacrene B (8.6%), borneol (6.1%) and cis-chrysanthenyl acetate (4.8%). Antimicrobial activity of the oil was evaluated against seven clinically significant bacterial and two fungal strains. The essential oil and its major constituents exhibited moderate to potent, broad-spectrum antibacterial and antifungal activities targeting both Gram-positive and Gram-negative bacteria. In vitro cytotoxicity evaluation against four human cancer cell lines THP-1 (leukemia), A-549 (lung), HEP-2 (liver) and Caco-2 (colon) showed that the essential oil exhibited concentration dependant growth inhibition in the 10-100 µg/ml dilution range, with IC(50) values of 10 µg/ml (THP-1), 25 µg/ml (A-549), 15.5 µg/ml (HEP-2) and 19.5 µg/ml (Caco-2). It was interesting to note that the essential oil also exhibited potent antioxidant activity.