Search results for: anticancer activity

Authors: Amanda Sheard, Garry Lee, Katherine Stockham

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Introduction: Health benefits associated with wine consumption have been well documented; these include anticancer, anti-inflammatory, and cardiovascular protection. The majority of these health benefits have been linked to polyphenols found within wine and grapes. Once consumed polyphenols exhibit free radical quenching capabilities. Environmental factors such as rainfall, temperature, CO2 levels and sunlight exposure have been shown to affect the polyphenol content of grapes. The objective of this work was to evaluate the effect of growing conditions on the antioxidant capacity of grapes obtained from a single plot vineyard in Perth. This was achieved through the analysis of samples using; oxygen radical antioxidant capacity (ORAC), cellular antioxidant activity (CAA) in human red blood cells, ICP-MS and ICP-OES, total polyphenols (PP’s), and total flavonoid’s (FLa). The data obtained was compared to observed climate data. The 14 Selected Vitis Vinefera L. cultivars included Cabernet franc, Cabernet Sauvignon, Carnelian, Chardonnay, Grenache, Melbec, Merlot, Orange muscat, Rousanne, Sauvignon Blanc, Shiraz, Tempernillo, Verdelho, and Voignier. Results: Notable variation’s between cultivars included results ranging from 125 mg/100 g-350 mg/100 g for PP’s, 93 mg/100 g–300 mg/100 g for FLa, 13 mM T.E/kg–33 mM T.E/kg for ORAC and 0.3 mM Q.E/kg–27 mM Q.E/kg CAA were found between red and white grape cultivars. No correlation was found between CAA and the ORAC obtained in this study; except that white cultivars were consistently lower than red. ICP analysis showed that seeds contained the highest concentration of copper followed by skins and flesh of the grape. A positive correlation between copper and ORAC was found. The ORAC, PP’s, and FLa in red grapes were consistently higher than white grape cultivars; these findings were supported by literature values. Significance: The cellular antioxidant activities of white and red wine cultivars were used to compare the bioactivity of these grapes against the chemical ORAC measurement. The common method of antioxidant activity measurement is the chemical value from ORAC analysis; however this may not reflect the activity within the human body. Hence, the measurements were also carried out using the cellular antioxidant activity to perform a comparison. Additionally, the study explored the influence of weather systems such as El Niño and La Niña on the polyphenol content of Australian wine cultivars grown in Perth.

Keywords: oxygen radical antioxidant activity, cellular antioxidant activity, total polyphenols, total flavonoids, wine grapes, climate

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Authors: Srie Rezeki Nur Endah, Richa Mardianingrum

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Cancer is one of the most feared diseases and is considered the leading cause of death worldwide. Generally, cancer drugs are synthetic drugs with relatively more expensive prices and have harmful side effects, so many people turn to traditional medicine, for example by utilizing herbal medicine. Erythrina poeppigiana is one of the plants that can be used as a medicinal plant containing 10,11-dihidroerisodin compounds that are useful anticancer etnofarmakologi. The purpose of this study was to identify the target of 10,11 dihydroerisodin receptor compound as in silico anticancer candidate. The pure isolate was tested physicochemically by MS (Mass Spectrometry), UV-Vis (Ultraviolet – Visible), IR (Infra Red), 13C-NMR (Carbon-13 Nuclear Magnetic Resonance), 1H-NMR (Hydrogen-1 Nuclear Magnetic Resonance), to obtain the structure of 10,11-dihydroerisodin alkaloid compound then identified to target receptors in silico. From the results of the study, it was found that 10,11-dihydroerisodin compound can work on the Serine / threonine-protein kinase Chk1 receptor that serves as an anti-cancer candidate.

Keywords: anti-cancer, Erythrina poeppigiana, target receptor, 10, 11- dihidroerisodin

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Authors: Kamel Zemour, Kada Mohamed Amine Chouhim, Mohamed Mairif, Tadj Eddine Adda Ardjan

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Many recent studies show the positive effect of phenolic compounds in olive oil on health. They are known for their biological properties, where they have shown potential activity as an antioxidant, anti-inflammatory, and antimicrobial agents. However, this characteristic is rarely studied in olive oil from different regions of Algeria. Different samples collected from the western region of Algeria were evaluated for their polyphenol content, antioxidant activity, and antimicrobial effect. The obtained results demonstrated that this oil is rich in polyphenols and revealed high antimicrobial activity against Staphylococcus aureus and Escherichia coli. Finally, this study has highlighted the nutritional and pharmaceutical importance of olive oil grown in Algeria.

Keywords: olive oil, polyphenols, antioxidant activity, antimicrobial activity

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Authors: Saman Khan, Imrana Naseem

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Copper is an essential trace element required for pro-angiogenic co-factors including vascular endothelial growth factor (VEGF). Elevated levels of copper are found in various types of cancer including prostrate, colon, breast, lung and liver for angiogensis and metastasis. Therefore, targeting copper via copper-specific chelators in cancer cells can be developed as effective anticancer treatment strategy. In continuation of our pursuit to design and synthesize copper chelators, herein we opted for a reaction to incorporate di-(2-picolyl) amine in 3-(bromoacetyl) coumarin (parent backbone) for the synthesis of complex 1. We evaluated lipid peroxidation, protein carbonylation, ROS generation, DNA damage and consequent apoptosis by complex 1 in exogenously added Cu(II) in human peripheral lymphocytes (simulate malignancy condition). Results showed that Cu(II)-complex 1 interaction leads to cell proliferation inhibition, apoptosis, ROS generation and DNA damage in human lymphocytes, and these effects were abrogated by cuprous chelator neocuproine and ROS scavengers (thiourea, catalase, SOD). This indicates that complex 1 cytotoxicity is due to redox cycling of copper to generate ROS which leads to pro-oxidant cell death in cancer cells. To further confirm our hypothesis, using the rat model of diethylnitrosamine (DEN) induced hepatocellular carcinoma; we showed that complex 1 mediates DNA breakage and cell death in isolated carcinoma cells. Membrane permeant copper chelator, neocuproine, and ROS scavengers inhibited the complex 1-mediated cellular DNA degradation and apoptosis. In summary, complex 1 anticancer activity is due to its copper chelation capability. These results will provide copper chelation as an effective targeted cancer treatment strategy for selective cytotoxic action against malignant cells without affecting normal cells.

Keywords: cancer treatment, copper chelation, ROS generation, DNA damage, redox cycling, apoptosis

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Authors: Nilüfer Yıldız Varan

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The antimicrobial activities of chitosan against various bacteria and fungi are well known, and the antimicrobial activity of chitosan depends on pH. This study investigates the antimicrobial activity at different pH levels. Nylon 6,6 fabrics were treated with different chitosan solutions. Additionally, samples were treated also in basic conditions to see the antimicrobial activities. AATCC Test Method 100 was followed to evaluate the antimicrobial activity using Staphylococcus aureus ATCC 6538 test inoculum. The pH of the chitosan solutions was controlled below 6.5 since chitosan shows its antimicrobial activity only in acidic conditions because of its poor solubility above 6.5. In basic conditions, the samples did not show any antimicrobial activity. It appears from SEM images that the bonded chitosan in the structures exists. In acidic media (ph < 6.5), all samples showed antimicrobial activity. No correlation was found between pH levels and antimicrobial activity in acidic media.

Keywords: chitosan, nylon 6, 6, crosslinking, pH stability, antimicrobial

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Authors: Wirot Likittrakulwong, Pisit Poolprasert, Tossaporn Incharoen

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Germinated paddy rice (GPR) has the potential to be used as a feed ingredient. However, their properties have not been fully investigated. This paper examined the nutrient digestibility and the relationship to immune activity in Roman hens fed with GPR. It was found that true and apparent metabolizable energy (ME) values of GPR were 3.20 and 3.28 kcal/g air dry, respectively. GPR exhibited high content of phytonutrients, especially GABA. GPR showed similar protein profiles in comparison to non-germinated paddy rice. For immune activity, the feed with GPR enhanced the immune activity of Roman hens under high stocking density stress as evidenced by the activity of superoxide dismutase (SOD) and lysozyme activity. In this study, GPR is proved to be a good source of functional ingredient for chicken feed.

Keywords: germinated paddy rice, nutrient digestibility, immune activity, functional property

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Authors: M. Koksal, T. Ozyazici, E. Gurdal, M. Yarım, E. Demirpolat, M. B. Y. Aycan

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The discovery of new drugs in cancer chemotherapy is still a major topic because of severe side effects, selectivity problems and resistance development potential of existing drugs. In recent years, combined anticancer therapies or multi-acting drugs are clinically preferred over traditional cytotoxic treatment, with the aim of avoiding resistance and toxic side effects. Arrangement of multi-acting targets can be carried out either by combination of several drugs with different mechanisms or by usage of a single chemical compound capable of regulating several targets of a disease with multiple factors. In literature, several pyrimidine and piperazine derivatives have been involved in the structure of many compounds which have been used as chemotherapeutic agents along with wide clinical applications. The aim of this study is to combine pyrimidine and piperazine core structures to research and develop novel piperazinylpyrimidine derivatives with selective cytotoxicity over cancer cells. In this study, a group of novel 6-fluorophenyl-3-[2-(substitutedpiperazinyl)ethyl] hexahydropyrimidine-2,4-dione derivatives designed to observe the desired anticancer activity due to pyrimidine and piperazine based scaffolds. Target compounds were obtained by the reaction of appropriate piperazine derivatives and 6-(2/4-fluorophenyl)-3-(2-chloroethyl)hexahydropyrimidine-2,4-dione. The synthetic pathway of 6-(2/4-fluorophenyl)-3-(2-chloroethyl)hexahydropyrimidine-2,4-dione was started with Rodionov reaction using aldehyde, malonic acid and ammonium acetate in ethanol. Isolated β-fluorophenyl-β-amino acids were treated with 2-chloroethylisocyanate in the presence of an aqueous sodium hydroxide solution at room temperature to yield the sodium salts of the corresponding ureido acids. By addition of a mineral acid, ureido acids were precipitated. Later, these ureido acids were refluxed in thionyl chloride to give the 6-(2/4-fluorophenyl)-3-(2-chloroethyl)hexahydropyrimidine-2,4-di-one which were furthermore treated with secondary amines. Structures of purified compounds were characterized with IR, 1H-NMR, 13C-NMR, mass spectroscopies and elemental analysis. All of the compounds gave satisfactory analytical and spectroscopic data, which were in full accordance with their depicted structures. In IR spectra of the compounds, N-H group was seen at 3230-3213 cm⁻¹. C-H was seen at 3100-2820 cm⁻¹ and C=O vibrational peaks were observed approximately at 1725 and 1665 cm⁻¹ in accordance with literature. In the NMR spectra of target compounds, the methylene protons of piperazine give two separate multiplet peaks around 3.5 and 4.5 ppm representing the successful N-alkylation of the structure. The cytotoxic activity of the synthesized compounds was investigated on human bronchial epithelial (BEAS 2B), lung (A549), colon adenocarcinoma (COLO205) and breast (MCF7) cell lines, by means of sulphorhodamine B (SRB) assays in triplicate. IC₅₀ values of the screened derivatives were found in range of 11.8-78 µM. This project was supported by The Scientific and Technological Research Council of Turkey (TUBITAK, Project no: 215S157).

Keywords: cytotoxicity, hexahydropyrimidine, piperazine, sulphorhodamine B assay

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Authors: Salma Mirza, Syeda Asma Naqvi, Khalid Mohammed Khan, M. Iqbal Choudhary

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In this study twenty-five (25) newly synthesized compounds substituted aryl thiazoles (SAT) 1-25 were synthesized, and in vitro cytotoxicity of these compounds was evaluated against four cancer cell lines namely, MCF-7 (ER+ve breast), MDA-MB-231 (ER-ve breast), HCT116 (colorectal), and, HeLa (cervical) and compared with the standard anticancer drug doxorubicin with IC50 value of 1.56 ± 0.05 μM. Among them, compounds 1, 4-8 and 19 were found to be active against all four cell lines. Compound 20 was found to be selectively active against MCF7 cells with IC50 value of 40.21 ± 4.15 µM, whereas compound 19 was active against only MCF7 and HeLa cells with IC50 values of 46.72 ± 1.8 and 19.86 ± 0.11 μM, respectively. These results suggest that aryl thiazoles 1 and 4 deserve to be investigated further in vivo as anti-cancer agents.

Keywords: anticancer agents, breast cancer cell lines (MCF7, MDA-MB-231), colorectal cancer cell line (HCT-116), cervical cancer cell line (HeLa), Thiazole derivatives

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Authors: Rock-Hyun Choi, Won-Seok Kang, Chang-Sik Son

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Physical activity is important for healthy living. Recently wearable devices which motivate physical activity are quickly developing, and become cheaper and more comfortable. In particular, fitness trackers provide a variety of information and need to provide well-analyzed, and user-friendly results. In this study, frequency analysis was performed to classify various data sets of Fitbit into simple activity status. The data from Fitbit cloud server consists of 263 subjects who were healthy factory and office workers in Korea from March 7th to April 30th, 2016. In the results, we found assumptions of activity state classification seem to be sufficient and reasonable.

Keywords: activity status, fitness tracker, heart rate, steps

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Authors: Hassina Harkat, Samiha Taybe, Salima Loucif, Valérie Beneteau, Patrick Pale

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Indole and its derivatives have attracted great interest because of their importance in the synthetic organic and medicinal chemistry. They are widely used as anti hypertension, anti tubercular, anticancer activity, antiviral, Alzheimer's disease, antioxidant properties, and free radical induced lipid peroxidation. Many drugs and natural products contain indole moiety, such as the vinca alkaloids, fungal metabolites and marine natural products. Generally applicable synthetic methods for indole moiety involve ring closure to form the pyrrole. Indole derivatives can also be accessed by further functionalization of the indole nucleus. Therefore we report a mild and efficient protocol for the synthesis of analogues of indole catalyzed via zeolithe USY doped with CuI under solvent-free conditions.

Keywords: indole, zeolithe, USY-CuI, heterogeneous catalysis

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Authors: Chien-Liang Chao, Yun-Sheng Lin

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Secondary metabolites are applied in the human life of the Chinese herbal medicine. Many drugs are originally extracted from natural products with combination of pharmaceutical and chemical studies. Crude extract of the leaves from Zamia furfureace L. has been shown to exhibit anticancer activities. The first chemical investigation of this plant was carried out by our group. In this study, four known compounds were isolated from Zamia furfureace L. with three lignins (Sesamin (1), Wodeshiol (2) and Paulownin (3)), and one dipeptide (Aurantiamide acetate (4)). The structures of these compounds were analyzed through the 1D-NMR(1H-NMR,13C-NMR)、2D-NMR(COSY、HMQC、HMBC、NOESY) spectroscopic analysis, and by comparison of variety of physical data (IR, mass spectrometry, ultraviolet, optical rotation). Among them, Aurantiamide acetate (4) exhibited weak cytotoxic activity against human gastric cancer cells.

Keywords: Zamia furfureace L., AGS, sesamin, Aurantiamide acetate, secondary metabolites

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Authors: Sobhy A. El-Sohaimy, Mohamed G. Shehata, Ashwani Mathur, Amira G. Darwish, Nourhan M. Abd El-Aziz, Pammi Gauba, Pooja Upadhyay

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Sea buckthorn is a temperate bush plant native to Asian and European countries, explored across the world in traditional medicine to treat various diseases due to the presence of an exceptionally high content of phenolics, flavonoids and antioxidants. In addition to the evaluation of nutrients and active compounds, the focus of the present work was to assess the optimal levels for L. plantarum RM1 growth by applying response surface methodology (RSM), and to determine the impact of juice fermentation on antioxidant, anti-hypertension and anticancer activity, as well as on organoleptic properties. Sea buckthorn berries were shown to contain good fiber content (6.55%, 25 DV%), high quality of protein (3.12%, 6.24 DV%) containing: histidine, valine, threonine, leucine and lysine (with AAS 24.32, 23.66, 23.09, 23.05 and 21.71%, respectively), and 4.45% sugar that pro- vides only 79 calories. Potassium was shown to be the abundant mineral content (793.43%, 22.66 DV), followed by copper and phosphorus (21.81 and 11.07 DV%, respectively). Sea buckthorn juice exhibited a rich phenolic, flavonoid and carotenoid content (283.58, 118.42 and 6.5 mg/g, respec- tively), in addition to a high content of vitamin C (322.33 mg/g). The HPLC profile indicated that benzoic acid is the dominant phenolic compound in sea buckthorn berries (3825.90 mg/kg). Antiox- idant potentials (DPPH and ABTS) of sea buckthorn showed higher inhibition than ascorbic acid. Antimicrobial potentials were most pronounced against Escherichia coli BA12296 (17.46 mm). The probiotic growth was 8.5 log cfu/mL, with juice concentration, inoculum size and temperature as the main contributors to probiotic growth with a 95% confidence level. Fermentation of sea buck- thorn juice with L. plantarum RM1 enhanced the functional phenolic and flavonoid content, as well as antioxidant and antimicrobial activities. The fermentation with L. plantarum RM1 enhanced the anti-hypertension and anticancer properties of the sea buckthorn juice and gained consumers’ sensorial overall acceptance.

Keywords: sea buckthorn juice, L. plantarum RM1, fermentation, antioxidant, antimicrobial, angiotensin converting enzyme inhibition

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Authors: L. Mallesha, C. S. Karthik, P. Mallu

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A series of new [1-(substituted-benzoyl)-piperidin-4-yl]-(2,4-difluoro-phenyl)-methanone oxime derivatives, 3(a-f) were synthesized and characterized by different spectral studies. All compounds were evaluated for their in vitro antibacterial activity against bacterial strains. These compounds were screened for their antioxidant activity by DPPH• and Fe2+ chelating assay. Antiproliferative effects were evaluated using the MTT assay method against two human cancer cell lines and one astrocytoma brain tumor cell line. Compound 3b exhibited moderate antibacterial activity when compared with other compounds. All the compounds showed antioxidant activity, where compound 3f was the best radical scavenger and Fe2+ ion scavenger. Compounds, 3b, and 3d showed good activity on all cell lines, whereas the other compounds in the series exhibited moderate activity.

Keywords: Piperidine, antibacterial, antioxidant, antiproliferative

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Authors: Zahra Dehghani, Hoda Dehghani, Elham Zarenezhad

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1,2,3-Triazole derivatives are important compounds in medicinal chemistry owing to their wide applications in drug discovery. They can readily associate with biologically targets through the hydrogen bonding and dipole interactions. The 1,2,3-triazole core is a key structural motif in many bioactive compounds, exhibiting a broad spectrum of biological activities, such as antiviral, anticancer, anti-HIV, antibiotic, antibacterial, and antimicrobial. Additionally, they have found significant industrial applications as dyes, agrochemicals, corrosion inhibitors, photo stabilizers, and photographic materials. we disclose the synthesis and characterization of 1-azido-3-(aryl-2-yloxy)propan-2-ol drivatives. The chemistry works well with various ß-azido alcohols involving aryloxy, alkoxy and alkyl residues, and also tolerates a wide spectrum of electron-donating and electron-withdrawing functional groups in both alkyne and azide molecules. Most of ß-azidoalcohols used in these experiments were pre-synthesized by the regioselective ring opening reaction of corresponded epoxides with sodium azide, whereas the majority of terminal alkynes were prepared via SN2-type reaction of propargyl bromide and corresponded nucleophiles. To evaluate the bioactivity of title compounds, the in vitro antifungal activity of all compound was investigated against several pathogenic fungi including Candida albicans, Candida krusei, Aspergillus niger, and Trichophyton rubrum , clotrimazole and fluconazole was used as standard antifungal drugs, also To understand the antibacterial activity of synthesized compounds, they were in vitro screened against E. coli and S. aureus as Gram-negative and Gram-positive bacteria, respectively. The in vitro tests have shown the promising antifungal but marginal antibacterial activity against tested fungi and bacteria.

Keywords: biological activities, antibacterial, antifungal, 1, 2, 3-Triazole

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Authors: Dawang D. N., Dasat G. S., Nden D.

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Endophyte means “in the plant” are referred to all microorganisms that live in the internal tissues of stems, petioles, roots and leaves of plants causing no apparent symptoms of disease. Secondary metabolites from fungal endophytes have an enormous potential applications as antioxidant, antimicrobial, anticancer and antidiabeties. Thus, this study aimed to determine the antimicrobial activity of these metabolites against some clinical isolates. The fungi were subjected to fermentation medium and the metabolites were extracted using ethyl acetate. The fungal extracts showed both antibacterial and antifungal activities with maximum zone of inhibition diameter of 10.5mm against Aspergillus fumigatus. Staphylococcus aureus was inhibited by all the five crude extracts with inhibition zone diameter of 4mm. Endophytic fungal crude extract2 (EDF2) exhibited antimicrobial effect against all the test organisms used, EDF4 was active against all test organisms except on Penicillium chrysogenum and Klebsiella pneumoniae. Antibacterial standard of ciprofloxacin which is 15mm is comparable to the effect of endophytic extract of EDF1 and EDF2. Klebsiella pneumoniae was resistant to EDF4 and EDF5. EDF3 showed a wide range of antimicrobial activity against all the test organisms used. The highest inhibition zone diameter of 10.50mm recorded against Aspergillus fumigatus is comparable to antifungal standard of fluconazole (15.5mm). The result of this study suggests that endophytic fungi associated with the roots of Irish potato could be a promising source of novel bioactive compounds of pharmaceutical and industrial importance.

Keywords: endophyte, fungal extract, antimicrobial, potato

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Authors: Turk Ayman, Ahn Jong Hoon, Khalife K. Hala, Gali-Muhtasib Hala, Lee Mi Kyeong

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Laurus nobilis is an aromatic plant widely distributed in the Mediterranean region. The leaves of this plant are frequently used as a spice and as a traditional medicine for several diseases. In our present study, the methanolic extract of L. nobilis leaves showed antioxidant activity. Chromatographic separations of the EtOAc fraction which had the highest antioxidant activity led to the isolation of 12 compounds. Among them, there was a new phenylpropanoid derivative, which was identified by 1D and 2D NMR experiments, as well as high resolution mass spectrometry. In addition, two major compounds, catechin and epicatechin, which showed strong antioxidant activity may be responsible for the antioxidant activity of L. nobilis leaves. Since different plant parts may contain different types of constituents which contribute to the biological activities, we investigated the antioxidant activity of different parts of L. nobilis such as leaves, stems and fruits. Stems of L. nobilis showed the most potent antioxidant activity, followed by leaves. Further quantitation of total phenol and flavonoids contents revealed a positive correlation between the content of these compounds and antioxidant activity. Taken together, phenolic compounds including flavonoids are responsible for antioxidant activity of L. nobilis. In addition, stem parts of L. nobilis are suggested as good sources for antioxidant activity. Conclusively, L. nobilis might be effective in several free radical mediated diseases.

Keywords: antioxidant activity, different parts, Laurus nobilis, phenolic compound

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Authors: Paiwan Buachan, Maneekarn Namsa-Aid, Suchada Jongrungruangchok, Foengchat Jarintanan, Wanlaya Uthaisang-Tanechpongtamb

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Lung cancer or pulmonary carcinoma is the uncontrolled growth of abnormal cells in one or both of the lungs. These abnormal cells can spread to other organs of the body through lymphatic system or bloodstream which is called metastatic stage that leading cause of cancer death. Terrein (C₈H₁₀O₃; MW= 154.06 kDa) is a secondary bioactive fungal metabolite, which was isolated from the Aspergillus terreus. In this study, we investigated the effects of terrein on the inhibition of human lung cancer cell proliferation and metastasis. The A549 human non-small cell lung cancer cell line was used as a model. Terrein significantly inhibited lung cancer cell proliferation measuring by a colorimetric MTT assay (IC₅₀ 0.32 mM) and significantly inhibited metastatic processes including migration, invasion, and adhesion that determined by wound healing assay, transwell assay, and adhesion assay, respectively. These findings indicate that terrein could be a potential therapeutic agent for lung cancer.

Keywords: terrein, lung cancer, anticancer, antimetastatic

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Authors: Muhammad Wahb

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Physical activity is increasingly recognized as a significant factor in maintaining optimal health and preventing chronic diseases. This research scrutinizes the long-term health benefits of sustained physical activity, employing a systematic review of epidemiological studies and randomized control trials conducted over the past decade. The study illuminates the protective effects of regular physical activity against cardiovascular disease, obesity, diabetes, and mental health disorders, with a special focus on the mechanisms involved. Furthermore, the paper provides insights into how public health initiatives can effectively promote physical activity among diverse populations, contributing to improved community health outcomes.

Keywords: physical activity, long-term health benefits, chronic disease prevention, public health

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Authors: Laila H. Abdel-Rahman, Mohamed Shaker S. Adam, Ahmed M. Abu-Dief, Hanan El-Sayed Ahmed

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In this investigation, Cu(II), Pd(II) and Ag(I) complexes with the tetra-dentate DSPH Schiff base ligand were synthesized. The DSPH Schiff base and its complexes were characterized by using different physicochemical and spectral analysis. The results revealed that the metal ions coordinated with DSPH ligand through azomethine nitrogen and phenolic oxygen. Cu(II), Pd(II) and Ag(I) complexes are present in a 1:1 molar ratio. Pd(II) and Ag(I) complexes have square planar geometries while, Cu(II) has a distorted octahedral (Oh) geometry. All investigated complexes are nonelectrolytes. The investigated compounds were tested against different strains of bacteria and fungi. Both prepared compounds showed good results of inhibition against the selected pathogenic microorganism. Moreover, the interaction of investigated complexes with CT-DNA was studied via various techniques and the binding modes are mainly intercalative and grooving modes. Operating Environment MOE package was used to do docking studies for the investigated complexes to explore the potential binding mode and energy. Furthermore, the growth inhibitory effect of the investigated compounds was examined on some cancer cells lines.

Keywords: tetradentate, antimicrobial, CT-DNA interaction, docking, anticancer

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Authors: Katharigatta N. Venugopala, Fernando Albericio, Bander E. Al-Dhubiab, T. Govender

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Recent years have witnessed a renaissance in the field of peptides that are obtained from various natural sources such as many bacteria, fungi, plants, seaweeds, vertebrates, invertebrates and have been reported for various pharmacological properties such as anti-TB, anticancer, antimalarial, anti-inflammatory, anti-HIV, antibacterial, antifungal, and antidiabetic, activities. In view of the pharmacological significance of natural peptides, serious research efforts of many scientific groups and pharmaceutical companies have consequently focused on them to explore the possibility of developing their potential analogues as therapeutic agents. Solid phase and solution phase peptide synthesis are the two methodologies currently available for the synthesis of natural or synthetic linear or cyclic depsi-peptides. From a synthetic point of view, there is no doubt that the solid-phase methodology gained added advantages over solution phase methodology in terms of simplicity, purity of the compound and the speed with which peptides can be synthesised. In the present study total synthesis, purification and structural elucidation of analogues of natural anti-TB cyclic depsi-peptides such as depsidomycin, massetolides and viscosin has been attempted by solid phase method using standard Fmoc protocols and finally off resin cyclization in solution phase method. In case of depsidomycin, synthesis of linear peptide on solid phase could not be achieved because of two turn inducing amino acids in the peptide sequence, but total synthesis was achieved by convergent solid phase peptide synthesis followed by cyclization in solution phase method. The title compounds obtained were in good yields and characterized by NMR and HRMS. Anti-TB results revealed that the potential title compound exhibited promising activity at 4 µg/mL against H37Rv and 16 µg/mL against MDR strains of tuberculosis.

Keywords: total synthesis, cyclic depsi-peptides, anti-TB activity, tuberculosis

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Authors: Hajar Al Rajaibi, Kawla Al Toubi, Saeed Al Jaadi, Deepali Jaju, Sanjay Jaju

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Background: The available evidence in Oman on lack of physical activity call for immediate intervention. Physical activity counseling by doctors to their patients is influenced by their attitudes and personal physical fitness. To our best knowledge, the physical activity status of Omani medical students has not been addressed before. These future doctors will have a critical role in improving physical activity in patients and thus their overall health. Objective: The aim of the study is to assess the physical activity level, physical fitness level, and attitudes towards physical activity among Sultan Qaboos University senior medical students. Methods: In this cross-sectional study (N=110; males 55), physical activity level was assessed using International Physical Activity Questionnaire (IPAQ ) short form and attitudes towards physical activity using a fifty-four-items Kenyon questionnaire. The physical fitness level was assessed by estimating maximal oxygen uptake (VO₂max) using Chester step test. Results: Female students reported more sitting time more than 7hr/day (85.5%) compared to male students (40%; p < 0.05). The IPAQ revealed moderate level of physical activity in 58% of students. Students showed a high positive attitude towards physical activity for health and fitness and low attitude for physical activity as tension and risk. Both female and male students had a similar level and attitude towards physical activity. Physical fitness level was excellent (VO₂max > 55ml O₂/kg/min) in 11% of students, good (VO₂max>44-54ml O₂/kg/min) in 49% and average to below-average in 40%. Objectively measured physical fitness level, subjectively reported physical activity level or attitudes towards physical activity were not correlated. Conclusion: Omani medical students have a positive attitude towards physical activity but moderate physical activity level. Longer sitting time in females need further evaluation. Efforts are required to understand reasons for present physical activity level and to promote good physical activity among medical students by creating more awareness and facilities.

Keywords: Chester step test, Kenyon scale, medical students, physical activity, physical fitness

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Authors: Faezeh Aghazadeh

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The catalytic activity of Pt/γ-Al₂O₃ and Pt-Fe/γ-Al₂O₃ catalysts was investigated to bring about the complete oxidation of 2-Propanol. Among them, Pt-Fe/γ-Al₂O₃ was found to be the most promising catalyst based on activity. The catalysts were characterized by (XRD), (SEM), (TEM) and ICP-AES techniques. Iron loadings on Pt/γ-Al₂O₃ had a great effect on catalytic activity, and Pt-Fe/γ-Al₂O₃ (1.75 wt% Fe) catalyst at calcination temperature 300°C was observed to be the most active, which might be contributed to the favorable synergetic effects between Pt and Fe, high activity and the well-dispersed bimetallic phase. The combustion of 2-Propanol in the vapor phase was carried out in a conventional flow U-shape glass reactor used in the differential mode at atmospheric pressure. 2-Propanol was analyzed by a gas chromatograph VARIAN 3800 CX equipped with an FID. As observed, better performance and activity were observed for Pt-Fe/Al₂O₃ bimetallic catalyst. These results indicate that the high dispersion on support gives a positive effect on catalytic activity.

Keywords: volatile organic compounds, bimetallic catalyst, catalytic activity, low temperature

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Authors: Bouchenak Fatima, Lmegharbi Abdelbaki, Houssem Degaichia, Benrebiha Fatima

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The essential oil composition of the leaf of Artemisia absinthium from region of Cherchell (The south of Algeria) was investigated by GC, GC-MS. 27 constituents were identified correspond to 84, 63% of the total oil. The major components are Thujone (60, 82%), Chamazulènel (16, 62%), ρ-cymène (4, 29%) and 2-carène (4.25%). The antimicrobial activity of oil was tested in vitro by two methods (agar diffusion and microdilution) on three plant pathogenic fungi. This oil has been tested for antimicrobial activity against three pathogenic fungi (Botrytis cinerea, Fusarium culmorum and Helminthosporium Sp.).The study of activity was evaluated by two methods: Method of diffusion in gelose and the minimum inhibitory concentration MIC. This oil exhibited an interesting antimicrobial activity. A preliminary study showed that this oil presented high toxicity against this fungus. These results, although preliminary show a good antifungal activity, to limit and inhibit stop the development of those pathogen agent.

Keywords: artemisia absinthian, extraction process, chemical study, antifungal activity

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Authors: Mahta Eskandarnejad

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The aim of this paper was to compare physical activity and mental toughness in the staff and students of the University of Tabriz. 615 people participated in this study and filled demographic questionnaire, mental thoughness48 (MTQ48) questionnaire and habitual physical activity questionnaire (Baecke physical activity questionnaire). The research sample included 355 students and 260 staff (615 questionnaires). For analyzing hypotheses MANOVA, correlation and independent t-test were used. Based on the result; some subscales of mental toughness and physical activity were significantly related. The result showed the significant correlation between mental toughness and physical activity in student and no significant correlation in staff. Students were significantly physically more active than staff, and mental toughness was higher in staff. There was no difference in mental toughness variable between active participants (active staff and student). The results of this study showed that mental toughness could influence the way a person cope with living conditions. It is expected that mental toughness changes can lead to changing in levels of physical activity. It should be noted that the other variables should not be ignored.

Keywords: Baecke physical activity questionnaire, mental toughness, physical activity, university staff, university student

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Authors: P. S. BEDI* , Neavty Thakur, Balvınder Sıngh

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In the present study an attempt has been made to prepare the crude extracts of leaves and stem of ‘Girardinia heterophylla’ by using various solvents like petroleum ether, ethanol and double distilled water. The samples were given the code NGLS 1, NGLS 2, NGLS 3, NGSS 1, NGSS 2 and NGSS 3 respectively. All the extracts were used to study their antimicrobial activity against gram positive bacteria eg. Bacillus subtilis, Gram negative bacteria eg. E. coli, K. pneumonia and antifungal activity against Aspergillus niger. The results of the antimicrobial activity showed that all the crude extracts of the plant posseses antibacterial activity. Maximum antibacterial activity was shown by NGLS 2, NGLS 3 and NGSS 3 against K. pneumonia. The growth of fungus A. niger was also inhibited by all the crude extracts. Maximum inhibition was shown by NGSS 2 followed by NGSS 1.

Keywords: Girardinia heterophylla, leaves and stem extracts, Antibacterial activity, antifungal activity.

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Authors: Grzegorz Swiderski, Agata Jablonska-Trypuc, Natalia Popow, Renata Swislocka, Wlodzimierz Lewandowski

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Doxorubicin belongs to the group of anthracycline antitumor antibiotics. Because of the wide spectrum of actions, it is one of the most widely used anthracycline antibiotics, including the treatment of breast, ovary, bladder, lung cancers as well as neuroblastoma, lymphoma, leukemia and myeloid leukemia. Antitumor activity of doxorubicin is based on the same mechanisms as for most anthracyclines. Like the metal ions affect the nucleic acids on many biological processes, so the environment of the metal chelates of antibiotics can have a significant effect on the pharmacological properties of drugs. Complexation of anthracyclines with metal ions may contribute to the production of less toxic compounds. In the framework of this study, the composition of complexes obtained in aqueous solutions of doxorubicin with metal ions (Cu2+ and Zn2+). Complexation was analyzed by spectrophotometric titration in aqueous solution at pH 7.0. The pH was adjusted with 0.02M Tris-HCl buffer. The composition of the complexes found was Cu: doxorubicin (1: 2) and a Zn: doxorubicin (1: 1). The effect of Dox, Dox-Cu and Dox-Zn was examined in MCF-7 breast cancer cell line, which were obtained from American Type Culture Collection (ATCC). The compounds were added to the cultured cells for a final concentration in the range of 0,01µM to 0,5µM. The number of MCF-7 cells with division into living and dead, was determined by direct counts of cells with the use of trypan blue dye using LUNA Logos Biosystems cell counter. ApoTox-Glo Triplex Assay (Promega, Madison, Wisconsin, USA) was used according to the manufacturer’s instructions to measure the MCF-7 cells’ viability, cytotoxicity and apoptosis. We observed a decrease in cells proliferation in a dose-dependent manner. An increase in cytotoxicity and decrease in viability in the ApoTox Triplex assay was also showed for all tested compounds. Apoptosis, showed as caspase 3/7 activation, was observed only in Dox treatment. In Dox-Zn and Dox-Cu caspase 3/7 activation was not observed. This work was financially supported by National Science Centre, Poland, under the research project number 2014/13/B/NZ7/02 352.

Keywords: anticancer properties, anthracycline antibiotic, doxorubicine, metal complexes

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Authors: Jarel Elgin Tolentino, Arby Denise Nera, Mary Rose Roco, Angela Vianca Aspa, Nikko Beltran, Else Dapat

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Drug resistance by cells has been the problem in the medical field for decades now. The use of medicinal plants as a source of creating powerful drugs has been nowadays recognized worldwide to treat such resistant diseases. In the present study, the potential for Diospyros philippinensis A. DC. to inhibit growth of both bacteria and cancer cell line was conducted. The leaf crude extracts were screened for the presence of phytochemicals and examined for potential bioactivities by employing several assays like Kirby-Bauer disc diffusion method, DPPH (2,2-diphenyl-1-picryl-hydrazyl-hydrate) assay and MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) tetrazolium assay for the antibacterial, antioxidant and cytotoxic activities of the extract, respectively. Phytochemical test results of the extracts revealed the presence of alkaloids, flavonoids, saponins, phenols, quinones, cardiac glycosides, phlobatannins, carbohydrate, cardenolides and proteins. The leaf extracts were found to exhibit antibacterial activity against gram-positive bacteria, high antioxidant activity (99.22% ± 0.005) but did not show any sign of cytotoxicity towards HCT116 (ATCC CCL-247). The study therefore concludes that D. philippinensis A. DC. leaf extract can be a source of antibacterial and chemopreventive agents. This claim may be used as basis for future investigation.

Keywords: bioassay, medicinal plants, plant crude extracts, phytochemical screening

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Authors: Rashmi Tamhankar, Madhav Bapat

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In many projects, we have to use human judgment for determining the duration of the activities which may vary from person to person. Hence, there is vagueness about the time duration for activities in network planning. Fuzzy sets can handle such vague or imprecise concepts and has an application to such network. The vague activity times can be represented by triangular fuzzy numbers. In this paper, a general network with fuzzy activity times is considered and conditions for the critical path are obtained also we compute total float time of each activity. Several numerical examples are discussed.

Keywords: PERT, CPM, triangular fuzzy numbers, fuzzy activity times

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Authors: Xiao Yang, Ji Zhang, Yingli Song, Hui Huang, Jing Zhang, Yan Wang, Rongrong Han, Zhixuan Xiang, Lu Chen, Lingling Gao

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Aim and Objectives: To examine physical activity self-efficacy, identify its predictors, and further explore the mechanism of action among the predictors in mainland Chinese pregnant women with high risk for gestational diabetes mellitus (GDM). Background: Physical activity could protect pregnant women from developing GDM. Physical activity self-efficacy was the key predictor of physical activity. Design: A cross-sectional study was conducted from October 2021 to May 2022 in Zhengzhou, China. Methods: 252 eligible pregnant women completed the Pregnancy Physical Activity Self-efficacy Scale, the Social Support for Physical Activity Scale, the Knowledge on Physical Activity Questionnaire, the 7-item Generalized Anxiety Disorder scale, the Edinburgh Postnatal Depression Scale, and a socio-demographic data sheet. Multiple linear regression was applied to explore the predictors of physical activity self-efficacy. Structural equation modeling was used to explore the mechanism of action among the predictors. Results: Chinese pregnant women with a high risk for GDM reported a moderate level of physical activity self-efficacy. The best-fit regression analysis revealed four variables explained 17.5% of the variance in physical activity self-efficacy. Social support for physical activity was the strongest predictor, followed by knowledge of the physical activity, intention to do physical activity, and anxiety symptoms. The model analysis indicated that knowledge of physical activity could release anxiety and depressive symptoms and then increase physical activity self-efficacy. Conclusion: The present study revealed a moderate level of physical activity self-efficacy. Interventions targeting pregnant women with high risk for GDM need to include the predictors of physical activity self-efficacy. Relevance to clinical practice: To facilitate pregnant women with high risk for GDM to engage in physical activity, healthcare professionals may find assess physical activity self-efficacy and intervene as soon as possible on their first antenatal visit. Physical activity intervention programs focused on self-efficacy may be conducted in further research.

Keywords: physical activity, gestational diabetes, self-efficacy, predictors

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Authors: Nilgün Öztürk, Hakan Sabahtin Ali, Hülya Tuba Kıyan

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The genus Chenopodium belongs to Amaranthaceae, is represented by approximately 250 species in the world and 15 species and three subspecies in Turkey. Chenopodium species are traditionally used to treat chest and abdominal pain, shortness of breath, cough and neurological disorders. Chenopodium quinoa Willd. (Quinoa) is native to Andes region of South America (especially Peru and Bolivia) and cultivated in many countries include also Turkey in the world nowadays. The seeds of quinoa are rich in protein, and the phytochemical composition consists of antioxidant substances such as polyphenolic compounds, flavonoids, vitamins, and minerals; anticancer and neuroprotective compounds such as tocotrienols; anti-inflammatory compounds such as carotenoids and anthocyanins and also saponins and starch. Food products of quinoa such as quinoa cereal bar, pasta and cornflakes are used in the diet made during many disorders like obesity, cardiovascular disorder, hypertension and Celiac disease. Also quinoa seems to have antimicrobial, anti-inflammatory and cholesterol-lowering properties because of its bioactive compounds. In this present study, the aqueous ethanolic extracts of the seeds of three different coloured genotypes of quinoa were investigated for their antioxidant activities using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, ferrous ion-chelating effect, ferric-reducing antioxidant power, ABTS radical cation decolorization assays and total phenolic contents using Folin-Ciocalteu assay. Among the three genotypes of quinoa; the aqueous ethanolic extract of the red genotype had the highest total phenolic content (83.54 ± 2.12 mg gallic acid/100 g extract) whereas the extract of the white genotype had the lowest total phenolic content (70.66 ± 0.25 mg gallic acid/100 g). According to the antioxidant activity results; the extracts showed moderate reducing power effect whereas weak ABTS radical cation decolorization and ferrous ion-chelating effect and also too weak DPPH radical scavenging activity when compared to the positive standards.

Keywords: amaranthaceae, antioxidant activity, Chenopodium quinoa willd., total phenolic content

Procedia PDF Downloads 153