Pharmaceuticals

This research aimed to design, optimize, and evaluate berberine-laden nanostructured lipid carriers overlaid with chitosan (BER-CTS-NLCs) for efficient brain delivery via the intranasal route. The nanostructured lipid carriers containing berberine (BER-NLCs) were formulated via hot homogenization and ultrasonication strategy and optimized for the influence of a variety of causal variables, including the amount of glycerol monostearate (solid lipid), poloxamer 407 (surfactant) concentration, and oleic acid (liquid lipid) amount, on size of the particles, entrapment, and the total drug release after 24 h. The optimal BER-NLCs formulation was then coated with chitosan. Their diameter, in vitro release, surface charge, morphology, ex vivo permeability, pH, histological, and in vivo (pharmacokinetics and brain uptake) parameters were estimated. BER-CTS-NLCs had a size of 180.9 ± 4.3 nm, sustained-release properties, positive surface charge of 36.8 mV, and augmented ex-vivo permeation via...

Apart from being one of the most important intermediates in chemical synthesis, broadly used in the formation of C–C bonds among other processes, the β-dicarbonyl structure is present in a huge number of biologically and pharmaceutically active compounds. In fact, mainly derived from the well-known antioxidant capability associated with the corresponding enol tautomer, β-diketones are valuable compounds in the treatment of many pathological disorders, such as cardiovascular and liver diseases, hypertension, obesity, diabetes, neurological disorders, inflammation, skin diseases, fibrosis, or arthritis; therefore, the synthesis of these structures is an area of overwhelming interest for organic chemists. This paper is devoted to the advances achieved in the last ten years for the preparation of 1,3-diketones, using different chemical (Claisen, hydration of alkynones, decarboxylative coupling) or catalytic (biocatalysis, organocatalytic, metal-based catalysis) methodologies: Additional...

Resumen: La bicalutamida es un antiandrógeno no esteroideo que se usa en el tratamiento del cáncer de próstata, este fármaco se une a los receptores citosólicos de andrógenos, inhibiendo así el crecimiento celular en los tejidos prostáticos. Dada la complejidad de síntesis, se facilita haciendo uso de precursores complejos; se propone un mecanismo para producir el iniciador 4-amino-2 (trifluorometil)-benzonitrilo que es el principal para llevar a cabo la síntesis. Además, se analizan los pasos de las dos vías sintéticas existentes del fármaco. Palabras clave: Bicalutamida, antiandrógeno, síntesis, precursor. Abstract: Bicalutamide is a non-steroidal anti-androgen used in the treatment of prostate cancer. This drug binds to androgen cytosolic receptors, thus inhibiting cell growth in prostate tissues. Given the complexity of synthesis, it is facilitated by making use of complex precursors; a mechanism is proposed to produce the initiator 4-amino-2-(trifluoromethyl)-benzonitrile which is the main one to perform synthesis. In addition, the steps of the drug´s two existing synthetic pathways are analyzed.

The annual worldwide suicide rate currently averages approximately 13 per 100,000 individuals per year (0.013% per year), with higher average rates for men than for women in all but a few countries, very low rates in children, and relatively high rates in elderly men. Suicide rates vary markedly between countries, reflecting in part differences in case-identification and reporting procedures. Rates of attempted suicide in the general population average 20-30 times higher than rates of completed suicide, but are probably under-reported. Research on the relationship between pharmacotherapy and suicidal behavior was rare until a decade ago. Most ecological studies and large clinical studies have found that a general reduction in suicide rates is significantly correlated with higher rates of prescribing modern antidepressants. However, ecological, cohort and case-control studies and data from brief, randomized, controlled trials in patients with acute affective disorders have found increases, particularly in young patients and particularly for the risk of suicide attempts, as well as increases in suicidal ideation in young patients. whether antidepressants are associated with specific aspects of suicidality (e.g., higher rates of completed suicide, attempted suicide and suicidal ideation) in younger patients with major OPEN ACCESS Pharmaceuticals 2010, 3 2862 affective disorders remains a highly controversial question. In light of this gap this paper analyzes research on the relationship between suicidality and antidepressant treatment.

Health care providers (HCPs) are increasingly aware of pressures on funding for health care services, including high cost medicines (HCMs). Allocating resources to innovative and expensive medications is particularly challenging and the decisionmaking processes and criteria used to allocate resources to HCMs have not been widely described in the literature. This case study aimed to describe the operations of the first reported High Cost Drug Sub-Committee (HCD-SC) in a public hospital in Australia. In addition the study also evaluated the decision-making process using Daniel and Sabin's ethical framework of "accountability for reasonableness". Some lessons emerged from the description of the operations of the HCD-SC. Decisions were not solely based on effectiveness and cost. Additional factors such as "clinical need" and the lack of an alternative treatment were involved in decisions about access to HCMs. Members of the HCD-SC also considered it was important to have consistency in the way decisions were being made. The findings from this study provide an evidence base for developing strategies to improve this hospital's decision-making process regarding access to HCMs.

Background: Calcium channel blockers are widely prescribed either as monotherapies or in combination therapies in the management of hypertension and other cardiovascular disorders. One of the major challenges with this class of drugs is their association with difficult to treat peripheral edema. There is limited literature evidence on the incidence and severity of CCB induced edema and the efficacy of management practices in developing countries. This study therefore aims to assess incidence and the common treatments. Methods: A total of 193 eligible subjects were enrolled into an eight week study and allocated into three treatment groups for each drug [Amlodipine 10mg or Nifedipine 20mg]. One group received no intervention, while the other two groups received either Bendrofluthiazide 5mg [BDF] or Lisinopril 5mg depending on blood pressure or other patient factors. Edema was monitored every two weeks throughout the study using standard tools. The data were analyzed using students t test, one way ANOVA and descriptive statistics as appropriate. P values ≤ 0.05 was considered statistically significant. Results/Discussion: The overall incidence of edema was about 29% at the end of the study period. Lisinopril addition to therapy resulted in significant reduction in incidence and severity of edema as opposed to other interventions. This suggests that ACEIs have a positive role in minimizing incidence of peripheral edema. Conclusion: Peripheral edema remains a complication factor in CCB therapy and ACEIs may be considered in management of edema induced by this class of drugs.

Microbubbles system is a newly invented non-invasive technique in which, in the presence of ultrasound waves or harmonic sounds
micropores shrinks and agitated to produce micro bubbles within the applied area. These bubbles have the capability to target any perfused
tissues within our body. Recently it was postulated that due to its narrow size range (1 to 10μm vesicular diameter) it can get easily engulf
by phagocytic blood cells which can be very effective on lymphocytic cancer. Micro bubbles are prepared by using mechanical agitation,
ultrasonication, pressurized gas-liquid mixing system etc. Micro bubbles are made up of a monolayer of protein shells, lipid shells, surfactant
shells, polymer shells, Polyelectrolyte multilayer shells. Initially, microbubbles are used as diagnostic tools but due to its versatility of uses and properties of surface conjugation of proteins, genes, micro molecular nutrients, drugs slowly it’s becoming a therapeutic delivery tool. ALBUNEX® (GE Healthcare) was the first albumin conjugated micro bubble which was been approved by US-FDA. Recently importance is been given for brain targeting using Micro bubble carrier system. It was observed that using passive and active transport micro streamed bubbles can able to transport through Blood Brain Barrier (BBB). It is very important to give more importance to its stability and canonization of globules for more industrial acceptability.

j o u r n a l h o m e p a g e : w w w . e l s e v i e r . c o m / l o c a t e / c h r o m b Fast liquid chromatography-quadrupole linear ion trap-mass spectrometry analysis of polyunsaturated fatty acids and eicosanoids in human plasma ଝ Available online xxx Keywords: Mass spectrometry Fast liquid chromatography Linear ion trap On-line solid-phase extraction Eicosanoids Polyunsaturated fatty acid metabolism a b s t r a c t

The present study was designed to develop a simple, validated liquid chromatographic method for the analysis of azithromycin in bulk and pharmaceutical dosage forms using ultraviolet detector. The best stationary phase was determined as C18 column, 5 μm, 250 mm × 4.6 mm. Mobile phase was optimized to obtain a fast and selective separation of the drug. Flow rate was 1.5 mL/min, Wavelength was set at 210 nm and the volume of each injection was 500 μL. An isocratic methanol/buffer mobile phase at the ratio of 90:10 v/v gave the best separation and resolution. The proposed method was accurate, precise, sensitive, and linear over a wide range of concentration of azithromycin. The developed method has the advantage of using UV detector compared to the USP method in which electrochemical detector has been used. The validated method was successfully applied to the determination of azithromycin in bulk and pharmaceutical dosage forms.

The aim of the present study was to formulate and evaluate Metformin HCl microspheres to produce a drug delivery system with better pharmaceutical and therapeutic properties. Metformin HCl microspheres were prepared by using ethyl cellulose as a release retardant polymer by solvent evaporation method .Formulations F1, F2 and F3 were prepared using ethyl cellulose in the drug polymer ratio of 1:1, 1:2 and 1:3. A plasticizer (N-dibutyl phthalate) was added in formulations F4,F5 and F6 .The prepared microspheres were evaluated for the parameters like Percentage yield, Particle size analysis, Micromeritic properties like angle of repose, bulk density, tapped density, compressibility index, Hausner’s ratio, melting point determination, drug content estimation, microencapsulation efficiency and in vitro drug release studies. The in vitro release of Metformin HCl was slow and extended over longer period of time. As the concentration of polymer was increased, the drug release was decreased. The drug release was found to be slow in formulations F4, F5 and F6 when compared to F1, F2 and F3. Thus the study clearly indicated a promising potential of sustained release Metformin HCl microspheres containing ethyl cellulose as rate controlling polymer for effectively treating diabetes mellitus.

A vancomicina é um antimicrobiano glicopeptídeco indicado em situações de infecções graves por MSRA, com uso difundido nas UTIs devido, sobretudo, às características assistenciais e ao perfil dos pacientes. No entanto, em virtude de apresentar estreita faixa terapêutica, apresenta variações importantes dos seus níveis séricos a partir da existência de algumas condições clínicas. Nesse sentido, o presente estudo teve como objetivo analisar os fatores que podem alterar a concentração sérica de vancomicina em pacientes em UTIs. Foi realizada uma revisão integrativa da literatura, durante março de 2020, nas bases de dados Scientific Electronic Library Online, Medical Literature Analysis and Retrieval System Online e Literatura Latino-Americana e do Caribe em Ciências da Saúde, através de três estratégias de busca formuladas a partir dos Descritores em Ciências da Saúde e cruzadas por meio do operador booleano AND. Foram encontrados 126 artigos, dos quais 32 compuseram o corpus de análise da pesquisa. A análise de conteúdo resultou na construção das categorias Função renal, Sepse, Peso, Idade, Queimadura, Terapias de substituição renal, Proteínas séricas, Ventilação mecânica, Incompatibilidades medicamentosas e Oxigenação por membrana extracorpórea. Observou-se que a existência de variados fatores que alteram a concentração sérica de vancomicina ratifica a necessidade de qualificação das iniciativas de segurança do paciente diante de estratégias que possibilitem o alcance do sucesso clínico e microbiológico da vancomicina.

Duvelisib (Copiktra®) is a dual inhibitor of phosphoinositide 3-kinases (PI3Kδ and PI3Kγ). In 2018, duvelisib was first approved by the Food and Drug Administration (FDA) for the treatment of adult patients with relapsed or refractory chronic lymphocytic leukaemia (CLL)/ small lymphocytic lymphoma (SLL) after at least two prior therapies. Duvelisib has also been approved under accelerated track for relapsed or refractory follicular lymphoma (FL) after at least two prior systemic therapies. In this review, we provide a series of information about duvelisib, such as the development of clinical trials for LLC/SLL and FL and the steps used for its synthesis.

In this review, we discuss novel natural products discovered within the last decade that are reported to have antifungal activity against pathogenic species. Nearly a hundred natural products were identified that originate from bacteria, alga, fungi, sponges and plants. Fungi were the most prolific source of antifungal compounds discovered during the period of review. The structural diversity of these antifungal leads encompasses all the major classes of natural products including polyketides, shikimate metabolites, terpenoids, alkaloids and peptides.

Richard Crocombe of Crocombe Spectroscopic Consulting surveys the use of portable spectrometers in pharmaceutical manufacturing, with an emphasis on vibrational spectroscopy. Ideal and typical features of portable spectrometers are reviewed, alongside explanation of why device characteristics and sample presentation are critical to obtaining meaningful results.

This paper formulates an empirical methodology that evaluates pharmaceutical innovation in the American antidepressant market by quantifying patient welfare benefits from innovation. While evaluating pharmaceutical innovation in antidepressants, I uncover and address the moral hazard issue that arises due to the existence of prescription drug insurance coverage. A combination of market-level data, drug and patient characteristics are used to estimate demand for all antidepressants between 1980 and 2001. The paper estimates large and varied patient welfare gains due to innovation and helps explain a detected divergence between social and private patient benefits by the existence of insurance.

With emergence of year 2020, the world has come up with a disaster in the form of SARS-CoV-2 or COVID-19 infection. Its outbreak forces the WHO to consider it as a pandemic disease, due to its worldwide transmission with crucial symptoms. Its impact was first noticed in Wuhan, China in December 2019 and hence term coined COVID-19 to this fatal disorder. The medical system is being put under pressure to control its spread and create more recovery. For primary measure to resolve the spread chain of infection the administration declared lockdown for discontinuity as social distancing is one of the weapons to fight against it. However, this pandemic harms the economy worldwide. But during this challenging scenario, the Pharmaceutical and Biotech industries around the world are having an opportunity to continue research in collaboration with renowned Universities research centers, government agencies for the novel discovery of vaccines based on innovative technologies to manage the treatment and to supply it globally. In this review article, based on the recent publication evidence, we fundamentally compile the challenges and opportunities facing by pharmaceutical industries for finding the vaccine and cure for pandemic COVID-19. This review anthologizes the various technologies based on which preventive and treatment measures would be prepared and providing a reference for future studies.

tCanada is the only Universal Health Insurance country in the OECD without universal insurance for outpa-tient prescription drugs, a situation generally perceived as unfair and inefficient. In June 2018, the federalgovernment launched an Advisory Council on the Implementation of National Pharmacare, to report in2019 on the best strategy to implement a national Pharmacare program that would provide all Canadiansaccess to affordable outpatient prescription drugs. The Council was asked to consider three options: auniversal public plan for all Canadians; a public catastrophic insurance plan that would kick off oncespending on prescription drugs reaches a given threshold; and a more modest patching of existing gaps,providing coverage to those who are not eligible to any form of insurance. Beyond the relative consensusaround the ideas that gaps in coverage should be filled to make drugs affordable to all, and that the costsof drugs are too high in Canada, the Council faces the challenge of addressing three underlying issues:1) what amount of income redistribution will result from each of the three options; 2) how much sav-ings would the implementation of a single payer generate? 3) what role restricting a national formularywould play in achieving those savings, and what would be the political consequences of narrowing theformulary?

-----ÖZET: Bugün, farklı farmasötik sınıflardan çeşitli antidepresif ajanlar klinik depresyon tedavisinde başarıyla kullanılmaktadır. Ne var ki Türkçe tıp literatüründe bu ilaçların güncel klinik kullanım ve sonuçlarına dair bol miktarda yayın bulunmasına karşın, bunların tarihi klinik gelişim sürecini kökenlere inerek, teferruatla bildiren çalışmalar çok azdır. Bu araştırmada, literatürdeki bu boşluğun dolduruluşuna katkıda bulunmak amaçlanmıştır. Araştırmada, antidepresif ajanların kısmen etki mekanizmalarına kısmen de kimyasal yapılarına göre düzenlenmiş olan klasik tasnifi izlenmiştir. PubMed ve ScienceDirect gibi veri tabanlarının ve çeşitli bilimsel dergilerin arşivlerinin retrospektif taranışı ile her bir farmasötik alt sınıfın başlangıcını teşkil eden prototipik antidepresanın keşfi; tarihi olay örgüsüne, ilgili tıbbi figürlere ve orijinal klinik araştırma sonuçlarına dair ilk elden bilimsel yayınlar üzerinden işlenmiştir. Antidepresif psikofarmakoterapi tarihindeki dönüm noktaları üzerinde durulmuş, başlıca ilaç sınıfları (monoamin oksidaz inhibitörleri, trisiklik ve tetrasiklik ajanlar ve monoaminerjik geri alım inhibitörleri) arasında bağlantılar kurulmuş ve yerine göre analojiler yapılmış ya da farklılıklar vurgulanmıştır. Varılan başlıca bir sonuç, antidepresif psikofarmakoterapi tarihinde tesadüfi gözlem eseri ("ilk kuşak/klasik") ajanlardan rasyonel dizaynla ilaç üretimine ("ikinci kuşak" antidepresanlara) geçişin interdisipliner iş birliğine borçlu olunan gelişmelerle mümkün olmuş olduğudur: Çeşitli bilimsel branşlardan kişilerce monoaminerjik konsantrasyon hipotezinin ortaya atılışı, monoamin oksidaz-A ve-B enzimlerinin keşfi, floresans mikroskopiye dayanan histokimyasal görüntüleme yönteminin geliştirilişi, antidepresif ajanların etki mekanizmalarının sistematik in vitro ve in vivo tetkikatla aydınlatılışı ve de antihistaminikler gibi mevcut kimyasalların ya da yeni maddelerin klinik çalışmalarla antidepresif potansiyelleri bakımından sınanışı gibi aşamalardan geçilerek, sonunda bugün majör depresif bozukluk tedavisinde başvurulan birincil ilaçlar olan monoaminerjik geri alım inhibitörlerine ulaşılmıştır.

-----ABSTRACT: Various antidepressive agents from different pharmaceutical classes are used successfully to treat depression today. Despite their well-documented clinical use and outcomes, however, the Turkish medical literature appears to lack studies dilating upon their historical development with reference to the origins and key events. Aimed at contributing to filling this gap, this study was built on the classical classification of antidepres-sive agents based partly on mechanism of action and chemical structure. PubMed, ScienceDirect, and various journal archives were reviewed retrospectively concerning the discovery of each agent that prototyped the pharmaceutical subclass investigated, with a focus on the timeline events, medical figures, and original clinical research results. The milestones in the history of antidepressive psychopharmacotherapy were highlighted, with connection and comparison between the main drug classes (monoamine oxidase inhibitors, tricyclics and tetracyclics, and monoaminergic reuptake inhibitors) through analogies and distinctions identified when appropriate. A main conclusion was that the consequential transition from the serendipitously obtained ("first-generation/classical") agents to rationally designed drug production (the "second-generation" antidepressants) was achieved by developments brought about by interdisciplinary collaboration. Production of the MRIs, pharmaceutics used primarily in treating major depressive disorder today, was processed through various stages by various scientific contributors propounding the monoaminergic concentration hypothesis, discovering the monoamine oxidase-A and-B enzymes, developing the histochemical visualization methodology by fluorescence microscopy, elucidating mechanisms of action of antidepressive agents through in vitro and in vivo investigation, and testing the existing chemicals such as antihistamines or new derivatives in clinical studies for their antidepressive potentials.

The ultimate target in the pharmaceutical and medical device industries is to ensure patient safety within the entire product life cycle, from R&D to distribution.

This presentation reviews the current focal points from MHRA GMP inspections.

Quality of medical products (both drugs and devices) becomes a social and ethical responsibility as products are developed, produced and distributed for preventing, treating and reducing discomforts of diseases.

The chromatographic separation was Analytical method Development and validation plays an important role in the discovery, Development and manufacture of pharmaceuticals. The methods used ensure the identity, purity, potency, and performance of drug products. There are many factors to consider when developing methods. The majority of the analytical development effort goes into validating a stability indicating HPLC Method. The goal of the HPLC Method is try and separate quantify the main active drugs, any reaction impurities, all available synthetic intermediates and degradants. A new, simple, precise, rapid and accurate RP-HPLC (Reverse Phase-High Performance Liquid Chromatography) method has been developed for the simultaneous estimation of Atenolol (AT) and Amlodipine Besylate (AB) in tablet formulations. The chromatographic separation was achieved on Water's 717 Plus Autosampler HPLC using octadecysilane bonded C 18 , 5 µm, 250 cm x 4.6 mm column maintained at ambient temperature with mobile phase, Buffer: Acetonitrile: Methanol, Mobile phase-mix volume of acetonitrile 45 volume or methanole 35 volume a 5 ml Tetrabutyl ammonium hydroxide in 1000 ml with makeup HPLC water of a mixture 20 volume, flow rate 1.5 ml/min, load volume 2 l and a run time of 1 min he detection was performed at 225 nm. Buffer was prepared with Tetrabutyl ammonium hydroxide and adjusted pH to 3.0 with Ortho-Phosphoric Acid.

This paper demonstrates how, by introducing a generic version of its previously-patented product, a branded firm can influence the equilibrium in the generic segment of the market for the product. This in turn can increase the firm's profits from selling the branded version. We then use structural estimates from previous literature to calculate the magnitude of the effects in the generic and branded segments.

As the pharmaceutical industry faces a more changing environment, talent management appears to be a key differentiating element. Key talent retention strategies must be assessed during the mergers and acquisitions negotiations and implemented during post-acquisition integration. The purpose of this paper is to show how this can be done.

The paper adopts a single-case approach to show how talent can be managed during the post-acquisition phase after a takeover. Focussing on the acquisition of Genentech by Roche in 2009, it demonstrates how the Swiss pharmaceutical giant overcame a difficult initial start to the acquisition by adopting a nuanced talent management strategy.

Propolis is a natural product with a plethora of biological effects, utilized by traditional medicine since antiquity. However, its application as a pharmaceutical is hindered by its variable composition and difficult standardization. CAPE has been shown to be a major component of propolis, with a large contribution to its pharmacological effects, among which the anti-inflammatory, antioxidant and antineoplastic have been attracting most attention. The current review article aims to present the cornerstone pharmacological studies of CAPE throughout the years, following its discovery, which confirmed its primary importance among propolis constituents and opened the path to its intensive research as a potential pharmaceutical. We present the diversity of drug delivery systems of CAPE, which have been developed to improve its efficacy in in vitro and in vivo disease models and discuss their primary promises and weaknesses. The increased interest in recent years over more practical approaches of CAPE research such as its pharmaceutical formulation comes to show that it has a potential to become commercialized as a pharmaceutical.

Eight pharmaceuticals, two polycyclic musk fragrances and nine endocrine disrupting chemicals were analysed in several waste water treatment plants (WWTPs). A membrane bioreactor in pilot scale was operated at different solid retention times (SRTs) and the results obtained are compared to conventional activated sludge plants (CASP) operated at different SRTs. The SRT is an important design parameter and its impact on achievable treatment efficiencies was evaluated. Different behaviours were observed for the different investigated compounds. Some compounds as the antiepileptic drug carbamazepine were not removed in any of the sampled treatment facilities and effluent concentrations in the range of influent concentrations were measured. Other compounds as bisphenol-A, the analgesic ibuprofen or the lipid regulator bezafibrate were nearly completely removed (removal rates 490%). The operation of WWTPs with SRTs suitable for nitrogen removal (SRT410 days at 10 1C) also increases the removal potential regarding selected micropollutants. No differences in treatment efficiencies were detected between the two treatment techniques. As in conventional WWTP also the removal potential of MBRs depends on the SRT. Ultrafiltration membranes do not allow any additional detention of the investigated substances due to size exclusion. However, MBRs achieve a high SRT within a compact reactor. Nonylphenolpolyehtoxylates were removed in higher extend in very lowloaded conventional WWTPs, due to variations of redox conditions, necessary for the degradation of those compounds.

Pharmaceutical residues are increasingly found in wastewater treatment plant effluents and river water in very low concentrations at nanograms per liter levels in many countries. In this study, samples were collected from seven wastewater treatment plants (WWTPs) and downstream surface waters in Bangkok, Thailand during July and October 2009 and January 2010. Solid phase extraction (SPE) followed by high-pressure liquid chromatography-mass spectrometry-mass spectrometry (HPLC/MS/MS) technique were used to detect eight pharmaceuticals including caffeine, acetaminophen, roxithromycin, ciprofloxacin, trimethoprim, lincomycin, enrofloxacin, and erythromycin. Levels of pharmaceutical residues in the influents on average were the highest for caffeine (9;052 ng=L), followed by acetaminophen (8;630 ng=L), and roxithromycin (235 ng=L). The same three pharmaceuticals showed the top three levels in the effluents (caffeine: 797 ng=L, acetaminophen: 92 ng=L, and roxithromycin: 50 ng=L). The concentration of caffeine was also the highest in downstream surface water samples (2;393:4 ng=L). Acetaminophen (839:3 ng=L) and roxithromycin (54:7 ng=L) were at the second and third highest levels. Caffeine and acetaminophen in WWTP effluents were at very low levels compared with the influent concentrations.

A novel is ligand namely 5,5'-(6-(4-methoxyphenoxy)-1,3,5-triazine-2,4-diyl)bis (azanediyl)diquinolin-8-ol (PBDQ-6)  has been prepared and characterized. This ligand was characterized by IR, 1H-NMR, and elemental analysis. Coordination polymers of this bis-ligand (NBDQ) were prepared with Cu(II), Ni(II), Co(II), Mn(II), and Zn(II) metal ions. All of these coordination polymers were characterized by elemental analyses, IR spectral and diffuse reflectance spectral studies. The thermal stability was evaluated by thermo gravimetric analyses (TGA). In addition, all of the coordination polymers have been characterized by their magnetic susceptibilities. All the novel synthesized compounds were screened for their antibacterial and antifungal activities.

Cellulite is associated with a complex array of adipocytes under the skin and vascular system. A herbal compress that was previously developed was proven to have an anti-cellulite effect in healthy volunteers within 2 weeks of treatment. However, its mechanism and ingredients responsible for reducing cellulite were not known. The purpose of this study was to investigate the activity of eight essential oils in, and two water extracts from, the ingredients of the herbal compress together with nine monoterpenoid constituents on the 3T3-L1 adipocytes. The vasodilatory effect on rat aortae was also studied. The adipocytes were induced by dexamethasone, 3-isobutyl-1-methylxanthine and insulin. At all concentrations tested, all essential oils, water extracts and their monoterpenoid constituents significantly inhibited lipid accumulation activity (p < 0.05) and decreased the amount of triglycerides when compared to untreated cells (p < 0.01). In addition, our results showed that the m...

Typhoid fever is a systemic infection caused by the bacterium Salmonella enterica subspecies enterica serotype typhi, a foremost public health predicament in developing countries. This study investigated hepatotoxicological changes associated with Salmonella typhi infection in Wistar rats and the potential of ethanol root extract of Millettia aboensis (EREMA) to reverse these changes. 51 animals were divided into six groups: group 1 was normal control with no treatment but were given feed and water ad libitum, group 2 was infected with Salmonella typhi without treatment (negative control), group 3, 4 and 5 were Salmonella typhi infected and treated with 100mg/kg, 200mg/kg and 400mg/kg of the extract respectively, and group 6 was infected and treated with 7.14mg/kg of ciprofloxacin. The animals were inoculated with a single infectious dose of Salmonella typhi bacterium (2.0 x 10 8 cfu/ml) and were subsequently treated with the graded doses of the extract and 7.14mg/kg of ciprofloxacin for a period of fifteen days. The rats were humanely sacrificed using diethyl ether anesthesia and blood samples taken for liver function investigation including [aspartate aminotransferase (AST) alanine aminotransferase (ALT), alkaline phosphatase (ALP), total bilirubin (TB), Albumin, conjugate bilirubin (CB) and total protein (TP)] and liver harvested and processed for histological assessment. Inoculation with S. typhi caused significant increase in all the liver function parameters and different degrees of damages to the liver cells. These were all reversed on treatment with ethanol root extract of Millettia aboensis. Thus the extract exhibited both anti-Salmonella typhi as well as hepato-curative potentials on the Kuffer cells.

Influenza A virus (IAV) infection is a common cause of acute exacerbations of chronic obstructive pulmonary disease (AECOPD). Since macrophage inflammatory protein 1 α, a chemokine that acts through CC-chemokine receptor (CCR)-5, appears elevated in COPD patients’ airways, we evaluated whether CCR5 antagonist Maraviroc could inhibit the exacerbated lung inflammatory response noted after IAV H1N1 infection in mice exposed to cigarette smoke (Cs). C57BL/6 mice, subjected or not to Cs inhalation for 11 days, were infected with H1N1 at day 7. Maraviroc (10 mg/kg) or dexamethasone (1 mg/kg) were given in a therapeutic schedule, followed by the analyses of lung function, survival rate, and inflammatory changes. As compared to mice subjected to Cs or H1N1 alone, the insult combination significantly worsened airway obstruction, neutrophil infiltration in the airways, and the survival rate. All changes were sensitive to Maraviroc but not dexamethasone. Maraviroc also reduced the accumulation...

The plants are possible sources of substances with antimicrobial activity, which have been extensively studied. The barks of Trichilia catigua are mainly used as stimulants, antioxidant, analgesic, vasodilator, antimicrobial, anti-inflammatory and anti-depressant. In the folk medicine their extracts are used as tonic for the treatment of fatigue, stress, impotence and memory deficits. The barks extract has a high content of phenolic compounds, including flavonoids and tannins. This study aimed to evaluate the in vitro antimicrobial activity against major microorganisms present on skin with acne of fifteen crude extracts obtained from T. catigua bark. We further aimed to use selected extracts to develop a cosmetic formulation for the treatment of acne vulgaris. The tests performed included disk diffusion in agar, determination of minimum inhibitory concentration (MIC), time-kill and survival curve analyses, and scanning electron microscopy analyses. The bacterial strains tested were Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Methicillin-Resistant Staphylococcus aureus (MRSA), Staphylococcus epidermidis, Cutibacterium acnes, and Bacillus cereus. Potent antimicrobial activity was exhibited by the TCE01 (water), TCE02 (methanol), and TCE12 (water: methanol: ethanol: 1:1:1, v/v) extracts. However, when included in cosmetic formulations, they showed different activities. All formulations showed non-Newtonian behavior and pseudoplastic flow, in addition to thixotropy. Formulations containing TCE02 and TCE12 at 1.0% (w/w) of extracts exhibited antimicrobial activity in topical formulations for acne treatment.

A bismuth-film electrode for use in cathodic electrochemical detection was employed in order to quantify sulfadiazine in pharmaceutical formulations. The bismuth film was deposited ex situ onto a glassy carbon substrate. Analysis of two sulfa drugs was carried out by differential-pulse voltammetry in 0.05 mol L −1 Britton-Robinson pH 4.5 solution. Sulfadiazine reduction was observed at −0.74 V vs. Ag/AgCl in one well-resolved irreversible reduction peak. The analytical curve with two slopes was obtained in the concentration range of 3.2-97.0 mol L −1 . The detection limit was 2.1 mol L −1 for concentrations of 3.2-20.0 mol L −1 (r = 0.9949) and 12.2 mol L −1 for concentrations between 20.0 and 97.0 mol L −1 (r = 0.9951). Recovery studies carried out with both sulfadiazine samples gave values from 93.6 to 109.3%. The accuracy of the results supplied by the bismuth-film electrode was compared to those obtained by the standard amperometric titration method. The relative error between them was lower than 2.0%.

Marine macro algae Sargassum's are commonly referred to as brown seaweeds. Commercially and continuously the pharmaceuticals industries are rapidly growing because always demand for new drug discovery is encouraged. Since brown seaweeds have ample source of bioactive compounds of primary or secondary metabolites. These potential bioactive compounds interest to improve the pharmaceuticals industry. This present study was investigated to explore the antibacterial and antifungal activity of the organic solvents extracts of the brown seaweed Sargassum. Phytochemical analysis of Brown seaweeds of Sargassum longifolium with six different organic solvents was analysed. The solvents like Dimethyl Sulfoxide, Benzene, Acetic acid, hexane, Di Ethyl ether and Chloroform has the extraction of phytochemical constituents. Among the six solvents Dimethyl Sulfoxide extract showed maximum number of phytochemical constituents and antibacterial and antifungal activity when compared to other five solvent extracts. The responsible functional groups in the solvent extract were identified by FTIR. These results statements be a necessary (or) recommended that the species of brown seaweeds (Sargassum longifolium) having a potential capacity as a source of antimicrobial compounds, which makes them interesting for screening for natural and highly bioactive secondary metabolites products it may leads to development of new pharmaceutical agents.

Background: Plant biotechnology revolutionized the branch of plant sciences contributing to improving crop production. Helicobacter pylori was predominantly seen among all the sectors of the human population, closely stuck to stomach ulcers and cancer. Even though traditional vaccines are effective in preventing H. pylori, edible and non-edible parts of special transgenic plants were also being generated to express its antigens which could elicit an immune response after consuming. The induce by contact with epithelium (iceA1) protein of H. pylori is associated with virulence and stated as predisposing factor to stomach cancer. Objectives: This study intends to study the expression levels of iceA1 gene in the brinjal plant. Materials and Methods: The present study, magnified the iceA1 gene from H. pylori strain 26695 and transformed it into callus of brinjal (from leaf explants) through Agrobacterium tumefacians (EHA105). pBI121 vector was used to construct the plant expression vector, and the transgenic plants generated were further validated through gene amplification and protein expression studies. Results: Out of the 46 plants obtained from this study, five of them were found to be positive for the iceA1 expression as seen on validation assays like gene amplification and protein expression studies. Conclusion: The study could beneficially produce a vaccine candidate against H. pylori from transgenic brinjal. In Addition, it could provide, valid scientific data which can further be used by researchers.