Bioassay guided fractionation of Boenninghausenia sessilicarpa (Rutaceae) resulted in the isolation of a new dimeric coumarin glucoside 9′-methoxyl rutarensin (1) and a cytotoxic compound rutamarin (4), as well as an antivirus component leptodactylone (8), together with six known coumarins. Their structures were elucidated by 1D- and 2D NMR spectroscopy and ESI-MS analyses, respectively. Rutamarin (4) showed significant inhibitory activities against A-549, Bel-7402, HepG-2 and HCT-8 tumour cell lines with IC50s of 1.318, 2.082, 2.306 and 2.497 μg/ml. In addition, leptodactylone (8) showed potent protective activity on cells infected by SARS-CoV with ratio of 60% at 100 μg/ml.
Four new chromone glycosides allo-aloeresin D (2),C-2′-decoumaroyl-aloeresin G (8), 2′-O-coumaroyl-(S)-aloesinol (9), 2′-O-[p-methoxy-(E)-cinnamoyl]-(S)-aloesinol (10) and nine known chromone glycosides (1, 3 - 7, 11 - 13) were isolated from two Aloe spp. plants, A. vera and A. nobilis. Among them, 1 and 8 showed significant inhibitory activity against BACE1 (β-secretase) with IC50 values of 39.0 and 20.5 × 10-6 M, as well as inhibition of Aβ1 - 42 production by 7.4 and 12.3 %, respectively, in B103 neuroblastoma cells at 30 ppm. The preliminary structure-activity relationships of Aloe chromone glucosides were also discussed.
1 January 2006 in Journal of Asian Natural Products Research
Bioassay-guided fractionation of the ethanol extract of Senecio scandens led to the isolation of four new compounds 1–4. These compounds were obtained as tautomeric mixture of α/β epimers, but their structures were confirmed unambiguously by 1D and 2D NMR spectra and LC NMR technology. 1H NMR spectra of pure 1α and 1β were furnished by HPLC NMR technology. Compounds 1–4 exhibited moderate cytotoxicities against five tumor cell lines.
A simple, rapid, accurate, and selective quantitative nuclear magnetic resonance method for the determination of tadalafil in bulk drugs and its tablets was established and evaluated. Spectra were obtained in dimethylsulfoxide-d6 using 2,4-dinitrotoluene as the internal standard. In this study, the method’s linearity, range, limit of quantification, stability, precision, and accuracy were validated. The results were consistent with those obtained from high-performance liquid chromatography analysis. Thus, the proposed method is a useful and practical tool for the determination of tadalafil in bulk drugs and its tablets.
1 October 2008 in Journal of Asian Natural Products Research
A convenient method for the synthesis and enantiomeric resolution of ( +/- )-pinocembrin has been developed. This route involves the hydrogenation of 5,7-dihydroxyflavone, the derivatization of racemic pinocembrin with chiral amine, and the separation of the diastereoisomers due to their different physical properties.