Falcipain inhibitors as potential therapeutics for resistant strains of malaria: a patent review.

Introduction: There is an urgent need to discover new antimalarial drugs due to emergence of resistance in the parasite to the existing drugs. Malarial cysteine proteases falcipin-2 (FP-2) and falcipain-3 (FP-3) are attractive targets for antimalarial chemotherapy. The structures and functions of FP-2/3, their binding domains and their interactions with small- and macro-molecules are well studied.

ACAT inhibitors: the search for novel cholesterol lowering agents.

Increased level of serum cholesterol (hyperlipidemia) is the most significant risk factor for the development of atherosclerosis. Cholesterol levels are affected by factors such as rate of endogenous cholesterol synthesis, biliary cholesterol excretion and dietary cholesterol absorption. Acyl CoA: Cholesterol O-acyl transferases (ACAT) are a small family of enzymes that catalyze cholesterol esterification and cholesterol absorption in intestinal mucosal cells and maintain the cholesterol homeostasis in the blood.

Distribution and diversity analysis of Bacillus thuringiensis cry genes in different soil types and geographical regions of India.

Molecular characterization of 117 Bacillus thuringiensis (Bt) isolates from various geographical locations was previously done by PCR amplification of cry genes. In present investigation, diversity of cry genes from different soil types and climatic environments was studied using rarefaction method. Presence of cry1, cry2, cry3, 7, 8, cry4, cry5, 12, 14, 21, cry11, cry13 and cyt1 genes from Bt strains isolated from various regions of India was determined by PCR amplification.

Formulation of niosomal gel for enhanced transdermal lopinavir delivery and its comparative evaluation with ethosomal gel.

The aim was to develop niosomal gel as a transdermal nanocarrier for improved systemic availability of lopinavir. Niosomes were prepared using thin-film hydration method and optimized for molar quantities of Span 40 and cholesterol to impart desirable characteristics. Comparative evaluation with ethosomes was performed using ex vivo skin permeation, fluorescence microscopy, and histopathology studies.

XPS, EXAFS, and FTIR as tools to probe the unexpected adsorption-coupled reduction of U(VI) to U(V) and U(IV) on Borassus flabellifer-based adsorbents.

Palm shell-based adsorbents prepared under five different thermochemical conditions and palm shell powder have been shown to be quite effective for removal of uranium from aqueous solutions. X-ray photoelectron spectroscopy (XPS), extended X-ray absorption fine structure (EXAFS), and Fourier transform infrared spectroscopy (FTIR) have been used to determine information about the speciation and binding of uranium on the adsorbents under study. Studies indicate that the uranium which is present as uranyl ion in aqueous solution is present in mixed valence states (U(IV), U(V), and U(VI)) when it is bound to the adsorbents.

Floating microspheres of valacyclovir HCl: Formulation, optimization, characterization, in vitro and in vivo floatability studies.

Floating microspheres are multiple unit Gastroretentive drug delivery systems. Valacyclovir hydrochloride (VCH) is L-valyl ester prodrug of acyclovir. VCH degrades in intestinal fluid.

Formulation and characterization of Cefuroxime Axetil nanoemulsion for improved bioavailability.

Cefuroxime Axetil nanoemulsion was formulated to address the problem of poor oral bioavailability. Formulation was manufactured utilizing Capmul MCM, Soya lecithin, Deoxycholic acid, Pluronic F127 and distilled water. Mean globular size of 121.

Improved percutaneous delivery of some NSAIDs for the treatment of arthritis.

Arthritis is a heterogeneous group of conditions that leads to joint symptoms and signs which are associated with defective integrity of articular cartilage. Major classes of drugs which are widely used for the treatment of arthritis are Non-Steroidal Anti-inflammatory Drugs (NSAIDs). Development of an efficient means of percutaneous delivery can increase drug concentration in local soft-tissues and joints while reducing the systemic distribution of a drug and its side effects.

Cartilage targeted chemical delivery of naproxen and ibuprofen for the treatment of arthritis.

NSAIDs are among the most widely used prescription drugs, for the treatment of pain and inflammation, particularly arthritis. Inhibitor of COX and NSAIDs relieve the signs and symptoms of inflammation by decreasing PG production but may cause GI and renal damage. Synthesis, stability studies and Y-imaging studies are carried out.

Synthesis of chiral bis-oxazines: a preliminary assessment of helical conformational framework.

A series of novel naphthalene attached bis-oxazines were synthesized and characterized. The bis-oxazines were studied by VT-NMR analysis to assess the possibility of conformational twist. The bis-oxazine prepared from (l)-methylvalinate show a helical conformational twist in the single crystal X-ray analysis.

Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors.

Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is a promising target for antimalarial chemotherapy and inhibition of this protease affects the growth of parasite adversely. A series of pyrido[1,2-a]pyrimidin-4-ones were synthesized and evaluated for their in vitro FP-2 inhibitory potential. Compounds (14,17) showed excellent FP-2 inhibition and can serve as lead compounds for further development of potent FP-2 inhibitors as potential antimalarial drugs.

Drug delivery systems from nose to brain.

The treatment of brain disorders is particularly challenging due to the presence of a variety of formidable obstacles to deliver drugs selectively and effectively to the brain. Blood-brain-barrier (BBB) constitutes the major obstacle to the uptake of drugs into the brain following systemic administration. Intranasal delivery offers a non-invasive and convenient method to bypass the BBB and delivery of therapeutics directly to the brain.

Ethnopharmacology guided screening of traditional Indian herbs for selective inhibition of Plasmodium specific lactate dehydrogenase.

Ethnopharmacological Relevance: Medicinal plants traditionally used to treat malaria can provide quality leads towards identifying novel anti-malarial drugs. Here we combined this approach with target based drug discovery and explored Plasmodium specific lactate dehydrogenase (LDH) inhibitory activity of 8 Indian plants which are ethnically used to treat malaria.

Methods: LDH from Indian Plasmodium falciparum and Plasmodium vivax strains, were cloned and expressed in Escherichia coli, followed by purification of recombinant enzymes (rPfLDH and rPvLDH respectively).

Acute and sub-chronic toxicological evaluation of hydro-methanolic extract of Coriandrum sativum L. seeds.

L. (CS) seeds are known to possess therapeutic potentials against a variety of physiological disorders. This study assesses acute and sub-chronic toxicity profile of hydro-methanolic extract of CS seeds using OECD guidelines.

Bioavailability enhancement of baclofen by gastroretentive floating formulation: statistical optimization, in vitro and in vivo pharmacokinetic studies.

Objectives: The study was aimed to improve bioavailability of baclofen by developing gastroretentive floating drug delivery system (GFDDS).

Methods: Preliminary optimization was done to select various release retardants to obtain minimum floating lag time, maximum floating duration and sustained release. Optimization by 3(2) factorial design was done using Polyox WSR 303 (X1) and HPMC K4M (X2) as independent variables and cumulative percentage drug released at 6 h (Q6h) as dependent variable.

Melatonin supplementation in rat ameliorates ovariectomy-induced oxidative stress.

Objective: The present study aims to determine the potential of melatonin supplementation in ameliorating tissue oxidative stress, elevated serum corticosterone and hepatic and renal dysfunction.

Materials And Methods: Adult Wistar rats, either ovariectomized or sham-operated, served as experimental or control groups, respectively. Rats received either melatonin, estrogen, progesterone or a combination of melatonin and estrogen for a period of 15 days.

Cardioprotective and antihypertensive effects of Enicostemma littorale Blume extract in fructose-fed rats.

We investigated the protective effects of Enicostemma littorale Blume (EL) extract on hypertension and insulin resistance along with its associated cardiovascular complications in high fructose (HF) fed rats. For this, rats were divided among 4 groups: (i) control, fed laboratory chow; (ii) fed with a high level of fructose; (iii) fed with a high level of fructose plus E. littorale extract; and (iv) fed with a high level of fructose plus rosiglitazone (Rg).

Studies on copper-yttria nanocomposites: high-energy ball milling versus chemical reduction method.

Oxide dispersion-strengthened copper-base composites are widely used for applications demanding high tensile strength, high hardness along with good electrical and thermal conductivity. Oxides of metals like aluminium, cerium, yttrium and zirconium are often used for this purpose as fine and uniformly distributed dispersoid particles in soft and ductile copper matrix. Such composites find applications as electrical contacts, resistance-welding tips, lead wires, continuous casting moulds, etc.

Effects of Lagenaria sicessaria fruit juice on lipid profile and glycoprotein contents in cardiotoxicity induced by isoproterenol in rats.

This study investigated antihyperlipidemic effects of Lagenaria siceraria fruit juice (LSFJ) in isoproterenol (ISO)induced cardiotoxicity in rats. Rats treated with ISO (200 mg/kg, s.c.

Synthesis of chiral helical 1,3-oxazines.

A series of novel 1,3-oxazines were prepared to construct a helical framework. The 1,3-oxazine attached to the phenanthrene unit showed a small bite angle θ (∼12°), while the units attached to [4]helicene showed a larger θ (∼35°) and exhibited helical isomers at ambient conditions. The diastereomers of the third type of helicene-like bis-oxazine attached to binaphthyl were easily separable and showed good thermal stability.

Advances in studies on collagenase inhibitors.

Matrix metalloproteinases (MMPs) play an important role in many physiological and pathological processes. Development of MMP inhibitors, in particular collagenase inhibitors, for the treatment of arthritis has been more challenging, undoubtedly. Small-molecular-weight collagenase inhibitors may be classified into several different arbitrary structural classes, depending on the catalytic zinc-binding function as well as other structural elements of the inhibitors.

Noncovalent surface grafting of uranium complexed cucurbit[5]uril oligomer onto palm shell powder: a novel approach for selective uranyl ion extraction.

Biomass - that is a new feather in your cap: palm shell powder was used as support for novel uranyl complexed cucurbit[5]uril oligomer to obtain a selective extractant for uranium. The key to the selectivity lies in the perfect environment of the two portals of cucurbit[5]uril for uranyl ion binding.

Carbon sources influence the nitrate removal activity, community structure and biofilm architecture.

Influence of the frequently used carbon sources in nitrate removal processes were evaluated in a lab-scale biofilm reactor. The NO3-N removal efficiency was in the order acetate>glucose>methanol>ethanol. Acetate-fed biofilm reduced nearly 100% NO3-N with negligible amount of NO2-N accumulation.

Protective role of Brassica olerecea and Eugenia jambolana extracts against H₂O₂ induced cytotoxicity in H9C2 cells.

This study assesses the efficacy of anthocyanin rich Brassica olerecea leaves (ARCE) and flavonoid rich Eugenia jambolana seed (EJSE) extracts as possible cardioprotective agents against hydrogen peroxide (H(2)O(2)) induced cytotoxicity in H9C2 cells. Presence of ARCE or EJSE resulted in a superior cell viability and cell integrity as revealed by cell viability and lactate dehydrogenase release assays and acridine orange and ethidium bromide staining of control and H(2)O(2) treated H9C2 cells. These extracts were also able to reduce the impact of H(2)O(2) induced lipid peroxidation and depletion of intracellular glutathione.

RFLP analysis of cry1 and cry2 genes of Bacillus thuringiensis isolates from India.

The PCR-RFLP method has been useful for detection of known genes and identification of novel genes. In the present study, degenerate primers were designed from five groups of cry1 genes for PCR-RFLP analysis. Bacillus thuringiensis (Bt) isolates from different regions were evaluated for PCR amplification of various cry1 genes using newly designed primers and cry2 genes using reported primers.