Search results for: Medicinal Chemistry
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 1251

Search results for: Medicinal Chemistry

1101 Exploring Students’ Visual Conception of Matter and Its Implications to Teaching and Learning Chemistry

Authors: Allen A. Espinosa, Arlyne C. Marasigan, Janir T. Datukan

Abstract:

The study explored how students visualize the states and classifications of matter using scientific models. It also identified misconceptions of students in using scientific models. In general, high percentage of students was able to use scientific models correctly and only a little misconception was identified. From the result of the study, a teaching framework was formulated wherein scientific models should be employed in classroom instruction to visualize abstract concepts in chemistry and for better conceptual understanding.

Keywords: visual conception, scientific models, mental models, states of matter, classification of matter

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1100 Effects of Drying Temperatures on the Qualitative and Quantitative Phytochemicals of Aqueous Extracts If the Calyces of Hibiscus Sabdariffa

Authors: John O. Efosa, S. Egielewa, M. A. Azeke

Abstract:

Hibiscus sabdariffa (Hs) is known for its delicacy and also for medicinal properties. The flower calyces are usually sun- or oven-dried after harvesting. There are unverified claims that calyces dried at lower temperatures have better medicinal potentials than those dried at higher temperatures. The present work, therefore, aimed to study the effects of drying temperatures on the photochemical composition and antioxidant potential of aqueous extracts of the calyces of Hs. The calyces were dried at different temperatures (freeze-drying at -580C, drying at 300C, 400C, and 500 C.) respectively to constant weight. Samples (25 g) of dried calyces from each drying temperatures were weighed and placed in clean conical flasks and extracted; each was used for the analysis. Validated analytical assays were used for the determination of the different Phytochemicals. From the results obtained, it was observed that drying at 30°C resulted in the highest retention of total phenols, total flavonoids, tannins, alkaloids and saponins. Using the Inhibition Concentration values (IC50), some antioxidant parameters were found to follow the same trend as the earlier mentioned phytochemicals. Drying at 30°C resulted in the highest retention of DPPH Radical Scavenging Activity, Ferric Reducing Antioxidant Potential (FRAP), Nitrite radical scavenging Activity, 2, 2-azinobis-3-ethylbenzotiazoline-6-sulfonic acid (ABTS) radical scavenging activity There were, however, significant reductions in vitamin C and oxalate contents as the drying temperature increased (P < 0.05). From the results, it recommended that the calyces of Hibiscus sabdariffa be dried at 30°C in order to optimally elicit its medicinal potentials.

Keywords: antioxidant, drying temperature, hibiscus sabdariffa, phytochemicals, quantitative

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1099 In-silico Antimicrobial Activity of Bioactive Compounds of Ricinus communis against DNA Gyrase of Staphylococcus aureus as Molecular Target

Authors: S. Rajeswari

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Medicinal Plant extracts and their bioactive compounds have been used for antimicrobial activities and have significant remedial properties. In the recent years, a wide range of investigations have been carried out throughout the world to confirm antimicrobial properties of different medicinally important plants. A number of plants showed efficient antimicrobial activities, which were comparable to that of synthetic standard drugs or antimicrobial agents. The large family Euphorbiaceae contains nearly about 300 genera and 7,500 speciesand one among is Ricinus communis or castor plant which has high traditional and medicinal value for disease free healthy life. Traditionally the plant is used as laxative, purgative, fertilizer and fungicide etc. whereas the plant possess beneficial effects such as anti-oxidant, antihistamine, antinociceptive, antiasthmatic, antiulcer, immunomodulatory anti diabetic, hepatoprotective, anti inflammatory, antimicrobial, and many other medicinal properties. This activity of the plant possess due to the important phytochemical constituents like flavonoids, saponins, glycosides, alkaloids and steroids. The presents study includes the phytochemical properties of Ricinus communis and to prediction of the anti-microbial activity of Ricinus communis using DNA gyrase of Staphylococcus aureus as molecular target. Docking results of varies chemicals compounds of Ricinus communis against DNA gyrase of Staphylococcus aureus by maestro 9.8 of Schrodinger show that the phytochemicals are effective against the target protein DNA gyrase. our studies suggest that the phytochemical from Ricinus communis such has INDICAN (G.Score 4.98) and SUPLOPIN-2(G.Score 5.74) can be used as lead molecule against Staphylococcus infections.

Keywords: euphorbiaceae, antimicrobial activity, Ricinus communis, Staphylococcus aureus

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1098 Superamolecular Chemistry and Packing of FAMEs in the Liquid Phase for Optimization of Combustion and Emission

Authors: Zeev Wiesman, Paula Berman, Nitzan Meiri, Charles Linder

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Supramolecular chemistry refers to the domain of chemistry beyond that of molecules and focuses on the chemical systems made up of a discrete number of assembled molecular sub units or components. Biodiesel components self arrangements is closely related/affect their physical properties in combustion systems and emission. Due to technological difficulties, knowledge regarding the molecular packing of FAMEs (biodiesel) in the liquid phase is limited. Spectral tools such as X-ray and NMR are known to provide evidences related to molecular structure organization. Recently, it was reported by our research group that using 1H Time Domain NMR methodology based on relaxation time and self diffusion coefficients, FAMEs clusters with different motilities can be accurately studied in the liquid phase. Head to head dimarization with quasi-smectic clusters organization, based on molecular motion analysis, was clearly demonstrated. These findings about the assembly/packing of the FAME components are directly associated with fluidity/viscosity of the biodiesel. Furthermore, these findings may provide information of micro/nano-particles that are formed in the delivery and injection system of various combustion systems (affected by thermodynamic conditions). Various relevant parameters to combustion such as: distillation/Liquid Gas phase transition, cetane number/ignition delay, shoot, oxidation/NOX emission maybe predicted. These data may open the window for further optimization of FAME/diesel mixture in terms of combustion and emission.

Keywords: supermolecular chemistry, FAMEs, liquid phase, fluidity, LF-NMR

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1097 Intersections and Consequences of the Epistemology and Methodology used in Equity-Related Chemistry Education Research

Authors: Vanessa R. Ralph, Kathryn N. Hosbein, Megan Y. Deshaye, Paulette Vincent-Ruz

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The language of the statement “persistent achievement gaps between demographic groups” communicates much about the philosophies inherent to the author. In this synthesis of two flagship journals of Chemistry Education Research: Chemistry Education Research and Practice and the Journal of Chemical Education, the use and investigation of equity was examined by the language, epistemology, and methodologies of the researchers. Findings include a considerable increase in the use and investigation of equity in these journals following the years 2012 and 2020. While an increase in consciousness of equity was apparent, epistemologies were stagnated. The majority reflects a deficit-oriented perspective wherein deficits are attributed to students as a “lack of achievement” inherent to specific “demographic groups” and minimized as “gaps” rather than systemic inequities. The lack of epistemological progress may be the result of reading and citing literature within discipline-based education research, failing to acknowledge the efforts propagated for decades by equity theory advancement in disciplines of sociology and psychology. To envision liberated educational systems across the globe, one must first contend with the biases within.

Keywords: liberating education research, philosophy of research, synthesis, review

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1096 Preparation of MgO Nanoparticles by Green Methods

Authors: Maryam Sabbaghan, Pegah Sofalgar

Abstract:

Over the past few decades, a significant amount of research activities in the chemical community has been directed towards green synthesis. This area of chemistry has received extensive attention because of environmentally benign processes as well as economically viable. In this article, the MgO nanoparticles were prepared by different methods in the present of ionic liquids. A wide range of Magnesium oxide particle sizes within the nanometer scale is obtained by these methods. The structure of these MgO particles was studied by using X-ray diffraction (XRD), Infrared spectroscopy (IR), and scanning electron microscopy (SEM). It was found that the formation of nanoparticle could involve the role of performed 'nucleus' and used template to control the growth rate of nucleuses. The crystallite size of the MgO products was in a range from 31 to 77 nm.

Keywords: MgO, ionic liquid, nanoparticles, green chemistry

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1095 Tetra Butyl Ammonium Cyanate Mediated Selective Synthesis of Sulfonyltriuret and Their Investigation towards Trypsin Protease Modulation

Authors: Amarjyoti Das Mahapatra, Umesh Kumar, Bhaskar Datta

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A pseudo peptide can mimic the biological or structural properties of natural peptides. They have become an increasing attention in medicinal chemistry because of their interesting advantages like more bioavailability and less biodegradation than compare to the physiologically active native peptides which increase their therapeutic applications. Many biologically active compounds contain urea as functional groups, and they have improved pharmacokinetic properties because of their bioavailability and metabolic stability. Recently we have reported a single-step synthesis of sulfonyl urea and sulfonyltriuret from sulfonyl chloride and sodium cyanate. But the yield of sulfonyltriuret was less around 40-60% because of the formation of other products like sulfonamide and sulfonylureas. In the present work, we mainly focused on the selective synthesis of sulfonyltriuret using tetrabutylammonium cyanate and sulfonyl chloride. More precisely, we are interested in the controlled synthesis of oligomeric urea mainly sulfonyltriuret as a new class of pseudo peptide and their application as protease modulators. The distinctive architecture of these molecules in the form of their pseudo-peptide backbone offers promise as a potential pharmacophore. The synthesized molecules have been screened on trypsin enzyme, and we observed that these molecules are the efficient modulator of trypsin enzyme.

Keywords: pseudo peptide, pharmacophore, sulfonyltriuret, trypsin

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1094 Cycas beddomei Dyer: An Endemic and Endangered Indian Medicinal Plant

Authors: Ayyavu Brama Dhayala Selvam

Abstract:

Herbal medicines are gaining importance due to holistic nature and lesser side effects. Cycas beddomei Dyer is one of the highly exploited medicinal plants in India. Due to over-exploitation of male and female cones, young leaves and starch-bearing pithy stems for edible, medicinal and socio-cultural practices by the locals, tribals and traders, the plant population has drastically declined in its natural habitats. Cycas beddomei is an endemic to India. The current IUCN status of this plant species in the wild is endangered. Perhaps, it is the only species of Cycas enlisted in Appendix I of CITES (Convention on International Trade in Endangered Species of wild fauna and flora). Endorsing the CITES decisions, the Government of India has placed C. beddomei in the “Negative List of Exports” during 1998. Though this plant has been banned legally, but illegally, it is highly exploited by different means. Therefore, conservation of this species is an urgent need of the hour. The present paper highlights unique morphological and anatomical characters of C. beddomei, along with its present status, major threats and conservation measures. Cycas beddomei can easily be identified by some of the distinguishing morphological and anatomical characters, viz., 2–4 mm wide leaflets with revolute margins; the apices of microsporophylls from the middle to apex of the pollen cones turn downwards on maturity; mucilage canal cells are seen in the midrib region of the leaflets; stomatal frequency is about 18 numbers at 250x; pollen grains are monocolpate and their diameter ranging from 22.5 to 30 µm.

Keywords: CITES, Cycas beddomei, endangered, endemic

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1093 Biosynthesis of Tumor Inhibitory Podophyllotoxin, Quercetin and Kaempferol from Callogenesis of Dysosma Pleiantha (Hance) Woodson

Authors: Palaniyandi Karuppaiya, Hsin Sheng Tsay, Fang Chen

Abstract:

Medicinal herbs do represent a huge and noteworthy reservoir for novel anticancer drugs discovery. Dysosma pleiantha (Hance) Woodson (Berberidaceae), one of the oldest traditional Chinese medicinal herb, highly prized by the mountain tribes of Taiwan and China for its medicinal properties contained pharmaceutically important antitumor compounds podophyllotoxin, quercetin and kaempferol. Among lignans, podophyllotoxin is an active antitumor compound and has now been modified to produce clinically useful drugs etoposide and teniposide. In recent years, natural populations of D. peliantha have declined considerably due to anthropogenic activities such as habitat destruction and commercial exploitation for medicinal applications. As to its overall conservation status, D. pleiantha has been ranked as threatened on the China Species Red List. In the present study, an efficient in vitro callus culture system of D. pleiantha was established on Gamborg’s medium with various combinations and concentrations of different auxins and cytokinins under dark condition. Best callus induction was recorded in 2 mg/L 2, 4 - Dichlorophenoxyacetic acid (2,4-D) along with 0.2 mg/L kinetin and the maximum callus proliferation was achieved at 1 mg/L 2,4-D. Among the explants tested, maximum callus induction (86 %) was achieved from tender leaves. Hence, in subsequent experiments, leaf callus was further investigated for suitable callus biomass and production level of anticancer compounds under the influence of different additives. A maximum fresh callus biomass (8.765 g) was recorded in callus proliferation medium contained 500 mg/L casein hydrolysate. High performance liquid chromatography results revealed that the addition of different concentrations of peptone (1, 2 and 4 g/L) in callus proliferation medium enhanced podophyllotoxin (16 fold), quercetin (12 fold) and kaempferol (5 fold) accumulation than control. Thus, the established in vitro callus culture under the influence of different additives may offer an alternative source of enhanced production of podophyllotoxin, kaempferol and quecertin without harming natural plant population.

Keywords: dysosma pleiantha, kaempferol, podophyllotoxin, quercetin

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1092 Benzoxaboralone: A Boronic Acid with High Oxidative Stability and Utility in Biological Contexts

Authors: Brian J. Graham, Ronald T. Raines

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The presence of a nearly vacant p orbital on boron endows boronic acids with unique abilities as a catalyst and ligand. An organocatalytic process has been developed for the conversion of biomass-derived sugars to 5-hydroxymethylfurfural, which is a platform chemical. Specifically, 2-carboxyphenylboronic acid (2-CPBA) has been shown to be an optimal catalyst for this process, promoting the desired transformation in the absence of metals. The attributes of 2-CPBA as a catalyst led to additional investigations of its structure and reactivity. 2-CPBA was found to exist as a cyclized benzoxaborolone adduct rather than a free carboxylic acid. This cyclization has profound consequences for the oxidative stability of the boronic acid. Stereoelectronic effects within the oxaborolone ring destabilize the oxidation transition state by reducing electron donation from the cyclic oxygen to the developing p orbital on boron. That leads to a 10,000-fold increase in oxidative stability while maintaining the normal reactivity of boronic acids toward diols (e.g., carbohydrates) and nucleophiles in proteins while also presenting numerous hydrogen-bond accepting and donating groups. Thus, benzoxaborolones are useful in catalysis, chemical biology, medicinal chemistry, and allied fields.

Keywords: bioisosteres, boronic acid, catalysis, oxidative stability, pharmacophore, stereoelectronic effects

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1091 Eucalyptus camendulensis and Its Drying Effect on Water and Essential Oil Content

Authors: Mehani Mouna, Segni Ladjel

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Medicinal and aromatic plants are promising and are characterized by the biosynthesis of odorous molecules that make up the so-called essential oils (EO), which have long been known for their antiseptic and therapeutic activity in folk medicine. The objective of this study was to evaluate the influence of drying in the shade on the water content and on the content of essential oils extracted from leaves of Eucalyptus camendulensis for better quality control of medicinal and aromatic plants. The water content of the Eucalyptus camendulensis plant material decreases during the drying process. It increased from 100 % to 0.006 % for the drying in the shade after ten days. The moisture content is practically constant at the end of the drying period. The drying in the shade increases the concentration of essential oils of Eucalyptus camendulensis. When the leaves of Eucalyptus camendulensis plant are in the shade, the maximum of the essential oil content was obtained on the eighth days; the recorded value was 1.43% ± 0.01%. Beyond these periods, the content continuously drops in before stabilizing. The optimum drying time is between 6 and 9 days.

Keywords: Eucalyptus camendulensis, drying, essential oils, water, content

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1090 Identifying Controlling Factors for the Evolution of Shallow Groundwater Chemistry of Ellala Catchment, Northern Ethiopia

Authors: Grmay Kassa Brhane, Hailemariam Siyum Mekonen

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This study was designed to identify the hydrogeochemical and anthropogenic processes controlling the evaluation of groundwater chemistry in the Ellala catchment which covers about 296.5 km2 areal extent. The chemical analysis revealed that the major ions in the groundwater are Ca2+, Mg2+, Na+, and K+ (cations) and HCO3-, PO43-, Cl-, NO3-, and SO42-(anions). Most of the groundwater samples (68.42%) revealed that the groundwater in the catchment is non-alkaline. In addition to the contribution of aquifer material, the solid materials and liquid wastes discharged from different sources can be the main sources of pH and EC in the groundwater. It is observed that the EC of the groundwater is fairly correlated with the DTS. This indicates that high mineralized water is more conductor than water with low concentration. The degree of salinity of the groundwater increases along the groundwater flow path from East to West; then, areas surrounding Mekelle City are highly saline due to the liquid and solid wastes discharged from the city and the industries. The groundwater facies in the catchment are predominated with calcium, magnesium, and bicarbonate which are labeled as Ca-Mg-HCO3 and Mg-Ca-HCO3. The main geochemical process controlling the evolution of the groundwater chemistry in the catchment is rock-water interaction, particularly carbonate dissolution. Due to the clay layer in the aquifer, the reverse is ion exchange. Non-significant silicate weathering and halite dissolution also contribute to the evolution of groundwater chemistry in the catchment. The groundwater in the catchment is dominated by the meteoritic origin although it needs further groundwater chemistry study with isotope dating analysis. The groundwater is under-saturated with calcite, dolomite, and aragonite minerals; hence, the more these minerals encounter the groundwater, the more the minerals dissolve. The main source of calcium and magnesium in groundwater is the dissolution of carbonate minerals (calcite and dolomite) since carbonate rocks are the dominant aquifer materials in the catchment. In addition to this, the weathering of dolerite rock is a possible source of magnesium ions. The relatively higher concentration of sodium over chloride indicates that the source of sodium-ion is reverse ion exchange and/or weathering of sodium-bearing materials, such as shale and dolerite rather than halite dissolution. High concentration of phosphate, nitrate, and chloride in the groundwater is the main anthropogenic source that needs treatment, quality control, and management in the catchment. From the Base Exchange Index Analysis, it is possible to understand that, in the catchment, the groundwater is dominated by the meteoritic origin, although it needs further groundwater chemistry study with isotope dating analysis.

Keywords: Ellala catchment, factor, chemistry, geochemical, groundwater

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1089 Investigation the Impact of Flipped Learning on Developing Meta-Cognitive Ability in Chemistry Courses of Science Education Students

Authors: R. Herscu-Kluska

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The rise of the flipped or inverted classroom meet the conceptual needs of our time. The evidence of increased student satisfaction and course grades improvement promoted the flipped learning approach. Due to the successful outcomes of the inverted classroom, the flipped learning became a pedagogy and educational rising strategy among all education sciences. The aim of this study is to analyze the effect of flipped classroom on higher order learning in chemistry courses since it has been suggested that in higher education courses, class time should focus on knowledge application. The results of this study indicate improving meta-cognitive thinking and learning skills. The students showed better ability to cope with higher order learning assignments during the actual class time, using inverted classroom strategy. These results suggest that flipped learning can be used as an effective pedagogy and educational strategy for developing higher order thinking skills, proved to contribute to building lifelong learning.

Keywords: chemistry education, flipped classroom, flipped learning, inverted classroom, science education

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1088 Synthesis of Star Compounds Bearing a Porphyrin Core and Cholic Acid Units by Using Click Chemistry: Study of the Optical Properties and Aggregation

Authors: Edgar Aguilar-Ortíz, Nicolas Lévaray, Mireille Vonlanthen, Eric G. Morales-Espinoza, Ernesto Rivera, Xiao Xia Zhu

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Four new star compounds bearing a porphyrin core and cholic acid units, (TPPh(Zn) tetra-CA, TPPh(2H) tetra-CA, TPPh(Zn) octa-CA and TPPh(2H) octa-CA), have been synthesized using the Click Chemistry approach, which consist on azide-alkyne couplings. These novel functionalized porphyrins were characterized by 1H and 13C NMR spectroscopy and their structure was confirmed by MALDI-TOF. The optical properties of these compounds were studied by absorption and fluorescence spectroscopy. On the other hand, order to evaluate the amphiphilic properties of the cholic acid units combined with the optical response of the porphyrin core, we performed absorption and fluorescence studies in function of the polarity of the environment. It was found that as soon as we increase the polarity of the solvent, the Zn-metallated porphyrins, (TPPh(Zn) tetra-CA and TPPh(Zn) octa-CA), are able to form J aggregates, whereas the free-base porphyrins, TPPh(2H) tetra-CA and TPPh(2H) octa-CA, behaved differently.

Keywords: aggregates, amphiphilic, cholic acid, click-chemistry, porphyrin

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1087 Construction of QSAR Models to Predict Potency on a Series of substituted Imidazole Derivatives as Anti-fungal Agents

Authors: Sara El Mansouria Beghdadi

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Quantitative structure–activity relationship (QSAR) modelling is one of the main computer tools used in medicinal chemistry. Over the past two decades, the incidence of fungal infections has increased due to the development of resistance. In this study, the QSAR was performed on a series of esters of 2-carboxamido-3-(1H-imidazole-1-yl) propanoic acid derivatives. These compounds have showed moderate and very good antifungal activity. The multiple linear regression (MLR) was used to generate the linear 2d-QSAR models. The dataset consists of 115 compounds with their antifungal activity (log MIC) against «Candida albicans» (ATCC SC5314). Descriptors were calculated, and different models were generated using Chemoffice, Avogadro, GaussView software. The selected model was validated. The study suggests that the increase in lipophilicity and the reduction in the electronic character of the substituent in R1, as well as the reduction in the steric hindrance of the substituent in R2 and its aromatic character, supporting the potentiation of the antifungal effect. The results of QSAR could help scientists to propose new compounds with higher antifungal activities intended for immunocompromised patients susceptible to multi-resistant nosocomial infections.

Keywords: quantitative structure–activity relationship, imidazole, antifungal, candida albicans (ATCC SC5314)

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1086 The Effect of Chitosan and Mycorrhization on Some Growth-Physiological Indices of Salvia leriifolia Benth.

Authors: Marzieh Fotovvat, Farzaneh Najafi, Ramazan Ali Khavari-Nejad, Daryush Talei, Farhad Rejali

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Salvia leriifolia Benth. is one of the valuable and perennial medicinal plants of the Lamiaceae family, geographically growing in the south and tropical regions of Khorassan and Semnan provinces in Iran. In recent years, several medicinal properties such as antimicrobial, antifungal, anti-diabetic, analgesic, and anti-inflammatory effects have been reported from this plant. The use of elicitors such as chitosan and Arbuscular mycorrhizal fungi (AMF) symbiosis are the main methods for increasing the production of secondary metabolites, growth, and physiological factors in plants. The main aim of this study was to investigate the effects of foliar spraying applications by chitosan and/or the contribution of AMF (Glomus interaradices) on some growth factors and chlorophyll content of S. leriifolia under glasshouse conditions. The sterilized seeds were germinated by placing them into a cocopeat. After one month, seedlings that were in the 2-4 leaf stage were transferred to plastic pots (garden soil and pumice at 2:1) with or without mycorrhizal fungi. Chitosan (0, 50, 100, 200, and 400 mg L-1) was sprayed four times in the fourth month of the vegetative period. The results showed that fresh leaf weight, fresh root weight, root height, and chlorophyll content could change in the plant treated with chitosan and AMF symbiosis. So that the highest chlorophyll content and fresh weight of roots and leaves were observed in the interaction of chitosan and G. interaradices. In general, by optimizing the chitosan concentration and the use of appropriate AMF symbiosis, it is possible to improve the growth and quality of the medicinal plant S. leriifolia.

Keywords: chitosan, chlorophyll, growth factors, mycorrhiza

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1085 Identification of the Alkaloids of the Belladone (Atropa belladonna L.) and Evaluation of Their Inhibitory Effects Against Some Microbial Strains

Authors: Ait Slimane-Ait Kaki Sabrina, Foudi Lamia

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The present work consists of the study of the bio-ecology and the therapeutic effects of the belladone (Atropa belladonna L.). It is a medicinal plant of the Solanacées family, herbaceous, robust 0.5 up to 1.50 m high. The phytochemical analysis of leaves revealed alkaloids, tannins, catechin, coumarins, mucilages, saponins, starch, and reducing compounds. The experimental study concerns the extraction and characterization of belladonna alkaloids. Analysis of the purified extract by staining tests confirmed the presence of tropane alkaloids. The dosage chromatography revealed the presence of components that have been identified atropine, scopolamine and hyoscyamine. Evaluation of antimicrobial and antifungal alkaloids from the methanol extract and aqueous extract of belladonna on pathogenic germs showed a positive bactericidal against strains of Escherichia coli and Staphylococcus aureus. Our preliminary results allow us an overall assessment of the medicinal value of Atropa belladonna.

Keywords: belladone, alkaloid, antibacterial activity, antifungal activity

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1084 Nonclassical Antifolates: Synthesis, Biological Evaluation and Molecular Modeling Study of Some New Quinazolin-4-One Analogues as Dihydrofolate Reductase Inhibitors

Authors: Yomna Ibrahim El-Gazzar, Hussien Ibrahim El-Subbagh, Hanan Hanaa Georgey, Ghada S. Hassan Hassan

Abstract:

Dihydrofolate reductase (DHFR) is an enzyme that has pivotal importance in biochemistry and medicinal chemistry. It catalyzes the reduction of dihydrofolate to tetrahydrofolate and intimately couples with thymidylate synthase. Thymidylate synthase is a crucial enzyme that catalyzes the reductive methylation of (dUMP) to (dTMP) utilizing N5, N10-methylenetetrahydrofolate as a cofactor. A new series of 2-substituted thio-quinazolin-4-one analogs was designed that possessed electron withdrawing or donating functional groups (Cl or OCH3) at position 6- or 7-, 4-methoxyphenyl function at position 3-.The thiol function is used to connect to either 1,2,4-triazole, or 1,3,4-thiadiazole via a methylene bridge. Most of the functional groups designed to be accommodated on the quinazoline ring such as thioether, alkyl to increase lipid solubility of polar compounds, a character very much needed in the nonclassical DHFR inhibitors. The target compounds were verified with spectral data and elemental analysis. DHFR inhibitions, as well as antitumor activity, were applied on three cell lines (MCF-7, CACO-2, HEPG-2).

Keywords: nonclassical antifolates, DHFR Inhibitors, antitumor activity, quinazoline ring

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1083 Survey of Some Important Nepalese and Russian Anti-Diabetic Herbs

Authors: Ram Prasad Baral, Vinogradov Dmitriy Valerievich, Rameshwar Adhikari

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Diabetes has posed a great threat to the human health worldwide, both in developed and developing countries. The disease has basically rooted from the dramatically changed way of living of the present day human civilization as our living has deviated from what the nature has adapted us for. In this context, due to availability of wide range of climatic condition and hence the wide spectrum of biodiversity, Nepal is blessed with a valuable reservoir of medicinal herbs. These assets have been utilized and developed practices in traditional medicines and Ayurvedic way of treatment over several thousand years in the region. It has been established since ancient times that each and every plant has a specific medicinal value. There are many plants’ products which have been utilized in Ayurvedic medicine for the effective treatment of diabetes. The medicaments are less expensive and pose practically no side effects. In this work, we report a general survey of anti-diabetic properties of some medicinal herbs with pronounced effects and their applications. The plants covered in this study originate from far western region of Nepal and include Ficus racemosa, Momordica charantia, Azadirachta indica, Helieteres isora, Saraca asoca, Ichnocarpus frutescens, Tinospora sinensis, Commiphora mukul, Coccinia grandis, and Hippophae salicifolia.

Keywords: Ficus racemosa, Momordica charantia, Azadirachta indica, Helieteres isora, Saraca asoca, Ichnocarpus frutescens, Tinospora sinensis, Commiphora mukul, Coccinia grandis, Hippophae salicifolia

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1082 Effect of UV-B Light Treatment on Nutraceutical Potential of an Indigenous Mushroom Calocybe Indica

Authors: Himanshi Rathore, Shalinee Prasad, Satyawati Sharma, Ajay Singh Yadav

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Medicinal mushrooms are acceptable all over the world not only because they have a unique flavour and texture but also due to the presence of great nutritional, nutraceutical and functional properties. High content of physiologically active substances like ergosterol, vitamin D, phenolic compounds, triterpenoids and steroids make these medicinal mushrooms a key source of nutraceuticals. Calocybe indica is a popular medicinal mushroom of India which is known to possess high amount of secondary metabolites including ergosterol (vitamin D2). The ergosterol gets converted to vitamin D in the presence of UV rays by a photochemical reaction. In lieu of the above facts the present study was undertaken to investigate the effect of UV-B light treatment on the vitamin D2 concentration, phenolic content and non volatile compounds in Calocybe indica. For this study, UV-B light source of intensity 5.3w/m2 was used to expose mushrooms for the time period of 0min, 30min, 60min and 90 min. It was found that the vitamin D2 concentration increased with the time duration i.e. 85±0.15 (0 min), 182±1.6 (30 min), 187±0.4 (60 min) and 182 ±0.8 (90 min) μg/g (dry weight). Highest concentration of vitamin D2 was found at 60 min duration. No discoloration in sliced mushrooms was observed during the exposure time. The results revealed that the exposure of mushrooms for a minimum of 30 min duration under UVB source can be a novel, convenient and cheapest way to increase the vitamin D content in mushrooms. This can be one of richest source to fulfil the recommended dietary allowances of vitamin D in our daily diets. The paper provides information on the enhancement of vitamin D content by UV lights and its effects on the non volatile (soluble sugars, free amino acids, 5′-nucleotides and phenolics) compounds will also be presented.

Keywords: Calocybe indica, ergosterol, nutraceutical, phenolics

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1081 Ethnobotany and Antimicrobial Effects of Medicinal Plants Used for the Treatment of Sexually Transmitted Infections in Lesotho

Authors: Sandy Van Vuuren, Lerato Kose, Annah Moteetee

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Lesotho, a country surrounded by South Africa has one of the highest rates of sexually transmitted infections (STI’s) in the world. In fact, the country ranks third highest with respect to infections related to the human immunodeficiency virus (HIV). Despite the high prevalence of STI’s, treatment has been a challenge due to limited accessibility to health facilities. An estimated 77% of the population lives in rural areas and more than 60% of the country is mountainous. Therefore, many villages remain accessible only by foot or horse-back. Thus, the Basotho (indigenous people from Lesotho) have a rich cultural heritage of plant use. The aim of this study was to determine what plant species are used for the treatment of STI’s and which of these have in vitro efficacy against pathogens such as Candida albicans, Gardnerella vaginalis, Oligella ureolytica, and Neisseria gonorrhoeae. A total of 34 medicinal plants were reported by traditional practitioners for the treatment of STI’s. Sixty extracts, both aqueous and organic (mixture of methanol and dichloromethane), from 24 of the recorded plant species were assessed for antimicrobial activity using the minimum inhibition concentration (MIC) micro-titre plate dilution assay. Neisseria gonorrhoeae (ATCC 19424) was found to be the most susceptible among the test pathogens, with the majority of the extracts (21) displaying noteworthy activity (MIC values ≤ 1 mg/ml). Helichrysum caespititium was found to be the most antimicrobially active species (MIC value of 0.01 mg/ml). The results of this study support, to some extent, the traditional medicinal uses of the evaluated plants for the treatment of STI’s, particularly infections related to gonorrhoea.

Keywords: Africa, Candida albicans, Gardnerella vaginalis, Neisseria gonorrhoeae, Oligella urealytica

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1080 Studies on Propagation of Celastrus paniculatus Willd: An Endangered Medicinal Plant

Authors: G. Raviraja Shetty, K. G. Poojitha

Abstract:

An experiment was conducted to study the effect of different growth regulators on seed germination and vegetative propagation by cuttings of an endangered medicinal plant species, Celastrus paniculatus Willd. at College of Horticulture, Mudigere during June- Sept 2014. Various growth parameters were recorded for seed germination and significantly higher results for Rate of germination (0.78), Plant vigour (2082.74), Plant height (22.10cm), number of leaves (7.83) fresh weight (136.58mg) and dry weight of plant (59.16mg) noticed in seeds treated with GA3 400 ppm when compared to control. In vegetative propagation the cuttings treated with IBA 2000 ppm recorded significantly highest sprouting percentage (98.00) when compared to control (71.00). The results of present investigation will be helpful for large scale multiplication of the species. It will also help for cultivation and conservation of this endangered species.

Keywords: Celastrus paniculatus Willd, seeds, germination, cuttings

Procedia PDF Downloads 386
1079 Screening of Potential Cytotoxic Activities of Some Medicinal Plants of Saudi Arabia

Authors: Syed Farooq Adil, Merajuddinkhan, Mujeeb Khan, Hamad Z. Alkhathlan

Abstract:

Phytochemicals from plant extracts belong to an important source of natural products which have demonstrated excellent cytotoxic activities. However, plants of different origins exhibit diverse chemical compositions and bioactivities. Therefore, the discovery of plants based new anticancer agents from different parts of the world is always challenging. In this study, methanolic extracts of different parts of 11 plants from Saudi Arabia have been tested in vitro for their anticancer potential on human liver cancer cell line (HepG2). Particularly, for this study, plants from Asteraceae, Resedaceae, and Polygonaceae families were chosen on the basis of locally available ethnobotanical data and their medicinal properties. Among 12 tested extract samples, three samples obtained from Artemisia monosperma stem, Ochradenus baccatus aerial parts, and Pulicaria glutinosa stem have demonstrated interesting cytotoxic activities with a cell viability of 29.3%, 28.4% and 24.2%, respectively. Whereas, four plant extracts including Calendula arvensis aerial parts, Scorzonera musilii whole plant, A. monosperma leaves show moderate anticancer properties bearing a cell viability ranging from 11.9 to 16.7%. The remaining extracts have shown poor cytotoxic activities. Subsequently, GC-MS analysis of methanolic extracts of the four most active plants extracts such as C. comosum, O. baccatus, P. glutinosa and A. monosperma detected the presence of 41 phytomolecules. Among which 3-(4-hydroxyphenyl) propionitrile (1), 8,11-octadecadiynoic acid methyl ester (2), 6,7-dimethoxycoumarin (3), and 1-(2-hydroxyphenyl) ethenone (4) were found to be the lead compounds of C. comosum, O. baccatus P. glutinosa and A. monosperma, respectively.

Keywords: medicinal plants, asteraceae, polygonaceae, hepg2

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1078 Flavonoid Content and Antioxidant Potential of White and Brown Sesame Seed Oils

Authors: Fatima Bello, Ibrahim Sani

Abstract:

Medicinal plants are the most important sources of life saving drugs for the majority of world’s population. People of all continents have used hundreds to thousands of indigenous plants in curing and management of many diseases. Sesame (Sesamum indicum L.) is one of the most widely cultivated species for its nutritious and medicinal seeds and oil. This research was carried out to determine the flavonoid content and antioxidant potential of two varieties of sesame seeds oil. Oil extraction was done using Soxhlet apparatus. The percentage oil yield for white and brown seeds were 47.85% and 20.72%, respectively. Flavonoid was present in both seeds with concentration of 480 mg/g and 360 mg/g in white and brown sesame seeds, respectively. The antioxidant potential was determined at different oil volume; 1.00, 0.75, 0.50 and 0.25ml. The results for the white and brown sesame seed oils were 96.8 and 70.7, 91.0 and 65.2, 83.1 and 55.4, 77.9 and 50.2, respectively. The white seed oil has higher oil yield than the brown seed oil. Likewise, the white seed oil has more flavonoid content than the brown seed oil and also better reducing power than the brown seed oil.

Keywords: antioxidant potential, brown sesame seeds, flavonoid content, sesame seed oil, Sesamum indicum L., white sesame seeds

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1077 Anti-Inflammatory Activity of Lavandula antineae Maire from Algeria

Authors: Soumeya Krimat, Tahar Dob, Aicha Kesouri, Ahmed Nouasri, Hafidha Metidji

Abstract:

Lavandula antineae Maire is an endemic medicinal plant of Algeria which is traditionally used for the treatment of chills, bruises, oedema and rheumatism. The objective of this study is to evaluate the anti-inflammatory of hydromethanolic aerial parts extract of Lavandula antineae for the first time using carrageenan-paw edema and croton oil-ear odema models. The plant extract, at the dose of 200 mg/kg, showed a significant anti-inflammatory activity (P˂0.05) in the carrageenan induced edema test in mice, showing 80.74% reduction in the paw thikness comparable to that produced by the standard drug aspirin 83.44% at 4h. When it was applied topically at a dosage of 1 and 2 mg per ear, the percent edema reduction in treated mice was 29.45% and 74.76%, respectively. These results demonstrate that Lavandula antineae Maire extract possess remarkable anti-inflammatory activity, supporting the folkloric usage of the plant to treat various inflammatory and pain diseases.

Keywords: lavandula antineae maire, medicinal plant, anti-inflammatory activity, carrageenan-paw edema, croton oil-ear edema

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1076 Traditional Herbal Medicine Used to Treat Infertility in Women by Traditional Practitioner of Malwa Region of Madhya Pradesh, India

Authors: Shweta Shriwas, Sumeet Dwivedi

Abstract:

Knowledge of use of traditional medicine is as old as human civilization in almost every system of medicine. Traditional practitioner viz., vaidhayas, ojha, hakim have their own herbal therapy in the treatment of infertility among women’s. Infertility is very common in developed and developing countries due to busy life style of women’s. The present study was initiated with an aim to identify medicinal plants resources from traditional practitioners of Malwa region of Madhya Pradesh to treat infertility. An ethnomedicinal study of Malwa region viz., Indore, Dewas, Ratlam, Ujjain, Dhar, Mandsour and Neemuch of Madhya Pradesh, India comprising fifty-seven study site was conducted during Jan-217 to June-2017. During the course of present investigation, the traditional use of medicinal plants for infertility in women was revealed by traditional practitioner. The botanical name, family, local name, part used, habit along with mode of their administration and dose duration were enumerated.

Keywords: herbal medicine, infertility, traditional, Malwa, Madhya Pradesh

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1075 A Systematic Review of the Antimicrobial Effects of Different Plant Extracts (Quercus infectoria) as Possible Candidates in the Treatment of Infectious Diseases

Authors: Sajjad Jafari

Abstract:

Background and Aim: The use of herbal medicines has a long history. Today, due to the resistance of microorganisms to antibiotics and antimicrobial substances, herbal medicines have attracted attention due to their significant antimicrobial effects and low toxicity. This study aims to systematically review the antimicrobial effects of different plant extracts (Quercus infectoria) as possible candidates for treating infectious diseases. Material and Methods: The present study is a review study by searching reputable scientific databases such as PubMed, Google Scholar, Scopus, and Web of Science from 2000 to 2023 using the keywords Antimicrobial, Quercus infectoria, Medicinal herbal, Infectious diseases the latest information obtained. Results: In this study, 45 articles were found and reviewed. Quercus infectoria is a small tree native to Greece, Asia Minor, and Iran. Quercus is a plant genus in the family of Fagaceae. This species is generally known under the name ‘‘baloot” in Iran and is commonly used as a medicinal plant. The extracts used included water, hydro-alcoholic, ethanol, methanol. This plant had high inhibition activity and a lethal effect on gram-positive and gram-negative bacteria of ATCC strains, hospital, and resistant strains. Therefore, in addition to antibacterial effects, antiparasitic and antifungal effects. The seed of the plant was the most used and the most effective antimicrobial extract among the ethanol and methanol extracts. Conclusion: The findings of this study suggest that Quercus infectoria has significant antimicrobial effects against a wide range of microorganisms. This makes it a potential candidate for the development of new antimicrobial drugs. Further research is needed to confirm the efficacy and safety of Quercus infectoria in clinical trials.

Keywords: antimicrobial, Quercus infectoria, medicinal herbal, infectious diseases

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1074 Phytochemical Analysis and Antioxidant Activity of Colocasia esculenta (L.) Leaves

Authors: Amit Keshav, Alok Sharma, Bidyut Mazumdar

Abstract:

Colocasia esculenta leaves and roots are widely used in Asian countries, such as, India, Srilanka and Pakistan, as food and feed material. The root is high in carbohydrates and rich in zinc. The leaves and stalks are often traditionally preserved to be eaten in dry season. Leaf juice is stimulant, expectorant, astringent, appetizer, and otalgia. Looking at the medicinal uses of the plant leaves; phytochemicals were extracted from the plant leaves and were characterized using Fourier-transform infrared spectroscopy (FTIR) to find the functional groups. Phytochemical analysis of Colocasia esculenta (L.) leaf was studied using three solvents (methanol, chloroform, and ethanol) with soxhlet apparatus. Powder of the leaves was employed to obtain the extracts, which was qualitatively and quantitatively analyzed for phytochemical content using standard methods. Phytochemical constituents were abundant in the leave extract. Leaf was found to have various phytochemicals such as alkaloids, glycosides, flavonoids, terpenoids, saponins, oxalates and phenols etc., which could have lot of medicinal benefits such as reducing headache, treatment of congestive heart failure, prevent oxidative cell damage etc. These phytochemicals were identified using UV spectrophotometer and results were presented. In order to find the antioxidant activity of the extract, DPPH (2,2-diphenyl-1-picrylhydrazyl) method was employed using ascorbic acid as standard. DPPH scavenging activity of ascorbic acid was found to be 84%, whereas for ethanol it was observed to be 78.92%, for methanol: 76.46% and for chloroform: 72.46%. Looking at the high antioxidant activity, Colocasia esculenta may be recommended for medicinal applications. The characterizations of functional groups were analyzed using FTIR spectroscopy.

Keywords: antioxidant activity, Colocasia esculenta, leaves, characterization, FTIR

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1073 On Supporting a Meta-Design Approach in Socio-Technical Ontology Engineering

Authors: Mesnan Silalahi, Dana Indra Sensuse, Indra Budi

Abstract:

Many research have revealed the fact of the complexity of ontology building process that there is a need to have a new approach which addresses the socio-technical aspects in the collaboration to reach a consensus. Meta-design approach is considered applicable as a method in the methodological model in a socio-technical ontology engineering. Principles in the meta-design framework is applied in the construction phases on the ontology. A portal is developed to support the meta-design principles requirements. To validate the methodological model semantic web applications were developed and integrated in the portal and also used as a way to show the usefulness of the ontology. The knowledge based system will be filled with data of Indonesian medicinal plants. By showing the usefulness of the developed ontology in a web semantic application, we motivate all stakeholders to participate in the development of knowledge based system of medicinal plants in Indonesia.

Keywords: socio-technical, metadesign, ontology engineering methodology, semantic web application

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1072 Income Generation and Employment Opportunity of the Entrepreneurs and Farmers Through Production, Processing, and Marketing of Medicinal Plants in Bangladesh

Authors: Md. Nuru Miah, A. F. M. Akhter Uddin

Abstract:

Medicinal plants are grown naturally in a tropical environment in Bangladesh and used as drug and therapeutic agents in the health care system. According to Bangladesh Agricultural Research Institute (BARI), there are 722 species of medicinal plants in the country. Of them, 255 plants are utilized by the manufacturers of Ayurvedic and Unani medicines. Medicinal plants like Aloevera, Ashwagonda, shotomul,Tulsi, Vuikumra, Misridana are extensively cultivated in some selected areas as well; where Aloevera scored the highest position in production. In the early 1980, Ayurvedic and Unani companies procured 80 percent of medicinal plants from natural forests, and the rest 20 percent was imported. Now the scenario has changed; 80 percent is imported, and the rest 20 percent is collected from local products(Source: Astudy on sectorbased need assessment of Business promotion council-Herbal products and medicinal plants, page-4). Uttara Development Program Society, a leading Non- Government development organization in Bangladesh, has been implementing a value chain development project under promoting Agricultural commercialization and Enterprises of Pally Karma Sahayak Foundation (PKSF) funded by the International Fund for Agricultural Development (IFAD) in Natore Sadar Upazila from April 2017 to sustainably develop the technological interventions for products and market development. The ultimate goal of the project is to increase income, generate employment and develop this sector as a sustainable business enterprise. Altogether 10,000 farmers (Nursery owners, growers, input supplier, processors, whole sellers, and retailers) are engaged in different activities of the project. The entrepreneurs engaged in medicinal plant cultivation did not know and follow environmental and good agricultural practices. They used to adopt traditional methodology in production and processing. Locally the farmers didn’t have any positive initiative to expand their business as well as developvalue added products. A lot of diversified products could be possible to develop and marketed with the introduction of post-harvest processing technology and market linkage with the local and global buyer. Training is imparted to the nursery owners and herbal growers on production technologies, sowing method, use of organic fertilizers/compost/pesticides, harvesting procedures, and storage facilities. Different types of herbal tea like Rosella, Moringa, Tulshi, and Basak are being produced and packed locally with a good scope of its marketing in different cities of the country. The project has been able to achieve a significant impact in the development of production technologies, but still, there is room for further improvement in processing, packaging, and marketing level. The core intervention of the current project to develop some entrepreneurs for branding, packaging, promotion, and marketing while considering environment friendly practices. The present strategies will strengthen the knowledge and skills of the entrepreneurs for the production and marketing of their products, maintaining worldwide accepted compliance system for easy access to the global market.

Keywords: aloe vera, herbs and shrubs, market, interventions

Procedia PDF Downloads 59