Synthesis and Antioxidant, Anticancer, and Antimicrobial Activities of Palmityl Ester Derivative of Carnosic Acid

Carnosic acid (CA) along with carnosol (CAR) is the strongest phenolic diterpene antioxidants (PDAs) present in rosemary plant. However, CA has low antioxidant activity in emulsion-type food system due to its polar nature. The identification and characterization of the anticancer and antimicrobial properties of natural products and their semisynthetic derivative such as that of CA and CAR have received significant interest over the years. The goals of this research were to synthesize lipophilic palmityl derivative (PE) of CA and study its antioxidant activity in bulk and emulsified corn oil. Anticancer properties against CCRF-CEM, K-562 and P388D1 leukemia cell lines and antimicrobial activity against Staphylococcus auerus (S. auerus), Bacillus cereus (B. cereus), Salmonella enterica, and Escherichia coli (E. coli) O157:H7 bacteria were also tested. A four steps synthetic route was designed. In the first step CAR was converted into a benzyloxy protected benzyl ester of CA (yield 78%). Reduction of the benzyl ester to a primary alcohol (yield 63%) followed by esterification with palmitoyl chloride gave the palmityl ester derivative (yield 97%). Finally, double bond reduction followed by deprotection of benzyloxy group gave PE (yield 99%). Overall yield for the route was 47%. The modification of CA affected functionality. PE had improved antioxidant activity in emulsified corn oil compared to bulk corn oil than the CA. However, CA was more effective in bulk oil. Compounds with hydroxyl groups were found to have cytotoxicity against three cell lines CCRF-CEM, P388D1 and K-562. Among compounds tested, CAR was found to be the most potent anticancer agent against all three cell lines. The study also indicated structure dependent activities for the compounds that had hydroxy group at the C-20 position. CA and CAR had antimicrobial activity against S. auerus, B. cereus, Salmonella, and E. coli O157:H7. S. auerus, B. cereus were more sensitive to CA and CAR than Salmonella, and E. coli O157:H7. Other compounds, without hydroxyl groups, did not have antimicrobial activity. Study also indicated that antimicrobial activity varied depending on functional group present at C-20 position. Compound PE did improve antioxidant activity in emulsion but did not improve antimicrobial activity

PENGGUNAAN MODEL PEMBELAJARAN KONTEKSTUAL UNTUK MENINGKATKAN SIKAP KERJA SAMA DAN HASIL BELAJAR SISWA TENTANG MACAM-MACAM SUMBER DAYA ALAM PADA PEMBELAJARAN IPS

Penelitian ini mengambil judul penggunaan model pembelajaran Kontekstual untuk meningkatkan sikap kerja sama dan hasil belajar siswa tentang macammacam sumber daya alam pada pembelajaran IPS (Penelitian Tindakan Kelas Pada Pembelajaran IPS di Kelas IV Sekolah Dasar Negeri Cipagalo 01 Kecamatan Bojongsoang Kabupaten Bandung). Penelitian ini bertujuan untuk meningkatkan sikap kerja sama dan hasil belajar siswa dalam proses pembelajaran. Penelitian ini merupakan penelitian tindakan kelas yang permasalahannya muncul dari dalam kelas tersebut. Berdasarkan hasil penelitian tindakan kelas yang telah dilakukan di dapat data bahwa dengan menggunakan model Kontekstual dapat meningkatkan sikap kerja sama dan hasil belajar siswa dalam proses pembelajaran di kelas IV SDN Cipagalo 01 Kabupaten Bandung. Ini dibuktikan dengan adanya peningkatan presentase sikap kerja sama dan hasil belajar siswa di setiap siklusnya. Hasil penelitiannya dapat dijelaskan bahwa di setiap siklusnya peningkatansikap kerja sama dan hasil belajarnya memperoleh hasil yang berbeda. Hasil belajar siswa di dalam kelas ternyata meningkat dari setiap siklus dengan di buktikannya melalui hasil tes, setiap siklus terlihat perubahan nilai siswa yang dapat mencapai KKM. Pada pra siklus nilai siswa masih di bawah rata-rata sehingga belum mencapai KKM hanya 10 orang dari jumlah siswa 38 dengan presentase 26,3%. Sedangkan hasil yang diharapkan yairu 75% dalam satu kelas mencapai nilai KKM. Presentasenya yaitu pada pra siklus yang mencapai KKM ada 10 orang dengan presentase 26,3%, siklus I yang mencapai nilai KKM 25 orang dengan presentase 65,8%, Berdasarkan hal tersebut berarti adanya peningkatan hasil pembelajaran dari pra siklus ke siklus I sebesar 39,5%. Dan pada siklus II yang mencapai KKM ada 35 orang dengan presentase 92%. Berdasarkan hal tersebut, berarti adanya peningkatan hasil belajar dari siklus I ke siklus II sebesar 26,2%. Untuk penilaian sikap kerja sama pada siklus I diperoleh nilai rata-rata sebesar 4,86 atau 60,52% dan siklus II dengan nilai ratarata 6,23 atau 89,47% dikatakan berhasil. Kata Kunci: kontekstual, sikap kerja sama, hasil belaja

Reinforcement learning based multi core scheduling (RLBMCS) for real time systems

Embedded systems with multi core processors are increasingly popular because of the diversity of applications that can be run on it. In this work, a reinforcement learning based scheduling method is proposed to handle the real time tasks in multi core systems with effective CPU usage and lower response time. The priority of the tasks is varied dynamically to ensure fairness with reinforcement learning based priority assignment and Multi Core MultiLevel Feedback queue (MCMLFQ) to manage the task execution in multi core system

A Unique Test Bench for Various System-on-a-Chip

This paper discusses a standard flow on how an automated test bench environment which is randomized with constraints can verify a SOC efficiently for its functionality and coverage. Today, in the time of multimillion gate ASICs, reusable intellectual property (IP), and system-on-a-chip (SoC) designs, verification consumes about 70 % of the design effort. Automation means a machine completes a task autonomously, quicker and with predictable results. Automation requires standard processes with well-defined inputs and outputs. By using this efficient methodology it is possible to provide a general purpose automation solution for verification, given today’s technology. Tools automating various portions of the verification process are being introduced. Here, we have Communication based SOC The content of the paper discusses about the methodology used to verify such a SOC-based environment. Cadence Efficient Verification Methodology libraries are explored for the solution of this problem. We can take this as a state of art approach in verifying SOC environments. The goal of this paper is to emphasize the unique testbench for different SOC using Efficient Verification Constructs implemented in system verilog for SOC verification

Comparative analysis of the toxicity of gold nanoparticles in zebrafish

The use of nanoparticles - particles that range in size from 1 to 100 nanometres - has become increasingly prevalent in recent years, bringing with it a variety of potential toxic effects. Zebrafish embryos were exposed during the 3-day post-fertilisation period to gold nanospheres (GSSs), gold nanorods (GNRs), gold nanorods coated with polystyrene-sulfate (PSS-GNRs), and gold nanorods coated with both polystyrene-sulfate and polyallamine hydrochloride (PAH/PSS-GNRs). All nanorods were stabilised with cetyltrimethylammonium bromide (CTAB). GNSs were the least toxic of the nanoparticles studied, with exposure resulting in no significant changes in mortality, hatching or heart rate. Exposure to GNRs and PSS-GNRs resulted in significant increases in mortality and significant decreases in hatching and heart rate. Treatment with GNRs caused significant changes in the expression of a variety of oxidative stress genes. The toxic effects of GNRs were ameliorated by coating them with polystyrene-sulfate and, to a more marked extent, with a double coating of polystyrene-sulfate and polyallamine hydrochloride

Antidiabetic activity of compounds isolated from the roots of Premna latifolia Roxb

Purpose: To evaluate the hypoglycaemic activity of the ethanol extract, chloroform  fraction, and three compounds isolated from Premna latifolia.Methods: The ethanol extract, chloroform fraction, and compounds 1 – 3 (isolated from the chloroform fraction) of P. latifolia were characterised by nuclear magnetic resonance (1H NMR, 13C NMR and 2D NMR). In vitro activity was assessed by α-amylase and α-glucosidase inhibitory activity assays. In vivo antidiabetic activity was evaluated in a streptozotocin-nicotinamide-induced rat model of diabetes. Fasting blood glucose (FBG), glycosylated haemoglobin (HbA1C), serum creatinine, blood urea nitrogen (BUN), liver enzymes, and antioxidant enzymes were  determined. Liver and pancreas histopathology was assessed.Results: Compounds 2 and 3 exhibited significant hypoglycaemic activity by reducing elevated FBG and HbA1C (p ≤ 0.001) and also exerted positive effects on blood and liver enzyme profiles, which were largely altered in diabetic control group. These compounds also showed significant antioxidant activity, increasing catalase, superoxide dismutase, and glutathione reductase, while lowering malondialdehyde (p ≤ 0.001). The histopathology results for the rats that received these compounds suggested regeneration of pancreatic β-cells.Conclusion: Compounds 2 and 3 isolated from the dried roots of P. latifolia possess significant hypoglycaemic activity, reno- and hepatoprotective effects, and antioxidant activity. They show promise as potential treatments for patients with diabetes.Keywords: Antioxidant, Hypoglycaemic, Premna latifolia, Stigmanstan-3β-olyl n-octadec-9ʹ, 12ʹ- dienoate, n-Tetracosanol, n-Tridecanyl n-Tetracosanoat

Anti-proliferative activity of silver nanoparticles

This is an Open Access article distributed under the terms of the Creative Commons Attribution Licens

PHARMACOGNOSTIC AND PHYSICOCHEMICAL STUDIES OF THE LEAVES AND STEM OF ACTINODAPHNE MADRASPATANA BEDD

Objective: To study the detailed pharmacognostic profile of the leaves and stem of Actinodaphne madraspatana Bedd (Lauraceae), an important medicinal plant in the Indian system of medicine. Methods: Leaf and stem samples of Actinodaphne madraspatana Bedd were studied by macroscopical, microscopical, physicochemical, phytochemical, fluorescence analysis of the powder of the plant and other methods for standardization recommended by WHO. Results: Macroscopically, the leaves are 6 in a whorl, 10-30 cm long, coriaceous, lanceolate, oblanceolate or elliptic. Microscopically, the leaf showed the presence of sunken stomata, prominent midrib, dorsiventral lamina, three stranded vascular system, small xylem and phloem elements with a vertical extension of bundle sheath fibres, tannin, non glandular trichomes and small epidermal peeling of the stem. Physicochemical parameters such as extractive values, ash content and fluorescent behavior of leaf powder were also determined. Preliminary phytochemical screening showed the presence of triterpenoids, flavonoids, glycosides and steroids.   Conclusions: This is the first report on the pharmacognostic and physicochemical studies of Actinodaphne madraspatana Bedd and is helpful in the characterization of the crude drug. Key words: Actinodaphne madraspatana Bedd, Pharmacognostic, Physicochemical, Fluorescence behaviorÂ&nbsp

Efficacy and safety of prucalopride in the treatment of chronic constipation

Background: Chronic constipation is a common condition that significantly impacts health care utilization, productivity, and quality of life. Laxatives are commonly used, although often insufficient in restoring normal bowel function or providing adequate relief. There remains a significant need for the development of novel agents to optimize treatment of this condition. Prucalopride, a selective, high-affinity 5-hydroxytryptamine 4 receptor agonist, stimulates gastrointestinal and colonic motility and alleviates common symptoms of chronic constipation. Here authors are evaluating efficacy and safety study of this drug in chronic constipation patient.Methods: This is a prospective observational study where chronic constipation patient treated with prucalopride 2 mg daily once were enrolled during 6 month period. Data at one week and four weeks were observed along with adverse effects. Efficacy assessed by the number of Spontaneous Complete Bowel Movements (SCBMs) per week recorded by patient diaries. Patients were defined as responders when they had a mean of three or more SCBMs per week over the whole treatment period. The primary efficacy end point was proportion of responders after 1 week and after 4 weeks of treatment.Results: A total of 43 patients diagnosed with chronic constipation and treated with prucalopride were included in study. The proportions of patients in the present study with at least three SCBMs per week (responders) were 44.2% (19 out of 43 patients) at 1 week and 46.5% (20 out of 43 patients) at 4 weeks. Treatment was well tolerated with minimal side effects. Common adverse effects reported in our study were gastrointestinal disorders like diarrhea, nausea and abdominal pain and nervous system disorders like headache and dizziness.Conclusions: Prucalopride is effective, has a good safety profile, and is well tolerated in chronic constipation treatment

Enhanced Genotoxicity of Silver Nanoparticles in DNA Repair Deficient Mammalian Cells

Silver nanoparticles (Ag-np) have been used in medicine and commercially due to their anti-microbial properties. Therapeutic potentials of these nanoparticles are being explored extensively despite the lack of information on their mechanism of action at molecular and cellular level. Here, we have investigated the DNA damage response and repair following Ag-np treatment in mammalian cells. Studies have shown that Ag-np exerts genotoxicity through double-strand breaks (DSBs). DNA-PKcs, the catalytic subunit of DNA dependent protein kinase, is an important caretaker of the genome which is known to be the main player mediating Non-homologous End-Joining (NHEJ) repair pathway. We hypothesize that DNA-PKcs is responsible for the repair of Ag-np induced DNA damage. In vitro studies have been carried out to investigate both cytotoxicity and genotoxicity induced by Ag-np in normal human cells, DNA-PKcs proficient, and deficient mammalian cells. Chemical inhibition of DNA-PKcs activity with NU7026, an ATP-competitive inhibitor of DNA-PKcs, has been performed to further validate the role of DNA-PKcs in this model. Our results suggest that Ag-np induced more prominent dose-dependent decrease in cell viability in DNA-PKcs deficient or inhibited cells. The deficiency or inhibition of DNA-PKcs renders the cells with higher susceptibility to DNA damage and genome instability which in turn contributed to greater cell cycle arrest/cell death. These findings support the fact that DNA-PKcs is involved in the repair of Ag-np induced genotoxicity and NHEJ repair pathway and DNA-PKcs particularly is activated to safeguard the genome upon Ag-np exposure