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Background: Several species of the genus Aspidosperma (Apocynaceae) are used for the treatment of human malaria in Brazil and other meso- and South American countries. Methods: Ethanol extract from Aspidosperma parvifolium trunk bark was submitted to acid–base extractions leading to alkaloid and neutral fractions. The alkaloid fraction was chromatographed over a silica gel column. Ethanol extract, fractions and uleine were analysed by HPLC–DAD, UPLC-ESI–MS/MS and HPLC-ESI-MicroTOF-MS. The anti-malarial activity was assayed against resistant and sensitive chloroquine Plasmodium falciparum strains by microscopic, [3H]-hypoxanthine incorporation and HRPII techniques. Cytotoxicity (CC50) was evaluated against Vero and HepG2 cell lines by the MTT technique; selectivity indexes (SI= CC50/IC50) were calculated. Results: The major peak in the HPLC–DAD chromatograms of the ethanol extract, alkaloid and neutral fractions suggested the presence of uleine that was isolated from the alkaloid fraction by column chromatography and was characterized by spectroscopic methods. A total of 15 alkaloids, besides uleine, were identified in the alkaloid fraction by UPLC-DAD-ESI–MS/MS and HPLC-ESI-MicroTOF-MS. The ethanol extract from Aspidosperma parvifolium and the neutral fraction were moderately active against P. falciparum strains. The alkaloid fraction and uleine disclosed high anti-malarial activity against chloroquine-resistant P. falciparum strain (IC50 <1 µg/mL). The ethanol extract, neutral fraction and uleine showed low cytotoxicity against Vero and HepG2 cell lines (CC50 >300 µg/mL). The alkaloid fraction showed moderate cytotoxicity to HepG2 cell line (CC50 = 74.4 µg/mL). High SI values (>10) were determined for all samples. Conclusion: Ethanol extract from Aspidosperma parvifolium trunk bark afforded uleine that is the major constituent of the alkaloid fraction and disclosed a good in vitro anti-malarial activity. Moreover, 15 other indole alkaloids have been identified along with uleine. [ABSTRACT FROM AUTHOR]

The ethanol extract and fractions from Coccoloba acrostichoides aerial parts were assayed for in vitro antimicrobial activity. The extract was active against the assayed bacteria while most of the fractions also inhibited fungal growth, especially the n-hexane and EtOAc fractions. The isolated β-sitosterol and betulin were tested, being the last one active against Fusarium oxysporum. [Copyright &y& Elsevier]

Bioguided fractionation of Xylopia sericea antiplasmodial dichloromethane leaves extract led to the isolation of (-)-7-oxo-ent-kaur-16-en-19-oic acid (C 20 H 28 O 3 ) that was identified by a combination of 1D and 2D NMR experiments (COSY, HMBC, HSQC, HSQC-TOCSY, HSQC-NOESY and NOESY) and by X-ray crystallography. A feature to be pointed out is its (4R) configuration that was inferred from the NOE experiments (HSQC-NOESY and NOESY) and X-ray crystallography. In vitro evaluation of this rare diterpene acid against the chloroquine-resistant strain Plasmodium falciparum W2 by the PfLDH method showed it disclosed a low antiplasmodial activity and was not cytotoxic to HepG2 cells (CC 50 862.6±6.7 μm) by the MTT assay. The unequivocal NMR signals assignments, the X-ray crystallographic structure, the assessment to the bioactivities and the occurrence this diterpene in X. sericea are reported here for the first time., (© 2019 Wiley-VHCA AG, Zurich, Switzerland.)

Cecropia glaziovi Sneth. (syn. C. glaziovii, C. glazioui) (Cecropiaceae) is a South American medicinal plant whose antihypertensive activity is attributed to its flavonoid and proanthocyanidin contents. The seasonal and intraspecific variations of these two classes of compounds in C. glaziovi leaves were assayed by spectrophotometry in samples of young and mature leaves collected from native, cultivated and micropropagated trees in the dry and rainy periods of the year. The total flavonoid and proanthocyanidin contents ranged from (0.64 +/- 0.21)% to (3.44 +/- 0.45)% and (2.23 +/- 0.92)% to (5.36 +/- 0.95)%, respectively, among the assayed populations. The flavonoid contents in native plants did not differ statistically between young and mature leaves within the same season, whereas it was higher in both young and mature leaves collected in the dry compared to those collected in the rainy period. For cultivated specimens, the results pointed to higher contents in the dry season, whereas no significant difference was observed for leaves of micropropagated (clone) plants collected in both periods. For the assayed populations, higher proanthocyanidin contents were found in the dry season, excepting the micropropagated (clone) plants, whose contents did not differ significantly between the dry and the rainy periods. Leaves of micropropagated (clone) and cultivated specimens showed less intraspecific variation in the flavonoid and proanthocyanidin contents than those from native trees. These features suggest that, as expected, cultivation of C. glaziovi is of great interest providing raw herbal material of better uniform quality.