Nano-delivery Systems and Therapeutic Applications of Phytodrug Mangiferin.

In order to cure a range of ailments, scientists have investigated a number of bioactive antioxidant compounds produced from natural sources. Mangiferin, a C-glycosyl xanthone-structured yellow polyphenol, is abundant in mangoes and other dietary sources. In-depth examinations found that it is effective in the treatment of a variety of disorders due to its antiviral, anti-inflammatory, antiproliferative, antigenotoxic, antiatherogenic, radioprotective, nephroprotective, antihyperlipidemic, and antidiabetic properties.

An Unusual Case of Anderson-Fabry Disease: Case Report.

Angiokeratoma is a group of capillary malformations characterized by the formation of variably sized dark red hyperkeratotic papules. Initially, it was believed that angiokeratoma corporis diffusum was a telltale sign of Anderson-Fabry disease; however, current consensus states that it is also seen in various other lysosomal enzymatic deficiencies. In this report, we present the case of a 12-year-old boy who developed angiokeratoma corporis diffusum with sensorineural deafness, acroparesthesias, and renal involvement.

Triple combination of palliative oral metronomic chemotherapy in recurrent and metastatic epithelial ovarian cancer: A retrospective study.

Background: Ovarian cancer is a leading cause of death from gynecological cancer in the world and in India. This study aims to evaluate the efficacy and toxicity profile of oral metronomic chemotherapy (MCT) in the form of etoposide, cyclophosphamide, and tamoxifen in recurrent and metastatic ovarian cancer.

Methods: This was a retrospective observational study that included those post-treatment patients who had the recurrent or metastatic disease after completion of treatment in 2018 at Regional Cancer Centre, Bikaner, Rajasthan.

An Intention-to-Treat-Analysis of the Efficacy of Immunotherapy Using Mycobacterium W Vaccine and Purified Protein Derivative of Tuberculin for Warts With Assessment of Improvement in Quality of Life.

Introduction: Lately, immunotherapy has evolved as a safe and reliable management option for treatment of warts. Various immunogens among others in use include vaccines and antigens like purified Protein Derivative of Tuberculin (PPD) and mycobacterium w (Mw) or mycobacterium indicum prani vaccines.

Objectives: The study was aimed to assess the effectiveness and safety profile of intralesional Mw vaccine against intralesional PPD for the management of multiple warts with assessment of the improvement in quality of life (QoL) using the Dermatology Life Quality Index questionnaire.

Falknor's needling method as a potential immunotherapy in palmo-plantar warts.

Background And Aim: Treatment of palmoplantar warts is a challenge for dermatologists. We aimed to study the efficacy and safety of Falknor's needling method in palmoplantar warts.

Methods: In an open, nonrandomized study, the index wart of eligible patients was punctured several times with a 26-gauge needle to produce a "beefy" red wound.

Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety.

Herein we describe structure-activity relationship (SAR) and metabolite identification (Met-ID) studies that provided insight into the origin of time-dependent inhibition (TDI) of cytochrome P450 3A4 (CYP3A4) by compound 1. Collectively, these efforts revealed that bioactivation of the fluoropyrimidine moiety of 1 led to reactive metabolite formation via oxidative defluorination and was responsible for the observed TDI. We discovered that substitution at both the 4- and 6-positions of the 5-fluoropyrimidine of 1 was necessary to ameliorate this TDI as exemplified by compound 19.

Induction Chemotherapy Followed by Concurrent Chemoradiation in the Management of Different Stages of Cervical Carcinoma: 5-year Retrospective Study.

Aim: The data of survival for Indian cervical cancer patients treated by indigenous modifications of the protocol are scarce. The objective of this retrospective study was to analyze the efficacy and tolerability in patients of cervical carcinoma treated by neoadjuvant chemotherapy followed by concurrent chemoradiation.

Materials And Methods: Three hundred and thirty two cases of squamous cell carcinoma of cervix who received 3 cycles of neoadjuvant chemotherapy followed concurrent chemoradiation were retrospectively analyzed for overall survival (OS), disease-free survival (DFS), and local pelvic control rate.

Evaluation of CYP1A1 and CYP2B1/2 m-RNA induction in rat liver slices using the NanoString technology: a novel tool for drug discovery lead optimization.

Cytochrome P450 (CYP) induction in rodents and humans is considered a liability for new chemical entities (NCEs) in drug discovery. In particular, CYP1A1 and CYP2B1/2 have been associated with the induction of liver tumors in oncogenicity studies during safety evaluation studies of potential drugs. In our laboratory, real time PCR (Taqman) has been used to quantify the induction of rat hepatic CYP1A1 and CYP2B1/2 in precision -cut rat liver slices.

High-throughput evaluation of CYP1A1 and 2B1 induction in rat liver slices using a semi-automated system.

Drug candidates with the propensity to induce rat CYP1A1 or 2B1 isoforms are believed to possess a greater tendency to induce hepatic tumors in oncogenicity studies. We have previously published on a manual rat liver slice assay that showed a satisfactory relationship between in vitro CYP2B1 m-RNA induction using real time PCR and the ex vivo pentoxyresorufin O-dealkylase (PROD) activity in liver microsomes prepared from rats treated daily via the oral route for 14 consecutive days with inducers or non-inducers. We now describe this automated in vitro high throughput liver slice technique to screen out drug candidates that are potent rodent CYP1A1 and/or CYP2B1 inducers.

Co-induction of CYP3A12 and 3A26 in dog liver slices by xenobiotics: species difference between human and dog CYP3A induction.

The induction of dog CYP3A12 and CYP3A26 mRNA levels was evaluated in liver slices after treatment with 22 xenobiotics. Eleven of the 22 xenobiotics increased 3A12 mRNA by more than four-fold, while nine did the same for 3A26 mRNA. A four-fold increase in the mRNA level was used as the cut-off for indication of induction based on the noise level of the real time-PCR.

Temporal evaluation of CYP mRNA in mice administered with prototypical P450 inducers: comparison with conventional protein/enzyme methods.

Assessment of cytochrome P450 (CYP) induction at the mRNA level in preclinical rodent studies has gained interest in recent years, but there are still concerns regarding correlations between the mRNA and the enzyme activity levels, especially in mice. The purpose of the present study was to systematically evaluate patterns of temporal changes of CYPs 1a1, 1a2, 2b10, 3a11, and 4a10 at mRNA, protein, and activity levels in order to determine to what extent mRNA levels could be used either qualitatively or quantitatively for the assessment of CYP enzyme induction. In this study, livers from male CD-1 mice treated daily with beta-naphthoflavone, phenobarbital, dexamethasone, clofibrate, and control vehicles were collected for RNA and microsomal analysis after 0.

Bioindicators of pollution in lentic water bodies of Nagpur city.

The present study deals with assessment of water quality of four selected lakes in the Nagpur city using physicochemical and biological parameters especially phytoplankton and zooplankton community. Tropic level and pollution status of lakes were assessed on the basis of the Palmer's Pollution Index, Shannon Wiener Index and physico-chemical parameters. 57 genera belonging to 7 groups of phytoplankton and 10 genera belonging to 3 groups of zooplankton were identified from the lakes.

Posaconazole (Noxafil, SCH 56592), a new azole antifungal drug, was a discovery based on the isolation and mass spectral characterization of a circulating metabolite of an earlier lead (SCH 51048).

Posaconazole (SCH 56592) is a novel triazole antifungal drug that is marketed in Europe and the United States under the trade name 'Noxafil' for prophylaxis against invasive fungal infections. SCH 56592 was discovered as a possible active metabolite of SCH 51048, an earlier lead. Initial studies have shown that serum concentrations determined by a microbiological assay were higher than those determined by HPLC from animals dosed with SCH 51048.

Use of high-performance liquid chromatographic and microbiological analyses for evaluating the presence or absence of active metabolites of the antifungal posaconazole in human plasma.

Posaconazole (SCH 56592) is a novel broad spectrum triazole antifungal agent that is currently in phase III clinical trials for the treatment of systemic fungal infections. This study was initiated to determine if orally administered posaconazole to humans would result in the formation of active metabolite(s). Plasma samples from a multiple-rising dose study in healthy volunteers were analyzed by validated HPLC and microbiological methods.

Generic fast gradient liquid chromatography/tandem mass spectrometry techniques for the assessment of the in vitro permeability across the blood-brain barrier in drug discovery.

Rapid, generic gradient liquid chromatography/tandem mass spectrometry (LC/MS/MS) assays, designed to accelerate sample analyses, have been developed to keep pace with the productivity of advanced synthetic procedures. In this study, LC/MS/MS was combined with an in vitro, cell-based, blood-brain barrier (BBB) model to evaluate the potential of new chemical entities (NCEs) to cross the BBB. This in vitro assay provides the permeability of discovery compounds across a monolayer of a primary culture of bovine brain microvessel endothelial cells in a fraction of the time that is required for in vivo studies (brain/plasma concentrations), using only 2 mg of the compound.

Simultaneous high-performance liquid chromatographic determination of SCH 59884 (phosphate ester prodrug of SCH 56592), SCH 207962 and SCH 56592 in dog plasma.

SCH 59884 is an IV prodrug of SCH 56592, the broad-spectrum azole antifungal agent that is active both orally and intravenously in animal models of infection. SCH 56592 is in phase III clinical trials for the treatment of serious systemic fungal infections. SCH 59884 is a carboxylate ester of SCH 56592 with gamma-butyric acid phosphate.