Objective To investigate Acacia honey from different altitudes regarding total phenols and flavonoids, laser-induced fluorescence (LIF) spectra and anticancer activity against human cancer cell lines. Methods Anticancer activity was investigated using sulforhodamine B cytotoxicity assays in the following human cancer cell lines: HCT116 (colon); MCF7 (breast), and HepG2 (liver). Total phenols and flavonoids were measured using spectrophotometric methods and LIF was used to differentiate between low and high-altitude honey. Results The LIF spectra differed between low and high-altitude Acacia honey. High altitude Acacia honey was characterized by significantly lower total phenol content (81.47 ± 1.25 mg gallic acid equivalent [GAE]/100 g) and increased total flavonoids (10.63 ± 0.53 mg quercetin equivalent [QE]/100 g) versus low altitude Acacia honey (91.33 ± 0.96 mg GAE/100 g and 8.78 ± 0.23 mg QE/100 g, respectively). Low altitude Acacia honey displayed increased IC50 values against HCT116 and MCF7 cells (264.17 ± 10.5 and 482.65 ± 20.3 µg/ml, respectively) versus high altitude Acacia honey (117.99 ± 12.7 and 189.82 ± 15.8 µg/ml, respectively). Conclusions High altitude Acacia honey had significantly more effective anticancer activity against HCT116 and MCF7 cells compared with low altitude honey.

Diabetes is a major health problem that is associated with high risk of various complications. Medicinal plants hold great promise against diabetes. The traditional use of Cleome droserifolia as an antidiabetic agent was correlated to its flavonol glycosides content. In the current study, five major flavonol glycosides appeared on the RP-HPLC chromatogram of the aqueous extract namely; quercetin-3-O-β-d-glucosyl-7-O-α-rhamnoside (1), isorhamnetin-7-O-β-neohesperidoside (2), isorhamnetin-3-O-β-d-glucoside (3) kaempferol-4′-methoxy-3,7-O-α-dirhamnoside (4), and isorhamnetin-3-O-α-(4″-acetylrhamnoside)-7-O-α-rhamnoside (5). The inhibitory activities of these compounds were tested in vitro against several enzymes involved in diabetes management. Only the relatively less polar methoxylated flavonol glycosides (4, 5) showed mild to moderate α-amylase and α-glucosidase inhibitory activities. Compounds 1–4 displayed remarkable inhibition of dipeptidyl peptidase IV (DPPIV) enzyme (IC50 0.194 ± 0.06, 0.573 ± 0.03, 0.345 ± 0.02 and 0.281 ± 0.05 µg/mL, respectively) comparable to vildagliptin (IC50 0.154 ± 0.02 µg/mL). Moreover, these compounds showed high potential in preventing diabetes complications through inhibiting aldose reductase enzyme and combating oxidative stress. Both isorhamnetin glycoside derivatives (2, 3) exhibited the highest activities in aldose reductase inhibition and compound 2 (IC50 5.45 ± 0.26 µg/mL) was even more potent than standard quercetin (IC50 7.77 ± 0.43 µg/mL). Additionally, these flavonols exerted excellent antioxidant capacities through 2, 2-diphenyl-1-picrylhydrazil (DPPH) and ferric reducing antioxidant (FRAP) assays.

The present work describes the synthesis and anticancer activity of new benzimidazole derivatives bearing 1,3,4-oxadiazoles as thymidylate synthase inhibitors. The newly synthesized molecules were confirmed by NMR, mass, FT-IR and...

Background. Apoptosis, a major form of programmed cell death, plays a vital role in regulating tissue development and maintenance of homeostasis in eukaryotes. Apoptosis can occur via a death receptor-dependent extrinsic or a mitochondrial-dependent intrinsic pathway and can be induced by various chemotherapeutic agents. In this study, the anticancer activity of Saussurea costus and its mode of intervention in human cancer cells of breast, colon, and liver were investigated. Results. In this study, the bioactives of S. costus leaves were extensively extracted in five solvents of different polarity. The cytotoxicity and anticancer effect of the extracted secondary metabolites were investigated against breast (MCF-7), liver (HepG2), and colon (HCT116) cancer cell lines using a Sulphorhodamine B (SRB) assay. Secondary metabolites extracted using hexane, methanol, ethyl acetate, and chloroform had the highest cytotoxicity and thus the greatest anticancer effect on all the cancer cell lines tested (IC50; ranging from 0.25 to 2.5 μg/ml), while butanol was comparatively less active (IC50; ranging from 23.2 to 25.5 μg/ml). Further investigation using DNA flow cytometry and fluorescent microscopy revealed that the extract arrested the cells in the G1 phase of cell cycle and induced apoptosis. Furthermore, the elevated expression level of proapoptotic proteins and decreased expression level of antiapoptotic proteins confirmed that the intrinsic (mitochondrial) pathway was involved in mediating the apoptosis of cancer cells upon treatment with S. costus extract. These results altogether suggest that S. costus could be a potential anticancer agent. Conclusion. These results suggest that the S. costus extract is the potential source of the secondary metabolites that could be used as anticancer agent to treat diverse cancers of breast, colon, and liver.

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