Differential Effect of 4H-Benzo[d] [1, 3]oxazines on the Proliferation of Breast Cancer Cell Lines.

BACKGROUND: A family of 4H-benzo[d][1,3]oxazines were obtained from a group of N-(2-alkynyl)aryl benzamides precursors via gold(I) catalysed chemoselective 6-exo-dig C-O cyclization. METHOD: The precursors and oxazines obtained were studied in breast cancer cell lines MCF-7, CAMA-1, HCC1954 and SKBR-3 with differential biological activity showing various degrees of inhibition with a notable effect for those that had an aryl substituted at C-2 of the molecules. 4H-benzo[d][1,3]oxazines showed an IC50 rating from 0.30 to 157.4 µM in MCF-7, 0.16 to 139 in CAMA-1, 0.09 to 93.08 in SKBR-3, and 0.51 to 157.2 in HCC1954 cells. RESULTS: We observed that etoposide is similar to benzoxazines while taxol effect is more potent. Four cell lines responded to benzoxazines while SKBR-3 cell line responded to precursors and benzoxazines. Compounds 16, 24, 25 and 26 have the potent effect in cell proliferation inhibition in the 4 cell lines tested and correlated with oxidant activity suggesting a possible mechanism by ROS generation. CONCLUSION: These compounds represent possible drug candidates for the treatment of breast cancer. However, further trials are needed to elucidate its full effect on cellular and molecular features of cancer.

Chemometric Evaluation of RI-Induced Phytochemicals in Phaseolus vulgaris Seeds Indicate an Improvement on Liver Enzymes in Obese Rats.

Liver enzymes alterations (activity or quantity increase) have been recognized as biomarkers of obesity-related abnormal liver function. The intake of healthy foods can improve the activity of enzymes like aspartate and alanine aminotransferases (AST, ALT), γ-glutaminyl transferase (GGT), and alkaline phosphatase (ALP). Beans have a high concentration of several phytochemicals; however, Restriction Irrigation (RI) during plant development amends their synthesis. Using chemometric tools, we evaluated the capacity of RI-induced phytochemicals to ameliorate the high activity of liver enzymes in obese rats. The rats were induced with a high-fat diet for 4 months, subsequently fed with 20% cooked beans from well-watered plants (100/100), or from plants subjected to RI at the vegetative or reproduction stage (50/100, 100/50), or during the whole cycle (50/50) for 3 months. A partial least square discriminant analysis indicated that mostly flavonols have a significant association with serum AST and ALT activity, while isoflavones lowered GGT and ALP. For AST and ALT activity in the liver, saponins remained significant for hepatocellular protection and flavonoids remained significant as hepatobiliary protectants by lowering GGT and ALP. A principal component analysis demonstrated that several flavonoids differentiated 100/50 treatment from the rest, while some saponins were correlated to 50/100 and 50/50 treatments. The intake of beans cultivated under RI improves obesity-impaired liver alterations.

Common Bean Seeds Obtained by Plant Water Restriction Ameliorates Obesity-Associated Cardiovascular Risk and Insulin Resistance.

The inclusion of beans in the diet has been recommended for obesity control. However, its beneficial effect varies depending on agroclimatic factors acting during plant development. The antiobesogenic capacity of Dalia bean (DB) seeds obtained by water restriction (WR) during the vegetative or reproductive stage of plant growth (50/100 and 100/50% of soil moisture in vegetative/reproductive stage, respectively), during the whole cycle (50/50), and well-watered plants (100/100) was researched. After phytochemical characterization, harvested beans from each experimental unit were pooled among treatments, based on a multivariate canonical discriminant analysis considering concentration of non-digestible carbohydrates (total, soluble and insoluble dietary fiber and resistant starch), phenolic compounds (total phenols, flavonoids, anthocyanins and condensed tannins) and total saponins, which showed no differences among replicas of each treatment. Obesity was induced in rats (UAZ-2015-36851) with a high fat diet (HFD) for four months. Afterwards, rats were fed with the HFD supplemented with 20% of cooked DB for three months. During treatment, 100/50 beans, improved blood triglycerides, cholesterol, and glucose, and alleviated early insulin resistance (IR) related to inhibition of lipase, α-amylase and -glucosidase activity. After sacrifice, a hypolipidemic capacity and atherogenic risk reduction was observed, especially from the 100/50 treatment, suggesting that intake of DB obtained from WR may prevent IR and dyslipidemia.

Functional Properties of Prickly Pear Cactus Fruit Peels Undergoing Supplemental Irrigation and Fruit Storage Conditions.

Prickly pear cactus fruit peels have been seen as organic waste. This study explored the effect of supplemental irrigation during fruit growth of 'Roja Lisa' (Opuntia ficus-indica) prickly pear cactus on the antioxidant, hypoglycemic and hypolipidemic properties of peel extracts from fruits collected at harvest and after storage conditions. The treatments were non-irrigated and supplemental irrigation and the storage conditions were cold or room temperature, and freshly harvested fruit. After each fruit quality evaluation, peels from each treatment combination were pooled and the concentrations of phenolic compounds, inhibition of an in vitro digestive enzyme, antioxidant capacity, and in vivo hypoglycemic (- control = 268 mg/dL versus fruit peel extracts = 204 mg/dL at 30 min) and hypolipidemic (- control = 203 mg/dL versus fruit peel extracts = 148 mg/dL at 30 min) properties were determined. Therefore, fruit peels could potentially be harnessed for human health benefits, instead of treated as organic waste.

Common bean seeds from plants subjected to severe drought, restricted- and full-irrigation regimes show differential phytochemical fingerprint.

Common bean is rich in phytochemicals like polyphenols, saponins, and steroidal glycosides, but its crop is greatly affected by drought. Thus, it is necessary to identify the irrigation regimes that improves its phytochemical profile without affecting seed yield. The aim of this study was to evaluate the differential effect of severe drought (SD), restricted irrigation (RI), and full irrigation (FI) on the phytochemical fingerprint of bean seeds through liquid chromatography-mass spectrometry and chemometric approach. Partial least square-discriminant analysis (PLS-DA) indicated that seeds from plants grown under RI where differentiated from those grown under FI and SD due to their high content of quercetin 3-O-rhamnoside and luteolin 7-O-glucoside. Regarding seed yield, no significant (p < 0.05) differences were observed between RI and FI, whereas SD decreased (p < 0.05) seed yield as compared to FI (47%). These results suggest that mild hydric stress (RI) can be used to induce phytochemicals without affecting seed yield.