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Introduction: The role of lipophilicity in drug discovery and design is a critical one. Lipophilicity is a key physicochemical property that plays a crucial role in determining ADMET (absorption, distribution, metabolism, excretion, and toxicity) properties and the overall suitability of drug candidates. There is increasing evidence to suggest that control of physicochemical properties such as lipophilicity, within a defined optimal range, can improve compound quality and the likelihood of therapeutic success. Areas covered: This review focuses on understanding lipophilicity, techniques used to measure lipophilicity, and summarizes the importance of lipophilicity in drug discovery and development, including a discussion of its impact on individual ADMET parameters as well as its overall influence on the drug discovery and design process, specifically within the past 15 years. Expert opinion: A current review of the literature reveals a continued reliance on the synthesis of novel structures with increased...

The influence of lipophilicity in drug discovery and design

Herein, we present a survey of the literature covering the development of molecular imprinting science and technology over the years 2004-2011. In total, 3779 references to the original papers, rev ...

Molecular imprinting science and technology: a survey of the literature for the years 2004-2011.

The analysis of phenolic compounds in plants attracts considerable attention. Conventional (reflux) extraction as well as microwave-assisted extraction of phenolic substances from aromatic plants using different solvents has been studied. RP-HPLC with UV detection was employed for the analysis of phenolic compounds. Total phenolic compounds were determined by the Folin–Ciocalteu assay. The amount of extractable phenolic substances for this method decreased with decreasing polarity of the solvent in the order water, 60% methanol, 60% acetone, and ethyl acetate/water (60:30, v/v) by using the conventional method. When microwave-assisted extraction was performed, the previous order was changed to 60% acetone, 60% methanol, water and ethyl acetate/water. The HPLC results have shown similar solvent effect for the two extraction methods. It was also proved that microwave-assisted extraction is a more effective technique compared to the conventional method. The extraction time was reduced, less solvent was used and the amount of extracted phenolic compounds was increased.

Application of microwave-assisted extraction to the fast extraction of plant phenolic compounds

Herbal medicines as diuretics: A review of the scientific evidence

Phytochemical and pharmacological studies on Orthosiphon stamineus Benth. (Lamiaceae) hydroalcoholic extracts

This paper presents a review of the literature concerning development of the stationary phases for thin-layer chromatography (TLC) in the last ten years. The silica gel remains the most important adsorbent for TLC separation. The kinetic properties of the silica-gel thin layer and the new TLC plates have been presented. Other materials used as stationary phase were alumina, zirconium oxide, Florisil, and ion-exchanger. Chemically new bonded stationary phase development is also discussed. The improvement of the separations of some organic mixtures by impregnation of silica gel, cellulose, or polyamide plates (with transition metal ions and silver salts) and their applications is presented. The impregnation of the thin layer with organic stationary phase and inclusion complexes is another method used for the enhancement of the separation efficiences. Another modality to improve the selectivity in TLC using ion-pairing as reagent of impregnation is described as well. The actual state of chiral separation by TLC is discussed with concrete references to recent advances in chiral stationary phases. The use of nonpolar chemically bonded stationary phases impregnated with transitional metal ions is presented as chiral stationary phases. The cellulose, modified cellulose, chitin, chitosan, and their derivatives are presented and their potential for the analysis of the racemates is discussed. The cyclodextrines and macrocyclic antibiotics were used with very good results for enantiomeric separation by TLC. A new separation approach with molecular imprinting polymers was reported as a chiral stationary phase in TLC. The examples provide a wide range of structural types that can be readily resolved enantiomerically by TLC.

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Stationary phases for thin-layer chromatography

Lipophilicity measurements by liquid chromatography.

A high performance liquid chromatographic (HPLC) method has been developed for simultaneous determination of seventeen phenolic compounds (one phenolic acid, seven cinnamic acid derivatives, four quercetin glycosides, five flavonol, and flavone aglycones) from plant material. Separation of all examined compounds was carried out in 35 minutes on a Zorbax SB‐C18 analytical column (100×3.0 mm, 3.5 µm) with methanol‐KH2PO4 buffer (40 mM, pH 2.3) as mobile phase in a linear gradient. The linearity of calibration curves for all compounds was very good (R2>0.999). The detection limits for the determined compounds were in the range of 18.4 to 91.9 ng/mL. The method was successfully applied for the determination of phenolic compounds from Geranium sanguineum dried herb, the following phenolic compounds being identified: caftaric acid (1.30 mg/g), caffeic acid (2.41 mg/g), hyperoside (1.64 mg/g), isoquercitrin (2.58 mg/g), rutin (1.71 mg/g), quercitrin (0.42 mg/g), quercetin (0.82 mg/g), kaempferol (0.19 m...

Determination of Phenolic Compounds from Geranium sanguineum by HPLC

Medicinal plants are widely used, nowadays, for the preparation of various pharmaceutical forms, or as food additives; therefore, the research focuses on validated methods of analysis by single or hyphenated HPLC. This review includes references to recent work for the analysis of flavonoids, terpenes, alkaloids, coumarins, alkamides, polyacetylene and some other compounds of interest which can be found in medicinal plants. Details of experimental conditions (sample preparation, chromatography) are included.

Simion Gocan

Papers

Phytochemical and pharmacological studies on Orthosiphon stamineus Benth. (Lamiaceae) hydroalcoholic extracts

Stationary phases for thin-layer chromatography

Lipophilicity measurements by liquid chromatography.

Determination of Phenolic Compounds from Geranium sanguineum by HPLC

Analysis of medicinal plants by hplc: recent approaches