A new anti-anxiety dietary supplement was developed for the animal health market, by combining 2 triterpene containing botanicals, Souroubea sympetala (Marcgraviaceae) with Platanus occidentalis (Platanaceae) A validated method for a quality control of the botanical blend was achieved using HPLC-APCI-MS. The method resulted in the detection and quantitative determination of betulinic acid (1), and ursolic acid (2) in P. occidentalis and 1, 2, lupeol (3), β-amyrin (4) and α-amyrin (5) in S. sympetala and the finished product Zentrol TM. Detections were at low ng on column for 1 and 2 and in low µg range for 3, 4 and 5 using calibration curves within 10-100 ng (R 2 > 0.993). Recovery of spiked samples for all the recoveries observed were > 94%. Inter-day and intraday variations were 0.8-3.5% and 5-10.4%, respectively. These results indicate the suitability of the developed analytical method to detect and quantify triterpenes of raw materials used in the manufacture of natural health products.
The Marcgraviaceae is a neotropical plant family of lianas and shrubs distributed throughout Central and South America, mainly in evergreen and semi-evergreen tropical forests. In this study, extracts of 12 Marcgraviaceae species were assessed for inhibition of bacterial quorum sensing (QS) in Chromobacterium violaceum, bacterial biofilm formation in Pseudomonas aeruginosa PA14, and fungal growth in Saccharomyces cerevisiae. Six species showed promising inhibitory activities in at least one of the three bioassays (Marcgravia nervosa Triana & Planch., Marcgravia polyantha Delp., Marcgravia schippii Standl., Marcgraviastrum subsessile (Benth.) Bedell, Schwartzia brasiliensis (Choisy) Bedell ex Gir-Cañas, and Schwartzia costaricensis (Gilg.) Bedell). Analyses of the crude extract of the leaves of Marcgravia nervosa using HPLC–APCI–MS showed the presence of five pentacyclic triterpenes: ursolic acid (2), betulinic acid (3), α–amyrin (4), β–amyrin (5), lupeol (6). Bioassay-guided fractionation of this plant resulted in the isolation and identification of 2-methoxy-1,4-naphthoquinone (1) as the active principle with a minimum inhibitory concentration (MIC) of 85–100 μmol·L−1 against Saccharomyces cerevisiae BY4741 (haploid) and BY4743 (diploid).
ABC transporters constitute a superfamily of transmembrane proteins that act mediating the translocation of several substrates across the membrane, using the energy of ATP hydrolysis. This mechanism of unrelated substrates efflux (multidrug resistance) has been associated with several diseases and it is a problem in chemotherapy efficacy. Nowadays, approximately 25% of the prescription drugs in the world are derived from plants. Casearia sylvestris is commonly found in the Americas and different parts of this plant are popularly used to treat several diseases. Previous studies have also confirmed the biological activities of C. sylvestris, such as anti-tumor, anti-leishmania, and antifungal properties. Then, the propose of this study was demonstrate that fraction 1-6 of C. sylvestris, essential oil, was able to reverse the fluconazole resistance phenotype in the Saccharomyces cerevisiae model mediated by the heterologous protein CaCdr2p from Candida albicans. The MIC value of fraction 1-6 combined with fluconazole in the checkerboard assay decreased approximately 4-fold, suggesting a synergistic effect. In addition, fraction 1-6 increased intracellular rhodamine 6G accumulation from 17% to 49% in the presence of glucose. Data indicate that C. sylvestris fraction 1-6 is a potential reverser of the fluconazole resistance phenotype.
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