Oryctes rhinoceros Linn. is one of the most serious pests of coconuts and other palms. Following bioassay guided method, a larvicidal compound, 22-hydroxyhopane has been isolated for the first time from methanol extract of leaves of Adiantum latifolium Lam. against the pest (LC50 value 20.81 μg...

Ultra-performance liquid chromatography (UPLC) and Single Standard for Determination of Multi-Components (SSDMC) are becoming increasingly important for quality control of medicinal herbs; this approach was developed for Ganoderma lucidum. Special attention was necessary for the appropriate sele...

A sequence of three reactions leads to an efficient synthesis of compound 5, a model for a newly discovered phytotoxic metabolite from a plant-pathogenic fungus Bipolaris cynodontis.

A novel C33 botryococcane in a sedimentary sample from the Maoming Basin in China was found to have a methyl group positioned β to the quaternary carbon C-10 in its structure based on IR, MS and NMR analyses and Lindeman-Adams modelling. This structure is inconsistent with the prediction from t...

Torbanites are kerogen-rich deposits chiefly of the remains of a colonial alga with a morphology similar to the one of extant Botryococcus braunii. A previous comparison of an immature torbanite (NE 70) and of the resistant biopolymer isolated from the outer walls of this green alga indicated cl...

Hydrolytically labile ω-chloro-ω-phenylthioglycosides, obtained from the corresponding ω-phenylthioglycosides on treatment with NCS in CCl4, are readily dealkoxyhalogenated with Zn/Ag-graphite in anhydrous solvents affording enantiomerically pure synthons bearing an aldehyde function at the o...

A new trienomycin antibiotic, (+)-trienomycin F (4), has been isolated and characterized. The structure was elucidated via spectroscopic comparison with semisynthetic 4 prepared from (+)-trienomycinol (5). The latter sequence implemented an endgame synthetic strategy designed to furnish the trie...

The C-9 to C-14 segment, a key intermediate for the total synthesis of Trienomycin and Micotrienins has been synthesized, involving Sharpless asymmetric epoxidation intramolecular radical cyclisation and MoOPH hydroxylation as key steps.

The C-9 to C-16 fragment, a key intermediate for the synthesis of a 21 membered ansamycin antibiotic, Trienomycin has been synthesized, involving Sharpless asymmetric epoxidation and the key stereoselective methylation of γ-δ-epoxy acrylates by Trimethylaluminium.

The solubility constant of N2O in aqueous 1-dimethylamino-2-propanol (1DMA2P) solution in the concentration range of 0–3.0 mol/L was measured over the temperature range of 298–333 K, and the data used to fit existing models: Redlich-Kister, semi-empirical, and polynomial. A new model has also ...

Four ring A steroidal epoxyenones as probable intermediate in the formation of catechol estrogens were synthesized. The isometric 1α,2α-epoxy-17β-hydroxyestr-4-en-3-one (9) and 1β,2β-epoxy-17β-hydroxyestr-4-en-3-one (8) were synthesized from 17β-hydroxy-5α-estra-3-one. The isometric 4α,...

Metabolic activation of estradiol leading to the formation of catechol estrogens is a prerequisite for its genotoxic activity. Both estrogen-o-quinones/semiquinones and estrogen 1,2-epoxides have been proposed to be responsible for this activity. Incubations of [3H]estradiol and [3H]1α,2α-epox...

The structural requirement of the prostaglandin D2 molecule for binding to the synaptic membrane fraction of rat brain was extensively studied by using various prostaglandin D derivatives. Most strict specificity was found in the structures of the cyclo-pentane ring and the double bond in 13,14-...

The objective of the study was to investigate the role of prostaglandin D2 during pregnancy and its mediator Lipocalin-type prostaglandin D2 synthase (L-PGDS) as a predictor of preterm birth (PTB). Transgenic L-PGDS (+/+), L-PGDS (−/−) and C57BL/6 control pregnant mice models were used to determ...

For the determination of prostaglandin (PG) D2 produced by cultured cells in response to external stimuli, immunological methods would be convenient and useful. However, PGD2 is unstable under the physiological conditions, so that it has been difficult to get a specific antibody for the parent P...

Prostaglandin (PG) D2 is relatively unstable and dehydrated non-enzymatically into PGJ2 derivatives, which are known to serve as pro-adipogenic factors by activating peroxisome proliferator-activated receptor (PPAR) γ, a master regulator of adipogenesis. 11-Deoxy-11-methylene-PGD2 (11d-11m-PGD2...

Earlier we have reported the effect of arecoline thiazolidinone and morpholino arecoline derivatives as muscarinic receptor 1 agonists in Alzheimer’s presenile dementia models. To elucidate further our Structure–Activity Relationship (SAR) studies on the chemistry and muscarinic receptor 1 bin...

ATP-binding cassette transporter G2/breast cancer resistance protein (ABCG2/BCRP) mediates drug–drug interactions that affect the secretion of drugs into milk. The aims of this study were: (1) to determine whether the major plasma metabolites of the flukicide triclabendazole (TCBZ), triclabenda...

The aim of the current work was to evaluate a potential pharmacokinetic interaction between the flukicide triclabendazole (TCBZ) and the broad-spectrum benzimidazole (BZD) anthelmintic oxfendazole (OFZ) in sheep. To this end, both an in vitro assay in microsomal fractions and an in vivo trial in...

Direct HPLC separation of the enantiomers of triclabendazole sulfoxide (TCBZ-SO), which is the main metabolite of the anthelmintic drug triclabendazole, was carried out using the polysaccharide-based Chiralpak AS-H and Chiralpak IF-3 chiral stationary phases (CSPs). The chromatographic behaviour...