Chemical investigation of the methanolic extract of pomegranate fruit following antibacterial activity directed isolation led to the isolation of pelargonidin-3-galactose, cyanidin-3-glucose, gallic acid, quercetin, and myricetin. All these compounds exhibited substantial activity against species of corynebacteria, staphylococci, streptococci, Bacillus subtilis, Shigella, Salmonella, Vibrio cholera, and Escherichia coli. However, all these compounds were more active against Gram-positive species. On comparing the activity of all the isolated pure compounds, it was found that gallic acid showed the highest antibacterial activity against all the tested sensitive strains and the activity of the remaining pure compounds was almost same due to the structural similarities of the compounds. The reason for antibacterial activity of all pure compounds was attributed to their phenolic structure.
The chemical investigation of the ethanolic extract of the root bark of Onosma hispidum following antibacterial activity directed isolation led to the isolation of 4-hydroxy-3-methoxy cinnamic acid (ferulic acid) and 4-hydroxy-3-methoxy benzoic acid (vanillic acid) which have been reported for the first time in this species. In addition to these compounds, the crude ethanolic extract and methanol fraction exhibited substantial bioactivity against species of corynebacteria, enterococci, staphylococci and streptococci. Ferulic acid was found more bioactive (being relatively more hydrophobic) compared to vanillic acid.
Crude methanolic extracts from Grewia asiatica, Eugenia jambolana and Carissa carandas were separated into four major fractions viz. phenolic acids, flavanols, flavonols and anthocyanins which were then analysed for their total phenolic, flavonoid contents, and antimicrobial effects. In addition, anthocyanin fraction was also analysed for total anthocyanins, total colour and polymeric pigments. Total phenolics and flavonoids were highest in the fractions from E. jambolana and lowest in C. carandas, the order being phenolic acid > flavanols > flavonols > anthocyanins in all fruits. All fractions showed significant antibacterial activity except anthocyanin. Being the most active, phenolic acid fractions were also tested for their antifungal activity, the fractions of C. carandas and G. asiatica substantially inhibited all the tested fungal species. These results are being reported for the first time.
ABSTRACT:Bazedoxifene (BZA) acetate, a novel estrogen receptor modulator being developed for the prevention and treatment of postmenopausal osteoporosis, undergoes extensive metabolism in women after oral administration. In this study, the in vitro metabolism of [ 14 C]BZA was determined in human hepatocytes and hepatic and intestinal microsomes, and the UDP glucuronosyltransferase (UGT) isozymes involved in the glucuronidation of BZA were identified. In addition, BZA was evaluated for its potential as a substrate of P-glycoprotein (P-gp) transporter in Caco-2 cell monolayers. BZA was metabolized to two monoglucuronides, BZA-4-glucuronide and BZA-5-glucuronide, in hepatocytes and in liver and intestinal microsomes including jejunum, duodenum, and ileum. Both BZA-4-glucuronide and BZA-5-glucuronide were major metabolites in the intestinal microsomes, whereas BZA-4-glucuronide was the predominant metabolite in liver microsomes and hepatocytes. The kinetic parameters of BZA-4-glucuronide formation were determined in liver, duodenum, and jejunum microsomes and with UGT1A1, 1A8, and 1A10, the most active UGT isoforms involved in the glucuronidation of BZA, whereas those of BZA-5-glucuronide were determined with all the enzyme systems except in liver microsomes and in UGT1A1 because the formation of the BZA-5-glucuronide was too low. K m values in liver, duodenum, and jejunum microsomes and UGT1A1, 1A8, and 1A10, were similar and ranged from 5.1 to 33.1 M for BZA-4-glucuronide formation and from 2.5 to 11.1 M for BZA-5-glucuronide formation. V max values ranged from 0.8 to 2.9 nmol/(min ⅐ mg) protein for BZA-4-glucuronide and from 0.1 to 1.2 nmol/(min ⅐ mg) protein for BZA-5-glucuronide. In Caco-2 cells, BZA appeared to be a P-gp substrate.
Campylobacter is well recognized as the leading cause of bacterial foodborne diarrheal disease worldwide; while, poultry has been identified as a significant cause of campylobacter infection in humans. The C. jejuni has been found to be the predominant species isolated from poultry samples and, yet, responsible for the majority of human campylobacteriosis. Campylobacter spp. are small, oxidase positive, microaerophilic, curved gram-negative rods exhibiting corkscrew motility and colonize the intestinal tract of most mammalian and avian species. From its very first description in late 19th century by Theodor Escherich until nowadays, a lot of research has been carried out providing a wealth of information regarding its microbiological properties. Since novel technologies constantly emerge, increasingly advanced methods for detection, identification and typing of Campylobacter spp. are becoming available. The aim of this article is to review the recent bibliography on Campylobacter focusing, especially, on its survival and growth characteristics, the laboratory methods used for its detection and isolation from clinical, animal, environmental, and food samples, the reported methods applied for its speciation, as well as the typing systems developed for subtyping of Campylobacter.
The pharmacokinetics of one of the most widely used non‐steroidal antiinflammatory drugs, naproxen, were studied in 28 healthy human volunteers at the two most commonly used dose levels, viz., 250 mg and 500 mg, in a cross‐over design. The plasma levels of naproxen were analysed by a modified high‐pressure liquid chromatography method. The plasma concentrations at higher doses were not proportional to dose, indicating a non‐linearity in the pharmacokinetics at the dose levels studied; this finding is new since earlier studies had studied only higher doses and assumed that at lower doses the pharmacokinetics would be linear. There was, however, no significant difference in the elimination half‐life (rate constant), time to reach peak concentration (Cmax ), mean residence time (MRT), or area under first moment curve (AUMC). The clearance and distribution volume of naproxen were substantially increased at higher dose resulting in statistically lower proportional concentration and the total area under the curve (AUC). These observations are explained on the basis of a change in the plasma protein binding resulting in more free naproxen available for quicker clearance and wider penetration into tissues. These findings have several important clinical implications for the long‐term use of naproxen as an antiarthritic drug. It is proposed that the clinical efficacy of naproxen can be increased and side‐effects reduced by giving it in small divided doses instead of large doses.
Congenital arteriovenous fistulas are a rare cause of neck mass in children, but should be considered in the differential diagnosis of paediatric patients presenting with pulsatile neck masses even when there is no history of trauma. Balloon embolisation is the treatment of choice because of the high risk of surgical complications in this region.
Persistent ductus venosus as a cause of cholestatic jaundice is very rare. Treatment varies, but is usually reserved for infants in whom complications develop. We report a 5-week-old female infant with cholestatic jaundice caused by a patent ductus venosus and subsequent successful treatment via a transcatheter occlusion using a vascular plug device.
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