Search results for: Thai medicinal plants
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 3246

Search results for: Thai medicinal plants

846 Hydrodynamics of Selected Ethiopian Rift Lakes

Authors: Kassaye Bewketu Zellelew

Abstract:

The Main Ethiopian Rift Valley lakes suffer from water level fluctuations due to several natural and anthropocentric factors. Lakes located at terminal positions are highly affected by the fluctuations. These fluctuations are disturbing the stability of ecosystems, putting very serious impacts on the lives of many animals and plants around the lakes. Hence, studying the hydrodynamics of the lakes was found to be very essential. The main purpose of this study is to find the most significant factors that contribute to the water level fluctuations and also to quantify the fluctuations so as to identify lakes that need special attention. The research method included correlations, least squares regressions, multi-temporal satellite image analysis and land use change assessment. The results of the study revealed that much of the fluctuations, specially, in Central Ethiopian Rift are caused by human activities. Lakes Abiyata, Chamo, Ziway and Langano are declining while Abaya and Hawassa are rising. Among the studied lakes, Abiyata is drastically reduced in size (about 28% of its area in 1986) due to both human activities (most dominant ones) and natural factors. The other seriously affected lake is Chamo with about 11% reduction in its area between 1986 and 2010. Lake Abaya was found to be relatively stable during this period (showed only a 0.8% increase in its area). Concerned bodies should pay special attention to and take appropriate measures on lakes Abiyata, Chamo and Hawassa.

Keywords: correlations, hydrodynamics, lake level fluctuation, landsat satellite images

Procedia PDF Downloads 251
845 An Improved Discrete Version of Teaching–Learning-Based ‎Optimization for Supply Chain Network Design

Authors: Ehsan Yadegari

Abstract:

While there are several metaheuristics and exact approaches to solving the Supply Chain Network Design (SCND) problem, there still remains an unfilled gap in using the Teaching-Learning-Based Optimization (TLBO) algorithm. The algorithm has demonstrated desirable results with problems with complicated combinational optimization. The present study introduces a Discrete Self-Study TLBO (DSS-TLBO) with priority-based solution representation that can solve a supply chain network configuration model to lower the total expenses of establishing facilities and the flow of materials. The network features four layers, namely suppliers, plants, distribution centers (DCs), and customer zones. It is designed to meet the customer’s demand through transporting the material between layers of network and providing facilities in the best economic Potential locations. To have a higher quality of the solution and increase the speed of TLBO, a distinct operator was introduced that ensures self-adaptation (self-study) in the algorithm based on the four types of local search. In addition, while TLBO is used in continuous solution representation and priority-based solution representation is discrete, a few modifications were added to the algorithm to remove the solutions that are infeasible. As shown by the results of experiments, the superiority of DSS-TLBO compared to pure TLBO, genetic algorithm (GA) and firefly Algorithm (FA) was established.

Keywords: supply chain network design, teaching–learning-based optimization, improved metaheuristics, discrete solution representation

Procedia PDF Downloads 40
844 Determination of Morphological Characteristics of Brassica napus, Sinapis arvensis, Sinapis alba and Camelina sativa

Authors: Betül Gıdık, Fadul Önemli

Abstract:

The Brassicaceae (Cruciferae) is an important family of plants that include many economically important vegetable production, industrial oilseed, spice, fodder crop species and energy production. Canola and mustard species that are in Brassicaceae family have too high contribution to world herbal production. In this study, genotypes of two kinds of (Caravel and Excalibul) canola (Brassica napus), wild mustard (Sinapis arvensis), white mustard (Sinapis alba) and Camelina (Camelina sativa) were grown in the experimental field, and their morphological characteristics were determined. According to the results of the research; plant length was varied between 76.75 cm and 151.50 cm, and the longest plant was belonging to species of Sinapis arvensis. The number of branches varied from 3.75 piece/plant to 17.75 piece/plant and the most numerous branch was counted in species of Sinapis alba. It was determined that the number of grains in one capsule was between 3.75 piece/capsule and 35.75 piece/capsule and the largest amount of grains in the one capsule was in the Excalibul variety of species of Brassica napus. In our research, it has been determined that the plant of Sinapis arvensis is a potential plant for industrial of oil production; such as Brassica napus, Sinapis alba and Camelina (Camelina sativa).

Keywords: Brassica napus, Camelina sativa, canola, Sinapis alba, Sinapis arvensis, wild mustard

Procedia PDF Downloads 184
843 Somatic Embryogenesis of Lachenalia viridiflora, a Critically Endangered Ornamental Geophyte with High Floricultural Potential

Authors: Vijay Kumar, Mack Moyo, Johannes Van Staden

Abstract:

Lachenalia viridiflora is a critically endangered bulbous plant with high potential on the international floriculture market. In the present study, an efficient protocol for in vitro plantlet regeneration through somatic embryogenesis was developed. Embryogenic callus was established on Murashige and Skoog (MS) basal medium supplemented with various concentrations and combinations of picloram and thidiazuron (TDZ). A high number of SEs (28.5 ± 1.49) with at different developmental stages of somatic embryos (SEs: globular embryos, torpedo and cotyledon embryo with bipolar characteristics) was obtained on Murashige and Skoog (MS) (Murashige and Skoog 1962) medium with 2.5 μM picloram, and 1.0 μM TDZ. Histological and scanning electron microscopic (SEM) analysis confirmed the presence of somatic embryos. Mature somatic embryos germinated and developed into plantlets after 6 weeks on half/full strength MS medium. High plant regeneration frequency (91.11 %) was achieved on full-strength MS medium supplemented with 5 μM phloroglucinol (PG). Well-developed healthy plantlets were successfully acclimatized in the greenhouse with a survival rate of 80%. The result of this study is beneficial in the mass propagation of high-quality Lachenalia viridiflora clonal plants for the commercial horticultural market and also provides a platform for future genetic transformation studies on the plant.

Keywords: horticultural plant, Lachenalia viridiflora, phloroglucinol, somatic embryogenesis, thidiazuron

Procedia PDF Downloads 616
842 Role of the Marshes in the Natural Decontamination of Surface Water: A Case of the Redjla Marsh, North-Eastern Algerian

Authors: S. Benessam, T. H. Debieche, A. Drouiche, S. Mahdid, F. Zahi

Abstract:

The marsh is the impermeable depression. It is not very deep and presents the stagnant water. Their water level varies according to the contributions of water (rain, groundwater, stream etc.), when this last reaches the maximum level of the marsh, it flows towards the downstream through the discharge system. The marsh accumulates all the liquid and solid contributions of upstream part. In the North-East Algerian, the Redjla marsh is located on the course of the Tassift river. Its contributions of water come from the upstream part of the river, often characterized by the presence of several pollutants in water related to the urban effluents, and its discharge system supply the downstream part of the river. In order to determine the effect of the marsh on the water quality of the river this study was conducted. A two-monthly monitoring of the physicochemical parameters and water chemistry of the river were carried out, before and after the marsh, during the period from November 2013 to January 2015. The results show that the marsh plays the role of a natural purifier of water of Tassift river, present by drops of conductivity and concentration of the pollutants (ammonium, phosphate, iron, chlorides and bicarbonates) between the upstream part and downstream of the marsh. That indicates that these pollutants are transformed with other chemical forms (case of ammonium towards nitrate), precipitated in complex forms or/and adsorbed by the sediments of the marsh. This storage of the pollutants in the ground of the marsh will be later on a source of pollution for the plants and river water.

Keywords: marsh, natural purification, urban pollution, nitrogen

Procedia PDF Downloads 248
841 Qualitative and Quantitative Analyses of Phytochemicals and Antioxidant Activity of Ficus sagittifolia (Warburg Ex Mildbread and Burret)

Authors: Taiwo O. Margaret, Olaoluwa O. Olaoluwa

Abstract:

Moraceae family has immense phytochemical constituents and significant pharmacological properties, hence have great medicinal values. The aim of this study was to screen and quantify phytochemicals as well as the antioxidant activities of the leaf and stem bark extracts and fractions (crude ethanol extracts, n-hexane, ethyl acetate and aqueous ethanol fractions) of Ficus sagittifolia. Leaf and stem bark of F. sagittifolia were extracted by maceration method using ethanol to give ethanol crude extract. The ethanol crude extract was partitioned by n-hexane and ethyl-acetate to give their respective fractions. All the extracts were screened for their phytochemicals using standard methods. The total phenolic, flavonoid, tannin, saponin contents and antioxidant activity were determined by spectrophotometric method while the alkaloid content was evaluated by titrimetric method. The amount of total phenolic in extracts and fractions were estimated in comparison to gallic acid, whereas total flavonoids, tannins and saponins were estimated corresponding to quercetin, tannic acid and saponin respectively. 2, 2-diphenylpicryl hydrazyl radical (DPPH)* and phosphomolybdate methods were used to evaluate the antioxidant activities of leaf and stem bark of F. sagittifolia. Phytochemical screening revealed the presence of flavonoids, saponins, terpenoids/steroids, alkaloids for both extracts of leaf and stem bark of F. sagittifolia. The phenolic content of F. sagittifolia was most abundant in leaf ethanol crude extract as 3.53 ± 0.03 mg/g equivalent of gallic acid. Total flavonoids and tannins content were highest in stem bark aqueous ethanol fraction of F. sagittifolia estimated as 3.41 ± 0.08 mg/g equivalent of quercetin and 1.52 ± 0.05 mg/g equivalent of tannic acid respectively. The hexane leaf fraction of F. sagittifolia had the utmost saponin and alkaloid content as 5.10 ± 0.48 mg/g equivalent of saponins and 0.171 ± 0.39 g of alkaloids. Leaf aqueous ethanol fraction of F. sagittifolia showed high antioxidant activity (IC50 value of 63.092 µg/mL) and stem ethanol crude extract (227.43 ± 0.78 mg/g equivalent of ascorbic acid) for DPPH and phosphomolybdate method respectively and the least active was found to be the stem hexane fraction using both methods (313.32 µg/mL; 16.21 ± 1.30 mg/g equivalent of ascorbic acid). The presence of these phytochemicals in the leaf and stem bark of F. sagittifolia are responsible for their therapeutic importance as well as the ability to scavenge free radicals in living systems.

Keywords: Moraceae, Ficus sagittifolia, phytochemicals, antioxidant

Procedia PDF Downloads 211
840 The Effect of Different Concentrations of Trichoderma harzianum Fungus on the Phytochemical and Antioxidative Parameters of Cauliflower (Brassica oleracea convar.botrytisl) in Soils Contaminated with Lead

Authors: Mohammad Javad Shakori, Esmaeil Babakhanzadeh Sajirani, Vajihe Esmaili

Abstract:

Today, the increasing contamination is an environmental concern. There is relationship between plants and microorganisms many years ago. In this regard, an experiment was conducted in order to investigate the effect of different levels of lead across three levels ‘zero, 50, and 100 mg/L’ and Trichoderma Harzanium fungus across three levels ‘5, 10, and 15%’ in a factorial design in the form of fully randomized blocks in three replications under form conditions in the climatic conditions of Shahroud in Dehlama Village. This research was performed in 2014-2015 on cauliflower. In this experiment, chlorophyll a, b, total, cartenoid, phenol, flavonoid, and antioxidant properties of cauliflowers were measured. The results indicated that the greatest level of chlorophyll a (75.723 mg/wet weight), chlorophyll b (27.378 mg/wet weight), and total chlorophyll (109.074 mg/wet weight) was related to the interactive effects of 5% treatment of Trichoderma fungus and 0mg/L lead. The results also indicated that the greatest amount of antioxidant (79.88% of free radical) and flavonoides (22.889 mg of coercetin/g of dry weight) was related to the interactive effects of lead 50 mg/L and the treatment of Trichoderma fungus 5%. Further, the greatest level of phenol (21.33 mg of Gaelic acid/ dry weight) was related to the interactive effects of lead 100 mg/L and Trichoderma fungus 5% . As carotenoids are a type of antioxidant and precursor of vitamin A, with the development of alignment effect with other antioxidants such as the total phenol, flavonoid, achieved desirable levels of antioxidant.

Keywords: antioxidant, lead, flavonoid, cauliflower, chlorophyll

Procedia PDF Downloads 261
839 Leaching Losses of Fertilizer Nitrogen as Affected by Sulfur and Nitrification Inhibitor Applications

Authors: Abdel Khalek Selim, Safaa Mahmoud

Abstract:

Experiments were designed to study nitrogen loss through leaching in soil columns treated with different nitrogen sources and elemental sulfur. The soil material (3 kg alluvial or calcareous soil) were packed in Plexiglas columns (10 cm diameter). The soil columns were treated with 2 g N in the form of Ca(NO3)2, urea, urea + inhibitor (Nitrapyrin), another set of these treatments was prepared to add elemental sulfur. During incubation period, leaching was performed by applying a volume of water that allows the percolation of 250-ml water throughout the soil column. The leachates were analyzed for NH4-N and N03-N. After 10 weeks, soil columns were cut into four equal segments and analyzed for ammonium, nitrate, and total nitrogen. Results indicated the following: Ca(NO3)2 treatment showed a rapid NO3 leaching, especially in the first 3 weeks, in both clay and calcareous soils. This means that soil texture did not play any role in this respect. Sulfur addition also did not affect the rate of NO3 leaching. In urea treatment, there was a steady increase of NH4- and NO3–N from one leachate to another. Addition of sulfur with urea slowed down the nitrification process and decreased N losses. Clay soil contained residual N much more than calcareous soil. Almost one-third of added nitrogen might have been immobilized by soil microorganisms or lost through other loss paths. Nitrification inhibitor can play a role in preserving added nitrogen from being lost through leaching. Combining the inhibitor with elemental sulfur may help to stabilize certain preferred ratio of NH4 to NO3 in the soil for the benefit of the growing plants.

Keywords: alluvial soil, calcareous soil, elemental sulfur, nitrate leaching

Procedia PDF Downloads 304
838 Analysis of Cascade Control Structure in Train Dynamic Braking System

Authors: B. Moaveni, S. Morovati

Abstract:

In recent years, increasing the usage of railway transportations especially in developing countries caused more attention to control systems railway vehicles. Consequently, designing and implementing the modern control systems to improve the operating performance of trains and locomotives become one of the main concerns of researches. Dynamic braking systems is an important safety system which controls the amount of braking torque generated by traction motors, to keep the adhesion coefficient between the wheel-sets and rail road in optimum bound. Adhesion force has an important role to control the braking distance and prevent the wheels from slipping during the braking process. Cascade control structure is one of the best control methods for the wide range of industrial plants in the presence of disturbances and errors. This paper presents cascade control structure based on two forward simple controllers with two feedback loops to control the slip ratio and braking torque. In this structure, the inner loop controls the angular velocity and the outer loop control the longitudinal velocity of the locomotive that its dynamic is slower than the dynamic of angular velocity. This control structure by controlling the torque of DC traction motors, tries to track the desired velocity profile to access the predefined braking distance and to control the slip ratio. Simulation results are employed to show the effectiveness of the introduced methodology in dynamic braking system.

Keywords: cascade control, dynamic braking system, DC traction motors, slip control

Procedia PDF Downloads 352
837 A Proposal for a Secure and Interoperable Data Framework for Energy Digitalization

Authors: Hebberly Ahatlan

Abstract:

The process of digitizing energy systems involves transforming traditional energy infrastructure into interconnected, data-driven systems that enhance efficiency, sustainability, and responsiveness. As smart grids become increasingly integral to the efficient distribution and management of electricity from both fossil and renewable energy sources, the energy industry faces strategic challenges associated with digitalization and interoperability — particularly in the context of modern energy business models, such as virtual power plants (VPPs). The critical challenge in modern smart grids is to seamlessly integrate diverse technologies and systems, including virtualization, grid computing and service-oriented architecture (SOA), across the entire energy ecosystem. Achieving this requires addressing issues like semantic interoperability, IT/OT convergence, and digital asset scalability, all while ensuring security and risk management. This paper proposes a four-layer digitalization framework to tackle these challenges, encompassing persistent data protection, trusted key management, secure messaging, and authentication of IoT resources. Data assets generated through this framework enable AI systems to derive insights for improving smart grid operations, security, and revenue generation. Furthermore, this paper also proposes a Trusted Energy Interoperability Alliance as a universal guiding standard in the development of this digitalization framework to support more dynamic and interoperable energy markets.

Keywords: digitalization, IT/OT convergence, semantic interoperability, VPP, energy blockchain

Procedia PDF Downloads 158
836 The Influence of Temperature on Apigenin Extraction from Chamomile (Matricaria recutita) by Superheated Water

Authors: J. Švarc-Gajić, A. Cvetanović

Abstract:

Apigenin is a flavone synthetized by many plants and quite abundant in chamomile (Matricaria recutita) in its free form and in the form of its glucoside and different acylated forms. Many beneficial health effects have been attributed to apigenin, such as chemo-preventive, anxiolytic, anti-inflammatory, antioxidant and antispasmodic. It is reported that free apigenin is much more bioactive in comparison to its bound forms. Subcritical water offers numerous advantages in comparison to conventional extraction techniques, such as good selectivity, low price and safety. Superheated water exhibits high hydrolytical potential which must be carefully balanced when using this solvent for the extraction of bioactive molecules. Moderate hydrolytical potential can be exploited to liberate apigenin from its bound forms, thus increasing biological potential of obtained extracts. The polarity of pressurized water and its hydrolytical potential are highly dependent on the temperature. In this research chamomile ligulate flowers were extracted by pressurized hot water in home-made subcritical water extractor in conditions of convective mass transfer. The influence of the extraction temperature was investigated at 30 bars. Extraction yields of total phenols, total flavonoids and apigenin depending on the operational temperature were calculated based on spectrometric assays. Optimal extraction temperature for maximum yields of total phenols and flavonoids showed to be 160°C, whereas apigenin yield was the highest at 120°C.

Keywords: superheated water, temperature, chamomile, apigenin

Procedia PDF Downloads 470
835 Effect of Wheat Germ Agglutinin- and Lactoferrin-Grafted Catanionic Solid Lipid Nanoparticles on Targeting Delivery of Etoposide to Glioblastoma Multiforme

Authors: Yung-Chih Kuo, I-Hsin Wang

Abstract:

Catanionic solid lipid nanoparticles (CASLNs) with surface wheat germ agglutinin (WGA) and lactoferrin (Lf) were formulated for entrapping and releasing etoposide (ETP), crossing the blood–brain barrier (BBB), and inhibiting the growth of glioblastoma multiforme (GBM). Microemulsified ETP-CASLNs were modified with WGA and Lf for permeating a cultured monolayer of human brain-microvascular endothelial cells (HBMECs) regulated by human astrocytes and for treating malignant U87MG cells. Experimental evidence revealed that an increase in the concentration of catanionic surfactant from 5 μM to 7.5 μM reduced the particle size. When the concentration of catanionic surfactant increased from 7.5 μM to 12.5 μM, the particle size increased, yielding a minimal diameter of WGA-Lf-ETP-CASLNs at 7.5 μM of catanionic surfactant. An increase in the weight percentage of BW from 25% to 75% enlarged WGA-Lf-ETP-CASLNs. In addition, an increase in the concentration of catanionic surfactant from 5 to 15 μM increased the absolute value of zeta potential of WGA-Lf-ETP-CASLNs. It was intriguing that the increment of the charge as a function of the concentration of catanionic surfactant was approximately linear. WGA-Lf-ETP-CASLNs revealed an integral structure with smooth particle contour, displayed a lighter exterior layer of catanionic surfactant, WGA, and Lf and showed a rigid interior region of solid lipids. A variation in the concentration of catanionic surfactant between 5 μM and 15 μM yielded a maximal encapsulation efficiency of ETP ata 7.5 μM of catanionic surfactant. An increase in the concentration of Lf/WGA decreased the grafting efficiency of Lf/WGA. Also, an increase in the weight percentage of ETP decreased its encapsulation efficiency. Moreover, the release rate of ETP from WGA-Lf-ETP-CASLNs reduced with increasing concentration of catanionic surfactant, and WGA-Lf-ETP-CASLNs at 12.5 μM of catanionic surfactant exhibited a feature of sustained release. The order in the viability of HBMECs was ETP-CASLNs ≅ Lf-ETP-CASLNs ≅ WGA-Lf-ETP-CASLNs > ETP. The variation in the transendothelial electrical resistance (TEER) and permeability of propidium iodide (PI) was negligible when the concentration of Lf increased. Furthermore, an increase in the concentration of WGA from 0.2 to 0.6 mg/mL insignificantly altered the TEER and permeability of PI. When the concentration of Lf increased from 2.5 to 7.5 μg/mL and the concentration of WGA increased from 2.5 to 5 μg/mL, the enhancement in the permeability of ETP was minor. However, 10 μg/mL of Lf promoted the permeability of ETP using Lf-ETP-CASLNs, and 5 and 10 μg/mL of WGA could considerably improve the permeability of ETP using WGA-Lf-ETP-CASLNs. The order in the efficacy of inhibiting U87MG cells was WGA-Lf-ETP-CASLNs > Lf-ETP-CASLNs > ETP-CASLNs > ETP. As a result, WGA-Lf-ETP-CASLNs reduced the TEER, enhanced the permeability of PI, induced a minor cytotoxicity to HBMECs, increased the permeability of ETP across the BBB, and improved the antiproliferative efficacy of U87MG cells. The grafting of WGA and Lf is crucial to control the medicinal property of ETP-CASLNs and WGA-Lf-ETP-CASLNs can be promising colloidal carriers in GBM management.

Keywords: catanionic solid lipid nanoparticle, etoposide, glioblastoma multiforme, lactoferrin, wheat germ agglutinin

Procedia PDF Downloads 229
834 Use of Waste Active Sludge for Reducing Fe₂O₃

Authors: A. Parra Parra, M. Vlasova, P. A. Marquez, M. Kakazey, M. C. Resendiz Gonzalez

Abstract:

The work of water treatment plants from various sources of pollution includes a biological treatment stage using activated sludge. Due to the large volume of toxic activated sludge waste (WAS) generated and soil contamination during its storage, WAS disposal technologies are being continuously developed. The most common is the carbonization of WAS. The carbonization products are various forms of ordered and disordered carbon material having different reactivity. The aim of this work was to study the reduction process of Fe₂O₃ mixed with activated sludge waste (WAS). It could be assumed that the simultaneous action of the WAS thermal decomposition process, accompanied by the formation of reactive nano-carbon, with carbothermal reduction of the Fe₂O₃, will permit intensify reduction of metal oxide up to stage of metal and iron carbide formation. The studies showed that the temperature treatment in the region of (800-1000) °C for 1 hour under conditions of oxygen deficiency is accompanied by the occurrence of reactions: Fe₂O₃ → Fe₃O₄ → FeO → Fe, which are typical for the metallurgical process of iron smelting, but less energy-intensive. Depending on the ratio of the WAS - Fe₂O₃ components and the temperature-time regime of reduction of iron oxide, it is possible to distinguish the stages of the predominant formation of ferromagnetic compounds, cast iron, and iron carbide. The results indicated the promise of using WAS as a metals oxide reducing agent and obtaining of ceramic-based on metal carbides.

Keywords: carbothermal reduction, Fe₂O₃, FeₓOᵧ-C, waste activated sludge

Procedia PDF Downloads 124
833 Bioflocculation Using the Purified Wild Strain of P. aeruginosa Culture in Wastewater Treatment

Authors: Mohammad Hajjartabar, Tahereh Kermani Ranjbar

Abstract:

P. aeruginosa EF2 was isolated and identified from human infection sources before in our previous study. The present study was performed to determine the characteristics and activity role of bioflocculant produced by the bacterium in flocculation of the wastewater active sludge treatment. The bacterium was inoculated and then was grown in an orbital shaker at 250 rpm for 5 days at 35 °C under TSB and peptone water media. After incubation period, culture broths of the bacterial strain was collected and washed. The concentration of the bacteria was adjusted. For the extraction of the bacterial bioflocculant, culture was centrifuged at 6000 rpm for 20 min at 4 °C to remove bacterial cells. Supernatant was decanted and pellet containing bioflocculant was dried at 105 °C to a constant weight according to APHA, 2005. The chemical composition of the extracted bioflocculant from the bacterial sample was then analyzed. Wastewater active sludge sample obtained from aeration tank from one of wastewater treatment plants in Tehran, was first mixed thoroughly. After addition of bioflocculant, improvements in floc density were observed with an increase in bioflocculant. The results of this study strongly suggested that the extracted bioflucculant played a significant role in flocculation of the wastewater sample. The use of wild bacteria and nutrient regulation techniques instead of genetic manipulation opens wide investigation area in the future to improve wastewater treatment processes. Also this may put a new path in front of us to attain and improve the more effective bioflocculant using the purified microbial culture in wastewater treatment.

Keywords: wastewater treatment, P. aeruginosa, sludge treatment

Procedia PDF Downloads 141
832 Deniplant Nutraceuticals for Endometriosis Pain

Authors: Gheorghe Giurgiu, Manole Cojocaru, Mihnea Andrei Nicodin

Abstract:

Background: Inflammation has the main role in the progression of endometriosis. The mechanisms by which endometriosis induces a chronic pain state remain poorly understood. Unfortunately, there is no known cure for endometriosis. But you can manage it with medication and at-home treatments. Some findings have highlighted the main role of inflammation in endometriosis by acting on proliferation, apoptosis, and angiogenesis. The introduction of new agents can be effective in improving the condition of patients; for example, plants are promising sources of bioactive natural components. Objectives: These natural compounds could be interesting strategies in therapy. While there is no absolute cure for this condition, some home remedies can relieve the pain and discomfort it brings. The purpose of this study is to summarize the potential action of Deniplant nutraceuticals in endometriosis by acting on inflammation. Materials and Methods: The primary symptoms of endometriosis are pelvic pain and infertility. The use of Deniplant nutraceuticals could be interesting in disease management for women. Results: Treating pain-related aspects of endometriosis would contribute to the improvement of mental health and daytime function. Because the microbiome can influence inflammation, new therapies can develop through its natural modulation. There are other options, including natural remedies, herbs like cinnamon twigs or licorice root, or supplements such as thiamine, magnesium, or omega-3 fatty acids. Conclusion: Deniplant nutraceuticals can downregulate inflammation in endometriosis. Nevertheless, the limited number of studies focusing on the different interactions of Deniplant nutraceuticals in endometriosis restricts its clear and immediate use in a therapeutic strategy.

Keywords: endometriosis, diet, Deniplant nutraceuticals, pain

Procedia PDF Downloads 59
831 Estimation of the Effectiveness of Tasik Kemajuan and Tasik Inovasi as Flood Detention Pond at UTHM Campus

Authors: Noor Aliza Binti Ahmad, Azra Munirah Mat Daud, Sabariah Musa, Mohamad Azhar MK

Abstract:

Flooding is a common natural disaster in Malaysia triggered by heavy rainfall. Urbanization that increases the construction of paved areas, subsequently raise surface runoff and reduce time of concentration. It increases flood magnitude and so that leads to greater flood problems as what has happened at Universiti Tun Hussein Onn Malaysia (UTHM) area in December 2006 and earlier 2007. Tasik Kemajuan and Tasik Inovasi were constructed as recreation ponds and have also functioned as flood ponds. Unfortunately, the flood problem still occurs persistently. Thus, the effectiveness of Tasik Kemajuan and Tasik Inovasi in reducing the flood problems need to be investigated and the causes of flood events at UTHM Campus need to be evaluated. The results from this study show that the conditions of Tasik Kemajuan and Tasik Inovasi are effective in reducing the flood water levels. It also can be concluded that increasing water level in both lakes in UTHM Campus are significantly influenced by presence of the grass and rubbish. During dry condition, the flow rates with three different days are 59.38m3/s, 60.71m3/s and 59.08m3/s and while for wet condition in two different days are 89.59 m3/s and 86.61m3/s. In conclusion, this system should be improved to prevent future flooding either widened or reduced drainage floor, and also perform maintenance on the plants that live around the lake.

Keywords: drainage system, flood detention, lakes, storm water

Procedia PDF Downloads 313
830 Energy Efficient Plant Design Approaches: Case Study of the Sample Building of the Energy Efficiency Training Facilities

Authors: Idil Kanter Otcu

Abstract:

Nowadays, due to the growing problems of energy supply and the drastic reduction of natural non-renewable resources, the development of new applications in the energy sector and steps towards greater efficiency in energy consumption are required. Since buildings account for a large share of energy consumption, increasing the structural density of buildings causes an increase in energy consumption. This increase in energy consumption means that energy efficiency approaches to building design and the integration of new systems using emerging technologies become necessary in order to curb this consumption. As new systems for productive usage of generated energy are developed, buildings that require less energy to operate, with rational use of resources, need to be developed. One solution for reducing the energy requirements of buildings is through landscape planning, design and application. Requirements such as heating, cooling and lighting can be met with lower energy consumption through planting design, which can help to achieve more efficient and rational use of resources. Within this context, rather than a planting design which considers only the ecological and aesthetic features of plants, these considerations should also extend to spatial organization whereby the relationship between the site and open spaces in the context of climatic elements and planting designs are taken into account. In this way, the planting design can serve an additional purpose. In this study, a landscape design which takes into consideration location, local climate morphology and solar angle will be illustrated on a sample building project.

Keywords: energy efficiency, landscape design, plant design, xeriscape landscape

Procedia PDF Downloads 250
829 Deciphering Suitability of Rhamnolipids as Emulsifying Agent for Hydrophobic Pollutants

Authors: Asif Jamal, Samia Sakindar, Ramla Rehman

Abstract:

Biosurfactants are amphiphilic surface active compounds obtained from natural resources such as plants and microorganisms. Because of their diverse physicochemical characteristics biosurfactant are replacing synthetic compounds in various commercial applications. In present study, a strain of P. aeruginosa was isolated from crude oil contaminated soil as efficient biosurfactant producers. The biosurfactant production was analyzed as a function of surface tension reduction, oil spreading capacity, emulsification index and hemolysis assay. This bacterial strain showed excellent emulsion activity of EI24 85%, surface tension reduction up to 28.6 mNm-1 and 7.0 mm oil displacement zone. Physicochemical and biological properties of extracted rhamnolipid were also investigated in current study. The chemical composition of product from strain PSS was analyzed by FTIR spectroscopy. The results revealed that extracted biosurfactant was rhamnolipid type in nature having RL-1 and RL-2 homologues. The surface behavior of rhamnolipid in aqueous phase was investigated varying extreme pH, temperature, salt conditions and with various hydrocarbons. The results indicated that biosurfactant produced by strain PSS Which showed stability during high temperature up to 121 C, salt concentrations up to 20% and pH range between (4—14). The emulsification activity with different hydrocarbons was also remarkable. It was concluded that rhamnolipid biosurfactant produced by strain PSS has excellent potential as emulsifying/remediation agent for broad range of hydrophobic pollutants.

Keywords: P. aeruginosa, bioremediation, rhamnolipid, surfactants

Procedia PDF Downloads 266
828 High-Performance Thin-layer Chromatography (HPTLC) Analysis of Multi-Ingredient Traditional Chinese Medicine Supplement

Authors: Martin Cai, Khadijah B. Hashim, Leng Leo, Edmund F. Tian

Abstract:

Analysis of traditional Chinese medicinal (TCM) supplements has always been a laborious task, particularly in the case of multi‐ingredient formulations. Traditionally, herbal extracts are analysed using one or few markers compounds. In the recent years, however, pharmaceutical companies are introducing health supplements of TCM active ingredients to cater to the needs of consumers in the fast-paced society in this age. As such, new problems arise in the aspects of composition identification as well as quality analysis. In most cases of products or supplements formulated with multiple TCM herbs, the chemical composition, and nature of each raw material differs greatly from the others in the formulation. This results in a requirement for individual analytical processes in order to identify the marker compounds in the various botanicals. Thin-layer Chromatography (TLC) is a simple, cost effective, yet well-regarded method for the analysis of natural products, both as a Pharmacopeia-approved method for identification and authentication of herbs, and a great analytical tool for the discovery of chemical compositions in herbal extracts. Recent technical advances introduced High-Performance TLC (HPTLC) where, with the help of automated equipment and improvements on the chromatographic materials, both the quality and reproducibility are greatly improved, allowing for highly standardised analysis with greater details. Here we report an industrial consultancy project with ONI Global Pte Ltd for the analysis of LAC Liver Protector, a TCM formulation aimed at improving liver health. The aim of this study was to identify 4 key components of the supplement using HPTLC, following protocols derived from Chinese Pharmacopeia standards. By comparing the TLC profiles of the supplement to the extracts of the herbs reported in the label, this project proposes a simple and cost-effective analysis of the presence of the 4 marker compounds in the multi‐ingredient formulation by using 4 different HPTLC methods. With the increasing trend of small and medium-sized enterprises (SMEs) bringing natural products and health supplements into the market, it is crucial that the qualities of both raw materials and end products be well-assured for the protection of consumers. With the technology of HPTLC, science can be incorporated to help SMEs with their quality control, thereby ensuring product quality.

Keywords: traditional Chinese medicine supplement, high performance thin layer chromatography, active ingredients, product quality

Procedia PDF Downloads 266
827 Identification of Potent and Selective SIRT7 Anti-Cancer Inhibitor via Structure-Based Virtual Screening and Molecular Dynamics Simulation

Authors: Md. Fazlul Karim, Ashik Sharfaraz, Aysha Ferdoushi

Abstract:

Background: Computational medicinal chemistry approaches are used for designing and identifying new drug-like molecules, predicting properties and pharmacological activities, and optimizing lead compounds in drug development. SIRT7, a nicotinamide adenine dinucleotide (NAD+)-dependent deacylase which regulates aging, is an emerging target for cancer therapy with mounting evidence that SIRT7 downregulation plays important roles in reversing cancer phenotypes and suppressing tumor growth. Activation or altered expression of SIRT7 is associated with the progression and invasion of various cancers, including liver, breast, gastric, prostate, and non-small cell lung cancer. Objectives: The goal of this work was to identify potent and selective bioactive candidate inhibitors of SIRT7 by in silico screening of small molecule compounds obtained from Nigella sativa (N. sativa). Methods: SIRT7 structure was retrieved from The Research Collaboratory for Structural Bioinformatics Protein Data Bank (RCSB PDB), and its active site was identified using CASTp and metaPocket. Molecular docking simulation was performed with PyRx 0.8 virtual screening software. Drug-likeness properties were tested using SwissADME and pkCSM. In silico toxicity was evaluated by Osiris Property Explorer. Bioactivity was predicted by Molinspiration software. Antitumor activity was screened for Prediction of Activity Spectra for Substances (PASS) using Way2Drug web server. Molecular dynamics (MD) simulation was carried out by Desmond v3.6 package. Results: A total of 159 bioactive compounds from the N. Sativa were screened against the SIRT7 enzyme. Five bioactive compounds: chrysin (CID:5281607), pinocembrin (CID:68071), nigellidine (CID:136828302), nigellicine (CID:11402337), and epicatechin (CID:72276) were identified as potent SIRT7 anti-cancer candidates after docking score evaluation and applying Lipinski's Rule of Five. Finally, MD simulation identified Chrysin as the top SIRT7 anti-cancer candidate molecule. Conclusion: Chrysin, which shows a potential inhibitory effect against SIRT7, can act as a possible anti-cancer drug candidate. This inhibitor warrants further evaluation to check its pharmacokinetics and pharmacodynamics properties both in vitro and in vivo.

Keywords: SIRT7, antitumor, molecular docking, molecular dynamics simulation

Procedia PDF Downloads 60
826 Physiological and Molecular Characterizations of Ricinus Communis Genotypes under Cadmium Stress

Authors: Rini Rahul, Manoj Kumar

Abstract:

Cadmium (Cd) is a poisonous trace metal, which is responsible for excess reactive oxygen species generation (ROS) in plants, thereby adversely affecting their productivity and commercial potential. Ricinus communis (castor) is an industry-efficient non-edible bioenergy crop used for phytoremediation and re-vegetation. We have determined the total Cd content in castor genotypes and established a relationship between the Cd tolerance mechanism and physiological parameters like chlorophyll fluorescence, the total photosynthetic activity, chlorophyll and carotenoid content as well as ROS generation and malondialdehyde content. This study is an effort to comprehend the interrelation between Cd toxicity (control, 250 µM and 500 µM), proline, various ROS scavenging enzymes (anti-oxidative in nature), nicotianamine synthase (NAS) and Natural resistance-associated macrophage protein (NRAMP) gene. The antioxidant enzyme activity increased for WM hence conferring Cd toxicity in this genotype. RcNRAMP genes showed differential expression in GCH2 and WM genotypes; this can also be one of the reasons for Cd toxicity and sensitivity in WM and GCH2, respectively. The cause of pronounced Cd tolerance in WM leaves can be because of enhanced expression of RcNAS1, RcNAS2 and RcNAS3 genes. Our results demonstrate that there is an interrelation between Cd toxicity (control, 250 µM and 500 µM), proline, various ROS scavenging enzymes (anti-oxidative in nature), NAS and NRAMP gene.

Keywords: ricinus communis, cadmium, reactive oxygen species, nicotianamine synthase, NRAMP, malondialdehyde

Procedia PDF Downloads 61
825 Taraxacum Officinale (Dandelion) and Its Phytochemical Approach to Malignant Diseases

Authors: Angel Champion

Abstract:

Chemotherapy and radiation use an acidified approach to induce apoptosis, which only kills mature cancer cells while resulting in gene and cell damage with significant levels of toxicity in tumor-affected tissues and organs. The acid approach, where the cells exterminated are not differentiated, induces the disappearance of white blood cells from the blood. This increases susceptibility to infection in severe forms of cancer spread. However, chemotherapy and radiation cannot kill cancer stem cells that metastasize, being the leading cause of 98% of cancer fatalities. With over 12 million new cancer cases symptomatic each year, including common malignancies such as Hepatocellular Carcinoma (HCC), this study aims to assess the bioactive constituents and phytochemical composition of Taraxacum Officinale (Dandelion). This analysis enables pharmaceutical quality and potency to be applied to studies on cancer cell proliferation and apoptosis. A phytochemical screening is carried out to identify the antioxidant components of Dandelion root, stem, and flower extract. The constituents tested for are phlorotannins, carbohydrates, glycosides, saponins, flavonoids, alkaloids, sterols, triterpenes, and anthraquinone glycosides. To conserve the existing phenolic compounds, a portion of the constituent tests will be examined with an acid, alcohol, or aqueous solvent. As a result, the qualitative and quantitative variations within the Dandelion extract that measure uniform effective potency are vital to the conformity for producing medicinal products. These medicines will be constructed with a consistent, uniform composition that physicians can use to control and effectively eradicate malignant diseases safely. Taraxacum Officinale's phytochemical composition comprises a highly-graded potency due to present bioactive contents that will essentially drive out malignant disease within the human body. Its high potency rate is powerful enough to eliminate both mature cancer cells and cancer stem cells without the cell and gene damage induced by chemotherapy and radiation. Correspondingly, the high margins of cancer mortality on a global scale are mitigated. This remarkable contribution to modern therapeutics will essentially optimize the margins of natural products and their derivatives, which account for 50% of pharmaceuticals in modern therapeutics, while preventing the adverse effects of radiation and chemotherapy drugs.

Keywords: antioxidant, apoptosis, metastasize, phytochemical, proliferation, potency

Procedia PDF Downloads 58
824 A Novel PfkB Gene Cloning and Characterization for Expression in Potato Plants

Authors: Arfan Ali, Idrees Ahmad Nasir

Abstract:

Potato (Solanum tuberosum) is an important cash crop and popular vegetable in Pakistan and throughout the world. Cold storage of potatoes accelerates the conversion of starch into reduced sugars (glucose and fructose). This process causes dry mass and bitter taste in the potatoes that are not acceptable to end consumers. In the current study, the phosphofructokinase B gene was cloned into the pET-30 vector for protein expression and the pCambia-1301 vector for plant expression. Amplification of a 930bp product from an E. coli strain determined the successful isolation of the phosphofructokinase B gene. Restriction digestion using NcoI and BglII along with the amplification of the 930bp product using gene specific primers confirmed the successful cloning of the PfkB gene in both vectors. The protein was expressed as a His-PfkB fusion protein. Western blot analysis confirmed the presence of the 35 Kda PfkB protein when hybridized with anti-His antibodies. The construct Fani-01 was evaluated transiently using a histochemical gus assay. The appearance of blue color in the agroinfiltrated area of potato leaves confirmed the successful expression of construct Fani-01. Further, the area displaying gus expression was evaluated for PfkB expression using ELISA. Moreover, PfkB gene expression evaluated through transient expression determined successful gene expression and highlighted its potential utilization for stable expression in potato to reduce sweetening due to long-term storage.

Keywords: potato, Solanum tuberosum, transformation, PfkB, anti-sweetening

Procedia PDF Downloads 455
823 The Transcriptome of Carnation (Dianthus Caryophyllus) of Elicited Cells with Fusarium Oxysporum f.sp. Dianthi

Authors: Juan Jose Filgueira, Daniela Londono-Serna, Liliana Maria Hoyos

Abstract:

Carnation (Dianthus caryophyllus) is one of the most important products of exportation in the floriculture industry worldwide. Fusariosis is the disease that causes the highest losses on farms, in particular the one produced by Fusarium oxysporum f.sp. dianthi, called vascular wilt. Gene identification and metabolic routes of the genes that participate in the building of the plant response to Fusarium are some of the current targets in the carnation breeding industry. The techniques for the identifying of resistant genes in the plants, is the analysis of the transcriptome obtained during the host-pathogen interaction. In this work, we report the cell transcriptome of different varieties of carnation that present differential response from Fusarium oxysporum f.sp. dianthi attack. The cells of the different hybrids produced in the outbreeding program were cultured in vitro and elicited with the parasite in a dual culture. The isolation and purification of mRNA was achieved by using affinity chromatography Oligo dT columns and the transcriptomes were obtained by using Illumina NGS techniques. A total of 85,669 unigenes were detected in all the transcriptomes analyzed and 31,000 annotations were found in databases, which correspond to 36.2%. The library construction of genic expression techniques used, allowed to recognize the variation in the expression of genes such as Germin-like protein, Glycosyl hydrolase family and Cinnamate 4-hydroxylase. These have been reported in this study for the first time as part of the response mechanism to the presence of Fusarium oxysporum.

Keywords: Carnation, Fusarium, vascular wilt, transcriptome

Procedia PDF Downloads 133
822 Micropollutant Carbamazepine: Its Occurrences, Toxicological Effects, and Possible Degradation Methods (Review)

Authors: Azad Khalid, Sifa Dogan

Abstract:

Because of its persistence in conventional treatment plants and broad prevalence in water bodies, the pharmaceutical chemical carbamazepine (CBZ) has been suggested as an anthropogenic marker to evaluate water quality. This study provides a thorough examination of the origins and occurrences of CBZ in water bodies, as well as the drug's toxicological effects and laws. Given CBZ's well-documented negative consequences on the human body when used medicinally, cautious monitoring in water is advised. CBZ residues in drinking water may enter embryos and newborns via intrauterine exposure or breast-feeding, causing congenital abnormalities and/or neurodevelopmental issues over time. The insufficiency of solo solutions was shown after an in-depth technical study of traditional and sophisticated treatment technologies. Nanofiltration and reverse osmosis membranes are more successful at removing CBZ than traditional activated sludge and membrane bioreactor techniques. Recent research has shown that severe chemical cleaning, which is essential to prevent membrane fouling, may lower long-term removal efficiency. Furthermore, despite the efficacy of activated carbon adsorption and advanced oxidation processes, a few issues such as chemical cost and activated carbon renewal must be carefully examined. Individual technology constraints lead to the benefits of combined and hybrid systems, namely the heterogeneous advanced oxidation process.

Keywords: carbamazepine, occurrence, toxicity, conventical treatment, advanced oxidation process (AOPs)

Procedia PDF Downloads 85
821 Oil Extraction from Microalgae Dunalliela sp. by Polar and Non-Polar Solvents

Authors: A. Zonouzi, M. Auli, M. Javanmard Dakheli, M. A. Hejazi

Abstract:

Microalgae are tiny photosynthetic plants. Nowadays, microalgae are being used as nutrient-dense foods and sources of fine chemicals. They have significant amounts of lipid, carotenoids, vitamins, protein, minerals, chlorophyll, and pigments. Oil extraction from algae is a hotly debated topic currently because introducing an efficient method could decrease the process cost. This can determine the sustainability of algae-based foods. Scientific research works show that solvent extraction using chloroform/methanol (2:1) mixture is one of the efficient methods for oil extraction from algal cells, but both methanol and chloroform are toxic solvents, and therefore, the extracted oil will not be suitable for food application. In this paper, the effect of two food grade solvents (hexane and hexane/ isopropanol) on oil extraction yield from microalgae Dunaliella sp. was investigated and the results were compared with chloroform/methanol (2:1) extraction yield. It was observed that the oil extraction yield using hexane, hexane/isopropanol (3:2) and chloroform/methanol (2:1) mixture were 5.4, 13.93, and 17.5 (% w/w, dry basis), respectively. The fatty acid profile derived from GC illustrated that the palmitic (36.62%), oleic (18.62%), and stearic acids (19.08%) form the main portion of fatty acid composition of microalgae Dunalliela sp. oil. It was concluded that, the addition of isopropanol as polar solvent could increase the extraction yield significantly. Isopropanol solves cell wall phospholipids and enhances the release of intercellular lipids, which improves accessing of hexane to fatty acids.

Keywords: fatty acid profile‎, microalgae‎, oil extraction‎, polar solvent‎

Procedia PDF Downloads 357
820 Hard Sludge Formation and Consolidation in Pressurized Water Reactor Steam Generators: An Experimental Study

Authors: R. Fernandez-Saavedra, M. B. Gomez-Mancebo, D. Gomez-Briceno

Abstract:

The gradual corrosion of PWR (Pressurized Water Reactor) feedwater, condensate and drain systems results in the inevitable liberation of corrosion products, principally metallic oxides, to the secondary circuit. In addition, other contaminants and impurities are introduced into the makeup water, auxiliary feedwater and by condenser leaks. All these compounds circulating in the secondary flow can eventually be transported to steam generators and be transformed into deposits on their surfaces. Deposits that accumulate on the tube sheet are known as sludge piles and when they consolidate and harden become into hard sludge. Hard sludge is especially detrimental because it favors tube deformation or denting at the top of tube sheet and further stress corrosion cracking (SCC). These failures affect the efficiency of nuclear power plants. In a recent work, a model for the formation and consolidation of hard sludge has been formulated, highlighting the influence of aluminum and silicon compounds in the initial formation of hard sludge. In this work, an experimental study has been performed in order to get a deeper understanding of the behavior of Al and Si species in hard sludge formation and consolidation. For this purpose, the key components of hard sludge (magnetite, aluminum and/or silicon sources) have been isothermally autoclaved in representative secondary circuit conditions during one week, and the resulting products have been chemically and structurally characterized by XRF and XRD techniques, respectively.

Keywords: consolidation, hard sludge, secondary circuit, steam generator

Procedia PDF Downloads 180
819 A More Sustainable Decellularized Plant Scaffold for Lab Grown Meat with Ocean Water

Authors: Isabella Jabbour

Abstract:

The world's population is expected to reach over 10 billion by 2050, creating a significant demand for food production, particularly in the agricultural industry. Cellular agriculture presents a solution to this challenge by producing meat that resembles traditionally produced meat, but with significantly less land use. Decellularized plant scaffolds, such as spinach leaves, have been shown to be a suitable edible scaffold for growing animal muscle, enabling cultured cells to grow and organize into three-dimensional structures that mimic the texture and flavor of conventionally produced meat. However, the use of freshwater to remove the intact extracellular material from these plants remains a concern, particularly when considering scaling up the production process. In this study, two protocols were used, 1X SDS and Boom Sauce, to decellularize spinach leaves with both distilled water and ocean water. The decellularization process was confirmed by histology, which showed an absence of cell nuclei, DNA and protein quantification. Results showed that spinach decellularized with ocean water contained 9.9 ± 1.4 ng DNA/mg tissue, which is comparable to the 9.2 ± 1.1 ng DNA/mg tissue obtained with DI water. These findings suggest that decellularized spinach leaves using ocean water hold promise as an eco-friendly and cost-effective scaffold for laboratory-grown meat production, which could ultimately transform the meat industry by providing a sustainable alternative to traditional animal farming practices while reducing freshwater use.

Keywords: cellular agriculture, plant scaffold, decellularization, ocean water usage

Procedia PDF Downloads 70
818 Identification, Synthesis, and Biological Evaluation of the Major Human Metabolite of NLRP3 Inflammasome Inhibitor MCC950

Authors: Manohar Salla, Mark S. Butler, Ruby Pelingon, Geraldine Kaeslin, Daniel E. Croker, Janet C. Reid, Jong Min Baek, Paul V. Bernhardt, Elizabeth M. J. Gillam, Matthew A. Cooper, Avril A. B. Robertson

Abstract:

MCC950 is a potent and selective inhibitor of the NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammasome that shows early promise for treatment of inflammatory diseases. The identification of major metabolites of lead molecule is an important step during drug development process. It provides an information about the metabolically labile sites in the molecule and thereby helping medicinal chemists to design metabolically stable molecules. To identify major metabolites of MCC950, the compound was incubated with human liver microsomes and subsequent analysis by (+)- and (−)-QTOF-ESI-MS/MS revealed a major metabolite formed due to hydroxylation on 1,2,3,5,6,7-hexahydro-s-indacene moiety of MCC950. This major metabolite can lose two water molecules and three possible regioisomers were synthesized. Co-elution of major metabolite with each of the synthesized compounds using HPLC-ESI-SRM-MS/MS revealed the structure of the metabolite (±) N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydroxypropan-2-yl)furan-2-sulfonamide. Subsequent synthesis of individual enantiomers and coelution in HPLC-ESI-SRM-MS/MS using a chiral column revealed the metabolite was R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydroxypropan-2-yl)furan-2-sulfonamide. To study the possible cytochrome P450 enzyme(s) responsible for the formation of major metabolite, MCC950 was incubated with a panel of cytochrome P450 enzymes. The result indicated that CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C18, CYP2C19, CYP2J2 and CYP3A4 are most likely responsible for the formation of the major metabolite. The biological activity of the major metabolite and the other synthesized regioisomers was also investigated by screening for for NLRP3 inflammasome inhibitory activity and cytotoxicity. The major metabolite had 170-fold less inhibitory activity (IC50-1238 nM) than MCC950 (IC50-7.5 nM). Interestingly, one regioisomer had shown nanomolar inhibitory activity (IC50-232 nM). However, no evidence of cytotoxicity was observed with any of these synthesized compounds when tested in human embryonic kidney 293 cells (HEK293) and human liver hepatocellular carcinoma G2 cells (HepG2). These key findings give an insight into the SAR of the hexahydroindacene moiety of MCC950 and reveal a metabolic soft spot which could be blocked by chemical modification.

Keywords: Cytochrome P450, inflammasome, MCC950, metabolite, microsome, NLRP3

Procedia PDF Downloads 239
817 Dynamics of Antioxidant and Anti-Radical Activity of the Extracts of Certain Plants of Kazakhstan

Authors: A. Kazbekova, A. Kudaibergenov, G. Atazhanova, S. Adekenov

Abstract:

In recent years, it achieved some progress such a direction as to study the possibility of correlation between different types of biological activity. In particular, in our work, we consider questions such as: the impact of the qualitative composition of total substances in the example of plant extracts on antioxidant and antiradical activity, the presents of correlation between these types of activity, etc. It is known that there is a relationship between the values of optical density of working solutions of extracts and corresponding bioactivity in vitro, in particular, the antioxidant and hepatoprotective effects. In this study, we have identified that among some studied species of wormwood (Artemisia viridis Wild, Artemisia jacutica Drob, Artemisia annua L, Artemisia siversiana Wild, Artemisia adamsii Bess, Artemisia tianschanica, Artemisia obtusiloba Ledeb., Artemisia heptopotamica), as well as extracts of Inula caspica, Аjania tenuifolia, Abies sibirica, Galatella songorica, Mentha asiatica and Thymus mugodzharicus it was identified that the highest content of polyphenol compounds is in Thymus mugodzharicus. At the same time, we determined the antioxidant and antiradical activity, which was the highest for the Thymus mugodzharicus. Butylhydroxyanisole and ascorbic acid were used as comparison substances. Also, it was established that antioxidant and anti-radical activities depend on the concentration of the of all investigated samples. Based on obtained data, we believe that the extract of Thymus mugodzharicus can be recommended for further study on the antioxidant and antiradical activity in vivo, as well as the opportunity of this sample to demonstrate hepatoprotective effect. The study was sponsored by SANTO academic program.

Keywords: in vitro, in vivo, antioxidant, hepatoprotective effect

Procedia PDF Downloads 307