Synthesis of Highly Functionalized Spirocycles and Pentafulvene-Containing Dyes Involving 2-(2'-ketoalkyl)-1,3-indandiones.

Synthesis of highly functionalized spiro[4.4]nonane and spiro[4.5]decane motifs by the reaction of dimethylacetylenedicarboxylate (DMAD) with 2-(2'-ketoalkyl)-1,3-indandiones and 2-(3'-ketoalkyl)-1,3-indandiones, respectively, has been developed by utilizing a catalytic amount of DABCO. The tertiary hydroxy-containing spiro[4.4]nonane products were converted into fully conjugated pentafulvene π-systems in an acidic medium through dehydration and unprecedented C-C bond rearrangement.

A Method to Access Highly Functionalized Dibenzobicyclo[3.2.1]octadienones: Application to the Construction of the 6/6/5/6/6 Carbon Skeleton of Rubialatin A.

The dibenzobicyclo[3.2.1]octadienone scaffold, which has been found in naphthocyclinones, engelharquinones, rubialatin A, etc., has been synthesized under mild transition metal-free conditions by aryne insertion reaction with 2-keto-1,3-indandiones. The application of this methodology has been demonstrated for the synthesis of the 6/6/5/6/6 scaffold of rubialatin A. 1H NMR experimental studies confirm that the reaction proceeds through the formation of benzocyclobutane followed by a 7-member carbocycle ring.

Managing arsenic (V) toxicity by phosphate supplementation in rice seedlings: modulations in AsA-GSH cycle and other antioxidant enzymes.

The toxic and non-essential metalloid arsenic (As) is ubiquitous in the environment with its absorption from the soil into the plants' roots posing detrimental effects on the crop plants and hence the food availability and food security are also threatened. The present study was intended to reduce the As-induced toxicity in rice seedlings (Oryza sativa L.) by phosphate (PO43-). For this, three concentrations of potassium phosphate (KH2PO4), 50, 100 and 150 µM were supplemented along with 50 µM As exposure to hydroponically grown 7-day-old rice seedlings. Supplementation of PO43- significantly recovered arsenic-induced diminutions in growth parameters and photosynthetic pigment contents which were due to the significant increase in superoxide radical (SOR, O2•¯) and hydrogen peroxide (H2O2). Supplementation of 50 µM PO43- could significantly increase the activity of APX (ascorbate peroxidase) and GR (glutathione reductase) while 100 µM PO43- could increase the activity of DHAR (dehydroascorbate reductase) and monodehydroascorbate reductase (MDHAR). As the amount of PO43- was increased, the ratio of AsA/DHA (reduced to oxidized ascorbate) and GSH/GSSG (reduced to oxidized glutathione) was increased significantly due to increase in the reduced form of the non-enzymes i.e. AsA and GSH. The activity of SOD (superoxide dismutase) and GPX (guaiacol peroxidase) decreased significantly after a substantive increase in their activities due to As stress while the CAT (catalase) activity further enhanced after the supplementation of 50 and 100 µM PO43-. Thus, the As-induced oxidative stress in the rice seedlings was managed by concerted modulations in the activities of SOD, GPX, CAT and AsA-GSH cycle enzymes and metabolites.

Apoptotic Effect and Anticancer Activity of Biosynthesized Silver Nanoparticles from Marine Algae Chaetomorpha linum Extract Against Human Colon Cancer Cell HCT-116.

The green approach of nanoparticle synthesis has gained more attention by researchers because of its nontoxic, eco-friendly, biocompatible, and sustainable nature. The present research investigated the anticancer effectiveness of silver nanoparticles synthesized from marine algae Chaetomorpha linum (C. linum) against colon cancer cell HCT-116 in vitro. Biosynthesized silver nanoparticles (C-AgNPs) are characterized using UV-spectrophotometry, dynamic light scattering (DLS), X-ray powder diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), and transmission electron microscopy (TEM). We demonstrated the dose-dependent cytotoxic effect of C-AgNPs in human colorectal carcinoma cells (HCT-116) using MTT assay. The apoptosis induction in HCT-116 cells caused by C-AgNPs has studied fluorescence microscope by staining with fluorogenic agents 4',6-diamidino-2-phenylindole (DAPI), rhodamine 123, and 2',7'-dichlorodihydrofluorescein diacetate (H2DCFDA). By using a flow cytometric test, the apoptotic action of C-AgNPs was performed. The immunoblotting study of caspases, as well as pro-apoptotic and anti-apoptotic protein expression, was studied using the PCR technique to understand the underlying molecular mechanism of C-AgNPs on cancer cells. The apoptotic studies showed an increase in the expression of apoptotic caspase 3, caspase 9, BH3-interacting domain death agonist (Bid), and Bax, along with a decrease in the anti-apoptotic protein like Bcl-2 and Bcl-xl, thereby veritably confirmed by immunoblotting and qPCR technique. The biosynthesized C-AgNPs was an efficient anticancer agent that can induce apoptosis in the HCT-116 colon cells.

Development of a high-performance liquid chromatographic method for determination of letrozole in wistar rat serum and its application in pharmacokinetic studies.

A fast, sensitive, and specific reversed-phase high-performance liquid chromatographic (RP-HPLC) method for the determination of letrozole in Wistar rat serum was developed. In this method, liquid-liquid extraction of letrozole was achieved using diethyl ether as the extracting solvent. The analysis was carried out on a reversed-phase C18 (250 mm × 4.6 mm, 5 µm) column with an isocratic mobile phase of methanol-water (70:30,v/v), at a flow rate of 1.0 mL min(-1). Detection was carried out at 239 nm with a UV-visible spectrophoto-metric detector. The method was shown to be selective and linear over the concentration range of 0.15-100 µg mL(-1). The intra-day and inter-day precision studies showed good reproducibility with coefficients of variation less than 11% for the analyte. The relative errors of intra- and inter-day accuracy were within -11.52 to -2.26%. The limit of quantification was evaluated to be 0.15 µg mL(-1). The method was successfully applied for the pharmacokinetic study of letrozole after oral administration of 10 mg kg(-1) of letrozole in six healthy Wistar rats.