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Prostate cancer is fourth most abundant cancer type around the globe. Brevifoliol, a rearranged taxoid from Taxus walllichiana needles has been derivatized as C5 esters using Steglich esterification reaction. Seventeen diverse analogues were evaluated against a panel of human cancer cell lines by MTT assay. Among these, two of the semi‐synthetic analogues, that is, 13 and 16 exhibited potent cytotoxicity, selectively against PC‐3, prostate cancer cell lines. In cell cycle analysis, analogue 13 induced S and G2/M phase arrest and induced apoptosis by activating caspase‐3. Compound 13 showed moderate efficacy in in‐vivo Ehrlich ascites carcinoma in Swiss albino mice. Further, compound 13 was found to be safe in Swiss albino mice up to 1,000 mg/kg dose in acute oral toxicity. Brevifoliol ester 13 may further be optimized for better efficacy. [ABSTRACT FROM AUTHOR]

Background Dengue fever virus transmitted by Aedes aegypti causes lethal mortalities of human beings, and, because of the lack of any vaccine, management of this vector, especially with phytochemicals, is essential. In the present investigation, the structure-activity relationship of monoterpenes and their acetyl derivatives was studied to identify structural features that are responsible for mosquitocidal activity. Results Derivatization of monoterpenes (eugenol, geraniol, linalool, L-menthol and terpeniole) followed by structure-activity relationship studies identified all five acetyl derivatives as having enhanced mosquitocidal activity against fourth-instar larvae of Aedes aegypti. Acetylation of the hydroxyl group in general increased activity in comparison with hydroxyl compounds. Based on LC50 values (ppm), the activities could be placed in the following order: eugenyl acetate (50.2) > linalyl acetate (119.7) > terpinyl acetate (287.1) > menthyl acetate (308.4) > geranyl acetate (325.5), as compared with monoterpenoids: eugenol (82.8) > linalool (242.6) > terpineol (331.7) > L-menthol (365.8) > geraniol (415.0). In eugenyl acetate, the presence of an aromatic ring and a side chain with an allylic double bond makes it most effective. Conclusion Bioactive functional groups identified in the study may contribute to the understanding of larvicidal activity of acetyl derivatives and may help in the development of ecofriendly mosquito larvicidal compounds. © 2013 Society of Chemical Industry [ABSTRACT FROM AUTHOR]

A rapid, sensitive and simple reverse-phase high-performance liquid chromatographic-electrospray ionization-mass spectrometry method for simultaneous determination of cleomiscosin A and cleomiscosin B has been developed and validated. The isomeric coumarinolignoids cleomiscosin A ( 1) and cleomiscosin B ( 2) were separated on a Waters symmetry C18 column with a solvent system composed of acetonitrile-methanol (1:2) and acetic acid-water (0.5 : 99.5) in a gradient elution mode. The absorption at 326 nm was chosen as the measuring wavelength in which resolution and baseline separation of compounds 1 and 2 could be obtained. The identity of the two isomeric compounds 1 and 2 in the samples were determined on a triple quadrupole mass spectrometer with ESI interface operating in the positive mode. Calibration curves were linear ( r2 > 0.993) over the concentration range 20-200 µg/mL for cleomiscosin A and 10-200 µg/mL for cleomiscosin B with acceptable accuracy and precision, respectively. The intra-day and inter-day precision were 1.13 and 0.82% for cleomiscosin A and 1.78 and 1.28% for cleomiscosin B, respectively. The validated method was successfully applied for the analysis of the above two compounds in different extracts of Cleome viscosa. Copyright © 2008 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]