Diabetes mellitus is one of the most prevalant diseases of adults. Agents with alpha-glucosidase inhibitory activity have been useful as oral hypoglycemic drugs for the control of hyperglycemia in patients with type 2; noninsulin-dependent, diabetes mellitus (NIDDM). Investigation of some medicinal herbs: Urtica dioica, Taraxacum officinale, Viscum album, and Myrtus communis with alpha-glucosidase inhibitor activity was conducted to identify a prophylactic effect for diabetes in vitro. All plants showed differing potent alpha-glucosidase inhibitory activity. However, Myrtus communis strongly inhibited the enzyme (IC50 = 38 microg/mL). The inhibitory effect of these plants and some common antidiabetic drugs against the enzyme source (baker's yeast, rabbit liver, and small intestine) were also searched. Approximately all inhibitors used in this study showed quite different inhibitory activities, according to alpha-glucosidase origins. Furthermore, subsequent separation of the active material from Myrtus communis by HPLC showed that only one fraction acted as an a-glucosidase inhibitor.
The success of cancer treatment depends on the response to chemotherapeutic agents. However, malignancies often acquire resistance to drugs if they are used frequently. Combination therapy involving both a chemotherapeutic agent and molecularly targeted therapy may have the ability to retain and enhance therapeutic efficacy. Here, we addressed this issue by examining the efficacy of a novel therapeutic strategy that combines AICAR and DOX within a multifunctional platform. In this context, we reported the bottom-up synthesis of Fe 3 O 4 @SiO 2 (FITC)-FA/AICAR/ DOX multifunctional nanoparticles aiming to neutralize survivin (BIRC5) to potentiate the efficacy of DOX against chemoresistance. The structure of nanoparticles was characterized by dynamic light scattering (DLS), zeta-potential measurement, X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA), and electron microscopy (SEM and STEM with EDX) techniques. Cellular uptake and cytotoxicity experiments demonstrated preferentially targeted delivery of nanoparticles and an efficient reduction of cancer cell viability in five different tumor-derived cell lines (A549, HCT-116, HeLa, Jurkat, and MIA PaCa-2). These results indicate that the multifunctional nanoparticle system possesses high inhibitory drug association and sustained cytotoxic effect with good biocompatibility. This novel approach which combines AICAR and DOX within a single platform might be promising as an antitumor treatment for cancer.
This study was performed to demonstrate α-glucosidase and α-amylase enzyme inhibitor activities using the methanolic extracts of Elaeagnus angustifolia leaves. Methanolic extracts were prepared by two different extraction methods [accelerated solvent extractor (ASE) and Soxhlet apparatus]. The analytical procedure involved the application of liquid chromatography. Our results showed that the ASE extracts inhibited α-amylase (10-100 µg/ ml) and α-glucosidase (10-50 µg/ml) dose-dependently exhibitedrp inhibitory activities with the extracts [α-amylase (40%) and α-glucosidase (56%)]. RP-HPLC analyses of the methanolic extracts were detected with vanillic acid and 4-hydroxybenzoic acid as the main phenolic acids in all the ASE extracts. Elaeagnus angustifolia leaf extracts may be attributed to the presence of vanillic acid and 4-hydroxybenzoic acid, there by confirming with its traditional use for the management of diabetes mellitus. We implicate that the anti-diabetic activity through in vitro assessments and support to the folkloric use of this plant for controlling type-2 diabetes mellitus in Turkey.
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