Antimicrobial Assessment of Resins from Calophyllum Antillanum and Calophyllum Inophyllum.

The Calophyllum genus is well-known for its antimicrobial and cytotoxic activities, and therefore, we analyzed these biological activities for resins of Calophyllum antillanum and Calophyllum inophyllum growing in Cuba. C. antillanum resins showed a potent activity against Plasmodium falciparum (IC50 = 0.3 ± 0.1 µg/mL), while its cytotoxicity against MRC-5 cells was much lower (IC50 = 21.6 ± 1.1 µg/mL). In contrary, the resin of C. inophyllum showed an unspecific activity. The presence of apetalic acid, isoapetalic acid, calolongic acid, pinetoric acid I, pinetoric acid II, isocalolongic acid, pinetoric acid III, and isopinetoric acid III in C. antillanum resins was also confirmed. These results demonstrated for the first time the potential activity of C. antillanum resins against P. falciparum.

One-step separation and purification of two chromones and one pyrone from Aloe barbadensis Miller: a comparison between reversed-phase flash chromatography and high-speed counter current chromatography.

INTRODUCTION: Chromones and pyrones are the major secondary metabolites of Aloe barbadensis Miller. As they are minor components of the plant, an efficient purification procedure for them is of great importance for promoting their pharmacological studies. OBJECTIVE: To develop efficient methods for one-step separation and purification of two chromones (5-((S)-2'-oxo-4'-hydroxypentyl)-2-hydroxymethylchromone (1) and 5-((4E)-2'-oxo-pentenyl)-2-hydroxymethylchromone (3)) and one pyrone (aloenin aglycone (2)) from A. barbadensis via reversed-phase flash chromatography (RP-FC) and high-speed counter current chromatography (HSCCC). METHODS: The RP-FC separation was performed using methanol:water (26:74, v/v) as the mobile phase at a flow rate of 20 mL/min. A solvent system composed of dichloromethane:methanol:water (3:1.5:1, v/v/v) was used for the HSCCC separation, at a flow rate of 2.0 mL/min. RESULTS: A one-step RP-FC operation within 110 min was successfully used for the purification of compounds 1 (27.9 mg, 96.5%), 2 (32.4 mg, 98.2%) and 3 (4.1 mg, 99.0%) from 129 mg of crude sample, and a one-step HSCCC separation within 95 min was successfully implemented for the purification of compounds 1 (31.1 mg, 97.6%), 2 (35.8 mg, 96.7%) and 3 (2.7 mg, 98.1%) from 134 mg of crude sample. CONCLUSION: The developed procedures were efficient, with low cost and high yield, which would afford sufficient amounts of high-purity compounds for chromatographic purposes and pharmacological activity screening.

Properties and cost effective method for production of the antitumor agent declauxin from sporulating Penicillium herquei.

Duclauxin, an antitumor agent, was isolated from sporulating Penicillium herquei (ATCC34665) grown on a medium of peanut hulls supplemented with potato starch solution (termed "Gostar"). The medium was inoculated with a sporulating subculture of P. herquei established on a 2% potato starch slurry supplemented with mineral salts. The P. herquei grew as well on Gostar as on an enriched medium. Duclauxin was isolated in crystalline form from Gostar-grown P. herquei. Comparison of costs of duclauxin obtained from inexpensive Gostar versus costly enriched media indicated that Gostar reduces production expenses. Duclauxin was not effective as an antibiotic against certain species of gram-positive and gram-negative bacteria, fungi, and viruses, but a concentration-dependent inhibition of wheat coleoptile growth was observed. Duclauxin was characterized by melting point, optical rotation, IR and NMR spectroscopy, MS and X-ray diffraction.