ABSTRACT
Aedes aegypti L. is known as the most relevant vector mosquito for viruses such as yellow fever, chikungunya, dengue, and Zika, especially in places with unplanned urbanization, and erratic water supply. Plants used in folk medicine have become a useful source of active compounds with the potential to control the dissemination of Ae. aegypti. Compounds isolated from Malvaceae sensu lato have been previously reported as larvicides, repellents, and insecticides. Recent studies have demonstrated the anti Ae. aegypti activity of sulfated flavonoids, an uncommon type of flavonoid derivatives. This research reports the phytochemical investigation of Sidastrum paniculatum (L.) Fryxell, a Malvaceae species with the potential against Ae. aegypti. Chromatographic procedures resulted in the isolation of the compounds: stearic acid (1), N-trans-feruloyltyramine (2), acacetin (3), apigenin (4), tiliroside (5), along with the sulfated flavonoids: wissadulin (6), 7,4'-di-O-methyl-8-O-sulfate flavone (7), yannin (8), beltraonin (9a), 7-O-sulfate isoscutellarein (paniculatumin) (9b), and condadin (10). This is the first report of compound 7-O-sulfate isoscutellarein (9b). The structures were elucidated by spectroscopic analysis (NMR, LC-HRMS and FT-IR). The sulfated flavonoids identified were submitted to a ligand-based and structure-based virtual screening against two targets: 1YIY (from adult Ae. aegypti) and 1PZ4 (from Ae. aegypti larvae). The results indicated that when the O-sulfate group is bearing the position 7, the structures are potentially active in 1PZ4 protein. On the other hand, flavonoids with the O-sulfate group bearing position 8 were showed to be more likely to bind to the 1YIY protein. Our findings indicated that S. paniculatum is a promising source of sulfated flavonoids with potential against Ae. aegypti.
ABSTRACT
INTRODUCTION: Many studies support the role of vitamin D in the pathogenesis of both types of diabetes. Pancreatic tissues express the vitamin D receptor (VDR) and vitamin D-binding protein; some allelic variations in genes involved in vitamin D metabolism and VDR are associated with glucose intolerance, defective insulin secretion, and sensitivity. Epidemiological links have been established between type 2 diabetes mellitus (DM) and hepatitis C virus (HCV) infection. AIM: To explore the possible therapeutic potential of pharmacologic doses of 1-α-hydroxy vitamin D therapy in improving pancreatic ß-cell function in HCV seropositive hemodialysis (HD) patients. PATIENTS AND METHODS: Twenty HCV seropositive HD patients and 20 HCV seronegative patients as control group were randomly selected from HD units. 1-α-Hydroxy vitamin D therapy was administrated in the dose ranged from 0.25 to 0.5 µg/day for 3 months. Corrected total serum calcium, phosphorus, intact parathyroid hormone (iPTH), 25-hydroxy vitamin D [25(OH) vitamin D], 1,25-dihydroxy vitamin D, and glucoparameters [fasting blood glucose, glycohemoglobin test (HbA1c%), homeostatic model assessment (HOMA)-insulin resistance, and HOMA-ß-cell function% (B%)] were measured under basal conditions and after 3 months of therapy. RESULTS: There was highly significant improvement in the concentrations of fetal bovine serum (FBS), serum insulin, HbA1c%, 25(OH) vitamin D, and HOMA-ß-cell function in HCV seropositive and HCV seronegative groups after oral 1-alphacalcidiol therapy (p < 0.001). Positive correlation exists between the percentage increase in serum insulin and that in HOMA-ß-cell function versus 25(OH) vitamin D (p < 0.021 and p < 0.027, respectively) in HCV negative group. CONCLUSION: 1-α-Hydroxy vitamin D oral therapy may improve glycemic control in HCV seropositive and HCV seronegative HD patients.
