Antiproliferative Activity and Antioxidant Potential of Extracts of Garcinia gardneriana.

The aim of this study was to evaluate the antiproliferative activity, the antioxidant potential, and the chemical profile obtained from the whole fruit and from leaves of Garcinia gardneriana, a fruit tree from Brazilian Cerrado. To determine in vitro antiproliferative activity, the following neoplastic cell lines were considered, along with an immortalized nontumor cell line. The antioxidant potential was determined, and the evaluation of antiradical air activity was performed. The levels of vitamin C and carotenoids were determined. The chemical profile was analyzed by high-performance liquid chromatography coupled to a diode array detector and a mass spectrometer using electrospray ionization interface. The chloroform fraction of the leaf showed antioxidant activity. The vitamin C content had lower values in fruits and higher in leaves. The content of carotenoids for fruits and leaves was expressive. The ethanolic extract and the hexane and chloroform fractions of fruits were active in all neoplastic lines tested. The leaves showed cytotoxic activity in the hexane fraction in the breast carcinoma line. The analysis of data obtained verified the presence of dimers, monomers, and tetramers of hexoses, polycarboxylic acids, xanthones, flavonoids, biflavonoids, and benzophenones.

Larvicidal efficacies of plants from Midwestern Brazil: melianodiol from Guarea kunthiana as a potential biopesticide against Aedes aegypti.

A total of 36 ethanol extracts from different anatomical parts of 27 plant species (18 families), native to the Pantanal and Cerrado biomes in Midwest Brazil, was assessed for their effect against Aedes aegypti larvae, the vector of dengue, hemorrhagic dengue, Zika and chikungunya fevers. Only the extract obtained from seeds of Guarea kunthiana (Meliaceae) proved active (LC50 = 169.93 µg/mL). A bioassay-guided investigation of this extract led to the isolation and identification of melianodiol, a protolimonoid, as the active constituent (LC50 = 14.44 mg/mL). Meliantriol, which was also obtained from the bioactive fraction, was nevertheless devoid of any larval toxicity, even at the highest concentration tested (LC50 > 100.0 mg/mL). These results indicate that the larvicidal activity of melianodiol stems from the presence of the carbonyl moiety at C-3 in the 21,23-epoxy-21,24,25-trihydroxy-tirucall-7-ene-type skeleton. The structures of both protolimonoids were established on the basis of spectral methods (1H and 13C NMR and MS). This is the first report on the toxicity of melianodiol against Ae. aegypti larvae. Based on the results, melianodiol can be regarded as a potential candidate for use as an ecologically sound biocontrol agent for reducing the larval population of this vector.

3ß-O-tigloylmelianol from Guarea kunthiana: a new potential agent to control Rhipicephalus (Boophilus) microplus, a cattle tick of veterinary significance.

Chemical investigation of Guarea kunthiana fruits, guided by their effect on the reproductive cycle of engorged females of the cattle tick Rhipicephalus (Boophilus) microplus-a major economic problem to the livestock industry worldwide-led to isolation of 3ß-O-tigloylmelianol, a new protolimonoid, from the bioactive hexane phase obtained by partitioning the crude ethanol extract. An adult immersion test was performed. The compound strongly inhibited egg-laying and hatchability (99.2% effectiveness at a 0.01% concentration). Melianone, isolated from the same phase, yielded unremarkable results in the adult immersion test. From the dichloromethane phase, melianol, melianodiol, meliantriol, and a new protolimonoid, 3ß-O-tigloylmeliantriol, were isolated, all of which, in the same manner as melianone, exhibited unremarkable results in the test. The structures of new and known compounds were mostly established by 1D- and 2D-NMR analyses and mass spectrometry data. This is the first report on the bioactivity of protolimonoids on the reproductive cycle of engorged females of R. (B.) microplus. 3ß-O-Tigloylmelianol proved a promising candidate for the development of a biocontrol agent against the cattle tick investigated, as an alternative to environmentally hazardous synthetic acaricides.

Intake of Polydextrose Alters Hematology and the Profile of Short Chain Fatty Acids in Partially Gastrectomized Rats.

Polydextrose (PDX) ingestion may increase the intestinal absorption of iron. This study evaluated the effects of 7.5% polydextrose supplementation on markers of iron uptake, transport and storage in partially gastrectomized rats. Half of a batch of 40 male Wistar rats (250 g) underwent Billroth II partial gastrectomy with anterior truncal vagotomy (GXT), while the other half underwent sham gastrectomy (SHAM). At 7 postoperative days, the animals were subdivided into four groups (n = 10): Sham Control and GXT Control (no polydextrose); Sham PDX and GXT PDX (with 7.5% PDX). The animals were euthanized after 60 day of PDX treatment. Organ weight, cecal pH, the characterization and quantification of short-chain fatty acids (SCFA), hematological parameters, hepatic iron content and the expression of ferroportin (FPT) in the jejunum, cecum, colon and liver were evaluated. PDX caused changes in the cecum of the supplemented animals, where there was a decrease in pH, increase in cecal wall and marked production of SCFA, especially acetic and propionic acids (p < 0.05). Hepatic iron levels were lower in GXT animals. PDX increased hemoglobin (HGB) values by 29.2% and hematocrit (HCT) by 55.8% in the GXT PDX group compared to the GXT Control group. The GXT PDX group had lower hepatic FPT expression (p < 0.05). PDX led to increased SCFA concentration in the supplemented animals. Considering that SCFAs play a central role in the increasing nutrients uptake, this mechanism may be involved in altering the hematology profile observed in these animals but not enough to reverse iron deficiency anemia in post-gastrectomy rats.

Larvicidal efficacies of plants from Midwestern Brazil: melianodiol from Guarea kunthiana as a potential biopesticide against Aedes aegypti

A total of 36 ethanol extracts from different anatomical parts of 27 plant species (18 families), native to the Pantanal and Cerrado biomes in Midwest Brazil, was assessed for their effect against Aedes aegypti larvae, the vector of dengue, hemorrhagic dengue, Zika and chikungunya fevers. Only the extract obtained from seeds of Guarea kunthiana (Meliaceae) proved active (LC50 = 169.93 μg/mL). A bioassay-guided investigation of this extract led to the isolation and identification of melianodiol, a protolimonoid, as the active constituent (LC50 = 14.44 mg/mL). Meliantriol, which was also obtained from the bioactive fraction, was nevertheless devoid of any larval toxicity, even at the highest concentration tested (LC50 > 100.0 mg/mL). These results indicate that the larvicidal activity of melianodiol stems from the presence of the carbonyl moiety at C-3 in the 21,23-epoxy-21,24,25-trihydroxy-tirucall-7-ene-type skeleton. The structures of both protolimonoids were established on the basis of spectral methods (1H and 13C NMR and MS). This is the first report on the toxicity of melianodiol against Ae. aegypti larvae. Based on the results, melianodiol can be regarded as a potential candidate for use as an ecologically sound biocontrol agent for reducing the larval population of this vector.