Identification of steroidal cardenolides from Calotropis procera as novel HIV-1 PR inhibitors: A molecular docking & molecular dynamics simulation study.

Background & objectives Despite advancements in antiretroviral therapy, drug-resistant strains of HIV (human immunodeficiency virus) remain a global health concern. Natural compounds from medicinal plants offer a promising avenue for developing new HIV-1 PR (protease) inhibitors. This study aimed to explore the potential of compounds derived from Calotropis procera, a medicinal plant, as inhibitors of HIV-1 PR.

Colour tunable photoluminescence studies of Dy/Eu co-doped BaPbAlFB glasses for epoxy-free w-LED applications.

Barium lead alumino fluoroborate (BaPbAlFB) glasses singly and co-doped with Dy and Eu ions were prepared by melt quench method and studied their photoluminescence (PL) properties along with energy migration. Singly doped Dy/Eu ions in BaPbAlFB glasses under 365 and 393 nm excitation wavelengths emit the PL bands through Dy: (F → H and F → H) and Eu: (D→F) transitions located at (Dy: 483 and 575 nm) and (Eu: 613 nm) respectively. Further, tunability of PL emissions is achieved by exciting the Dy/Eu co-doped BaPbAlFB glasses at various wavelengths.

Structural Investigation and Optical Properties of Dysprosium (Dy) Ions Doped Oxyfluoro Antimony Borate Glasses for Photonics Applications.

Dysprosium oxide-doped glasses with a composition of 60BO-10SbO-10AlO-10NaF-(10-x) LiF-xDyO (x = 0.1,0.5, 1.

White light emission from Dy-doped ZnO + BiO + BaF + BO + TeO glasses: Structural and spectroscopic properties.

The ZnO + BiO + BaF + BO + TeO (ZnBiBaBFTe) host glass was prepared by melt quenching technique with the aim of achieving white light emission from Dy ions. Their structural and spectroscopic properties were systemically investigated by X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), UV-Visible absorption, emission spectra and decay times. Judd-Ofelt (JO) parameters (Ω) evaluated from absorption spectrum were utilized to calculate the radiative parameters for F level of Dy ions.

Antiobesity efficacy of asiatic acid: down-regulation of adipogenic and inflammatory processes in high fat diet induced obese rats.

In the current study, we evaluated the effects of Asiatic acid (AA) on lipid metabolic markers in HFD-induced obese Sprague-Dawley rat model. AA (20 mg/kg BW) was administered orally to HFD-fed rats for 42 days. Changes in body composition, glucose, insulin resistance (IR) and lipid profiles of tissues, plasma and the pattern of gene expression of peroxisome proliferator-activated receptor-γ (PPAR-γ) and its target genes fatty-acid synthase (FAS), adipocyte protein-2 (aP2) and uncoupling protein-2 (UCP-2) and pro-inflammatory factor tumor necrosis factor (TNF)-α were observed in experimental rats.

Reversal of high fat diet-induced obesity through modulating lipid metabolic enzymes and inflammatory markers expressions in rats.

In this study, we evaluated the ameliorative potential of Cucurbita maxima seeds oil (CSO (100 mg/kg body weight)) supplementation to high fat diet (HFD)-induced obese rats for 30 days on the changes in body weight, markers of lipid metabolism such as LDL, HDL, triglycerides, total cholesterol, adiponectin, leptin, amylase, and lipase. We also investigated the effects of CSO on the changes of lipid metabolic enzymes such as fatty-acid synthase, acetyl CoA carboxylase, carnitine palmitoyl transferase-1, HMG CoA reductase, and inflammatory markers (TNF-α and IL-6). Administration of CSO revealed significant diminution in body weight gain, altered the activity, expressions of lipid marker enzymes and inflammatory markers.

Anti obese potential of Cucurbita maxima seeds oil: effect on lipid profile and histoarchitecture in high fat diet induced obese rats.

In this study, we made an attempt to evaluate the potential of Cucurbita maxima seeds oil (CSO) against high-fat diet (HFD)-induced obesity in rats. We investigated the effect of CSO (100 mg/kg body weight) supplementation over 30 days on the changes of HFD-induced obese rats in body weight, biochemical parameters and lipid profile as well as investigated the effects of CSO on the histopathological changes. Oral administration with CSO revealed significant diminution in body weight gain, glucose and insulin levels, which altered the activity of lipid profile and restored the pathological alterations.

Obesity-alleviating potential of asiatic acid and its effects on ACC1, UCP2, and CPT1 mRNA expression in high fat diet-induced obese Sprague-Dawley rats.

The present study evaluated the effects of asiatic acid (AA), a pentacyclic triterpenoid from Centella asiatica on lipid metabolism parameters in a rat model of obesity induced using a high fat diet (HFD) for 42 days. AA (20 mg/kg body weight [BW]) was administered orally once daily for 42 days, and an orlistat-treated group of rats (10 mg/kg BW) was included for comparison. Changes in BW, blood glucose levels, insulin resistance and leptin, adiponectin, amylase, and lipase levels in the blood; lipid profiles of plasma; liver antioxidants levels; and acetyl CoA carboxylase(ACC), uncoupling protein-2 (UCP2), and carnitine palmitoyltransferase-1 (CPT1) mRNA expression were observed in the experimental rats.

Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.

A series of colchicine site binding tubulin inhibitors were synthesized by the modification of the combretastatin pharmacophore. The ring B was replaced by the pharmacologically relevant benzothiazole scaffolds, and the cis configuration of the olefinic bond was restricted by the incorporation of a triazole and tetrazole rings which is envisaged by the structural resemblance to a tubulin inhibitor like combretastatin (CA-4). These compounds were evaluated for their antiproliferative activity on selected cancer cell lines and an insight in the structure activity relationship was developed.

Studies on effect of oat and cheese incorporation on sensory and textural quality of short-dough type biscuit.

In view of their growing importance in human nutrition, incorporation of oats and cheese during the manufacture of short-dough type biscuits was studied. Rolled oats were incorporated at 25, 35 and 45 % of refined wheat flour in short-dough type biscuit formulation. Cheddar and processed cheese were used for flavouring purpose at three levels each, viz.

Structural changes in response to bioaccumulation of iron and mercury in Chromolaena odorata (L.) King & Robins.

A comparative study was designed to elucidate the effect of iron and mercury on the morphological and anatomical changes as well as bioaccumulation potential in Chromolaena odorata. Plants were grown in half-strength Hoagland nutrient medium artificially contaminated with known quantities of HgCl2 (15 μM) and FeCl3 (1000 μM). Bioaccumulation of Hg and Fe was maximum in the root, and comparatively reduced bioaccumulation was recorded in the stem and leaves.

Synthesis of 2-anilinopyridyl-triazole conjugates as antimitotic agents.

A series of 2-anilinopyridyl–triazole conjugates (6a–t) were prepared and evaluated for their cytotoxic activity against a panel of three human cancer cell lines. Among them compounds 6q, 6r and 6s showed significant cytotoxic activity with IC50 values ranging from 0.1 to 4.

Synthesis and biological evaluation of imidazo[1,5-a]pyridine-benzimidazole hybrids as inhibitors of both tubulin polymerization and PI3K/Akt pathway.

A series of imidazo[1,5-a]pyridine-benzimidazole hybrids (5a–aa) were prepared and evaluated for their cytotoxic activity against a panel of sixty human tumor cell lines. Among them compounds 5d and 5l showed significant cytotoxic activity with GI50 values ranging from 1.06 to 14.

Optical studies of Sm³⁺ ions doped zinc alumino bismuth borate glasses.

Zinc Alumino Bismuth Borate (ZnAlBiB) glasses doped with different concentrations of samarium (Sm(3+)) ions were prepared by using melt quenching technique and characterized for their lasing potentialities in visible region by using the techniques such as optical absorption, emission and emission decay measurements. Radiative properties for various fluorescent levels of Sm(3+) ions were estimated from absorption spectral information using Judd-Ofelt (JO) analysis. The emission spectra and con-focal photoluminescence images obtained by 410 nm laser excitation demonstrates very distinct and intense orange-red emission for all the doped glasses.

Nano-CuFe2O4 as a magnetically separable and reusable catalyst for the synthesis of diaryl/aryl alkyl sulfides via cross-coupling process under ligand-free conditions.

An efficient protocol was developed for the CuFe(2)O(4) nanopowder-catalyzed aryl-sulfur bond formation between aryl halide and thiol/disulfide. A variety of aryl sulfides were synthesized in impressive yields with good chemoselectivity and functional group tolerance in the presence of a catalytic amount of CuFe(2)O(4), Cs(2)CO(3) as base, in nitrogen atmosphere, under ligand-free conditions, in DMSO as solvent at 100 °C. The catalyst is air-stable, inexpensive, magnetically separable and recyclable up to four cycles.

Recyclable heterogeneous copper oxide on alumina catalyzed coupling of phenols and alcohols with aryl halides under ligand-free conditions.

An efficient alumina-supported CuO-catalyzed O-arylation of phenols and aliphatic alcohols with various aryl as well as heteroaryl halides under ligand-free conditions are reported. This protocol provides a variety of diaryl ether and bis-diaryl ether motifs by reacting different aryl/aliphatic halides with differently substituted phenols and saturated alcohols in the presence of a catalytic amount of CuO on alumina and KOH as a base at moderate temperature under nitrogen atmosphere. The described methodology is simple, straightforward and efficient to afford the cross-coupled products in high yields under ligand-free conditions.

Papillon-Lefevre syndrome with pseudoainhum.

An interesting episode of Papillon-Lefevre syndrome in a 25-year-old female with diffuse palmoplantar keratoderma, periodontitis and pseudoainhum of the toes is reported for academic interest. Her skin lesions improved with topical keratolytics and oral retinoid (acitretin) whereas periodontic problems showed significant improvement with systemic antibiotics and proper implementation of oral hygienic measures. She is undergoing oral rehabilitation with orthodontic surgical procedures.

Recyclable heterogeneous iron catalyst for C-N cross-coupling under ligand-free conditions.

An efficient and ligand-free C-N cross-coupling of aryl halides with various heterocycles using Fe/C(g) as a recyclable catalyst is reported. The yields are excellent to moderate.

Nano indium oxide as a recyclable catalyst for C-S cross-coupling of thiols with aryl halides under ligand free conditions.

An efficient ligand-free C-S cross-coupling of aryl halides with aromatic/alkyl thiols has been developed using a catalytic amount of nanocrystalline indium oxide as a recyclable catalyst with KOH as the base in DMSO at 135 degrees C. A variety of aryl sulfides can be synthesized in excellent yields utilizing this protocol.

Indium-catalyzed C-S cross-coupling of aryl halides with thiols.

Indium-catalyzed C-S cross-coupling of aromatic and alkane thiols with aryl halides proceeds smoothly in the presence of In(OTf)(3) (10 mol %), TMEDA (20 mol %), and KOH as a base in DMSO at 135 degrees C. When this protocol was utilized, a variety of thiols could be cross-coupled with aryl halides to afford the corresponding aryl sulfides in good to excellent yields.

Copper oxide nanoparticle-catalyzed coupling of diaryl diselenide with aryl halides under ligand-free conditions.

A new, efficient and ligand-free cross-coupling reaction of aryl halides and diaryl diselenides using a catalytic amount of nanocrystalline CuO as a recyclable catalyst with KOH as the base in DMSO at 110 degrees C is reported. This protocol has been utilized for the synthesis of a variety of aryl selenides in excellent yields from the readily available aryl halides and diaryl diselenides.