Fitoterapia
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Aqueous and acetone extracts of O. stamineus leaves reduce the adhesion of uropathogenic E. coli (UPEC, strain UTI89) to T24 bladder cells significantly (IC25 ~ 524 mg/mL, resp. 40 μg/mL). The acteonic extract had no cytotoxic effects against UPEC in concentrations that inhibited the bacterial adhesion. The extract significantly reduced the gene expression of fimH, fimC, fimD, csgA and focG, which are strongly involved in the formation of bacterial adhesins. ⋯ With the exception of eupatorin, all of these flavones reduced the bacterial adhesion in a concentration depending manner, indicating that B-ring hydroxylation and methoxylation seems to have a major impact on the antiadhesive activity. In addition, this was confirmed by investigation of the flavones chrysoeriol and diosmetin, which had only very weak antiadhesive activity. From these data, Orthosiphon extracts can be assessed to have a pronounced antiadhesive activity against UPEC, based on a variety of polymethoxylated flavones.
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Fruits from Apium graveolens (Celery) are used traditionally in Persian and European medicine for the treatment of uncomplicated urinary tract infections. No data are available on A. graveolens extract on the interplay between uropathogenic E. coli and the eukaryotic host cells and on quorum sensing of the bacteria. The present study aimed to characterize an antiadhesive and anti quorum sensing effect of a characterized A. graveolens extract by specific in vitro assays and to correlate these effects with in vivo data obtained by an animal infection model. ⋯ CSE exerts a dose dependent antiadhesive activity against UPEC strains NU14 and UTI89. CSE inhibited in a concentration-dependent manner bacterial quorum sensing. 4- and 7-day pretreatment of animals with CSE transurethrally infected with UPEC NU14, significantly reduced the bacterial load in bladder tissue. CSE is assessed as an antiadhesive extract for which the traditional use in phytotherapy for UTI is justified.
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Cranberry procyanidins and quercetin derivatives are considered possible active compounds against urinary tract infections (UTIs). In this paper a small group (n=6) of healthy subjects consumed a product containing 360mg of cranberry extract (42.6% w/w of PAC-A and 14.6% w/w of PAC-B) and 200mg of quercetin. Urine samples were collected after 2,4,6,8, and 24h. ⋯ Metabolomic analysis revealed that valeric acid and valerolactone derivatives that were detected in 6 and 8h sample, while 4-hydroxy-5-(phenyl)-valeric acid-O-glucuronide and 5-(3',4'-dihydroxyphenyl)-γ-valerolactone at 6h and 4-hydroxy-5-(phenyl)-valeric acid-O-sulphate, 3-hydroxyphenyl-valeric acid, 5-(4'-hydroxyphenyl)-gamma-valerolactone-4'-O-glucuronide and 4-hydroxy-5-(3'-hydroxyphenyl)-valeric acid-3'-O-sulphate were the most abundant at 8h. The present study shows that the antiadhesive properties of urine sample after cranberry consumption are not ascribable to the direct effect of PAC-A, because their levels in urinary output are in the range of ng/mL. On the other hand, significant metabolites that were detected are mainly metabolites of intestinal action on polyphenols and PACs, as well as glucuronidated and sulphated quercetin, suggesting an important role of intestinal modification of phytoconstituents in the cranberry extract mechanism of action.
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The rhizomes from Agropyron repens are traditionally used for the treatment of uncomplicated urinary tract infections. Extracts prepared with solvents of different polarity did not show any cytotoxic effects against different strains of uropathogenic E. coli (UPEC) and human T24 bladder cells under in vitro conditions. ⋯ Bioassay guided fractionation of AAE led to the identification of (E)-hexadecyl-3-(4-hydroxyphenyl)-acrylate (hexadecyl-coumaric acid ester) 1 as the compound responsible for inhibiting the UPEC adhesion to T24 bladder cells. 1 reduced the bacterial invasion into the bladder cells as shown by a specific invasion assay. Additionally, 1 was obtained by chemical synthesis, and also the synthetic structural analogs 2 and 3 were tested for their potential antiadhesive activity, indicating that a shorter alkyl chain at the ester function as well as the lack of hydroxylation of the phenyl moiety will abolish the antiadhesive activity.
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Three new (1-3) and seven known (4-10) triterpenoids, together with one new (11) and fifteen known (12-26) dibenzocyclooctadiene lignans, were isolated from the fruit of Schisandra sphenanthera Rehd. et Wils. Their structures were elucidated by extensive analysis of spectroscopic methods, including HRESIMS, 1D and 2D NMR spectra and CD experiments. ⋯ The lignans (11-26) were tested for their neuroprotective activities against CoCl2, H2O2 and Aβ25-35-induced SH-SY5Y cell injuries and showed considerable neuroprotective effects of different degrees. And at the low concentration of 3.2nM, compounds 14, 17-19, 23 in CoCl2-induced, compounds 11, 13-15, 17, 19-20, 22-24 in H2O2-induced, and compounds 12-14, 19, 25-26 in Aβ25-35-induced SH-SY5Y cell injury models, showed statistically significant neuroprotective activities compared with the negative control group, respectively.